Search Result
Results for "A-Kinase-Anchoring Proteins Inhibitors" in MCE Product Catalog:
8518
Inhibitors & Agonists
18
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-U00439
-
-
- HY-70027A
-
-
- HY-70027
-
-
- HY-U00439A
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Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
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- HY-131005
-
-
- HY-W013478
-
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- HY-P1376
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G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
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Endocrinology
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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- HY-P1376A
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G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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-
- HY-121879
-
-
- HY-15847
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HS38
|
DAPK
|
Cardiovascular Disease
|
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders.
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- HY-103700B
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(Rac)-Azide-phenylalanine
|
Others
|
Others
|
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins.
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- HY-B0178A
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-
- HY-15890
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-
- HY-B0843
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Metalaxyl
|
Fungal
|
Infection
|
Metalaxyl is a fungicide that inhibits protein synthesis in fungi. Metalaxyl inhibits the growth of potato blight (P. infestans) fungal isolates from Serbian potato fields (EC50s=0.3-3.9 μg/mL).
|
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- HY-P1289
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[Ala113]MBP(104-118)
|
PKC
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Others
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[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM.
|
-
- HY-17561
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G-418 disulfate
Geneticin sulfate; Antibiotic G-418 sulfate
|
Bacterial
Antibiotic
|
Infection
|
G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells.
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- HY-P1289A
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[Ala107]MBP(104-118)
|
PKC
|
Others
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[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM.
|
-
- HY-19373
-
-
- HY-P1289C
-
-
- HY-P1289B
-
-
- HY-136217
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PU 23
|
Others
|
Cancer
|
PU 23 is a non-carboxylic multidrug resistance protein 4 (MRP4) inhibitor as an active agent reducing resistance to anticancer agent 6-Mercaptopurine.
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-
- HY-15435
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CHAPS
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Others
|
Others
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CHAPS, a derivative of Cholic acid, is a zwitterionic detergent for solubilizing membrane proteins. CHAPS is used for stabilization of various protein-DNA complexes and can retain biochemical activity of proteins in solution.
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- HY-126245
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Keap1-Nrf2-IN-1
|
Keap1-Nrf2
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Metabolic Disease
Inflammation/Immunology
|
Keap1-Nrf2-IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models.
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- HY-115467
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MitoBloCK-10
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Others
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Metabolic Disease
|
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70.
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- HY-W012037
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8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
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- HY-18979
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Lactimidomycin
|
Influenza Virus
|
Cancer
Infection
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.
|
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- HY-50730
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Asparagusic acid
|
Parasite
|
Infection
|
Asparagusic acid a sulfur-containing flavor component produced by Asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
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- HY-108136A
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Bisindolylmaleimide X hydrochloride
BIM-X hydrochloride; Ro31-8425 hydrochloride
|
PKC
CDK
|
Cardiovascular Disease
|
Bisindolylmaleimide X hydrochloride (BIM-X hydrochloride) is a potent and selective protein kinase C (PKC) inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC50 of 200 nM.
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- HY-117737A
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RRD-251
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Raf
Apoptosis
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Cancer
|
RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.
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- HY-115292
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Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
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Cancer
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Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
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- HY-P1290
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PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
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PKA
|
Neurological Disease
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
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- HY-125974
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HM03
|
HSP
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Cancer
|
HM03 is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 has anticancer activity.
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- HY-136304
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- HY-116677
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- HY-P1290A
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PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
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- HY-10392
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Sutezolid
PNU-100480; U-100480; PF-02341272
|
Bacterial
Antibiotic
|
Infection
|
Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis.
|
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- HY-B0470
-
Neomycin sulfate
|
Bacterial
Antibiotic
Phospholipase
|
Infection
|
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis.
|
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- HY-135813
-
LtaS-IN-1
|
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.
|
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- HY-P1247
-
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- HY-129337
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Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
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- HY-P1247A
-
-
- HY-125586
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β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
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- HY-101918
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DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-B0239
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Chloramphenicol
|
Bacterial
Antibiotic
|
Infection
|
Chloramphenicol, a broad-spectrum antibiotic, acts as a potent inhibitor of bacterial protein biosynthesis. Chloramphenicol acts primarily on the 50S subunit of bacterial 70S rihosomes and inhibits peptide bond formation by suppressing peptidyl transferase activity.
|
-
- HY-15187
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Filanesib
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.
|
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- HY-115688
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- HY-14165
-
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- HY-16787
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ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
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- HY-18728
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- HY-116144
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Picaridin
Lcaridin
|
Parasite
|
Infection
|
Picaridin (Lcaridin) is a broad spectrum arthropod repellent. The repellent and deterrent activities of Picaridin involve olfactory sensing in mosquitoes, and ticks, via their interactions with odorant receptor proteins.
|
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- HY-P1446
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Cholera toxin
Choleragen
|
Adenylate Cyclase
|
Inflammation/Immunology
|
Cholera toxin (Choleragen), an AB(5)-subunit toxin, enters host cells by binding the ganglioside GM1 at the plasma membrane (PM) and travels retrograde through the trans-Golgi Network into the endoplasmic reticulum (ER). Choleragen activates adenylate cyclase by catalyzing ADP-ribosylation of Gs alpha, the stimulatory guanine nucleotide-binding protein.
|
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- HY-19313
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LLY-507
|
Histone Methyltransferase
|
Cancer
|
LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
|
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- HY-17389
-
Genipin
(+)-Genipin
|
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.
|
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- HY-125957
-
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-B0275
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Oxytetracycline
|
Bacterial
HSV
Endogenous Metabolite
Antibiotic
|
Infection
|
Oxytetracycline is an antibiotic belonging to the tetracycline class. Oxytetracycline potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline also possesses anti-HSV-1 activity.
|
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- HY-B0275A
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Oxytetracycline hydrochloride
|
Bacterial
HSV
Antibiotic
Endogenous Metabolite
|
Infection
|
Oxytetracycline hydrochloride is an antibiotic belonging to the tetracycline class. Oxytetracycline hydrochloride potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline hydrochloride is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline hydrochloride also possesses anti-HSV-1 activity.
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-
- HY-113025A
-
L-hydroxylysine dihydrochloride
(2S,5R)-5-Hydroxylysine dihydrochloride
|
Endogenous Metabolite
|
Others
|
L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues.
|
-
- HY-19614
-
BMS-795311
|
CETP
|
Cardiovascular Disease
|
BMS-795311 is a potent and orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP), with IC50s of 4 nM in an enzyme-based scintillation proximity assay (SPA) and 0.22 μM in a human whole plasma assay (hWPA), respectively.
|
-
- HY-43722
-
Lenalidomide-Br
|
Ligand for E3 Ligase
|
Cancer
|
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
|
-
- HY-W008990
-
Xanthosine 5'-monophosphate sodium salt
5'-Xanthylic acid sodium salt
|
Others
|
Metabolic Disease
|
Xanthosine 5'-monophosphate sodium salt (5'-Xanthylic acid sodium salt) is an intermediate in purine metabolism. Xanthosine 5'-monophosphate sodium salt can be used for genetic code, nucleic acid structure, and DNA, RNA and protein synthesis research.
|
-
- HY-B0275B
-
Oxytetracycline dihydrate
|
Bacterial
HSV
Antibiotic
Endogenous Metabolite
|
Infection
|
Oxytetracycline dihydrate is an antibiotic belonging to the tetracycline class. Oxytetracycline dihydrate potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline dihydrate is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline dihydrate also possesses anti-HSV-1 activity.
|
-
- HY-124806
-
TTP-8307
|
Enterovirus
DNA/RNA Synthesis
HCV
|
Infection
|
TTP-8307 is a potent inhibitor of the replication of several rhino- and enteroviruses. TTP-8307 inhibits coxsackievirus B3 (CVB3; EC50=1.2 μM) and poliovirus by interfering with the synthesis of viral RNA. TTP-8307 exerts antiviral activity through oxysterol-binding protein (OSBP).
|
-
- HY-N4136
-
Lonicerin
|
Bacterial
Apoptosis
|
Infection
|
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitory activity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury.
|
-
- HY-18962
-
AMI-1
|
Histone Methyltransferase
|
Cancer
|
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
|
-
- HY-17480
-
Bendazac
|
Others
|
Inflammation/Immunology
|
Bendazac is an oxyacetic acid with anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties. Bendazac acts by preventing protein denaturation and delays the cataractogenic process.
|
-
- HY-120072
-
PF-3450074
PF-74
|
HIV
|
Infection
|
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
|
-
- HY-B0220
-
Erythromycin
|
Bacterial
Antibiotic
|
Infection
|
Erythromycin is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-15583
-
-
- HY-18962A
-
AMI-1 free acid
|
Histone Methyltransferase
|
Cancer
|
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding.
|
-
- HY-W087383
-
-
- HY-18572A
-
2,4-D sodium salt
Sodium 2,4-dichlorophenoxyacetate; 2,4-Dichlorophenoxyacetic acid sodium salt
|
DNA/RNA Synthesis
|
Others
|
2,4-D sodium salt (Sodium 2,4-dichlorophenoxyacetate) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D sodium salt acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D sodium salt inhibits DNA and protein synthesis and thereby prevents normal plant growth and development.
|
-
- HY-18572
-
2,4-D
2,4-Dichlorophenoxyacetic acid
|
DNA/RNA Synthesis
|
Others
|
2,4-D (2,4-Dichlorophenoxyacetic acid) is a selective systemic herbicide for the control of broad-leaved weeds. 2,4-D acts as a plant hormone, causing uncontrolled growth in the meristematic tissues. 2,4-D inhibits DNA and protein synthesis and thereby prevents normal plant growth and development.
|
-
- HY-103374
-
Phenserine
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
AChE
Amyloid-β
|
Neurological Disease
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-129624A
-
Bisindolylmaleimide VIII acetate
Ro 31-7549 acetate; Bis VIII acetate
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
|
-
- HY-122470
-
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-B0220E
-
Erythromycin A dihydrate
|
Bacterial
Antibiotic
|
Infection
|
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-125837A
-
MS31 trihydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells.
|
-
- HY-106443A
-
-
- HY-18669
-
ML346
|
HSP
|
Cancer
|
ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70. ML346 restores protein folding in conformational disease models, without significant cytotoxicity or lack of specificity. ML346 induces specific increases in genes and protein effectors of the heat shock response (HSR), including chaperones such as Hsp70, Hsp40, and Hsp27.
|
-
- HY-126323
-
TCMDC-135051
|
Parasite
|
Infection
|
TCMDC-135051 is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 has antiparasiticidal activity (EC50=320 nM).
|
-
- HY-126323B
-
TCMDC-135051 hydrochloride
|
Parasite
|
Infection
|
TCMDC-135051 hydrochloride is a highly selective and potent protein kinase PfCLK3 inhibitor with low off-target toxicity. TCMDC-135051 hydrochloride prevents trophozoite-to-schizont transition, disrupts transcription and reduces transmission to the mosquito vector. TCMDC-135051 hydrochloride has antiparasiticidal activity (EC50=320 nM).
|
-
- HY-W042156
-
Aegeline
|
Fungal
|
Neurological Disease
|
Aegeline, a main alkaloid, mimics the yeast SNARE protein Sec22p in suppressing α-synuclein and Bax toxicity in yeast. Aegeline restores growth of yeast cells suppressed by either αsyn or Bax. Antioxidant activity.
|
-
- HY-P1318
-
Ac-RYYRIK-NH2
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-106443
-
-
- HY-B0509
-
Amikacin hydrate
BAY 41-6551 hydrate
|
Bacterial
Antibiotic
|
Infection
|
Amikacin hydrate (BAY 41-6551 hydrate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin hydrate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin hydrate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin hydrate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
|
-
- HY-N1347
-
Robinetin
3,3',4',5',7-Pentahydroxyflavone
|
Fungal
HIV Integrase
Bacterial
|
Infection
|
Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation.
|
-
- HY-106443B
-
-
- HY-P1318A
-
Ac-RYYRIK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-121750
-
CCG-222740
|
Ras
ROCK
|
Cancer
|
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
|
-
- HY-11007
-
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-N6785
-
Okadaic acid
|
Phosphatase
Parasite
Apoptosis
|
Infection
|
Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively. Okadaic acid eliminate metazoan symbionts/parasites by apoptosis.
|
-
- HY-B0509B
-
Amikacin disulfate
BAY 41-6551 disulfate
|
Bacterial
Antibiotic
|
Infection
|
Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
|
-
- HY-107813
-
Amikacin sulfate
BAY 41-6551 sulfate
|
Bacterial
Antibiotic
|
Infection
|
Amikacin sulfate (BAY 41-6551 sulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin sulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin sulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin sulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria.
|
-
- HY-130354
-
Dibutyryl-cGMP sodium
Bt2cGMP sodium
|
Potassium Channel
|
Cardiovascular Disease
|
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels.
|
-
- HY-W002820
-
2-Amino-5-phenylpyridine
|
Endogenous Metabolite
|
Cancer
|
2-Amino-5-phenylpyridine is a mutagenic heterocyclic aromatic amine that is formed by pyrolysis of phenylalanine in proteins. 2-Amino-5-phenylpyridine is in broiled sardines and is considered as potentially carcinogenic.
|
-
- HY-18619
-
YL-109
|
Aryl Hydrocarbon Receptor
|
Cancer
|
YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness.
|
-
- HY-111285
-
HAMNO
NSC111847
|
Others
|
Cancer
|
HAMNO is a novel protein interaction inhibitor of replication protein A (RPA).
|
-
- HY-100430
-
CCF642
|
Others
|
Cancer
|
CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity.
|
-
- HY-W014102
-
-
- HY-136528
-
RA-9
|
Deubiquitinase
Apoptosis
|
Cancer
|
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
|
-
- HY-107116
-
MAP4343
|
Microtubule/Tubulin
|
Neurological Disease
|
MAP4343 is the 3-methylether derivative of Pregnenolone. MAP4343 binds in vitro to microtubule-associated protein 2 (MAP2), stimulates the polymerization of tubulin, enhances the extension of neurites and protects neurons against neurotoxic agents.
|
-
- HY-70075
-
-
- HY-130979
-
-
- HY-101453
-
Ceefourin 1
|
Others
|
Cancer
|
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma.
|
-
- HY-109565
-
ASTX660
|
IAP
|
Cancer
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-A0122
-
-
- HY-113534
-
MV1
|
IAP
Apoptosis
|
Others
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand.
|
-
- HY-13313
-
XL888
|
HSP
|
Cancer
|
XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.
|
-
- HY-117015
-
Purfalcamine
|
Parasite
|
Infection
|
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage.
|
-
- HY-50882
-
ELN318463
|
γ-secretase
|
Neurological Disease
|
ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC50s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.
|
-
- HY-N5118
-
Chimonanthine
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
|
-
- HY-134592
-
-
- HY-16657
-
-
- HY-U00431
-
-
- HY-P2260
-
Tat-beclin 1
|
Autophagy
HIV
|
Infection
|
Tat-beclin 1, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
|
-
- HY-129239
-
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. ASLAN003 inhibits protein synthesis via activation of AP-1 transcription factors. ASLAN003 induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-110173
-
TC-G 1005
|
GPCR19
|
Metabolic Disease
|
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
|
-
- HY-112504A
-
-
- HY-100457
-
-
- HY-W015445
-
SD-169
|
p38 MAPK
|
Metabolic Disease
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-P1746A
-
Protein Kinase C (19-31) (TFA)
PKC (19-31) (TFA)
|
PKC
|
Inflammation/Immunology
|
Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-P1746
-
Protein Kinase C (19-31)
PKC (19-31)
|
PKC
|
Inflammation/Immunology
|
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-101503
-
HTS01037
|
FABP
|
Metabolic Disease
|
HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
|
-
- HY-19761
-
-
- HY-19541
-
-
- HY-13518
-
-
- HY-B0472
-
-
- HY-111872
-
SNIPER(ABL)-020
|
SNIPER
Bcr-Abl
|
Cancer
|
SNIPER(ABL)-020, conjugating Dasatinib (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein.
|
-
- HY-14657
-
-
- HY-100862
-
BRCA1-IN-2
|
PARP
|
Cancer
|
BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions.
|
-
- HY-107597
-
SU3327
|
JNK
|
Metabolic Disease
Inflammation/Immunology
|
SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
|
-
- HY-59354
-
Maleic hydrazide
|
DNA/RNA Synthesis
|
Cancer
|
Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins.
|
-
- HY-100984
-
HA-100
|
PKA
PKC
Myosin
|
Cancer
|
HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase with IC50s of 4, 8, 12 and 240 μM, respectively.
|
-
- HY-114189
-
GW284543
UNC10225170
|
MEK
|
Cancer
|
GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein.
|
-
- HY-111858
-
-
- HY-P0222
-
PKI(5-24)
|
PKA
|
Others
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-U00329
-
-
- HY-106130
-
-
- HY-10183
-
-
- HY-N0082
-
-
- HY-15870
-
SR 11302
|
Others
|
Cancer
Inflammation/Immunology
|
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-114657A
-
Benproperine phosphate
|
Arp2/3 Complex
|
Cancer
Inflammation/Immunology
|
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.
|
-
- HY-14393
-
Emodin
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
|
Cancer
|
Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
|
-
- HY-P1045
-
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1045A
-
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-19991
-
-
- HY-B1228
-
Ribostamycin sulfate
Vistamycin sulfate
|
Bacterial
Antibiotic
|
Infection
|
Ribostamycin sulfate (Vistamycin sulfate) is a broad-spectrum antimicrobial, inhibits bacterial protein synthesis at the level of 30S and 50S ribosomal subunit binding, also inhibits the chaperone activity of protein disulfide isomerase (PDI), used in pharmacokinetic and nephrotoxicity studies
|
-
- HY-P0222A
-
PKI(5-24) TFA
|
PKA
|
Others
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.
|
-
- HY-B1743A
-
-
- HY-50759
-
-
- HY-133248
-
-
- HY-133247
-
-
- HY-15979
-
H-89
|
PKA
Autophagy
|
Neurological Disease
|
H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
|
-
- HY-16786
-
AI-10-49
|
Others
|
Cancer
|
AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.
|
-
- HY-P1401
-
Protein Kinase C (19-36)
|
PKC
|
Metabolic Disease
|
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response.
|
-
- HY-D1270
-
Direct Violet 1
|
SARS-CoV
|
Infection
|
Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 µM.
|
-
- HY-128347
-
-
- HY-122862
-
RAS inhibitor Abd-7
|
Ras
|
Cancer
|
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.
|
-
- HY-B1358
-
-
- HY-128853
-
-
- HY-13502
-
-
- HY-13502A
-
-
- HY-111117
-
-
- HY-U00270
-
-
- HY-N0193
-
-
- HY-101525
-
-
- HY-15300
-
-
- HY-10499
-
-
- HY-100496
-
Nucleocidin
4'-Fluoro-5'-O-sulfamoyladenosine; NSC 521007
|
Bacterial
|
Infection
|
Nucleocidin is an antitrypanosomal antibiotic, inhibiting the transfer of labeled amino acid from S-RNA to protein.
|
-
- HY-112258
-
IMP-1088
|
DNA/RNA Synthesis
|
Infection
|
IMP-1088 is a potent human N-myristoyltransferases NMT1 and NMT2 dual inhibitor with IC50s of <1 nM for HsNMT1 and HsNMT2. IMP-1088 has a Kd of <210 pM for HsNMT1. IMP-1088 efficiently blocks rhinovirus replication by blocking rhinovirus virus-encoded protein (VP0) N-myristoylation. IMP-1088 protects host cells from the cytotoxic effects of viral infection.
|
-
- HY-18983
-
Calyculin A
(-)-Calyculin A
|
Phosphatase
|
Cancer
|
Calyculin A ((-)-Calyculin A) is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM, respectively.
|
-
- HY-108391
-
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Apoptosis
PKC
Autophagy
|
Cancer
Inflammation/Immunology
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
|
-
- HY-N2036
-
Mosloflavone
|
Enterovirus
Bacterial
|
Infection
|
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
|
-
- HY-17640
-
-
- HY-102059
-
-
- HY-130839
-
-
- HY-W010128
-
-
- HY-15857
-
CW-069
|
Kinesin
|
Cancer
|
CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC50 of 75 μM.
|
-
- HY-12312
-
-
- HY-100025A
-
-
- HY-19810
-
-
- HY-101295
-
Pan-RAS-IN-1
|
Ras
|
Cancer
|
Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.
|
-
- HY-B0408A
-
-
- HY-128642
-
FAPI-2
|
Others
|
Cancer
|
FAPI-2 is a fibroblast activation protein (FAP) inhibitor for cancer research.
|
-
- HY-138295
-
KRAS inhibitor-10
|
Ras
|
Cancer
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- HY-133735A
-
GRP-60367 hydrochloride
|
Others
|
Infection
|
GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein.
|
-
- HY-100341
-
M2I-1
|
Others
|
Others
|
M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC).
|
-
- HY-111489B
-
-
- HY-D0852
-
Sodium orthovanadate
|
Phosphatase
|
Cancer
|
Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
|
-
- HY-N2301
-
-
- HY-16587
-
Saridegib
IPI-926; Patidegib
|
Smo
|
Cancer
|
Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway.
|
-
- HY-16207
-
-
- HY-14987
-
-
- HY-128643
-
FAPI-4
|
Others
|
Cancer
|
FAPI-4 is a fibroblast activation protein (FAP) inhibitor used in cancer research.
|
-
- HY-13250
-
Silvestrol aglycone
|
Others
|
Cancer
|
Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
|
-
- HY-111192
-
IPR-803
|
Ser/Thr Protease
|
Cancer
|
IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity.
|
-
- HY-12762
-
QS11
|
Others
|
Cancer
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-P1420
-
TAT-cyclo-CLLFVY
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
|
-
- HY-18982
-
Anisomycin
Flagecidin; Wuningmeisu C
|
DNA/RNA Synthesis
JNK
Bacterial
Apoptosis
Antibiotic
|
Cancer
Infection
|
Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic isolated from Streptomyces griseolus.
|
-
- HY-15886
-
-
- HY-125269
-
TED-347
|
YAP
|
Cancer
|
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity.
|
-
- HY-77048
-
IRAK-4 protein kinase inhibitor 2
|
IRAK
|
Inflammation/Immunology
|
IRAK-4 protein kinase inhibitor 2 (compound 1) is a potent inhibitor of interleukin-1 (IL-1) receptor-associated kinase-4 (IRAK-4), with an IC50 of 4 μM. IRAK-4 protein kinase inhibitor 2 can be used for the research of inflammatory and immune-related conditions or disorders.
|
-
- HY-16592
-
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-15450A
-
INCB 3284
|
CCR
|
Endocrinology
|
INCB 3284 is a potent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 can be used in the research of acute liver failure.
|
-
- HY-19319
-
-
- HY-100527
-
AN2718
|
Fungal
|
Infection
|
AN2718 inhibits fungal growth by blocking protein synthesis using the oxaborole tRNA trapping (OBORT) mechanism.
|
-
- HY-111744
-
-
- HY-100464
-
tBID
|
DYRK
|
Cancer
|
tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 µM.
|
-
- HY-13433
-
-
- HY-N7089
-
Benzoyleneurea
|
Bacterial
|
Infection
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-10542A
-
(Z)-GW 5074
|
Raf
|
Neurological Disease
|
(Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder.
|
-
- HY-12825
-
BHPI
|
Estrogen Receptor/ERR
|
Cancer
|
BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
|
-
- HY-14443
-
XMD8-92
|
ERK
Epigenetic Reader Domain
|
Cancer
|
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.
|
-
- HY-101512
-
A-395
|
Histone Methyltransferase
|
Cancer
|
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
|
-
- HY-P1191
-
JIP-1(153-163)
T1-JIP
|
JNK
|
Others
|
JIP-1(153-163) (TI-JIP) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-19764
-
GSK2983559 active metabolite
|
RIP kinase
|
Cancer
|
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
|
-
- HY-W041994
-
GMBS
|
Others
|
Cancer
|
GMBS is a heterobifunctional cross-linker. GMBS can be used in chemical cross-linking of proteins coupled with mass spectrometry (CXMS) to study protein folding and to map the interfaces between interacting proteins.
|
-
- HY-100222
-
CZ415
|
mTOR
|
Cancer
|
CZ415 is a potent and highly selective mTOR inhibitor with a pIC50 of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.
|
-
- HY-12622
-
HSP70-IN-1
|
HSP
|
Cancer
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
|
-
- HY-133246
-
-
- HY-12479A
-
Epetraborole hydrochloride
GSK2251052 hydrochloride
|
Bacterial
|
Infection
|
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".
|
-
- HY-126146
-
-
- HY-14775
-
Nesbuvir
HCV-796
|
HCV
|
Infection
|
Nesbuvir is a nonnucleoside inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase.
|
-
- HY-114439
-
MtbHU-IN-1
|
Bacterial
|
Infection
|
MtbHU-IN-1 is an inhibitor of Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU), with a Kd of 98 nM for binding to WT MtbHU.
|
-
- HY-B0974
-
-
- HY-17412
-
-
- HY-120179A
-
LP-922761 hydrate
|
Others
|
Neurological Disease
|
LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-120179
-
LP-922761
|
Others
|
Neurological Disease
|
LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
|
-
- HY-18370
-
-
- HY-100869A
-
MM-589 TFA
|
Histone Methyltransferase
|
Cancer
|
MM-589 TFA is a potent inhibitor of WD repeat domain 5 (WDR5) and mixed lineage leukemia (MLL) protein-protein interaction. MM-589 binds to WDR5 with an IC50 of 0.90 nM and inhibits the MLL H3K4 methyltransferase activity with an IC50 of 12.7 nM.
|
-
- HY-P1052
-
Myelin Basic Protein(87-99)
|
Others
|
Inflammation/Immunology
|
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
|
-
- HY-107643
-
Reversan
CBLC4H10
|
P-glycoprotein
|
Cancer
|
Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
|
-
- HY-100737
-
ML349
|
Phospholipase
|
Cancer
|
ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
|
-
- HY-50714
-
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-13327
-
Evacetrapib
LY2484595
|
CETP
|
Cardiovascular Disease
|
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.
|
-
- HY-111621
-
DC661
|
Autophagy
Apoptosis
|
Cancer
|
DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
|
-
- HY-P1191A
-
JIP-1(153-163) TFA
T1-JIP TFA
|
JNK
|
Others
|
JIP-1(153-163) TFA (TI-JIP TFA) is a peptide inhibitor of c-JNK, based on residues 153-163 of JNK-interacting protein-1 (JIP-1) (Modifications: Phe-11 = C-terminal amide).
|
-
- HY-B0027
-
-
- HY-13867
-
-
- HY-101770
-
-
- HY-13949
-
SRPIN340
SRPK inhibitor
|
SRPK
Virus Protease
|
Cancer
|
SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
|
-
- HY-N0242
-
-
- HY-13992
-
AP20187
B/B Homodimerizer
|
FKBP
|
Metabolic Disease
|
AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
|
-
- HY-124718
-
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-112210
-
Shield-1
|
FKBP
|
Others
|
Shield-1 is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize the entire fusion protein.
|
-
- HY-10087
-
Navitoclax
ABT-263
|
Bcl-2 Family
|
Cancer
|
Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.
|
-
- HY-16663
-
ITX3
|
Others
|
Others
|
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.
|
-
- HY-100235
-
-
- HY-100390
-
(S)-ML753286
|
BCRP
|
Cancer
|
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
|
-
- HY-116788
-
Lipofermata
|
Others
|
Cancer
|
Lipofermata is a fatty acid transport proteins (FATP) inhibitor that abrogates lipid transport into melanoma cells and reduces melanoma growth and invasion.
|
-
- HY-N0083
-
-
- HY-14667
-
Lomitapide
AEGR-733; BMS-201038
|
Others
|
Cardiovascular Disease
|
Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
|
-
- HY-U00460
-
-
- HY-N2506
-
-
- HY-133083
-
BAY-474
|
c-Met/HGFR
|
Cancer
|
BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
|
-
- HY-16927
-
-
- HY-U00070
-
Dirlotapide
CP742033; Slentrol
|
Others
|
Metabolic Disease
|
Dirlotapide (CP742033) is a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) that reliably produces weight loss in obese dogs.
|
-
- HY-115496
-
-
- HY-N0774
-
Isofraxidin
|
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
|
-
- HY-P2503
-
-
- HY-131132A
-
-
- HY-120859
-
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-19805
-
STO-609
|
CaMK
AMPK
Autophagy
|
Metabolic Disease
|
STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
|
-
- HY-114166
-
-
- HY-50908
-
Ridaforolimus
MK-8669; Deforolimus; AP23573
|
mTOR
Autophagy
|
Cancer
|
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
|
-
- HY-12801
-
DiZPK
|
Others
|
Others
|
DiZPK is a photocrosslinker for identifying direct protein-protein interactions in living prokaryotic and eukaryotic cells.
|
-
- HY-15317
-
RI-1
|
RAD51
|
Cancer
|
RI-1 is a RAD51 inhibitor, with IC50s ranging from 5 to 30 μM. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319. RI-1 inactivates RAD51 by directly binding to a protein surface that serves as an interface between protein subunits in RAD51 filaments. RI-1 can disrupt homologous recombination in human cells.
|
-
- HY-15873
-
-
- HY-15979A
-
H-89 dihydrochloride
|
PKA
Autophagy
|
Others
|
H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
|
-
- HY-N0862
-
-
- HY-108330
-
AG126
Tyrphostin AG126
|
ERK
|
Inflammation/Immunology
|
AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
|
-
- HY-122913
-
Borussertib
|
Akt
|
Cancer
|
Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt.
|
-
- HY-12241
-
AZ82
|
Kinesin
|
Cancer
|
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
|
-
- HY-16586
-
-
- HY-119254
-
BAY-850
|
Others
|
Metabolic Disease
|
BAY-850 is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC50 of 166 nM.
|
-
- HY-14668
-
-
- HY-N6789
-
-
- HY-13820
-
-
- HY-B1425
-
-
- HY-15096
-
MKT-077
FJ-776
|
HSP
|
Cancer
|
MKT-077 is a rhodacyanine dye and also a heat shock protein 70 (Hsp70) inhibitor which exhibits significant antitumor activity.
|
-
- HY-111557
-
YM-254890
|
P2Y Receptor
|
Cardiovascular Disease
|
YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
|
-
- HY-100625
-
-
- HY-N2403
-
Dihydrolycorine
|
Others
|
Neurological Disease
|
Dihydrolycorine is isolated from Lycoris radiate Herb with antihypertensive and neuroprotective activities. Dihydrolycorine is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step.
|
-
- HY-109142
-
Ziresovir
AK0529; RO-0529
|
RSV
|
Infection
|
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species.
|
-
- HY-133953
-
-
- HY-137179
-
Glyco-diosgenin
|
Others
|
Others
|
Glyco-diosgenin is a synthetic surfactant and detergent for extracting proteins from membranes for structure and function studies, and single-particle cryo-electron microscopy (cryoEM) studies of membrane proteins.
|
-
- HY-112610
-
CF53
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
|
-
- HY-N0005
-
Curcumin
Diferuloylmethane; Natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Cancer
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-117626
-
LP-935509
|
Others
|
Inflammation/Immunology
Neurological Disease
|
LP-935509 is a selective, ATP-competitive and brain-penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with an IC50 and a Ki of 3.3 nM and 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure.
|
-
- HY-N6796
-
Manumycin A
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
|
Cancer
Infection
|
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
|
-
- HY-107096
-
CH-0793076
TP3076
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-12830
-
M-110
|
Pim
|
Cancer
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
|
-
- HY-18986
-
-
- HY-112654
-
-
- HY-117286
-
(S)-JQ-35
TEN-010
|
Epigenetic Reader Domain
|
Cancer
|
(S)-JQ-35 (TEN-010) is an inhibitor of the Bromodomain and Extra-Terminal (BET) family bromodomain-containing proteins with potential antineoplastic activity.
|
-
- HY-136434
-
m-Chloramphenicol
m-threo-Chloramphenicol
|
Others
|
Others
|
m-Chloramphenicol (m-threo-Chloramphenicol) is an impurity of Chloramphenicol. Chloramphenicol, a broad-spectrum antibiotic, acts as a potent inhibitor of bacterial protein biosynthesis.
|
-
- HY-18072
-
GSK2606414
|
PERK
Autophagy
Apoptosis
|
Cancer
|
GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
|
-
- HY-135301
-
-
- HY-112782
-
-
- HY-101524
-
-
- HY-138202
-
-
- HY-15205
-
Ganetespib
STA-9090
|
HSP
Apoptosis
|
Cancer
|
Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
|
-
- HY-12588
-
Thiamet G
|
Autophagy
|
Cancer
|
Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.
|
-
- HY-100462
-
-
- HY-N2065
-
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-19530
-
PF-2771
|
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-103097
-
ST271
|
Phospholipase
|
Others
|
ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
|
-
- HY-115688A
-
(S)-TXNIP-IN-1
|
Others
|
Others
|
(S)-TXNIP-IN-1 is the less active S-enantiomer of TXNIP-IN-1 (HY-115688). TXNIP-IN-1 is a TXNIP-TRX complex inhibitor which can be used in the research of TXNIP-TRX complex associated metabolic disorder (diabetes), cardiovascular disease, or inflammatory disease
|
-
- HY-N2098
-
Obtusifolin
|
NF-κB
|
Cancer
|
Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway. Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein.
|
-
- HY-130613
-
MAC-545496
|
Bacterial
|
Infection
|
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
|
-
- HY-116999
-
IR415
|
HBV
|
Infection
|
IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
|
-
- HY-15295
-
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-N4317
-
Ethoxysanguinarine
|
Apoptosis
|
Cancer
|
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine inhibits viability and induces apoptosis of colorectal cancer cells by inhibiting protein phosphatase 2A (CIP2A).
|
-
- HY-N6684
-
Deoxynivalenol
|
Others
|
Metabolic Disease
|
Deoxynivalenol, a mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors.
|
-
- HY-112180
-
JNJ-678
JNJ-53718678
|
RSV
|
Infection
|
JNJ-678 (JNJ-53718678) is a novel fusion protein inhibitor. JNJ-678 has the potential for respiratory syncytial virus (RSV) treatment.
|
-
- HY-103483
-
-
- HY-15187A
-
(R)-Filanesib
(R)-ARRY-520
|
Kinesin
|
Cancer
|
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of Filanesib (HY-15187). Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
|
-
- HY-N1477
-
-
- HY-13442
-
Eribulin
B1939; E7389; ER-086526
|
Microtubule/Tubulin
Apoptosis
|
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-133740
-
MS117
|
Histone Methyltransferase
|
Cancer
|
MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC50 of 18 nM.
|
-
- HY-114349
-
-
- HY-102079
-
-
- HY-101563
-
-
- HY-13343
-
ZM 336372
|
Raf
Apoptosis
|
Cancer
|
ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
|
-
- HY-10394S
-
Linezolid D3
PNU-100766 D3
|
Bacterial
|
Infection
|
Linezolid D3 is a deuterium labeled Linezolid (PNU-100766). Linezolid is a synthetic antibiotic that acts by inhibiting the initiation of bacterial protein synthesis.
|
-
- HY-112438
-
MF-094
|
Deubiquitinase
|
Cancer
|
MF-094 is a potent and selective USP30 inhibitor with an IC50 of 120 nM. MF-094 increases protein ubiquitination and accelerates mitophagy.
|
-
- HY-18257
-
Rolitetracycline
|
Bacterial
Antibiotic
|
Infection
|
Rolitetracycline, a derivative of tetracycline, is a broad-spectrum antibiotic. Rolitetracyclin has a role as a protein synthesis inhibitor, an antiprotozoal drug and a prodrug.
|
-
- HY-13442A
-
Eribulin mesylate
B1939 mesylate; E7389 mesylate; ER-086526 mesylate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Eribulin mesylate (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-123931
-
ZLDI-8
|
Notch
Phosphatase
Apoptosis
|
Cancer
|
ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
|
-
- HY-100007
-
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-100432
-
LOC14
|
Others
|
Inflammation/Immunology
Neurological Disease
|
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding.
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.
|
-
- HY-P0289
-
CEF3
|
Influenza Virus
|
Infection
|
CEF3 (SIIPSGPLK) corresponds to aa 13-21 of the influenza A virus M1 protein. The matrix (M1) protein of influenza A virus is a multifunctional protein that plays essential structural and functional roles in the virus life cycle.
|
-
- HY-P1850
-
-
- HY-107096B
-
CH-0793076 TFA
TP3076 TFA
|
Topoisomerase
|
Cancer
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-100595
-
Sodium stibogluconate
Stibogluconate trisodium nonahydrate
|
Phosphatase
|
Cancer
|
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
|
-
- HY-13977A
-
PKR-IN-C16
|
Others
|
Neurological Disease
|
PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.
|
-
- HY-122615
-
SPOP-IN-6b
|
Others
|
Cancer
|
SPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor extracted from patent CN 107141287, SPOP-B-88.
|
-
- HY-15873A
-
-
- HY-50883
-
BMS 299897
|
γ-secretase
|
Neurological Disease
|
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
|
-
- HY-16642A
-
-
- HY-12801A
-
DiZPK Hydrochloride
|
Others
|
Others
|
DiZPK Hydrochloride is a structural analog of pyrrolysine (Pyl), acting as a photocrosslinker for identifying direct protein-protein interactions in living prokaryotic and eukaryotic cells.
|
-
- HY-110177
-
SP-100030
|
NF-κB
|
Inflammation/Immunology
|
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
|
-
- HY-115497
-
BRD5529
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
BRD5529 is a selective CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction inhibitor with an IC50 of 8.6 μM. BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways.
|
-
- HY-133021
-
Arazine
N-Acetyl-S-farnesyl-L-cysteine
|
Others
|
Inflammation/Immunology
|
Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
|
-
- HY-16659
-
EHT 1864
|
Ras
|
Neurological Disease
Cancer
|
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.
|
-
- HY-128971
-
LHVS
|
Cathepsin
Parasite
|
Infection
|
LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
|
-
- HY-100472
-
ZYZ-488
|
Caspase
|
Cancer
|
ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
|
-
- HY-114492
-
GSK547
GSK'547
|
RIP kinase
|
Cancer
|
GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
|
-
- HY-N0141
-
Parthenolide
(-)-Parthenolide
|
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-17593
-
Solithromycin
CEM-101; OP-1068
|
Bacterial
Antibiotic
|
Infection
|
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis.
|
-
- HY-133146
-
DJ001
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
|
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.
|
-
- HY-B2236
-
DL-Lysine
(±)-2,6-Diaminocaproic acid
|
Others
|
Metabolic Disease
|
DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
|
-
- HY-B2236A
-
DL-Lysine monohydrate
(±)-2,6-Diaminocaproic acid monohydrate
|
Others
|
Metabolic Disease
|
DL-Lysine monohydrate is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
|
-
- HY-B1898
-
Metadoxine
|
PKA
|
Metabolic Disease
|
Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
|
-
- HY-110263
-
-
- HY-122386
-
Kirromycin
Mocimycin; Delvomycin
|
Bacterial
Antibiotic
|
Infection
|
Kirromycin (Mocimycin) is an antibiotic produced by Streptomyces ramocissimus. Kirromycin is a bacterial protein synthesis inhibitor that immobilizes elongation factor Tu (EF-Tu) on the elongating ribosome.
|
-
- HY-18563
-
4-Phenoxybenzylamine
|
HCV
|
Infection
|
4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
|
-
- HY-B1848
-
Hexaflumuron
|
Others
|
Others
|
Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis.
|
-
- HY-B1849
-
Hexazinone
|
Others
|
Infection
|
Hexazinone is a nonselective herbicide from the triazine family. Hexazinone binds to the D-1 quinone protein of the electron transport chain in photosystem II to inhibit the photosynthesis.
|
-
- HY-18623
-
VI 16832
|
Others
|
Cancer
|
VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
|
-
- HY-43961
-
E3 ligase Ligand 8
|
Ligand for E3 Ligase
|
Cancer
|
E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-100585
-
Splitomicin
Splitomycin
|
HDAC
|
Cancer
|
Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM.
|
-
- HY-N2000
-
Bellidifolin
|
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities. Bellidifolin also acts as a viral protein R (Vpr) inhibitor.
|
-
- HY-B2172
-
Vitamin K
|
Others
|
Cardiovascular Disease
|
Vitamin K is a group of fat soluble vitamins, important for the function of numerous proteins within the body, such as the coagulation factors, osteocalcin and matrix-Gla protein.
|
-
- HY-P0137
-
-
- HY-P2283
-
-
- HY-128806
-
E3 ligase Ligand 9
|
Ligand for E3 Ligase
|
Cancer
|
E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
|
-
- HY-N0830
-
-
- HY-129939
-
-
- HY-18717
-
-
- HY-135397
-
(R)-Linezolid
(R)-PNU-100766
|
Others
|
Infection
|
(R)-Linezolid is an impurity of Linezolid (PNU-100766). Linezolid, the first member of the class of oxazolidinone synthetic antibiotic, acts by inhibiting the initiation of bacterial protein synthesis.
|
-
- HY-B2006
-
Fenvalerate
|
Phosphatase
Bacterial
|
Infection
|
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
|
-
- HY-P2478
-
-
- HY-13624A
-
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-13624
-
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-124325
-
PIP-199
|
DNA Alkylator/Crosslinker
|
Cancer
|
PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.
|
-
- HY-101518
-
APG-115
AA-115
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
|
-
- HY-108262
-
UCN-02
7-epi-Hydroxystaurosporine
|
PKC
PKA
|
Cancer
|
UCN-02 (7-epi-Hydroxystaurosporine) is a selective protein kinase C (PKC) inhibitor produced by Streptomyces strain N-12, with IC50s of 62 nM and 250 nM for PKC and protein kinase A (PKA), respectively. UCN-02 (7-epi-Hydroxystaurosporine) displays cytotoxic effect on the growth of HeLa S3 cells.
|
-
- HY-114410
-
CCI-006
|
Mitochondrial Metabolism
|
Cancer
|
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells.
|
-
- HY-N7068
-
-
- HY-13756A
-
-
- HY-W009602
-
Phenylalanylalanine
H-Phe-Ala-OH
|
Others
|
Others
|
Phenylalanylalanine (H-Phe-Ala-OH) is a dipeptide composed of phenylalanine and alanine. Phenylalanylalanine is an incomplete breakdown product of protein digestion or protein catabolism.
|
-
- HY-128699
-
D-Desthiobiotin
|
Endogenous Metabolite
|
Others
|
D-Desthiobiotin is a biotin derivative used in affinity chromatography and protein chromatography, also can be used for protein and cell labeling, detection and isolation.
|
-
- HY-103194
-
KH7
|
Others
|
Others
|
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC50s of 3-10 μM toward both recombinant purified human sACt protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.
|
-
- HY-17504A
-
Rosuvastatin
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-19639
-
E-982
|
Others
|
Others
|
E-982 is a steroid used for the on-line screening of the DNA unwinding element binding protein (DUE-B) immobilized protein column.
|
-
- HY-13756
-
-
- HY-114492A
-
(Rac)-GSK547
|
RIP kinase
|
Cancer
|
(Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
|
-
- HY-111860
-
SNIPER(ABL)-013
|
SNIPER
Bcr-Abl
|
Cancer
|
SNIPER(ABL)-013, conjugating GNF5 (ABL inhibitor) to Bestatin (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 20 μM.
|
-
- HY-111548
-
Spastazoline
|
Others
|
Others
|
Spastazoline is a potent and selective spastin (a microtubule-severing AAA protein) inhibitor, with an IC50 of 99 nM for Human spastin. Spastazoline shows no effect on ATPase activity of a recombinant human VPS4.
|
-
- HY-N6729
-
HT-2 Toxin
|
Others
|
Metabolic Disease
|
HT-2 Toxin is an active, deacetylated metabolite of the T-2 toxin. HT-2 toxin inhibits protein synthesis and cell proliferation in plants.
|
-
- HY-N4185
-
-
- HY-B1596A
-
Ceftizoxime sodium
SKF-88373
|
Bacterial
Antibiotic
|
Infection
|
Ceftizoxime sodium (SKF-88373) is third generation cephalosporin effective against Gram-negative and Gram-positive bacteria. It binds penicillin-binding proteins (PBPs) and inhibits the bacterial cell wall synthesis.
|
-
- HY-W011109
-
CKI-7
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
|
-
- HY-N6791
-
KT5823
|
PKA
PKC
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
|
-
- HY-N6732
-
K-252a
SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
PKC
PKA
CaMK
Trk Receptor
Autophagy
|
Infection
|
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
|
-
- HY-101903A
-
BMS-309403 sodium
|
FABP
|
Metabolic Disease
Cardiovascular 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-101903
-
BMS-309403
|
FABP
|
Metabolic Disease
Cardiovascular 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-A0036
-
Bazedoxifene acetate
TSE-424 acetate
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
-
- HY-P1597
-
Malantide
|
PKA
PKC
|
Cancer
|
Malantide is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide is also an efficient substrate for PKC with a Km of 16 μM.
|
-
- HY-14865C
-
Omadacycline hydrochloride
PTK0796 hydrochloride; Amadacycline hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
Omadacycline (PTK 0796) hydrochloride, a tetracycline antibacterial agent, acts through the inhibition of protein synthesis. Omadacycline hydrochloride exhibits activity against a broad spectrum of bacteria, including Gram-positive, Gram-negative, anaerobic, and atypical pathogens. Omadacycline hydrochloride can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections.
|
-
- HY-123979
-
ζ-Stat
NSC37044
|
PKC
Apoptosis
|
Cancer
|
ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
|
-
- HY-13264
-
Degrasyn
WP1130
|
Deubiquitinase
Bcr-Abl
Autophagy
Apoptosis
|
Cancer
|
Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
|
-
- HY-111752
-
EML4-ALK kinase inhibitor 1
|
ALK
|
Cancer
|
EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
|
-
- HY-N1255
-
Scoulerine
(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
|
Cancer
|
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
|
-
- HY-12048
-
-
- HY-122903A
-
(-)-TK216
|
Others
|
Others
|
(-)-TK216 is an enantiomer of TK216. TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. TK216 directly binds EWS-FLI1 and inhibits EWS-FLI1 protein interactions.
|
-
- HY-15555
-
EPZ005687
|
Histone Methyltransferase
|
Cancer
|
EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, and has 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.
|
-
- HY-112157
-
-
- HY-N6650
-
-
- HY-N6651
-
Isocryptotanshinone
|
STAT
Phosphatase
|
Cancer
|
Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
|
-
- HY-128585
-
-
- HY-112149
-
-
- HY-16911
-
AFN-1252
API-1252; Debio 1452
|
Bacterial
Antibiotic
|
Infection
|
AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.
|
-
- HY-111854
-
SNIPER(ABL)-015
|
SNIPER
Bcr-Abl
|
Cancer
|
SNIPER(ABL)-015, conjugating GNF5 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5 μM .
|
-
- HY-120508
-
Pivanex
AN-9; Pivalyloxymethyl butyrate
|
HDAC
Bcr-Abl
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
|
-
- HY-122727
-
STL127705
|
DNA-PK
|
Cancer
|
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM).
|
-
- HY-15286
-
Sodium 4-pentynoate
|
Others
|
Others
|
Sodium 4-pentynoate is a alkynylacetate analogue, can be metabolically incorporated onto cellular proteins through biosynthetic mechanisms for profiling of acetylated proteins in diverse cell types.
|
-
- HY-A0031
-
Bazedoxifene
TSE-424
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
|
-
- HY-P1597A
-
Malantide TFA
|
PKA
PKC
|
Cancer
|
Malantide TFA is a synthetic dodecapeptide derived from the site phosphorylated by cAMP-dependent protein kinase (PKA) on the β-subunit of phosphorylase kinase. Malantide TFA is a highly specific substrate for PKA with a Km of 15 μM and shows protein inhibitor (PKI) inhibition >90% substrate phosphorylation in various rat tissue extracts. Malantide TFA is also an efficient substrate for PKC with a Km of 16 μM.
|
-
- HY-A0031A
-
Bazedoxifene hydrochloride
TSE-424 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
|
-
- HY-123979A
-
ζ-Stat trisodium
NSC37044 trisodium
|
PKC
Apoptosis
|
Cancer
|
ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat trisodium can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro.
|
-
- HY-17504
-
Rosuvastatin Calcium
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-17504C
-
(3R,5R)-Rosuvastatin
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Metabolic Disease
Cardiovascular Disease
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-17504D
-
(3S,5R)-Rosuvastatin
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Metabolic Disease
Cardiovascular Disease
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-104021
-
GSK840
GSK'840
|
RIP kinase
|
Inflammation/Immunology
|
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
|
-
- HY-12429
-
Beclabuvir
BMS-791325
|
HCV
|
Infection
|
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
|
-
- HY-69220
-
7-Octynoic acid
|
PROTAC Linker
|
Cancer
|
7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-126457
-
Thalidomide-propargyl
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-propargyl is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-propargyl can be connected to the ligand for protein by a linker to form the IMiD containing PROTACs.
|
-
- HY-114164
-
Thrombin
|
Thrombin
|
Neurological Disease
|
Thrombin is a trypsin-like allosteric serine protease. Thrombin enables site-specific cleavage of fusion proteins with an accessible Thrombin recognition sequence and can be used to digest GST-tagged proteins.
|
-
- HY-135127
-
-
- HY-14175
-
Begacestat
GSI-953
|
γ-secretase
|
Neurological Disease
|
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease.
|
-
- HY-B0751
-
Fumagillin
Amebacilin; NSC9168
|
Parasite
HIV
Antibiotic
|
Infection
|
Fumagillin(NSC9168) is a complex biomolecule and used as an antimicrobial agent. Fumagillin can inhibits HIV‐1 infection through the inhibition of HIV-1 viral protein R (Vpr) activity.
|
-
- HY-N0374
-
-
- HY-100716
-
IPI549
|
PI3K
|
Cancer
|
IPI549 is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. IPI549 shows >100-fold selectivity over other lipid and protein kinases.
|
-
- HY-124512
-
Quercetin pentaacetate
Pentaacetylquercetin
|
RSV
|
Infection
Inflammation/Immunology
|
Quercetin pentaacetate could interact with F-protein with lower binding energy and better stability to block viral adhesion. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface.
|
-
- HY-129035
-
-
- HY-18990
-
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-125402
-
GSK-843
GSK'843
|
RIP kinase
|
Inflammation/Immunology
|
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
|
-
- HY-101920
-
Autophinib
|
Autophagy
|
Cancer
Neurological Disease
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
|
-
- HY-W010983
-
-
- HY-P1479
-
-
- HY-P1479A
-
-
- HY-135682
-
-
- HY-108317
-
ABL127
|
Others
|
Cancer
|
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
|
-
- HY-101354
-
-
- HY-10299
-
GSK-923295
|
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-P0271
-
-
- HY-N2419
-
Erythrodiol
|
Endogenous Metabolite
|
Metabolic Disease
|
Erythrodiol is an olive oil component. Erythrodiol promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein. Erythrodiol is a good candidate to be further explored for therapeutic or preventive application in the context of atherosclerosis.
|
-
- HY-P0219
-
Microcystin-LA
|
Phosphatase
|
Cancer
|
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
|
-
- HY-107777
-
LLY-283
|
Histone Methyltransferase
|
Cancer
|
LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.
|
-
- HY-13997
-
Ombitasvir
ABT-267
|
HCV
|
Infection
|
Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
|
-
- HY-15789
-
Elbasvir
MK-8742
|
HCV
|
Infection
|
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
|
-
- HY-13671
-
LW6
HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
|
-
- HY-N5011
-
5,7-Dimethoxyflavone
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
|
-
- HY-103710
-
IBR2
|
RAD51
Apoptosis
|
Cancer
|
IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.
|
-
- HY-B1099
-
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- HY-109187A
-
Posenacaftor sodium
PTI-801 sodium
|
CFTR
|
Inflammation/Immunology
|
Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).
|
-
- HY-111945
-
Cys modifier 1
|
Others
|
Others
|
Cys modifier 1 (compound 7) is a cysteine-selective protein modifier for protein bioconjugation. A fluorescent carbonylacrylic derivative bearing nitrobenzofurazan (λex=465nm and λem539 nm)[1].
|
-
- HY-122866
-
ZT-12-037-01
|
Ras
|
Cancer
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-W015977
-
Prion Protein 106-126 (human)
PrP 106-126 (human)
|
Apoptosis
|
Neurological Disease
|
Prion Protein 106-126 (human), a peptide fragment of prion, and can induct neuronal apoptosis, antiproteinase K digestion, fiber formation, and mediate the conversion of normal cellular prion protein (PrP c) into pathogenic isoform (PrP Sc). Prion Protein 106-126 (human) is generally used as the model to investigate neural degeneration of prion disease.
|
-
- HY-B0754A
-
-
- HY-Y0781
-
-
- HY-113079
-
-
- HY-133028
-
CKI-7 free base
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
|
-
- HY-14136
-
-
- HY-12530
-
Velpatasvir
GS-5816
|
HCV
|
Cancer
|
Velpatasvir (VEL, GS-5816) is a novel pan-genotypic hepatitis C virus (HCV) nonstructural protein 5A (NS5A) inhibitor with activity against genotype 1 (GT1) to GT6 HCV replicons.
|
-
- HY-138142
-
Euphol acetate
|
Others
|
Metabolic Disease
|
Euphol acetate is a triterpene that can be isolated from Euphorbia broteri. Euphol acetate is an inhibitor of hepatic transport proteins organic anion-transporting polypeptide 1/3 (OATP1B1/3).
|
-
- HY-111879
-
Biotin-BS
|
SNIPER
|
Cancer
|
Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
|
-
- HY-14137
-
-
- HY-134598A
-
653-47 hydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM.
|
-
- HY-19537
-
-
- HY-134598
-
653-47
|
Epigenetic Reader Domain
|
Cancer
|
653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM.
|
-
- HY-P0271A
-
Syntide 2 TFA
|
CaMK
Calcium Channel
|
Neurological Disease
|
Syntide 2 (TFA), a Ca 2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected.
|
-
- HY-100779
-
Rimacalib
SMP 114
|
CaMK
Autophagy
|
Metabolic Disease
|
Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
|
-
- HY-13960
-
-
- HY-19825
-
Rebeccamycin
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
|
-
- HY-B1156
-
Cephradine
Cefradine; SQ-11436
|
Bacterial
TOPK
Antibiotic
|
Infection
|
Cephradine (Cefradine) is the first-generation broad-spectrum cephalosporin antibiotic, which also acts as an inhibitor of TOPK (T-LAK cell-originated protein kinase) and suppresses skin inflammation induced by excessive solar ultraviolet.
|
-
- HY-102080
-
SAFit2
|
FKBP
|
Cancer
|
SAFit2 is a highly potent, highly selective FK506-binding protein 51 (FKBP51) inhibitor with a Ki of 6 nM and also enhances AKT2-AS160 binding.
|
-
- HY-108709
-
CC-671
|
CDK
|
Cancer
|
CC-671 is a dual TTK protein kinase/CDC2-like kinase (CLK2) inhibitor with IC50s of 0.005 and 0.006 μM for TTK and CLK2, respectively.
|
-
- HY-N1481
-
Methyl linoleate
|
Others
|
Metabolic Disease
|
Methyl linoleate, a major active constituent of Sageretia thea fruit (HFSF), is a major anti-melanogenic compound. Methyl linoleate downregulates microphthalmia-associated transcription factor (MITF) and tyrosinase-related proteins.
|
-
- HY-P0281A
-
TAT TFA
|
HIV
|
Infection
|
TAT TFA (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins.
|
-
- HY-13407
-
Gossypol
BL 193
|
Bcl-2 Family
|
Cancer
|
Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
|
-
- HY-B0958
-
Mupirocin
BRL-4910A; Pseudomonic acid
|
Bacterial
Antibiotic
|
Infection
|
Mupirocin (BRL-4910A) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin (BRL-4910A) apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
|
-
- HY-17406
-
Tolcapone
Ro 40-7592
|
COMT
Amyloid-β
|
Neurological Disease
|
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-14435
-
Pyridone 6
|
JAK
|
Cancer
|
Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
|
-
- HY-19615B
-
MS023 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
|
-
- HY-19615
-
MS023
|
Histone Methyltransferase
|
Cancer
|
MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
|
-
- HY-B0510
-
Trimethoprim
|
Antifolate
Bacterial
Antibiotic
|
Infection
|
Trimethoprim is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.
|
-
- HY-123823
-
Nitroaspirin
NCX 4016
|
COX
Apoptosis
|
Cancer
|
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
|
-
- HY-125834
-
GMB-475
|
PROTAC
Bcr-Abl
Apoptosis
|
Cancer
|
GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
|
-
- HY-109172
-
Ezeprogind
AZP-2006
|
Amyloid-β
|
Neurological Disease
|
Ezeprogind (AZP-2006) is an orally active neurotrophic inducer. Ezeprogind targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
|
-
- HY-129241
-
AGX51
|
Others
|
Cancer
|
AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
|
-
- HY-N6062
-
Perivine
Perivin
|
Others
|
Neurological Disease
|
Perivine (Perivin) targets protein retinoblastoma-associated proteins (RbAp48) and resolves the instability of the RbAp48-FOG-1 complex. Perivine can be used for the study of Alzheimer's disease.
|
-
- HY-23095
-
Thalidomide-5-OH
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-5-OH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-P0281
-
TAT
|
HIV
|
Infection
|
TAT (YGRKKRRQRRR) is derived from the transactivator of transcription (TAT) of human immunodeficiency virus-1 (HIV-1) and is a cell-penetrating peptide. TAT can increase the yields and the solubility of heterologous proteins.
|
-
- HY-101213
-
OSW-1
|
Others
|
Cancer
|
OSW-1, isolated from Ornithogalum caudatum, is a specific antagonist of osterol-binding protein (OSBP) and OSBP-related protein 4 (ORP4) with GI50s in the nanomolar range in human cancer lines.
|
-
- HY-B2145
-
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-136179
-
ZAP-180013
|
Tyrosinase
|
Inflammation/Immunology
|
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
|
-
- HY-B0510C
-
Trimethoprim lactate
|
Antifolate
Bacterial
|
Infection
|
Trimethoprim lactic is a bacteriostatic antibiotic and an orally active dihydrofolate reductase inhibitor. Trimethoprim lactic is active against a wide range of Gram-positive and Gram-negative aerobic bacteria. Trimethoprim lactic has the potential for urinary tract infections, Shigellosis and Pneumocystis pneumonia treatment.
|
-
- HY-120323
-
DRI-C21045
|
TNF Receptor
|
Inflammation/Immunology
|
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
|
-
- HY-101180
-
C2 Ceramide
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
|
Endocrinology
Metabolic Disease
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- HY-124828
-
CMLD-2
|
Apoptosis
|
Cancer
|
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation.
|
-
- HY-12219A
-
MSI-1436 lactate
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-N1963
-
Curzerene
|
Gutathione S-transferase
|
Cancer
|
Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
|
-
- HY-114712
-
SJ572403
SJ403
|
Others
|
Cancer
|
SJ572403 (SJ403) is an inhibitor of disordered protein p27(Kip1). p27(Kip1) is a regulator of the CDKs that control eukaryotic cell division.
|
-
- HY-111863
-
SNIPER(ABL)-047
|
SNIPER
Bcr-Abl
|
Cancer
|
SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM.
|
-
- HY-N6258
-
Kahweol
|
AMPK
Apoptosis
|
Metabolic Disease
|
Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
|
-
- HY-19369
-
-
- HY-N4108
-
Hypophyllanthin
|
P-glycoprotein
|
Cancer
Inflammation/Immunology
|
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
|
-
- HY-101564
-
JNJ-64619178
|
Histone Methyltransferase
|
Cancer
|
JNJ-64619178 is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer.
|
-
- HY-15662
-
Tulathromycin A
Tulathromycin; CP 472295
|
Antibiotic
Bacterial
|
Infection
|
Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 µM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects.
|
-
- HY-12219
-
MSI-1436
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-112730
-
PEO-IAA
2-(1H-Indol-3-yl)-4-oxo-4-phenyl-butyric acid
|
Others
|
Others
|
PEO-IAA is an indole-3-acetic acid (IAA) antagonist. PEO-IAA is an auxin antagonist that binds to transport inhibitor response 1/auxin signaling F-box proteins (TIR1/AFBs).
|
-
- HY-15880
-
CCT007093
|
Phosphatase
Apoptosis
Autophagy
|
Cancer
|
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy.
|
-
- HY-101032
-
RIPA-56
|
RIP kinase
|
Inflammation/Immunology
|
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting
protein 1 (RIP1) with an IC50 of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome.
|
-
- HY-12831
-
-
- HY-111431A
-
-
- HY-114236
-
Ezeprogind disulfate
AZP-2006 disulfate
|
Amyloid-β
|
Neurological Disease
|
Ezeprogind (AZP-2006) disulfate is an orally active neurotrophic inducer. Ezeprogind disulfate targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind disulfate is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
|
-
- HY-117661
-
SPHINX31
|
SRPK
|
Cancer
|
SPHINX31 is a potent and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 is a potential topical therapeutic for neovascular eye disease.
|
-
- HY-N0781
-
Linderalactone
|
Apoptosis
|
Cancer
|
Linderalactone is an important sesquiterpene lactone isolated from Radix linderae. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 µM.
|
-
- HY-131081
-
γ-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin (HY-19610) and β-Amanitin (HY-125586).
|
-
- HY-15874A
-
Fiboflapon sodium
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-B0843A
-
Metalaxyl-M
(R)-Metalaxyl
|
Fungal
|
Infection
|
Metalaxyl-M ((R)-Metalaxyl) is the active (R)-enantiomer of Metalaxyl. Metalaxyl-M is a broad-spectrum fungicide that inhibits protein and ribosomal RNA synthesis in fungi. Metalaxyl is used for research of plant diseases caused by pathogens of the Oomycota division.
|
-
- HY-N1549
-
-
- HY-101867
-
AU1235
|
Bacterial
|
Cancer
Infection
|
AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane.
|
-
- HY-111903
-
Levomecol
|
Bacterial
|
Infection
|
Levomecol (Chloramphenicol), made up of Chloramphenicol, Methyluracil, is a broad-spectrum antibiotic that is derived from the bacterium Streptomyces venezuelae. Levomecol (Chloramphenicol)) stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.
|
-
- HY-12600
-
AZD5582
|
IAP
Apoptosis
|
Cancer
|
AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
|
-
- HY-12833
-
AMZ30
|
Others
|
Others
|
AMZ30 is a selective, covalent inhibitors of protein phosphatase methylesterase-1(PME-1; IC50=600 nM); selectively inactivates PME-1 and reduces the demethylated form of PP2A in living cells.
|
-
- HY-12594
-
Paritaprevir
ABT-450; Veruprevir
|
HCV Protease
HCV
|
Infection
|
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
|
-
- HY-15874
-
Fiboflapon
GSK2190915; AM-803
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-15136
-
-
- HY-111871
-
SNIPER(ABL)-033
|
SNIPER
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.
|
-
- HY-17013A
-
Dofequidar fumarate
MS-209
|
P-glycoprotein
|
Cancer
|
Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.
|
-
- HY-15141
-
-
- HY-N3942
-
Glabranine
|
HIV
Influenza Virus
|
Infection
|
Glabranine, an flavonoid, is isolated from Tephrosia s.p, exerts a inhibitory effect in vitro on the dengue virus.
Glabranine forms interaction with the soluble ectodomain of DENV type 2 (DENV2) E protein.
|
-
- HY-103597
-
Thalidomide-O-COOH
Cereblon ligand 3; E3 ligase Ligand 3
|
Ligand for E3 Ligase
|
Others
|
Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-17510
-
Gossypol (acetic acid)
(±)-Gossypol-acetic acid; BL-193 (acetic acid)
|
Bcl-2 Family
|
Cancer
|
Gossypol acetic acid ((±)-Gossypol-acetic acid), a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
|
-
- HY-N0288
-
-
- HY-101664
-
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-14865B
-
Omadacycline tosylate
PTK 0796 tosylate; Amadacycline tosylate
|
Bacterial
Antibiotic
|
Infection
|
Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline tosylate exhibits activity against a broad spectrum of bacteria, including Gram-positive, Gram-negative, anaerobic, and atypical pathogens. Omadacycline tosylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections.
|
-
- HY-P1474
-
β-Amyloid (22-35)
Amyloid β-Protein (22-35)
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-101712
-
-
- HY-P0136
-
-
- HY-100825
-
-
- HY-B0754
-
-
- HY-18705
-
-
- HY-N0722
-
-
- HY-B0449
-
Methacycline hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.
|
-
- HY-100612
-
T16Ainh-A01
|
Chloride Channel
|
Others
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-100596
-
AS1842856
|
Autophagy
|
Metabolic Disease
|
AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 only reduces the activity of FoxO1 by binding with it, without affecting its transcription and protein expression.
|
-
- HY-13744
-
Rubitecan
RFS 2000; 9-Nitrocamptothecin
|
Topoisomerase
|
Cancer
|
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
|
-
- HY-112721
-
FDI-6
|
Others
|
Cancer
|
FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
|
-
- HY-N7101
-
Cefpodoxime Proxetil
U-76,252; CS-807
|
Bacterial
Antibiotic
|
Infection
|
Cefpodoxime Proxetil is a first oral and broad spectrum antibiotic that belongs to the third generation of cephalosporin. Cefpodoxime Proxetil binds to penicillin binding proteins (PBPs), which inhibits peptidoglycan synthesis, finally results in interfering bacterial cell wall biosynthesis.
|
-
- HY-112140
-
JH-VIII-157-02
|
ALK
|
Cancer
|
JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
|
-
- HY-10858
-
WAY 316606
|
sFRP-1
|
Cancer
|
WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
|
-
- HY-N2451
-
-
- HY-11002
-
CP-466722
|
ATM/ATR
|
Cancer
|
CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 4.1 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
|
-
- HY-121515
-
DPM-1001
|
Phosphatase
|
Metabolic Disease
|
DPM-1001 is a potent, specific, orally bioavailable and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM, an an analog of the specific PTP1B inhibitor trodusquemine (MSI-1436; IC50=600 nM). DPM-1001 has anti-diabetic property.
|
-
- HY-108847
-
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-N2204
-
Swertiajaponin
|
Tyrosinase
|
Inflammation/Immunology
|
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
|
-
- HY-13423
-
-
- HY-N6715
-
Tenuazonic acid
|
Influenza Virus
Bacterial
|
Infection
|
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor.
|
-
- HY-18981
-
Decursin
(+)-Decursin
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
|
-
- HY-12467
-
OTS964 hydrochloride
|
TOPK
CDK
Apoptosis
|
Cancer
|
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
|
-
- HY-129774
-
Phthalimide-PEG4-MPDM-OH
|
PROTAC Linker
|
Cancer
|
Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-130715
-
tert-Butyl 11-aminoundecanoate
|
PROTAC Linker
|
Cancer
|
tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-P1474A
-
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (22-35) (TFA)
|
Amyloid-β
|
Neurological Disease
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-129773
-
Phthalimide-PEG4-PDM-OTBS
|
PROTAC Linker
|
Cancer
|
Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-131159
-
Thalidomide-O-C8-Boc
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-O-C8-Boc is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-Boc can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-122903
-
TK216
|
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-U00398
-
-
- HY-B0779
-
-
- HY-Y0511
-
-
- HY-106262B
-
Delcasertib hydrochloride
KAI-9803 hydrochloride; BMS-875944 hydrochloride
|
PKC
|
Inflammation/Immunology
Cardiovascular Disease
|
Delcasertib (KAI-9803) hydrochloride is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) hydrochloride could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
|
-
- HY-108707
-
LY3130481
|
iGluR
|
Neurological Disease
|
LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC50 of 65 nM.
|
-
- HY-111532
-
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
|
-
- HY-106262
-
Delcasertib
KAI-9803; BMS-875944
|
PKC
|
Inflammation/Immunology
Cardiovascular Disease
|
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor. Delcasertib (KAI-9803) could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
|
-
- HY-123475
-
Sisunatovir
RV521
|
RSV
|
Infection
|
Sisunatovir (RV521), an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.
|
-
- HY-19753
-
KS176
|
BCRP
|
Cancer
|
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively). Displays no inhibitory activity against P-gp or MRP1.
|
-
- HY-N0698
-
-
- HY-100758
-
FUBP1–IN-1
|
Others
|
Cancer
|
FUBP1–IN-1 is a potent FUSE binding protein 1 (FUBP1) inhibitor which interferes with the binding of FUBP1 to its single stranded target DNA FUSE sequence , with an IC50 value of 11.0 μM.
|
-
- HY-103131
-
PNU-142633
|
5-HT Receptor
|
Neurological Disease
|
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.
|
-
- HY-34477
-
2-Iodoacetamide
Iodoacetamide
|
Others
|
Others
|
2-Iodoacetamide (Iodoacetamide), an alkylating agent, is a commonly used agent for alkylation of cysteine during sample preparation for proteomics.
|
-
- HY-100126
-
Tubercidin
7-Deazaadenosine
|
Bacterial
DNA/RNA Synthesis
Influenza Virus
Antibiotic
|
Infection
|
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC50 of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.
|
-
- HY-15463
-
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
Imatinib (STI571) 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-103596
-
Thalidomide-4-OH
Cereblon ligand 2; E3 ligase Ligand 2
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-4-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-133144
-
Lenalidomide-OH
|
Ligand for E3 Ligase
|
Cancer
|
Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
|
-
- HY-103243
-
TCPOBOP
|
Bcl-2 Family
|
Cancer
|
TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss. TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins.
|
-
- HY-P9807
-
-
- HY-16706A
-
Remodelin hydrobromide
|
Histone Acetyltransferase
|
Cancer
|
Remodelin, a specific inhibitor of N-acetyltransferase NAT10, can ameliorate Hutchinson-Gilford Progeria Syndrom (HGPS) cellular phenotypes. Remodelin acts in a progerin- and FTI-independent pathway, by targeting and inhibiting NAT10. NAT10 is a protein with histone acetylation activity and primarily identified to be involved in regulation of telomerase activity.
|
-
- HY-112698
-
CA-5f
|
Autophagy
Apoptosis
|
Cancer
|
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
|
-
- HY-130149
-
MRTX849
|
Ras
|
Cancer
|
MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
|
-
- HY-114489B
-
-
- HY-B0764A
-
Bucladesine calcium
Dibutyryl cAMP calcium salt; DBcAMP calcium salt
|
PKA
Phosphodiesterase (PDE)
Apoptosis
|
Others
|
Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
|
-
- HY-114489A
-
Haemanthamine
|
Apoptosis
Influenza Virus
Parasite
|
Cancer
Infection
Neurological Disease
|
Haemanthamine is a crinine-type alkaloid isolated from the Amaryllidaceae plants with potent anticancer activity. Haemanthamine targets ribosomal that inhibits protein biosynthesis during the elongation stage of translation. Haemanthamine has pro-apoptotic, antioxidant, antiviral, antimalarial and anticonvulsant activities.
|
-
- HY-N1934
-
-
- HY-101047
-
D-erythro-Sphingosine
Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
|
-
- HY-N6030
-
(Rac)-Dencichin
2-Amino-3-(carboxyformamido)propanoic acid
|
Others
|
Others
|
(Rac)-Dencichin (2-Amino-3-(carboxyformamido)propanoic acid) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
|
-
- HY-18991
-
CCG215022
|
PKA
|
Cancer
|
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
|
-
- HY-121172
-
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-13509
-
CCG-50014
|
RGS Protein
|
Inflammation/Immunology
|
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
|
-
- HY-114146
-
-
- HY-101404A
-
-
- HY-P0248
-
Kemptide
|
PKA
|
Metabolic Disease
|
Kemptide is a synthetic heptapeptide that acts as a specific substrate for cAMP-dependent protein kinase (PKA).
|
-
- HY-113380
-
-
- HY-117291A
-
-
- HY-130952
-
Thalidomide-O-C8-COOH
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
|
-
- HY-126316
-
Zapalog
|
FKBP
|
Others
|
Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis.
|
-
- HY-N0686
-
-
- HY-136466
-
A2ti-2
|
Virus Protease
|
Infection
|
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-136465
-
A2ti-1
|
Virus Protease
|
Infection
|
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-137497
-
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-131335
-
p38α inhibitor 2
|
p38 MAPK
|
Inflammation/Immunology
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
|
-
- HY-N2344
-
Procyanidin A1
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-16909
-
Leptomycin B
CI 940; LMB
|
CRM1
Fungal
Antibiotic
|
Cancer
Infection
|
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
|
-
- HY-124712
-
Divin
|
Bacterial
|
Infection
|
Divin, a potent chelator of iron, is a potent inhibitor of bacterial cell division with bacteriostatic effect in Gram-negative and Gram-positive bacteria. Divin disrupts the assembly of late division proteins, reduces peptidoglycan remodeling at the division site, and blocks compartmentalization of the cytoplasm.
|
-
- HY-10394
-
Linezolid
PNU-100766
|
Bacterial
Antibiotic
|
Infection
|
Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics.
|
-
- HY-111756
-
BLM-IN-1
|
Apoptosis
|
Cancer
|
BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
|
-
- HY-112038A
-
GSK2983559
|
RIP kinase
|
Inflammation/Immunology
|
GSK2983559 (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor, which has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
|
-
- HY-N1094
-
Verminoside
|
PARP
MDM-2/p53
|
Inflammation/Immunology
|
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins.
|
-
- HY-131318
-
Lenalidomide-I
|
Ligand for E3 Ligase
|
Cancer
|
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
|
-
- HY-100558
-
Bafilomycin A1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Cancer
Infection
|
Bafilomycin A1 is a specific inhibitor of vacuolar H +-ATPase (V-ATPase) with I50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
|
-
- HY-115038
-
-
- HY-Y0252
-
-
- HY-16271
-
Kevetrin hydrochloride
4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
|
MDM-2/p53
|
Cancer
|
Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.
|
-
- HY-P1774
-
-
- HY-W002292
-
-
- HY-12359
-
-
- HY-13755
-
Sulforaphane
|
HDAC
Keap1-Nrf2
Apoptosis
|
Cancer
Inflammation/Immunology
|
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
|
-
- HY-P1189
-
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-N0814
-
Phytic acid
Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-107613
-
R 59-022
DKGI-I; Diacylglycerol Kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-112292A
-
GW806742X hydrochloride
|
Mixed Lineage Kinase
VEGFR
|
Cancer
|
GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC50=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis.
|
-
- HY-112292
-
GW806742X
|
Mixed Lineage Kinase
VEGFR
|
Others
|
GW806742X, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a Kd of 9.3 μM. GW806742X has activity against VEGFR2 (IC50=2 nM). GW806742X retards MLKL membrane translocation and inhibits necroptosis.
|
-
- HY-117684A
-
DDD107498 succinate
DDD-498 succinate
|
Parasite
CaMK
Autophagy
|
Infection
|
DDD107498 succinate (DDD-498 succinate) is a potent and orally active antimalarial agent, inhibits multiple life-cycle stages of the parasite, with an EC50 of 1 nM against P. falciparum 3D7. DDD107498 succinate inhibits protein synthesis by targeting eEF2/CaMKIII, with an EC50 of 2 nM for WT-PfeEF2.
|
-
- HY-13771
-
Ursodiol
Ursodeoxycholic acid; UDCA
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
Ursodiol (Ursodeoxycholic acid; UDCA) is a potent liver-specific fatty acid transport protein 5 (FATP5) inhibitor. Ursodiol inhibit LCFA uptake by primary hepatocytes in a FATP5-dependent manner. Ursodiol reduces cholesterol absorption and is used to dissolve gallstones and has the potential for obesity-associated fatty liver disease research.
|
-
- HY-77251
-
TAK1/MAP4K2 inhibitor 1
|
MAP4K
MAP3K
|
Cancer
|
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
|
-
- HY-10300
-
Narlaprevir
SCH 900518
|
HCV
HCV Protease
|
Infection
|
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir (SCH 900518) also inhibits the hepatitis C virus (HCV) nonstructural protein 3 serine protease. Narlaprevir (SCH 900518) can be used for chronic hepatitis C research.
|
-
- HY-108355
-
R59949
|
PKC
|
Cancer
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
|
-
- HY-17406S
-
Tolcapone D7
Ro 40-7592 D7
|
COMT
Amyloid-β
|
Neurological Disease
|
Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-103238
-
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
|
-
- HY-129772
-
Phthalimide-PEG3-C2-OTs
|
PROTAC Linker
|
Cancer
|
Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-40178
-
NH2-C4-NH-Boc
|
PROTAC Linker
|
Cancer
|
NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-116494
-
ML753286
|
BCRP
|
Cancer
|
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.
|
-
- HY-112799
-
DK419
|
Wnt
β-catenin
|
Cancer
|
DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
|
-
- HY-107486
-
Nosiheptide
Multhiomycin; RP 9671
|
Bacterial
Antibiotic
|
Infection
|
Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth.
|
-
- HY-101483
-
Dihydromunduletone
DHM
|
Others
|
Cancer
Neurological Disease
|
Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
|
-
- HY-N6795
-
Leptomycin A
|
CRM1
HIV
|
Infection
|
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
|
-
- HY-14454
-
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-100591
-
SirReal2
|
Sirtuin
|
Cancer
Inflammation/Immunology
Neurological Disease
|
SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1.
|
-
- HY-131275
-
Imatinib Impurity E
|
Others
|
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-131717
-
Thalidomide-NH-CH2-COOH
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide-NH-CH2-COOH is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
|
-
- HY-129608
-
Lenalidomide-acetylene-C5-COOH
Cereblon ligand-linker Conjugate
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
Lenalidomide-acetylene-C5-COOH (compound 43; Cereblon ligand-linker Conjugate) is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-acetylene-C5-COOH can be connected to the ligand for protein by a linker to form PROTAC.
|
-
- HY-15486
-
Salubrinal
|
Phosphatase
HSV
Autophagy
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
|
-
- HY-108254
-
Bisindolylmaleimide IV
Arcyriarubin A
|
PKC
CMV
|
Infection
|
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
|
-
- HY-N0379
-
-
- HY-13262
-
-
- HY-P1895
-
-
- HY-P0265
-
-
- HY-B0438
-
-
- HY-B0198A
-
-
- HY-107988
-
-
- HY-B0412
-
-
- HY-P1903
-
-
- HY-B0198
-
-
- HY-N6631
-
-
- HY-11010
-
AS601245
|
JNK
|
Cancer
Inflammation/Immunology
Neurological Disease
|
AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.
|
-
- HY-D0254
-
Gallein
Pyrogallol phthalein
|
Others
|
Cancer
|
Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.
|
-
- HY-13649
-
Indibulin
ZIO 301; D 24851
|
Microtubule/Tubulin
Apoptosis
|
Cancer
Neurological Disease
|
Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.
|
-
- HY-N7599
-
Chrysophanol triglucoside
|
Phosphatase
Glucosidase
|
Metabolic Disease
|
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
|
-
- HY-128849
-
Eprodisate
|
Others
|
Inflammation/Immunology
|
Eprodisate is a new compound designed to interfere with interactions between amyloidogenic proteins and glycosaminoglycans and thereby inhibit polymerization of amyloid fibrils and deposition of the fibrils in tissues.
Eprodisate slow the progression of AA amyloidosis-related renal disease and has possible applicability to other types of amyloidosis.
|
-
- HY-13290
-
KN-62
|
CaMK
P2X Receptor
Autophagy
|
Metabolic Disease
Cancer
|
KN-62 is a selective and potent inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with IC50 of 0.9 μM, KN-62 also displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-126254
-
BI-4924
|
Others
|
Cancer
|
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
|
-
- HY-117113
-
JI051
|
Notch
|
Cancer
|
JI051 is a stabilizer for the Hes1-PHB2 interaction, interacts with a cancer-associated protein chaperone prohibitin 2 (PHB2), induces cell-cycle arrest by inhibiting the Notch downstream effector gene Hes1. Anti-cancer activity.
|
-
- HY-14776
-
Quarfloxin
CX-3543
|
DNA/RNA Synthesis
|
Cancer
|
Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
|
-
- HY-N4327
-
Eurycomalactone
|
NF-κB
|
Infection
Inflammation/Immunology
|
Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
|
-
- HY-14452
-
Fatostatin
125B11
|
Fatty Acid Synthase (FASN)
|
Cancer
|
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-N0814A
-
Phytic acid dodecasodium salt hydrate
Inositol hexaphosphate dodecasodium salt hydrate; myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-100131
-
GSK481
|
RIP kinase
|
Inflammation/Immunology
|
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM.
|
-
- HY-P1189A
-
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-111747
-
TBAJ-587
|
Bacterial
|
Infection
Cardiovascular Disease
|
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 µg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization.
|
-
- HY-118567
-
Bis(maltolato)oxovanadium(IV)
BMOV
|
Phosphatase
|
Metabolic Disease
|
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.
|
-
- HY-15785
-
TAS-116
|
HSP
|
Cancer
|
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
|
-
- HY-N1074
-
Warangalone
Scandenolone
|
Parasite
PKA
|
Infection
Inflammation/Immunology
|
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
|
-
- HY-122725B
-
-
- HY-118870
-
-
- HY-122725
-
Lenalidomide-C5-NH2
Cereblon Ligand-Linker Conjugates 19; E3 ligase Ligand-Linker Conjugates 31
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTAC, such as MDM2 PROTAC degrader.
|
-
- HY-42424
-
(S,R,S)-AHPC-Me hydrochloride
VHL ligand 2 hydrochloride; E3 ligase Ligand 1
|
Ligand for E3 Ligase
|
Cancer
|
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-42424A
-
(S,R,S)-AHPC-Me dihydrochloride
VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
|
Ligand for E3 Ligase
|
Cancer
|
(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-15779
-
K145
|
SPHK
Apoptosis
|
Cancer
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity.
|
-
- HY-125171
-
IAXO-102
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
|
-
- HY-15779A
-
K145 hydrochloride
|
SPHK
Apoptosis
|
Cancer
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.
|
-
- HY-137377
-
TAS-119
|
Aurora Kinase
|
Cancer
|
TAS-119 is a potent, selective and orally active Aurora A inhibitor with an IC50 of 1.0 nM. TAS-119 shows high selectivity for Aurora A over other protein kinases, including Aurora B (IC50 of 95 nM). TAS-119 has potent antitumor activites.
|
-
- HY-107222
-
Lysionotin
|
Others
|
Inflammation/Immunology
|
Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
|
-
- HY-112038
-
GSK2983559 free acid
|
RIP kinase
|
Inflammation/Immunology
|
GSK2983559 free acid (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples.
|
-
- HY-125039
-
N-Acetyl lysyltyrosylcysteine amide
|
Glutathione Peroxidase
|
Neurological Disease
Cardiovascular Disease
|
N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
|
-
- HY-113248
-
-
- HY-112171
-
-
- HY-131960
-
-
- HY-P1580
-
-
- HY-B0621
-
-
- HY-131163
-
BM-Cyclin
|
Antibiotic
|
Infection
|
BM-Cyclin is a combination of two antibiotics, Tiamulin and Minocycline, both of which prevent protein synthesis.
|
-
- HY-15291
-
-
- HY-12411
-
-
- HY-16714
-
4-Azido-L-phenylalanine
p-Azidophenylalanine; p-Azido-L-phenylalanine
|
Others
|
Others
|
4-Azido-L-phenylalanine is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments.
|
-
- HY-16714A
-
4-Azido-L-phenylalanine hydrochloride
p-Azidophenylalanine hydrochloride; p-Azido-L-phenylalanine hydrochloride
|
Others
|
Others
|
4-Azido-L-phenylalanine hydrochloride is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments.
|
-
- HY-112609
-
-
- HY-41547
-
Thalidomide 4-fluoride
Cereblon ligand 4; E3 ligase Ligand 4
|
Ligand for E3 Ligase
|
Cancer
|
Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966).
|
-
- HY-130245
-
PCSK9 ligand 1
|
Ser/Thr Protease
|
Metabolic Disease
|
PCSK9 ligand 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 ligand 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.
|
-
- HY-129811
-
Bis-ANS dipotassium
|
Microtubule/Tubulin
|
Neurological Disease
|
Bis-ANS dipotassium is a fluorescent probe of hydrophobic protein. Bis-ANS binds to tubulin with a Kd of 2 μM. Bis-ANS dipotassium is a potent biphasic modulator of protein liquid-liquid phase separation (LLPS). Bis-ANS dipotassium promotes LLPS at low concentrations but suppresses LLPS at high concentrations.
|
-
- HY-125845A
-
(S,S,S)-AHPC hydrochloride
(S,S,S)-VH032-NH2 hydrochloride
|
Ligand for E3 Ligase
|
Cancer
|
(S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
|
-
- HY-10230
-
Midostaurin
PKC412; CGP 41251
|
PKC
|
Cancer
|
Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- HY-124796
-
Qstatin
|
Bacterial
|
Infection
|
QStatin is a potent and selective inhibitor of SmcR (V. harveyi LuxR homologue) with an EC50 of 208.9 nM, binding tightly to SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin shows pan-QS (Vibrio quorum sensing) inhibitor activity in diverse Vibrio species and attenuates their virulence in an aquatic host. QStatin may be a sustainable antivibriosis agent useful in aquacultures.
|
-
- HY-18756A
-
NSC-87877 disodium
|
Phosphatase
Apoptosis
|
Cancer
|
NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
|
-
- HY-18756
-
NSC-87877
|
Phosphatase
Apoptosis
|
Others
|
NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
|
-
- HY-136570
-
GSK778
iBET-BD1
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
Inflammation/Immunology
|
GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
|
-
- HY-13547
-
ADPM06
|
Apoptosis
|
Cancer
|
ADPM06, a lead candidate azadipyrromethene, is a novel nonporphyrin photodynamic therapeutic (PDT) agent. ADPM06 exhibits IC50 values in the micro-molar range in human tumor cells and induces apoptosis.
|
-
- HY-B0220D
-
Erythromycin thiocyanate
|
Bacterial
Antibiotic
|
Infection
|
Erythromycin thiocyanate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin thiocyanate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-101569
-
LXS196
|
PKC
|
Cancer
|
LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research.
|
-
- HY-119917
-
Gossypetin
|
p38 MAPK
Bacterial
|
Cancer
Infection
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
|
-
- HY-100500
-
Lenampicillin hydrochloride
KBT 1585 hydrochloride
|
Bacterial
|
Cancer
|
Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection .
|
-
- HY-N6818
-
5,7,4'-Trimethoxyflavone
|
Apoptosis
Caspase
PARP
|
Cancer
|
5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
|
-
- HY-126396
-
Sordarin sodium
|
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
Sordarin is a potent diphthamide-dependent eEF2 inhibitor with antifungal properties. Sordarin targets eEF2 so as to inhibit protein translation by blocking eEF2-mediated translocation of tRNAs. Sordarin inhibits translation specifically in certain fungi (e.g. C. albicans, C. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae).
|
-
- HY-10118
-
Filibuvir
|
HCV
DNA/RNA Synthesis
|
Infection
|
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively. Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation.
|
-
- HY-12270
-
T-5224
|
MMP
|
Others
|
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.
|
-
- HY-124745
-
KY-05009
|
MAP4K
Wnt
Apoptosis
|
Cancer
|
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
|
-
- HY-122815
-
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-130618
-
Boc-C1-PEG3-C4-OH
|
PROTAC Linker
|
Cancer
|
Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-19800
-
ML-098
CID-7345532
|
Ras
|
Cancer
|
ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.
|
-
- HY-P1053
-
-
- HY-W000450
-
-
- HY-P0291
-
Kemptide Phospho-Ser5
|
PKA
|
Others
|
Kemptide (Phospho-Ser5) is a phosphate acceptor peptide that serves as a specific substrate for cAMP-dependent protein kinase (PKA).
|
-
- HY-19347
-
-
- HY-P0315
-
Crosstide
|
Akt
|
Others
|
Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.
|
-
- HY-109567
-
Gemcabene
PD-72953
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
|
-
- HY-120006A
-
(rel)-AR234960
|
ERK
|
Cardiovascular Disease
|
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
|
-
- HY-130641
-
Br-C10-methyl ester
|
PROTAC Linker
|
Cancer
|
Br-C10-methyl ester is a PROTAC linker, which refers to the alkyl/ether composition. Br-C10-methyl ester is used in the synthesis of a series of PROTACs (MS432). PROTACs contain two different ligands connected by a linker; one is the VHL ligand portion and the other is for the target protein.
|
-
- HY-10704
-
PTP1B-IN-1
PTP1B inhibitor
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
|
-
- HY-16926
-
CK-666
|
Arp2/3 Complex
|
Others
|
CK-666 is a cell-permeable inhibitor of actin-related protein Arp2/3 complex, and binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation.
|
-
- HY-12728
-
Tautomycin
|
Phosphatase
|
Inflammation/Immunology
|
Tautomycin, an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus, is a potent and specific inhibitor of protein phosphatases 1 and 2A and induces contraction of smooth muscle under Ca 2+-free conditions, with Kiapp values of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively.
|
-
- HY-117656
-
ESI-05
NSC 116966
|
Others
|
Others
|
ESI-05 (NSC 116966) is a specific antagonist of EPAC2 (exchange protein directly activated by cAMP 2), with an IC50 of 0.4 µM. ESI-05 (NSC 116966) inhibits cAMP-mediated activation of EPAC2 as well as EAPC2 mediated Rap1 activation.
|
-
- HY-B0117D
-
Tigecycline hydrate
GAR-936 hydrate
|
Bacterial
Autophagy
Antibiotic
|
Infection
|
Tigecycline hydrate (GAR-936 hydrate) is a broad spectrum glycylcycline antibiotic. Tigecycline hydrate is bacteriostatic, that inhibits protein synthesis by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation. Tigecycline hydrate is active against resistant strains of Gram-positive and Gram-negative bacteria.
|
-
- HY-18901
-
RIPK1-IN-4
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.
|
-
- HY-115470
-
CLK-IN-T3
|
CDK
DYRK
|
Cancer
|
CLK-IN-T3 is a high potent, selective, and stable CDC-like kinase (CLK) inhibitor with IC50s of 0.67 nM, 15 nM, and 110 nM for CLK1, CLK2, and CLK3 protein kinases, respectively. CLK-IN-T3 has anti-cancer activity.
|
-
- HY-15510B
-
Tenovin-6 Hydrochloride
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-129065
-
Nourseothricin sulfate
Streptothricin sulfate
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells.
|
-
- HY-135902A
-
Synucleozid hydrochloride
NSC 377363 hydrochloride
|
DNA/RNA Synthesis
|
Neurological Disease
|
Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-128171
-
Diflapolin
|
FLAP
Epoxide Hydrolase
|
Inflammation/Immunology
|
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of 30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM).
|
-
- HY-B0537A
-
Pentamidine dihydrochloride
MP-601205 dihydrochloride
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-129113
-
α-Chaconine
|
COX
|
Inflammation/Immunology
|
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-14452A
-
Fatostatin hydrobromide
125B11 hydrobromide
|
Fatty Acid Synthase (FASN)
|
Cancer
|
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-B0537
-
Pentamidine
MP-601205
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-N2513
-
β-Boswellic acid
|
Lipoxygenase
DNA/RNA Synthesis
|
Cancer
|
β-Boswellic acid is isolated from the gum resin of Boswellia serrate.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
|
-
- HY-15510
-
Tenovin-6
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-124822
-
COH-SR4
|
AMPK
|
Cancer
Metabolic Disease
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation, and can be used for the research of obesity and related metabolic disorders.
|
-
- HY-B0879A
-
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
-
- HY-100434
-
PD-161570
|
FGFR
PDGFR
EGFR
Src
TGF-β Receptor
|
Cancer
Cardiovascular Disease
|
PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
|
-
- HY-P0228
-
-
- HY-114165
-
-
- HY-P0265A
-
-
- HY-16079
-
AZD3514
|
Androgen Receptor
|
Cancer
|
AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.
|
-
- HY-15448
-
-
- HY-U00004
-
OSIP-486823
OSIP 486823; OSIP486823; CP248
|
Microtubule/Tubulin
|
Cancer
|
OSIP-486823 is a novel microtubule-interfering agent with distinct biological effects on both protein kinase G (PKG) and microtubules.
|
-
- HY-P0195
-
-
- HY-42360
-
SMCC
|
ADC Linker
|
Cancer
|
SMCC is a protein crosslinker. SMCC-conjugated antigen coupled spleen cells to induce antigen-specific immune responses.
|
-
- HY-129099
-
N-Desmethyltamoxifen
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-100853
-
IWP-O1
|
Porcupine
Wnt
|
Cancer
|
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
|
-
- HY-P1297
-
CRF(6-33)(human)
|
CRFR
|
Neurological Disease
|
CRF(6-33)(human) is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) has anti-obesity effect.
|
-
- HY-P1098
-
Ac2-26
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-100433
-
PACMA 31
|
Others
|
Cancer
|
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues.
|
-
- HY-19828
-
Herboxidiene
GEX1A
|
DNA/RNA Synthesis
|
Cancer
|
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
|
-
- HY-100725
-
BM212
|
Bacterial
|
Infection
|
BM212 is a potent Mycobacterial membrane protein Large 3 (MmpL3) inhibitor. BM212 has strong bactericidal activity against both M. tuberculosis and some nontuberculosis mycobacteria. BM212 exhibits antimycobacterial activity against M. tuberculosis H37Rv with a MIC of 5 µM.
|
-
- HY-100573
-
Necrosulfonamide
|
Mixed Lineage Kinase
|
Cancer
|
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-N4113
-
Glycycoumarin
|
Autophagy
|
Cancer
|
Glycycoumarin is a major bioactive coumarin of licorice. Glycycoumarin inhibits hepatocyte lipoapoptosis through activation of autophagy and inhibition of ER stress-mediated JNK and GSK-3-mediated mitochondrial pathway. Glycycoumarin exerts anti-liver cancer activity by directly targeting T-LAK cell-originated protein kinase .
|
-
- HY-13491
-
GNF-5837
|
Trk Receptor
|
Cancer
|
GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
|
-
- HY-N3028
-
Taccalonolide B
|
Microtubule/Tubulin
|
Cancer
|
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.
|
-
- HY-129099A
-
N-Desmethyltamoxifen hydrochloride
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-122054
-
BPK-29
|
Others
|
Cancer
|
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-134653
-
5-Ph-IAA
|
Others
|
Cancer
|
5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.
|
-
- HY-N1967
-
Dihydrocurcumin
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
|
-
- HY-109567A
-
Gemcabene calcium
PD-72953 calcium
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
Gemcabene calcium (PD-72953 calcium), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
|
-
- HY-122054A
-
BPK-29 hydrochloride
|
Others
|
Cancer
|
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-110258
-
ML334
LH601A
|
Keap1-Nrf2
|
Cancer
|
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
|
-
- HY-108511A
-
PB28
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Cancer
Infection
|
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
|
-
- HY-N6712
-
Thiolutin
Acetopyrrothin
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
|
-
- HY-10037
-
Quiflapon
MK-591
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
|
-
- HY-110266
-
GN44028
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
|
-
- HY-10466
-
Daclatasvir
BMS-790052; EBP 883
|
HCV
|
Infection
|
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.
|
-
- HY-100499
-
Tyrphostin AG 528
Tyrphostin B66; AG 528
|
EGFR
|
Cancer
|
Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively.
Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2. Tyrphostin AG 528 is also an anticancer agent.
|
-
- HY-107426
-
Verrucarin A
Muconomycin A
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
|
-
- HY-10465
-
Daclatasvir dihydrochloride
BMS-790052 dihydrochloride; EBP 883 dihydrochloride
|
HCV
|
Infection
|
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively.
|
-
- HY-12523
-
Peptide M
|
Others
|
Others
|
Peptide M is a 50 aa synthetic peptide derived from a streptococcal M protein containing an additional C-terminal cysteine residue.
|
-
- HY-D1025
-
C-Phycocyanin
C-PC
|
Others
|
Cancer
|
C-phycocyanin (C-PC) is a water-soluble protein pigment which is also widely used as an excellent nutrient supplement for human beings.
|
-
- HY-B1654
-
-
- HY-P1344A
-
-
- HY-13233A
-
Talabostat mesylate
Val-boroPro mesylate; PT100 mesylate
|
Dipeptidyl Peptidase
|
Cancer
Inflammation/Immunology
|
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
|
-
- HY-N2484
-
Methylnissolin
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade.
|
-
- HY-13233
-
Talabostat
Val-boroPro; PT100
|
Dipeptidyl Peptidase
|
Cancer
Inflammation/Immunology
|
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.
|
-
- HY-131442
-
Alkyne tyramide
|
Others
|
Others
|
Alkyne tyramide is a clickable ascorbate peroxidase 2 (APEX2) probe. Alkyne tyramide substantially improves APEX-labeling efficiency in intact yeast cells, as it is more cell wall-permeant than APEX2 substrate biotin-phenol (BP). Alkyne tyramide also facilitates the identification of APEX-labeling sites, allowing the unambiguous assignment of membrane topology of mitochondrial proteins.
|
-
- HY-A0072S
-
Zilpaterol-d7
|
Adrenergic Receptor
|
Endocrinology
|
Zilpaterol-d7 is a deuterium labeled Zilpaterol. Zilpaterol is a β-adrenergic receptor agonist that putatively, through activation of protein kinase A, increases protein synthesis in skeletal muscle fibers as well as reduces lipogenesis and increases lipolysis in adipose tissues. Formulations containing Zilpaterol have been used to increase lean body weight and improve feed efficiency in commercial beef cattle.
|
-
- HY-B1599
-
Chloramphenicol palmitate
|
Bacterial
|
Infection
|
Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes.
|
-
- HY-12533
-
Disopyramide
Dicorantil; SC-7031
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
|
Disopyramide (Dicorantil) is a class IA antiarrhythmic drug with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action.
|
-
- HY-130604
-
DT2216
|
PROTAC
Apoptosis
|
Cancer
|
DT2216 is a potent and selective BCL-XL 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.
|
-
- HY-B1816
-
-
- HY-17439
-
Salinomycin sodium salt
Salinomycin sodium; Sodium salinomycin
|
Wnt
β-catenin
Bacterial
Autophagy
Apoptosis
Antibiotic
|
Cancer
|
Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt (Salinomycin sodium) acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt (Salinomycin sodium) shows selective activity against human cancer stem cells.
|
-
- HY-100538A
-
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-P1098A
-
Ac2-26 TFA
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-B0817
-
Pyridaben
|
Parasite
|
Infection
|
Pyridaben is a METI acaricide that inhibits mitochondrial electron transport at complex I (METI; Ki = 0.36 nmol/mg protein in rat brain mitochondria). Pyridaben is active against a variety of mites, inducing 100% mortality of C. malaccensis, D. farina, and T. putrescentia when administered via filter paper contact at doses of 25, 100, and 200 mg/mL, respectively.
|
-
- HY-B0644
-
Sucralfate
Sucrose octasulfate-aluminum complex
|
Bacterial
|
Infection
Inflammation/Immunology
Cancer
|
Sucralfate (Sucrose octasulfate-aluminum complex) is a potent and orally active gastroprotectant with no systemic effects. Sucralfate inhibits peptic activity and binds to negatively charged subepithelial proteins exposed during mucosal injury, forming a viscous layer that protects the vascular bed and proliferative zone. Sucralfate is used for prevention and treatment of several gastrointestinal diseases in vivo.
|
-
- HY-114407
-
TD-428
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
|
-
- HY-12278
-
K02288
|
TGF-β Receptor
|
Others
|
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
|
-
- HY-101379A
-
8-Bromo-cGMP sodium
|
Calcium Channel
|
Neurological Disease
Cardiovascular Disease
|
8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator. 8-Bromo-cGMP sodium significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects and results in vasodilator responses.
|
-
- HY-P1297A
-
CRF(6-33)(human) TFA
|
CRFR
|
Neurological Disease
|
CRF(6-33)(human) TFA is a CRF binding protein (CRF-BP) ligand inhibitor. CRF(6-33)(human) TFA competitively binds the CRF-BP but not the post-synaptic CRF receptors. CRF(6-33)(human) TFA has anti-obesity effect.
|
-
- HY-122181B
-
OTS186935 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
|
-
- HY-130619
-
Boc-C1-PEG3-C4-OBn
|
PROTAC Linker
|
Cancer
|
Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
|
-
- HY-103463
-
SA57
|
FAAH
MAGL
|
Neurological Disease
|
SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
|
-
- HY-B0537B
-
Pentamidine isethionate
MP-601205 isethionate
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-Y0017
-
-
- HY-P0225
-
-
- HY-N0593
-
-
- HY-32341
-
Seocalcitol
EB 1089
|
VD/VDR
|
Cancer
|
Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.
|
-
- HY-10996A
-
-
- HY-B1654A
-
-
- HY-N0593A
-
-
- HY-112779
-
Pertussis Toxin
|
Others
|
Infection
|
Pertussis Toxin is a protein-based AB5-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough.
|
-
- HY-N7698A
-
-
- HY-19863
-
-
- HY-124131
-
DS-437
|
Histone Methyltransferase
|
Cancer
Inflammation/Immunology
|
DS-437 is a dual PRMT5/7 inhibitor (IC50s of PRMT5/7=6 μM). DS-437 is selective for PRMT5 and PRMT7 over 29 other human protein-, DNA-, and RNA-methyltransferases. DS-437 is a S-adenosylmethionine (SAM)-competitive inhibitor of PRMT5. DS-437 also inhibits DNMT3A and DNMT3B, with IC50s of 52 and 62 μM, respectively. DS-437 inhibits the methylation of FOXP3.
|
-
- HY-104040
-
MKC8866
|
IRE1
|
Cancer
|
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
|
-
- HY-141178
-
-
- HY-141181
-
-
- HY-133049
-
-
- HY-130146
-
-
- HY-130382
-
-
- HY-121507
-
-
- HY-130554
-
-
- HY-141187
-
-
- HY-107425
-
MZ 1
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
MZ 1 is a PROTAC BRD4 degrader. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
|
-
- HY-41921
-
-
- HY-130390
-
-
- HY-141159
-
-
- HY-141166
-
-
- HY-133230
-
-
- HY-130563
-
-
- HY-112559
-
-
- HY-141160
-
-
- HY-115414
-
-
- HY-130147
-
-
- HY-141161
-
-
- HY-141183
-
-
- HY-130374
-
-
- HY-133229
-
-
- HY-130137
-
-
- HY-141180
-
-
- HY-130389
-
-
- HY-130375
-
-
- HY-117045
-
-
- HY-126977
-
-
- HY-141189
-
-
- HY-141179
-
-
- HY-120587
-
-
- HY-141177
-
-
- HY-126891
-
-
- HY-141169
-
-
- HY-130378
-
-
- HY-130584
-
-
- HY-114670
-
-
- HY-141162
-
-
- HY-134591
-
-
- HY-130373
-
-
- HY-130819
-
-
- HY-130380
-
-
- HY-130384
-
-
- HY-141188
-
-
- HY-113921
-
-
- HY-141168
-
-
- HY-140015
-
-
- HY-10969
-
Obatoclax Mesylate
GX15-070 Mesylate
|
Bcl-2 Family
Autophagy
Parasite
|
Cancer
Infection
|
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
|
-
- HY-124418
-
SBI-477
|
Others
|
Metabolic Disease
|
SBI-477 is a chemical probe stimulated insulin signaling by deactivating the transcription factor MondoA, leading to reduced expression of the insulin pathway suppressors thioredoxin-interacting protein (TXNIP) and arrestin domain–containing 4 (ARRDC4). SBI-477 coordinately inhibits triacylglyceride (TAG) synthesis and enhances basal glucose uptake in human skeletal myocytes.
|
-
- HY-111753A
-
WDR5-IN-4 TFA
|
Histone Methyltransferase
|
Cancer
|
WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity.
|
-
- HY-P1306
-
Obestatin(rat)
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-14428
-
ICG-001
|
β-catenin
Apoptosis
|
Cancer
|
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
|
-
- HY-N4170
-
Chebulic acid
|
Others
|
Metabolic Disease
|
Chebulic acid, a phenolcarboxylic acid compound isolated from Terminalia chebula, has potent anti-oxidant activity,
which breaks the cross-links of proteins induced by advanced glycation end-products (AGEs) and inhibits the formation of AGEs. Chebulic acid is effective in controlling elevated metabolic parameters, oxidative stress and renal damage, supporting its beneficial effect in diabetic nephropathy.
|
-
- HY-16918
-
Heptamidine
SBi4211
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-117282
-
JG-98
|
HSP
Apoptosis
|
Cancer
|
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
|
-
- HY-N3187
-
-
- HY-10969A
-
Obatoclax
GX15-070
|
Bcl-2 Family
Autophagy
Parasite
|
Cancer
Infection
|
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
|
-
- HY-B0665
-
Fibrin
|
Others
|
Cardiovascular Disease
|
Fibrin, isolated from bovine blood, is an insoluble protein produced in response to bleeding. Fibrin is the major component of the blood clot and is used for coagulation.
|
-
- HY-P0216
-
-
- HY-P0313
-
CEF6
|
Influenza Virus
|
Infection
|
CEF6 is a 9-aa-long peptide corresponding to aa 418-426 of the influenza A virus (H1N1) nucleocapsid protein.
|
-
- HY-N2111
-
-
- HY-136269
-
-
- HY-W018004
-
-
- HY-138065
-
Iodoacetyl-LC-biotin
|
Apoptosis
|
Others
|
Iodoacetyl-LC-biotin is a biotinylated electrophile probe that can be used to investigate the scope and characteristics of protein covalent binding to subcellular proteomes.
|
-
- HY-122720
-
SEC inhibitor KL-1
KL-1
|
Others
|
Cancer
|
SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM.
|
-
- HY-123972
-
SEC inhibitor KL-2
KL-2
|
Others
|
Cancer
|
SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM.
|
-
- HY-124675
-
MYCMI-6
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
|
-
- HY-10230S
-
Midostaurin-D5
PKC412-D5; CGP 41251-D5
|
Others
|
Cancer
|
Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- HY-128598
-
MD2-TLR4-IN-1
|
Toll-like Receptor (TLR)
|
Cancer
Inflammation/Immunology
|
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
|
-
- HY-18303
-
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
AMG-47a is a potent and orally bioavailable lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2,p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-10029
-
Nutlin-3a
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
|
-
- HY-N0322
-
Cholesterol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Metabolic Disease
|
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
|
-
- HY-P1051
-
β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-P1051A
-
β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
|
Amyloid-β
|
Neurological Disease
|
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-12695B
-
-
- HY-113352
-
7-Methylguanine
|
Endogenous Metabolite
|
Others
|
7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein–DNA interactions and a key component of DNA sequencing method.
|
-
- HY-103449
-
-
- HY-12306
-
8-Bromo-cAMP sodium salt
8-Br-Camp sodium salt
|
PKA
|
Cancer
|
8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt), a cyclic AMP analog, is an activator of cyclic AMP-dependent protein kinase (PKA).
|
-
- HY-130259
-
LC3-mHTT-IN-AN2
|
Autophagy
|
Neurological Disease
|
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-130258
-
LC3-mHTT-IN-AN1
|
Autophagy
|
Neurological Disease
|
LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-P9804
-
Anti-MERS-2E6 mAb
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-B0956
-
Paromomycin sulfate
Aminosidine sulfate
|
Antibiotic
Parasite
Bacterial
|
Infection
|
Paromomycin (Aminosidine) sulfate, a neomycin (HY-B0470) derivative, is a broad spectrum aminoglycoside antibiotic with amebicidal and bactericidal effects. Paromomycin sulfate prematures termination of translation of mRNA and inhibits protein synthesis by specifically binds to the RNA oligonucleotide at the A site of bacterial 30S ribosomes. Paromomycin sulfate can be used for the research of bacterial and parasitic infections.
|
-
- HY-16918A
-
Heptamidine dimethanesulfonate
SBi4211 dimethanesulfonate
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-129491
-
O-Desmethyl Midostaurin
CGP62221; O-Desmethyl PKC412
|
PKC
|
Cancer
|
O-Desmethyl Midostaurin (CGP62221; O-Desmethyl PKC412) is the active metabolite of Midostaurin (HY-10230) via cytochrome P450 liver enzyme metabolism. O-Desmethyl Midostaurin can be used as an indicator for Midostaurin metabolism in vivo. Midostaurin is a multi-targeted protein kinase inhibitor with IC50 ranging from 22-500 nM.
|
-
- HY-12649
-
Y16
|
Ras
|
Cancer
|
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
|
-
- HY-136571
-
GSK046
iBET-BD2
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK046 (iBET-BD2) is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
|
-
- HY-137892
-
GSK620
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
|
-
- HY-15652
-
Freselestat
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
|
-
- HY-114158A
-
Pronase E (Activity≥4000 U/mg)
Pronase (Activity≥4000 U/mg)
|
Others
|
Others
|
Pronase E (Activity≥4000 U/mg) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-131018
-
-
- HY-103633
-
-
- HY-N0666B
-
Aspartic acid calcium
Calcium L-aspartate
|
Others
|
Cardiovascular Disease
|
Aspartic acid calcium (Calcium L-aspartate) is a chelate where calcium is attached to an amino acid naming L-Aspartic acid. L-Aspartic acid is an amino acid and serves as a building block for proteins in the body.
|
-
- HY-112929
-
DT-061
|
Phosphatase
|
Cancer
|
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
|
-
- HY-112484
-
RS-246204
|
Others
|
Cancer
|
RS-246204 is a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein.
|
-
- HY-136456
-
2-NP-AMOZ
|
Others
|
Others
|
2-NP-AMOZ is a 2-nitrophenyl derivative of AMOZ (a metabolite of antibiotic Furaltadone), can be used to detect protein bound AMOZ.
|
-
- HY-124622
-
-
- HY-A0098
-
Tunicamycin
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
|
-
- HY-19719
-
Miransertib
ARQ-092
|
Akt
Parasite
|
Cancer
Infection
|
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-101855
-
Anle138b
|
Amyloid-β
|
Neurological Disease
|
Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
|
-
- HY-107024
-
Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
|
Others
|
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
|
-
- HY-137315
-
TML-6
|
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-100233
-
IQ-1S free acid
|
JNK
|
Cancer
Inflammation/Immunology
|
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
|
-
- HY-110135A
-
NBI-31772 hydrate
|
IGF-1R
|
Neurological Disease
|
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.
|
-
- HY-W014316
-
5-Bromo-5-nitro-1,3-dioxane
|
Bacterial
Fungal
|
Infection
|
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol.
|
-
- HY-122895
-
E64FC26
|
Apoptosis
|
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-P1306A
-
Obestatin(rat) TFA
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-16908A
-
Lefamulin acetate
BC-3781 acetate
|
Bacterial
Antibiotic
|
Infection
|
Lefamulin acetate (BC-3781 acetate) is an orally active antibiotic for community-acquired bacterial pneumonia (CABP) treatment. Lefamulin acetate (BC-3781 acetate) is the first semi-synthetic pleuromutilin for systemic treatment of bacterial infections in humans. Lefamulin acetate (BC-3781 acetate) inhibits protein synthesis by binding to the peptidyl transferase center of the 50S bacterial ribosome, preventing the binding of transfer RNA for peptide transfer.
|
-
- HY-126047B
-
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-122198
-
ML367
|
Others
|
Cancer
|
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation.
|
-
- HY-N0762
-
Isobavachin
|
Others
|
Neurological Disease
|
Isobavachin, an antioxidant isaolated from Psoralea morisiana with a prenyl group at position 8 of ring A, promotes neuronal differentiation and the potential role of its protein prenylation.
|
-
- HY-P0228A
-
-
- HY-N0023
-
Cistanoside A
|
Others
|
Inflammation/Immunology
|
Cistanoside A is a phenylethanoid isolated from Cistanche deserticola, reduces NO accumulation, but shows no effect on iNOS mRNA, iNOS protein levels or iNOS activity. Anti-inflammatory effect.
|
-
- HY-N4322
-
-
- HY-128808
-
cIAP1 ligand 1
E3 ligase Ligand 12
|
Ligand for E3 Ligase
|
Cancer
|
cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER.
|
-
- HY-114158
-
Pronase E (Activity≥7000 U/g)
Pronase (Activity≥7000 U/g)
|
Others
|
Others
|
Pronase E (Activity≥7000 U/g) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-112331
-
SJ000291942
|
TGF-β Receptor
|
Cancer
|
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
|
-
- HY-14537
-
-
- HY-120722
-
TCH-165
|
Proteasome
|
Cancer
|
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
|
-
- HY-115446A
-
Lenalidomide-C4-NH2 hydrochloride
Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively.
|
-
- HY-B0779A
-
(5E,9E,13E)-Teprenone
(5E,9E,13E)-Geranylgeranylacetone
|
Others
|
Metabolic Disease
|
(5E,9E,13E)-Teprenone ((5E,9E,13E)-Geranylgeranylacetone) is an isomer of Teprenone with antiulcer activity. (5E,9E,13E)-Teprenone induces transcriptional activation of HSP genes that may increase gastric mucosal defense at conditions of stress.
|
-
- HY-129938
-
-
- HY-116896
-
LY117018
|
Estrogen Receptor/ERR
|
Cancer
|
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines.
|
-
- HY-A0162
-
Quinupristin
|
Bacterial
|
Infection
|
Quinupristin is a streptogramin antibiotic. Quinupristin blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits .
|
-
- HY-A0162A
-
Quinupristin mesylate
|
Bacterial
|
Infection
|
Quinupristin mesylate is a streptogramin antibiotic. Quinupristin mesylate blocks peptide bond synthesis to prevent the extension of polypeptide chains and promote the detachment of incomplete protein chains in the bacterial ribosomal subunits.
|
-
- HY-B0129
-
Aztreonam
SQ-26,776
|
Bacterial
Antibiotic
|
Infection
|
Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very high affinity for penicillin-binding protein 3 (PBP-3).
|
-
- HY-136276
-
DMNB-caged-Serine
|
Others
|
Others
|
DMNB-caged-Serine photoactivates to release serine by visible blue light (405 nm) in cells. DMNB can be incorporated into S.cerevisiae proteins when introduces into growth medium at millimolar concentrations.
|
-
- HY-15464D
-
(S)-Gossypol acetic acid
(S)-(+)-Gossypol acetic acid
|
Bcl-2 Family
|
Cancer
|
(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
|
-
- HY-109101
-
Risdiplam
RG7916; RO7034067
|
DNA/RNA Synthesis
|
Neurological Disease
|
Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.
|
-
- HY-109052
-
Atabecestat
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
|
-
- HY-17408
-
-
- HY-117570
-
KSC-34
|
Others
|
Neurological Disease
|
KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.
|
-
- HY-100218A
-
RSL3
(1S,3R)-RSL3
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) (ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells.
|
-
- HY-135774
-
6-Hydroxybenzbromarone
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
|
-
- HY-128342
-
Complement C5-IN-1
|
Complement System
|
Inflammation/Immunology
|
Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM.
|
-
- HY-10206
-
Amuvatinib
MP470; HPK 56
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
|
-
- HY-15652A
-
Freselestat quarterhydrate
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
|
-
- HY-100487
-
TAK-243
MLN7243
|
E1/E2/E3 Enzyme
NF-κB
Apoptosis
|
Cancer
|
TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
|
-
- HY-112544
-
IK1 inhibitor PA-6
PA-6
|
Potassium Channel
|
Cardiovascular Disease
|
IK1 inhibitor PA-6 (PA-6), a pentamidine analogue, is a selective and potent IK1 (KIR2.x ion-channel-carried inward rectifier current) inhibitor, with IC50 values of 12-15 nM for human and mouse KIR2.x currents. IK1 inhibitor PA-6 (PA-6) elevates KIR2.1 protein expression and induces intracellular KIR2.1 accumulation. IK1 inhibitor PA-6 (PA-6) has the potential to treat atrial fibrillation and arrhythmia.
|
-
- HY-B0268A
-
Enoxacin hydrate
Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Infection
Cancer
|
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- HY-112163
-
Zotatifin
eFT226
|
Eukaryotic Initiation Factor (eIF)
SARS-CoV
Apoptosis
|
Cancer
|
Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC50=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC90=37 nM). Zotatifin induces cell apoptosis.
|
-
- HY-B0268
-
Enoxacin
AT 2266; CI 919
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Cancer
Infection
|
Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- HY-108601A
-
Ro 32-0432 hydrochloride
|
PKC
|
Inflammation/Immunology
Neurological Disease
|
Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
|
-
- HY-16558
-
Butein
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
|
-
- HY-131033
-
L-Azidonorleucine hydrochloride
|
Others
|
Others
|
L-Azidonorleucine hydrochloride, an unnatural amino acid, is A Methionine surrogate. L-Azidonorleucine hydrochloride can be used to label mammalian cell proteins and identify a diverse set of methionyl-tRNA synthetase (MetRS) mutants .
|
-
- HY-109103
-
Tegatrabetan
BC2059
|
β-catenin
|
Cancer
|
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
|
-
- HY-114406
-
TD-106
|
Ligand for E3 Ligase
|
Cancer
|
TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
|
-
- HY-119053
-
MS7972
|
MDM-2/p53
|
Cancer
|
MS7972 is a small molecule that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM.
|
-
- HY-W016781
-
D-Arginine
H-D-Arg-OH
|
Others
|
Others
|
D-arginine (H-D-Arg-OH) is the D-isomer of arginine. Arginine is an α-amino acid that is used in the biosynthesis of proteins. D-Arginine is an inactive form of L-arginine.
|
-
- HY-110285
-
ML382
|
Others
|
Neurological Disease
|
ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
|
-
- HY-101763A
-
(S,R,S)-AHPC hydrochloride
VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride
|
Ligand for E3 Ligase
|
Cancer
|
(S,R,S)-AHPC hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
|
-
- HY-125593
-
APG-1387
|
IAP
Apoptosis
|
Cancer
|
APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
|
-
- HY-P0299A
-
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
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TGF-β Receptor
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Cancer
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LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
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- HY-10341
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Fasudil Hydrochloride
HA-1077 Hydrochloride; AT-877 Hydrochloride
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ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
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Cancer
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Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator.
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- HY-117958
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HJC0197
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Others
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Cancer
Metabolic Disease
Cardiovascular Disease
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HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.
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- HY-19918A
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Anatabine dicitrate
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NF-κB
Amyloid-β
nAChR
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Inflammation/Immunology
Neurological Disease
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Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
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- HY-120327
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KY-226
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Phosphatase
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Metabolic Disease
Neurological Disease
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KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
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- HY-14855
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Tedizolid
TR 700; Torezolid; DA-7157
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Bacterial
Antibiotic
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Infection
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Tedizolid (TR 700; Torezolid; DA-7157) is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
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- HY-P1468
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β-Amyloid (1-28)
Amyloid β-Protein (1-28)
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Amyloid-β
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Neurological Disease
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β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
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- HY-131443
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TRC-766
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Others
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Others
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TRC-766 is a negative control of RTC-5 (TRC-382). TRC-766 binds protein phosphatase 2A (PP2A) and does not activate the phosphatase.
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- HY-108717
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Protease K
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Others
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Others
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Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures.
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- HY-119506
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KL044
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Others
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Metabolic Disease
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KL044, a stabilizer of the clock protein cryptochrome (CRY) , is a potent chemical probe with a pEC50 value of 7.32, leading to the extension of the circadian period and repression of Per2 activity.
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- HY-P1466
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β-Amyloid 1-16
Amyloid β-Protein (1-16)
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Amyloid-β
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Neurological Disease
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β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
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- HY-112718
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- HY-15454
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Xevinapant
AT-406; Debio 1143; SM-406
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IAP
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Cancer
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Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM, respectively.
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- HY-103693
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NAZ2329
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Phosphatase
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Cancer
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NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
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- HY-12725
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ML324
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Histone Demethylase
HSV
CMV
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Cancer
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ML324 is a potent JMJD2 demethylase inhibitor with antiviral activity. ML324 also exhibits inhibition for the histone demethylase KDM4B, with an IC50 of 4.9 μM. ML324 has potent anti-viral activity against both herpes simplex virus (HSV) and human cytomegalovirus (hCMV) infection via inhibition viral IE gene expression.
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- HY-N0135
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Tanshinone IIA
Dan Shen ketone
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VEGFR
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Cardiovascular Disease
Cancer
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Tanshinone IIA (Tan IIA) is one of the main fat-soluble compositions in the root of red-rooted salvia. Tanshinone IIA may suppress angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2.
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- HY-136595
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3,5-Difluoro-L-tyrosine
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Phosphatase
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Others
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3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs).
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- HY-P1113
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- HY-P1113A
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- HY-101572
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MHP
Methyl caprooyl tyrosinate
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SPHK
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Inflammation/Immunology
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MHP (Methyl caprooyl tyrosinate) is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production. MHP (Methyl caprooyl tyrosinate) enhances antimicrobial defense and innate immunity.
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- HY-P2657
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