Search Result
Results for "
Elys Inhibitors
" in MedChemExpress (MCE) Product Catalog:
1548
Inhibitors & Agonists
16
Biochemical Assay Reagents
51
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-112371
-
|
CDK
|
Cancer
|
(S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM) .
|
-
-
- HY-15282
-
-
-
- HY-163901
-
|
HPV
Apoptosis
|
Infection
|
E6-272 is an inhibitor for human papillomavirus 16 (HPV 16). E6-272 inhibits the proliferation of HPV-positive cells SiHa and CaSki with GI50 of 32 nM and 62 nM. E6-272 induces apoptosis in cell SiHa and CaSki .
|
-
-
- HY-116683
-
MAL2-11B
|
HSP
DNA/RNA Synthesis
|
Infection
Cancer
|
116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70 .
|
-
-
- HY-124202
-
|
Cathepsin
|
Others
|
SQ 32602 is an inhibitor of cathepsin E, with the IC50 of 88 nM .
|
-
-
- HY-164956
-
|
Cathepsin
Beta-secretase
|
Cancer
|
TB-9, a Tasiamide B (HY-N15154) derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively .
|
-
-
- HY-N9814
-
|
NO Synthase
|
Inflammation/Immunology
|
Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity . Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity .
|
-
-
- HY-156523
-
|
MAP4K
|
Cancer
|
TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM,respectively,in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition .
|
-
-
- HY-135605
-
FCE26644
|
FGFR
|
Cancer
|
PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility .
|
-
-
- HY-148918
-
|
β-catenin
Wnt
|
Cancer
|
E722-2648 is a potent β-catenin/BCL9 complex inhibitor. E722-2648 specifically inhibits β-catenin/BCL9 complex formation and Wnt activity. E722-2648 disrupts cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation. E722-2648 has antitumor activity .
|
-
-
- HY-N3149
-
|
STAT
Apoptosis
Reactive Oxygen Species
|
Cancer
|
(E)-2-Hydroxycinnamaldehyde is an aldehyde that can be separated from the stem bark of cinnamon. (E)-2-Hydroxycinnamaldehyde inhibits cell proliferation and induces apoptosis by inhibiting signal transduction of STAT3 and reactive oxygen species production. (E)-2-Hydroxycinnamaldehyde has antitumor activity .
|
-
-
- HY-168889
-
|
RSV
SARS-CoV
|
Infection
|
HRSV/hCoV-229E-IN-1 (compound 8X) is a potent HRSV and hCoV-229E inhibitor with an IC50 value of 2.1 µM for hCoV-229E. HRSV/hCoV-229E-IN-1 inhibits cell viability .
|
-
-
- HY-106749
-
-
-
- HY-P3235
-
|
Factor VIIa
|
Others
|
E-76 is a peptide with anticoagulant activity. E-76 inhibits blood coagulation by specifically binding to exogenous coagulation factor VIIa (FVIIa). E-76 can be used to study blood coagulation-related diseases .
|
-
-
- HY-106619
-
-
-
- HY-100962
-
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor .
|
-
-
- HY-19530
-
|
Kinesin
|
Cancer
|
PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC50 of 16.1 nM; PF-2771 is used as an anticancer agent.
|
-
-
- HY-120331
-
|
HIV
HIV Protease
|
Infection
|
U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with Ki of 20 nM, 560 nM and 2100 nM, respectively .
|
-
-
- HY-15582G
-
-
-
- HY-165378
-
(E)-Dosulepin hydrochloride; (E)-Dothep hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
(E)-Dothiepin ((E)-Dosulepin;(E)-Dothep) hydrochloride is an antidepressant agent with sedative/anxiolytic activity. (E)-Dothiepin hydrochloride is an inhibitor preferring of noradrenaline uptake than serotonin uptake. (E)-Dothiepin hydrochloride facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. (E)-Dothiepin hydrochloride is also an antagonist of histamine H1-receptor without cardiotoxicity. (E)-Dothiepin hydrochloride exhibits significant analgesic activity in psychogenic facial pain,idiopathic fibromyalgia syndrome or rheumatoid arthritis .
|
-
-
- HY-161898
-
|
Kinesin
|
Cancer
|
CENP-E-IN-3 (compound 4) is a potent CENP-E inhibitor. CENP-E-IN-3 has the potential for the research of cancer .
|
-
-
- HY-139134
-
-
-
- HY-110319
-
(E/Z)-FK866 hydrochloride; (E/Z)-APO866 hydrochloride
|
NAMPT
Apoptosis
|
Inflammation/Immunology
Cancer
|
(E/Z)-Daporinad hydrochloride ((E/Z)-FK866 hydrochloride) is a potent inhibitor of nicotinamide phosphoribose transferase (NAMPT). (E/Z)-Daporinad hydrochloride induces apoptosis by specifically inhibiting NAMPT to gradually deplete intracellular NAD +. (E/Z)-Daporinad hydrochloride can be used in the study of cancer biology and inflammatory diseases .
|
-
-
- HY-119407
-
|
Kinesin
|
Cancer
|
Terpendole E is a mitotic kinesin Eg5 inhibitor. Terpendole E inhibits both motor and microtubule-stimulated ATPase activities of human Eg5. Terpendole E induces formation of a monoastral spindle in M phase .
|
-
-
- HY-14178A
-
|
ERK
|
Others
|
(R)-VX-11e (Compound 1) is an ERK2 inhibitor .
|
-
-
- HY-14178
-
|
ERK
|
Cancer
|
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
|
-
-
- HY-17536A
-
(E)-KPT-330
|
CRM1
|
Cancer
|
(E)-Selinexor ((E)-KPT-330) is the E-isomer of Selinexor (HY-17536). Selinexor is the selective, orally active CRM1 inhibitor .
|
-
-
- HY-153178
-
|
E1/E2/E3 Enzyme
|
Others
|
HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor. HECT E3-IN-1 (compound 3) disrupts Ub binding to the noncovalent Ub-binding site of Nedd4-1 .
|
-
-
- HY-117762
-
PNU-83836E
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
U-83836E (PNU-83836E) is a compound with anti-inflammatory and antioxidant activities that reduces lung inflammation inhibiting oxidative stress and ROS production. U-83836E has shown potential for treating asthma and lung inflammation in animal models .
|
-
-
- HY-14971
-
(E)-AKTIV
|
Akt
|
Cancer
|
(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic .
|
-
-
- HY-137488
-
|
PROTACs
Raf
|
Cancer
|
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
|
-
-
- HY-13296
-
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
|
-
-
- HY-122746
-
|
Histone Methyltransferase
|
Cancer
|
E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase .
|
-
-
- HY-107459
-
(E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42
|
EGFR
STAT
JAK
|
Cancer
|
(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
-
- HY-15162G
-
MMAE; SGD-1010; Vedotin
|
Microtubule/Tubulin
Apoptosis
ADC Cytotoxin
|
Cancer
|
Monomethyl auristatin E (MMAE) (GMP) is Monomethyl auristatin E (HY-15162) produced by using GMP guidelines. Monomethyl auristatin E is a tubulin polymerization inhibitor .
|
-
-
- HY-161395
-
|
Bacterial
|
Infection
|
IDD-8E is an effective anti-pseudomonal agent (MIC =4.4 µM ) with no cytotoxicity. IDD-8E shows significant pseudomonal killing and disruption of pseudomonal biofilm. IDD-8E binds to the ATP-binding pocket of WaaP and also inhibits other ESKAPE pathogens.
|
-
-
- HY-P10428
-
|
HPV
|
Infection
|
E6AP-mimicking peptide (compound 13) is a high-affinity, selective, irreversible and potent peptide-based covalent HPV16 E6 inhibitor targeting the 16E6 oncoprotein using a cysteine-reactive acrylamide warhead. E6AP-mimicking peptide has a Ki of 17 nM. E6AP-mimicking peptide targets all residues appearing in the binding pocket of E6 to disrupt the binding interface of 16E6 and E6AP. E6AP-mimicking peptide selectively binds and crosslinks to MBP-16E6 in PBS or a protein mixture .
|
-
-
- HY-N14981
-
-
-
- HY-P5720
-
|
Bacterial
|
Infection
|
Peptide 5e is an antimicrobial peptide. Peptide 5e inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 5, 25 μg/mL respectively .
|
-
-
- HY-119173
-
-
-
- HY-155676
-
-
-
- HY-N12875
-
|
Tyrosinase
|
Others
|
Ailancoumarin E (Compound 5) is a derivative of Coumarin (HY-N0709). Ailancoumarin E exhibits antifeedant activity toward Plutella xylostella, and inhibits growth of third instar larva. Ailancoumarin E inhibits tyrosinase with IC50 of 14.21 μM .
|
-
-
- HY-121988
-
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
INF4E is a potent NLRP3 inflammasome inhibitor. INF4E inhibits caspase-1 and NLRP3 ATPase activities. INF4E shows protection against the IR-induced myocardial injury and dysfunction .
|
-
-
- HY-N9768
-
9-oxo-ODA
|
Fungal
PPAR
|
Infection
|
(10E,12E)-9-Oxo-10,12-octadecadienoic acid (9-oxo-ODA) is a PPARα agonist that can be isolated from the basidiomycete Gomphus floccosus. (10E,12E)-9-Oxo-10,12-octadecadienoic acid enhances fatty acid oxidation through PPARα activation, thereby inhibiting triglyceride accumulation. (10E,12E)-9-Oxo-10,12-octadecadienoic acid also has antifungal (Fungal) activity .
|
-
-
- HY-108938
-
|
Cytochrome P450
Fungal
Parasite
|
Infection
|
SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h) .
|
-
-
- HY-19183
-
-
-
- HY-113714
-
|
Bacterial
|
Infection
|
C562-1101 is a small molecule potent botulinum neurotoxins E serotype (BoNT/E) inhibitor .
|
-
-
- HY-157976
-
dinor-PGE1
|
Endogenous Metabolite
Prostaglandin Receptor
|
Others
|
Dinorprostaglandin E1 (dinor-PGE1) is the hepatocyte metabolite of prostaglandin E1 and prostaglandin E. Prostaglandin E1 and prostaglandin E inhibit glucagon, epinephrine, isoproterenol (beta-adrenergic agonist), or epinephrine-stimulated glycogenolysis when co-treated with Isoproterenol (HY-B0468) .
|
-
-
- HY-114942
-
Prostaglandin E1 Et ester; PGE1-EE
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Prostaglandin E1 ethyl ester (Prostaglandin E1 Et ester) is the esterified form of Prostaglandin E1 (PGE1; HY-B0131). Prostaglandin E1 (Alprostadil) is a prostaglandin receptor ligand that induces vasodilation and inhibits platelet aggregation .
|
-
-
- HY-77293
-
|
Apoptosis
Keap1-Nrf2
|
Cancer
|
(E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells .
|
-
- HY-168061
-
|
Bacterial
|
Infection
|
HldA/E-IN-1 (compound 8) is a dual inhibitor of HldA/E, with IC50 values of 17.2 μM and 67.8 μM for HldA/E, respectively. HldA/E-IN-1 can be used in the study of anti-bacterial infection .
|
-
- HY-129116
-
|
SARS-CoV
Cathepsin
|
Infection
|
SSAA09E1 is a cathepsin L blocker (IC50: 5.33 μM).SSAA09E1 inhibits stages of viral entry. SSAA09E1 can be used for SARS-CoV infection research
|
-
- HY-P9804
-
MERS-2E6; MERS Antibody-2E6
|
SARS-CoV
|
Infection
|
Anti-MERS-2E6 mAb (MERS-2E6; MERS Antibody-2E6), a human neutralizing antibody IgG1 (CHO expressed) that can compete for the binding of the virus Spike protein to the receptor (CD26), thereby inhibiting virus invasion into host cells.
|
-
- HY-16667
-
|
Early 2 Factor (E2F)
|
Cancer
|
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
|
-
- HY-N9376
-
|
NO Synthase
|
Inflammation/Immunology
|
Kansuinine E is a plant-derived nitric oxide inhibitor (IC50=6.3 μM). Kansuinine E belongs to jatrophane-type diterpenoids and is isolated from the roots of E. kansui .
|
-
- HY-131404
-
TPBM
1 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
|
-
- HY-160506
-
|
PROTACs
c-Met/HGFR
Apoptosis
|
Cancer
|
PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker;Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)) .
|
-
- HY-121569
-
|
Kinesin
|
Cancer
|
Syntelin is a selective centromere protein E (CENP-E) inhibitor with IC50 at 160 nM. Syntelin has antitumor activity .
|
-
- HY-145825A
-
|
Bcl-2 Family
|
Cancer
|
(E)-Mcl-1 inhibitor 7 (Example 34) is a Mcl-1 inhibitor (Ki: <1 nM, IC50: <500 nM). (E)-Mcl-1 inhibitor 7 can be used for research of cancers .
|
-
- HY-U00050
-
E-10-OH-NT
|
Drug Metabolite
|
Neurological Disease
|
(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline (HY-B1417). Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline (HY-B0527A) . E-10-OH-NT is about 50% as potent as nortriptyline as an inhibitor of the neuronal uptake of norepinephrine in vitro and exhibits less anticholinergic effects in man.
|
-
- HY-103164
-
|
Adenosine Receptor
Monoamine Oxidase
|
Neurological Disease
|
(E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research .
|
-
- HY-139795
-
|
HDAC
|
Cancer
|
ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC50s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model .
|
-
- HY-W072025
-
|
Cytochrome P450
Keap1-Nrf2
Heme Oxygenase (HO)
Reactive Oxygen Species
|
Inflammation/Immunology
|
CYP2E1-IN-1 (Compound 10) is an orally active cytochrome P450 2E1 (CYP2E1) inhibitor with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. CYP2E1-IN-1 activates the Nrf2/HO-1 signaling pathway and inhibits ROS production, thereby alleviating pancreatic injury. CYP2E1-IN-1 has significant anti-inflammatory and antioxidant activities and can effectively reduce inflammation and oxidative stress in severe acute pancreatitis (SAP). CYP2E1-IN-1 can be used in the study of SAP and other inflammatory-related diseases .
|
-
- HY-113896
-
|
Cholecystokinin Receptor
|
Others
|
U-67827E is a cholecystokinin (CCK) agonist that decreases food intake over a prolonged period of time in baboons. U-67827E may affect the latency to food by inhibiting the movement of food in the stomach and magnifying a gastric distention signal .
|
-
- HY-148664
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
eIF4E-IN-4 (Compound 33) is a selective inhibitor of eukaryotic initiation factor 4E (eIF4E) with biochemical
activity value of 95 nM. eIF4E-IN-4 inhibits cap-dependent mRNA translation with an IC50 value of 2.5 μM. eIF4E-IN-4 can be used for breast cancer, colon cancer, and head and neck cancer study .
|
-
- HY-14427
-
-
- HY-15166A
-
(E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
|
CDK
JAK
FLT3
|
Cancer
|
(E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor .
|
-
- HY-105516
-
|
Interleukin Related
|
Inflammation/Immunology
|
E5090 is an orally active inhibitor of IL-1 generation which is converted in vivo into the pharmacologically active deacetylated form (DA-E5090). E5090 can be utilized in immunology research .
|
-
- HY-132169
-
|
SARS-CoV
|
Infection
|
HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, with an EC50 of 0.65 μM and 0.6 μM in MTS and CPE cells, respectively .
|
-
- HY-15582
-
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
Auristatin E is a cytotoxic microtubule polymerization inhibitor with potent and selective antitumor activity. Auristatin E is a cytotoxin in antibody-drug conjugates (ADC). Auristatin E inhibits cell division by blocking the polymerisation of tubulin, promising for research in B-cell malignancies. Auristatin E, a synthetic analogue of the Dolastatin 10 (HY-15580), is linear peptides comprised of four amino acids .
|
-
- HY-129727
-
|
DNA/RNA Synthesis
Reactive Oxygen Species
Mitosis
|
Others
|
(E)-MS0019266 is a potent inhibitor of DNA damage repair. (E)-MS0019266 inhibits ribonucleotide reductase by generating reactive oxygen species. (E)-MS0019266 also reduces expression of genes related to cell cycle arrest and mitosis, including polo-like kinase 1, kinesin family member 20a, cyclin B1 and aurora kinase A. (E)-MS0019266 is promising for research of inhibitors of ribonucleotide reductase and polo-like kinase 1 .
|
-
- HY-19384
-
E 6087
|
COX
|
Inflammation/Immunology
|
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2).?Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models .
|
-
- HY-15166
-
(E/Z)-TG02; (E/Z)-SB1317
|
CDK
JAK
FLT3
|
Cancer
|
(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer .
|
-
- HY-145309
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
eIF4E-IN-3 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-3 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 485) .
|
-
- HY-170810
-
|
Bacterial
|
Infection
|
E.coli Gyrase B-IN-1 (Compound 10g) is a E.coli Gyrase B inhibitor with antibacterial activities. E.coli Gyrase B-IN-1 has potent inhibitory activity against E. coli, with a MIC value of 0.12 mM. E.coli Gyrase B-IN-1 is promising for research of antimicrobial agents .
|
-
- HY-111477
-
(E/Z)-RPL-554
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
(E/Z)-Ensifentrine is a dual inhibitor of PDE3/4. (E/Z)-Ensifentrine reduces the inflammatory cells into the airways. (E/Z)-Ensifentrine has bronchodilatory and anti-inflammatory activities in vitro and in vivo model .
|
-
- HY-W019710
-
|
HDAC
|
Neurological Disease
|
(E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington’s disease .
|
-
- HY-N14887
-
|
Antibiotic
Bacterial
|
Infection
Cancer
|
Phleomycin E is a heteropeptide antibiotic. Phleomycin E has anti-Gram-positive bacteria, negative bacteria and mycobacterium effects. Phleomycin E extends the survival time of mice transplanted with Ehrman's ascites cancer. Phleomycin E inhibits airy entity carcinoma in mice with an IC50 of 0.31 μg/mL .
|
-
- HY-Z7592
-
(E)-THR-221
|
Antibiotic
Bacterial
Penicillin-binding protein (PBP)
|
Infection
|
(E)-Cefodizime ((E)-THR-221) is an antibiotic. (E)-Cefodizime can selectively bind to penicillin-binding proteins (PBPs) and inhibit the synthesis of the bacterial cell wall, thereby exerting antibacterial activity. (E)-Cefodizime is promising for research of various bacterial infectious diseases, such as for preoperative infection prophylaxis .
|
-
- HY-138813A
-
(E/Z)-SU-12662 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
(E/Z)-N-Desethylsunitinib hydrochloride ((E/Z)-SU-12662 hydrochloride) is a compound with potential anti-tumor activity that inhibits VEGF-R2 and PDGF-Rβ tyrosine kinases. (E/Z)-N-Desethylsunitinib hydrochloride is the main active metabolite of sunitinib and has the ability to competitively inhibit ATP .
|
-
- HY-164587
-
|
DOCK
|
Metabolic Disease
|
E197 is the inhibitor for DOCK5 that destroys the podosome belt structure of osteoclasts, thereby inhibiting the bone resorption (IC50=3.44 μM in human osteoclast). E197 inhibits the Rac in DOCK5 expressing HEK293 cell with an IC50 of 36 μM. E197 prevents the bone loss in mouse ovariectomized models .
|
-
- HY-169858
-
|
PGE synthase
|
Inflammation/Immunology
|
Prostaglandin E2 Inhibitor 3 (Compound 3) is a selectivity microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50 = 0.2 µM). Prostaglandin E2 Inhibitor 3 has higher selectivity for mPGES-1 than cyclooxygenases (COX)-1/2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH). Prostaglandin E2 Inhibitor 3 has anti-inflammatory activity and can attenuate zymosan-induced peritoneal leukocyte migration in mice .
|
-
- HY-N14770
-
|
MMP
|
Infection
|
Matlystatin E is a metalloproteinase (MMP) inhibitor .
|
-
- HY-112097
-
E260
1 Publications Verification
|
Others
|
Cancer
|
E260 is a Fer/FerT kinase inhibitor.
|
-
- HY-N3007A
-
|
Others
|
Inflammation/Immunology
|
(E)-Naringenin chalcone is an orally active anti-allergic agent. (E)-Naringenin chalcone also has antioxidant, anti-inflammatory activities. (E)-Naringenin chalcone can improve adipocyte functions. (E)-Naringenin chalcone inhibits histamine release from rat peritoneal mast cell .
|
-
- HY-18956
-
(E/Z)-Sephin1; (E/Z)-IFB-088
|
Phosphatase
|
Inflammation/Immunology
|
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research .
|
-
- HY-13540
-
GPI 21016
|
PARP
|
Cancer
|
E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent .
|
-
- HY-18956B
-
(E/Z)-Sephin1 acetate; (E/Z)-IFB-088 acetate
|
Phosphatase
|
Inflammation/Immunology
|
(E/Z)-Icerguastat ((E/Z)-Sephin1) acetate is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat acetate can be used for protein misfolding diseases research .
|
-
- HY-N15506
-
|
NO Synthase
|
Inflammation/Immunology
|
Cycloneroside E is a sesquiterpene aminoglycoside compound discovered from Trichoderma sp. SCSIOW21. Cycloneroside E has the activity of inhibiting the production of NO. In macrophage RAW 264.7 cells, its IC50 value for inhibiting the production of NO is 48.0 µM. Cycloneroside E can be used in the research of the anti-inflammatory field .
|
-
- HY-18957C
-
BGB-283 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-N0272R
-
|
Others
|
Inflammation/Immunology
|
Eleutheroside E (Standard) is the analytical standard of Eleutheroside E. This product is intended for research and analytical applications. Eleutheroside E is an important component of Eleutheroside and has antioxidant, anti-fatigue, anti-inflammatory, antibacterial, immunomodulatory and cardioprotective effects. Eleutheroside E may inhibit the MAPK signaling pathway, thereby inhibiting H/R-induced NF-κB activation and oxidative stress, reducing metabolic reprogramming, and protecting myocardium from ischemia-reperfusion (I/R) injury. Eleutheroside E also counteracts the effects of high altitude hypobaric hypoxia (HAHI) by inhibiting inflammation and pyroptosis .
|
-
- HY-124205
-
-
- HY-13068
-
E-7050
|
c-Met/HGFR
VEGFR
|
Cancer
|
Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
|
-
- HY-139149A
-
|
Histone Acetyltransferase
|
Cancer
|
(E/Z)-NiCur is the active isomer of NiCur (HY-139149). (E/Z)-NiCur is a potent CBP histone acetyltransferase (HAT) inhibitor .
|
-
- HY-113481
-
-
- HY-126308
-
|
Cytochrome P450
|
Cancer
|
(E/Z)-DMU2139 (Compound 180) is the E/Z isomer of DMU2139 (HY-101285). (E/Z)-DMU2139 is a potent and specific CYP1B1 inhibitor (IC50: 4 nM) .
|
-
- HY-N2953
-
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
Borapetoside E can be isolated from T. crispa. Borapetoside E improves hyperglycemia, insulin resistance, hepatic steatosis, hyperlipidemia, and oxygen consumption in obese mice. Borapetoside E also inhibits SREBPs expression in the liver and adipose tissue .
|
-
- HY-161897
-
|
Kinesin
|
Cancer
|
CENP-E-IN-2 (compound 3) is a photoswitchable CENP-E inhibitor, with the pIC50 of 6.82 without light illumination and 5.85 with 365 nm light illumination. CENP-E-IN-2 has antitumor activity .
|
-
- HY-N6928R
-
|
Toll-like Receptor (TLR)
|
Metabolic Disease
Cancer
|
Mogroside III-E (Standard) is the analytical standard of Mogroside III-E. This product is intended for research and analytical applications. Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity .
|
-
- HY-116538
-
trans-10,cis-12 CLA2
|
Endogenous Metabolite
PPAR
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
(10E,12Z)-Octadeca-10,12-dienoic acidactivates PPAR α and inhibits adipocyte differentiation . (10E,12Z)-Octadeca-10,12-dienoic acid and its downstream metabolites have various antioxidant and antitumor activities. (10E,12Z)-Octadeca-10,12-dienoic acid is effective orally .
|
-
- HY-161732
-
|
Bcl-2 Family
|
Cancer
|
GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL .
|
-
- HY-114041S1
-
RvE1-d4-1
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Inflammation/Immunology
|
Resolvin E1-d4-1 is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production .
|
-
- HY-113205
-
15-keto-PGE2
|
Endogenous Metabolite
Prostaglandin Receptor
STAT
PPAR
|
Cancer
|
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth .
|
-
- HY-100227
-
E 64c
2 Publications Verification
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-107415
-
|
Raf
|
Cancer
|
PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines .
|
-
- HY-100733
-
-
- HY-N9867
-
|
TNF Receptor
|
Inflammation/Immunology
|
Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α .
|
-
- HY-153771
-
|
Bacterial
|
Infection
|
Du011 is an E. coli polysaccharide capsule biogenesis inhibitor that targets MprA. Du011 can be used in research against E. coli infection .
|
-
- HY-168684
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
E3 Ligase Ligand-linker Conjugate 136 is an E3 ligase ligand-linker conjugate. E3 Ligase Ligand-linker Conjugate 136 can be used to synthesize c-Myc inhibitor 7 (HY-148837) .
|
-
- HY-122895A
-
|
Apoptosis
PDI
|
Cancer
|
(E/Z)-E64FC26 is a mixture complex of E-E64FC26 and Z-E64FC26. E64FC26 (E-E64FC26) is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6. E64FC26 shows anti-myeloma activity .
|
-
- HY-N14647
-
-
- HY-14176G
-
γ-Secretase-IN-1
|
γ-secretase
|
Cancer
|
Compound E (GMP) is a GMP-grade Compound E (HY-14176). GMP-grade small molecules can be used as adjuvant reagents in cell therapy. Compound E is a γ-secretase inhibitor. Compound E inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50 values of 0.24, 0.37, and 0.32 nM, respectively .
|
-
- HY-113691
-
|
Lipoxygenase
|
Others
|
(E)-L-652343 is a compound with potent cyclooxygenase and 5-lipoxygenase inhibitory activity. (E)-L-652343 can effectively inhibit the synthesis of products of these two pathways in vivo. (E)-L-652343 showed high sensitivity and specificity in the detection of geometric isomers in canine and human plasma. (E)-L-652343 showed selective metabolism in vivo, and the elimination rate of the E isomer was faster than that of the Z isomer .
|
-
- HY-10082A
-
(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
|
DNA/RNA Synthesis
|
Cancer
|
(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis .
|
-
- HY-162884
-
|
β-glucuronidase
|
Infection
|
EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC50 of 2.68 μM and a Ki value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity .
|
-
- HY-110090
-
|
Microtubule/Tubulin
Kinesin
Apoptosis
|
Cancer
|
UA62784 is a microtubule polymerization inhibitor that interacts with tubulin dimers. UA62784 is a novel specific inhibitor of centromere protein E (CENP-E) kinesin. UA62784 can be used for the study of pancreatic cancer .
|
-
- HY-162562
-
|
PCSK9
|
Cardiovascular Disease
|
E28362 is a novel small molecule PCSK9 inhibitor. E28362 blocks the interaction between PCSK9 and LDLR, thereby preventing the degradation of LDLR and maintaining cholesterol homeostasia. E28362 is a promising lead compound for the study of hyperlipidemia and atherosclerosis .
|
-
- HY-123901
-
|
Apoptosis
|
Cancer
|
Garcinone E is a natural xanthone found in the rind of the mangosteen fruit. Garcinone E induces apoptosis and inhibits cancer cell migration. Garcinone E has anticancer effects on different human cancer cell lines, including colorectal, breast, and hepatocellular carcinomas .
|
-
- HY-114041S
-
RvE1-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Inflammation/Immunology
|
Resolvin E1-d4 (RvE1-d4) is deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production .
|
-
- HY-B0131S
-
-
- HY-121508
-
|
NF-κB
|
Inflammation/Immunology
Cancer
|
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). (E/Z)-IT-603 is also an IĸBα/c-Rel inhibitor. IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases .
|
-
- HY-155942
-
|
p38 MAPK
Raf
|
Cancer
|
B-Raf IN 19 (compound 31) is a BRAF inhibitor that inhibits BRAF(WT) and BRAF(V600E) (IC50: 0.57 μM and 0.28 μM, respectively). B-Raf IN 19 inhibits MAPK signaling in melanoma cells .
|
-
- HY-13650
-
E 7070
|
Molecular Glues
Carbonic Anhydrase
|
Cancer
|
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
|
-
- HY-137487
-
|
PROTACs
Raf
|
Cancer
|
PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.
|
-
- HY-135377
-
(2E)-2,3-Dehydroxy Atorvastatin
|
Drug Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
Atorvastatin 3-Deoxyhept-2E-Enoic Acid ((2E)-2,3-Dehydroxy Atorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids .
|
-
- HY-100738
-
NSC144303
|
Apoptosis
|
Cancer
|
Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
|
-
- HY-13013
-
|
TGF-beta/Smad
|
Inflammation/Immunology
|
(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1 .
|
-
- HY-Y0367
-
-
- HY-100229
-
E64d; E64c ethyl ester
|
Cathepsin
SARS-CoV
|
Neurological Disease
|
Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-80013B
-
|
CDK
|
Cancer
|
(E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect .
|
-
- HY-137117
-
15-keto Prostaglandin E1
|
Drug Metabolite
|
Others
|
15-keto-PGE1 is an inactive Prostaglandin E1 (PGE1) metabolite. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation .
|
-
- HY-124644
-
|
HIV
Phosphatase
|
Infection
|
1E7-03, a low MW tetrahydroquinoline derivative targeting protein phosphatase-1, can inhibit HIV-1 transcription .
|
-
- HY-Y0248AS
-
-
- HY-167685
-
|
Bacterial
|
Inflammation/Immunology
|
(E/Z)-Aureusidin is a flavonoid compound with antioxidant activity. (E/Z)-Aureusidin can inhibit the production of reactive oxygen species and reduce cell damage. (E/Z)-Aureusidin has anti-inflammatory effects and can reduce the expression of inflammatory factors. (E/Z)-Aureusidin has inhibitory effects on a variety of bacteria, indicating its potential antimicrobial properties .
|
-
- HY-B1388
-
Homatropine methobromide
|
mAChR
|
Neurological Disease
|
Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
|
-
- HY-161439
-
|
Akt
|
Cancer
|
Akt1-IN-4 (Compound 62) is an AKT1-E17K inhibitor with an IC50 value of less than 15 nM .
|
-
- HY-100287
-
|
Prostaglandin Receptor
Phospholipase
|
Endocrinology
|
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
|
-
- HY-107622
-
|
ERK
MEK
|
Metabolic Disease
|
(E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
|
-
- HY-15162R
-
MMAE (Standard); SGD-1010 (Standard); Vedotin (Standard)
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Monomethyl auristatin E (MMAE) (Standard) is the analytical standard of Monomethyl auristatin E (HY-15162). This product is intended for research and analytical applications. Monomethyl auristatin E is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) against several different cancer types .
|
-
- HY-106890
-
57G709
|
Angiotensin Receptor
PDGFR
|
Cardiovascular Disease
|
E4177 (57G709) is an orally active angiotensin II receptor antagonist. E4177 can inhibit the growth of vascular smooth muscle cells (HASMC) and the increase of cell surface area. In addition, E4177 can also increase the expression of platelet-derived growth factor (PDGF) receptor. E4177 can be used in the study of vascular diseases .
|
-
- HY-W263279
-
(E)-Wy-8678
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease .
|
-
- HY-18956A
-
(E/Z)-Sephin1 hydrochloride; (E/Z)-IFB-088 hydrochloride
|
Phosphatase
|
Neurological Disease
|
(E/Z)-Icerguastat hydrochloride ((E/Z)-Sephin1 hydrochloride) is a selective inhibitor with activity that prolongs the phosphorylation effects of eIF2α. (E/Z)-Icerguastat hydrochloride protects cells from defects in proteostasis. (E/Z)-Icerguastat hydrochloride was shown to significantly extend the survival of infected prion mice in a mouse model. (E/Z)-Icerguastat hydrochloride effectively reduces PrPSc expression and prion sequence activity in various neuronal cell lines persistently infected with different prion strains .
|
-
- HY-N14639
-
|
EGFR
|
Infection
|
Paeciloquinone E can inhibit the EGFR protein tyrosine kinase .
|
-
- HY-N14339
-
-
- HY-139825
-
-
- HY-79205
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-17 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-49413
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-2 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78903A
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-10 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-43149
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-5 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78908
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-11 is an intermediate reactant in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-33048
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-1 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78903
-
|
Microtubule/Tubulin
Drug Intermediate
|
Cancer
|
Monomethyl auristatin E intermediate-9 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78901A
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-8 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78911
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-13 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-17547
-
|
HSP
|
Cancer
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy .
|
-
- HY-79196
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-15 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-79198
-
|
Microtubule/Tubulin
Drug Intermediate
ADC Cytotoxin
|
Cancer
|
Monomethyl auristatin E intermediate-16 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-168512
-
|
Raf
|
Cancer
|
BRAFV600E-IN-1 (compound 9S) is a BRAF inhibitor. BRAFV600E-IN-1 has a significant apoptosis-inducing effect in cell lines expressing mutant KRAS and cancer cells expressing BRAFV600E .
|
-
- HY-78910
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-12 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-43147
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-4 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78899
-
|
Microtubule/Tubulin
Drug Intermediate
|
Cancer
|
Monomethyl auristatin E intermediate-6 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78901
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-7 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-78913
-
|
ADC Cytotoxin
|
Cancer
|
Monomethyl auristatin E intermediate-14 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-100640R
-
|
Reference Standards
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Roflumilast Impurity E (Standard) is the analytical standard of Roflumilast Impurity E. This product is intended for research and analytical applications. Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
|
-
- HY-43146
-
|
Microtubule/Tubulin
|
Cancer
|
Monomethyl auristatin E intermediate-3 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-110169
-
|
Phosphatase
|
Cardiovascular Disease
Cancer
|
(E/Z)-3PO is a potent PFKFB3 inhibitor. (E/Z)-3PO can inhibit the glycolysis process, reduce the extracellular acidification rate, and inhibit the capillary tube formation, migration of endothelial cells, and the formation of aortic sprouts, thereby suppressing angiogenesis. (E/Z)-3PO is promising for research of diseases such as cancer, acute lung injury, pulmonary fibrosis, and atherosclerosis .
|
-
- HY-N10213
-
|
NO Synthase
|
Infection
|
Septeremophilane E is a compound isolated from fungus Septoria rudbeckiae, a plant pathogenic fungus isolated from the halophyte Karelinia caspia. Septeremophilane E significantly inhibits the production of nitric oxide (NO) .
|
-
- HY-118008
-
|
5-HT Receptor
|
Neurological Disease
|
Lesopitron (E-4424) is a 5-HT receptor agonist with potent anxiolytic-like effects. Lesopitron inhibits forskolin-stimulated adenylate cyclase activity with an IC50 value of 125 nM .
|
-
- HY-19831
-
-
- HY-N10865
-
|
NO Synthase
|
Inflammation/Immunology
|
Chloranthalactone E (compound 6), a labdane diterpene, can be isolated from the aerial parts of Chloranthus serratus. Chloranthalactone E inhibits NO production in LPS-activated RAW 264.7 macrophages .
|
-
- HY-122881A
-
(E/Z)-JTP-0819958
|
IKK
|
Cancer
|
(E/Z)-HOIPIN-1 ((E/Z)-JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 value >2.8 μM. HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.
|
-
- HY-RI03069
-
|
MicroRNA
|
Cancer
|
mmu-miR-3473e inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-3473e inhibitor
mmu-miR-3473e inhibitor
- HY-RI00523
-
|
MicroRNA
|
Cancer
|
hsa-miR-302e inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-302e inhibitor
hsa-miR-302e inhibitor
- HY-RI00675
-
|
MicroRNA
|
Cancer
|
hsa-miR-320e inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-320e inhibitor
hsa-miR-320e inhibitor
- HY-RI00848
-
|
MicroRNA
|
Cancer
|
hsa-miR-378e inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-378e inhibitor
hsa-miR-378e inhibitor
- HY-12026
-
|
EGFR
|
Cancer
|
WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
|
-
- HY-145262
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-2 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 1188) . eIF4E-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-128043
-
AY-23578; Doproston B; 11-Deoxy-PGE1
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
11-Deoxy prostaglandin E1 (AY-23578; Doproston B) is an analog of prostaglandin E1 (PGE1) with bronchodilator activity. 11-Deoxy prostaglandin E1 inhibits histamine-induced bronchoconstriction and causes relaxation of tracheal strips in isolated guinea pigs .
|
-
- HY-158570
-
|
Bacterial
|
Infection
|
(2E)-Eicosenoic acid is an inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase A (PtpA). (2E)-Eicosenoic acid exhibits strong inhibitory activity against PtpA with an IC50 value in the low micromolar range. (2E)-Eicosenoic acid can be used for research on Mycobacterium tuberculosis infection .
|
-
- HY-101284A
-
|
Cytochrome P450
|
Cancer
|
(E/Z)-DMU2105 (Compound 7k) is a potent and highly selective CYP1B1 inhibitor. (E/Z)-DMU2105 inhibits human CYP1B1 enzyme bound to yeast-derived microsomes with an IC50 value of 10 nM. (E/Z)-DMU2105 also potently inhibits CYP1B1 expressed within ‘live’ recombinant yeast and human HEK293 kidney cells with an IC50 value of 63.65 nM. (E/Z)-DMU2105 can be used for the research of cancer, glaucoma, ischemia and obesity .
|
-
- HY-N0998
-
|
Melanocortin Receptor
|
Cancer
|
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 μM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
|
-
- HY-163479
-
|
Eukaryotic Initiation Factor (eIF)
MNK
|
Cancer
|
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970) .
|
-
- HY-145240
-
|
Eukaryotic Initiation Factor (eIF)
|
Infection
Cancer
|
eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y) .
|
-
- HY-114080A
-
E-3123 mesylate
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis .
|
-
- HY-114080
-
E-3123
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis .
|
-
- HY-N2682A
-
|
Carbonic Anhydrase
|
Cancer
|
(E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors . And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area .
|
-
- HY-P990280
-
|
TNF Receptor
|
Others
|
Anti-Mouse CD27 Antibody (RM27-3E5) is a rat-derived IgG2a, κ type antibody inhibitor, targeting to mouse CD27.
|
-
- HY-168125
-
|
JNK
|
Cancer
|
JNK-IN-18 (compund 23b) is a JNK1 inhibitor with IC50 of 2 nM, compared to JNK2 and BRAF(V600E) with IC50 of 125 nM and 98 nM, respectively .
|
-
- HY-11004
-
|
Raf
Apoptosis
|
Cancer
|
AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
|
-
- HY-136149
-
|
SARS-CoV
Virus Protease
|
Infection
|
Mpro inhibitor N3 is a potent SARS-CoV-2 MPro inhibitor with an EC50 value of 16.77 µM. Mpro inhibitor N3 shows antiviral activities against HCoV-229E, FIPV, IBV and MHV-A59 .
|
-
- HY-N14816
-
|
Acyltransferase
|
Infection
|
Glisoprenin E is a cholesterol acyltransferase (ACAT) inhibitor, and it can inhibit the formation of Appressorium on the hydrophobic surface of Magnaporthegrisea .
|
-
- HY-143281
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities .
|
-
- HY-B0131R
-
Alprostadil(Standard); PGE1 (Standard)
|
Prostaglandin Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
Cancer
|
Prostaglandin E1 (Standard) is the analytical standard of Prostaglandin E1. This product is intended for research and analytical applications. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases .
|
-
- HY-10261BR
-
|
EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
|
Others
|
(E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
|
-
- HY-W007888R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
Prostaglandin E1 (Standard) is the analytical standard of Prostaglandin E1. This product is intended for research and analytical applications. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases .
|
-
- HY-149518
-
|
EGFR
Apoptosis
|
Others
|
EGFR/BRAFV600E-IN-3 is a EGFR, BRAFV600E and EGFRT790M inhibitor with IC50 value of 57 nM, 68 nM and 9.70 nM. EGFR/BRAFV600E-IN-3 is an apoptotic inducer and also displays promising antioxidant activity .
|
-
- HY-123960B
-
|
Phosphatase
|
Neurological Disease
|
(E/Z)-Raphin1 is an inhibitor of PPP1R15B, a regulatory subunit of protein phosphatase 1. (E/Z)-Raphin1 is orally available and can cross the blood-brain barrier. (E/Z)-Raphin1 can be used in neurological research .
|
-
- HY-14566S3
-
E2020-d4 free base
|
Isotope-Labeled Compounds
|
Neurological Disease
Cancer
|
Donepezil-d4 (E2020-d4 (free base)) is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
|
-
- HY-W727525
-
-
- HY-145915A
-
|
Ras
|
Cancer
|
(E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction .
|
-
- HY-N12649
-
-
- HY-N14288
-
-
- HY-N14425
-
-
- HY-137458A
-
ARQ 751 trihydrochloride
|
Akt
|
Cancer
|
Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer .
|
-
- HY-161461
-
|
Amylases
|
Neurological Disease
|
E234G HYPE-IN-1 (Compound I2.10) is an inhibitor of AMPylation directed by the Huntingtin-interacting protein E (HYPE), possessing low micromolar bioactivity, low cytotoxicity, and blood-brain barrier permeability. E234G HYPE-IN-1 can inhibit the AMPylation of B-cell immunoglobulin-binding protein (BiP), the primary substrate of HYPE. E234G HYPE-IN-1 is suitable for development as a HYPE-specific therapeutic agent for clinical conditions such as neurodegenerative diseases and diabetes .
|
-
- HY-12001
-
|
EGFR
|
Cancer
|
WZ3146 is a mutant selective EGFR inhibitor with IC50s of
2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
|
-
- HY-173164
-
|
EGFR
Raf
Apoptosis
|
Cancer
|
EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAF V600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity .
|
-
- HY-P990248
-
|
Cadherin
|
Others
|
Anti-Mouse E-Cadherin/CD324 Antibody (DECMA-1) is a rat-derived IgG1, κ type antibody inhibitor, targeting to mouse E-Cadherin/CD324.
|
-
- HY-116100
-
-
- HY-N0060BR
-
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
|
-
- HY-157886
-
-
- HY-131667
-
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy .
|
-
- HY-137894A
-
PF-07104091 hydrate
|
CDK
GSK-3
|
Cancer
|
PF-07104091 hydrate is a potent and selective CDK2/cyclin E1 and GSK3β inhibitor, with Kis of 1.16 and 537.81 nM, respectively. PF-07104091 hydrate has anti-tumor activity for cyclin E1-amplified cancers. (patent WO2020157652A2).
|
-
- HY-116532
-
|
Bcl-2 Family
|
Cancer
|
YCW-E11 is a Bcl-2, and Mcl-1 inhibitor with Ki values of 0.83 and 0.33 μM, respectively. YCW-E11 induces cell apoptosis through the mitochondrial pathway and exhibits antitumor activity. YCW-E11 can be utilized in cancer research .
|
-
- HY-101015
-
|
Phospholipase
Apoptosis
|
Inflammation/Immunology
|
(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM .
|
-
- HY-173253
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
E3 Ligase Ligand-linker Conjugate 173 is an E3 Ligase Ligand-Linker Conjugate. E3 Ligase Ligand-linker Conjugate 173 can be used to synthesize YN14-H (HY-173250) to induce apoptosis and inhibits migration, and exert antitumor activity in vivo .
|
-
- HY-14176A
-
|
γ-secretase
|
Cancer
|
(1R,3S)-Compound E is the isomer of Compound E (HY-14176), and can be used as an experimental control. Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
|
-
- HY-P1427A
-
|
Potassium Channel
|
Neurological Disease
|
Guangxitoxin 1E TFA is the TFA salt form of Guangxitoxin 1E (HY-P1427). Guangxitoxin 1E TFA is a peptide toxin and a selective inhibitor for voltage-gated potassium channel KV2.1 and KV2.2 with IC50 of 1-3 nM. Guangxitoxin 1E TFA enhances glucose-stimulated intracellular calcium ion oscillations and increases insulin secretion in a glucose-dependent manner .
|
-
- HY-125539
-
|
Fungal
Antibiotic
|
Infection
|
Roridin E is an antibiotic that has cell-inhibiting and fungicidal activities similar to verrucarin .
|
-
- HY-15199
-
CEP-32496 hydrochloride; RXDX-105 hydrochloride
|
Raf
|
Cancer
|
Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
|
-
- HY-156859
-
-
- HY-156859A
-
|
Bacterial
|
Infection
|
NSC309401 is an inhibitor of E. coli DHFR (IC50: 189 nM, KD: 14.57 nM) .
|
-
- HY-78931
-
|
ADC Linker
|
Cancer
|
Boc-Dap-NE is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-N10340
-
Clauszoline I
|
Others
|
Cancer
|
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitory activities against proliferation of synoviocytes and cancer cells.
|
-
- HY-10299
-
|
Kinesin
Apoptosis
|
Cancer
|
GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.
|
-
- HY-128978
-
|
Phosphatase
|
Metabolic Disease
|
(E,E)-RAMB4 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1 .
|
-
- HY-RI01593
-
|
MicroRNA
|
Cancer
|
hsa-miR-519e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-519e-3p inhibitor
hsa-miR-519e-3p inhibitor
- HY-RI01594
-
|
MicroRNA
|
Cancer
|
hsa-miR-519e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-519e-5p inhibitor
hsa-miR-519e-5p inhibitor
- HY-RI01681
-
|
MicroRNA
|
Cancer
|
hsa-miR-548e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-548e-3p inhibitor
hsa-miR-548e-3p inhibitor
- HY-RI01602
-
|
MicroRNA
|
Cancer
|
hsa-miR-520e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-520e-5p inhibitor
hsa-miR-520e-5p inhibitor
- HY-RI01601
-
|
MicroRNA
|
Cancer
|
hsa-miR-520e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-520e-3p inhibitor
hsa-miR-520e-3p inhibitor
- HY-RI03049
-
|
MicroRNA
|
Cancer
|
mmu-miR-344e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-344e-3p inhibitor
mmu-miR-344e-3p inhibitor
- HY-RI01572
-
|
MicroRNA
|
Cancer
|
hsa-miR-518e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-518e-3p inhibitor
hsa-miR-518e-3p inhibitor
- HY-RI00544
-
|
MicroRNA
|
Cancer
|
hsa-miR-30e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-30e-5p inhibitor
hsa-miR-30e-5p inhibitor
- HY-RI03202
-
|
MicroRNA
|
Cancer
|
mmu-miR-467e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-467e-3p inhibitor
mmu-miR-467e-3p inhibitor
- HY-RI03465
-
|
MicroRNA
|
Cancer
|
mmu-miR-669e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-669e-3p inhibitor
mmu-miR-669e-3p inhibitor
- HY-RI03203
-
|
MicroRNA
|
Cancer
|
mmu-miR-467e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-467e-5p inhibitor
mmu-miR-467e-5p inhibitor
- HY-RI01573
-
|
MicroRNA
|
Cancer
|
hsa-miR-518e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-518e-5p inhibitor
hsa-miR-518e-5p inhibitor
- HY-RI03174
-
|
MicroRNA
|
Cancer
|
mmu-miR-466e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-466e-5p inhibitor
mmu-miR-466e-5p inhibitor
- HY-RI00009
-
|
MicroRNA
|
Cancer
|
hsa-let-7e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-let-7e-3p inhibitor
hsa-let-7e-3p inhibitor
- HY-RI00543
-
|
MicroRNA
|
Cancer
|
hsa-miR-30e-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-30e-3p inhibitor
hsa-miR-30e-3p inhibitor
- HY-RI03466
-
|
MicroRNA
|
Cancer
|
mmu-miR-669e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-669e-5p inhibitor
mmu-miR-669e-5p inhibitor
- HY-RI01682
-
|
MicroRNA
|
Cancer
|
hsa-miR-548e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
hsa-miR-548e-5p inhibitor
hsa-miR-548e-5p inhibitor
- HY-RI03050
-
|
MicroRNA
|
Cancer
|
mmu-miR-344e-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
|
-
mmu-miR-344e-5p inhibitor
mmu-miR-344e-5p inhibitor
- HY-15391A
-
|
VEGFR
FGFR
|
Cancer
|
Lucitanib (E-3810) dihydrochloride is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
|
-
- HY-15391
-
E-3810
|
VEGFR
FGFR
|
Cancer
|
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively .
|
-
- HY-13433
-
|
Calcium Channel
SARS-CoV
Apoptosis
|
Infection
Cancer
|
Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca 2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types .
|
-
- HY-N0060BS
-
(E)-Coniferic acid-d3
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299 .
|
-
- HY-N0346AR
-
-
- HY-W145436
-
-
- HY-N4119
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor .
|
-
- HY-113687
-
|
Bacterial
|
Infection
|
T145 is an oxazolidinone with antibacterial activity that inhibits growth of gram negatives (K. pneumoniae, A. baumannii, P. aeruginosa and E. cloacae), gram positives (E. faecalis and S. aureus) and acid fast pathogens (Mab, Mav and Mtb) .
|
-
- HY-N2963
-
|
ERK
p38 MAPK
JAK
STAT
TNF Receptor
Interleukin Related
COX
Arginase
|
Inflammation/Immunology
|
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis .
|
-
- HY-78899A
-
|
Microtubule/Tubulin
|
Cancer
|
(4R,5S)-Monomethyl auristatin E intermediate-6 is an intermediate reagent in the synthesis of Monomethyl auristatin E (HY-15162). Monomethyl auristatin E (MMAE) is a microtubule/tubulin inhibitor with anticancer activity. MMAE is widely used as the cytotoxic component (ADC Cytotoxin) of antibody-drug conjugates (ADCs) .
|
-
- HY-120997
-
Berbamine p-nitrobenzoate
|
Calmodulin
|
Cancer
|
E6 Berbamine (Berbamine p-nitrobenzoate) is a potent calmodulin (CaM) antagonist. E6 Berbamine inhibits the activity of calmodulin (CaM)-dependent myosin light chain kinase (MLCK), with a Ki of 0.95 μM . E6 Berbamine also shows anti-leukemia activities, with an IC50 of 2.13 μM in K562 cells .
|
-
- HY-155097
-
|
SARS-CoV
|
Infection
|
ARS-CoV-2-IN-53 (Compd 5d) can inhibit the replication of SARS-CoV-2 with an EC50 value of 14.3 μM. ARS-CoV-2-IN-5 shows significant antiviral activity against human coronavirus 229E (HCoV-229E) .
|
-
- HY-104068
-
|
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 μM. Naphthol AS-E can be used for cancer research.
|
-
- HY-N5164
-
|
Antibiotic
Fungal
|
Infection
|
Arborcandin E is a 1,3-β-glucan synthase inhibitor that serves as an antifungal antibiotic. Arborcandin E exhibits IC50 values of 0.1 μg/mL and 0.012 μg/mL against Candida albicans and Aspergillus fumigatus, respectively. Additionally, Arborcandin E has an MIC of 0.5-2 μg/mL against the genus Candida .
|
-
- HY-155611
-
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase,exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.,chronic obstructive pulmonary disease) .
|
-
- HY-108516
-
|
Wnt
PARP
|
Cancer
|
TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively .
|
-
- HY-173153
-
|
JNK
PERK
MEK
NO Synthase
|
Inflammation/Immunology
Cancer
|
BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities .
|
-
- HY-15338A
-
|
CDK
|
Cancer
|
(E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively .
|
-
- HY-156612
-
-
- HY-N14132
-
-
- HY-N10232
-
|
Others
|
Infection
|
Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis .
|
-
- HY-113794
-
SSYA10-001
|
Filovirus
|
Infection
|
DSHS00884 is a potent human papillomavirus E6 inhibitor with an IC50 of 10 μM .
|
-
- HY-149583
-
-
- HY-N2346
-
|
ADC Cytotoxin
Microtubule/Tubulin
|
Cancer
|
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
|
-
- HY-N1783
-
|
Phosphatase
|
Cancer
|
(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1B inhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1B inhibitory activity without cytotoxicity .
|
-
- HY-168336
-
|
PPAR
|
Metabolic Disease
|
E0924G is an orally active activator for PPARδ with EC50 of 2.82 μM. E0924G promotes the upregulation of osteoprotegerin (OPG) with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibites F-actin ring formation in RAW264.7 macrophages. E0924G regulates the bone density and bone loss in ovariectomized (OVX) and age-related osteoporosis models .
|
-
- HY-W008914
-
|
EGFR
|
Cancer
|
(E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor .
|
-
- HY-N6772
-
|
Autophagy
|
Cancer
|
Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation .
|
-
- HY-137567
-
|
Prostaglandin Receptor
|
Cancer
|
Prostaglandin E1 ethanolamide is an analog of prostaglandin E1 (PGE1) and may effectively inhibit GLI2-induced expression of target genes, including Gli1 and Ptch1, and tumor growth .
|
-
- HY-138063
-
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-B0428D
-
(E/Z)-OKY-046 sodium
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
(E/Z)-Ozagrel (sodium) [(E/Z)-OKY-046 (sodium)] is an EZ configuration mixture of Ozagrel (sodium) (HY-B0428A). Ozagrel (sodium) is a thromboxane A2 (TXA2) synthase inhibitor. Ozagrel (sodium) is an antiplatelet agent, which selectively inhibits human platelet aggregation with an IC50 of 53.12 μM .
|
-
- HY-126390
-
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-155602
-
|
CDK
|
Cancer
|
CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC50s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells .
|
-
- HY-15870A
-
|
AP-1
|
Inflammation/Immunology
Cancer
|
(6E)-SR 11302 is a E-isomer of SR 11302. SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE) .
|
-
- HY-114041
-
RvE1
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production .
|
-
- HY-142076A
-
|
CDK
|
Cancer
|
CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
|
-
- HY-142076
-
|
CDK
|
Cancer
|
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression .
|
-
- HY-176051
-
RgE
|
GLUT
|
Cancer
|
Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [ 3H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC50 values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells .
|
-
- HY-112149A
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
(E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2 .
|
-
- HY-115519
-
|
Casein Kinase
|
Cancer
|
(E/Z)-GO289 is a potent and selective casein kinase 2 (CK2) inhibitor (IC50=7 nM). (E/Z)-GO289 strongly lengthens circadian period. (E/Z)-GO289 exhibits cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function .
|
-
- HY-117921
-
|
Interleukin Related
|
Inflammation/Immunology
|
DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.
|
-
- HY-162938
-
|
E1/E2/E3 Enzyme
|
Cancer
|
Skp2 inhibitor 3 (E35), an antitumor agent, is a potent S‑Phase Kinase-associated Protein 2 (SKP2) inhibitor, with an IC50 of 4.86 μM for Skp2-Cks1 binding. Skp2 inhibitor 3 (E35) significantly inhibits colony formation and migration, as well as arrests the cell cycle at the S-phase .
|
-
- HY-N14812
-
|
Fungal
|
Infection
|
Neobulgarone E is an anthraquinone derivative of Neobulgaria pura HA A07-97, a fungus of the ascomycetes class. Neobulgarone E can inhibit the formation of Appressorium in Magnaporthe grisea and has weak cytotoxicity without antifungal, antibacterial or phytotoxicity .
|
-
- HY-14660S
-
GSK2118436A-d9; GSK2118436-d9
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively .
|
-
- HY-100372
-
(RS)-ECPG
|
mGluR
|
Neurological Disease
|
E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation .
|
-
- HY-118556
-
|
Prostaglandin Receptor
|
Endocrinology
|
Prostaglandin E2 serinol amide is a weak inhibitor of the hydrolysis of [3H]2-oleoylglycerol. Prostaglandin E2 serinol amide is non-hydrolyzable to produce PGE2 and thus cannot inhibit leukotriene B4 biosynthesis, superoxide production, migration and antimicrobial peptide release .
|
-
- HY-N1901
-
-
- HY-111643
-
-
- HY-15166B
-
(E/Z)-TG02 citrate; (E/Z)-SB1317 citrate
|
CDK
JAK
FLT3
|
Cancer
|
(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor .
|
-
- HY-139982
-
|
Bacterial
|
Infection
|
OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacterial strains .
|
-
- HY-157170
-
-
- HY-125386
-
-
- HY-18972
-
PLX8394; FORE8394
|
Raf
|
Cancer
|
PLX8394 is a potent and selective BRaf inhibitor, with an IC50 of appr 5 nM for BRAF V600E.
|
-
- HY-N10830
-
|
Others
|
Infection
|
(±)-Nirtetralin is an isomer of Nirtetralin, which inhibits growth of hepatitis E virus (HEV) in HepaRG cells .
|
-
- HY-172877
-
|
Raf
EGFR
Apoptosis
Bcl-2 Family
|
Cancer
|
EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway .
|
-
- HY-108241
-
|
OGA
|
Metabolic Disease
|
(Z)-PUGNAc is a potent O-GlcNAcase inhibitor. (Z)-PUGNAc is a vastly more potent inhibitor of O-GlcNAcase than the E form .
|
-
- HY-149922
-
|
LOX-1
|
Cardiovascular Disease
|
DKI5, also known as (E)-N’-benzylidenehydrazinecarbothiohydrazide, is a LOX-1 inhibitor with an IC50 value of 22.5 μM .
|
-
- HY-10834
-
|
β-catenin
|
Cancer
|
β-catenin-IN-6 is a β-catenin inhibitor, targeting to canonical Wingless-related integration site signaling pathway. β-catenin-IN-6 inhibits human colorectal cancer cells proliferation, as well as in a β-catenin/RK3E mouse model .
|
-
- HY-10568
-
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate .
|
-
- HY-137772R
-
|
Drug Metabolite
|
Others
|
Captopril EP Impurity E (Standard) is the analytical standard of Captopril EP Impurity E. This product is intended for research and analytical applications. Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-160662
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research .
|
-
- HY-B0131
-
Alprostadil; PGE1
|
Prostaglandin Receptor
Endogenous Metabolite
|
Cardiovascular Disease
Endocrinology
Cancer
|
Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases .
|
-
- HY-155048
-
|
Bacterial
|
Infection
|
BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
|
-
- HY-402815
-
|
Drug Intermediate
|
Cancer
|
(E)-4-(Naphthalen-2-yl)but-3-en-2-one (Compound 7) is a small active molecule that can be used as building block. (E)-4-(Naphthalen-2-yl)but-3-en-2-one exhibits anti-leukemic activity, that inhibits the proliferation of human chronic myeloid leukemia cell K562 with an IC50 of 7.6 μM .
|
-
- HY-13779
-
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
(E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the treatment of Alzheimer’s disease (AD) .
|
-
- HY-106784A
-
|
Fungal
Apoptosis
|
Neurological Disease
|
(E)-Ajoene is a oxygenated ajoene and organosulfur compound, which can be acquired via allicin decomposing. The polysulfides from garlic can be converted by human red blood cells into hydrogen sulfide (H2S) and allyl glutathione. (E)-Ajoene has been proved to show neuroprotective effects against ischemic damage. (E)-Ajoene is orally active to inhibit lipid peroxidation. (E)-Ajoene increases the number of cresyl violet-positive neurons and decreases the number of reactive gliosis in the CA1 region .
|
-
- HY-N0060B
-
(E)-Coniferic acid
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
|
-
- HY-N7661
-
|
PPAR
|
Metabolic Disease
|
4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression .
|
-
- HY-114509
-
|
Bacterial
|
Infection
Metabolic Disease
|
Anilazine is a fungicide and inhibit the growth of Rhizobium sp. and E. coli. Anilazine inhibits glucose oxidation and succinate oxidation and also inhibits in vitro succinic dehydrogenase activity .
|
-
- HY-148602
-
|
E1/E2/E3 Enzyme
|
Cancer
|
KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively .
|
-
- HY-14571
-
E7820
4 Publications Verification
ER68203-00
|
Molecular Glues
Integrin
|
Cancer
|
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity .
|
-
- HY-N10950
-
|
Dopamine Receptor
|
Cancer
|
Vanicoside E is an antioxidant and antitumor agent. Vanicoside E inhibits L-Tyrosine (HY-N0473) and L-DOPA (HY-N0304) with IC50s of 45.23 μM and 189.96 μM, respectively .
|
-
- HY-119648A
-
|
CD38
|
Inflammation/Immunology
|
(E/Z)-CCR-11 (Comp 12) is a selective CD38 inhibitor, with an IC50 of 20.8 μM against CD38 cyclase. (E/Z)-CCR-11 promotes increases in cellular NAD+ levels and interferon γ .
|
-
- HY-173155
-
|
Akt
|
Cancer
|
AKT1-IN-9 (4) is a selective mutant AKT1(E17K) inhibitor, with EC50 values of 9 nM and 995 nM in LAPC4-CR and SkBr3 cells, respectively .
|
-
- HY-100229R
-
E64d (Standard); E64c ethyl ester (Standard)
|
Reference Standards
Cathepsin
SARS-CoV
|
Neurological Disease
|
Aloxistatin (Standard) is the analytical standard of Aloxistatin. This product is intended for research and analytical applications. Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-15599
-
SSR
|
FGFR
|
Cancer
|
SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
|
-
- HY-106119
-
|
Prostaglandin Receptor
|
Infection
|
Camonagrel is a compound that has inhibitory effects on Prostaglandin E2. Camonagrel is a potent thromboxane synthase inhibitor .
|
-
- HY-156369
-
-
- HY-152082
-
-
- HY-N2519
-
(E)-Laricin
|
Fungal
|
Infection
|
(E)-Coniferin is the isomer of Coniferin. Coniferin is a glucoside of coniferyl alcohol. Coniferin inhibits fungal growth and melanization .
|
-
- HY-137422
-
-
- HY-143715
-
|
Ligands for E3 Ligase
|
Cancer
|
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
|
-
- HY-161867
-
|
Thrombin
|
Others
|
Platelet aggregation-IN-1 (Compound 10e) is an inhibitor for platelet aggregation, that inhibits 100% thrombin-induced platalet aggregation at 50 μM .
|
-
- HY-10016
-
|
γ-secretase
|
Neurological Disease
|
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat .
|
-
- HY-N0665
-
(8E)-Nuezhenide
|
NF-κB
Wnt
|
Inflammation/Immunology
|
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
|
-
- HY-10261B
-
(E/Z)-BIBW 2992
|
EGFR
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
Autophagy
|
Others
Cancer
|
(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells .
|
-
- HY-P2138
-
|
HIV Protease
|
Others
|
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
|
-
- HY-118628
-
N-(p-Amylcinnamoyl) anthranilic acid; ACA
|
Phospholipase
TRP Channel
|
Cardiovascular Disease
|
(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
|
-
- HY-119403
-
|
Cytochrome P450
|
Cancer
|
4-Phenyl-1,2,3-thiadiazole is an CYP2B4 and CYP2E1 inhibitor. 4-Phenyl-1,2,3-thiadiazole inhibits the oxidation of 1-phenylethanol to acetophenone by CYP2B4 and CYP2E1 .
|
-
- HY-121149B
-
(E/Z)-3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
|
-
- HY-129241
-
|
DNA/RNA Synthesis
DNA Alkylator/Crosslinker
|
Cancer
|
AGX51 is the first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and viability reduction. AGX51 can inhibit TNBC and has an IC50 of about 25 nM. AGX51 can be used in cancer research.
|
-
- HY-106350
-
U-63196E; AC-1370
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Cefpimizole (U-63196E) is a broad-spectrum cephalosporin antibiotic. Cefpimizole inhibits many Ampicillin (HY-B0522)-resistant bacteria, and is active against gram-negative species. Cefpimizole augments phagocytosis of macrophages and neutrophils .
|
-
- HY-106350A
-
U-63196E sodium; AC-1370 sodium
|
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
Cefpimizole (U-63196E) sodium is a broad-spectrum cephalosporin antibiotic. Cefpimizole sodium inhibits many Ampicillin (HY-B0522)-resistant bacteria, and is active against gram-negative species. Cefpimizole sodium augments phagocytosis of macrophages and neutrophils .
|
-
- HY-126144A
-
|
GSK-3
|
Metabolic Disease
|
(E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM .
|
-
- HY-168557
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-101 (compound 10O) is a potent and orally active SARS-CoV-2 inhibitor with an EC50 value of 0.64 µM for HCoV-229E. SARS-CoV-2-IN-101 shows cyotoxicity. SARS-CoV-2-IN-101 decreases the expression of HCoV-229E N protein and RNA level. SARS-CoV-2-IN-101 shows broad-spectrum anti-coronaviral effect .
|
-
- HY-19760B
-
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD) .
|
-
- HY-146442
-
|
Raf
|
Cancer
|
BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-P5570
-
|
Antibiotic
Bacterial
|
Infection
|
Aurein 2.3 is an antibiotic antimicrobial peptide. Aurein 2.3 partially inhibits E.coli ATPase activity and inhibits cell growth .
|
-
- HY-163408
-
|
Phosphatase
|
Others
|
ALP-IN-1 (Compound 7e) is an alkaline phosphatase (ALP) inhibitor (IC50 = 0.308 µM) .
|
-
- HY-12740
-
-
- HY-13475
-
-
- HY-163836
-
|
Drug Derivative
|
Others
|
HMBPP analog 1 (6e), a Trifluoromethyl analog, is the weakest agonist but the strongest inhibitor HMBPP ELISA response .
|
-
- HY-15599A
-
SSR free acid
|
FGFR
|
Cancer
|
SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
|
-
- HY-101627
-
-
- HY-101445
-
-
- HY-123399
-
-
- HY-128357
-
ACX-362E; GLS-362E
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI) .
|
-
- HY-N15300
-
|
Fungal
|
Infection
|
Acremorin E (Compound 7) is a terpenoid compound with antifungal activity. Acremorin E exerts its anti-C. gattiii effect by upregulating genes related to biosynthesis and RNA binding of ribosomes, as well as inhibiting RNA and nucleic acid metabolism and ATPase activity (MIC: 8 μg/mL) .
|
-
- HY-100226
-
|
Integrin
|
Inflammation/Immunology
|
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases .
|
-
- HY-131553
-
Vitamin E succinate
|
Apoptosis
|
Cancer
|
D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer .
|
-
- HY-13012G
-
E-616452; SJN 2511
|
TGF-β Receptor
|
Metabolic Disease
|
RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor .
|
-
- HY-14176
-
γ-Secretase-IN-1
|
γ-secretase
|
Cancer
|
Compound E is a γ-secretase inhibitor. Compound E blocks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
|
-
- HY-156978
-
Wy-48252
|
Leukotriene Receptor
|
Others
|
Ritolukast (Wy-48252) is an orally active aerosol leukotriene (LTD4/E4) receptor antagonist. Ritolukast can be used to inhibit the bronchoconstriction caused by aerosol LTD4 in guinea pigs, with an ID50 of 0.5mg/kg .
|
-
- HY-W1000105
-
-
- HY-13012
-
E-616452; SJN 2511
|
Organoid
TGF-β Receptor
|
Metabolic Disease
|
RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
|
-
- HY-117203A
-
|
CDK
|
Cancer
|
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM .
|
-
- HY-12756A
-
|
Toll-like Receptor (TLR)
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Inflammation/Immunology
|
E6446 dihydrochloride is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 dihydrochloride is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 dihydrochloride also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-12756
-
E6446
1 Publications Verification
|
Toll-like Receptor (TLR)
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
Inflammation/Immunology
|
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses. E6446 is also a potent SCD1 inhibitor (KD: 4.61 μM), significantly inhibiting adipogenic differentiation and hepatic lipogenesis through SCD1-ATF3 signaling. E6446 also improves liver pathology in high-fat diet (HFD)-fed mice and may be useful in the study of non-alcoholic fatty liver disease (NAFLD) .
|
-
- HY-169761
-
|
Histone Methyltransferase
|
Cardiovascular Disease
|
WIZ-IN-1 (Example 2) is a Wiz inhibitor (DC50: 0.36 μM). WIZ-IN-1 can be used for research of inherited blood disorders (e.g., hemoglobinopathies, e.g., beta- hemoglobinopathies), such as sickle cell disease and beta-thalassemia .
|
-
- HY-P1427
-
|
Potassium Channel
|
Neurological Disease
|
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons .
|
-
- HY-110144
-
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-116619
-
(E/Z)-NVP-LAQ824; (E/Z)-LAQ824
|
HDAC
Apoptosis
|
Others
|
(E/Z)-Dacinostat ((E/Z)-NVP-LAQ824) is a histone deacetylase inhibitor that has the ability to induce apoptosis and enhance the activity of fludarabine in killing leukemia cells. (E/Z)-Dacinostat can trigger the production of reactive oxygen species (ROS) and DNA damage, enhance the killing effect of fludarabine on leukemia cells, and induce apoptosis. Its mechanism is related to the regulation of DNA repair processes and intracellular signaling pathways.
|
-
- HY-121638
-
|
Apoptosis
DGK
|
Inflammation/Immunology
Cancer
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-N6928
-
-
- HY-101041
-
(E)-Tyrphostin AG 556
|
EGFR
|
Inflammation/Immunology
|
(E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production .
|
-
- HY-161291
-
|
CDK
|
Cancer
|
CDK2-IN-25 (compound 7e) is a CDK2 inhibitor with an IC50 of 0.149 μM .
|
-
- HY-N13884
-
|
Antibiotic
Bacterial
|
Infection
|
Amythiamicin D is a thiopeptide antibiotic that inhibits the growth of many Gram-positive bacteria, but not Gram-negative bacteria such as E.coli .
|
-
- HY-144280
-
|
Bacterial
|
Infection
|
MsbA-IN-2 (compound 12) is a potent lipopolysaccharide transporter MsbA inhibitor with an IC50 of 2 nM for E. coli MsbA .
|
-
- HY-118851
-
-
- HY-117065
-
|
Bacterial
|
Infection
|
MAC173979 is a inhibitor of PABA synthesis in E. coli. MAC173979 can be used for study of antibacterial drug development .
|
-
- HY-122210
-
-
- HY-149517
-
|
EGFR
Raf
Caspase
Bcl-2 Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAF V600E, and EGFR T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency .
|
-
- HY-124704
-
|
SULT
|
Neurological Disease
|
Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair .
|
-
- HY-162253
-
|
HIV
|
Infection
|
HIV-1 inhibitor-64 (Compound 7c) is a wild-type HIV-1 inhibitor that effectively suppresses the activity of HIV-1 mutants E138K/Q148K and G140S/Q148R with EC50 values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS .
|
-
- HY-19343
-
BMS-908662
|
Raf
|
Cancer
|
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. XL-281 exhibits antitumor activity .
|
-
- HY-110159
-
(E/Z)-A77 1726
|
Dihydroorotate Dehydrogenase
|
Infection
Inflammation/Immunology
|
(E/Z)-Teriflunomide ((E/Z)-A77 1726) is the active metabolite of
Leflunomide (HY-B0083). Leflunomide is an immunomodulatory agent that may exert effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). Leflunomide can be used for the research of rheumatoid arthritis (RA) .
|
-
- HY-P5580
-
|
Bacterial
|
Infection
Cancer
|
Dermaseptin-B3 inhibits the growth of Gram-positive and Gram-negative bacteria (MIC: 1.3, 2.3, 5.0, 2.6, 2.3 μM for S. aureus, P. aeruginosa, P. aeruginosa, E. (ATCC 25922), E. (54127) respectively). Dermaseptin-B3 also inhibits tumor cell proliferation .
|
-
- HY-110140
-
|
CaMK
|
Cardiovascular Disease
Neurological Disease
|
(E)-KN-93 phosphate is an inhibitor for Ca 2+/calmodulin-dependent protein kinase II (CaMK II) with IC50 of 9 μM and 3 μM, for CaMKIIδ monomer and CaMKIIδ dodecamer. (E)-KN-93 phosphate binds competitively with Ca 2+/CaM, and disrupts their interaction with CaMK II, and thus inhibits the CaMK II activation .
|
-
- HY-148106
-
|
Ligands for E3 Ligase
|
Cancer
|
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription .
|
-
- HY-156337
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-63 (Compound R3e) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-63 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 1.99 μM and 1.92 μM, respectively .
|
-
- HY-162149
-
|
Bacterial
|
Infection
|
Urease-IN-12 (compound 5e) is a competitive urease inhibitor (IC50: 0.35 μM) with the potential to inhibit gastritis and peptic ulcer caused by Helicobacter pylori .
|
-
- HY-130840
-
|
Bacterial
|
Cancer
|
LolCDE-IN-2 is a potent Lol protein (LolCDE) inhibitor. LolCDE-IN-2 inhibits E. coli MG1655 with a MIC of 2 μg/ml. Antibacterial activity .
|
-
- HY-159112
-
|
HDAC
|
Cancer
|
AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells .
|
-
- HY-101587
-
-
- HY-14971A
-
AKTIV
|
Akt
|
Cancer
|
Akt inhibitor-IV (AKTIV) acts as a PI3K-Akt inhibitor at the E isomer (HY-14971), with potent cytotoxicity .
|
-
- HY-126257
-
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
|
-
- HY-149260
-
-
- HY-145268
-
|
Cadherin
|
Cancer
|
SLEC-11 is a CDH1/E-cadherin modulator that potently inhibits cell death in E-cadherin-deficient cells (EC50=8.2 μM). SLEC-11 can be used to study potential synthetic lethal therapies for gastric cancer .
|
-
- HY-P10820
-
|
HIV
|
Infection
|
N36Mut(e,g) is a gp41-targeted HIV fusion peptide inhibitor. N36Mut(e,g) acts by disrupting the homotrimeric coiled-coil of N-terminal helices in the pre-hairpin intermediate to form heterotrimers .
|
-
- HY-130519
-
|
CDK
|
Cancer
|
Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle .
|
-
- HY-16261B
-
(E/Z)-Aldoxorubicin hydrochloride; Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride
|
Topoisomerase
Drug-Linker Conjugates for ADC
|
Cancer
|
MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties .
|
-
- HY-161987
-
|
Bacterial
|
Infection
|
LpxH-IN-2 (compound 014) is a potent LpxH inhibitor. LpxH-IN-2 shows antibacterial activity for E. coli .
|
-
- HY-N14829
-
|
Antibiotic
Bacterial
Fungal
|
Infection
|
Naphthoquinomycin A is an Ansa antibiotic with anti-Gram-positive bacteria and fungi activity, and can inhibit the synthesis of E. coli fatty acids .
|
-
- HY-P4204
-
|
Bacterial
|
Infection
|
Ranalexin is an antimicrobial peptide. Ranalexin inhibits S. aureus, E. coli, P. aerugiaosa with MICs of 4, 32, 128 μg/mL .
|
-
- HY-118211
-
|
Bacterial
|
Infection
|
EcDsbB-IN-9 (Compound 9) is a potent E. coli DsbB (EcDsbB) inhibitor with an IC50 of 1.7 μM and a Ki of 46 nM .
|
-
- HY-125158A
-
|
Aurora Kinase
|
Cancer
|
(E/Z)-HOI-07 is a potent and selective Aurora B inhibitor. HOI-07 has antitumor activity .
|
-
- HY-15184
-
Azalomycin B; Gopalamicin; Efomycin E
|
Autophagy
Antibiotic
|
Cancer
|
Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells .
|
-
- HY-N14522
-
|
Bacterial
|
Infection
Cancer
|
Gilvocarcin E has anti-Gram-positive bacterial activity and can inhibit sarcoma 180 and P388 leukemia cells .
|
-
- HY-18600B
-
-
- HY-117250
-
|
Bacterial
|
Infection
|
EcDsbB-IN-10 (compound 12) is an inhibitor of EcDsbB (E. coli DsbB) enzyme, with a Ki of 0.8 nM and an IC50 of 18.85 nM .
|
-
- HY-15200
-
CEP-32496; RXDX-105
|
Raf
|
Cancer
|
Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
|
-
- HY-16261A
-
(E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone
|
Topoisomerase
Drug-Linker Conjugates for ADC
|
Cancer
|
MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties .
|
-
- HY-147381
-
|
Bacterial
|
Others
|
MetRS-IN-1 (Compound 27) is an E. coli methionyl-tRNA synthetase (MetRS) inhibitor (IC50=237 nM) .
|
-
- HY-155238
-
|
GABA Receptor
|
Neurological Disease
|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
|
-
- HY-14177
-
|
Raf
|
Cancer
|
Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-146443
-
|
Raf
|
Cancer
|
BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases .
|
-
- HY-N0346A
-
-
- HY-N4119R
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
Neoeriocitrin (Standard) is the analytical standard of Neoeriocitrin. This product is intended for research and analytical applications. Neoeriocitrin, isolated from Drynaria Rhizome,?shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor .
|
-
- HY-146033
-
|
HPV
|
Cancer
|
HPV18-IN-1 (Compound H1) is a potent inhibitor of HPV18. HPV18-IN-1 prevents cervical cancer cells from premature cell procession and abnormal proliferation. HPV18-IN-1 supresses E7-Rb-E2F cellular pathway and DNA methylation. HPV18-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-N0665R
-
|
NF-κB
Wnt
|
Inflammation/Immunology
|
Specnuezhenide (Standard) is the analytical standard of Specnuezhenide. This product is intended for research and analytical applications. Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
|
-
- HY-19357
-
-
- HY-113113S
-
13,14-Dihydroprostaglandin E1-d4; PGE0-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
13,14-Dihydro PGE1-d4 (13,14-Dihydroprostaglandin E1-d4) is deuterium labeled 13,14-Dihydro PGE1. 13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
|
-
- HY-135194R
-
|
Drug Metabolite
Reference Standards
|
Others
|
Risperidone E-oxime (Standard) is the analytical standard of Risperidone E-oxime. This product is intended for research and analytical applications. Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
|
-
- HY-136149A
-
|
SARS-CoV
Virus Protease
|
Infection
|
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively .
|
-
- HY-170381
-
|
α-synuclein
|
Neurological Disease
|
α-syn aggregation inhibitor-1 (Compound 2e) is an inhibitor for α-syn aggregation. α-syn aggregation inhibitor-1 inhibits the cell viability of SH-SY5Y .
|
-
- HY-N7310
-
-
- HY-U00003
-
-
- HY-18997
-
PLX7904
3 Publications Verification
PB04
|
Raf
|
Cancer
|
PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAF V600E in mutant RAS expressing cells.
|
-
- HY-N14833
-
|
Antibiotic
Bacterial
Fungal
|
Infection
|
Naphthoquinomycin B is an Ansa antibiotic with anti-Gram-positive bacteria and fungi activity, and can inhibit the synthesis of E. coli fatty acids .
|
-
- HY-W083026
-
-
- HY-147317
-
|
Microtubule/Tubulin
|
Cancer
|
Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity .
|
-
- HY-N10433
-
Icarisids E
|
Xanthine Oxidase
|
Metabolic Disease
|
Xanthine oxidase-IN-9 (Icarisids E) (Compound 2) is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 31.81 μM .
|
-
- HY-W013411
-
(E/Z)-UIC-1005
|
Raf
|
Cancer
|
(E/Z)-Locostatin ((E/Z)-UIC-1005) is a racemic of Locostatin. Locostatin (UIC-1005) is a potent RKIP inhibitor. Locostatin binds Raf kinase inhibitor RKIP protein and disrupts the interaction of RKIP with Raf-1 kinase and G protein-coupled receptor kinase 2. Locostatin inhibits cell proliferation and migration. Locostatin aggravates thioacetamide (HY-Y0698)-induced acute liver failure in mice .
|
-
- HY-124760
-
|
mTOR
PI3K
CDK
|
Cancer
|
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM) .
|
-
- HY-170367
-
|
Bacterial
|
Infection
|
Antimicrobial agent-35 (Compound c9) exhibits antibacterial agent, that inhibits S. aureus, E. coli, E. faecalis, and S. maltophilia with MIC of 0.5-2 μg/mL. Antimicrobial agent-35 exhibits cytotoxicity against HT-22 with IC50 of 130.4 μg/mL .
|
-
- HY-172602
-
|
Antibiotic
Bacterial
Reactive Oxygen Species
|
Infection
|
ROS inducer 9 (compound 4e) is an antibacterial agent with a MIC value of 0.25 μg/mL against E. coli. ROS inducer 9 kills bacteria by inhibiting GSH activity and increasing ROS levels. ROS inducer 9 shows low toxicity to erythrocytes and RAW 264.7 cells .
|
-
- HY-125263
-
|
Estrogen Receptor/ERR
|
Cancer
|
OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
|
-
- HY-19717
-
S-[(1E)-1,2-Dichloroethenyl]-L-cysteine
|
TNF Receptor
|
Inflammation/Immunology
|
DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
|
-
- HY-161438
-
|
Akt
|
Cancer
|
Akt1-IN-3 (Compd 7) is an inhibitor of AKT1. Akt1-IN-3 inhibits AKT1- E17K with IC50 < 15 nM .
|
-
- HY-14177A
-
|
Raf
|
Cancer
|
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-121638A
-
|
Apoptosis
DGK
|
Cancer
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-132135
-
|
Polo-like Kinase (PLK)
|
Cancer
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- HY-116115
-
17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA
|
NF-κB
PPAR
|
Inflammation/Immunology
|
17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy .
|
-
- HY-143251
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity .
|
-
- HY-148100A
-
NOX-E36 sodium
|
CCR
|
Cancer
|
Emapticap pegol sodium is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol sodium is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
|
-
- HY-148100
-
NOX-E36
|
CCR
|
Inflammation/Immunology
Cancer
|
Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36) .
|
-
- HY-109045A
-
BTA074 hydrochloride; AP 611074 hydrochloride
|
E1/E2/E3 Enzyme
HPV
|
Infection
|
Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research .
|
-
- HY-77113
-
|
Raf
|
Cancer
|
B-Raf IN 11 (ZINC72115182) is a selective B-Raf V600E inhibitor (IC50=76 nM), shows selectivity for
B-Raf V600E over B-Raf WT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research
|
-
- HY-78931G
-
|
ADC Linker
|
Cancer
|
Boc-Dap-NE (GMP) is Boc-Dap-NE (HY-78931) produced by using GMP guidelines. Boc-Dap-NE is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-163455
-
|
HCN Channel
|
Neurological Disease
|
pan-HCN-IN-1 (Compound J&J12e) is an inhibitor for hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, with IC50 of 58 nM. pan-HCN-IN-1 reduces the voltage sag response and enhances EPSP summation in ex vivo rats brain slices .
|
-
- HY-109045
-
BTA074; AP 611074
|
E1/E2/E3 Enzyme
HPV
|
Infection
|
Teslexivir (BTA074) is a potent antiviral agent. Teslexivir is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir can be used for condyloma research .
|
-
- HY-107574
-
|
Histone Methyltransferase
AP-1
NF-κB
PKA
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
TC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers .
|
-
- HY-N12295
-
|
Others
|
Inflammation/Immunology
|
Ciwujianoside D1 is a natural product that can inhibit histamine release induced by anti-immunoglobulin E from rat peritoneal mast cells .
|
-
- HY-169011
-
|
Herbicide
|
Others
|
Phytoene desaturase-IN-3 (compound 8e) is a potent inhibitor of Phytoene desaturase . Phytoene desaturase-IN-3 has herbicidal activity .
|
-
- HY-N2586
-
|
Others
|
Inflammation/Immunology
|
Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 .
|
-
- HY-136266
-
|
HCV
|
Cancer
|
HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e .
|
-
- HY-153607
-
|
Cadherin
|
Cancer
|
HDAC-IN-55(8j) is a small molecular compound that can increase the expression of E-cadherin and inhibit the proliferation of cancer cells .
|
-
- HY-150046
-
|
NEKs
|
Cancer
|
Nek2-IN-6 (Compound 28e) is a potent never in mitosis (NIMA) related kinase 2 (Nek2) inhibitor .
|
-
- HY-132821A
-
E2027 maleate
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
Irsenontrine (E2027) maleate is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine maleate can be used for the research of neurological diseases .
|
-
- HY-42649
-
|
Bacterial
|
Neurological Disease
|
NSC 14699 is a small molecule non-peptide inhibitor of botulinum neurotoxin serotype E. NSC 14699 is promising for research of therapeutic and cosmetic agents .
|
-
- HY-168126
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-56 (compund 12e) is a potent VEGFR-2 inhibitor (IC50=45.9 nM) .
|
-
- HY-163838
-
|
Bacterial
|
Infection
|
Quorum sensing-IN-6 (compound 27) is a quorum sensing (QS) inhibitor with IC50 values of 8 and 106 nM for E.coli and Pyocyanin, respectively .
|
-
- HY-Y0367S
-
Maleic-2,3-d2 acid
|
Bacterial
Endogenous Metabolite
|
Infection
|
Maleic Acid-d2 is the deuterium labeled Maleic Acid . Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes .
|
-
- HY-161248
-
|
Microtubule/Tubulin
|
Cancer
|
E7130 is a microtubule inhibitor, which ameliorates the tumor microenvironment through suppression of cancer-associated fibroblasts (CAF) and promotion of tumor vasculature remodeling .
|
-
- HY-12846
-
|
Raf
|
Cancer
|
CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
|
-
- HY-P10848
-
|
Bacterial
|
Infection
|
RJPXD33 is the inhibitor for LpxD and LpxA with IC50 of 3.5 μM and 19 μM. RJPXD33 RJPXD33 inhibits LpxD and LpxA in E. coli with Kd of 6 μM and 20 μM .
|
-
- HY-18652
-
Ro 5126766; CH5126766
|
MEK
Raf
|
Cancer
|
Avutometinib (Ro 5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
|
-
- HY-129636A
-
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-168282
-
|
PROTACs
MAP4K
|
Cancer
|
DD205-291 is an orally active PROTAC HPK1 degrader, with a DC50 value of 5.3 nM. DD205-291 inhibits SLP-76 phosphorylation and induces IL-2 and IFN-γ expression (Pink: HPK1 protein ligand HY-168283; E3+linker: HY-168284; Blue: E3: HY-W115490; Black: linker: HY-W210252) .
|
-
- HY-168326
-
|
DNA/RNA Synthesis
Microtubule/Tubulin
|
Cancer
|
Antiproliferative agent-64 (Compound 76) is an inhibitor for eukaryotic translation initiation factor 4E (eIF4E), that block the secondary structure of mRNA, thereby inhibiting protein translation. Antiproliferative agent-64 inhibits the 5' untranslated region (5'UTR) of c-Myc (c-myc 5'UTR) with an EC50 of 1.2 nM, inhibits 5'UTR encoding tubulin (tub 5'UTR) with an EC50 of 40 nM. Antiproliferative agent-64 inhibits the proliferation of MDA-MB-231 with an EC50 of 7 nM .
|
-
- HY-N6850
-
|
Apoptosis
Pyroptosis
AMPK
Bcl-2 Family
JAK
STAT
Calcium Channel
Interleukin Related
TNF Receptor
SOD
Reactive Oxygen Species
PPAR
|
Cardiovascular Disease
Inflammation/Immunology
|
Calenduloside E is a pentacyclic triterpenoid saponin that can be extracted from the bark and roots of Aralia ovata, and has anti-inflammatory and anti-apoptotic activities. Calenduloside E alleviates atherosclerosis by regulating macrophage polarization, improves mitochondrial function by regulating the AMPK-SIRT3 pathway, and alleviates acute liver injury. In addition, Calenduloside E promotes the interaction between L-type calcium channels and Bcl-2 related apoptosis genes, inhibits calcium overload, and alleviates myocardial ischemia/reperfusion injury. Calenduloside E also improves non-alcoholic fatty liver disease by regulating heat shock-dependent pathways, and inhibits ROS mediated JAK1-STAT3 pathways to reduce cellular inflammatory responses .
|
-
- HY-158061
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase II inhibitor 20 (Compound 3e) is a potent topoisomerase II (Topoisomerase II) inhibitor with an IC50 of 0.98 µM. Topoisomerase II inhibitor 20 induces apoptosis and has broad-spectrum anticancer activity .
|
-
- HY-157164
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity .
|
-
- HY-111871
-
|
SNIPERs
Bcr-Abl
|
Cancer
|
SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM (ABL inhibitor: HY-15814; ABL inhibitor activity control: HY-131178; E3 ligase ligand: HY-128808; linker: HY-130500; E3 ligase ligand + linker: HY-128819) .
|
-
- HY-N12320
-
|
Antibiotic
|
Infection
|
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
|
-
- HY-117693
-
|
ATM/ATR
|
Cancer
|
(E/Z)-Mirin is a mixture of (E)-Mirin and Mirin ((Z)-Mirin) (HY-19959) configurations. Among them, Mirin is an inhibitor of MRN (Mre11-Rad50-Nbs1). Mirin prevents MRN-dependent ATM activation without affecting ATM protein kinase activity .
|
-
- HY-148233S
-
|
Casein Kinase
|
Others
|
JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure .
|
-
- HY-78931F
-
|
Drug Intermediate
|
Cancer
|
(R,S,S,S,R)-Boc-Dap-NE is an isomer of the dipeptide Boc-Dap-NE (HY-78931). Boc-Dap-NE is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-78931C
-
|
Drug Intermediate
|
Cancer
|
(S,S,R,S,R)-Boc-Dap-NE is an isomer of the dipeptide Boc-Dap-NE (HY-78931). Boc-Dap-NE is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-78931E
-
|
Drug Intermediate
|
Cancer
|
(R,S,R,S,R)-Boc-Dap-NE is an isomer of the dipeptide Boc-Dap-NE (HY-78931). Boc-Dap-NE is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-N3617
-
-
- HY-161251
-
|
E1/E2/E3 Enzyme
|
Cancer
|
SPOP-IN-2 (compound E1) is a Speckle-type POZ protein (SPOP) inhibitor with IC50 of 0.58 μM, which disrupt the SPOP-subtrate interaction and selectively inhibits proliferation of ccRCC .
|
-
- HY-14596
-
NPI 031L
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
|
-
- HY-U00112
-
BLE 00084; E2MATE; ES-J 995
|
Steroid Sulfatase
|
Cancer
|
Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM.
|
-
- HY-162025
-
|
mTOR
PI3K
|
Cancer
|
mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 40 nM .
|
-
- HY-13442
-
B1939; E7389; ER-086526
|
Microtubule/Tubulin
Apoptosis
ADC Cytotoxin
|
Cancer
|
Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
|
-
- HY-112798
-
|
Apolipoprotein
|
Neurological Disease
|
PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
|
-
- HY-18926
-
|
VEGFR
|
Cancer
|
VEGFR2-IN-7 (compound E) is an inhibitor of VEGFR2. VEGFR2-IN-7 can used in study cancers .
|
-
- HY-P0135
-
|
Bacterial
|
Infection
|
Penta lysine is an antibacterial agent, that inhibits E. coli, A. baumannii, P. aeruginos, S. aureus, and B. subtilis, with MIC of 1.1-18 μM .
|
-
- HY-149325
-
|
Others
|
Others
|
RPE65-IN-1(Compound 16e) is a potent RPE65 inhibitor, which can be used in retinopathy-related research .
|
-
- HY-162292
-
|
PI3K
Kinesin
|
Cancer
|
Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer .
|
-
- HY-122903B
-
|
DNA/RNA Synthesis
|
Others
|
(+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor .
|
-
- HY-15811
-
ACK1-B19
|
Tyrosinase
|
Cancer
|
XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
|
-
- HY-132821
-
-
- HY-158347
-
-
- HY-13442A
-
B1939 mesylate; E7389 mesylate; ER-086526 mesylate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Eribulin (E7389) mesylate is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin mesylate inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
|
-
- HY-A0163D
-
(E)-Clopenthixol
|
Antibiotic
Bacterial
Parasite
|
Infection
|
trans-Clopenthixol ((E)-Clopenthixol) is an antibiotic, without neuroleptic effect. trans-Clopenthixol can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro .
|
-
- HY-15741
-
-
- HY-78933
-
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC .
|
-
- HY-14660A
-
GSK2118436 Mesylate; GSK 2118436B
|
Raf
|
Cancer
|
Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for Raf V600E and c-Raf, respectively.
|
-
- HY-153428
-
-
- HY-101243
-
|
Tyrosinase
|
Cancer
|
XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
|
-
- HY-135813
-
|
Bacterial
|
Infection
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely .
|
-
- HY-10981A
-
E7080 mesylate
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-10981
-
E7080
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-108887
-
|
Raf
|
Cancer
|
Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells .
|
-
- HY-12558
-
DP-4978
|
Raf
Autophagy
|
Cancer
|
LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively.
|
-
- HY-N15306
-
|
Apoptosis
|
Cancer
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-172798
-
|
Bcl-2 Family
|
Cancer
|
XZ338 is a highly selective degrader targeting BCL-XL. XZ338 does not degrade BCL-2. XZ338 inhibits MOLT-4 cells with a IC50 value of 3.7 nM. XZ338 has anti-proliferative activity. XZ338 can be used for anti-cancer study. (Target protein ligand: HY-19741; E3 ligase: HY-112078; linker: HY-172799; E3+liner: HY-172800) .
|
-
- HY-51424S
-
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an IC50?of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf .
|
-
- HY-W007972R
-
|
Others
|
Others
|
Anilazine (Standard) is the analytical standard of Anilazine. This product is intended for research and analytical applications. Anilazine is a fungicide and inhibit the growth of Rhizobium sp. and E. coli. Anilazine inhibits glucose oxidation and succinate oxidation and also inhibits in vitro succinic dehydrogenase activity .
|
-
- HY-114509R
-
|
Bacterial
|
Infection
Metabolic Disease
|
Anilazine (Standard) is the analytical standard of Anilazine. This product is intended for research and analytical applications. Anilazine is a fungicide and inhibit the growth of Rhizobium sp. and E. coli. Anilazine inhibits glucose oxidation and succinate oxidation and also inhibits in vitro succinic dehydrogenase activity .
|
-
- HY-130642
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
(S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901 .
|
-
- HY-170975
-
|
VD/VDR
|
Cancer
|
UG-650 is a non-Gemini analog of UVB1 that combines the structural features of UVB1 and MC 1288. UG-650 can bind to the vitamin D receptor (VDR) and inhibit the proliferation of MCF-7 cells and the migration of MC3T3-E1 cells .
|
-
- HY-149271
-
|
Bacterial
DNA/RNA Synthesis
Topoisomerase
|
Infection
|
Anti-MRSA agent 7 (Compound 12) is a potent antibacterial agent. Anti-MRSA agent 7 inhibits S. aureus DNA gyrase, E. coli DNA gyrase, S. aureus topo IV and E. coli topo IV with IC50s of 0.185, 0.365, 0.341 and 0.059 μM, respectively .
|
-
- HY-117857
-
-
- HY-168109
-
|
Antibiotic
Bacterial
|
Infection
|
Antibacterial agent 246 (compound A33) is a antibacterial agent and has minimum inhibitory concentrations (MICs) of 0.5-4 μg/mL against twenty-three Gram-positive bacteria. Antibacterial agent 246 in combination with Polymyxin E(HY-113678) E inhibits the growth of various Gram-negative bacteria with the fractional inhibitory concentration index of 0.066 .
|
-
- HY-109055
-
E2609
|
Beta-secretase
|
Neurological Disease
|
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research .
|
-
- HY-N4283A
-
|
Fungal
|
Infection
|
(E)-Coniferyl alcohol is the isomer of Coniferyl alcohol. Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbenoids and coumarin. Coniferyl alcohol specifically inhibits fungal growth .
|
-
- HY-18957
-
BGB-283
|
EGFR
Raf
|
Cancer
|
Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively.
|
-
- HY-A0163C
-
(E)-Clopenthixol dihydrochloride
|
Antibiotic
Bacterial
Parasite
|
Infection
|
trans-Clopenthixol ((E)-Clopenthixol) dihydrochloride is an antibiotic agent, without neuroleptic effect. trans-Clopenthixol dihydrochloride can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro .
|
-
- HY-15496
-
ER-806201
|
MEK
FLT3
|
Cancer
|
E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
|
-
- HY-13496
-
|
c-Fms
|
Inflammation/Immunology
Cancer
|
JNJ-28312141 is an inhibitor for colony-stimulating factor-1 receptor (CSF-1R or FMS), with an IC50 of 0.69 nM. JNJ-28312141 inhibits proliferation of BDBM, MV-4-11, M-o7e, TF-1 with an IC50s of 2.6, 21, 41 and 150 nM, respectively. JNJ-28312141 exhibits anti-inflammatory activity in mouse arthritis model .
|
-
- HY-150065
-
|
Parasite
|
Infection
Inflammation/Immunology
|
Antimalarial agent 15 (Compound 4e) is a parasite inhibitor. Antimalarial agent 15 shows antimalarial activity, and can inhibit P. falciparum 3D7 parasite growth (IC50=20 nM) .
|
-
- HY-111370
-
|
mTOR
|
Cancer
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates .
|
-
- HY-135742
-
Lenvatinib impurity 10
|
VEGFR
|
Cancer
|
Lenvatinib N-Oxide (Lenvatinib impurity 10) is the impurity of Lenvatinib (HY-10981). Lenvatinib (E7080) is an orally active, multi-targeted tyrosine kinase inhibitor .
|
-
- HY-N4182
-
|
Akt
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation .
|
-
- HY-19167
-
AS 013; Lipo-pro-prostaglandin E1
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Ecraprost is a prodrug of prostaglandin E1. Ecraprost inhibits platelet adhesion, macrophage infiltration and proliferating cell nuclear antigen positive cell expression on the injured arterial walls .
|
-
- HY-145712
-
|
FKBP
|
Cancer
|
ElteN378 is an inhibitors of FKBP12e. ElteN378 can be used in study Alzheimer disease, Parkinson disease, Amyotrophic Lateral Sclerosis, proliferation disorders and cancer .
|
-
- HY-100640
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a agent which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
|
-
- HY-W1006754
-
-
- HY-14566
-
-
- HY-14660
-
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-I0727
-
|
Drug Metabolite
|
Others
|
Sofosbuvir impurity E is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-18785
-
|
IGF-1R
|
Endocrinology
Cancer
|
Indirubin Derivative E804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.
|
-
- HY-168853
-
|
Bacterial
|
Infection
|
Antibacterial agent 261 (compound 43) is a potent inhibitor of peptidomimetic peptide deformylase (PDF), with IC50 of 2.5 and 10.6 nM for S. aureus and E. coli, respectively .
|
-
- HY-N12914
-
(+)-Tanzawaic acid B; GS-1302-1; 10-Deoxytanzawaic acid E
|
Reactive Oxygen Species
|
Others
|
Tanzawaic acid B ((+)-Tanzawaic acid B; GS-1302-1; 10-Deoxytanzawaic acid E) is a superoxide anion production inhibitor and can be isolated from Penicillium citrinum .
|
-
- HY-124330
-
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively .
|
-
- HY-109081
-
E7727
|
DNA/RNA Synthesis
|
Cancer
|
Cedazuridine (E7727) (Compound 7a) is an orally active cytidine deaminase (CDA) inhibitor with an IC50 value of 0.4 μM. Cedazuridine can be used for cancer research .
|
-
- HY-139746
-
|
Beta-lactamase
Bacterial
|
Infection
|
FPI-1602 is a β-lactamase inhibitor. FPI-1602 displays marked antimicrobial activity against P. aeruginosa, E. coli, and Enterobacter spp. .
|
-
- HY-109081A
-
E7727 hydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
Cedazuridine (E7727) (Compound 7a) hydrochloride is an orally active cytidine deaminase (CDA) inhibitor with an IC50 value of 0.4 μM. Cedazuridine hydrochloride can be used for cancer research .
|
-
- HY-15605
-
LGX818
|
Raf
|
Cancer
|
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
- HY-15767
-
TAK-632
4 Publications Verification
|
Raf
Aurora Kinase
|
Cancer
|
TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively.
|
-
- HY-18957B
-
BGB-283 maleate
|
EGFR
Raf
|
Others
Cancer
|
Lifirafenib (BGB-283) maleate is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively .
|
-
- HY-145752
-
|
PROTACs
SGK
Autophagy
|
Cancer
|
HaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two Halo-tagged endoplasmic reticulum-localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM. HaloPROTAC-E significantly and selectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) labeled with Halo and inhibits autophagy.
|
-
- HY-P99843
-
|
TROP2
ADC Antibody
|
Cancer
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
- HY-78931B
-
|
Drug Intermediate
|
Cancer
|
(S,S,S,S,R)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE (HY-78931), and can be used as an experimental control. Boc-Dap-NE, is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-N14342
-
|
Bacterial
|
Infection
|
Manumycin E has anti-Gram-positive bacteria and Escherichia coli effects, but the effect is very weak against other anti-Gram-negative bacteria, and has no effect on fungi. Manumycin E inhibits RAS Faraday base transfer and has weak cytotoxic activity against human cloned cancer cell lines HCT-116 (IC50 is 15.6 μg/mL) .
|
-
- HY-122895
-
E64FC26
2 Publications Verification
|
Apoptosis
PDI
|
Cancer
|
E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6, respectively. E64FC26 shows anti-myeloma activity .
|
-
- HY-78931A
-
|
Drug Intermediate
|
Cancer
|
(R,S,S,R,S)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE (HY-78931), and can be used as an experimental control. Boc-Dap-NE, is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-N7224
-
SF-1854
|
Bacterial
Antibiotic
|
Infection
|
N-Formylfortimicin A (SF-1854) is an aminoglycoside antibiotic with broad-spectrum antibacterial activity. It primarily acts on bacterial ribosomes to inhibit protein synthesis and exhibits notable inhibitory effects against various Gram-positive and Gram-negative bacteria (e.g., E. coli with a MIC of 12.5-50 μg/mL), making it a potential candidate for research on bacterial infection-related diseases .
|
-
- HY-51424
-
|
Raf
|
Cancer
|
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
|
-
- HY-113054
-
|
Acyltransferase
Bacterial
Endogenous Metabolite
|
Infection
Metabolic Disease
|
DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase .
|
-
- HY-N0170
-
-
- HY-148441
-
|
Others
|
Metabolic Disease
|
NDH-1 inhibitor-1 (compound 27) is a potent NDH-1 inhibitor with pI50 values of <4, 5.40, 6.15 µM for Bovine SMP (submitochondrial particles), Potato SMP and E. coli, respectively .
|
-
- HY-138102
-
|
SARS-CoV
|
Infection
|
SSAA09E3 is a SARS-CoV entry inhibitor that inhibits SARS/HIV pseudotyped virus entry with an EC50 of 9.7 μM in 293T cells and inhibits SARS-CoV infection of Vero cells with an EC50 of 0.15 μM .
|
-
- HY-161385
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
|
-
- HY-117707
-
|
Raf
|
Cancer
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
|
-
- HY-141640
-
|
PROTACs
EGFR
|
Cancer
|
MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)) .
|
-
- HY-100388
-
|
SHP2
Phosphatase
|
Cancer
|
SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2 D61Y, SHP2E69K, SHP2 A72V, SHP2 E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth .
|
-
- HY-147825
-
|
EGFR
Raf
Apoptosis
|
Cancer
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-131252
-
Dihydro E2020
|
Cholinesterase (ChE)
|
Neurological Disease
|
Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively .
|
-
- HY-P990292
-
|
Interleukin Related
|
Others
|
Anti-Mouse CD132 (common γ chain) Antibody (3E12) is a rat-derived IgG2b type antibody inhibitor, targeting to mouse CD132.
|
-
- HY-P5204
-
K1-EJ hybrid
|
Bacterial
|
Infection
|
Enterocin Hybrid 1 is a antibacterial agent, a antibacterial composition. Enterocin Hybrid 1 inhibits Vancomycin (HY-B0671)-resistant E. faecium, Staphylococcus haemoliticus .
|
-
- HY-141841
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
|
-
- HY-152954
-
|
DAPK
|
Inflammation/Immunology
|
DRAK1/2-IN-1 (compound 10e) is an active dual DRAK1 and DRAK2 inhibitor with Kd values of 1 μM and 6 μM, respectively .
|
-
- HY-172946
-
|
PROTACs
STAT
|
Cancer
|
SD-2301 is a PROTAC based STAT3 degrader (Red: STAT3 inhibitor (HY-172947), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-103081
-
|
β-glucuronidase
Bacterial
|
Infection
Cancer
|
β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively .
|
-
- HY-173512
-
|
Tyrosinase
|
Metabolic Disease
|
mTYR-IN-1 (compound 3e) is a reversible and competitive mTYR inhibitor with an IC50 of 4.86 μM. mTYR-IN-1 can be used in the study of skin pigmentation .
|
-
- HY-P990291
-
-
- HY-158241
-
|
Bacterial
|
Infection
|
GmhA-IN-1 (compound 17) is an inhibitor of GmhA with an IC50 value of 2.4 nM. GmhA-IN-1 enhances the activity of erythromycin and rifampicin on wild-type E. coli .
|
-
- HY-143280
-
|
Topoisomerase
|
Cancer
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-158172
-
|
E1/E2/E3 Enzyme
|
Others
|
Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ligase Casitas B-lineage lymphoma proto-oncogene B (CPL-B). Cbl-b-IN-18 inhibits the phosphorylation of CPL-B (IC50< 100 nM) .
|
-
- HY-19719
-
ARQ-092
|
Akt
Parasite
|
Infection
Cancer
|
Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib is effective against Leishmania .
|
-
- HY-114903
-
GSK-3 Inhibitor X
|
GSK-3
CDK
|
Neurological Disease
Metabolic Disease
Cancer
|
(E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM) .
|
-
- HY-19719A
-
ARQ-092 hydrochloride
|
Akt
Parasite
|
Infection
Cancer
|
Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib hydrochloride is effective against Leishmania .
|
-
- HY-100349
-
|
PDGFR
VEGFR
|
Cancer
|
SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively .
|
-
- HY-165154
-
Desdanine; Pyracrimycin A
|
Antibiotic
Bacterial
Fungal
Pyruvate Kinase
Oxidative Phosphorylation
|
Infection
Inflammation/Immunology
|
Cyclamidomycin (Desdanine) is an acrylamide antibiotic with antibacterial activity. Cyclamidomycin inhibits nucleoside diphosphate kinase and pyruvate kinase (in E. coli) and oxidative phosphorylation in rat liver mitochondria. Cyclamidomycin is active against S. aureus, M. flavus, S. lutea, B. subtilis, E. coli, S. flexneri, S. typhosa, P. vulgaris, and K. pneumoniae (MICs=3.12-25 mg/ml) .
|
-
- HY-150641
-
|
CDK
Apoptosis
DNA/RNA Synthesis
Molecular Glues
|
Cancer
|
CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II .
|
-
- HY-139743
-
Aditoprim
|
Antifolate
Bacterial
|
Infection
|
Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics .
|
-
- HY-135715
-
|
PAI-1
|
Others
|
(E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM .
|
-
- HY-161762A
-
|
Influenza Virus
|
Cancer
|
(E/Z)-RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with IC50 of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner.
|
-
- HY-136567
-
|
Raf
|
Cancer
|
TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay .
|
-
- HY-162500
-
|
Fungal
|
Infection
|
Antifungal agent 99 (Compound E1) is a fungal succinate dehydrogenase (SDH) inhibitor. Antifungal agent 99 reduces mycelial density and significantly increase the mitochondrial number in mycelia cytoplasm .
|
-
- HY-147133
-
|
VEGFR
|
Cancer
|
VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
|
-
- HY-18169
-
Fab-001
|
Bacterial
|
Infection
|
MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively.
|
-
- HY-114304
-
COH000
1 Publications Verification
|
E1/E2/E3 Enzyme
|
Cancer
|
COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro .
|
-
- HY-162592
-
|
Phosphatase
|
Cancer
|
EYA2-IN-1(compound 2e) is a novel allosteric EYA2 inhibitor. EYA2-IN-1 has anti-tumor activity .
|
-
- HY-P5730
-
|
Bacterial
|
Infection
|
Peptide 5g is an antimicrobial peptide. Peptide 5g inhibits E. coli, S. aureus, and C. albicans with MIC values of 30, 10, 12.5 μg/mL respectively .
|
-
- HY-135844
-
LS-102
2 Publications Verification
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment .
|
-
- HY-157297
-
|
CDK
|
Cancer
|
CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .
|
-
- HY-168573
-
|
BCRP
|
Cancer
|
AZ99 (compound 7) is a potent ABCG2 inhibitor. AZ99 inhibits ABCG2-mediated transport of estrone-3-sulfate (E1S) into proteoliposomes and ABCG2 ATPase activity .
|
-
- HY-N10079
-
Jatrophan
|
SHP2
|
Cancer
|
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .
|
-
- HY-164152
-
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-131553R
-
|
Apoptosis
|
Cancer
|
D-α-Tocopherol Succinate (Standard) is the analytical standard of D-α-Tocopherol Succinate. This product is intended for research and analytical applications. D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer .
|
-
- HY-19717S
-
S-[(1E)-1,2-Dichloroethenyl]-L-cysteine-13C3,15N
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
DCVC- 13C3, 15N is 15N and 13C labeled DCVC. DCVC (S-[(1E)-1,2-Dichloroethenyl]-L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures .
|
-
- HY-116096
-
15(R)-Prostaglandin E1; 15-Epiprostaglandin E1
|
15-PGDH
|
Others
|
15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1) is a stereoisomer of PGE1 (HY-B0131) but with less biological activity . 15-epi-PGE1 is a non-competitive inhibitor for human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH) with an IC50 of 170 μM .
|
-
- HY-144271
-
|
Raf
|
Cancer
|
RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
|
-
- HY-146724
-
|
Histone Methyltransferase
|
Cancer
|
Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells .
|
-
- HY-164152A
-
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-172390
-
|
Bacterial
|
Infection
|
Florfenicol-propanoate-piperidin (Compound 1) is the derivative of Florfenicol (HY-B1374). Florfenicol-propanoate-piperidin exhibits antibacterial activity, inhibits E. coli ATCC25922, Salmonella CICC110420, S. aureus ATCC29213, B. subtilis CMCC(B)63501, E. faecalis ATCC29212, S. suis CVCC606, and Haemophilus parasuis with MIC of 2-8 μM .
|
-
- HY-128979
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a agent-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC .
|
-
- HY-169973
-
|
Beta-lactamase
Bacterial
|
Infection
|
PhoPS is the photocaged inhibitor for β-lactamase. PhoPS is activated upon light irradiation, and active β-lactamase inhibitor Sulbactam (HY-B0334) is released. PhoPS inhibits the synthesis of bacterial cell wall and the formation of E. coli biofilm, exhibits antimicrobial activity .
|
-
- HY-172789
-
|
mTOR
Apoptosis
|
Cancer
|
mTOR inhibitor-27 (Compound 7e) is a mammalian target of rapamycin (mTOR) inhibitor with an IC50 value of 5.47 μM. mTOR inhibitor-27 can induce tumor cell apoptosis and arrest the cell cycle in the S-phase, thereby inhibiting cancer cell growth. mTOR inhibitor-27 is promising for research of cancers, such as skin cancer .
|
-
- HY-121374
-
|
Tyrosinase
|
Infection
|
Cardanol diene is a phenol found in cashew nut shell liquid that inhibits tyrosinase with an IC50 value of 52.5 μM in vitro.1 Cardanol diene is also used to synthesize cardanol-metal complexes that inhibit uropathogenic E. coli biofilm formation.
|
-
- HY-172098
-
|
Parasite
|
Infection
|
CpNMT-IN-1 (Compound 11e) is an against N-myristoyltransferase of C. parvum (CpNMT) inhibitor with an IC50 value of 2.5 μM. CpNMT-IN-1 also inhibits the growth of C. parvum with an EC50 value of 6.9 μM .
|
-
- HY-15162
-
MMAE; SGD-1010; Vedotin
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
|
-
- HY-161427
-
|
HSP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
HSP90-IN-30 (compound 3e) inhibits HSP90 chaperone activity. HSP90-IN-30 inhibits the activity of HIF-1 transcriptional under hypoxia with an IC50 value of 2.16 μM .
|
-
- HY-110204
-
Heclin
2 Publications Verification
|
E1/E2/E3 Enzyme
Akt
MyD88
|
Others
|
Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC50 values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer .
|
-
- HY-P9934
-
C7E3
|
Integrin
|
Cardiovascular Disease
|
Abciximab (C7E3), a chimeric mouse/human monoclonal antibody fragment, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors .
|
-
- HY-161782
-
|
Amylases
|
Metabolic Disease
|
α-Amylase-IN-7 (Compound 6e) is an inhibitor for α-Amylase with an IC50 of 40 μM. α-Amylase-IN-7 exhibits potential as an antidiabetic agent .
|
-
- HY-W598456
-
|
Drug Intermediate
|
Cancer
|
Brigimadlin intermediate-1 is an intermediate of the E3 ubiquitin protein ligase MDM-2 inhibitor Brigimadlin (HY-152859) and can be used to synthesize Antibody-Drug Conjugates (ADCs) .
|
-
- HY-150977
-
-
- HY-150976
-
-
- HY-148831
-
|
Bacterial
|
Infection
|
Antibacterial agent 135 (example 7) is a potent antibacterial agent. Antibacterial agent 135 can inhibit P. aeruginosa, A. baumannii, E. coli, and K. pneumoniae, with MIC>64 μg/mL .
|
-
- HY-119749
-
|
Bacterial
|
Infection
|
Diazaborine is an inhibitor for enoyl-acyl carrier protein (enoyl ACP) in an NAD+-dependent manner. Diazaborine exhibits antibacterial activity, MIC for E. coli and K. pneumoniae is 25 and 3.12 μg/mL .
|
-
- HY-161983
-
|
Influenza Virus
|
Infection
|
Neuraminidase-IN-22 (compound 3e) is a potent, selective and orally active neuraminidase inhibitor with an IC50 value of 0.03 µM. Neuraminidase shows cytotoxicity and anti-influenza A virus activity .
|
-
- HY-N11570
-
|
Others
|
Inflammation/Immunology
|
Phaeocaulisin E (Compound 5) is a guaiane-type sesquiterpene that inhibits LPS HY-(HY-D1056)-induced NO production in RAW 264.7 macrophages with an IC50 of 10.3 μM .
|
-
- HY-W017401
-
BIT
|
Bacterial
|
Infection
Cancer
|
Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
|
-
- HY-156336
-
|
Polo-like Kinase (PLK)
|
Cancer
|
PLK1-IN-7 (compound 30e) is a potent PLK1 inhibitor, with an IC50 of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities .
|
-
- HY-128067
-
Hexamethylene amiloride; HMA
|
Sodium Channel
HIV
Apoptosis
|
Infection
Cancer
|
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively .
|
-
- HY-155507
-
|
c-Myc
|
Cancer
|
c-Myc inhibitor 11 (Compound 67e) is a c-MYC inhibitor (pEC50: 6.4). c-Myc inhibitor 11 has high clearance levels, moderate volume of distribution and short half-life in rat pharmacokinetic assay. c-Myc inhibitor 11 can be used for cancer research .
|
-
- HY-171477
-
|
Estrogen Receptor/ERR
|
Cancer
|
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
|
-
- HY-16023A
-
EM-652; SCH 57068
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
|
-
- HY-19340
-
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
|
-
- HY-153603
-
|
Raf
|
Cancer
|
B-Raf IN 15 (Compound 7) is a BRAF inhibitor. B-Raf IN 15 inhibits BRAF WT and BRAF V600E with IC50s of 2.0 and 0.8 μM. B-Raf IN 15 can be used for the research of cancer .
|
-
- HY-P10389
-
|
Bacterial
|
Infection
|
Globomycin derivative G2A (Compound G2A) is an inhibitor for lipoprotein signal peptidase II (LspA), with an IC50 of 604 nM. Globomycin derivative G2A inhibits E. coli, P. aeruginosa and A. baumannii, with MIC ranging from 12.5 to 32 μg/mL .
|
-
- HY-N14627
-
|
Bacterial
|
Infection
|
Liposidomycin A has antibacterial effect, but the antibacterial activity is weak. Liposidomycin A has strong inhibition of mycobacteria (MIC is 0.16 μg/mL). Liposidomycin A has the function of inhibiting glycopeptide biosynthesis, and can inhibit the glycopeptide biosynthesis of E.coli with an IC50 of 0.03 μg/mL .
|
-
- HY-127140
-
|
Others
|
Infection
|
Cardanol triene is a phenol found in cashew nut shell liquid that reversibly inhibits tyrosinase with an IC50 value of 40.5 μM in vitro. A mixture of cardanol mono-, di-, and triene is used to synthesize cardanol-metal complexes that inhibit uropathogenic E. coli biofilm formation.
|
-
- HY-N13710
-
|
EBV
|
Infection
Cancer
|
20-Hydroxylucidenic acid E2 is a triterpenoid compound found in Ganoderma lucidum. It exhibits significant inhibitory effects on inflammation induced by TPA (HY-18739). Additionally, 20-Hydroxylucidenic acid E2 can suppress the expression of EBV early antigen induced by TPA (HY-18739), with a IC50 of 290 mol ratio/32 pmol TPA (meaning that when the molar concentration of this compound is 290 times that of 32 pmol of TPA, it can inhibit 50% of EBV early antigen expression). Therefore, 20-Hydroxylucidenic acid E2 has potential applications in anti-inflammatory and anticancer research .
|
-
- HY-153215
-
|
Ligands for E3 Ligase
|
Cancer
|
MEL24 is an Mdm2 E3 ligase inhibitor that reduces cell survival and increases sensitivity to DNA damaging agents in a p53-dependent manner for in vitro antitumor studies .
|
-
- HY-149834
-
|
Parasite
|
Infection
|
Antileishmanial agent-18 (Compound 1e) is an antileishmanial agent. Antileishmanial agent-18 effectively inhibits growth of L. donovani promastigotes. Antileishmanial agent-18 is safe for host cells .
|
-
- HY-130223
-
11β-Dinoprostone; 11β-PGE2
|
Prostaglandin Receptor
|
Endocrinology
|
11β-Prostaglandin E2 (11β-Dinoprostone), a Prostanoid derivative, inhibits [ 3H]PGE2 binding to hypothalamic membranes in the rat with a Ki of 53.3 nM .
|
-
- HY-150250
-
|
Raf
|
Cancer
|
B-Raf IN 13 is a BRAF inhibitor with an IC50 of 3.55 nM in BRAF V600E enzyme assay. B-Raf IN 13 has anticaner effects (WO2020261156A1, Example 74) .
|
-
- HY-176184
-
-
- HY-176134
-
|
PROTACs
Ras
|
Cancer
|
RP03707 is a PROTAC based KRAS G12D degrader (Red: KRAS G12D inhibitor (HY-134813), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-159779
-
-
- HY-153444
-
|
Histone Acetyltransferase
|
Cancer
|
KAT6-IN-1 (compound E) is a potent inhibitor of histone acetyltransferases KAT6A and KAT6B. KAT6-IN-1 can be used in cancer research .
|
-
- HY-157435
-
|
E1/E2/E3 Enzyme
|
Cancer
|
PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumor effect .
|
-
- HY-147661
-
|
Antifolate
|
Infection
|
DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research .
|
-
- HY-155973
-
-
- HY-122903A
-
|
DNA/RNA Synthesis
|
Cancer
|
(-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity .
|
-
- HY-P5701
-
|
Bacterial
Fungal
|
Infection
|
EP2 is an antimicrobial peptide. EP2 has antibacterial and antifungal activities. EP2 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 11.4 μg/mL .
|
-
- HY-160702
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
DMBA-SIL-Mal-MMAE is a cytotoxin-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked DMBA-SIL-Mal .
|
-
- HY-114503A
-
|
DNA/RNA Synthesis
|
Cancer
|
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-136638
-
|
Bacterial
|
Infection
|
ML328 is a selective inhibitor of bacterial AddAB and RecBCD helicase-nucleases with IC50 values of 26 and 5.1 μM, respectively. ML328 is a gyrase inhibitor. ML328 strongly inhibits the growth of E. coli in the presence of phage. ML328 can be used for the research of bacterial infection .
|
-
- HY-10981S1
-
E7080-d5
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-13973A
-
|
GSK-3
|
Metabolic Disease
|
GSK-3 inhibitor 1 (compound core 3) is a GSK-3 inhibitor that induces stem/progenitor cell self-renewal (e.g. induces stem/progenitor cell proliferation while maintaining the ability to differentiate into tissue cells in the progeny) .
|
-
- HY-119423
-
|
MMP
|
Cancer
|
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively .
|
-
- HY-10981S
-
E7080-d4
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-125263B
-
|
Estrogen Receptor/ERR
|
Cancer
|
(R)-OP-1074 is an isomer of OP-1074 (HY-125263) and can serve as a control compound in experiments. OP-1074, a pure anti-estrogen drug, is a selective ER degrader (PA-SERD) with specific anti-estrogenic activity against ERα and ERβ, inhibiting 17β-estradiol (E2)-stimulated transcription with IC50 values of 1.6 and 3.2 nM, respectively.
|
-
- HY-150766
-
|
Bacterial
|
Infection
|
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics .
|
-
- HY-15504A
-
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-163031
-
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-B-IN-28 (compound 10e) is a potent hMAO-B inhibitor with an IC50 of 1.9±0.5 nM. MAO-B-IN-28 can be used as a candidate for neurodegenerative diseases research .
|
-
- HY-N2391
-
-
- HY-161259
-
|
JAK
|
Inflammation/Immunology
|
JAK-IN-36 (Compound 12e) is a potent and selective inhibitor of Janus Kinase 1 (JAK1) with a IC50 value of 2.2 nM. JAK-IN-36 can be used in the study of autoimmune diseases .
|
-
- HY-109080
-
HM95573; GDC-5573; RG6185
|
Raf
|
Cancer
|
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively .
|
-
- HY-162417
-
|
Herbicide
|
Others
|
PPO-IN-12 (Compound E-Ic) an inhibitor for nicotiana tabacum protoporphyrinogen IX oxidase (NtPPO), with the Ki of 3 nM. Antibacterial agent 208 exhibits a board herbicide spectrum, with good inhibitory activity against broadleaf weeds .
|
-
- HY-141432
-
Cbl-b-IN-3
|
E1/E2/E3 Enzyme
|
Cancer
|
NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research .
|
-
- HY-108697A
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
(Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM .
|
-
- HY-100566
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
SuO-Val-Cit-PAB-MMAE is a agent-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the peptide SuO-Val-Cit-PAB .
|
-
- HY-15432
-
(E/Z)-b-AP15
|
Deubiquitinase
|
Cancer
|
(E/Z)-NSC-687852 is a isomer of NSC-687852 (HY-13989). NSC687852 (b-AP15) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14 .
|
-
- HY-113113
-
13,14-Dihydroprostaglandin E1
|
Endogenous Metabolite
|
Metabolic Disease
|
13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
|
-
- HY-RI00523A
-
|
MicroRNA
|
Cancer
|
hsa-miR-302e antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-302e antagomir
hsa-miR-302e antagomir
- HY-132991
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487) .
|
-
- HY-RI03069A
-
|
MicroRNA
|
Cancer
|
mmu-miR-3473e antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-3473e antagomir
mmu-miR-3473e antagomir
- HY-161356
-
|
SARS-CoV
|
Infection
|
BPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 μM and 0.14 μM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077) .
|
-
- HY-RI00675A
-
|
MicroRNA
|
Cancer
|
hsa-miR-320e antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-320e antagomir
hsa-miR-320e antagomir
- HY-RI00848A
-
|
MicroRNA
|
Cancer
|
hsa-miR-378e antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-378e antagomir
hsa-miR-378e antagomir
- HY-W348485
-
|
mTOR
|
Cancer
|
WRX606 is an inhibitor for mTOR complex 1 (mTORC1). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 S6K1 (IC50=10 nM), and the phosphorylation of the eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50=0.27 μM) in MCF-7. WRX606 exhibits cytotoxicity to HepG2 with IC50 of 17 nM. WRX606 exhibits antitumor efficacy in mouse models .
|
-
- HY-11009
-
|
CDK
PKC
|
Cancer
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor .
|
-
- HY-100818
-
TAS-120
|
FGFR
|
Cancer
|
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
- HY-W012267
-
2-Bromo-1-(2-methoxyphenyl)ethanone
|
Bacterial
|
Infection
|
2-Bromo-2'-methoxyacetophenone is an irreversible inhibitor for MurA, that inhibits MurA in E. coli with an IC50 of 0.38 μM. 2-Bromo-2'-methoxyacetophenone can be used in antibacterial research for blocking bacterial cell wall synthesis .
|
-
- HY-14596S
-
NPI 031L-d4
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
Genistein-d4 is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis .
|
-
- HY-133980
-
|
Drug Metabolite
|
Cancer
|
O-Demethyl Lenvatinib is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-19622
-
|
PGE synthase
|
Inflammation/Immunology
|
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro .
|
-
- HY-114267
-
|
mTOR
|
Others
|
Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
|
-
- HY-131262
-
4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol
|
SARS-CoV
Toll-like Receptor (TLR)
|
Others
|
Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro .
|
-
- HY-146617
-
|
Glutaminase
Apoptosis
|
Cancer
|
GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity .
|
-
- HY-172795
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
|
-
- HY-100388R
-
|
SHP2
Reference Standards
Phosphatase
|
Cancer
|
SHP099 (Standard) is the analytical standard of SHP099. This product is intended for research and analytical applications. SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth .
|
-
- HY-173054
-
|
Bacterial
|
Infection
|
FtsZ-IN-12 (Compound 16e) is the inhibitor for filamentous temperature-sensitive mutant Z (FtsZ) that promotes the polymerization of FtsZ protein, inhibits its GTPase activity, thereby interfering with bacterial cell division process. FtsZ-IN-12 exhibits boardspectrum antibacterial activity that inhibits B. subtilis ATCC9372, B. pumilus CMCC63202, S. aureus ATCC25923, E. coli BW25113 and A. baumannii ATCC19606 with MIC of 0.062-1 μg/mL. FtsZ-IN-12 inhibits the formation of bacterial biofilms and exhibits a clearing effect on mature biofilms. FtsZ-IN-12 exhibits bactericidal activity without hemolytic toxicity to mammalian red blood cells (15 mg/kg) .
|
-
- HY-150044
-
|
DNA/RNA Synthesis
Topoisomerase
Bacterial
|
Infection
|
Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area .
|
-
- HY-13270A
-
E7010 hydrochloride
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-169226
-
|
HDAC
|
Inflammation/Immunology
|
HDAC6-IN-51 (Compound 7e) is a selective HDAC6 inhibitor with an IC50 value of 42.9 nM. HDAC6-IN-51 exhibits good anti-lung fibrosis activity .
|
-
- HY-W062696
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity .
|
-
- HY-W016867
-
|
Fungal
Bacterial
|
Infection
|
4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
|
-
- HY-162139
-
|
Bacterial
|
Inflammation/Immunology
|
Urease-IN-11 (Compound 6e) is a competitive urease inhibitor (IC50)=10.41 µM). Urease-IN-11 can be used to study diseases such as urease-related gastritis and peptic ulcer .
|
-
- HY-12529
-
|
CDK
Apoptosis
|
Cancer
|
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
|
-
- HY-15694
-
SMIP004
4 Publications Verification
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells .
|
-
- HY-109080A
-
HM95573 TFA; GDC-5573 TFA; RG6185 TFA
|
Raf
|
Cancer
|
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively .
|
-
- HY-147819
-
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity .
|
-
- HY-122985
-
|
Cholinesterase (ChE)
|
Metabolic Disease
|
Graphislactone A is an antioxidant, which is found in Cephalosporium IFB-E001 and M. olivacea. Graphislactone A inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM. Graphislactone A is promising for research of oxidative damage-initiated diseases .
|
-
- HY-169850
-
|
Drug Intermediate
|
Others
|
7,8-Dihydroxy-4H-chromen-4-one is an active small molecule, that can be used as building block for synthesis of E3 ubiquitin-protein ligase inhibitor .
|
-
- HY-103436
-
|
E1/E2/E3 Enzyme
|
Cancer
|
NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation .
|
-
- HY-N12340
-
|
Flavivirus
|
Infection
|
Wulfenioidin H (Compound 5) is a diterpenoid, exhibits activity against Zika virus (ZIKV) with an EC50 value 8.50 μM. Wulfenioidin H interferes with the replication of the ZIKV by inhibiting the expression of the ZIKV envelope (E) protein .
|
-
- HY-N7944
-
|
Others
|
Cancer
|
Eucommiol is a natural product that can be isolated from the roasted leaves of E. ulmoides. Eucommiol inhibits growth of Molt 4B cells. Eucommiol reduces spontaneous activity and increases the sleep ratio in mice .
|
-
- HY-163449
-
|
Phosphatase
|
Metabolic Disease
Cancer
|
NPP3-IN-1 (Compound 3e) is an inhibitor of phosphodiesterase/pyrophosphatase-3 (NPP3) (IC50: 0.24 μM and 1.37 μM for NPP3 and NPP1 respectively .
|
-
- HY-150557
-
|
Cytochrome P450
|
Cancer
|
CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM .
|
-
- HY-161910
-
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
SH-E4A-66 is a C 2-COUPLr (COvalent Protein Ligator) with carbazole scaffold barring heterogeneous cysteine reactive warheads (acrylamide and chloroacetamide). SH-E4A-66 is capable of coupling with EML4-ALK (EC50=1.5 μM) and inhibiting the activity of EML4-ALK kinase (IC50=2.3 μM) .
|
-
- HY-173125
-
|
PROTACs
Btk
|
Cancer
|
FDU73 is a highly effective and selective BTK PROTAC degrader with a DC50 of 2.9 nM (in JeKo-1 cells). FDU73 can inhibit the proliferation of tumor cells and exhibits anti-tumor activity . (Pink: BTK ligand-14 (HY-173126); Black: Linker (HY-168297); Blue: E3 ligase ligand 59 (HY-173378); E3 ligase ligand+Linker (HY-173127))
|
-
- HY-12473
-
|
PI3K
SARS-CoV
|
Cancer
|
Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively . Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43 .
|
-
- HY-120599
-
VERU-111; ABI-231
|
Microtubule/Tubulin
Apoptosis
HPV
|
Cancer
|
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
|
-
- HY-14596R
-
NPI 031L (Standard)
|
EGFR
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
Genistein (Standard) is the analytical standard of Genistein. This product is intended for research and analytical applications. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
|
-
- HY-118773
-
A22 hydrochloride
|
Bacterial
Antibiotic
|
Inflammation/Immunology
|
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
|
-
- HY-N14629
-
|
Bacterial
|
Infection
|
Liposidomycin C has antibacterial effect, but the antibacterial activity is weak. Liposidomycin C has strong inhibition of mycobacteria (MIC is 0.16 μg/mL). Liposidomycin C has the function of inhibiting glycopeptide biosynthesis, and can inhibit the glycopeptide biosynthesis of E.coli with an IC50 of 0.03 μg/mL .
|
-
- HY-133980A
-
|
Drug Metabolite
|
Cancer
|
O-Demethyl Lenvatinib hydrochloride is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET. Lenvatinib shows potent antitumor activities .
|
-
- HY-N3617R
-
Laricin (Standard)
|
Fungal
|
Infection
|
Coniferin (Standard) is an analytical standard for Coniferin. This product is intended for research and analytical applications. Coniferin (Laricin) is a glucoside of coniferyl alcohol. Coniferin inhibits fungal melanization. Coniferin inhibits the release of certain hormones from cells, including Prostaglandin E2 and Thromboxane B2 .
|
-
- HY-105309
-
|
DYRK
|
Cardiovascular Disease
|
GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia .
|
-
- HY-N14628
-
|
Bacterial
|
Infection
|
Liposidomycin B has antibacterial effect, but the antibacterial activity is weak. Liposidomycin B has strong inhibition of mycobacteria (MIC is 0.16 μg/mL). Liposidomycin B has the function of inhibiting glycopeptide biosynthesis, and can inhibit the glycopeptide biosynthesis of E.coli with an IC50 of 0.03 μg/mL .
|
-
- HY-158402
-
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
Anti-inflammatory agent 84 (Compound 4D) is a derivative of Coumarin (HY-N0709) with antimicrobial and anti-inflammatory activities. Anti-inflammatory agent 84 inhibits E. coli, Candida albicans, Staphylococcus aureus and methicillin-resistant S. aureus (MRSA), with MIC of 312, 156, 19 and 316 μg/mL, respectively. Anti-inflammatory agent 84 inhibits biofilm formation of S. aureus, E. coli and MRSA, with IC50 of 185, 321 and 99 μM, respectively. Anti-inflammatory agent 84 inhibits nitric oxide production in Lipopolysaccharide (HY-D1056)-stimulated RAW264.7 macrophage cell .
|
-
- HY-10981R
-
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-10981AR
-
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-148789
-
OP-1250
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
|
-
- HY-14566S
-
-
- HY-159904
-
|
Acyltransferase
|
|
ChAT IN-1 is a selective Choline Acetyltransferase (ChAT) inhibitor. It can be used to study mechanisms related to the overexpression of non-neuronal ChAT in cancers (e.g., colorectal and lung cancers) and Alzheimer’s disease (AD) .
|
-
- HY-115502
-
(E)-BCI
|
Phosphatase
|
Inflammation/Immunology
|
BCI ((E)-BCI) is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI can be used in inflammatory disease research .
|
-
- HY-14566S1
-
E2020-d5 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
|
-
- HY-115502A
-
(E)-BCI hydrochloride
|
Phosphatase
|
Inflammation/Immunology
|
BCI ((E)-BCI) hydrochloride is a DUSP6 (dual specificity phosphatase 6) inhibitor. BCI hydrochloride shows anti-inflammatory activity and decreases reactive oxygen species (ROS) production. BCI hydrochloride can be used in inflammatory disease research .
|
-
- HY-146983
-
|
Carbonic Anhydrase
|
Cancer
|
hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases .
|
-
- HY-153034
-
|
Proteasome
Phosphatase
|
Cancer
|
LONP1-IN-2 (Compound 9e) is a potent and selective LONP1 inhibitor with an IC50 value of 0.093 μM. LONP1-IN-2 can be used in research of cancer .
|
-
- HY-B0034
-
E2020
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-169334
-
|
Endogenous Metabolite
|
Metabolic Disease
|
BDK-IN-1 (compound (-)-43) is a BDK inhibitor with the IC50 of 0.23 μM and the max inhibition of 90%. BDK-IN-1 decreases the level of phospho-E1 and can be used for study of cardiometabolic diseases .
|
-
- HY-158425
-
|
Bacterial
|
Infection
|
Antimicrobial agent-31 (compound 4a) is a potent antimicrobial agent. Antimicrobial agent-31 inhibits Salmonella enterica serovar Typhimurium and E.coli with MIC values of 19.24, 11.31 µg/mL, respectively .
|
-
- HY-157311
-
|
Glycosidase
|
Cancer
|
α-Glucosidase-IN-45 (compound 11E) is an inhibitor of α-glucosidase. α-Glucosidase-IN-45 is a novel indol-fused pyrano[2,3-D]pyrimidine compound .
|
-
- HY-161352
-
|
Virus Protease
|
Infection
|
NPI52 (Compound E1) is a foot-and-mouth disease virus 3C protease (FMDV 3Cpro) inhibitor, with IC50 values of 0.05 and 0.11 µM in FRET and cell-based assay, respectively .
|
-
- HY-126681
-
NHS-VC-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
SC-VC-PAB-MMAE is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB .
|
-
- HY-162099
-
|
EGFR
|
Cancer
|
VEGFR-IN-4 (Compound 6e) is an epidermal growth factor receptor (EGFR) inhibitor. VEGFR-IN-4 has potent antiproliferative activity with an IC50 value of 24.6nM against HCC827 cells .
|
-
- HY-158399
-
|
STAT
|
Inflammation/Immunology
|
STAT6-IN-5 (compound 84) is a STAT6 inhibitor (IC50=0.24 μM), which can be used for the research of inflammatory diseases and allergic diseases (e.g. atopic dermatitis) .
|
-
- HY-172605
-
|
Steroid Sulfatase
|
Cancer
|
Steroid sulfatase-IN-9 (compound 54E) is a steroid sulfatase (STS) inhibitor with the inhibition rates of 87.03% at 10 μM. Steroid sulfatase-IN-9 shows no detectable toxic effects in zebrafish larvae model .
|
-
- HY-101445A
-
|
Tyrosinase
|
Cancer
|
(R)-Trolox is a vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM . The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM) .
|
-
- HY-B0621
-
CGA89317
|
Parasite
Caspase
Bcl-2 Family
PARP
Pyroptosis
|
Infection
|
Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
|
-
- HY-156712
-
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .
|
-
- HY-P2136
-
COG1410
2 Publications Verification
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
|
-
- HY-147416
-
BI 1029539; GS-248; OX-MPI
|
PGE synthase
|
Infection
Cancer
|
Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity .
|
-
- HY-146206
-
|
Carbonic Anhydrase
|
Cancer
|
HCAIX-IN-1 (compound 21e) is a potent and selective HCAIX inhibitor with KIs of 694.9, 126.6, 3.3, 9.8 nM for hCA I, hCA II, hCA IX, hCA XII, respectively .
|
-
- HY-137341
-
|
PROTACs
YTHDF
|
Cancer
|
SK-3-91 is a PROTAC-type multi-kinase degrader that can jointly induce the degradation of the largest number of unique kinases (more than 125 unique kinases). SK-3-91 induces protein degradation through the ubiquitin biotinylation (E-STUB) pathway. SK-3-91 degrades YTHDF2. SK-3-91 inhibits cell proliferation and induces morphological changes. (Pink: TAE648 ligand (HY-169396); Blue: E3 ligase ligand (HY-131717); Black: Linker (HY-140819). The E3 ligase ligand and linker can form a conjugate (HY-169397)) .
|
-
- HY-103019A
-
(±)-BAY-1251152; (±)-VIP152
|
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
(±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-RI03050A
-
|
MicroRNA
|
Cancer
|
mmu-miR-344e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-344e-5p antagomir
mmu-miR-344e-5p antagomir
- HY-RI03202A
-
|
MicroRNA
|
Cancer
|
mmu-miR-467e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-467e-3p antagomir
mmu-miR-467e-3p antagomir
- HY-RI01682A
-
|
MicroRNA
|
Cancer
|
hsa-miR-548e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-548e-5p antagomir
hsa-miR-548e-5p antagomir
- HY-103019
-
(+)-BAY-1251152; (+)-VIP152; (S)-Enitociclib
|
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
(+)-Enitociclib ((+)-BAY-1251152) is the enantiomer of Enitociclib (HY-103019E) with (+) optical rotation. Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-RI01681A
-
|
MicroRNA
|
Cancer
|
hsa-miR-548e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-548e-3p antagomir
hsa-miR-548e-3p antagomir
- HY-RI03049A
-
|
MicroRNA
|
Cancer
|
mmu-miR-344e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-344e-3p antagomir
mmu-miR-344e-3p antagomir
- HY-RI01594A
-
|
MicroRNA
|
Cancer
|
hsa-miR-519e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-519e-5p antagomir
hsa-miR-519e-5p antagomir
- HY-RI01572A
-
|
MicroRNA
|
Cancer
|
hsa-miR-518e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-518e-3p antagomir
hsa-miR-518e-3p antagomir
- HY-RI00009A
-
|
MicroRNA
|
Cancer
|
hsa-let-7e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-let-7e-3p antagomir
hsa-let-7e-3p antagomir
- HY-130604
-
DT2216
1 Publications Verification
|
Bcl-2 Family
PROTACs
Apoptosis
|
Cancer
|
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker) .
|
-
- HY-RI01593A
-
|
MicroRNA
|
Cancer
|
hsa-miR-519e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-519e-3p antagomir
hsa-miR-519e-3p antagomir
- HY-RI03466A
-
|
MicroRNA
|
Cancer
|
mmu-miR-669e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-669e-5p antagomir
mmu-miR-669e-5p antagomir
- HY-RI01573A
-
|
MicroRNA
|
Cancer
|
hsa-miR-518e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-518e-5p antagomir
hsa-miR-518e-5p antagomir
- HY-103019B
-
(R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152
|
Drug Isomer
CDK
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
(-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
|
-
- HY-RI03203A
-
|
MicroRNA
|
Cancer
|
mmu-miR-467e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-467e-5p antagomir
mmu-miR-467e-5p antagomir
- HY-RI00543A
-
|
MicroRNA
|
Cancer
|
hsa-miR-30e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-30e-3p antagomir
hsa-miR-30e-3p antagomir
- HY-RI01601A
-
|
MicroRNA
|
Cancer
|
hsa-miR-520e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-520e-3p antagomir
hsa-miR-520e-3p antagomir
- HY-RI03174A
-
|
MicroRNA
|
Cancer
|
mmu-miR-466e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-466e-5p antagomir
mmu-miR-466e-5p antagomir
- HY-RI03465A
-
|
MicroRNA
|
Cancer
|
mmu-miR-669e-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
mmu-miR-669e-3p antagomir
mmu-miR-669e-3p antagomir
- HY-RI00544A
-
|
MicroRNA
|
Cancer
|
hsa-miR-30e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-30e-5p antagomir
hsa-miR-30e-5p antagomir
- HY-RI01602A
-
|
MicroRNA
|
Cancer
|
hsa-miR-520e-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
|
-
hsa-miR-520e-5p antagomir
hsa-miR-520e-5p antagomir
- HY-149202
-
|
PGE synthase
|
Inflammation/Immunology
|
UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50s of 0.10 μM and 2.00 μM for inhibiting PGE2 production in human (SK-N-AS) and murine (BV2) cells, respectively .
|
-
- HY-N8382
-
|
Cytochrome P450
|
Neurological Disease
|
Chalepensin, a furanocoumarin, is a competitive CYP2A6 inhibitor. Chalepensin also inhibits human CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to different extents .
|
-
- HY-170897
-
|
CDK
|
Cancer
|
CDK2-IN-40 is a CDK2 (Cyclin dependent kinase 2) inhibitor, extracted from patent WO 2024/254245 A1 (Example 1). CDK2-IN-40 inhibits CDK2/Cyclin E1 with an IC50 of ≤ 10 nM .
|
-
- HY-170361
-
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
MTHFD2-IN-5 (Compound 16e) is a selective inhibitor for MTHFD2 with an IC50 of 66 nM. MTHFD2-IN-5 inhibits the proliferation of MOLM-14 with a GI50 of 720 nM. MTHFD2-IN-5 exhibits antitumor efficacy in mouse models .
|
-
- HY-15575
-
MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
|
-
- HY-122178
-
|
PGE synthase
|
Cardiovascular Disease
|
5-trans U-44069 is the trans isomer of the thromboxane receptor agonist U-44069 (HY-121825). 5-trans U-44069 inhibits prostaglandin E2 synthase activity .
|
-
- HY-122289
-
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
|
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
|
-
- HY-121582
-
(E)-EPH 116
|
Drug Isomer
|
Cancer
|
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer .
|
-
- HY-138067
-
|
SARS-CoV
|
Inflammation/Immunology
|
SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
|
-
- HY-125415
-
|
PGE synthase
|
Inflammation/Immunology
|
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA) .
|
-
- HY-155271
-
|
Carbonic Anhydrase
|
Others
|
hCAXII-IN-7 (compound 6e) is a hCA XII inhibitor. hCAXII-IN-7 has BBB permeability. hCAXII-IN-7 induces 786-0, SF-539 and HS 578 T cells apoptotic .
|
-
- HY-132821B
-
(R)-E2027
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine (HY-132821), is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases .
|
-
- HY-168004
-
|
Bacterial
|
Infection
|
FolB-IN-1 (Compound 3e) is an inhibitor of FolB that can suppress the activity of FolB enzyme from Mycobacterium tuberculosis (MtFolB). FolB-IN-1 exhibits antimycobacterial activity with an MIC value of 40 µg/mL (108 µM) .
|
-
- HY-164958
-
|
Cathepsin
Beta-secretase
|
Cancer
|
TB-11 is a Cathepsin D inhibitor, with IC50s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research .
|
-
- HY-155282
-
-
- HY-N10226
-
|
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
Thielavin B is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin B effectively influences the prostaglandin E2 synthesis from the endoperoxide. Thielavin B is significantly effective on carrageenan-induced oedema of rats when administered intravenously .
|
-
- HY-164980
-
|
Kinesin
|
Cancer
|
KIF18A-IN-16 (Compound 15) is a fused ring KIF18A inhibitor. KIF18A-IN-16 can be used in oncology (e.g., colon, breast, lung cancer) studies .
|
-
- HY-162635
-
|
Amylases
Glycosidase
|
Metabolic Disease
|
α-Amylase/α-Glucosidase-IN-14 (compound 6E) is an oral bioactive inhibitor of α-amylase and α-glucosidase, with the IC50s of 45.53 μM and 27.73 μM, respectively .
|
-
- HY-147841
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-19831A
-
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
(Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity .
|
-
- HY-133828
-
|
5-HT Receptor
SARS-CoV
|
Infection
|
Cinanserin (SQ 10643) is a potent and selective 5-HT2 antagonist with Ki values of 41, 3500 nM for 5-HT2, 5-HT1, respectively. Cinanserin also is a SARS-CoV 3CL pro inhibitor with an KD value of 49.4, 18.2 µM for SARS-CoV 3CL pro, HCoV-229E 3CL pro, respectively. Cinanserin reduces systemic burn edema levels .
|
-
- HY-128429
-
(E)-2-Hexenal
|
Fungal
Biochemical Assay Reagents
|
Infection
|
trans-2-Hexenal ((E)-2-Hexenal) is a volatile compound widely present in fresh plants, vegetables, and fruits, with a unique leafy aroma. trans-2-Hexenal has antifungal activity and can also inhibit the germination of soybean seeds and the growth of seedlings. In addition, trans-2-Hexenal can be used to determine low-molecular-weight carbonyl compounds that are reactive with biological nucleophiles in biological samples .
|
-
- HY-157154
-
|
SARS-CoV
|
Infection
|
MAT-POS-e194df51-1 is an orally active, non-covalent and non-peptide SARS-CoV-2 main protease (M pro) inhibitor with an IC50 value of 37nM. MAT-POS-e194df51-1 is cytotoxic with EC50 values of 64 nM and 126 nM in A549-ACE2-TMPRSS2 cells and HeLa -ACE2 cells, respectively .
|
-
- HY-16023
-
EM-652 hydrochloride; SCH 57068 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .
|
-
- HY-157145
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-69 (Compound 7E) is a non-covalent SARS-CoV-2 inhibitor with an EC50 value of 7.4 μM. SARS-CoV-2-IN-69 is a potent inhibitor of SARS-CoV-2 main protease (M pro) and a non-covalent inhibitor of papain (PL pro) .
|
-
- HY-139743R
-
|
Antifolate
Bacterial
|
Infection
|
Aditoprime (Standard) is the analytical standard of Aditoprime. This product is intended for research and analytical applications. Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics .
|
-
- HY-161958
-
|
PROTACs
Histone Acetyltransferase
|
Cancer
|
dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-associated protein (EP300), which was developed based on the crystal structure of bromodomain (BRD) inhibitors. dCE-2 is composed of E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), PROTAC Linker tert-Butyl 11-aminoundecanoate (HY-130715) (black part) and PROTAC target protein ligand EP300/CBP ligand 2 (HY-161960) (red part), of which the target protein ligand activity control is EP300/CBP ligand 1 (HY-161959), and the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C10-Boc (HY-161961) [1] .
|
-
- HY-162384
-
|
Histone Methyltransferase
|
Cancer
|
EPIC-0628 is an inhibitor of the HOTAIR-EZH2 interaction and promotes ATF3 expression. The long noncoding RNA HOTAIR has been found to regulate glioblastoma (GBM) progression and mediate DNA damage repair (DDR) by interacting with the catalytic subunit EZH2 of PRC2. EPIC-0628 also inhibits the ATF3-p38-E2F1 DDR pathway to inhibit the HR pathway and upregulates CDKN1A (p21) expression, causing cell cycle arrest. EPIC-0628 also synergizes with Temozolomide (TMZ) (HY-17364) to enhance its in vivo potency .
|
-
- HY-B0876
-
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-161513
-
|
COX
NO Synthase
|
Inflammation/Immunology
|
iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects .
|
-
- HY-169977
-
|
SARS-CoV
|
Infection
|
CKP-25 is an inhibitor for the interaction between Spike RBD-ACE2, that prevents the virus from entering the host cell, thereby reducing the replication and virus infection. CKP-25 inhibits SARS-CoV-2 with IC50 of 3.5 μM in Vero E6 cell .
|
-
- HY-163199
-
|
ASCT
mTOR
Apoptosis
Autophagy
|
Cancer
|
ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth .
|
-
- HY-B0497
-
BAY2353
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-144279
-
|
Bacterial
|
Infection
|
MsbA-IN-1 is a highly potent MsbA inhibitor with IC50 of 4 nM. MsbA-IN-1 has activity against wild-type E. coli with MIC of 79 μM. MsbA-IN-1 possesses sufficient permeability across the fully intact outer membrane of Gram-negative bacteria to inhibit MsbA .
|
-
- HY-B0497A
-
BAY2353 sodium
|
Antibiotic
STAT
Parasite
|
Infection
Cancer
|
Niclosamide (BAY2353) sodium is an orally active antihelminthic agent used in parasitic infection research . Niclosamide sodium is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide sodium has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-12418
-
E7449; 2X-121
|
PARP
|
Cancer
|
Stenoparib (E7449) is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
|
-
- HY-B0497B
-
BAY2353 monohydrate
|
STAT
Antibiotic
Parasite
|
Infection
Cancer
|
Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research . Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-141877B
-
YS43-22 (isomer)
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-161789
-
|
PROTACs
SARS-CoV
Virus Protease
|
Infection
|
PROTAC SARS-CoV-2 Mpro degrader-3 (Compound P2) exhibits antiviral activity through the degradation of the main protease (Mpro) of human coronaviruses (HCoVs) (DC50=27 μM). PROTAC SARS-CoV-2 Mpro degrader-3 inhibits the viral replication, with EC50 of 4.6 μM, 4.6 μM, and 0.71 μM, for human coronaviruses HCoV-229E, HCoV-OC43 and SARS-CoV-2, respectively. (Pink: ligand for target protein Mpro ligand 2 (HY-161791); Black: linker (HY-161792); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
|
-
- HY-Y0367R
-
|
Endogenous Metabolite
Bacterial
|
Infection
|
Maleic Acid (Standard) is the analytical standard of Maleic Acid. This product is intended for research and analytical applications. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
IC50 & Target: GAD .
In Vitro: The MICs of WT 10403S for the acids (e.g., Maleic Acid) are 34 mM, 25 mM, 31 mM and 30 mM which correspond to pH values prior to growth of 4.84, 5.14, 5.32 and 5.02 respectively. Of all compounds tested, Maleic Acid is the least inhibitory despite acting at a lower pH (4.84). The most acid resistant (10403S) and the weakest (EGD-e) strain are challenged with 8.6 mM and 4.3 mM of each organic acid at pH 3 and 3.3 respectively. On both strains, Maleic Acid is the most bactericidal .
|
-
- HY-161804
-
|
PROTACs
Dengue Virus
|
Infection
|
GNF-2-deg is a PROTAC degrader for dengue virus envelope protein (DENV E protein) with DC50 of 0.83 μM. GNF-2-deg prevents viral entry by inhibiting E-mediated membrane fusion, prevents virion production by protein degradation, and thereby exhibits antiviral activity against DENV 2 with EC90 of 3.5 μM. GNF-2-deg exhibits antiviral activity against ZIKV, JEV, WNV and YFV with EC90 of 1.96-7.79 μM. (Pink: ligand for target protein (HY-161805); Black: linker (HY-42149); Blue: ligand for E3 ligase (HY-23095))
|
-
- HY-P10257
-
|
Bacterial
|
Infection
|
KR-12 human is an active segment of LL-37, which exhibits antimicrobial activity against gram-negative bacteria. KR-12 human inhibits E. coli K-12 with MIC of 66 μM .
|
-
- HY-173467
-
|
PROTACs
c-Myc
|
Cancer
|
PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader (Red: MYC inhibitor (HY-173469), black: linker (HY-W008296), Blue: E3 ligase ligand (HY-14658)) .
|
-
- HY-B1123
-
-
- HY-N1407
-
|
Cytochrome P450
|
Inflammation/Immunology
|
Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM .
|
-
- HY-115570A
-
(Z/E)-GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
(Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM .
|
-
- HY-146068
-
|
Cathepsin
|
Neurological Disease
|
AEP-IN-1 (Compound 13e) is a CNS agent-like non-covalent inhibitor of asparagine endopeptidase (AEP), with the IC50 of 89 nM. AEP-IN-1 can be used for the research of numerous neurological diseases such as Alzheimer’s disease (AD) .
|
-
- HY-125568
-
|
MMP
|
Others
|
Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E .
|
-
- HY-156382
-
|
Akt
ERK
E1/E2/E3 Enzyme
|
Cancer
|
SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. SPOP-IN-1 leads to the accumulation of tumor suppressors PTEN and DUSP7 and decreased levels of phosphorylated AKT and ERK in clear-cell renal cell carcinoma .
|
-
- HY-N2463
-
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity .
|
-
- HY-123971
-
|
HDAC
PROTACs
|
Cancer
|
HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research .
|
-
- HY-156395
-
|
E1/E2/E3 Enzyme
|
Cancer
|
MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .
|
-
- HY-173203
-
|
CDK
|
Cancer
|
CDK2-IN-43 (Compound 3a) is a CDK2-cyclin E2 inhibitor with an IC50 value of 6.0 nM. CDK2-IN-43 can be used in the research of the anti-cancer field .
|
-
- HY-131232
-
Desmorpholinyl ABT-263-NH-Me
|
Bcl-2 Family
Ligands for Target Protein for PROTAC
|
Cancer
|
Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557) .
|
-
- HY-138075
-
|
Antibiotic
Bacterial
|
Infection
|
Obafluorin is a β-Lactone Antibiotic, that can be produced by Pseudomonas fluorescens ATCC 39502. Obafluorin exhibits antibacterial activity against a range of Gram-positive and Gram-negative bacteria. Obafluorin fully inhibits E. coli threonyl-tRNA synthetase .
|
-
- HY-N1079
-
|
Bacterial
Apoptosis
|
Infection
Cancer
|
Vitexilactone is a diterpenoid that can be isolated from the leaves of Vitex negundo L. Vitexilactone shows antimicrobial activity towards E. coli. Vitexilactone induces cell apoptosis and inhibits cell cycle of cancer cells. Vitexilactone can be used for the research of cancer .
|
-
- HY-137516A
-
|
PROTACs
Ras
|
Cancer
|
LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849 .
|
-
- HY-137772
-
|
Drug Metabolite
|
Others
|
Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM) .
|
-
- HY-106550
-
RS 84135
|
Prostaglandin Receptor
|
Endocrinology
|
Enprostil (RS 84135) is a prostaglandin E2 derivative. Enprostil can inhibit amogastrin-stimulated gastric acid secretion, as well as reducing the secretion of pepsin. Enprostil can also serve as an antiulcer agent, used for research of duodenal or gastric ulcers .
|
-
- HY-N8085
-
|
NF-κB
|
Inflammation/Immunology
|
Icariside F2 is a potent NF-κB inhibitor with an IC50 value of 16.25 μM. Icariside F2 is an aromatic glycoside isolated from the leaves of E. ulmoides Oliver. Icariside F2 has anti-inflammatory activity .
|
-
- HY-100818R
-
TAS-120 (Standard)
|
Reference Standards
FGFR
|
Cancer
|
Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
- HY-155051
-
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
Antiproliferative agent-25 (Compound 3s4) is a selective PRMT5 inhibitor (IC50: 0.11 μM). Antiproliferative agent-25 up-regulates hnRNP E1 protein level. Antiproliferative agent-25 forms H-bond interactions with SAM and E444 residue of PRMT5. Antiproliferative agent-25 has antiproliferative effects against A549 cells by inducing apoptosis and inhibiting cell migration. Antiproliferative agent-25 has high clearances with T1/2 of only 21.8 and 4.7 min in human and rat liver microsomes .
|
-
- HY-173369
-
|
MAGL
Ligands for E3 Ligase
|
Cancer
|
PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249) .
|
-
- HY-N11009
-
|
EBV
|
Infection
|
11-Oxomogroside II A1 (compound 7) is an oxidized cucurbitin. It can be isolated from the ethanol extract of Rohanberry fruit. 11-Oxomogroside II A1 inhibits the activation of Epstein-Barr virus (EBV) early antigen (EBV-EA) induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). 11-Oxomogroside II A1 also weakly inhibits the activation of (±)-(E)-methyl-2-[(E)-hydroxyimino]-5-nitro-6-methoxy-3-hexemide (NOR 1), a nitric oxide (NO) donor .
|
-
- HY-101257
-
|
CDK
|
Cancer
|
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-163206
-
|
Cathepsin
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-77 (compound 11e) is a cathepsin L and cathepsin S inhibitor with Ki values of 111 nM and 103 nM, respectively. SARS-CoV-2-IN-77 inhibits SARS-CoV-2 with an EC50 value of 38.4 nM in Calu-3 cells without showing cytotoxicity .
|
-
- HY-129531
-
|
E1/E2/E3 Enzyme
|
Neurological Disease
|
MuRF1-IN-1 is an orally active MuRF1 inhibitor. MuRF1-IN-1 can inhibit the interaction between MuRF1 and titin as well as E3 ligase activity. MuRF1-IN-1 can alleviate skeletal muscle atrophy and dysfunction in cardiac cachexia .
|
-
- HY-107411
-
(6E)-Bromoenol lactone
|
Phospholipase
|
Inflammation/Immunology
|
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx .
|
-
- HY-147980
-
|
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
Aβ-IN-5 (Compound e12) is an orally active Aβ aggregation inhibitor. Aβ-IN-5 also inhibits AChE and BuChE with IC50 values of 21.29 μM and 1.32 μM, respectively. Aβ-IN-5 shows excellent neuroprotective effects and low neurotoxicity .
|
-
- HY-B0876A
-
4-Methylpyrazole hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-149292
-
|
Casein Kinase
|
Cancer
|
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
|
-
- HY-146805
-
|
MNK
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
EB1 is the inhibitor of kinases MNK with IC50s of 0.69 μM (MNK1) and 9.4 μM (MNK2). EB1 selectively inhibits the growth of cancer cells, but not normal cells. EB1 also increases cell apoptosis and suppresses eIF4E phosphorylation .
|
-
- HY-169630
-
|
NF-κB
Prostaglandin Receptor
NO Synthase
Syk
|
Inflammation/Immunology
|
DBMB is an inhibitor of spleen tyrosine kinase (Syk), capable of significantly inhibiting the activity of Syk kinase. DBMB exhibits anti-inflammatory activity by suppressing the signaling of NF-κB, which in turn reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2). DBMB can be utilized in research on inflammatory diseases .
|
-
- HY-157996
-
|
c-Fms
|
Neurological Disease
|
CSF1R-IN-21 (compound 7e) is a CSF-1R Inhibitor with an IC50 value of 31 nM. CSF1R-IN-21 inhibits CSF-1R auto-phosphorylation and can be used for the research of neurodegenerative diseases .
|
-
- HY-149410
-
|
Topoisomerase
|
Cancer
|
MSN8C, an analog of mansonone E, is a novel catalytic inhibitor of human DNA topoisomerase II. MSN8C induces cancer cell apoptosis. MSN8C shows significant anti-tumor cell proliferation activity in vitro .
|
-
- HY-15605R
-
|
Raf
|
Cancer
|
Encorafenib (Standard) is the analytical standard of Encorafenib. This product is intended for research and analytical applications. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
- HY-147960
-
|
Glycosyltransferase
|
Infection
|
Glycosyltransferase-IN-1 (compound 5m) is a potent glycosyltransferase inhibitor, with an IC50 of 82.8 μM. Glycosyltransferase-IN-1 shows antibacterial activity, with MIC values of 6 μg/mL for MSSA, MRSA, B. subtilis and 12 μg/mL for E. coli .
|
-
- HY-172263
-
|
Antibiotic
Bacterial
|
Infection
|
KU13 is an inhibitor of nontuberculous mycobacteria (NTM). The minimum inhibitory concentrations (MIC) of KU13 against Mycobacterium and E. coli are 0.032-8 μg/mL and 2 μg/mL, respectively. KU13 can be used for research in the field of anti-infection .
|
-
- HY-N12267
-
(E/Z)-Terrestribisamide
|
Melanocortin Receptor
|
Metabolic Disease
|
N,N′-Diferuloylputrescine ((E/Z)-Terrestribisamide) is a inhibitor of pigmentation with 57% reduction. N,N′-Diferuloylputrescine significantly reduces the protein level of MITF. N,N′-Diferuloylputrescine has strong antioxidant activities as radical scavengers against reactive oxygen species .
|
-
- HY-145881
-
|
Bacterial
|
Infection
|
Elongation factor P-IN-2 is a potent inhibitor elongation factor P (EFP). Elongation factor P-IN-2 is a β-lysine derivative compound. Elongation factor P-IN-2 affects the proliferation rates of E. coli .
|
-
- HY-168172
-
|
Lactate Dehydrogenase
|
Cancer
|
LDH-IN-3 (compound E38) is an inhibitor of LDH, promising protective agent for ischemic nerve damage in the eye and brain. LDH-IN-3 acts its function via HO-1/SIRT1 pathway. .
|
-
- HY-14660R
-
|
Raf
|
Cancer
|
Dabrafenib (Standard) is the analytical standard of Dabrafenib. This product is intended for research and analytical applications. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively .
|
-
- HY-118827
-
Quadrisol; CERM 10202; PM 150
|
COX
|
Inflammation/Immunology
|
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
|
-
- HY-12057
-
Vemurafenib
Maximum Cited Publications
83 Publications Verification
PLX4032; RG7204; RO5185426
|
Raf
Autophagy
|
Cancer
|
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-160643
-
|
CDK
|
Cancer
|
CDK2-IN-27 (compound 1) is a potent CDK2 inhibitor with IC50 values of <10, >10-20 nM for CDK2/cyclin E1, CDK2/cyclin B1, respectively .
|
-
- HY-14566R
-
E2020 (free base) (Standard)
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
Donepezil (Standard) is the analytical standard of Donepezil. This product is intended for research and analytical applications. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively .
|
-
- HY-128842
-
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .
|
-
- HY-128843
-
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase .
|
-
- HY-161597
-
|
PROTACs
|
Cancer
|
PROTAC DYRK2 degrader 1 (compound CP134) is a PROTAC degrader of DYRK2 (Red: DYRK2 inhibitor(HY-161598), black: linker (HY-42776), Blue: E3 ligase ligand (HY-10984)) .
|
-
- HY-108372
-
PROTAC Linker 2
|
PROTAC Linkers
|
Cancer
|
Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
|
-
- HY-145880
-
|
Bacterial
|
Infection
|
Elongation factor P-IN-1 is a potent inhibitor elongation factor P (EFP). Elongation factor P-IN-1 is a β-lysine derivative compound. Elongation factor P-IN-1 affects the proliferation rates of E. coli .
|
-
- HY-168729
-
|
Bacterial
|
Infection
|
Antibacterial agent 256 (Compound C09) is an inhibitor for type I signal peptidase (SPase I). Antibacterial agent 256 inhibits gram-positive bacteria, that inhibits S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1 and S. suis P1/7, with MIC of 1-16 μg/mL. Antibacterial agent 256 exhibits cytotoxicity in cancer cell HEp-2 and Caco-2 with CC50 of 14.65 μg/mL and 21.93 μg/mL. Antibacterial agent 256 exhibits a hemolytic activity on mouse RBCs, with an HC50 of 13.29 μg/mL. Antibacterial agent 256 ameliorates the MRSA skin infection in mouse model .
|
-
- HY-157510
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
|
-
- HY-18099A
-
E-52862 hydrochloride
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
|
-
- HY-157511
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-O-C5-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C5-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C5-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
|
-
- HY-173081
-
|
SARS-CoV
|
Infection
|
4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin (Compound 2d) is a broad-spectrum anti-coronaviral agent via targeting frameshifting element (FSE). 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin inhibits HCoV-OC43 and HCoV-229E with EC50 values of 0.85 μM and 1.45 μM. 4"-(2-(p-Chlorophenyl)acetoxyl)spiramycin shows a dual-target mechanism that acts on both viral FSE RNA and host DIS3L2 .
|
-
- HY-169378
-
|
PROTACs
c-Myc
|
Cancer
|
CSI86 is a MYC-targeting PROTAC degrader with antiproliferative activity (IC50: 13-18 μM) . CSI86 is composed of MYC inhibitor (red part) CSI118 TFA (HY-169379), E3 ligase ligand (blue part) VH032 (HY-120217), and PROTAC linker (black part) Succinic anhydride (HY-79369). The conjugate composed of E3 ligase ligand and linker is (S,R,S)-CO-C2-acid (HY-131866).
|
-
- HY-171788
-
|
N-myristoyltransferase
|
Cancer
|
NMT-IN-8 (Compound Ex.129) is an orally active and highly selective inhibitor of N-myristoyl transferase (NMT) with an IC50 value of <10 nM. NMT-IN-8 binds to the peptide binding pocket of NMT, blocking its catalyzed protein N-myristoylation to interfere with key pathways such as protein trafficking, signal transduction, and viral replication. NMT-IN-8 is promising for research of oncology (e.g., MYC-addicted cancers, B-cell lymphoma) and infectious diseases (e.g., malaria, HIV, rhinovirus infection) .
|
-
- HY-129105
-
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
Chlormethiazole is an potent and orally active GABAA agonist . Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus .
|
-
- HY-149316
-
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension .
|
-
- HY-161419
-
|
Histone Methyltransferase
|
Cancer
|
EZH2-IN-18 (compound 9e) is a potent inhibitor of enhancer of zeste homologue 2 (EZH2 WT) , with the IC50 of 1.01 nM. EZH2-IN-18 shows inhibition in proliferation and induction in apoptosis in tumor cells .
|
-
- HY-151160
-
|
Bacterial
|
Infection
|
LasR-IN-1 (compound 9g) is a potent LasR inhibitor. LasR-IN-1 has good efficacy toward E. coli. LasR-IN-1 shows anti-bacterial activity, with a MIC of 28.13 μM against P. aeruginosa .
|
-
- HY-126686
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
Mal-Phe-C4-VC-PAB-MMAE is made by MMAE conjugated to Mal-Phe-C4-VC-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody agent conjugate.
|
-
- HY-15605S
-
LGX818-13C,d3
|
Isotope-Labeled Compounds
Raf
|
Cancer
|
Encorafenib- 13C,d3 is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E (EC50=4 nM).
|
-
- HY-106611
-
SR 33287
|
Phospholipase
|
Cancer
|
Brinazarone (SR 33287) is an inhibitor for acid lysosomal sphingomyelinase, and leads to cellular lipidosis. Brinazarone potentiates the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells .
|
-
- HY-D2336
-
|
PROTACs
|
Cancer
|
PROTAC Aster-A degrader-1 (compound NGF3) is a degrader of the sterol transport protein Aster-A. PROTAC Aster-A degrader-1 can be used as a fluorescence probe. (Red: Aster-A inhibitor, black: linker, Blue: E3 ligase ligand) .
|
-
- HY-N0153
-
Naringoside
|
Cytochrome P450
Autophagy
Mitophagy
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .
|
-
- HY-149391
-
|
PROTACs
Btk
|
Inflammation/Immunology
|
PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .
|
-
- HY-128773
-
|
Bacterial
|
Infection
|
MRL-494, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
|
-
- HY-10981S2
-
E7080-15N,d4
|
VEGFR
c-Kit
FGFR
RET
PDGFR
Isotope-Labeled Compounds
|
Cancer
|
Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities .
|
-
- HY-N3535
-
|
Prostaglandin Receptor
Lipoxygenase
|
Inflammation/Immunology
|
Canniprene, an isoprenylated bibenzyl unique to Cannabis sativa, is a potent inhibitor of 5-lipoxygenase (5-LO) activity (IC50=0.4 μM) and cyclooxygenase/microsomal prostaglandin E2 synthase (PGE2; IC50=10 μM). Canniprene inhibits the production of inflammatory eicosanoids and affects the generation of prostaglandins .
|
-
- HY-W846144
-
|
MNK
|
Cancer
|
ETP-45835 is slective and potent MNK inhibitor with IC50s of 575 nM and 646 nM for MNK1 and MNK2, respectively. ETP-45835 shows little activity against 24 other kinases. ETP-45835 inhibits eIF4E Ser209 phosphorylation in cells, and has anticancer effects .
|
-
- HY-155121
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-56 (Compound 63) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-56 has antiviral activity. SARS-CoV-2-IN-56 inhibits SARS-CoV-2 in Vero E6 cells, with an IC50 of 0.7 μM .
|
-
- HY-172870
-
-
- HY-155119
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-54 (Compound 2) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-54 has antiviral activity. SARS-CoV-2-IN-54 inhibits SARS-CoV-2 in Vero E6 cells, with an IC50 of 21.4 μM .
|
-
- HY-N0153R
-
Naringoside (Standard)
|
Endogenous Metabolite
Cytochrome P450
Mitophagy
Autophagy
|
Inflammation/Immunology
Cancer
|
Naringin is a major flavanone glycoside obtained from tomatoes, grapefruits, and many other citrus fruits. Naringin exhibits biological properties such as antioxidant, anti-inflammatory, and antiapoptotic activities. Naringin also inhibits proliferation and invasion and induces apoptosis in human osteosarcoma cells by inhibiting zinc finger E-box binding homeobox 1 (Zeb1) .
|
-
- HY-12828A
-
|
CDK
DYRK
|
Infection
Neurological Disease
|
KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM) .
|
-
- HY-155571
-
|
MDM-2/p53
IAP
|
Cancer
|
MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .
|
-
- HY-161257
-
|
Autophagy
|
Cancer
|
CDC20-IN-1 (Compound E1) is a specific inhibitor of CDC20 and can be used in triple-negative breast cancer research. CDC20-IN-1 can induce autophagy in cancer cells and inhibit MDA-MB-231 cell proliferation, with an IC50 value of 1.43 μM .
|
-
- HY-128773A
-
|
Bacterial
|
Infection
|
MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias .
|
-
- HY-B0497C
-
BAY2353 olamine
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research . Niclosamide olamin is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide olamin has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-161869
-
|
Histone Methyltransferase
|
Metabolic Disease
|
LSD1-IN-32 (compound 11e) is a potent LSD1 inhibitor with an IC50 value of 0.99 µM. LSD1-IN-32 inhibits RANKL-induced osteoclastogenesis, bone resorption and F-actin belt formation. LSD1-IN-32 has the potential for the research of osteoporosis .
|
-
- HY-155805
-
|
CDK
|
Cancer
|
CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .
|
-
- HY-101257B
-
|
CDK
|
Cancer
|
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-169869
-
|
Raf
|
Cancer
|
Pan-Raf/RTK inhibitor 1 (compound I-16) is a potent pan-Raf inhibitor with IC50 values of 3.49 nM (BRaf V600E), 8.86 nM (ARaf), 5.78 nM (BRaf WT), and 1.65 nM (CRaf). Pan-Raf/RTK inhibitor 1 exhibits antiproliferative activities against various cancer cell lines and can be utilized in cancer research .
|
-
- HY-164427
-
|
SHP2
ERK
|
Cancer
|
SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
|
-
- HY-W412264
-
|
Pim
|
Cancer
|
Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer .
|
-
- HY-173026
-
|
Herbicide
|
Others
|
Herbicidal agent 7 (Compound 15c) is the inhibitor for protoporphyrinogen IX oxidase (PPO). Herbicidal agent 7 blocks the plant pigment synthesis, exhibiting herbicidal activity against broadleaf weeds (such as Z. elegans and A. theophrasti) and grass weeds (such as S. glauca and E. crusgalli) .
|
-
- HY-156651
-
EDP-235
|
SARS-CoV
|
Infection
|
Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections .
|
-
- HY-161896
-
|
GABA Receptor
|
Neurological Disease
|
Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models .
|
-
- HY-N7148
-
D-γ-Tocopherol; (+)-γ-Tocopherol
|
COX
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity .
|
-
- HY-174263
-
|
Bacterial
|
Infection
|
PaFabV-IN-1 (Compound 3e) is a selective Pseudomonas aeruginosa enoyl-acyl carrier protein reductase (PaFabV) inhibitor with an IC50 value of 0.25 μM. PaFabV-IN-1 is promising for research of infections caused by P. aeruginosa and other Gram-negative bacteria .
|
-
- HY-163572
-
|
PI4P5K
|
Cancer
|
PIP5K1α-IN-1 (Compound 3e) is an inhibitor for phosphatidylinositol 4-phosphate 5-kinase type I α (PIP5K1α) with an IC50 of 0.46 μM .
|
-
- HY-153866
-
|
Casein Kinase
|
Cancer
|
CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
|
-
- HY-A0163CR
-
(E)-Clopenthixol dihydrochloride (Standard)
|
Antibiotic
Bacterial
Parasite
|
Infection
|
trans-Clopenthixol (dihydrochloride) (Standard) is the analytical standard of trans-Clopenthixol (dihydrochloride). This product is intended for research and analytical applications. trans-Clopenthixol ((E)-Clopenthixol) dihydrochloride is an antibiotic agent, without neuroleptic effect. trans-Clopenthixol can be used to inhibit Pseudomonas aeruginosa and Plasmodium falciparum in vitro[1][2].
|
-
- HY-152916
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
mp-dLAE-PABC-MMAE is a agent-linker conjugate for ADC. mp-dLAE-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (HY-15162). mp-dLAE-PABC-MMAE can be used to synthesis antibody-drug conjugates (ADCs) .
|
-
- HY-130794
-
-
- HY-101466A
-
|
FGFR
|
Cancer
|
E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively .
|
-
- HY-162078
-
|
Casein Kinase
|
Cancer
|
Antiproliferative agent-46 (compound 5e) is an inhibitor of the casein kinase-2 enzyme (CK2) receptor. Antiproliferative agent-46 has a potent antiproliferative activity with an IC50 value of 5.75 μM on the U87 cell line .
|
-
- HY-123575
-
|
Leukotriene Receptor
|
Inflammation/Immunology
|
LY 245769, a omega-trifluoro analog, is a leukotriene E4 (LTE4) inhibitor. LY 245769 interfers the omega-oxidation of N-acetyl-LTE4 and leukotriene B4 (LTB4) with IC50s of 4 μM .
|
-
- HY-153866A
-
|
Casein Kinase
|
Cancer
|
CK1-IN-2 (compound Nr.4) hydrochloride is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
|
-
- HY-151104
-
|
Influenza Virus
|
Infection
|
Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively .
|
-
- HY-N12339
-
|
Virus Protease
|
Infection
|
Wulfenioidin F is a diterpenoid, that can be isolated from the whole plant of Orthosiphon wulfenioides. Wulfenioidin F exhibits activity against Zika virus (ZIKV) with an EC50 of 8.07 μM. Wulfenioidin F interferes with the replication of the ZIKV by inhibiting the expression of the ZIKV envelope (E) protein .
|
-
- HY-172457
-
|
MNK
|
Cancer
|
NUCC-0200808 (Compound 12g) is an inhibitor of MNK1 with an IC50 of 42 nM. NUCC-0200808 reduces eIF4E phosphorylation and cell viability in AML cells, and induces apoptosis. NUCC-0200808 holds promise for research in the field of leukemia .
|
-
- HY-106139A
-
TBC-1269Z
|
P-selectin
|
Inflammation/Immunology
|
Bimosiamose disodium (TBC-1269Z) is a nonoligosaccharide pan-selectin inhibitor with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose disodium has anti-inflammatory effects .
|
-
- HY-152859
-
BI 907828
|
E1/E2/E3 Enzyme
MDM-2/p53
|
Cancer
|
Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research .
|
-
- HY-169007
-
|
STAT
|
Inflammation/Immunology
|
STAT3-IN-34 (Compound 15E) is an inhibitor for STAT3, and inhibits the nuclear translocation and transcriptional regulator activity of STAT3. STAT3-IN-34 inhibits the proliferation of cell HaCaT with IC50 of 0.008 μM. STAT3-IN-34 inhibits IL-17A expression and ameliorates Imiquimod (HY-B0180)-induced psoriasis in mice .
|
-
- HY-161788
-
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
DNA Gyrase-IN-11 (Compound 23Be) is an inhibitor for protein synthesis (IC50 is 0.74 μM) and DNA replication. DNA Gyrase-IN-11 inhibits DNA gyrase, that inhibits E. coli DNA supercoiling with IC50 of 11.9 μM. DNA Gyrase-IN-11 exhibits antibacterial efficacy, that inhibits Streptococcus pneumoniae, Streptococcus pyogenes, Haemophilus influenzae and Staphylococcus aureus, with MICs of 0.008-0.25 μg/mL .
|
-
- HY-131275
-
|
Drug Metabolite
|
Others
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
|
-
- HY-122903
-
|
DNA/RNA Synthesis
|
Cancer
|
TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor . TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions. TK216 blocks the binding between EWS-FLI1 and RNA helicase A. TK216 has anticancer activity .
|
-
- HY-159890
-
|
SARS-CoV
|
Infection
|
MTI013 is a selective SARS-CoV-2 nsp14 Mtase inhibitor (IC50: 2.98 μM) and an antiviral agent (IC50: 10.33 μM in HCoV-229E-infected Huh7 cells). MTI013 also shows a synergistic antiviral effect with the RdRp inhibitor SHEN26 (HY-155488) .
|
-
- HY-146061
-
|
Ras
|
Cancer
|
KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
|
-
- HY-170799
-
|
DNA/RNA Synthesis
SARS-CoV
Arenavirus
|
Infection
|
HNC-1664 is the orally active inhibitor for RNA-dependent RNA polymerase (RdRP). HNC-1664 exhibits broad-spectrum antiviral activity against coronavirus (SARS-CoV-2 wildtype and its mutants XBB.1.18, HK.3.1, BF.7.14, BA.1HCoV-229E, HCoV-OC43) and arenavirus. HNC-1664 exhibits anti-infectious activity in SARS-CoV-2 Delta infected mouse models .
|
-
- HY-157515
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide 4'-ether-PEG2-azide is a click chemistry modified cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide 4'-ether-PEG2-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkynyl groups. Thalidomide 4'-ether-PEG2-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs .
|
-
- HY-156751A
-
RO7656594
|
PROTACs
Androgen Receptor
|
Cancer
|
GDC-2992 (Compound 28A) is an orally active androgen receptor (AR) degrader. GDC-2992 degrads AR with a DC50 value of 2.7 nM and inhibits proliferation with an IC50 valude of 9.7 nM in VCaPcells. GDC-2992 can be used for prostatic cancer study. (Structure Note: Pink: target protein ligand (HY-130845); Blue: E3 ligase ligand (HY-W1003189A); Black: linker (HY-169975); E3 ligase ligand +linker (HY-169976A)) .
|
-
- HY-168274
-
|
PROTACs
Apoptosis
|
Cancer
|
PROTAC TRIB2 degrader-1 (Compound 5k) is an effective TRIB2 degrader that selectively induces TRIB2 degradation through the CRBN-dependent ubiquitin-proteasome pathway. PROTAC TRIB2 degrader-1 can inhibit cell proliferation and induce cell apoptosis, and can be used in cancer research. (Target protein ligand (Pink): HY-168275; linker (black): HY-168276; E3 Ligase Ligand-Linker Conjugates: HY-168277; E3 ligase (Blue): HY-W023573) .
|
-
- HY-W017401R
-
|
Bacterial
|
Infection
Cancer
|
Benzisothiazolone (Standard) is the analytical standard of Benzisothiazolone. This product is intended for research and analytical applications. Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
|
-
- HY-100947
-
-
- HY-169051
-
|
Sirtuin
|
Cancer
|
SIRT-IN-5 is a SIRT3 inhibitor, with an IC50 value of 2.88 μM. SIRT-IN-5 can promote the differentiation of multiple myeloma cells, along with an increase in the expression of the differentiation antigen CD49e and human immunoglobulin light chains λ and κ .
|
-
- HY-101466
-
|
FGFR
|
Cancer
|
E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively .
|
-
- HY-162387
-
-
- HY-130626
-
|
RSV
Influenza Virus
|
Infection
|
RSV/IAV-IN-1 (compound 14e) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-1 has lesser cytotoxicity than the clinical agent, Ribavirin. RSV/IAV-IN-1 has the potential for the research of RSV and/or IAV infections .
|
-
- HY-163864
-
|
PROTACs
|
Cancer
|
SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of SMARCA with DC50<100nM (red: SMARCA inhibitor, black: linker (HY-Y1215), blue: E3 ligase ligand (HY-163927) ) .
|
-
- HY-168648
-
|
Bacterial
Fungal
Dihydrofolate reductase (DHFR)
|
Infection
|
DNA Gyrase/DHFR-IN-1 is a dual inhibitor of bacterial DNA gyrase and DHFR, with IC50s of 182 μM and 3.90 μM for E. coli DNA gyrase and DHFR respectively. DNA Gyrase/DHFR-IN-1 has bactericidal and antifungal activity .
|
-
- HY-137309
-
|
HIV
|
Others
|
4-Deoxy-4α-phorbol is a tetracyclic diterpene found in E. desmondi. It has been used in the semisynthesis of inhibitors of the HIV-1-induced cytopathic effect on MT-4 cells and 4α-phorbol esters .
|
-
- HY-N3344
-
|
Fungal
|
Others
|
Macrocarpal C can be isolated from the 95 % ethanol extract of fresh leaves of E. globulus. Macrocarpal C inhibits the growth of T. mentagrophytes via an increase in the permeability of the fungal membrane. Macrocarpal C increases the production of intracellular ROS and? induces apoptosis as a consequence of DNA fragmentation .
|
-
- HY-101445G
-
|
Reactive Oxygen Species
Ferroptosis
Apoptosis
|
Cancer
|
Trolox (GMP) is Trolox (HY-101445) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Trolox is an analogue of vitamin E with a powerful antioxidant effect. Trolox is also a powerful inhibitor of membrane damage .
|
-
- HY-173411
-
|
Glycosidase
SARS-CoV
|
Infection
Inflammation/Immunology
|
DNJ-20 is an α-glucosidase inhibitor (IC50: 55.3 μg/mL). DNJ-20 has broad-spectrum anti-SARS-CoV-2 activity. DNJ-20 inhibits the correct processing of viral glycoproteins by interfering with the endoplasmic reticulum-associated glycoprotein folding process (ERQC), thereby blocking the formation and infection of viral particles. DNJ-20 has IC50 values up to 1.49 uM against several SARS-CoV-2 variants, as well as HCoV-229E and HCoV-0C43。DNJ-20 can be used for pan-coronavirus research .
|
-
- HY-170524
-
|
SARS-CoV
DNA Methyltransferase
|
Infection
|
TDI-015051 is an orally active inhibitor for SARS-CoV-2 nonstructural protein 14 (NSP14) with an IC50 ≤0.15 nM. TDI-015051 inhibits SARS-CoV-2 NSP14 in Huh-7.5 cell (EC50=11.4 nM) and in ACE2-TMPRSS2 expressing A549 cell (EC50=64.7 nM). TDI-015051 also inhibits other coronaviruses like α-hCoV-NL63, α-hCoV-229E and β-hCoV-MERS with IC50s of 1.7, 2.6 and 3.6 nM, respectively. TDI-015051 binds to the SAH-stabilized cap binding pocket, inhibits viral RNA methylation and viral replication, and exhibits anti-infectious activity in mouse models .
|
-
- HY-133680
-
|
Tyrosinase
|
Others
|
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-B0034S
-
E2020-d5
|
Cholinesterase (ChE)
|
Neurological Disease
|
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-N3513
-
Kuwanon C
|
OAT
|
Cardiovascular Disease
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8?±1.5 μM.
|
-
- HY-131717A
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
Thalidomide-NH-CH2-COOH TFA is a ligand-linker conjugate for the E3 ligase Cereblon (CRBN). Thalidomide-NH-CH2-COOH TFA can be conjugated to multi-targeted kinase inhibitors to transform them into selective degraders .
|
-
- HY-170803
-
|
Bacterial
|
Infection
|
KPC-IN-1 (compound 1e) is an inhibitor of Klebsiella pneumoniae carbapenemase KPC-2 (IC50=8.3 nM). KPC is a β-lactamase expressed in Gram-negative bacteria that hydrolyzes carbapenems. KPC causes significant bacterial resistance to carbapenem antibiotics .
|
-
- HY-147818
-
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
DNA Gyrase-IN-2 (Compound 22a) is a bacterial DNA gyrase B inhibitor with IC50s of 3.29-10.49 and 4.41-5.61 µM for E. coli DNA gyrase and M. tuberculosis DNA gyrase. Anti-tubercular and antibacterial activity .
|
-
- HY-B0034S1
-
E2020-d4
|
Cholinesterase (ChE)
|
Neurological Disease
|
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-162678
-
|
HDAC
|
Neurological Disease
|
HDAC-IN-75 (5d) is a HDAC inhibitor, with IC50 values of 6.32 nM and 1352 nM for HDAC6 and HDAC1, respectively. HDAC-IN-75 (5d) promotes vision rescue in the atp6v0e1 –/– zebrafish model of photoreceptor dysfunction .
|
-
- HY-170957
-
-
- HY-158335
-
|
Parasite
|
Infection
|
DXR-IN-1 (Compound 13E) is an inhibitor of 1-deoxy-D-ketose 5-phosphate reductoisomerase (DXR). DXR-IN-1 is highly selective for P. falciparum DXR (IC50=0.030 μM). DXR-IN-1 inhibits the growth of P. falciparum by binding to the active site of DXR and blocking its catalytic activity .
|
-
- HY-18299A
-
NG-60
|
CDK
Autophagy
Apoptosis
|
Cancer
|
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
|
-
- HY-156325
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-62 (Compound R3b) is an inhibitor of SARS-CoV-2 replication and has low cytotoxicity. SARS-CoV-2-IN-62 inhibits viral replication in Vero E6 cells and Calu-3 cells, with EC50 values of 2.97 μM and 3.82 μM, respectively .
|
-
- HY-173406
-
|
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
RSK-IN-2 (Compound 3e) is a RSK inhibitor, with IC50 s of 37.89 nM (RSK2), 30.78 nM (RSK1), 20.51 nM (RSK3), 91.28 nM (RSK4). RSK-IN-2 inhibits tumor cell proliferation, induces apoptosis and causes cell cycle arrest in the G2/M phase .
|
-
- HY-161770
-
|
Ligands for E3 Ligase
|
Cancer
|
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-172959
-
|
Mitochondrial Metabolism
|
Cardiovascular Disease
|
mPTP-IN-1 (Compound 14e) is a mitochondrial permeability transition pore (mPTP) inhibitor. mPTP-IN-1 blocks calcium-induced mPTP opening by targeting the C subunit of ATP synthase. mPTP-IN-1 can be used to study myocardial ischemia/reperfusion injury (IRI) .
|
-
- HY-146133
-
|
Bacterial
Antibiotic
|
Infection
|
LA-Bac8c is a Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties. LA-Bac8c inhibits S. aureus, MRSA, S. epidermidis, E. coli, and P. aeruginosa with MICs of 1, 4, 8, 8, and 8 μg/mL .
|
-
- HY-162595
-
|
Bacterial
|
Infection
|
BDM88855 is an allosteric inhibitor for the homolog AcrB protein. BDM88855 can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- HY-18629A
-
|
Apoptosis
CDK
Autophagy
|
Cancer
|
(E/Z)-SU9516 is the isomer of SU9516 (HY-18629). SU9516 is a potent CDK2 inhibitor,with an IC50 of 22 nM,and also shows inhibitory effects on CDK1 and CDK4,with IC50s of 40,200 nM,respectively.
|
-
- HY-100859
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1 .
|
-
- HY-162595A
-
|
Bacterial
|
Infection
|
BDM88855 hydrochloride is an allosteric inhibitor for the homolog AcrB protein. BDM88855 hydrochloride can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- HY-147286A
-
-
- HY-146541
-
|
FGFR
|
Cancer
|
FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3 .
|
-
- HY-161294
-
|
COX
|
Cancer
|
COX-2-IN-41 (compound 5e) is a selective inhibitor of COX-2 (IC50=1.74 μM). Compared with COX-1, the selectivity IC50 (COX-1)/IC50(COX-2) =16.32 .
|
-
- HY-117556
-
|
HIV
|
Infection
|
U-104489 is a HIV-1 inhibitor with the Ki values of 0.13, 0.12 and > 100 μM aganist HIV-1 RT p66/p51 wild type (G190), G190A and G190E, respectively .
|
-
- HY-15460
-
|
Bacterial
Antibiotic
|
Infection
|
CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-139909
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
CL2E-SN-38, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor .
|
-
- HY-100507
-
-
- HY-155072
-
|
PROTACs
Btk
|
Cancer
|
PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research (Blue: E3 ligand (HY-W440230), Black: linker HY-168297;Pink:BKT inhibitor (HY-150898)) 1.
|
-
- HY-173422
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .
|
-
- HY-153221
-
|
CDK
|
Cancer
|
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC50 values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .
|
-
- HY-149398
-
|
Apoptosis
PARP
CDK
|
Cancer
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
- HY-149380
-
|
Raf
|
Cancer
|
Vem-L-Cy5 (compound 3),modified with the NIR fluorophore cyanine-5 (Cy5),is a Vemurafenib (HY-12057)-based inhibitor of BRAF. Vem-L-Cy5 targets to BRAF V600E,and also inhibits MEK phosphorylation. Vem-L-Cy5 has cell permeability,and inhibits cell growth of many types of cancer .
|
-
- HY-124371
-
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects .
|
-
- HY-129389
-
|
Glycosyltransferase
|
Cancer
|
Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation .
|
-
- HY-110354
-
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Infection
Cancer
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-144122
-
|
HIV
|
Infection
|
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
|
-
- HY-150825
-
|
IAP
Ligands for E3 Ligase
|
Cancer
|
CST530 is an inhibitor of apoptosis protein (IAP) antagonist. CST530 is an IAP-type Ligands for E3 Ligase. CST530 binds to the BIR3 domain of IAP and interferes with its function, thereby promoting the ubiquitination and degradation of cIAP1. CST530 can be used to prepare PROTACs .
|
-
- HY-12057S1
-
PLX4032-d7; RG7204-d7; RO5185426-d7
|
Isotope-Labeled Compounds
Raf
Autophagy
|
Cancer
|
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-169065
-
|
Bacterial
|
Infection
|
Antibacterial agent 241 is a histidine kinase (HK) inhibitor, with IC50 values of 14 μM and 238 μM for CckA and PhoQ, respectively. Antibacterial agent 241 shows moderate antibacterial activity against E. coli DC2, Bacillus cereus, and Bacillus subtilis, with a MIC range of 12-74 μg/mL .
|
-
- HY-161998
-
|
Bacterial
Urease
|
Others
|
Urease-IN-16 (compound 4e) is a urease inhibitor, with an IC50 value of 132 μmol/L. Urease-IN-16 can coordinate with the nickel atom through the oxygen atoms of carbonyl or boronic acid groups. Urease-IN-16 shows great potential as an additive in the development of efficient fertilizers and medical applications .
|
-
- HY-161465
-
|
HDAC
|
Inflammation/Immunology
|
HDAC8-IN-7 (H7E), a HDAC8 inhibitor, exerts retinoprotective effects against glaucomatous injury via ameliorating aberrant Müller glia activation and oxidative stress. HDAC8-IN-7 alleviates functional and structural defects within the inner retina .
|
-
- HY-169410
-
|
SARS-CoV
Virus Protease
|
Infection
|
3CLPro-IN-3 (Compound A36) is an inhibitor for SARS-CoV-2 3CLpro with IC50 of 51.3 nM. 3CLPro-IN-3 exhibits antiviral activity against human coronavirus 229E, OC43 and mouse hepatitis virus MHV .
|
-
- HY-12057S
-
|
Isotope-Labeled Compounds
Raf
Autophagy
|
Cancer
|
Vemurafenib-d5 is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-158308
-
|
HDAC
|
Cancer
|
HDAC6-IN-41 (Compound E24) is a selective inhibitor for histone deacetylase 6 (HDAC6), with IC50 of 14 and 422 nM, for HDAC6 and HDAC8, respectively. HDAC6-IN-41 upregulates the acetylation of α-tubulin and histone site SMC3 .
|
-
- HY-158321
-
|
Fungal
Succinate Dehydrogenase
|
Infection
|
SDH-IN-15 (Compound 5e) is an inhibitor of succinate dehydrogenase (SDH) (IC50=2.04 μM). SDH-IN-15 has significant antifungal activity. SDH-IN-15 blocks the mitochondrial respiratory chain of the fungus through inhibition of SDH, resulting in fungal death .
|
-
- HY-P99205
-
|
ADC Antibody
|
Cancer
|
Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity .
|
-
- HY-P5702
-
|
Bacterial
Apoptosis
Fungal
|
Infection
|
EP3 is an antimicrobial peptide. EP3 has antibacterial and antifungal activities. EP3 inhibits E. gallinarum, P. pyocyanea, A. baumanii, K. terrigena with a MIC value of 12.85 μg/mL. EP3 also shows antitumor activity against cancer cells, and induces cell apoptosis .
|
-
- HY-163722
-
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
EGFR/DHFR-IN-1 (Compound 10e) is a dual inhibitor of EGFR and DHFR with IC50s of 0.151 and 0.541 µM, respectively. EGFR/DHFR-IN-1 arrests the cell cycle at both G0-G1 and S phases .
|
-
- HY-125176
-
G907
1 Publications Verification
|
Bacterial
|
Infection
|
G907 is a selective antagonist of ATP-binding cassette (ABC) transporter MsbA with anti-microbial activity. G907 inhibits E. coli MsbA with an IC50 value of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket .
|
-
- HY-139909A
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor .
|
-
- HY-126298
-
|
Raf
|
Cancer
|
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively .
|
-
- HY-172318
-
|
NKCC
|
Neurological Disease
|
IAMA-6 is a selective NKCC1 inhibitor with neuroprotective effects. IAMA-6 can be used for the study of brain conditions, including drug-resistant epilepsy (e.g. temporal lobe epilepsy (TLE) and Dravet syndrome (DrS)), autism spectrum disorders (ASD) and Down syndrome (DoS) .
|
-
- HY-P991330
-
|
CD73
|
Cancer
|
BMS-986179 is a human monoclonal antibody (mAb) targeting NT5E/CD73. BMS-986179 inhibits CD73 enzymatic activity in tumor vasculature and tumor cells. BMS-986179 can be used in advanced solid tumors research .
|
-
- HY-10929
-
UNC0224
2 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .
|
-
- HY-N12763
-
SNH
|
Bacterial
Renin
|
Inflammation/Immunology
|
Sodium new houttuyfonate (SNH) is a partially reversible NDM-1 inhibitor with an IC50 of 14.2 μM. Sodium new houttuyfonate is an inhibitor against renin and angiotensin I converting enzyme (ACE). Sodium new houttuyfonate can recover the antibacterial activity of Meropenem (HY-13678) against E. coli BL21/pET15b-blaNDM-1 .
|
-
- HY-149881
-
|
Bacterial
|
Infection
|
Quorum sensing-IN-2 (compound 23e) is a quorum sensing inhibitor, which can reduce the pathogenicity of bacteria without affecting bacterial growth. Quorum sensing-IN-2 inhibits bacterial infections with little hemolytic activity. Quorum sensing-IN-2 shows synergistic effect with Ciprofloxacin (HY-B0356) in the bacteremia model infected with P. aeruginosa PAO1 .
|
-
- HY-B0497R
-
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide (Standard) is the analytical standard of Niclosamide. This product is intended for research and analytical applications. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-B0497BS
-
BAY2353-13C6 monohydrate
|
STAT
Parasite
Antibiotic
|
Cancer
|
Niclosamide- 13C6 (monohydrate) is the 13C labeled Niclosamide monohydrate . Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research . Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells .
|
-
- HY-117273
-
|
Raf
Autophagy
|
Cancer
|
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
|
-
- HY-N12563
-
|
c-Myc
Apoptosis
|
Cancer
|
γ-Sitosterol is an inhibitor for c-Myc. γ-Sitosterol inhibits the proliferation of cancer cell MCF-7 and A549 with IC50 of 240.73 μg/mL and 696.6 μg/mL, arrests the cell cycle at G2/M phase, and induces apoptosis. γ-Sitosterol upregulates the expression of cell cycle regulators cyclin B/E .
|
-
- HY-B0876R
-
|
Cytochrome P450
|
Metabolic Disease
|
Fomepizole (Standard) is the analytical standard of Fomepizole. This product is intended for research and analytical applications. Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning .
|
-
- HY-123967
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research .
|
-
- HY-136439
-
|
Bacterial
Antibiotic
Apoptosis
|
Infection
|
4-Epianhydrotetracycline hydrochloride is a major intermediate product of Tetracycline (HY-A0107). 4-Epianhydrotetracycline hydrochloride shows lethal effects and induces cell apoptosis of zebrafish embryos. 4-Epianhydrotetracycline hydrochloride inhibits Shewanella, E. coli and P. aeruginosa with MIC values of 2, 1 and 64 mg/L, respectively .
|
-
- HY-B0621R
-
|
Parasite
Caspase
Bcl-2 Family
PARP
Pyroptosis
|
Infection
|
Triclabendazole (Standard) is the analytical standard of Triclabendazole. This product is intended for research and analytical applications. Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
|
-
- HY-118827S
-
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
Vedaprofen-d3 is the deuterium labeled Vedaprofen. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
|
-
- HY-B0034R
-
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
Donepezil (Hydrochloride) (Standard) is the analytical standard of Donepezil (Hydrochloride). This product is intended for research and analytical applications. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-150774
-
|
HDAC
HSP
Apoptosis
|
Cancer
|
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer .
|
-
- HY-114737
-
|
Bacterial
|
Infection
|
L-573655 is a reversible inhibitor of UDP-3-O-[R-3-hydroxymyristoyl]-GlcNAc deacetylase with an IC50 value of 8.5 μM. L-573655 possesses antibacterial activity against a wild-type strain of E. coli. with MIC values of 200-400 μg/mL .
|
-
- HY-15575S
-
MC-Val-Cit-PAB-MMAE-d8; mc-vc-PAB-MMAE-d8
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
VcMMAE-d8 is an isotope of VcMMAE (HY-15575). VcMMAE-d8 is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc) .
|
-
- HY-122958
-
|
α-synuclein
|
Neurological Disease
|
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research .
|
-
- HY-113758
-
|
Leukotriene Receptor
|
Inflammation/Immunology
|
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4 .
|
-
- HY-163437
-
|
Bacterial
Fungal
|
Infection
|
Antitubercular agent-45 (Compound 5g) is an antifungal and antitubercular agent. Antitubercular agent-45 inhibits S. aureus, MRSA, B. subtilis, E. coli, C. albicans with MIC values of 6.4, 10.8, 6.1, 8.4 , 8.1 μM respectively .
|
-
- HY-153608
-
|
Histone Demethylase
|
Cancer
|
JHDM-IN-1 (Compound 1) is a Jumonji C domain-containing HDMs (JHDM) inhibitor with IC50s of 3.4, 4.3, 5.9, 10 and 43 μM against JMJD2C, JMJD2A, JMJD2E, PHF8 and JMJD3, respectively .
|
-
- HY-158551
-
|
PROTACs
Bcl-2 Family
|
Cancer
|
PROTAC BcI-2/BcI-xI Degrader-1 (15) is a PROTAC based BcI-2/BcI-xI degrader (Red: BcI-2/BcI-xI inhibitor (HY-158677), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-146371
-
|
COX
|
Inflammation/Immunology
|
COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study .
|
-
- HY-125660
-
|
E1/E2/E3 Enzyme
MDM-2/p53
|
Infection
|
Leucettamol A is an inhibitor of Ubc13 (ubiquitin E2 enzyme)-Uev1A interaction, with an IC50 of 50 μg/mL. Leucettamol A can potentially activate the expression of cancer suppressor p53 and is a precursor of anticancer agents. Leucettamol A can be isolated from a marine sponge, Leucetta aff. Microrhaphis .
|
-
- HY-10014
-
R547
2 Publications Verification
|
CDK
GSK-3
Apoptosis
|
Cancer
|
R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-168901
-
|
Src
|
Cancer
|
Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC50 values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity .
|
-
- HY-143289
-
|
NTPDase
|
Cardiovascular Disease
Cancer
|
NTPDase-IN-3 (Compound 5e) is a NTPDase inhibitor, with IC50 values of: 0.38 μM (NTPDase3), 0.05 μM (NTPDase8), 0.21 μM (NTPDase1), and 1.07 μM (NTPDase2). NTPDase-IN-3 can be used in the research of cancers and thrombosis .
|
-
- HY-124819
-
|
Bacterial
|
Infection
|
D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively . D13-9001 exhibits antibiotic activities .
|
-
- HY-161275
-
|
EGFR
|
Cancer
|
BI-4732 a potent inhibitor EGFR-activating (E19del and L858R) and T790M mutations, with high blood-brian barrier penetration, targeting a broad range of EGFR mutations, including C797S. BI-4732 has anti-tumor activity .
|
-
- HY-78738G
-
|
ADC Linker
|
Cancer
|
MC-Val-Cit-PAB GMP is a GMP grade MC-Val-Cit-PAB (HY-78738). MC-Val-Cit-PAB is an intermediate in the synthesis of VcMMAE (HY-15575), which is a Drug-Linker Conjugates for ADC. Monomethyl auristatin E can be used to inhibit Microtubule/Tubulin as ADC Cytotoxin.
|
-
- HY-W458364
-
1-(Isothiazol-3-yl)ethanone
|
Cytochrome P450
|
Inflammation/Immunology
|
1-(Isothiazol-3-yl)ethan-1-one (Q11) is a CYP2E1 inhibitor. 1-(Isothiazol-3-yl)ethan-1-one can be used in rheumatoid arthritis and sepsis related research .
|
-
- HY-156169
-
|
Carbonic Anhydrase
|
Cancer
|
hCAIX/XII-IN-7 (compound 3e) is a potent hCA IX and XII inhibitor with Kis of 3.2 nM, 9.2 nM, 503.7 nM and 59 nM for hCA I, hCA II, hCA IX and hCA XII, respectively. hCAIX/XII-IN-7 has the potential for hypoxic tumors research .
|
-
- HY-111260
-
|
CDK
GSK-3
Apoptosis
|
Cancer
|
R547 mesylate is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively .
|
-
- HY-109785A
-
|
Bacterial
|
Infection
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-107779
-
|
Raf
|
Cancer
|
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
|
-
- HY-150331
-
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
DNA ligase-IN-2 (compound 2) is a potent LigA inhibitor and inhibits the DNA-independent autoadenylation activity of both full-length LigA and a truncated enzyme, LigA:AD (IC50=29 nM). DNA ligase-IN-2 effectively inhibits the growth of Staphylococcus aureus in vitro, with MIC valuse of 1, 1, and >64 μg/mL for S. aureus ATCC 29213, S. aureus ATCC 700699 and E. coli ATCC 25922, respectively .
|
-
- HY-168893
-
|
Src
Apoptosis
IAP
Survivin
Akt
mTOR
JAK
STAT
Ras
p38 MAPK
|
Cancer
|
K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer .
|
-
- HY-N8301
-
LL-Z 1272ζ
|
Bacterial
|
Infection
|
Ilicicolin F is a fungal metabolite that has been found in Fusarium and has diverse biological activities. It inhibits T. vivax alternative oxidase and the E. coli ubiquinol oxidase cytochrome bo (IC50s=0.43 and 0.37 μM, respectively) but not the E. coli ubiquinol oxidase cytochrome bd (IC50=85 μM).2 Ilicicolin F is active against the fungi A. fumigatus and C. albicans (MICs=1.66-3.33 and 6.66-13.33 μg/mL, respectively). It is cytotoxic to HeLa cells with an EC50 value of 0.003 μg/mL.
|
-
- HY-128429S
-
(E)-2-Hexenal-d2-1
|
Isotope-Labeled Compounds
Fungal
Biochemical Assay Reagents
|
Infection
|
trans-2-Hexenal-d2-1 is the deuterium labeled trans-2-Hexenal (HY-128429). trans-2-Hexenal ((E)-2-Hexenal) is a volatile compound widely present in fresh plants, vegetables, and fruits, with a unique leafy aroma. trans-2-Hexenal has antifungal activity and can also inhibit the germination of soybean seeds and the growth of seedlings. In addition, trans-2-Hexenal can be used to determine low-molecular-weight carbonyl compounds that are reactive with biological nucleophiles in biological samples .
|
-
- HY-170669
-
|
PROTACs
CRM1
Apoptosis
NF-κB
|
Cancer
|
PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) .
|
-
- HY-12678S1
-
NMS-E628-d8; RXDX-101-d8
|
Isotope-Labeled Compounds
Autophagy
Anaplastic lymphoma kinase (ALK)
Trk Receptor
ROS Kinase
|
Cancer
|
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
|
-
- HY-155007
-
|
Bacterial
|
Infection
|
DNA gyrase B-IN-2 (Compound E) is a 2-aminobenzothiazole-based DNA gyrase B inhibitor with promising activity against ESKAPE bacterial pathogens. DNA gyrase B-IN-2 showed low nanomolar inhibition of DNA gyrase (IC50 < 10 nM) and broad-spectrum antibacterial activity against pathogens belonging to the ESKAPE group, with the minimum inhibitory concentration < 0.03 μg/mL for most Gram-positive strains and 4–16 μg/mL against Gram-negative E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae.DNA gyrase B-IN-2 can be used for the research of infection .
|
-
- HY-117068S
-
(R,E)-Bromoenol lactone-d7
|
Isotope-Labeled Compounds
Phospholipase
|
Others
|
(R)-Bromoenol lactone-d7 ((R,E)-Bromoenol lactone-d7) is deuterium labeled (R)-Bromoenol lactone. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). (R)-BEL inhibits human recombinant iPLA2γ with an IC50 of approximately 0.6 μM .
|
-
- HY-168923
-
|
Enterovirus
|
Infection
|
HR-568 exhibits broad-spectrum anti-enterovirus activity. HR-568 inhibits enterovirus species EV-A71, E30 and CVA24 in cell MRC-5 with EC50 of 1.53 μM, 0.4 μM and 1.22 μM. HR-568 targets hydrophobic canyon pocket on the enterovirus capsid protein, and inhibits the virus replication .
|
-
- HY-172215
-
|
Herbicide
Protoporphyrinogen IX oxidase
|
Others
|
PPO-IN-18 (Compound g13) is the inhibitor for protoporphyrinogen oxidase (PPO) that inhibits Echinochloa crus-galli PPO (EcPPO) with an IC50 of 0.109 μM. PPO-IN-18 exhibits herbicidal effect against E. crus-galli, Digitaria sanguinalis, Setaria faberi, Ipomoea nil, Chenopodium quinoa, and Abutilon theophrasti, without significant toxicity in crops (150-300 g ai/ha) .
|
-
- HY-115959
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
Anticancer agent 34 (compound 9), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 34 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/ml. Anticancer agent 34 inhibits A549, PC3 cell growth with IC50s of 8.4 µg/ml, 7.8 µg/ml, respectively .
|
-
- HY-155477
-
|
E1/E2/E3 Enzyme
|
Cancer
|
Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM .
|
-
- HY-162362
-
|
PROTACs
GLP Receptor
|
Cancer
|
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .
|
-
- HY-115961
-
|
Bacterial
|
Inflammation/Immunology
Cancer
|
Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively .
|
-
- HY-147513
-
|
Akt
Apoptosis
|
Cancer
|
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .
|
-
- HY-168960
-
|
Reactive Oxygen Species
Bacterial
|
Infection
|
ROS inducer 8 (Compound 11g) is the inhibitor for glutathione (GSH), that induces the ROS accumulation in Enterococcus faecalis, thereby exhibiting antibacterial activity. ROS inducer 8 disrupts the biofilm, inhibits S. aureus and E. faecalis with MIC of 8 μg/mL and 2 μg/mL, exhibits post-antibiotic effect. ROS inducer 8 exhibits low hemolytic toxicity to sheep erythrocytes (HC50 > 1280 μg/mL) .
|
-
- HY-112847B
-
(E/Z)-Sulfo-N-succinimidyl oleate sodium
|
Mitophagy
|
Inflammation/Immunology
|
(E/Z)-Sulfosuccinimidyl oleate sodium is a racemic compound of (Z)-Sulfosuccinimidyl oleate sodium and (Z)-Sulfosuccinimidyl oleate sodium isomers. Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate sodium has anti-inflammatory effect .
|
-
- HY-172462
-
|
Bacterial
|
Infection
|
Mtb-IN-11 (Compound 1e) is an inhibitor of Mycobacterium tuberculosis salicylate synthase (MbtI), with an IC50 of 11.2 μM. Mtb-IN-11 exhibits good in vitro anti-tuberculosis activity, with a MIC99 of 32 μM against M. bovis BCG. Mtb-IN-11 can be used for the research of tuberculosis .
|
-
- HY-167114
-
|
Aurora Kinase
PKC
|
Cancer
|
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo .
|
-
- HY-151168
-
|
β-glucuronidase
Bacterial
|
Inflammation/Immunology
Cancer
|
3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 μM, an Ki value of 0.58 μM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies .
|
-
- HY-128382
-
E 151
|
Enterovirus
|
Infection
|
Brilliant black BN (E151) is an azo dye and a food colorant . Brilliant black BN is a promising antiviral agent against EV71 infection via inhibiting the interaction between EV71 and its cellular uncoating factor cyclophilin A. Brilliant black BN has the potential for the investigation of contagious disease .
|
-
- HY-N7626
-
|
Fungal
Glycosidase
|
Infection
|
Eleutherol is a naphthalene isolated from E. americana with antifungal activities . Eleutherol is against yeasts Candida albicans, C. tropicalis, Saccharomyces cerevisiae and Cryptococcus neoformans with MIC values between 7.8 µg/mL and 250 µg/mL . Eleutherol inhibits α-glucosidase function with an IC50>1.00 mM .
|
-
- HY-17531
-
|
Herbicide
|
Others
|
Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations . Pyraclonil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-160456
-
|
FABP
|
Metabolic Disease
|
FABP4/5-IN-4 (compound E1) is a potent inhibitor of FABP4 and FABP5, with the IC50s of 3.78 μM and 5.72 μM, respectively. FABP4/5-IN-4 plays an important role in metabolism disorder like diabetes mellitus .
|
-
- HY-N2106
-
|
NF-κB
COX
PGE synthase
NO Synthase
|
Inflammation/Immunology
|
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes . Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells .
|
-
- HY-139279
-
TPX-0131
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
|
-
- HY-132253
-
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Polatuzumab vedotin is an antibody-drug conjugate targeting CD79b. It contains a humanized anti-CD79b IgG1 monoclonal antibody linked to monomethyl auristatin E (MMAE), a potent microtubule inhibitor. Polatuzumab vedotin has the potential for the research of Large B-cell lymphomas (LBCL) .
|
-
- HY-168212
-
-
- HY-147977
-
|
Aldose Reductase
|
Cancer
|
ALR1/2-IN-1 (Compound 6e) is an aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitor with IC50 values of 3.26 μM and 3.06 μM against ALR1 and ALR2, respectively. ALR1/2-IN-1 shows anticancer activity .
|
-
- HY-12291
-
HMSL 10017-101-1
|
Raf
|
Cancer
|
HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
|
-
- HY-14658
-
-
- HY-161285
-
|
MMP
|
Cancer
|
MMP-9/10-IN-2 (compound 6e) is a potent inhibitor of MMP10 and MMP9, with IC50 of 0.076 μM for MMP10, and 93.18% inhibition at 0.5 μM for MMP9. MMP-9/10-IN-2 plays an important role in anti-tumor .
|
-
- HY-N12096
-
α-Acetylsalazinic acid
|
Bacterial
|
Infection
|
Galbinic acid (α-Acetylsalazinic acid), a lichen acid, shows antibacterial activities against the Gram-positive bacteria B. cereus, B. subtilis, and S. aureus (MICs=62.5, 62.5, 250 μg/ml, respectively). Galbinic acid inhibits the Gram-negative bacterium E. coli (MIC=125 μg/ml) .
|
-
- HY-163845
-
|
PROTACs
HDAC
|
Cancer
|
YX862 is a selective HDAC8 PROTAC degrader and induces the degradation of HDAC8 with maximum degradation > 95% at 250 nM in MDA-MB-231 cells(Sturcture Note:(Blue: VHL E3 ligand (HY-112078), Black: linker;Pink: HDAC8 inhibitor (HY-163846)) .
|
-
- HY-144878
-
|
c-Myc
|
Cancer
|
VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration .
|
-
- HY-B0621S
-
CGA89317-d3
|
Parasite
Microtubule/Tubulin
Isotope-Labeled Compounds
|
Others
|
Triclabendazole-d3 is the deuterium labeled Triclabendazole (HY-B0621). Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
|
-
- HY-151357
-
|
Bacterial
|
Infection
|
MraY-IN-3 (12a) is a potent bacterial translocase MraY inhibitor with an IC50 value of 140 µM. MraY-IN-3 acts on E. coli K12, B. subtilis W23 and P. fluorescens Pf-5 with the MIC50 values of 7 µg/mL, 12 µg/mL, and 46 µg/mL, respectively .
|
-
- HY-155843
-
|
CDK
SARS-CoV
Virus Protease
|
Infection
|
CDK9-IN-25 (compound 4a) is an imidazopyrazine CDK9 inhibitor (IC50: 0.24 μM). CDK9-IN-25 has good affinity to the main protease of COVID-19 and has antiviral activity against human coronavirus 229E (IC50: 63.28 μM) .
|
-
- HY-N8296
-
|
Bacterial
|
Infection
|
Saccharocarcin A is an antibiotic originally isolated from S. aerocolonigenes subsp. antibiotica. It is active against M. luteus, S. aureus, E. coli, P. aeruginosa, and C. albicans in a disc assay. Saccharocarcin A inhibits C. trachomatis infection by 88% without inducing cytotoxicity in McCoy cells when used at a concentration of 0.5 μg/mL.
|
-
- HY-101647
-
RP 60475
|
Topoisomerase
|
Cancer
|
Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
|
-
- HY-149866
-
|
Cytochrome P450
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
|
-
- HY-115933
-
|
EGFR
Raf
|
Cancer
|
EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAF V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity .
|
-
- HY-110287
-
|
APC
Mitosis
|
Cancer
|
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
|
-
- HY-160691
-
|
Aurora Kinase
|
Others
|
GW814408X is a kinase chemical genome group (KCGS) compound that inhibits the AURKC kinase involved in cell cycle progression, checkpoint regulation, and cell division. GW814408X exhibits cell line-dependent toxicity, e.g., cytotoxic effects on HeLa cells. GW814408X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays .
|
-
- HY-168447
-
|
Bacterial
|
Infection
|
D-PheTrAP is a bisubstrate analog inhibitor of 1-Deoxy-d-xylulose 5-phosphate synthase (DXPS). D-PheTrAP inhibits Escherichia coli DXPS (EcDXPS) and Pseudomonas aeruginosa DXPS (PaDXPS) with IC50 values of 0.52 μM, 2.1 μM, 2.4 μM, and 1.7 μM for wild-type (WT) EcDXPS, EcA426E, WT PaDXPS, and PaE431A, respectively .
|
-
- HY-N4110R
-
|
Cytochrome P450
|
Metabolic Disease
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-B0497S2
-
BAY2353-d3
|
Isotope-Labeled Compounds
Antibiotic
STAT
Parasite
|
Infection
Cancer
|
Niclosamide-d3 (BAY2353-d3) is deuterium labeled Niclosamide. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-174274
-
|
ERK
|
Cancer
|
ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF V600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma .
|
-
- HY-116620
-
|
Neurokinin Receptor
|
Infection
|
Benzomalvin C is a weak antagonist of the neurokinin-1 (NK1) receptor inhibiting binding of substance P by 46% when used at 100 μg/mL in vitro. It is also a weak inhibitor of indolamine 2,3-dioxygenase (IDO) with an IC50 value of 130 μM for recombinant IDO. It is isolated from Penicillium and contains an epoxide group at C-19 and C-20, which is not present in benzomalvins A, B, or E.
|
-
- HY-17624
-
Neomycin B; Fradiomycin B
|
Bacterial
Antibiotic
|
Infection
|
Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections .
|
-
- HY-168593
-
|
β-catenin
PROTACs
Wnt
Histone Demethylase
|
Cancer
|
PROTAC KDM3 degrader-1 (Compound 4) is a CRBN-recruiting PROTAC designed based on the IOX1 (HY-12304) scaffold. PROTAC KDM3 degrader-1 selectively degrades the KDM3A and KDM3B proteins, thereby inhibiting the Wnt/β-catenin signaling pathway. PROTAC KDM3 degrader-1 significantly suppresses the self-renewal capacity of colorectal cancer stem cells and inhibits the growth of colorectal cancer tumors. PROTAC KDM3 degrader-1 is suitable for research on colorectal cancer (Target protein ligand (Pink): HY-12304; linker (Black): HY-22335; Conjugate of E3 ligase ligand and linker: HY-112599; E3 ligase (Blue): HY-41547) .
|
-
- HY-173250
-
|
PROTACs
Ras
Apoptosis
|
Cancer
|
YN14-H is a PROTAC degrader targeting KRAS G12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo. (Structure Note: Pink: target protein ligand (HY-173252); Blue: E3 ligase ligand (HY-125905); Black: linker (HY-Y0840); E3 ligase ligand + linker (HY-173253) .
|
-
- HY-162719
-
|
SARS-CoV
|
Infection
|
RH12 is a dual inhibitor for SARS-CoV-2 related RNA-dependent RNA polymerase (RdRp, IC50 is 4.42 nM) and human transmembrane serine protease 2 (TMPRSS2, IC50 is 4.2 nM). RH12 exhibits antiviral efficacy. RH12 inhibits viral replication and absorption, and exhibits a 90.5% virucidal effects on Vero-E6 cells. RH12 inhibits cell viability of Calu-3 with an IC50 of 17.5 nM .
|
-
- HY-129284
-
|
COX
Wnt
|
Cancer
|
APHS is a specific and covalent COX-2 inhibitor with neuroprotective effects. COX-2 is a prostaglandin (PG) synthetase overexpressed in colorectal cancer (CRC) and has pleiotropic cancer-promoting effects. APHS modifies COX-2 by acetylating the active site (serine 516), thereby inhibiting prostaglandin production. The neuroprotective activity of APHS is inhibited by prostaglandin E2. APHS also co-inhibits the WNT pathway, an anti-tumor mechanism in addition to COX-2 inhibition .
|
-
- HY-117523
-
(Z)-Tyrphostin RG13022
|
EGFR
|
Cancer
|
(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells .
|
-
- HY-12304
-
|
Histone Demethylase
|
Cancer
|
IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively . IOX1 also inhibits ALKBH5 .
|
-
- HY-163677
-
|
PROTACs
PI3K
Akt
|
Cancer
|
ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC50 <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))
|
-
- HY-Y0445A
-
|
PDK-1
NKCC
PDHK
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Sodium dichloroacetate is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor. Sodium dichloroacetate also stimulates pyruvate dehydrogenase (PDH) activity and works as a Na +-K +-2Cl − cotransporter (NKCC) inhibitor. Sodium dichloroacetate prevents the phosphorylation of the E1α subunit of PDC, promoting the entry of pyruvate into the mitochondria for oxidative metabolism, reducing lactate production, and simultaneously increasing the production of reactive oxygen species (ROS). Sodium dichloroacetate inhibits tumor cell proliferation and induces apoptosis. Sodium dichloroacetate is promising for research of cancers .
|
-
- HY-150612
-
|
p38 MAPK
|
Cancer
|
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
|
-
- HY-173357
-
|
PROTACs
JAK
STAT
|
Inflammation/Immunology
|
TYD-68 is a highly efficient and selective CRBN-recruited TYK2 PROTAC degrader with a DC50 value of 0.42 nM. TYD-68 significantly inhibits IL-12 and IFN-α-induced STAT4 and STAT1 phosphorylation, thereby blocking TYK2-dependent signaling pathways.
TYD-68 can be used in the study of psoriasis. (Pink: Target protein ligand (HY-173359); Black: Linker (HY-W007732B); Blue: E3 ligase ligand (HY-14658); E3 ligase ligand + Linker (HY-173358)) .
|
-
- HY-154860
-
|
PROTACs
Btk
|
Cancer
|
PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation. (Pink: Btk ligand (HY-19834); Blue: E3 ligase ligand (HY-14658); Black: linker (HY-Y0966); E3 ligase ligand + linker (HY-131717)) .
|
-
- HY-P1633
-
PG1
|
Bacterial
ERK
COX
NF-κB
Apoptosis
NO Synthase
Dengue Virus
|
Infection
Inflammation/Immunology
|
Protegrin-1 is an orally active antibacterial peptide. Protegrin-1 activates ERK, COX2, NFκB, inhibits Apoptosis, and NO production. Protegrin-1 has antibacterial activity against S. aureus, E. faecium, E. coli, P. aeruginosa and K. Pneumoniae, with MBC values between 10 and 20 µM. Protegrin-1 has antiviral activity against dengue NS2B-NS3. Protegrin-1 has anti-inflammatory activity. Protegrin-1 is used in the study of inflammatory diseases and infections .
|
-
- HY-N1407R
-
|
Cytochrome P450
|
Inflammation/Immunology
|
Polygalaxanthone III (Standard) is the analytical standard of Polygalaxanthone III. This product is intended for research and analytical applications. Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM .
|
-
- HY-113068
-
|
Tyrosinase
|
Metabolic Disease
|
(rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-170760
-
|
Bacterial
|
Infection
|
Antibacterial agent 258 (Compound 11e) is an antibacterial agent, that destory the bacteria cell membrane, and inhibits various gram-positive bacteria (MIC for Staphylococcus aureus is 1-2 μg/mL). Antibacterial agent 258 exhibits low hemolytic activity and low cytotoxicity. Antibacterial agent 258 exhibits anti-infectious efficacy in mouse models .
|
-
- HY-W016867R
-
|
Fungal
Bacterial
|
Infection
|
4-Chlorosalicylic acid (Standard) is the analytical standard of 4-Chlorosalicylic acid. This product is intended for research and analytical applications. 4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
|
-
- HY-135194
-
|
Drug Metabolite
|
Others
|
Risperidone E-oxime is an impurity of Risperidone . Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
|
-
- HY-12057R
-
|
Raf
Autophagy
|
Cancer
|
Vemurafenib (Standard) is the analytical standard of Vemurafenib. This product is intended for research and analytical applications. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively . Vemurafenib induces cell autophagy .
|
-
- HY-144675A
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines .
|
-
- HY-W587663
-
|
Dihydrofolate reductase (DHFR)
|
Infection
|
4 '-DTMP is a DHFR inhibitor with Ki of 5.1 nM (DHFR WT) and 34.3 nM (DHFR L28R), respectively. 4 '-DTMP carries a polar modification that induces additional local interactions with the enzyme. In particular, the hairpin structure on the M20 ring is related to the internal communication of the DHFR. 4 '-DTMP has potential inhibition of E.coli .
|
-
- HY-163339
-
|
Beta-lactamase
|
Infection
|
Metallo-β-lactamase-IN-14 (Compound 17e) is a Metallo-β-Lactamase inhibitor. Metallo-β-lactamase-IN-14 shows inhibition activity against VIM-1 and VIM-2. Metallo-β-lactamase-IN-14 has antibacterial activity against Gram-negative (GN) bacteria and P. aeruginosa .
|
-
- HY-P2136F
-
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Biotin-COG1410 TFA is a biotin labled COG1410 (HY-P2136). COG1410 is an apolipoprotein E-derived peptide and an apoptosis inhibitor. COG1410 exerts neuroprotective and antiinflammatory effects in a murine model of traumatic brain injury (TBI). COG1410 can be used for the research of neurological disease .
|
-
- HY-106054
-
|
Prostaglandin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
Nocloprost, a prostaglandin E2 (PGE2) analog, is an orally active EP1- and EP3-receptor agonist. Nocloprost inhibits evoked [ 3H]ACh release. Nocloprost has gastroprotective and ulcer-healing properties. Nocloprost accelerates the healing of chronic gastric ulcerations and enhances mucosal growth in rats .
|
-
- HY-14658S
-
-
- HY-159087
-
|
PROTACs
|
Cancer
|
RGB110 (Compound 10d) is a PROTAC inhibitor for D-dopachrome tautomerase with an IC50 of 5.9 μM. RGB110 causes no degradation of D-DT. (Pink: ligand for target protein (HY-159164); Black: linker (HY-W125017); Blue: ligand for E3 ligase CRBN (HY-10984))
|
-
- HY-108705
-
|
Molecular Glues
Bcl-2 Family
|
Cancer
|
BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity .
|
-
- HY-100180R
-
LCB01-0371 (Standard)
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
4-Chlorosalicylic acid (Standard) is the analytical standard of 4-Chlorosalicylic acid. This product is intended for research and analytical applications. 4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
|
-
- HY-W020790
-
sLeX
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability?to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
|
-
- HY-164309
-
|
Drug-Linker Conjugates for ADC
|
Cancer
|
DBCO-PEG3-Glu-Val-Cit-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG3-Glu-Val-Cit-PABC-MMAE contains a potent tubulin inhibitor Monomethyl auristatin E (MMAE, HY-15162) and can be used for synthesis of dual-drug ADC .
|
-
- HY-16952
-
(±)-Bepridil; Org 5730
|
Calcium Channel
Sodium Channel
SARS-CoV
|
Infection
Cardiovascular Disease
|
Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells .
|
-
- HY-118827R
-
|
COX
|
Inflammation/Immunology
|
Vedaprofen (Standard) is the analytical standard of Vedaprofen. This product is intended for research and analytical applications. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory agent (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM .
|
-
- HY-162250
-
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
|
-
- HY-151166
-
|
β-glucuronidase
Bacterial
|
Cancer
|
β-Glucuronidase-IN-2 is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.24 μM, an Ki value of 1.09 μM. β-Glucuronidase-IN-2 shows antiproliferative activity. β-Glucuronidase-IN-2 has the potential for the research of anti-cancer and anti-inflammatory therapies .
|
-
- HY-132253A
-
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Polatuzumab vedotin solution is an antibody-drug conjugate targeting CD79b. It contains a humanized anti-CD79b IgG1 monoclonal antibody linked to monomethyl auristatin E (MMAE), a potent microtubule inhibitor. Polatuzumab vedotin solution has the potential for the research of Large B-cell lymphomas (LBCL) .
|
-
- HY-16772
-
α-Tocotrienol quinone; PTC-743; Vatiquinone; NCT04378075
|
Mitochondrial Metabolism
Ferroptosis
|
Neurological Disease
|
EPI-743 (Vatiquinone; α-Tocotrienol quinone; PTC-743; NCT04378075) is a potent cellular oxidative stress protectant, inhibits ferroptosis in cells, which could be used for the study for mitochondrial diseases. EPI-743 is a synthetic analog of vitamin E with oral activity, targets repletion of reduced intracellular glutathione .
|
-
- HY-162229
-
|
SARS-CoV
|
Infection
|
GRL-190-21 (compound 5e) is an inhibitor for SARS-Cov-2-Mpro with a Ki of 0.04 nM and exhibits antiviral activity in VeroE6 cells with EC50 of 0.26 μM. GRL-190-21 reduces the infectivity, replication, and cytopathic effect of SARS-CoV-2 without significant toxicity .
|
-
- HY-144675
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines .
|
-
- HY-172087
-
|
VD/VDR
|
Inflammation/Immunology
|
VDR agonist 3 (Compound E15) is a potent vitamin D receptor (VDR) agonist. VDR agonist 3 can effectively inhibit HSC activation through VDR. VDR agonist 3 significantly reduces liver fibrosis without causing hypercalcemia in a CCl4-induced mouse liver fibrosis model .
|
-
- HY-144096
-
|
Histone Methyltransferase
|
Cancer
|
EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17) .
|
-
- HY-101647A
-
RP 60475 dimesylate
|
Topoisomerase
|
Cancer
|
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
|
-
- HY-131295
-
|
MEK
Ligands for Target Protein for PROTAC
|
Cancer
|
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
|
-
- HY-149351
-
|
NF-κB
|
Cardiovascular Disease
|
NF-κB-IN-10 (compound E1) is an NF-κB inhibitor that can improve heart failure by reducing oxidative stress and inflammation by regulating Nrf2/NF-κB signaling pathway. NF-κB-IN-10 inhibits LPS-induced NO production and expression of iNOS and COX-2 in RAW264.7 cells. NF-κB-IN-10 can be used in the research of cardiovascular diseases .
|
-
- HY-156586
-
ASN90
|
OGA
Tau Protein
|
Neurological Disease
|
Egalognastat (ASN90) is a selective, brain-penetrant and orally active O-GlcNAcase (OGA) enzyme inhibitor with an IC50 value of 10.2 nM. Egalognastat increases O-GlcNAcylation of intracellular proteins like tau and α-synuclein, preventing their aggregation and toxicity. Egalognastat does not inhibit hexosaminidase (Hex). Egalognastat can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies (e.g., Alzheimer’s disease and Parkinson’s disease) .
|
-
- HY-131044
-
|
Bacterial
Fungal
|
Infection
|
5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione (Compound 4) has antimicrobial, anti-diabetic and antioxidant activities. 5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione inhibits B. subtilis, S. aureus, K. pneumonia, E. coli, and S. typhi with MICs of 4.5-9.9 μΜ/mL, and inhibits A. niger and C. albicans with MICs of 4.99 μΜ/mL .
|
-
- HY-155981
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 3CLpro-IN-18 (Compound 3C) is a covalent SARS-CoV-2 3CLpro inhibitor (IC50s: 0.478 μM). SARS-CoV-2 3CLpro-IN-18 inhibits SARS-CoV-2 in Vero E6 cells (EC50= 2.499 μM) with low cytotoxicity (CC50 > 200 μM) .
|
-
- HY-161346
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
EBET-1055 is a bromodomain and extra-terminal (BET) protein degrader (EBET) composed of a BET inhibitor (EBET-590, HY-161387), an E3 ubiquitin ligase ligand and connectors. EBET-1055 effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC). EBET-1055 also simultaneously modulates cancer-associated fibroblast (CAF) activity, upregulating all reporter gene activities in organoid co-cultures .
|
-
- HY-168073
-
|
EGFR
VEGFR
Apoptosis
Microtubule/Tubulin
|
Cancer
|
EGFR/VEGFR2-IN-1 (Compound 10e) is a VEGFR-2 and EGFR inhibitor (IC50: 0.26 and 0.14 μM respectively). EGFR/VEGFR2-IN-1 inhibits tubulin polymerization with an IC50 of 40.9 μM. EGFR/VEGFR2-IN-1 induces apoptosis. EGFR/VEGFR2-IN-1 can be used for research of antileukemia and antilymphoma .
|
-
- HY-163985
-
|
PROTACs
FGFR
Apoptosis
|
Cancer
|
PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2.
PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM.
PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker:HY-163986) .
|
-
- HY-B0168A
-
|
Serotonin Transporter
PERK
|
Neurological Disease
|
Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
- HY-B0168
-
|
Serotonin Transporter
PERK
|
Neurological Disease
|
Milnacipran is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran inhibits pERK1/2 activation. Milnacipran has antidepressant, anxiolytic and analgesic properties. Milnacipran inhibits biting behavior in mice. Milnacipran can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
- HY-156106
-
|
Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .
|
-
- HY-103046
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent .
|
-
- HY-100864
-
|
PGE synthase
|
Inflammation/Immunology
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) .
|
-
- HY-100507A
-
CC 122 hydrochloride
|
E1/E2/E3 Enzyme
Apoptosis
Molecular Glues
NF-κB
|
Inflammation/Immunology
Cancer
|
Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities .
|
-
- HY-44432
-
ABT-263-piperazine
|
Ligands for Target Protein for PROTAC
Bcl-2 Family
|
Cancer
|
Navitoclax-piperazine (ABT-263-piperazine) is a Navitoclax (HY-10087) analog and BCL-XL inhibitor. Navitoclax-piperazine is the ligand for target protein of PROTAC DT2216 (HY-130604). Navitodax-pperaie and E3 ubiquitin ligase VHL ligand can be used to synthesize PROTAC DT2216 (HY-130604) .
|
-
- HY-163147
-
|
Influenza Virus
|
Infection
|
PAN endonuclease-IN-1 (Compound 23) is a potent PAN endonuclease inhibitor, with Kd values of 277 μM, 384 μM and 328 μM for WT, I38T and E23K PAN endonucleases, respectively. The RNA-dependent RNA polymerase acidic N-terminal (PAN) endonuclease, a critical component of influenza viral replication machinery, is an antiviral target .
|
-
- HY-114366
-
|
CXCR
|
Others
|
BC-1485 is a small molecule inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1). BC-1485 protects PIAS4 from ubiquitin-mediated degradation. BC-1485 decreases α-SMA, BAL and CXCL1. BC-1485 ameliorates fibrotic lung injury in murine models .
|
-
- HY-169160
-
|
Bacterial
|
Infection
|
Anti-MRSA agent 18 (E17) is an inhibitor of MRSA with MIC values of 2 μg/mL for S. aureus and 4 μg/mL for MRSA, respectively. Anti-MRSA agent 18 interacts with bacterial cell membrane phosphatidylglycerol and cardiolipin, causing changes in cell membrane permeability and polarization, increased intracellular ROS, and DNA and protein leakage, thereby accelerating bacterial death .
|
-
- HY-137315S
-
-
- HY-151489
-
|
Cyclophilin
|
Neurological Disease
Metabolic Disease
Cancer
|
CypE-IN-1 is a potent and subtype-selective cyclophilin E (CypE) inhibitor. CypE-IN-1 has CypE affinity with IC50 and Ki values of 0.013 μM and 0.072 μM, respectively. CypE-IN-1 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes .
|
-
- HY-171140
-
|
PROTACs
HDAC
|
Cancer
|
PROTAC HDAC6 degrader 3 (Compound 4) is a selective inhibitor and degrader for HDAC6 with an IC50 of 686 nM and a DC50 of 171 nM. PROTAC HDAC6 degrader 3 promotes the acetylation of α-tubulin . (Pink: ligand for target protein (HY-171141); Blue: ligand for E3 ligase VHL (HY-150803))
|
-
- HY-N4237
-
|
Prostaglandin Receptor
Potassium Channel
|
Inflammation/Immunology
|
Saikogenin D is isolated from?Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores .
|
-
- HY-15610
-
RG 7421; MEK inhibitor 1
|
MEK
Apoptosis
|
Cancer
|
GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
|
-
- HY-158158
-
|
Histone Methyltransferase
|
Cancer
|
CARM1-IN-5 (Compound 17e) is a potent and selective inhibitor of CARM1 (IC50= 2 nM). CARM1-IN-5 effectively prevents CARM1 from methylating substrate proteins by directly interacting with CARM1. CARM1-IN-5 exhibits significant antiproliferative effects on melanoma cell lines .
|
-
- HY-149675
-
|
VEGFR
c-Met/HGFR
|
Cancer
|
VEGFR-2/c-Met-IN-2 (compound 3e) is a VEGFR-2/c-Met inhibitor, with IC50 values of 83 and 48 nM, respectively. VEGFR-2/c-Met-IN-2 exhibits cytotoxic activity against HCT-116 cell line (IC50: 3.403 µM) .
|
-
- HY-12847
-
|
Raf
Src
Apoptosis
|
Cancer
|
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
|
-
- HY-129454
-
Antibiotic TPU-0037-A
|
Antibiotic
|
Infection
|
TPU-0037A is an antibiotic and a congener of lydicamycin. It inhibits the growth of Gram-positive bacteria, including methicillin-resistant S. aureus (MRSA), B. subtilis, and M. luteus (MICs=1.56-12.5 μg/mL), but not Gram-negative E. coli, P. mirabilis, P. vulgaris, or P. aeruginosa strains (MICs=>50 μg/mL).
|
-
- HY-P10836
-
|
Dengue Virus
|
Infection
|
DN59 is a 33 amino acid peptide that mimics the dengue virus type 2 E stem region. DN59 inhibits all four serotypes of dengue virus (IC50: 2-5 μM) as well as other flaviviruses. N59 causes the release of genomic RNA by interacting directly with viral particles. DN59 has antiviral activity .
|
-
- HY-170430
-
|
Molecular Glues
E1/E2/E3 Enzyme
|
Cancer
|
HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21 .
|
-
- HY-12678
-
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-157139
-
|
Carbonic Anhydrase
Phosphatase
|
Inflammation/Immunology
|
ALP/Carbonic anhydrase-IN-1 (Compound 1e) is a dual carbonic anhydrase (CA) and alkaline phosphatase (ALP) inhibitor. ALP/Carbonic anhydrase-IN-1 shows IC50 values of 0.44 µM, 1.61 µM, 0.51 µM, and 0.107 µM for CA-II, CA-IX, CA-XII, and ALP, respectively .
|
-
- HY-W109513
-
|
Amino Acid Derivatives
|
Inflammation/Immunology
|
Boc-Lys(Z)-OH (DCHA) is a involves in synthesis thymosin β4, βg and β6 fragments, and increases E-rosette forming capacity in Lupus Nephritis model. Boc-Lys(Z)-OH (DCHA) involves in synthesis Boc-Lyz-OCH3 and acts as a reagent of peptidyl thrombin inhibitors production .
|
-
- HY-144123
-
|
HIV
|
Infection
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-172159
-
|
HDAC
Apoptosis
|
Cancer
|
FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
|
-
- HY-159579
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
CW-3308 is an orally effective PROTAC that selectively targets BRD9 and is expected to be used to inhibit synovial sarcoma, rhabdomyoma, and other BRD9-dependent human diseases. CW-3308 is composed of PROTAC target protein ligand Naphthyridin-Me-dimethoxybenzene-COOH (HY-159596) (red part), Linker 3-Azaspiro[5.5]undecane-9-methanol (HY-159598) (black part), E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine (HY-159597) (blue part), where the conjugate of E3 ubiquitin ligase ligand + linker is Thalidomide-pyrrolidine-C-azaspiro (HY-159599) [1] .
|
-
- HY-173523
-
|
PROTACs
CDK
c-Myc
|
Cancer
|
KI-CDK9d-32 is a CDK9 PROTAC degrader (DC50: 0.89 nM). KI-CDK9d-32 promotes the ubiquitination and degradation of CDK9. KI-CDK9d-32 inhibits the MYC pathway and disrupts nucleolar homeostasis. KI-CDK9d-32 has anticancer activity. (Pink: CDK9 ligand (HY-153718); Blue: E3 ligase CRBN ligand (HY-163233); Black: Linker (HY-W011657); E3 ligase CRBN ligand-linker conjugate (HY-173525)) .
|
-
- HY-149209
-
|
PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
|
-
- HY-170390
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC50=559 nM for VHL in live HEK293; IC50=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC50 of 111 nM . (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))
|
-
- HY-17624A
-
Neomycin B sulfate; Fradiomycin B sulfate
|
Antibiotic
Bacterial
|
Infection
|
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections .
|
-
- HY-173496
-
|
Sialyltransferase
|
Cancer
|
ST6GAL1-IN-1 (compound 4e) is a potent and selective ST6GAL1 inhibitor with an IC50 of 20.0 μM. ST6GAL1-IN-1 exhibits antimetastatic activity and effectively inhibiting MDA-MB-231 cell migration. ST6GAL1-IN-1 also suppresses tumor growth and metastasis in vivo .
|
-
- HY-P10816
-
Ac-(DLeu)LLLRVK-Amba
|
Bacterial
|
Infection
Cancer
|
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
|
-
- HY-127146
-
|
Antibiotic
Bacterial
|
Infection
|
Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
|
-
- HY-125789
-
|
Bacterial
|
Infection
|
PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection .
|
-
- HY-155107
-
|
Mitochondrial Metabolism
Bacterial
|
Infection
|
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study .
|
-
- HY-161083
-
|
PARP
Histone Methyltransferase
|
Cancer
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-169131
-
|
AMPK
|
Cancer
|
ALKBH1-IN-4 prodrug (Compound 29E) is a prodrug of a DNA N6-methyladenine demethylase ALKBH1 inhibitor that significantly increases the abundance of 6mA in cells and upregulates the AMPK signaling pathway, thereby inhibiting the viability of gastric cancer cells. ALKBH1-IN-4 prodrug exhibits excellent cellular activity and favorable metabolic exposure in vivo, and holds promise for research in gastric cancer .
|
-
- HY-N4110
-
|
Cytochrome P450
NF-κB
Interleukin Related
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders .
|
-
- HY-162583
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
|
-
- HY-155479
-
|
Bacterial
|
Infection
|
PqsR-IN-3 (compound 16e) is a selective inhibitor of the pqs system (IC50=3.7 μM) and its associated virulence factor pyocyanin (IC50=2.7 μM). PqsR-IN-3 inhibits bacterial biofilm synthesis and is significantly cytotoxic against Pseudomonas aeruginosa. PqsR-IN-3 has synergistic effects with several antibiotics, such as Ciprofloxacin (HY-B0356) and Tobramycin (HY-B0441) .
|
-
- HY-162147
-
|
mTOR
Autophagy
|
Inflammation/Immunology
|
Nur77 modulator 3 (9e) can bind to Nur77 and inhibit TGF-β1-induced α-SMA and COLA1 expression in a Nur77-dependent manner. Nur77 modulator 3 induces Nur77 expression and enhances autophagic flux by inhibiting the mTORC1 signaling pathway in vitro and in vivo. Nur77 modulator 3 blocks the progression of hepatic fibrosis .
|
-
- HY-125778
-
|
Others
|
Metabolic Disease
|
Cochlioquinone is a sesquiterpene metabolite originally isolated from C. miyabeanus. It is a phytotoxin that inhibits root growth of finger millet (E. coracana) and rice plants (O. sativa) by 59.9 and 51.7%, respectively, when used at a concentration of 100 ppm.2 Cochlioquinone B inhibits NADH oxidase and NADH-2,3-dimethoxy-5-pentyl-1,4-benzoquinone reductase from bovine heart mitochondria.
|
-
- HY-157810
-
|
Aldose Reductase
|
Cancer
|
AKR1C3-IN-11 (Compound 6e) is a Aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 2.0 μM. AKR1C3-IN-11 inhibit cell proliferation in combination with abiraterone (HY-70013). AKR1C3-IN-11 can be used for the research of prostate cancer .
|
-
- HY-114402
-
|
PROTACs
Androgen Receptor
|
Cancer
|
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study the treatment of castration-resistant prostate cancer (mCRPC) .
ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).
|
-
- HY-172151
-
|
Herbicide
Protoporphyrinogen IX oxidase
|
Others
|
PPO-IN-17 (Compound 6R) is the inhibitor protoporphyrinogen IX oxidase (PPO) that inhibits Nicotiana tobacco PPO (NtPPO) with Ki of 30.34 nM. PPO-IN-17 exhibits herbicidal activity that inhibits barnyardgrass (E. crus-galli), foxtail grass (D. sanguinalis), alfalfa (M. sativa) and Canada cocklebur (C. canadensis) (>95% inhibition rate at a concentration of 37.5 g/hm 2). PPO-IN-17 exhibits no toxicity on rice (at a concentration of 75 g/hm 2) or on honeybees (at a concentration of 6400 mg/kg) .
|
-
- HY-114564
-
E5510
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Satigrel (E5510) is a potent inhibitor of platelet aggregation. Satigrel inhibits collagen- and arachidonic acid-induced platelet aggregation through preventing thromboxane A2 synthesis by selective inhibition of the target enzyme, PGHS1, which exists in platelets. Satigrel inhibits PGHS1 (IC50: 0.081 μM) and PGHS2 (IC50: 5.9 μM). Satigrel is against Type III PDE, Type V and Type II (IC50: 15.7 μM, 39.8 μM and 62.4 μM, respectively) .
|
-
- HY-150109A
-
|
HDAC
|
Cancer
|
Purinostat is a selective inhibitor of HDAC I/IIb with anti-leukemic activity. Purinostat mesylate (HY-150109), the mesylate salt of Purinostat, inhibits the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDAC I/IIb to inhibit several important factors for leukemic stem cell (LSC) survival, including c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Purinostat mesylate increases glutamate metabolism in LSC by increasing GLS1 .
|
-
- HY-172363
-
|
Succinate Dehydrogenase
Fungal
|
Infection
|
Succinate dehydrogenase-IN-6 (Compound E23) is the inhibitor for succinate dehydrogenase that inhibits SDH in Rhizoctonia solani with an IC50 of 11.76 μM. Succinate dehydrogenase-IN-6 disrupts fungal cell membrane, exhibits board-spectrum antifungal activity that inhibits R. solani, V. dahliae, A. solani and C. gloeosporioides with EC50s of 0.41, 0.27, 1.15, 0.27 μg/mL, respectively. Succinate dehydrogenase-IN-6 exhibits no significant toxicity in rice and zebrafish (LC50 > 12.5 μg/mL) .
|
-
- HY-155938
-
|
Acyltransferase
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Cyano-myracrylamide is an inhibitor of zinc finger DHHC domain-containing palmitoyltransferase 20 (zDHHC20) with an IC50 value of 1.35 µM. Cyano-myracrylamide also inhibits the S-Acylation of EGFR and CD36. Cyano-myracrylamide also inhibits S-acylation of Legionella E3 ligase GobX, MyD88, and Ras, which are substrates of zDHHC20, zDHHC9, and zDHHC6, respectively, in HEK293T cells expressing recombinant Legionella GobX, recombinant human MyD88, or endogenous Ras .
|
-
- HY-164474
-
|
MEK
|
Cancer
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-163913
-
|
SARS-CoV
|
Infection
|
SARS-CoV-IN-5 (compound 49) is a highly selective, nonpeptidic and noncovalent 3CL pro inhibitor with IC50s of 38 nM, 21.1 nM and 86 nM for 3CL pro of SARS-CoV-1, SARS-CoV-2, Bat coronavirus WIV1, respectively. SARS-CoV-IN-5 inhibits the replication of the SARS-CoV-2 delta variant with an EC50 of 0.272 μM. SARS-CoV-IN-5 significantly reduces the lung viral copies in a K18-hACE2 transgenic mouse model. SARS-CoV-IN-5 has good target-specific and potential broad-spectrum anticoronavirus activities against SARS-CoV-1, WIV1, MERS, HCoV-OC43, HCoV-229E, and HKU9 .
|
-
- HY-160547
-
|
PROTACs
Androgen Receptor
|
Metabolic Disease
|
PROTAC AR Degrader-5 (compound A46) is a potent AR PROTACs degrader with an IC50 value of 49 nM. PROTAC AR Degrader-5 inhibits sebaceous plaque and induces hair regeneration (Pink: ligand for target protein (HY-169967); black: linker (HY-169966); Blue: E3 ligase ligand (HY-125845)) .
|
-
- HY-132296
-
|
FAK
PROTACs
|
Cancer
|
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
|
-
- HY-N3513R
-
|
Others
|
Cardiovascular Disease
|
Mulberrin (Standard) is the analytical standard of Mulberrin. This product is intended for research and analytical applications. Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-W028350
-
|
HIV
DNA/RNA Synthesis
|
Infection
|
NSC727447 is an inhibitor of ribonuclease H (Rnase H) of HIV-1 and HIV-2. NSC727447 has little activity against E. coli RNase H, but great selectivity over human Rnase H, with IC50s value of 2.0 μM, 2.5 μM, 100 μM, 10.6 μM, respectively .
|
-
- HY-135969
-
|
Bacterial
|
Infection
|
Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable . Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively .
|
-
- HY-137315
-
|
Amyloid-β
NF-κB
mTOR
Keap1-Nrf2
|
Neurological Disease
|
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research .
|
-
- HY-116788
-
|
Bacterial
|
Infection
|
Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM .
|
-
- HY-168586
-
|
PROTACs
IRAK
|
Cancer
|
PROTAC IRAK4 degrader-12 is a PROTAC based on Cereblon ligand, inducing a maximum degradation rate of IRAK4 of 108.46% in K562 cells with an IC50 value of 4.87 nM ( Structure Note: Pink, IRAK4 inhibitor (HY-168611); Blue, E3 (HY-W733885); Black, linker (HY-168613)) .
|
-
- HY-147742
-
|
JAK
|
Inflammation/Immunology
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF) .
|
-
- HY-113068S
-
|
Isotope-Labeled Compounds
Tyrosinase
|
Metabolic Disease
|
β-Tocopherol-d3 is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol can also prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-W348072
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-59 (compound E07), an imidazoline derivative, is a non-peptide small molecule inhibitor of SARS-CoV-2 that targets the main protease (Mpro) of the coronavirus. SARS-CoV-2-IN-59 has a strong interaction with residues on Mpro (Met 165, Gln 166, Met 165, His 41, Gln 189) .
|
-
- HY-N7148S1
-
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
Cancer
|
γ-Tocopherol-d4 is the deuterium labeled γ-Tocopherol. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity .
|
-
- HY-100507R
-
CC 122 (Standard)
|
Reference Standards
E1/E2/E3 Enzyme
Apoptosis
Molecular Glues
NF-κB
|
Inflammation/Immunology
Cancer
|
Avadomide (Standard) is the analytical standard of Avadomide. This product is intended for research and analytical applications. Avadomide is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide exhibits potent antitumor and immunomodulatory activities .
|
-
- HY-P1001A
-
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
Ac-DEVD-CHO TFA is a peptide inhibitor of caspase-3 (Ki=230 pM) and caspase-7. Ac-DEVD-CHO TFA reduces caspase-3 activity and apoptosis induced by Prostaglandin E2 (HY-101952) in rat cortical neurons. Ac-DEVD-CHO TFA is promising for research of neurodegenerative diseases and cancers .
|
-
- HY-143898
-
|
Pim
|
Cancer
|
PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases .
|
-
- HY-B0149
-
cyclocapron
|
IGF-1R
AMPK
MMP
Mitophagy
PROTAC Linkers
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis. Tranexamic acid is a PROTAC linker. Tranexamic acid is used to synthesize PROTACs (e.g. LZ-07 (HY-172590)) .
|
-
- HY-155156
-
|
Endogenous Metabolite
|
Cardiovascular Disease
|
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice .
|
-
- HY-162281
-
|
PROTACs
SOS1
Ras
|
Cancer
|
PROTAC SOS1 degrader-6 (compound 23) is an effective SOS1 PROTACs degrader that synergizes with KRAS G12C inhibitors . PROTAC SOS1 degrader-6 consists of the target protein ligand (red part) SOS1 Ligand intermediate-7 (HY-169371), E3 ubiquitin ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and PROTAC linker (black part) 5-Bromopentanoic acid (HY-W016456). Among them, the E3 ubiquitin ligase ligand + linker can form (S,R,S)-AHPC-CO-C4-bromine (HY-169372).
|
-
- HY-155157
-
|
Endogenous Metabolite
|
Cardiovascular Disease
|
PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice .
|
-
- HY-P991223
-
|
Transmembrane Glycoprotein
TNF Receptor
|
Cancer
|
NC762 is a humanized IgG1κ monoclonal antibody that targets human B7-H4 (B7 homolog 4). NC762 has enhanced binding to CD16a (FcγRIIIa) after being Fc engineered with three point mutations (S239D/A330L/I332E; DLE) and demonstrate increased antibody-dependent cellular cytotoxicity (ADCC) activity. NC762 inhibits tumor growth in vivo through binding to tumor-expressing B7-H4. NC762 can be studies in research on cancer such as advanced or metastatic solid tumors .
|
-
- HY-145925B
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
CFT8634 is an orally bioavailable PROTAC BRD9 targeted degrader based on the E3 ubiquitin ligase CRBN mechanism. CFT8634 can be used for the study of synovial sarcoma and SMARCB1-deficient solid tumors (Pink: BRD9 ligand (HY-169988); Blue: E3 ligase ligand (HY-169989); Black: linker (HY-169991). CFT8634 is a heterobifunctional molecule that binds to BRD9 at one end and recruits CRBN at the other end, which can inhibit the growth of tumor cells that depend on BRD9. CFT8634 can be used for the study of SMARCB1-related cancers (such as synovial sarcoma and malignant rhabdoid tumor) .
|
-
- HY-147414
-
PF-114
|
Bcr-Abl
|
Cancer
|
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-170820
-
|
Molecular Glues
|
Cancer
|
XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822) .
|
-
- HY-12542
-
F 368
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is also a calcium channel protein inhibitor. Dantrolene inhibits the release of Ca 2+ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases). Dantrolene offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties .
|
-
- HY-B1077
-
R-16341
|
Calcium Channel
Dopamine Receptor
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca 2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml .
|
-
- HY-170585
-
|
COX
NF-κB
|
Inflammation/Immunology
|
COX-2-IN-51 (E25) is a potent COX-2 inhibitor, with an IC50 of 70.7 nM. COX-2-IN-51 significantly inhibits LPS-induced release of NO and PGE2, expression of COX-2 and iNOS, and activation of NF-κB pathway. COX-2-IN-51 exhibits anti-inflammatory and analgesic effects in diverse murine models through inhibiting NF-κB pathway. COX-2-IN-51 has lower gastrointestinal side effects than Indomethacin (HY-14397) .
|
-
- HY-162873
-
|
MEK
Raf
|
Cancer
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
|
-
- HY-12302
-
9-Bromopaullone; NSC-664704
|
CDK
GSK-3
|
Cancer
|
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
|
-
- HY-154968
-
|
RSV
|
Infection
|
RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM),and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM,HEp-2),also exhibits activity and lowers virus titers in mouse models of RSV infection .
|
-
- HY-14657
-
F 440
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
Dantrolene sodium is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium is also a calcium channel protein inhibitor. Dantrolene sodium inhibits the release of Ca 2+ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases). Dantrolene sodium offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties .
|
-
- HY-171007
-
-
- HY-N2278
-
Leachianone E
|
Tyrosinase
Glycosidase
|
Cancer
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .
|
-
- HY-B0497G
-
BAY2353
|
Antibiotic
Parasite
STAT
|
Cancer
|
Niclosamide (GMP) is Niclosamide (HY-B0497) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research . Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells . Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells .
|
-
- HY-147405
-
PF-07284890; ARRY-461
|
Raf
ERK
|
Cancer
|
Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies .
|
-
- HY-101903A
-
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-13811
-
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
|
-
- HY-171006
-
|
Caspase
PARP
Pyroptosis
Interleukin Related
IFNAR
|
Infection
Inflammation/Immunology
|
IRF1-IN-1 (Compound I-2) is an IRF1 inhibitor. IRF1-IN-1 decreases the recruitment of IRF1 to the promoter of CASP1. IRF1-IN-1 inhibits cell death signaling pathway (i.e., cleavage of Caspase 1, GSDMD, IL-1 and PARP1). IRF1-IN-1 has a protective effect on ionizing radiation-induced inflammatory skin injury .
|
-
- HY-176193
-
|
P-glycoprotein
|
Cancer
|
P-gp modulator-7 (Compound 9e) is a P-glycoprotein (P-gp) inhibitor. P-gp modulator-7 occupies the channel entrance of P-gp with a unique T-shaped configuration, hindering the peristaltic extrusion mechanism of transmembrane domains TM12 and TM9, thereby inhibiting P-gp from pumping drugs out of cells and reversing the multidrug resistance (MDR) of tumor cells. P-gp modulator-7 is promising for research of cancers .
|
-
- HY-101903
-
|
FABP
|
Cardiovascular Disease
Metabolic Disease
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-12033
-
2-ME2; NSC-659853
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-172408
-
|
Reverse Transcriptase
HIV
|
Infection
|
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC50 of 6.2-250 nM .
|
-
- HY-N14671
-
|
Antibiotic
Bacterial
|
Infection
|
Hedamycin is a quinone antibiotic. Hedamycin has anti-Gram-positive bacteria, negative bacterium, mycobacterium and yeast fungus activity (MIC is 0.031-3.2 μg/mL). 0.8 μg/mL of Hedamycin can inhibit Tetrahymena pyriformis. Hedamycin also can inhibit rat duodenum adenocarcinoma, rats Walker 256 tumor (50 μg/kg/day), HeLa cell (IG50 is 0.00013 μg/mL), e. coli lysogenic W1709 (λ) phage (MIC is 0.0125 μg/mL) .
|
-
- HY-112158
-
ERGi-USU
|
Ser/Thr Kinase
|
Cancer
|
NSC139021 (ERGi-USU) is a RIOK2 inhibitor with anticancer activity. RIOK2 can highly selectively inhibit the growth of ERG-positive cancer cells with IC50s of 30-400 nM against cell lines. RIOK2 also causes cell cycle arrest and apoptosis in glioblastoma via induction of Skp2 and Skp2-p27/p21-Cyclin E/CDK2-pRb signaling .
|
-
- HY-119271
-
SDS-1-021
|
c-Myc
Apoptosis
|
Cancer
|
CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism .
|
-
- HY-162489
-
|
Bcr-Abl
|
Others
|
Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .
|
-
- HY-10581A
-
AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-N12105
-
|
HBV
|
Infection
|
Dihydrodehydrodiconiferyl alcohol 9-O-β-D-xylopyranoside is an anti-hepatitis B virus (anti-HBV) agent. Dihydrodehydrodiconiferyl alcohol 9-O-β-D-xylopyranoside inhibits HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion on Hep G2.2.15 cell line, with IC50 values of 1.67 and >2.15 mM, respectively .
|
-
- HY-10581B
-
AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-163651
-
(R)-CR6086
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
(R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with Ki of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC50 of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice .
|
-
- HY-108467
-
GGsTop
3 Publications Verification
Nahlsgen
|
γ-Glutamyl Transferase (GGT)
|
Cardiovascular Disease
|
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
|
-
- HY-130854
-
|
E3 Ligase Ligand-Linker Conjugates
Autophagy
Apoptosis
|
Cancer
|
Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A) .
|
-
- HY-131907
-
|
Bacterial
|
Infection
|
LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively .
|
-
- HY-173361
-
|
Microtubule/Tubulin
|
Cancer
|
Anticancer agent 270 (Compound 8e) is an inhibitor that acts on tubulin. Its IC50 value against MCF-7 breast cancer cells is 1.02 μM. Through a dual mechanism of action, namely inducing Apoptosis and destabilizing microtubules, it exerts significant anti-proliferative activity against breast cancer cells. Anticancer agent 270 can be applied to research in the field of cancer .
|
-
- HY-115672
-
KS15
2 Publications Verification
|
Cryptochrome
|
Cancer
|
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
|
-
- HY-173225
-
|
Bacterial
|
Infection
|
MRSA/VRE-IN-1 (Compound 3e) is an inhibitor against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). The MIC/MBC of MRSA/VRE-IN-1 against VRE is 3.6/7.3 µM, and against MRSA is 7.3/14.6 µM. MRSA/VRE-IN-1 can be used in the research of the anti-infection field .
|
-
- HY-144307
-
|
Aurora Kinase
PKC
|
Cancer
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-126898
-
|
Lipoxygenase
PGE synthase
|
Inflammation/Immunology
|
5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity .
|
-
- HY-100573A
-
|
Mixed Lineage Kinase
|
Cancer
|
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
|
-
- HY-N7148R
-
|
COX
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
γ-Tocopherol (Standard) is the analytical standard of γ-Tocopherol. This product is intended for research and analytical applications. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity .
|
-
- HY-133680S
-
|
Isotope-Labeled Compounds
|
Others
|
β-Tocopherol-d4 is a deuterium labeled β-Tocopherol (HY-133680). β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-N6979
-
20-Hydroxyecdysone
|
Caspase
Autophagy
Endogenous Metabolite
|
Cardiovascular Disease
|
Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Serratula coronata which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP . Crustecdysone exhibits regulatory or protective roles in the cardiovascular system . Crustecdysone is an active metabolite of Ecdysone (HY-N0179) .
|
-
- HY-W037817
-
Dimethyl glutamate
|
Potassium Channel
Bacterial
|
Infection
Metabolic Disease
|
Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism .
|
-
- HY-152161
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
|
-
- HY-B0168S
-
|
Isotope-Labeled Compounds
Serotonin Transporter
PERK
|
Neurological Disease
|
Milnacipran-d10 (hydrochloride) is the deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
- HY-B0168AS
-
|
Isotope-Labeled Compounds
Serotonin Transporter
PERK
|
Neurological Disease
|
Milnacipran-d5 hydrochloride is deuterium labeled Milnacipran hydrochloride (HY-B0168A). Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
- HY-17531R
-
|
Herbicide
|
Others
|
Pyraclonil (Standard) is the analytical standard of Pyraclonil. This product is intended for research and analytical applications. Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations . Pyraclonil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P99107A
-
|
Antibody-Drug Conjugates (ADCs)
Apoptosis
|
Cancer
|
Brentuximab vedotin (solution) (cAC10-vcMMAE) is an antibody-drug conjugate (ADC) comprising an anti-CD30 antibody and the cytotoxic agent Monomethyl auristatin E (MMAE). Brentuximab vedotin (solution) inhibits CD30-positive cells with an IC50 of 2.5 ng/mL. Brentuximab vedotin (solution) can be used for the research of relapsed and refractory Hodgkin lymphoma .
|
-
- HY-105070A
-
E5564
|
EBV
Toll-like Receptor (TLR)
|
Infection
Inflammation/Immunology
|
Eritoran tetrasodium (E5564) is a Toll-like receptor 4 (TLR4) antagonist. Eritoran tetrasodium protects mice against lethal influenza virus infection, such as Ebola virus (EBOV), Marburg virus (MARV). Eritoran tetrasodium decreases the level of granulocytosis, may alleviate the severity of the "cytokine storm". Eritoran tetrasodium inhibits pathogenesis of filovirus infection. Eritoran tetrasodium has anti-inflammatory activity .
|
-
- HY-149085A
-
|
RAR/RXR
|
Cancer
|
(E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer .
|
-
- HY-14658R
-
|
Ligands for E3 Ligase
Autophagy
Apoptosis
Reference Standards
|
Inflammation/Immunology
Cancer
|
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
|
-
- HY-158027
-
|
Raf
VEGFR
FGFR
|
Cancer
|
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer .
|
-
- HY-Z10518
-
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
|
((3R,5R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate) calcium(II) is an impurity found in bulk preparations of the HMG-CoA reductase inhibitor Rosuvastatin (HY-17504A).
|
-
- HY-160264
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756) .
|
-
- HY-133680R
-
|
Tyrosinase
|
Others
|
β-Tocopherol (Standard) is the analytical standard of β-Tocopherol. This product is intended for research and analytical applications. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-161901
-
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice .
|
-
- HY-162848
-
|
PI3K
|
Cancer
|
IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC50 values for PI3Kγ and PI3Kδ of 4.0 and 9.1 nM, respectively. IHMT-PI3K-315 has antitumor activity .
|
-
- HY-146977
-
|
PDK-1
|
Cancer
|
LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases .
|
-
- HY-151574
-
|
Parasite
|
Infection
|
PfGSK3/PfPK6-IN-1 (compound 23e) is a potent inhibitor of plasmodial kinases PfGSK3 and PfPK6, with IC50s of 97 nM and 8 nM, respectively. PfGSK3/PfPK6-IN-1 exerts antiplasmodial activity against blood stage Pf3D7 parasites with an EC50 value of 1.4 mM .
|
-
- HY-10581
-
AM-1155; BMS-206584; PD135432
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml) . Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-138678
-
|
Ligands for E3 Ligase
|
Cancer
|
(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
|
-
- HY-N11499
-
|
Bacterial
|
Infection
Inflammation/Immunology
|
Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models .
|
-
- HY-15460R
-
|
Bacterial
Antibiotic
|
Infection
|
CHIR-090 (Standard) is the analytical standard of CHIR-090. This product is intended for research and analytical applications. CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-127110
-
|
Phospholipase
|
Others
Neurological Disease
Inflammation/Immunology
|
AK106-001616 is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) (IC50=3.8 nmol/L). AK106-001616 is able to reduce the production of prostaglandins (PG) E2 and leukotrienes (LT) B4 by stimulated cells. AK106-001616 can be used in the study of inflammatory diseases, neuropathic pain and pulmonary fibrosis .
|
-
- HY-N0074
-
|
COX
|
Inflammation/Immunology
|
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory agent on airway inflammation .
|
-
- HY-141432G
-
Cbl-b-IN-3
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
Cancer
|
NX-1607 (Cbl-b-IN-3) (GMP) is a GMP-grade NX-1607 (HY-141432). GMP-grade small molecules can be used as adjuvant agents in cell therapy. NX-1607 (GMP) enhances antigen recall, reduces T cell exhaustion and increases cytokine production. NX-1607 is an inhibitor of Cbl-b (an E3 enzyme) .
|
-
- HY-10581C
-
AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
Inflammation/Immunology
|
Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-144736
-
|
Virus Protease
|
Infection
|
NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively .
|
-
- HY-148044
-
|
β-glucuronidase
Bacterial
|
Infection
|
UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes .
|
-
- HY-168247
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC50: < 10 nM in A549 cell; IC50: 15 nM for A549). Blue: E3 ligase ligand (HY-112078), Black: linker (HY-168249), Pink: BRM/BRG1 inhibitor (HY-168248) .
|
-
- HY-168554
-
|
PROTACs
STING
|
Inflammation/Immunology
|
STING-IN-10 (P8) is a dual STING PROTAC degrader and inhibitor with a DC50 value of 2.58 μM in THP-1 cells. STING-IN-10 has anti-inflammatory activity .(Pink: Target protein ligand (HY-168676); Black: linker (HY-W123015); Blue: E3 ligase ligand (HY-126457))
|
-
- HY-119894
-
NSC 102809
|
Antibiotic
|
Infection
|
Althiomycin is a polyketide synthase-derived thiazole antibiotic originally isolated from S. althioticus. It is active against Gram-positive bacteria, including S. aureus, S. epidermidis, and S. pyogenes (MICs=25, 25, and 3.1 μg/mL, respectively).2 Althiomycin inhibits protein synthesis in E. coli when used at concentrations of 1 and 10 μg/mL but not in isolated rabbit reticulocytes at 100 μg/mL.
|
-
- HY-169920
-
|
HIV
Reverse Transcriptase
|
Infection
|
HIV-1 inhibitor-79 (Compound 3k) is an HIV inhibitor that exhibits significant inhibitory activity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) .
|
-
- HY-12542A
-
Dantrolene sodium hydrate
|
Calcium Channel
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
|
Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is also a calcium channel protein inhibitor. Dantrolene sodium hemiheptahydrate inhibits the release of Ca 2+ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases). Dantrolene sodium hemiheptahydrate offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties .
|
-
- HY-161849
-
|
Histone Demethylase
|
Metabolic Disease
|
LSD1-IN-31 (compound 11e) can directly bind to LSD1/CoREST complex to reduce LSD1 demethylation enzymatic activity. LSD1-IN-31 inhibits LSD1 demethylation activity and influences its downstream IκB/NF-κB signaling pathway. LSD1-IN-31 inhibits osteoclastic bone loss in vitro and in vivo. LSD1-IN-31 can be used for osteoporosis research .
|
-
- HY-173150
-
|
YAP
|
Cancer
|
YAP-IN-1 (Compound (+)-1) is an autophagy (Autophagy) inhibitor targeting YAP1. YAP-IN-1 binds to the Hippo pathway transcription factor YAP1 with a Kd of 9.13 μM and induces its degradation via the chaperone-mediated autophagy (CMA) pathway. This process inhibits Rab7-mediated fusion of autophagosomes and lysosomes, thereby reducing overall autophagy levels without affecting lysosomal function. YAP-IN-1 holds promise for research in cancer (e.g., liver cancer, breast cancer, etc.) .
|
-
- HY-141431
-
|
E3 Ligase Ligand-Linker Conjugates
|
Inflammation/Immunology
Cancer
|
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent .
|
-
- HY-12843
-
|
CDK
ERK
|
Cancer
|
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities .
|
-
- HY-B1119
-
|
Bacterial
Fungal
Antibiotic
Apoptosis
|
Infection
Cancer
|
Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-156153
-
|
Histone Methyltransferase
|
Cancer
|
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
|
-
- HY-107573
-
|
Histone Demethylase
|
Cancer
|
KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro .
|
-
- HY-170838
-
|
PDHK
|
Cancer
|
PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect). PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293 .
|
-
- HY-147947
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
|
-
- HY-125728
-
|
Bacterial
Parasite
HCV
|
Infection
|
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM . Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively . Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum .
|
-
- HY-123045
-
|
CDK
|
Cancer
|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
|
-
- HY-169021
-
|
JNK
|
Cancer
|
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
|
-
- HY-B0827
-
MTI-446
|
nAChR
Parasite
|
Infection
Cardiovascular Disease
|
Dinotefuran is an orally active and competitive inhibitor and insecticide targeting insect nicotinic acetylcholine receptors (nAChRs). Dinotefuran blocks neural signaling and induces neural dysfunction in insects. Dinotefuran binds to [ 3H]epibatidine in the neural cord membrane of American cockroach with an IC50 of 890 nM and to [ 3H]α-bungarotoxin with an IC50 of 36.1 μM. Dinotefuran exhibits knockdown activity (KD50=0.351 nmol/g) and lethal activity (LD50=0.173 nmol/g) against German cockroach. Dinotefuran is mainly used for agricultural pest control, such as field control of piercing-sucking and chewing insects (e.g., aphids, planthoppers), while its environmental toxicological effects (e.g., oxidative stress and reproductive neurotoxicity on earthworms) are also a research focus to assess ecological risks .
|
-
- HY-150612S
-
|
Isotope-Labeled Compounds
p38 MAPK
|
Cancer
|
(R)-STU104-d6 is a deuterium labeled (R)-STU104 (HY-150612). (R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
|
-
- HY-P1723
-
Spexin
1 Publications Verification
Neuropeptide Q
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Neurological Disease
|
Spexin (Neuropeptide Q) is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin can function through both central and peripheral actions. Spexin upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-P5439
-
|
PKC
MARCKS
|
Others
|
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitory activity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
|
-
- HY-P1723A
-
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
Apoptosis
Ferroptosis
Autophagy
|
Cardiovascular Disease
Metabolic Disease
|
Spexin (Neuropeptide Q) TFA is a selective agonist of galanin receptors GAL2 and GAL3, and is a conserved peptide that functions as a neurotransmitter/neuromodulator and endocrine factor. Spexin TFA can function through both central and peripheral actions. Spexin TFA upregulates Beclin 1 to inhibit ferroptosis induced by excessive autophagy, reduces the uptake of long-chain fatty acids by adipocytes, and regulates energy metabolism by increasing lipid oxidation (e.g., reducing the respiratory exchange ratio in rodents). Spexin TFA improves cardiac function in the Doxorubicin hydrochloride (HY-15142)-induced cardiotoxicity model, protects mitochondrial membrane potential, and reduces iron accumulation and lipid peroxidation. Spexin TFA can be used to study obesity and its related metabolic disorders, cardiovascular diseases (e.g., cardioprotection), and side effects of tumor chemotherapy .
|
-
- HY-B0168AR
-
|
Reference Standards
Serotonin Transporter
PERK
|
Neurological Disease
|
Milnacipran (hydrochloride) (Standard) is the analytical standard of Milnacipran hydrochloride (HY-B0168A). This product is intended for research and analytical applications. Milnacipran hydrochloride is an orally active Serotonin (HY-B1473A) and Norepinephrine (HY-13715) reuptake inhibitor. Milnacipran hydrochloride inhibits monoamine transporters, especially the norepinephrine transporter and the serotonin transporter (Ki values of 31 and 8.5 nM, respectively). Milnacipran hydrochloride inhibits pERK1/2 activation. Milnacipran hydrochloride has antidepressant, anxiolytic and analgesic properties. Milnacipran hydrochloride inhibits biting behavior in mice. Milnacipran hydrochloride can be used in the study of major depressive disorder, anxiety disorders, and neuropathic pain (e.g., fibromyalgia) .
|
-
- HY-148273
-
KRAS G12D inhibitor 17
|
PROTACs
Ras
|
Cancer
|
Setidegrasib (KRAS G12D inhibitor 17, Example 8) is a PROTAC KRAS degrader (DC50: 37 nM). Setidegrasib induces the degradation of G12D-mutation KRAS protein. Setidegrasib has antitumor effect. (Blue: E3 ligase ligand (HY-168699); Black: linker (HY-168698); Pink: G12D ligand (HY-168700)) .
|
-
- HY-10424
-
PHA-848125
|
CDK
Autophagy
|
Cancer
|
Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-148864
-
|
Epigenetic Reader Domain
|
Cancer
|
JQ1-TCO is the double bond E configuration of JQ1-TCO (HY-148864A). JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1 (HY-13030), an inhibitor of BET. JQ1-TCO is suitable for click chemistry and can be used as molecular probes in vitro and in vivo .
|
-
- HY-146492
-
|
VEGFR
Raf
Apoptosis
|
Cancer
|
VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase .
|
-
- HY-164306
-
|
PROTACs
PARP
|
Cancer
|
PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for PARP with a DC50<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC50 <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))
|
-
- HY-139328
-
|
CDK
|
Cancer
|
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-169434
-
Lon-TK-BMS-1
|
PD-1/PD-L1
|
Cancer
|
LTB is a prodrug formed by coupling glycolysis inhibitor (Lonidamine (HY-B0486)) with PD1/PDL1 blocker (BMS-1 (HY-19991)) by thioketal linkage. LTB can further encapsulate photosensitizer chlorine e6 (Ce6) (HY-13594) to construct a co-delivery photodynamic nanoplatform (LTB-6 NPs) by self-assembly .
|
-
- HY-136439R
-
|
Bacterial
Antibiotic
Apoptosis
|
Infection
|
4-Epianhydrotetracycline (hydrochloride) (Standard) is the analytical standard of 4-Epianhydrotetracycline (hydrochloride). This product is intended for research and analytical applications. 4-Epianhydrotetracycline hydrochloride is a major intermediate product of Tetracycline (HY-A0107). 4-Epianhydrotetracycline hydrochloride shows lethal effects and induces cell apoptosis of zebrafish embryos. 4-Epianhydrotetracycline hydrochloride inhibits Shewanella, E. coli and P. aeruginosa with MIC values of 2, 1 and 64 mg/L, respectively .
|
-
- HY-114758
-
|
Biochemical Assay Reagents
Ferrochelatase
|
Cardiovascular Disease
|
Pyridoxal isonicotinoyl hydrazone is an orally active and lipophilic iron-specific chelator that acts as a non-competitive inhibitor of ferrochelatase (FECH) by binding iron ions. Pyridoxal isonicotinoyl hydrazone disrupts heme biosynthesis, leading to reduced FECH stability and increased protoporphyrin IX (PPIX) accumulation. Pyridoxal isonicotinoyl hydrazone is promising for research of iron-overload diseases (e.g., β-thalassemia) .
|
-
- HY-162004
-
|
NF-κB
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
NF-κB-IN-14 (compound 5e) significantly inhibits nitric oxide production in LPS-induced macrophages (IC50: 6.4 μM). NF-κB-IN-14 disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway suppression. NF-κB-IN-14 reduces ear edema and inflammation in an atopic dermatitis mouse model .
|
-
- HY-161779
-
|
Molecular Glues
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
|
-
- HY-173009
-
|
PROTACs
Cyclophilin
HCV
HIV
|
Infection
|
PROTAC CG167 is a selective and potent CypA PROTAC degrader. PROTAC CG167 degrades CypA in a dose-dependent manner (Jurkat: DC50: 123 nM). PROTAC CG167 can inhibit HIV-1 and HCV and exhibits antiviral activity . (Pink: CypA Ligand (HY-170997); Black: Linker (HY-W123015); Blue: E3 Ligase Ligand (HY-112078))
|
-
- HY-147237
-
|
Bacterial
|
Infection
|
LpxC-IN-10 (Compound A) is a high selectivity inhibitor of LpxC. LpxC-IN-10 exhibits MIC values of 0.5 μg/mL against E. coli and K. pneumoniae. LpxC-IN-10 (Compound A) can be used for the research of bacterial infection . LpxC-IN-10 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-W097792
-
5'-O-DMT-dU
|
DNA/RNA Synthesis
|
Others
|
5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine (5'-O-DMT-dU) is a competitive inhibitor of E. coli dUTP nucleotidohydrolase (dUTPase), with the Ki higher than 1000 μM. 5'-O-(4,4'-Dimethoxytrityl)-2'-deoxyuridine can be used in machine-assisted DNA synthesis by synthesizing nucleosidic phosphoramidite blocks .
|
-
- HY-100022A
-
eFT508 hydrochloride
|
MNK
PD-1/PD-L1
|
Cancer
|
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-169165
-
|
Fungal
|
Infection
|
14α-Demethylase-IN-1 (compound 2e) is a 14α-demethylase inhibitor and can be used as an antifungal agent. 14α-Demethylase-IN-1 (48 h) exhibits MIC50 values of 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM for C. albicans, C. parapsilosis, C. krusei, and C. glabrata, respectively .
|
-
- HY-128686
-
KAG-308
2 Publications Verification
|
Prostaglandin Receptor
|
Inflammation/Immunology
Endocrinology
|
KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor .
|
-
- HY-155540
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 3CLpro-IN-14 (compound 11j) is an orally active SARS-CoV-2 3CLpro inhibitor. SARS-CoV-2 3CLpro-IN-14 shows significant anti-SARS-CoV-2 activity (EC50 = 0.18 μM) and low cytotoxicity (CC50 > 50 μM) in Vero E6 cells .
|
-
- HY-130439
-
|
SOD
|
Metabolic Disease
|
EUK 8 and EUK 134 are synthetic catalytic scavengers of reactive oxygen species with superoxide dismutase (SOD) and catalase mimetic activity.1 EUK 124 is a structural analog of EUK 8 and EUK 134 with significantly reduced activity. EUK 124 and EUK 8 inhibit superoxide-mediated reduction of an electron acceptor (i.e., SOD mimetic activity), with IC50 values of 5 μM and 0.7 μM, respectively.
|
-
- HY-164529
-
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-W181530
-
|
Molecular Glues
CDK
Apoptosis
Ligands for E3 Ligase
|
Cancer
|
NCT02 is a molecular glue degrader based on the E3 ubiquitin ligase DDB1 that targets CDK12 and its binding partner CCNK. NCT02 triggers the ubiquitination and proteasomal degradation of CCNK, thereby downregulating CDK12 protein levels and inhibiting its downstream signaling pathways. NCT02 can induce tumor cell apoptosis, arrest the cell cycle, and selectively inhibit the proliferation of colorectal cancer cells carrying TP53 defects or belonging to the consensus molecular subtype CMS4. NCT02 has the potential to inhibit tumor growth in in vitro and in vivo models .
|
-
- HY-18200A
-
E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
|
-
- HY-142444
-
|
VAP-1
|
Metabolic Disease
|
SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3) .
|
-
- HY-170824
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
SMD-3236 is a SMARCA2-targeted PRAOTAC degrader designed based on SMARCA ligands and VHL-1 ligands, with long-lasting antitumor activity in vivo. SMARCA2 is a synthetic lethal target in SMARCA4-deficient cancer cells, and SMD-3236 has a 2000-fold selectivity for degradation of SMARCA2 over SMARCA4, with a DC50< 1 nM and a Dmax>95%. SMD-3236 can induce SMARCA2 loss in tumor tissues while retaining SMARCA4 protein, and inhibit tumor growth in the H838 smarca4-deficient human cancer xenograft model. SMD-3236 is composed of target protein ligand (red part) SMI-1074 (HY-170817), PROTAC linker (black part) (trans-4-Ethynylcyclohexyl)methyl methanesulfonate (HY-170825), and E3 ligase ligand (blue part) SMARCA2 ligand-14 (HY-170826), of which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 159 (HY-170827) .
|
-
- HY-111546
-
BI-3663
1 Publications Verification
|
PROTACs
FAK
|
Cancer
|
BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker . Anti-cancer activity .
|
-
- HY-111140
-
|
PGE synthase
Lipoxygenase
|
Inflammation/Immunology
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells .
|
-
- HY-12678R
-
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-D0823
-
Sulfo-Cy3 NHS ester; Sulfo Cyanine3 NHS ester
|
Fluorescent Dye
|
Others
|
Cy3-SE (Sulfo-Cy3 NHS ester; Sulfo Cyanine3 NHS ester) is a sulfonated cyanine dye-derived fluorescent labeling reagent with λex of about 515 nm and λem of about 568 nm. Cy3-SE can interact with the π-π stacking of biomolecules (e.g., nucleoside monophosphates, proteins), inhibiting the photoisomerization process and increasing the fluorescence quantum yield and lifetime .
|
-
- HY-139329
-
|
CDK
|
Cancer
|
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-114324A
-
|
PROTACs
PARP
|
Cancer
|
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-150286
-
|
Prion Protein
|
Neurological Disease
|
SM875 is a cellular prion protein (PrP) degrader (IC50: 7.87 μM). SM875 targets PrP folding intermediates and promotes its degradation through the autophagy-lysosomal pathway. SM875 only acts on nascent, immature PrP molecules and has no effect on mature PrP before synthesis. SM875 can inhibit prion replication and has potential in the study of neurodegenerative diseases (i.e., prion diseases) .
|
-
- HY-162493
-
|
Bacterial
|
Infection
|
MBL-IN-3 (compound 72922413) is a New Delhi metallo-β-lactamase-1 (NDM-1) inhibitor(IC50=54±4 μM). MBL-IN-3 is identified and shown to lower minimum inhibitory concentrations (MICs) of Meropenem (HY-13678) for a panel of E. coli and K. pneumoniae clinical isolates expressing NDM-1. MBL-IN-3 can be used for antibiotic sensitizer research .
|
-
- HY-139327
-
|
CDK
|
Cancer
|
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-168152
-
|
SARS-CoV
Virus Protease
|
Infection
|
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
|
-
- HY-156453
-
|
PAK
Apoptosis
|
Cancer
|
PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1 .
|
-
- HY-10581AS
-
AM-1155-d3 hydrochloride; BMS-206584-d3 hydrochloride; PD135432-d3 hydrochloride
|
Isotope-Labeled Compounds
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-146019A
-
|
HIV
|
Infection
|
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
|
-
- HY-171830
-
YX39-105
|
PROTACs
Tyrosinase
Apoptosis
|
Cancer
|
MS105 is an orally active and selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. MS105 recruits VHL E3 ligase via the VHL ligand moiety to promote PTK6 ubiquitination and proteasomal degradation, inhibiting breast cancer cell proliferation, migration, and inducing apoptosis. MS105 is promising for research of breast cancer. (Pink: BRK inhibitor P21d hydrochloride (HY-115514); Black: linker (HY-W105727); Blue: (S,R,S)-AHPC (HY-125845)) .
|
-
- HY-115693
-
|
Bacterial
|
Infection
|
CAP 3 is a cholic acid-peptide conjugate (CAP) antimicrobial agent. CAP 3 effectively inhibits Gram-negative bacteria, with MIC99 (minimum inhibitory concentration for 99% bacterial killing) values of 8 μM, 16 μM, and 16 μM against E. coli, Klebsiella pneumoniae and Acinetobacter baumannii, respectively. CAP 3 exerts its antibacterial effects by disrupting the structural integrity of the bacterial lipopolysaccharide (LPS) outer membrane. CAP 3 rapidly kills bacteria, inhibits biofilm formation, and effectively combats drug-resistant strains and persistent bacterial infections .
|
-
- HY-17624AR
-
|
Antibiotic
Bacterial
|
Infection
|
Framycetin (sulfate) (Standard) is the analytical standard of Framycetin (sulfate). This product is intended for research and analytical applications. Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections .
|
-
- HY-157327
-
|
Bcr-Abl
|
Cancer
|
AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL. AKE-72 inhibits BCR-ABL WT, BCR-ABL T315, BCR-ABL E255K, BCR-ABL F3171, BCR-ABL H396P and BCR-ABL Q252H with IC50s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line .
|
-
- HY-161261
-
|
AAK1
SARS-CoV
|
Infection
|
SARS-CoV-2-IN-81 (compound 12e) is a potent AAK1 inhibitor with an IC50 value of 9.38 nM. SARS-CoV-2-IN-81 shows anti-viral property against SARS-CoV-2. SARS-CoV-2-IN-81 attenuates AAK1-induced phosphorylation of AP2M1 threonine 156 and disrupts the direct interaction between AP2M1 and ACE2, ultimately inhibiting SARS-CoV-2 infection .
|
-
- HY-153066
-
KIF18A-IN-7
|
Kinesin
Microtubule/Tubulin
Apoptosis
|
Cancer
|
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
|
-
- HY-155527
-
|
SARS-CoV
|
Infection
|
SARS-CoV-2 Mpro-IN-9 (compound c7) is a nonpeptidic, noncovalent SARS-CoV-2 M pro inhibitor (IC50=0.085 μM), with improved physicochemical and drug metabolism and pharmacokinetics (DMPK) properties. SARS-CoV-2 Mpro-IN-9 inhibits viral replication (EC50=1.10 μM) in SARS-CoV-2-infected Vero E6 cells, while exhibits low cytotoxic effects (CC50>50 μM) .
|
-
- HY-18299
-
NG 95
|
CDK
Parasite
|
Infection
Cancer
|
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
|
-
- HY-134816
-
|
Toll-like Receptor (TLR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
D-Glucan is an orally effective Dectin-1 receptor immune activator with antioxidant properties (reducing TNF-α). D-Glucan activates macrophages and neutrophils to scavenge free radicals, inhibit oxidative stress and inflammatory responses, and improve insulin sensitivity. D-Glucan promotes glycolysis by enhancing the activity of the antioxidant enzyme glutathione, inhibiting gluconeogenesis and activating GK. D-Glucan can be used in the research of liver damage protection (antagonizing Acetaminophen (HY-66005) toxicity), radiation protection (synergistic with vitamin E) and diabetes (improving glucose metabolism) .
|
-
- HY-163105
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin/NEDDylation-IN-1 (compound C11) is a dual inhibitor of tubulin (Microtubule/Tubulin)-NEDDylation (IC50 for tubulin=2.40 μM), which has strong anti-proliferative activity. Neddylation is a protein post-translational modification that covalently tags the ubiquitin-like protein NEDD8 to target proteins. Tubulin/NEDDylation-IN-1 forms hydrogen bonds with residues of tubulin and E1 NEDD8 activating enzyme (NAE) through methoxy and dithiocarbamate groups and inhibits NEDDylation and microtubulin in an ATP-dependent manner. tube polymerization .
|
-
- HY-N8936
-
|
Others
|
Inflammation/Immunology
|
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
|
-
- HY-170978
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
|
-
- HY-162875
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRD4 Degrader-27 (compound 6b) is a PROTAC that selectively targets BRD4 (rather than BRD2/BRD3) and can also inhibit the expression of KLF5 transcription factor and exert anti-cancer activity. PROTAC BRD4 Degrader-27 is composed of E3 ubiquitinase ligand Thalidomide-4-OH (HY-103596) (red part), PROTAC Linker γ-Aminobutyric acid (HY-N0067) (black part) and PROTAC target protein ligand PROTAC BRD4 ligand-3 (HY-162876) (blue part), of which the active control of the target protein ligand is Mivebresib (HY-100015), and the conjugate of E3 ubiquitin ligase ligand + Linker is Pomalidomide 4'-alkylC3-acid (HY-131875) [1] .
|
-
- HY-150797
-
QA-68-ZU81
|
PROTACs
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
|
-
- HY-169086
-
|
PROTACs
|
Cancer
|
KL-465 is a PROTAC degrader for MAGE-A3, that degrades MAGE-A3 with a DC50 of 2 μM in HeLa cell. KL-465 inhibits viability of MAGE-A3 positive cancer cell HCT116, A375 and HeLa. (Blue: Ligand for E3 ligase (HY-151227); Black: Linker (HY-W679862); Pink: Ligand for target protein (HY-169087))
|
-
- HY-N2013
-
Aristololactam; Aristolactam
|
Drug Metabolite
Aquaporin
Cadherin
TGF-beta/Smad
|
Endocrinology
Cancer
|
Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .
|
-
- HY-155060
-
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
Antibacterial agent 144 (compound 8e) is an antibacterial agent,with better effect against multi-resistant Staphylococcus aureus than Chloromycin and Amoxicillin (HY-B0467A). Antibacterial agent 144 destroys the cytoplasmic membrane of bacteria,and inhibits the biofilms formation. Antibacterial agent 144 binds to HSA (Kd=13.2 μM),and exerts bactericidal efficacy. Antibacterial agent 144 also binds with DNA to for supramolecular complex to obstruct DNA replications .
|
-
- HY-146491
-
|
VEGFR
Raf
Apoptosis
|
Cancer
|
VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase .
|
-
- HY-168869
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer . (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
|
-
- HY-164992
-
MRG002; Trastuzumab MMAE
|
Antibody-Drug Conjugates (ADCs)
EGFR
Microtubule/Tubulin
|
Cancer
|
Trastuzumab vedotin (MRG002) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab vedotin is composed of a humanized anti-HER2 antibody Trastuzumab (HY-P9907), an enzymatically cleavable peptide-linker Valine-citrulline, a tubulin inhibitor Monomethyl auristatin E (MMAE; HY-15162). Trastuzumab vedotin can be used for the research of HER2-positive breast cancer .
|
-
- HY-163453
-
|
EGFR
|
Cancer
|
HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50 NCI-N87 = 1.63 nM, IC50 BT474= 15.17 nM, IC50 BaF3-HER2YVMA = 1.49 nM .
|
-
- HY-P1122
-
|
Formyl Peptide Receptor (FPR)
|
Infection
Inflammation/Immunology
|
Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.
|
-
- HY-P991443
-
|
CD73
|
Cancer
|
IPH5301 is a human IgG1 monoclonal antibody (mAb) targeting NT5E/CD73. IPH5301 has a functionally silent Fc domain, specifically inhibits soluble and membrane CD73 enzyme activity, and restores the proliferation of immune T cells. IPH5301 can be used in anti-tumor immunity research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-144323
-
|
PROTACs
PERK
|
Cancer
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
|
-
- HY-164619
-
|
CDK
SARS-CoV
|
Infection
Cancer
|
CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC50 of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC50 of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC50 of 145.92 μM .
|
-
- HY-176421
-
|
PROTACs
PI3K
|
Cancer
|
PROTAC PI3K/110β degrader-1 (J-9) is a PROTAC based PI3K/110β degrader (Red: PI3K/110β inhibitor (HY-75124), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-10581AR
-
AM-1155 hydrochloride (Standard); BMS-206584 hydrochloride (Standard); PD135432 hydrochloride (Standard)
|
Reference Standards
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin (hydrochloride) (Standard) is the analytical standard of Gatifloxacin (hydrochloride). This product is intended for research and analytical applications. Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml)[1]. Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-159961
-
|
SARS-CoV
Virus Protease
|
Infection
|
SARS-CoV-2 Mpro-IN-34 (Compound 26) is an inhibitor for SARS-CoV-2 Mpro with an IC50 of 6 nM. SARS-CoV-2 Mpro-IN-34 exhibits inhibitory efficacy against OC43 Mpro with an IC50 of 33 nM. SARS-CoV-2 Mpro-IN-34 exhibits antiviral activity in SARS-CoV-2 infected Vero E6 cell with an EC50 of 0.103 μM .
|
-
- HY-17598
-
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
|
-
- HY-155845
-
|
Parasite
|
Infection
|
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC50 of 0.0198-0.096 μM .
|
-
- HY-117026
-
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-P99705
-
RG-7599; DNIB-0600A; NaPi2b-ADC
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
Lifastuzumab vedotin (RG-7599; DNIB0600A) is an antibody-drug conjugate (ADC) that comprises a humanized IgG1 anti-NaPi2b monoclonal antibody (MNIB2126A) and a potent antimitotic agent, monomethyl auristatin E (MMAE), which inhibits cell division by blocking the polymerization of tubulin. Lifastuzumab vedotin has the potential for non-small cell lung cancer (NSCLC) and platinum-resistant ovarian cancer (PROC) research .
|
-
- HY-136055
-
VH032-C5-COOH
|
E3 Ligase Ligand-Linker Conjugates
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases .
|
-
- HY-100022
-
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-168205
-
|
HSP
Apoptosis
|
Cancer
|
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
|
-
- HY-163168
-
CFT-4531
|
PROTACs
DNA/RNA Synthesis
|
Cancer
|
aTAG 4531 (CFT-4531) is a potent, selective, and onmechanism tool degrader of MTH1 with DC50 value of 0.28 nM and Ki value of 1.8 nM. The degradation activity is due to the intricate formation of the ternary complex between the MTH1 aTAG, CRBN E3 ligase, and aTAG tool degrader. Red: MTH1 aTAG inhibitor (HY-134725), Blue: CRBN ligand (HY-126457), Black: linker (HY-108374) .
|
-
- HY-N6979R
-
|
Caspase
Autophagy
Endogenous Metabolite
|
Cardiovascular Disease
|
Crustecdysone (Standard) is the analytical standard of Crustecdysone. This product is intended for research and analytical applications. Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Serratula coronata which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP . Crustecdysone exhibits regulatory or protective roles in the cardiovascular system . Crustecdysone is an active metabolite of Ecdysone (HY-N0179) .
|
-
- HY-128912
-
|
Histone Demethylase
|
Cancer
|
Arborinine is a potent and orally activeLSD1 inhibitor. Arborinine increases the expression of H3K4me1/2, H3K9me1/2, E-cad protein and decreases the expression of UBE2O protein level. Arborinine induces cell cycle arrest at S phase. Arborinine shows antitumor activity .
|
-
- HY-112450
-
|
CDK
|
Cancer
|
Olomoucine II is a potent CDK inhibitor with IC50 values of 0.06, 0.1, 0.45, 7.6, 19.8 µM for CDK9/cyclin T, CDK2/cyclin E, CDK7/cyclin H, CDK1/cyclin B, CDK4/cyclin D1, respectively. Olomoucine II shows antiproliferative activity .
|
-
- HY-164239
-
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
NH2-PEG3-VC-PAB-MMAE is a drug-linker conjugate for ADC, consisting of a cleavable ADC linker (NH2-PEG3-VC-PAB) and a potent tubulin inhibitor Monomethyl auristatin E (MMAE) (HY-15162). NH2-PEG3-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs) .
|
-
- HY-W016149
-
Dichloro-1,2-dithiacyclopentenone
|
Bacterial
|
Infection
|
4,5-Dichloro-3H-1,2-dithiol-3-one (Dichloro-1,2-dithiacyclopentenone) is an E. coli FabH inhibitor (IC50: 2.9 µM). 4,5-Dichloro-3H-1,2-dithiol-3-one can be used as a slimicide in the manufacture of food-contact paper and paperboard .
|
-
- HY-113068R
-
|
Tyrosinase
|
Metabolic Disease
|
(rel)-β-Tocopherol (Standard) is the analytical standard of (rel)-β-Tocopherol. This product is intended for research and analytical applications. (rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-168495
-
|
Amylases
Glycosidase
|
Metabolic Disease
|
α-Amylase-IN-12 (Compound 5e) is an α-amylase inhibitor (IC50: 0.15 mM) with a mixed inhibition. α-Amylase-IN-12 has an IC50 of 9.40 mM against α-glucosidase. α-Amylase-IN-12 promotes glucose uptake in yeast cells and exhibits significant antiglycation activity at high concentrations. α-Amylase-IN-12 can be used for the research of diabetes .
|
-
- HY-171793
-
|
PPAR
|
Metabolic Disease
|
DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes .
|
-
- HY-B1077R
-
|
Calcium Channel
Dopamine Receptor
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Penfluridol (Standard) is the analytical standard of Penfluridol. This product is intended for research and analytical applications. Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca 2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml .
|
-
- HY-136797
-
|
Dengue Virus
|
Infection
|
BP13944 is a potential small molecule inhibitor discovered by high-throughput screening. It can effectively inhibit the expression of dengue virus (DENV) replicons with an EC50 value of 1.03±0.09 μM. BP13944 can inhibit the replication or viral RNA synthesis of all four serotypes of DENV, but is ineffective against Japanese encephalitis virus. BP13944 may target the DENV NS3 protease, and the E66G amino acid substitution in the NS3 protease region will cause the virus to become resistant to BP13944. BP13944 has no obvious cytotoxicity. As there is currently no effective dengue vaccine and treatment, BP13944, as an effective small molecule inhibitor, may become a potential agent for the treatment of dengue in the future.
|
-
- HY-12033S1
-
2-ME2-13C6; NSC-659853-13C6
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
2-Methoxyestradiol- 13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-164978
-
|
Kinesin
|
Cancer
|
KIF18A-IN-14 (Compound Example 81) is a KIF18A inhibitor. KIF18A-IN-14 is available in two forms, EX81-A and its enantiomer EX81-B. EX81-A and EX81-B inhibit OVCAR-3 cells viability with IC50s of 0-0.01 μM and 0.01-0.1 μM, respectively. KIF18A-IN-14 can be used in tumor (e.g. colon, breast, lung) studies .
|
-
- HY-12033S2
-
2-ME2-d5; NSC-659853-d5
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
2-Methoxyestradiol-d5 is the deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-W011428
-
|
CDK
|
Others
Cancer
|
Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 μM), CDK/p35 kinase (IC50=3 μM) and ERK1/p44 MAP kinase (IC50=25 μM) . Olomoucine regulates cell cycle and shows anti-melanin tumor activity .
|
-
- HY-134903
-
|
mTOR
|
Cancer
|
(32-Carbonyl)-RMC-5552 is a potent mTOR inhibitor. (32-Carbonyl)-RMC-5552 inhibits mTORC1 and mTORC2 substrate (p-P70S6K-(T389), p-4E-BP1-(T37/36), AND p-AKT1/2/3-(S473)) phosphorylation with pIC50s of > 9, >9 and between 8 and 9, respectively (patent WO2019212990A1, example 2) .
|
-
- HY-W653962
-
|
Isotope-Labeled Compounds
Apoptosis
Antibiotic
Fungal
Bacterial
|
Infection
Cancer
|
Triclosan- 13C6 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-W747491
-
|
Isotope-Labeled Compounds
Antibiotic
Apoptosis
Bacterial
Fungal
|
Cancer
|
Triclosan- 13C12 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-B0507A
-
|
Antibiotic
Bacterial
|
Endocrinology
Cancer
|
Sulfathiazole sodium is an orally active, endocrine disruptor targeting the steroidogenic pathway, specifically enhancing the activity of CYP19 in human adrenal cancer cells (H295R) and upregulating the mRN expression of CYP17, CYP19, and 3β-HSD. Sulfathiazole sodium increases the production of 17-estradiol (E2) and has endocrine disrupting effects on aquatic organisms such as the Japanese medaka fish. Sulfathiazole sodium is also a cathodic corrosion inhibitor. It inhibits the corrosion of copper by chloride ions through chemical and physical adsorption on the copper surface, reduces the corrosion current density and shifts the corrosion potential negatively .
|
-
- HY-B1119R
-
|
Reference Standards
Bacterial
Fungal
Antibiotic
Apoptosis
|
Infection
Cancer
|
Triclosan (Standard) is the analytical standard of Triclosan. This product is intended for research and analytical applications. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-167673
-
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
Cancer
|
RNF5-IN-1 (FX12) is a selective RNF5 degrader. RNF5-IN-1 binds to RNF5 and inhibits its E3 activity, and promotes proteasomal degradation of RNF5 in an endoplasmic reticulum (ER)-associated degradation (ERAD) way in cells. RNF5-IN-1 inhibits α-1-antitrypsin (NHK) dislocation with an IC50 value of 2.7 μM. RNF5-IN-1 can be used for research of cystic fibrosis, acute myeloid leukemia, and certain viral infections .
|
-
- HY-159898
-
|
Cholinesterase (ChE)
Amyloid-β
Tau Protein
NOD-like Receptor (NLR)
Reactive Oxygen Species
Mitochondrial Metabolism
|
Neurological Disease
|
AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model .
|
-
- HY-169177
-
|
JNK
|
Inflammation/Immunology
|
JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
|
-
- HY-168963
-
|
PROTACs
Btk
Itk
p38 MAPK
|
Inflammation/Immunology
Cancer
|
PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway . (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
|
-
- HY-10424R
-
PHA-848125 (Standard)
|
CDK
Autophagy
|
Cancer
|
Milciclib (Standard) is the analytical standard of Milciclib. This product is intended for research and analytical applications. Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
|
-
- HY-10581CR
-
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
Inflammation/Immunology
|
Gatifloxacin (sesquihydrate) (Standard) is the analytical standard of Gatifloxacin (sesquihydrate). This product is intended for research and analytical applications. Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml) . Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis?in vivo.
|
-
- HY-W013268
-
(+)-N-3-Benzylnirvanol
|
Cytochrome P450
|
Metabolic Disease
|
(S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 .
|
-
- HY-168551
-
|
PROTACs
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
PROTAC ALK degrader-3 (4B) is an orally active ALK degrader based on PROTACs, which can effectively induce persistent degradation of ALK fusion protein in Karpas 299 cells and strong inhibition of downstream pathways,IC50 is 119.33 nM. PROTAC ALK degrader-3 exhibits antitumor activity. (Structure Note: PINK, ALK Inhibitor (HY-15656); Blue, E3 (HY-W023573); Black, linker (HY-168552)) .
|
-
- HY-161498
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
XYD198 (Compound 14h) is an orally active degrader for CBP/p300. XYD198 inhibits CBP/p300 bromodomain with IC50 of 213.5 nM. XYD198 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161499))
|
-
- HY-161494
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)) .
|
-
- HY-160876
-
|
Keap1-Nrf2
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury .
|
-
- HY-W019806
-
LNFP I
|
Endogenous Metabolite
CDK
Reactive Oxygen Species
Apoptosis
Enterovirus
Bacterial
|
Infection
Inflammation/Immunology
|
Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development .
|
-
- HY-W844796
-
(S)-2-Amino-5-methylhex-5-enoic acid
|
Bacterial
Amino Acid Derivatives
|
Infection
|
2-Amino-5-methyl-5-hexenoic acid ((S)-2-Amino-5-methylhex-5-enoic acid) is a Methionine analog that competes with methionine and resulting in inhibition of cell growth. 2-Amino-5-methyl-5-hexenoic acid inhibits protein synthesis but not DNA or RNA synthesis in S. typhimurium TA1535 and E. coli K-12 .
X
|
-
- HY-125810
-
|
HIV
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-124379
-
TPCK
1 Publications Verification
L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK
|
Ser/Thr Protease
HPV
Apoptosis
PDK-1
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is an effective serine protease inhibitor and also a blocker of the PDK1/Akt pathway. TPCK can modify the E7 protein in actively keratinocyte cells. TPCK can induce cellular apoptosis, suppress tumor growth, reduce hypoxic-ischemic brain injury in rat pups, and affect vascular permeability in inflamed rats .
|
-
- HY-144269
-
|
Raf
|
Cancer
|
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
|
-
- HY-163705
-
|
PROTACs
FGFR
|
Cancer
|
BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717))
|
-
- HY-B2228
-
|
Biochemical Assay Reagents
|
Cancer
|
Proteinase, Aspergillus oryzae is a serine protease that hydrolyzes peptide bonds in protein substrates, preferring alkaline conditions (optimal pH 10.5). It efficiently degrades casein, poly-L-glutamic acid, and poly-L-lysine, with activity irreversibly inhibited by diisopropylfluorophosphate (DFP) and potato inhibitor. This enzyme catalyzes proteolysis via serine residues in its active site, finding applications in food processing (e.g., soy sauce fermentation), detergents, and leather industries due to its high yield in solid-state fermentation and cost-effective production.
|
-
- HY-170343
-
|
PROTACs
SWI/SNF Complex
|
Cancer
|
PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM . (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
|
-
- HY-168242
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC BRM/BRG1 degrader-1 (Example 253) is a PROTAC BRM/BRG1 degrader, with DC50 of 10-100 nM for BRM, > 1 μM for BRG1. PROTAC BRM/BRG1 degrader-1 can be used for cancer research. Blue: E3 ligase ligand (HY-168243), black: linker (HY-168244). Red: BRM/BRG1 inhibitor (HY-W539427) .
|
-
- HY-158328A
-
-
- HY-150596
-
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-10581R
-
|
Bacterial
Topoisomerase
Antibiotic
|
Infection
|
Gatifloxacin (Standard) is the analytical standard of Gatifloxacin. This product is intended for research and analytical applications. Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml) . Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
|
-
- HY-144749
-
|
Aldose Reductase
|
Cancer
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-172820
-
DP303c
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer .
|
-
- HY-168867
-
|
PROTACs
RET
Apoptosis
|
Cancer
|
RD-23 is an orally active and selective RET PROTAC degrader. RD-23 promotes ubiquitination and degradation of RET G810C mutation, with a DC50 value of 11.7 nM. RD-23 inhibits the activation of downstream Shc signaling and induces Apoptosis. RD-23 can be used for the research of RET-related cancers (Pink: RET ligand-2 (HY-168868); Blue: E3 ligase CRBN ligand; Black: linker) .
|
-
- HY-151916
-
|
Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
|
Cancer
|
Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-1 induces Apoptosis .
|
-
- HY-103636
-
|
Sirtuin
PROTACs
|
Cancer
|
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM) .
|
-
- HY-174086
-
|
Glutathione Peroxidase
Ferroptosis
ROS Kinase
|
Cancer
|
PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)) .
|
-
- HY-157581
-
|
PROTACs
EGFR
|
Cancer
|
MS39 (compound 6) is a PROTAC targeting EGFR. MS39 is composed of PROTAC target protein ligand N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-(piperazin-1-yl)propoxy)quinazolin-4-amine (HY-W109039) (red part), E3 ligase ligand (S,R,S)-AHPC (HY-125845) (blue part) and PROTAC Linker Undecanedioic acid (HY-W014125) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-CO-C9-acid (HY-139345). MS39 reduces the expression of EGFR and downstream signaling in HCC-827 and H3255 cells. MS39 inhibits the proliferation of H3255 cells .
|
-
- HY-157213
-
|
Apoptosis
PROTACs
FLT3
|
Cancer
|
LWY713 is a PROTAC-class FLT3 degrader (DC50=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).
|
-
- HY-134807
-
|
P2X Receptor
5-HT Receptor
Autophagy
|
Cancer
|
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
|
-
- HY-119271A
-
(-)-SDS-1-021
|
c-Myc
Apoptosis
|
Cancer
|
(-)-CMLD010509 ((-)-SDS-1-021) is an isomer of CMLD010509 (SDS-1-021) (HY-119271). CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism .
|
-
- HY-125876
-
|
PROTACs
Bcl-2 Family
|
Cancer
|
PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1 (Blue: CRBN ligand, Black: linker;Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
|
-
- HY-156444
-
|
HDAC
CDK
Apoptosis
|
Cancer
|
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
|
-
- HY-N15267
-
|
FAK
Akt
mTOR
|
Cancer
|
Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
|
-
- HY-101903R
-
|
Reference Standards
FABP
|
Cardiovascular Disease
Metabolic Disease
|
BMS-309403 (Standard) is the analytical standard of BMS-309403. This product is intended for research and analytical applications. BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-173405
-
|
Ras
PI3K
|
Cancer
|
VVD-699 is a covalent RAS-PI3K inhibitor. VVD-699 covalently binds to cysteine 242 in the RAS binding domain of PI3K p110α, thereby blocking the ability of RAS to activate PI3K activity. VVD-699 is able to inhibit the growth of RAS-mutated and HER2-overexpressing tumors. VVD-699 can be used to study cancers associated with RAS mutations (e.g., H358 lung cancer cells, A549 cells, FaDu cells) .
|
-
- HY-170403
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
|
-
- HY-172208
-
|
PROTACs
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
PROTAC cGAS degrader-1 (Compound TH35) is an effective and selective cGAS PROTAC degrader, with DC50 values of 0.9 μM and 4.6 μM in THP-1 and RAW 264.7 cells, respectively. PROTAC cGAS degrader-1 can inhibit the activation of cGAS signaling induced by dsDNA. PROTAC cGAS degrader-1 has anti-inflammatory activity and can be used in the research of cGAS-related inflammatory diseases. (Pink: cGAS inhibitor (HY-133916); Black: Linker (HY-W411604); Blue: E3 ligase ligand (HY-43722))
|
-
- HY-162702
-
|
PROTACs
Androgen Receptor
|
Cancer
|
AZ‘3137 is an orally active PROTAC-type androgen receptor (AR) degrader with a DC50 value of 22 nM. AZ‘3137 can degrade L702H mutant AR (DC50 of 92 nM). AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Pink: AR Ligand (HY-172954); Blue: CRBN ligand (HY-172955); Black: linker (HY-W262798); E3 Ligand+Linker: HY-172956) .
|
-
- HY-164979
-
|
Kinesin
|
Cancer
|
KIF18A-IN-15 (Compound Example 36) is a KIF18A inhibitor, available in two forms, EX36-A and its enantiomer EX36-B, with IC50s of 0.01-0.1 μM, respectively. EX36-A and EX36-B inhibit OVCAR-3 cells viability with IC50s of 0.01-0.1 μM and 0-0.01 μM, respectively. KIF18A-IN-15 can be used in tumor (e.g. colon, breast, lung) studies .
|
-
- HY-101903AR
-
|
Reference Standards
FABP
|
Cardiovascular Disease
Metabolic Disease
|
BMS-309403 (sodium) (Standard) is the analytical standard of BMS-309403 (sodium). This product is intended for research and analytical applications. BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
|
-
- HY-12033S
-
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
2-Methoxyestradiol- 13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .
|
-
- HY-153803
-
|
PROTACs
Molecular Glues
Btk
|
Cancer
|
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
|
-
- HY-164476
-
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-132844
-
HL-085
|
MEK
|
Cancer
|
Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRAS G12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
|
-
- HY-170958
-
|
Src
Apoptosis
|
Cancer
|
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
|
-
- HY-12678S
-
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-N12537A
-
|
Aryl Hydrocarbon Receptor
PD-1/PD-L1
|
Cancer
|
(2R,3S)-PD-1/PD-L1-IN-38 (Compound (±)-13e) is an orally active Ah receptor (AhR) antagonist with in vivo and in vitro anticancer activity. (2R,3S)-PD-1/PD-L1-IN-38 promotes the secretion of INF-γ by CD8 +T cells and inhibits the signal transduction of PD-1/PD-L1 .
|
-
- HY-130241
-
|
HIV
|
Infection
|
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme .
|
-
- HY-A0003
-
CC-5013
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Inflammation/Immunology
Cancer
|
Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
|
-
- HY-172784
-
|
PI3K
Akt
Apoptosis
|
Cancer
|
Anticancer agent 273 (Compound 9q) is a potent anticancer agent found in matrine. Anticancer agent 273 inhibits the proliferation of cancer cells (e.g., HeLa cells with an IC50 value of 4.48 μM). Anticancer agent 273 exerts anticancer effects by modulating the expression of PI3K/AKT and activating transcription factor 4 (ATF4), which promotes endoplasmic reticulum stress and induces apoptosis. Anticancer agent 273 is promising for research of cancers, such as cervical cancer .
|
-
- HY-A0003B
-
CC-5013 hemihydrate
|
Ligands for E3 Ligase
Molecular Glues
Apoptosis
|
Cancer
|
Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells .
|
-
- HY-130122
-
|
Molecular Glues
PROTACs
Apoptosis
|
Cancer
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
|
-
- HY-17598R
-
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
|
-
- HY-12892
-
|
SphK
Apoptosis
|
Cancer
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .
|
-
- HY-46531
-
|
Ligands for E3 Ligase
|
Inflammation/Immunology
Cancer
|
Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1) .
|
-
- HY-N3103
-
Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate
|
Tyrosinase
|
Inflammation/Immunology
|
p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate; Ethyl trans-4-hydroxycinnamate) is a non-competitive, reversible inhibitor of tyrosinase (IC50=4.89 μg/mL, Ki=1.83 μg/mL), which can quench the intrinsic fluorescence of the enzyme. p-Coumaric Acid Ethyl Ester changes the binding affinity of L-tyrosine by inducing conformational changes in the catalytic domain of tyrosinase, and does not bind to the copper ion of the enzyme. p-Coumaric Acid Ethyl Ester is used in the development of medicines, cosmetics and fruit preservation products using pollen .
|
-
- HY-168731
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
AChE/BChE-IN-25 (Compound 6e) is the orally active inhibitor for hAChE and eqBChE with IC50 of 7.9 nM and 0.79 nM. AChE/BChE-IN-25 exhibits antioxidant activity, that scavenges free radical with IC50 of 22.91 μM. AChE/BChE-IN-25 exhibits neuroprotective effects by reducing mitochondrial and cellular oxidative stress in the Drosophila Alzheimer's disease model. AChE/BChE-IN-25 ameliorates Scopolamine (HY-N0296)-induced spatial and cognitive memory impairment in mouse model .
|
-
- HY-168935
-
|
NO Synthase
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
Anti-inflammatory agent 95 (Compound 2e) is an anti-inflammatory agent that exhibits the most potent anti-inflammatory activity in LPS (HY-D1056)-induced RAW 264.7 mouse macrophages.
It significantly inhibits the production of NO, with an IC50 of 8.8 μM, and reduces the secretion of TNF-α and IL-1β, with inhibition rates reaching 60% and over 90%, respectively, at a concentration of 100 μM.
Anti-inflammatory agent 95 holds promise for research in the field of inflammatory diseases .
|
-
- HY-144730
-