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Results for "

Elys Inhibitors

" in MCE Product Catalog:

519

Inhibitors & Agonists

5

Screening Libraries

1

Dye Reagents

2

Biochemical Assay Reagents

5

Peptides

1

MCE Kits

3

Inhibitory Antibodies

45

Natural
Products

28

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-N9814
    Shanciol B

    NO Synthase Inflammation/Immunology
    Shanciol B, isolated from the ethyl acetate extract of the air-dried whole plant of Pholidota imbricate Hook, inhibits nitric oxide (NO) production and 1,1-diphenyl-2-picrylhydrazil (DPPH) radical scavenging activity. Shanciol B is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with anti-inflammatory activity.
  • HY-112371
    (S)-CR8

    CDK Cancer
    (S)-CR8 is the S-isomer of CR8. (S)-CR8 is a potent and selective CDK inhibitor with IC50s of 0.060, 0.080, 0.11, 0.12, and 0.15 μM for CDK2/cyclin E, CDK2/cyclin A, CDK9/cyclin T, CDK5/p25, and CDK1/cyclin B, respectively. (S)-CR8 reduces SH-SY5Y cells survival (IC50 0.40 μM).
  • HY-15282
    E-64

    Proteinase inhibitor E 64

    Cathepsin Autophagy Bacterial Inflammation/Immunology Cancer
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
  • HY-100962
    (E)-AG 99

    (E)-Tyrphostin 46; (E)-Tyrphostin AG 99

    EGFR Cancer
    (E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
  • HY-116683
    116-9e

    MAL2-11B

    HSP DNA/RNA Synthesis Cancer Infection
    116-9e (MAL2-11B) is a Hsp70 co-chaperone DNAJA1 inhibitor. 116-9e inhibits Simian Virus 40 (SV40) replication and DNA synthesis. 116-9e inhibits tumor antigen (TAg)’s endogenous ATPase activity and the TAg-mediated activation of Hsp70.
  • HY-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-139134
    S-2E

    HMG-CoA Reductase (HMGCR) Acetyl-CoA Carboxylase Cardiovascular Disease
    S-2E is an orally active and noncompetitive HMG-CoA reductase and acetyl-CoA carboxylase inhibitor. S-2E has an anti-hyperlipidemic action. S-2E has the potential for familial hypercholesterolemia and mixed hyperlipidemia research.
  • HY-137487
    PROTAC BRAF-V600E degrader-1

    PROTACs Raf Cancer
    PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth.
  • HY-14178
    VX-11e

    ERK Cancer
    VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with Ki < 2 nM.
  • HY-15166
    (E/Z)-Zotiraciclib

    (E/Z)-TG02; (E/Z)-SB1317

    CDK JAK FLT3 Cancer
    (E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor of CDK2, JAK2, and FLT3. (E/Z)-Zotiraciclib ((E/Z)-TG02) can be used for the research of cancer.
  • HY-13296
    PYR-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
  • HY-15166A
    (E/Z)-Zotiraciclib hydrochloride

    (E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride

    CDK JAK FLT3 Cancer
    (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.
  • HY-14971
    (E)-Akt inhibitor-IV

    (E)-AKTIV

    Akt Cancer
    (E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic.
  • HY-107459
    (E/Z)-AG490

    (E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

    EGFR STAT JAK Cancer
    (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
  • HY-122746
    E67-2

    Histone Methyltransferase Cancer
    E67-2, as the E67 derivative, is a low-toxicity, selective KIAA1718 Jumonji domain inhibitor with an IC50 value of 3.4 µM. E67-2 selectively inhibits histone H3 lysine 9 (H3K9) Jumonji demethylase as well as histone H3 lysine 4 (H3K4) demethylase.
  • HY-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-19183
    E-5324

    Acyltransferase Metabolic Disease
    E-5324 is potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT) with IC50s of 44 to 190 nM.
  • HY-77293
    (E)-[6]-Dehydroparadol

    Apoptosis Keap1-Nrf2 Cancer
    (E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells.
  • HY-103164
    (E)-8-(3-Chlorostyryl)caffeine

    Adenosine Receptor Monoamine Oxidase Neurological Disease
    (E)-8-(3-Chlorostyryl)caffeine is a selective adenosine A2A receptor antagonist. (E)-8-(3-Chlorostyryl)caffeine inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM by a pathway that is independent of its actions on the A2A receptor. (E)-8-(3-Chlorostyryl)caffeine has the potential for Parkinson's disease research.
  • HY-108938
    SDZ285428

    Cytochrome P450 Fungal Parasite Infection
    SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
  • HY-119173
    PBD-150

    Amyloid-β Neurological Disease
    PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a Ki value of 490 nM.
  • HY-121988
    INF4E

    NOD-like Receptor (NLR) Inflammation/Immunology
    INF4E is a potent NLRP3 inflammasome inhibitor. INF4E inhibits caspase-1 and NLRP3 ATPase activities. INF4E shows protection against the IR-induced myocardial injury and dysfunction.
  • HY-131404
    TPBM

    Estrogen Receptor/ERR Cancer
    TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth.
  • HY-U00050
    (E)-10-Hydroxynortriptyline

    E-10-OH-NT

    Drug Metabolite Neurological Disease
    (E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline (HY-B1417). Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline (HY-B0527A). E-10-OH-NT is about 50% as potent as nortriptyline as an inhibitor of the neuronal uptake of norepinephrine in vitro and exhibits less anticholinergic effects in man.
  • HY-N9376
    Kansuinine E

    Others Inflammation/Immunology
    Kansuinine E is a plant-derived nitric oxide inhibitor (IC50=6.3 μM). Kansuinine E belongs to jatrophane-type diterpenoids and is isolated from the roots of E. kansui.
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Cancer
    RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with an IC50 of 4 nM.
  • HY-16667
    HLM006474

    Early 2 Factor (E2F) Cancer
    HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
  • HY-145309
    eIF4E-IN-3

    Eukaryotic Initiation Factor (eIF) Cancer
    eIF4E-IN-3 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-3 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 485).
  • HY-145262
    eIF4E-IN-2

    Eukaryotic Initiation Factor (eIF) Cancer
    eIF4E-IN-2 is a potent inhibitor of eukaryotic initiation factor 4e (eIF4e). eIF4E-IN-2 has the potential for researching eIF4e dependent diseases, including the research of cancer (extracted from patent WO2021003157A1, compound 1188).
  • HY-14427
    4E1RCat

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC50 an of ∼4 μM.
  • HY-132169
    HCoV-229E-IN-1

    SARS-CoV Infection
    HCoV-229E-IN-1 is a potent inhibitor of HCoV-229E replication, with an EC50 of 0.65 μM and 0.6 μM in MTS and CPE cells, respectively.
  • HY-122895A
    (E/Z)-E64FC26

    Apoptosis Cancer
    (E/Z)-E64FC26 is a mixture complex of E-E64FC26 and Z-E64FC26. E64FC26 (E-E64FC26) is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC50s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6. E64FC26 shows anti-myeloma activity.
  • HY-19384
    Enflicoxib

    E 6087

    COX Inflammation/Immunology
    Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models.
  • HY-13540
    E7016

    GPI 21016

    PARP Cancer
    E7016 (GPI 21016) is an orally available PARP inhibitor. E7016 can enhance tumor cell radiosensitivity in vitro and in vivo through the inhibition of DNA repair. E7016 acts as a potential anticancer agent.
  • HY-18956
    (E/Z)-Icerguastat

    (E/Z)-Sephin1; (E/Z)-IFB-088

    Phosphatase Inflammation/Immunology
    (E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research.
  • HY-13068
    Golvatinib

    E-7050

    c-Met/HGFR VEGFR Cancer
    Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
  • HY-112097
    E260

    Others Cancer
    E260 is a Fer/FerT kinase inhibitor.
  • HY-100733
    4E2RCat

    Eukaryotic Initiation Factor (eIF) Autophagy Virus Protease Neurological Disease
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  • HY-N2682A
    (E)-Dehydrodiconiferyl alcohol

    Carbonic Anhydrase Cancer
    (E)-Dehydrodiconiferyl alcohol behaves as good hCA IX and hCA XII dual inhibitors. And (E)-Dehydrodiconiferyl alcohol suppresses the NF-κB nuclear translocation in connective tissue of healing area.
  • HY-136266
    HCV-IN-29

    HCV Cancer
    HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e.
  • HY-10981S1
    Lenvatinib-d5

    E7080-d5

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib-d5 (E7080-d5) is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10981S
    Lenvatinib-d4

    E7080-d4

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib-d4 (E7080-d4) is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-100227
    E 64c

    Cathepsin SARS-CoV Metabolic Disease
    E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-B0131S
    Prostaglandin E1-d4

    Prostaglandin Receptor Endogenous Metabolite Endocrinology Cardiovascular Disease
    Prostaglandin E1-d4 (Alprostadil-d4) is the deuterium labeled Prostaglandin E1. Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.
  • HY-107415
    PLX7922

    Raf Cancer
    PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines.
  • HY-135377
    Atorvastatin 3-Deoxyhept-2E-Enoic Acid

    (2E)-2,3-Dehydroxy Atorvastatin

    Others Metabolic Disease Inflammation/Immunology
    Atorvastatin 3-Deoxyhept-2E-Enoic Acid ((2E)-2,3-Dehydroxy Atorvastatin) is an impurity of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor and has the ability to effectively decrease blood lipids.
  • HY-N2586
    Tenuifoliside C

    Others Inflammation/Immunology
    Tenuifoliside C, isolated from polygala tenuifolia willd, significantly inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1.
  • HY-100229
    Aloxistatin

    E64d; E64c ethyl ester

    Cathepsin SARS-CoV Neurological Disease
    Aloxistatin (E64d) is a cell-permeable and irreversible broad-spectrum cysteine protease inhibitor. Aloxistatin (E64d) exhibits entry-blocking effect for MERS-CoV.
  • HY-W263279
    (E)-Guanabenz

    (E)-Wy-8678

    Adrenergic Receptor Neurological Disease Cardiovascular Disease
    (E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
  • HY-10082A
    (E)-3-AP

    (E)-PAN-811; (E)-NSC# 663249; (E)-OCX191

    DNA/RNA Synthesis Cancer
    (E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis.
  • HY-N4119
    Neoeriocitrin

    Cholinesterase (ChE) Neurological Disease
    Neoeriocitrin, isolated from Drynaria Rhizome, shows activity on proliferation and osteogenic differentiation in MC3T3-E1. Neoeriocitrin is a potent acetylcholinesterase (AChE) inhibitor.
  • HY-13013
    (E)-SIS3

    TGF-beta/Smad Inflammation/Immunology
    (E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
  • HY-100287
    2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide

    Prostaglandin Receptor Phospholipase Endocrinology
    2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
  • HY-Y0367
    Maleic Acid

    Endogenous Metabolite Bacterial Infection
    Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
  • HY-B1388
    Homatropine methylbromide

    Homatropine methobromide

    mAChR Neurological Disease
    Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
  • HY-15582
    Auristatin E

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates. Auristatin E inhibits cell division by blocking the polymerisation of tubulin.
  • HY-114041S1
    Resolvin E1-d4-1

    RvE1-d4-1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin E1-d4-1 (RvE1-d4-1) is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
  • HY-W008914
    (E/Z)-CP-724714

    EGFR Cancer
    (E/Z)-CP-724714 is a racemic compound of (E)-CP-724714 and (Z)-CP-724714 isomers. CP-724714 is a potent and selective orally active ErbB2 (HER2) inhibitor.
  • HY-12026
    WZ4002

    EGFR Cancer
    WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
  • HY-N0060BS
    (E)-Ferulic acid-d3

    (E)-Coniferic acid-d3

    β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite Cancer
    (E)-Ferulic acid-d3 ((E)-Coniferic acid-d3) is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
  • HY-19831
    4EGI-1

    Eukaryotic Initiation Factor (eIF) Autophagy Apoptosis Cancer
    4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
  • HY-17547
    NMS-E973

    HSP Cancer
    NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
  • HY-14566S
    Donepezil-d7 hydrochloride

    E2020-d7

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d7 (hydrochloride) (E2020-d7) is the deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
  • HY-139825
    Indoluidin E

    Dihydroorotate Dehydrogenase Cancer
    Indoluidin E selectively inhibits DHODH and suppresses cancer cell growth.
  • HY-12001
    WZ-3146

    EGFR Cancer
    WZ3146 is a mutant selective EGFR inhibitor with IC50s of 2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
  • HY-11004
    AZ 628

    Raf Apoptosis Cancer
    AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
  • HY-N0998
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one

    Others Cancer
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 µM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders.
  • HY-137458A
    Vevorisertib trihydrochloride

    ARQ 751 trihydrochloride

    Akt Cancer
    Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer.
  • HY-145240
    eIF4E-IN-1

    Eukaryotic Initiation Factor (eIF) Cancer Infection
    eIF4E-IN-1 is a potent inhibitor of eIF4E. eIF4E-IN-1 inhibits immunosuppression components such as immune checkpoint proteins PD-1, PD-L1, LAG3, TIM3, and/or IDO, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease (extracted from patent WO2021003194A1, compound Y).
  • HY-N10213
    Septeremophilane E

    Others Infection
    Septeremophilane E is a compound isolated from fungus Septoria rudbeckiae, a plant pathogenic fungus isolated from the halophyte Karelinia caspia. Septeremophilane E significantly inhibits the production of nitric oxide (NO).
  • HY-15391
    Lucitanib

    E-3810

    VEGFR FGFR Cancer
    Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
  • HY-15166B
    (E/Z)-Zotiraciclib citrate

    (E/Z)-TG02 citrate; (E/Z)-SB1317 citrate

    CDK JAK FLT3 Cancer
    (E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.
  • HY-114080A
    Patamostat mesylate

    E-3123 mesylate

    Ser/Thr Protease Inflammation/Immunology
    Patamostat (E-3123) mesylate is a potent protease inhibitor. Patamostat mesylate potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat mesylate may possess suppressing effects on pathogenesis and development of acute pancreatitis.
  • HY-114080
    Patamostat

    E-3123

    Ser/Thr Protease Inflammation/Immunology
    Patamostat (E-3123) is a potent protease inhibitor. Patamostat potently inhibits trypsin, plasmin and thrombin with IC50s of 39 nM, 950 nM and 1.9 μM, respectively. Patamostat may possess suppressing effects on pathogenesis and development of acute pancreatitis.
  • HY-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-128978
    (E,E)-RAMB4

    Phosphatase Metabolic Disease
    (E,E)-RAMB4 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1.
  • HY-107574
    TC-E 5003

    Histone Methyltransferase Inflammation/Immunology
    TC-E 5003 is a selective PRMT1 inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 has anti-inflammatory properties in TLR4 signaling.
  • HY-116100
    (E/Z)-HA155

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Neurological Disease
    (E/Z)-HA155 is a potent autotaxin (ATX) type I inhibitor. (E/Z)-HA155 can be used for researching cancer, fibrotic diseases, inflammation, pain and angiogenesis.
  • HY-104068
    Naphthol AS-E

    Histone Acetyltransferase Epigenetic Reader Domain Cancer
    Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.
  • HY-101015
    (2E)-OBAA

    Phospholipase Apoptosis Inflammation/Immunology
    (2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.
  • HY-15199
    Agerafenib hydrochloride

    CEP-32496 hydrochloride; RXDX-105 hydrochloride

    Raf Cancer
    Agerafenib hydrochloride is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-145915A
    (E/Z)-ZINC09659342

    Ras Cancer
    (E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction.
  • HY-143281
    Topoisomerase II inhibitor 5

    Topoisomerase Cancer
    Topoisomerase II inhibitor 5 (Compound E24) is a DNA topoisomerase II inhibitor with anticancer activities.
  • HY-112149A
    (E/Z)-ZL0420

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    (E/Z)-ZL0420 is a racemic compound of (Z)-ZL0420 and (E)-ZL0420 isomers. (E)-ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2.
  • HY-115519
    (E/Z)-GO289

    Casein Kinase Cancer
    (E/Z)-GO289 is a potent and selective casein kinase 2 (CK2) inhibitor (IC50=7 nM). (E/Z)-GO289 strongly lengthens circadian period. (E/Z)-GO289 exhibits cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function.
  • HY-B0034S1
    Donepezil-d4 hydrochloride

    E2020-d4

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d4 hydrochloride (E2020-d4) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-13433
    Thapsigargin

    Calcium Channel SARS-CoV Apoptosis Cancer Infection
    Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca 2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.
  • HY-114041
    Resolvin E1

    RvE1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
  • HY-N6772
    Cytochalasin E

    Autophagy Cancer
    Cytochalasin E, an epoxide containing Aspergillus-derived fungal metabolite, inhibits angiogenesis and tumor growth. Cytochalasin E is a potent actin depolymerization agent, and it binds and caps the barbed end of actin filaments to prevent actin elongation.
  • HY-15338A
    (E/Z)-TG003

    CDK Cancer
    (E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively.
  • HY-100372
    E4CPG

    (RS)-ECPG

    mGluR Neurological Disease
    E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Apoptosis Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-50876
    (E)-Daporinad

    FK866; APO866

    NAMPT Autophagy Cancer
    (E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
  • HY-N10232
    Agistatin E

    Others Infection
    Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.
  • HY-113794
    DSHS00884

    SSYA10-001

    Filovirus Infection
    DSHS00884 is a potent human papillomavirus E6 inhibitor with an IC50 of 10 μM.
  • HY-108516
    TC-E 5001

    PARP Cancer
    TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively.
  • HY-10016
    E 2012

    γ-secretase Neurological Disease
    E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
  • HY-121508
    (E/Z)-IT-603

    NF-κB Cancer Inflammation/Immunology
    (E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
  • HY-N0665
    Specnuezhenide

    (8E)-Nuezhenide

    NF-κB Wnt Inflammation/Immunology
    Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).
  • HY-B0131
    Prostaglandin E1

    Alprostadil; PGE1

    Prostaglandin Receptor Endogenous Metabolite Endocrinology Cardiovascular Disease
    Prostaglandin E1 (Alprostadil) is a prostanoid receptor ligand, with Kis of 1.1 nM, 2.1 nM, 10 nM, 33 nM and 36 nM for mouse EP3, EP4, EP2, IP and EP1, respectively. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation. Prostaglandin E1 can be used as a vasodilator for the research of peripheral vascular diseases.
  • HY-125568
    Pyridoxatin

    Others Others
    Pyridoxatin is a free radical scavenger of microbial origin. Pyridoxatin is isolated from a fungus culture identified as Acremonium sp. BX86. Pyridoxatin inhibits lipid peroxidation induced by free radicals in rat liver microsomes free from vitamin E.
  • HY-N0060B
    (E)-Ferulic acid

    (E)-Coniferic acid

    β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite Cancer
    (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
  • HY-19760B
    I-BET282E

    Epigenetic Reader Domain Inflammation/Immunology
    I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
  • HY-146442
    BRAF V600E/CRAF-IN-1

    Raf Cancer
    BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases.
  • HY-15162A
    MMAE-d8

    Monomethyl auristatin E-d8; Deuterated labeled MMAE

    Microtubule/Tubulin ADC Cytotoxin Cancer
    MMAE-d8 (Monomethyl auristatin E-d8) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.
  • HY-111643
    6-Amino-5-azacytidine

    Bacterial Infection
    6-Amino-5-azacytidine inhibits the growth of bacteria E. coli.
  • HY-139982
    OX11

    Bacterial Infection
    OX11 is a selective inhibitor of S. pneumoniae, P. aeruginosa, and E. coli bacterial strains.
  • HY-15599
    SSR128129E

    SSR

    FGFR Cancer
    SSR128129E is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-14176
    Compound E

    γ-Secretase-IN-1

    γ-secretase Cancer
    Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
  • HY-108241
    (Z)-PUGNAc

    Others Metabolic Disease
    (Z)-PUGNAc is a potent O-GlcNAcase inhibitor. (Z)-PUGNAc is a vastly more potent inhibitor of O-GlcNAcase than the E form.
  • HY-N7661
    4β-Hydroxywithanolide E

    PPAR Metabolic Disease
    4β-Hydroxywithanolide E, isolated from Physalis peruviana L., inhibits adipocyte differentiation of 3T3-L1 cells through modulation of mitotic clonal expansion. 4β-Hydroxywithanolide E is an adipogenesis inhibitor and inhibits PPARγ, C/EBPα, and the adipocyte-specific molecule aP2 mRNA expression.
  • HY-12740
    Lotamilast

    RVT-501; E6005

    Phosphodiesterase (PDE) Inflammation/Immunology
    Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.
  • HY-N2519
    (E)-Coniferin

    (E)-Laricin

    Fungal Infection
    (E)-Coniferin is the isomer of Coniferin. Coniferin is a glucoside of coniferyl alcohol. Coniferin inhibits fungal growth and melanization.
  • HY-15599A
    SSR128129E free acid

    SSR free acid

    FGFR Cancer
    SSR128129E free acid is an orally available and allosteric FGFR inhibitor with an IC50 of 1.9 μM for FGFR1.
  • HY-101627
    YM17E

    Acyltransferase Metabolic Disease
    YM17E is an inhibitor of acyl CoA:cholesterol acyltransferase (ACAT), with IC50 of 44 nM in rabbit liver microsomes in vitro.
  • HY-137422
    D-erythro-MAPP

    D-e-MAPP

    Others Cancer Neurological Disease
    D-erythro-MAPP (D-e-MAPP) is a ceramidase inhibitor, with an IC50 of 1-5 μM in vitro.
  • HY-14571
    E7820

    ER68203-00

    Integrin Cancer
    E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
  • HY-131553
    D-α-Tocopherol Succinate

    Vitamin E succinate

    Apoptosis Cancer
    D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer.
  • HY-100226
    A-205804

    Integrin Inflammation/Immunology
    A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
  • HY-128357
    Ibezapolstat

    ACX-362E; GLS-362E

    Bacterial DNA/RNA Synthesis Infection
    Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI).
  • HY-121638
    CU-3

    Apoptosis Cancer Inflammation/Immunology
    CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-150046
    Nek2-IN-6

    Others Cancer
    Nek2-IN-6 (Compound 28e) is a potent never in mitosis (NIMA) related kinase 2 (Nek2) inhibitor.
  • HY-126144A
    (E/Z)-GSK-3β inhibitor 1

    GSK-3 Metabolic Disease
    (E/Z)-GSK-3β inhibitor 1 is a racemic compound of (E)-GSK-3β inhibitor 1 and (Z)-GSK-3β inhibitor 1 isomers. GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC50 of 4.9 nM.
  • HY-P1427
    Guangxitoxin 1E

    Potassium Channel Neurological Disease
    Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.
  • HY-15460
    CHIR-090

    Bacterial Infection
    CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM.
  • HY-101445
    Trolox

    Reactive Oxygen Species Ferroptosis Apoptosis Cancer
    Trolox is an analogue of vitamin E with a powerful antioxidant effect. Trolox is also a powerful inhibitor of membrane damage.
  • HY-146443
    BRAF V600E/CRAF-IN-2

    Raf Cancer
    BRAF V600E/CRAF-IN-2 (Compound 9c) is a potent inhibitor of BRAF V600E/CRAF with IC50s of 0.888 and 0.229 μM, respectively. BRAF V600E/CRAF-IN-2 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-2 has the potential for the research of cancer diseases.
  • HY-143715
    Cereblon inhibitor 1

    Ligands for E3 Ligase Cancer
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research.
  • HY-122903B
    (+)-TK216

    DNA/RNA Synthesis Others
    (+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor.
  • HY-117203A
    CDK12-IN-E9

    CDK Cancer
    CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM.
  • HY-126257
    AKT-IN-3

    Akt Apoptosis Cancer
    AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells.
  • HY-146033
    HPV18-IN-1

    HPV Cancer
    HPV18-IN-1 (Compound H1) is a potent inhibitor of HPV18. HPV18-IN-1 prevents cervical cancer cells from premature cell procession and abnormal proliferation. HPV18-IN-1 supresses E7-Rb-E2F cellular pathway and DNA methylation. HPV18-IN-1 has the potential for the research of cancer diseases.
  • HY-19357
    E3330

    APX-3330

    DNA/RNA Synthesis NF-κB AP-1 HIF/HIF Prolyl-Hydroxylase VEGFR Reactive Oxygen Species Cancer Neurological Disease Cardiovascular Disease
    E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.
  • HY-125263
    OP-1074

    Estrogen Receptor/ERR Cancer
    OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
  • HY-130519
    Cdc7-IN-7

    CDK Cancer
    Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-N6928
    Mogroside III-E

    Others Cancer Metabolic Disease
    Mogroside III-E is a cucurbitane-type compound isolated from Siraitia grosvenorii, inhibits NO release, with anti-fibrotic activity.
  • HY-130306
    Zaragozic acid E

    Farnesyl Transferase Endogenous Metabolite Cancer
    Zaragozic acid E, a fungal metabolite, is a potent inhibitor of squalence synthetase with IC50s of 2.3-28 nM.
  • HY-101041
    (E)-AG 556

    (E)-Tyrphostin AG 556

    EGFR Inflammation/Immunology
    (E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production.
  • HY-144280
    MsbA-IN-2

    Bacterial Infection
    MsbA-IN-2 (compound 12) is a potent lipopolysaccharide transporter MsbA inhibitor with an IC50 of 2 nM for E. coli MsbA.
  • HY-15200
    Agerafenib

    CEP-32496; RXDX-105

    Raf Cancer
    Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAF V600E with a Kd of 14 nM.
  • HY-N0346A
    (E)-Ethyl p-methoxycinnamate

    COX Cancer Infection Inflammation/Immunology
    (E)-Ethyl p-methoxycinnamate is a natural product found in Kaempferia galangal with anti-inflammatory, anti-neoplastic and anti-microbial effects. (E)-Ethyl p-methoxycinnamate inhibits COX-1 and COX-2 in vitro with IC50s of 1.12 and 0.83 μM, respectively.
  • 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 the TNBC cell lines with IC50s of nearly 25 μM. AGX51 can be used for the research of cancer.
  • HY-124704
    Chst15-IN-1

    Others Neurological Disease
    Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair.
  • HY-15184
    Elaiophylin

    Azalomycin B; Gopalamicin; Efomycin E

    Autophagy Cancer
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
  • HY-16261B
    MC-DOXHZN hydrochloride

    (E/Z)-Aldoxorubicin hydrochloride; Doxorubicin(6-maleimidocaproyl)hydrazone hydrochloride

    Topoisomerase Drug-Linker Conjugates for ADC Cancer
    MC-DOXHZN ((E/Z)-Aldoxorubicin) hydrochloride is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
  • HY-U00003
    ICAM-1-IN-1

    Integrin Inflammation/Immunology
    ICAM-1-IN-1 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 values of 7 and 5 nM, respectively.
  • HY-18997
    PLX7904

    PB04

    Raf Cancer
    PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAF V600E in mutant RAS expressing cells.
  • HY-16261A
    MC-DOXHZN

    (E/Z)-Aldoxorubicin; Doxorubicin(6-maleimidocaproyl)hydrazone

    Topoisomerase Drug-Linker Conjugates for ADC Cancer
    MC-DOXHZN ((E/Z)-Aldoxorubicin) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), with acid-sensitive properties.
  • HY-148100
    Emapticap pegol

    NOX-E36

    Others Cancer Inflammation/Immunology
    Emapticap pegol is a inhibitor of pro-inflammatory chemokine C-C motif-ligand 2 (CCL2). Emapticap pegol is a 40-nucleotide oligonucleotide aptamer, displays different Spiegelmers (L-RNA aptamer) isform in human (NOX-E36) and mouse (mNOX-E36).
  • HY-109045A
    Teslexivir hydrochloride

    BTA074 hydrochloride; AP 611074 hydrochloride

    E1/E2/E3 Enzyme HPV Infection
    Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.
  • HY-19717
    DCVC

    S-[(1E)-1,2-dichloroethenyl]--L-cysteine

    TNF Receptor Inflammation/Immunology
    DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
  • HY-109045
    Teslexivir

    BTA074; AP 611074

    E1/E2/E3 Enzyme HPV Infection
    Teslexivir (BTA074) is a potent antiviral agent. Teslexivir is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir can be used for condyloma research.
  • HY-121638A
    (5Z,2E)-CU-3

    Apoptosis Cancer
    (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
  • HY-130840
    LolCDE-IN-2

    Bacterial Cancer
    LolCDE-IN-2 is a potent Lol protein (LolCDE) inhibitor. LolCDE-IN-2 inhibits E. coli MG1655 with a MIC of 2 μg/ml. Antibacterial activity.
  • HY-N6738
    Bafilomycin B1

    Bacterial Fungal Antibiotic Infection
    Bafilomycin B1 is a macrolide antibiotic isolated from Streptomyces sp, inhibits Gram-positive bacteria and fungi, and acts as an inhibitor of K +-dependent ATPase of E. coli.
  • HY-14177
    Raf inhibitor 1

    Raf Cancer
    Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
  • HY-124295
    MPT0E028

    HDAC Akt Apoptosis Cancer
    MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
  • HY-126396
    Sordarin sodium

    CaMK 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. albicansC. glabrata, and C. neoformans) while unable to do so in some other fungal species (e.g. Candida parapsilosis and Candida lusitaniae).
  • HY-136149A
    Mpro inhibitor N3 hemihydrate

    SARS-CoV Virus Protease Infection
    Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.
  • HY-14177A
    Raf inhibitor 1 dihydrochloride

    Raf Cancer
    B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
  • HY-N7310
    Gomisin E

    Others Others
    Gomisin E, a dibenzocyclooctadiene lignan isolated from the fruits of Schizandra chinensis, inhibits NFAT transcription with an IC50 of 4.73 μM.
  • HY-147317
    Epothilone E

    Microtubule/Tubulin Cancer
    Epothilone E is a related compound of epothilone, which inhibits microtubule protein function and blocks cell division, and has anti-tumor activity.
  • HY-N10433
    Xanthine oxidase-IN-9

    Icarisids E

    Xanthine Oxidase Metabolic Disease
    Xanthine oxidase-IN-9 (Icarisids E) (Compound 2) is a potent xanthine oxidase (XOD) inhibitor with an IC50 of 31.81 μM.
  • HY-147381
    MetRS-IN-1

    Others Others
    MetRS-IN-1 (Compound 27) is an E. coli methionyl-tRNA synthetase (MetRS) inhibitor (IC50=237 nM).
  • HY-150774
    HDAC6/HSP90-IN-2

    HDAC HSP Apoptosis Cancer
    HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 (compound 6e) can be used for the research of cancer.
  • HY-10930
    UNC0321

    Histone Methyltransferase Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-132135
    (1E)-CFI-400437 dihydrochloride

    Polo-like Kinase (PLK) Cancer
    (1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.
  • HY-10929
    UNC0224

    Histone Methyltransferase Cancer
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-12846
    CCT196969

    Raf Cancer
    CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
  • HY-112798
    PH-002

    Others Neurological Disease
    PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
  • HY-13442
    Eribulin

    B1939; E7389; ER-086526

    Microtubule/Tubulin Apoptosis ADC Cytotoxin Cancer
    Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
  • HY-132821A
    Irsenontrine maleate

    E2027 maleate

    Phosphodiesterase (PDE) Neurological Disease
    Irsenontrine (E2027) maleate is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine maleate can be used for the research of neurological diseases.
  • HY-15811
    XMD8-87

    ACK1-B19

    Tyrosinase Cancer
    XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
  • HY-B1122
    L-Cycloserine

    (S)-Cycloserine; (S)-4-Amino-3-isoxazolidone

    GABA Receptor HIV Neurological Disease Cancer
    L-Cycloserine ((S)-4-Amino-3-isoxazolidone) irreversibly inhibits GABA pyridoxal 5′-phosphate-dependent aminitransferase in E.
  • 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-15741
    Mc-MMAE

    Maleimidocaproyl-monomethylauristatin E

    Microtubule/Tubulin Drug-Linker Conjugates for ADC Cancer
    Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.
  • HY-14660A
    Dabrafenib Mesylate

    GSK2118436 Mesylate; GSK 2118436B

    Raf Cancer
    Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for Raf V600E and c-Raf, respectively.
  • HY-101243
    XMD16-5

    Tyrosinase Cancer
    XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
  • HY-130642
    (S,R,S)-AHPC-Me-C10-Br

    E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-Me-C10-Br is a synthesized E3 ligase ligand-linker conjugate. (S,R,S)-AHPC-Me-C10-Br incorporates a VHL E3 ligase linker and MS432 based on the MEK1/2 inhibitor PD0325901.
  • HY-124760
    hSMG-1 inhibitor 11e

    mTOR PI3K CDK Cancer
    hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
  • HY-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.
  • HY-143251
    Tubulin inhibitor 13

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 13 (E27) is a potent tubulin inhibitor with an IC50 value of 16.1 μM for the tubulin polymerization inhibition. Tubulin inhibitor 13 inhibits migration and invasion of cancer cells, induces apoptosis and has anticancer activity.
  • HY-14596
    Genistein

    NPI 031L

    EGFR Autophagy Apoptosis Endogenous Metabolite Cancer
    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
  • HY-U00112
    Estradiol 3-sulfamate

    BLE 00084; E2MATE; ES-J 995

    Others Cancer
    Estradiol 3-sulfamate (BLE 00084; E2MATE; ES-J 995) is a potent, long-acting, and orally active steroid sulfatase inhibitor; inhibits estrone sulfatase with an IC50 of 251 nM and a Ki of 133 nM.
  • HY-18652
    Ro 5126766

    CH5126766

    MEK Raf Cancer
    Ro 5126766 (CH5126766) is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAF V600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
  • HY-132821
    Irsenontrine

    E2027

    Phosphodiesterase (PDE) Neurological Disease
    Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine can be used for the research of neurological diseases.
  • HY-18957
    Lifirafenib

    BGB-283

    EGFR Raf Cancer
    Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively.
  • HY-78933
    Fmoc-MMAE

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC.
  • HY-147825
    EGFR/BRAFV600E-IN-1

    EGFR Raf Apoptosis Cancer
    EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.
  • HY-117857
    MRT00033659

    Casein Kinase Checkpoint Kinase (Chk) MDM-2/p53 Early 2 Factor (E2F) Cancer
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
  • HY-15496
    E6201

    ER-806201

    MEK FLT3 Cancer
    E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy.
  • HY-107411S
    Bromoenol lactone-d7

    (6E)-Bromoenol lactone-d7

    Phospholipase Inflammation/Immunology
    Bromoenol lactone-d7 ((6E)-Bromoenol lactone-d7) is the deuterium labeled Bromoenol lactone. Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx.
  • HY-12558
    LY3009120

    DP-4978

    Raf Autophagy Cancer
    LY3009120 (DP-4978) is a pan RAF inhibitor which inhibits BRAF V600E, BRAF WT and CRAF WT with IC50s of 5.8, 9.1 and 15 nM, respectively.
  • HY-100640
    Roflumilast Impurity E

    Phosphodiesterase (PDE) Inflammation/Immunology
    Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
  • HY-109055
    Elenbecestat

    E2609

    Beta-secretase Neurological Disease
    Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
  • HY-17531
    Pyraclonil

    Others Others
    Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations.
  • HY-I0727
    Sofosbuvir impurity E

    Others Others
    Sofosbuvir impurity E is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
  • HY-18785
    Indirubin Derivative E804

    IGF-1R Cancer Endocrinology
    Indirubin Derivative E804 is a potent inhibitor of Insulin-like Growth Factor 1 Receptor (IGF1R), with an IC50 of 0.65 μM for IGF1R.
  • HY-N4283A
    (E)-Coniferyl alcohol

    Fungal Infection
    (E)-Coniferyl alcohol is the isomer of Coniferyl alcohol. Coniferyl alcohol is an intermediate in biosynthesis of eugenol and of stilbenoids and coumarin. Coniferyl alcohol specifically inhibits fungal growth.
  • HY-15605
    Encorafenib

    LGX818

    Raf Cancer
    Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
  • HY-15767
    TAK-632

    Raf Aurora Kinase Cancer
    TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively.
  • HY-10981A
    Lenvatinib mesylate

    E7080 mesylate

    VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10981
    Lenvatinib

    E7080

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-N2346
    Tubulysin E

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin E is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin E is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • 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-14566
    Donepezil

    E2020 free base

    Cholinesterase (ChE) Neurological Disease Cancer
    Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
  • HY-14660
    Dabrafenib

    GSK2118436A; GSK2118436

    Raf Cancer
    Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
  • HY-N4182
    Licochalcone E

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza inflate, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation.
  • HY-141841
    SARS-CoV-2-IN-7

    SARS-CoV Infection
    SARS-CoV-2-IN-7 inhibits viral replication with a nanomolar IC50 value (844 nM) in SARS-CoV-2-infected Vero E6 cells.
  • HY-124330
    Tripolin A

    (E)-Tripolin A

    Aurora Kinase Others
    Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
  • HY-139746
    FPI-1602

    Bacterial Infection
    FPI-1602 is a β-lactamase inhibitor. FPI-1602 displays marked antimicrobial activity against P. aeruginosa, E. coli, and Enterobacter spp..
  • HY-109081A
    Cedazuridine hydrochloride

    E7727 hydrochloride

    Others Cancer
    Cedazuridine (E7727) (Compound 7a) hydrochloride is an orally active cytidine deaminase (CDA) inhibitor with an IC50 value of 0.4 μM. Cedazuridine hydrochloride can be used for cancer research.
  • HY-N0170
    Indole-3-carbinol

    I3C; 3-Indolemethanol

    NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite Cancer
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
  • HY-114903
    (E/Z)-BIO-acetoxime

    GSK-​3 Inhibitor X

    GSK-3 CDK Cancer Metabolic Disease Neurological Disease
    (E/Z)-BIO-acetoxime (GSK-3 Inhibitor X) is a potent and selective GSK-3α/β inhibitor, with an IC50 of 10 nM. (E/Z)-BIO-acetoxime shows more than 200-flod selectivity over CDK5/p25, CDK2/cyclin A and CDK1/cyclin B (IC50=2.4, 4.3, 63 μM).
  • HY-19719A
    Miransertib hydrochloride

    ARQ-092 hydrochloride

    Akt Parasite Cancer Infection
    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research. Miransertib hydrochloride is effective against Leishmania.
  • HY-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-100349
    SU4312

    PDGFR VEGFR Cancer
    SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
  • HY-115502A
    BCI hydrochloride

    (E)-BCI hydrochloride

    Phosphatase Cancer Inflammation/Immunology
    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.
  • HY-124379
    TPCK

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease HPV Cancer Inflammation/Immunology
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.
  • HY-144271
    RAF-IN-1

    Raf Cancer
    RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively.
  • HY-150641
    CDK-IN-9

    CDK Apoptosis Cancer
    CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II.
  • HY-51424
    PLX-4720

    Raf Cancer
    PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
  • HY-103081
    β-Glucuronidase-IN-1

    Bacterial Cancer Infection
    β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively.
  • HY-147133
    VEGFR2-IN-2

    VEGFR Cancer
    VEGFR2-IN-2 (compound 6e) is a potent and selective VEGFR2 inhibitor with an IC50 of 19.32 nM. VEGFR2-IN-2 can be used for researching
  • HY-18169
    MUT056399

    Fab-001

    Bacterial Infection
    MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli with 50% inhibitory concentration IC50s of 12 nM and 58 nM, respectively.
  • HY-131252
    Dihydro Donepezil

    Dihydro E2020

    Cholinesterase (ChE) Neurological Disease
    Dihydro Donepezil (Dihydro E2020) is a metabolite of Donepezil. Donepezil is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bAChE and hAChE, respectively.
  • HY-11009
    CGP60474

    CDK PKC Cancer
    CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
  • HY-113054
    DL-Glyceraldehyde 3-phosphate

    Acyltransferase Bacterial Endogenous Metabolite Infection Metabolic Disease
    DL-Glyceraldehyde 3-phosphate is an intermediate in several metabolic pathways, including glycolysis and gluconeogenesis. DL-Glyceraldehyde 3-phosphate is a potent inhibitor of the growth of E. coli. DL-Glyceraldehyde 3-phosphate is a competitive inhibitor of the acyltransferase.
  • HY-150065
    Antimalarial agent 15

    Parasite Infection Inflammation/Immunology
    Antimalarial agent 15 (Compound 4e) is a parasite inhibitor. Antimalarial agent 15 shows antimalarial activity, and can inhibit P. falciparum 3D7 parasite growth (IC50=20 nM).
  • HY-111370
    mTOR inhibitor-2

    mTOR Cancer
    mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
  • HY-16023A
    Acolbifene

    EM-652; SCH 57068

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.
  • HY-146724
    Dot1L-IN-7

    Histone Methyltransferase Cancer
    Dot1L-IN-7 (compound 25) is a potent and selective disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 1.0 μM. Dot1L-IN-7 selectively killed Mixed Lineage Leukemia (MLL)-AF9 without showing any effect on the growth of E2A-HLF cells.
  • HY-128979
    Deruxtecan analog 2

    Drug-Linker Conjugates for ADC Cancer
    Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a drug-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC.
  • HY-135715
    (E)-UK122 TFA

    Others Others
    (E)-UK122 TFA is the isomer of UK122 TFA. UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM.
  • HY-136567
    TBAP-001

    Raf Cancer
    TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay.
  • HY-114304
    COH000

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • HY-143280
    Topoisomerase II inhibitor 4

    Topoisomerase Cancer
    Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect.
  • HY-15162
    Monomethyl auristatin E

    MMAE; SGD-1010; Vedotin

    Microtubule/Tubulin ADC Cytotoxin Apoptosis Cancer
    Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
  • HY-135844
    LS-102

    E1/E2/E3 Enzyme Inflammation/Immunology
    LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
  • HY-P9934
    Abciximab

    C7E3

    Integrin Cardiovascular Disease
    Abciximab (C7E3), a chimeric mouse/human monoclonal antibody, is a glycoprotein (GP) IIb/IIIa inhibitor. Abciximab inhibits platelet aggregation and leucocyte adhesion by binding to the glycoprotein IIb/IIIa, vitronectin and Mac-1 receptors.
  • HY-128067
    5-(N,N-Hexamethylene)-amiloride

    Hexamethylene amiloride; HMA

    Sodium Channel HIV Apoptosis Cancer Infection
    5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
  • HY-139743
    Aditoprime

    Aditoprim

    Antifolate Bacterial Infection
    Aditoprime (Aditoprim), a selective bacterial dihydrofolate reductase (DHFR) inhibitor, inhibits the transformation of dihydrofolic acid to tetrahydrofolic acid. Aditoprime inhibits E.coli and L.casei DHFR with IC50 of 47 and 520 nM, respectively. Aditoprime has a broad antimicrobial spectrum, good antibacterial activity and excellent pharmacokinetics.
  • HY-150977
    β-Glucuronidase/hCAII-IN-2

    Carbonic Anhydrase Cancer Metabolic Disease Neurological Disease
    β-Glucuronidase/hCAII-IN-2 (Compound 12e) is a potent β-glucuronidase and hCA II inhibitor with an IC50 of 670.7 μM and 21.77 μM, respectively.
  • HY-150976
    β-Glucuronidase/hCAII-IN-1

    Carbonic Anhydrase Cancer Metabolic Disease Neurological Disease
    β-Glucuronidase/hCAII-IN-2 (Compound 12e) is a potent β-glucuronidase and hCA II inhibitor with an IC50 of 440.1 μM and 4.91 μM, respectively.
  • HY-147661
    DHFR-IN-2

    Antifolate Infection
    DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research.
  • HY-122903A
    (-)-TK216

    DNA/RNA Synthesis Cancer
    (-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity.
  • HY-N2391
    p-Hydroxycinnamic acid

    Endogenous Metabolite Prostaglandin Receptor Endocrinology
    p-Hydroxycinnamic acid, a common dietary phenol, could inhibit platelet activity, with IC50s of 371 μM, 126 μM for thromboxane B2 production and lipopolysaccharide-induced prostaglandin E2 generation, respectively.
  • HY-12473
    Vps34-IN-2

    PI3K SARS-CoV Cancer
    Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43.
  • HY-120599
    Sabizabulin

    VERU-111; ABI-231

    Microtubule/Tubulin Apoptosis HPV Cancer
    VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer.
  • HY-150766
    KPC-2-IN-1

    Bacterial Infection
    KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics.
  • HY-19340
    TMS

    (E)-2,3',4,5'-tetramethoxystilbene

    Cytochrome P450 Cancer
    TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC5050
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-100818
    Futibatinib

    TAS-120

    FGFR Cancer
    Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM).
  • HY-142444
    SSAO/VAP-1 inhibitor 1

    Others Metabolic Disease
    SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).
  • HY-15504A
    RGB-286638 free base

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-15504
    RGB-286638

    CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-130223
    11β-Prostaglandin E2

    11β-Dinoprostone; 11β-PGE2

    Prostaglandin Receptor Endocrinology
    11β-Prostaglandin E2 (11β-Dinoprostone), a Prostanoid derivative, inhibits [ 3H]PGE2 binding to hypothalamic membranes in the rat with a Ki of 53.3 nM.
  • HY-109080
    Belvarafenib

    HM95573; GDC-5573; RG6185

    Raf Cancer
    Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF v600E and C-RAF respectively.
  • HY-W016867
    4-Chlorosalicylic acid

    Fungal Bacterial Infection
    4-Chlorosalicylic acid is a pharmaceutical intermediate. Inhibits monophenolase and diphenolase activity with IC50s of 1.89 mM and 1.10 mM. Potent antimicrobial activity. Against E. coli with the MIC of 250 μg/mL and with the MBC of 500 μg/mL.
  • HY-108697A
    (Rac)-PT2399

    HIF/HIF Prolyl-Hydroxylase Cancer
    (Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM.
  • HY-100566
    SuO-Val-Cit-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    SuO-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the peptide SuO-Val-Cit-PAB.
  • HY-12529
    Ro-3306

    CDK Apoptosis Cancer
    Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
  • HY-114267
    Cbz-B3A

    mTOR Others
    Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
  • HY-109080A
    Belvarafenib TFA

    HM95573 TFA; GDC-5573 TFA; RG6185 TFA

    Raf Cancer
    Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively.
  • HY-147819
    DNA Gyrase-IN-3

    Bacterial DNA/RNA Synthesis Infection
    DNA Gyrase-IN-3 (Compound 28) is a bacterial DNA gyrase B inhibitor with IC50s of 5.41-15.64 µM for E. coli DNA gyrase. Anti-tubercular and antibacterial activity.
  • HY-W062696
    BC-1382

    E1/E2/E3 Enzyme Inflammation/Immunology
    BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
  • HY-139589
    Zaloglanstat

    ISC-27864; GRC-27864

    PGE synthase Inflammation/Immunology Neurological Disease
    Zaloglanstat (ISC-27864) is the inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1), and can be used to study asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases, etc.
  • HY-15694
    SMIP004

    E1/E2/E3 Enzyme Apoptosis Cancer
    SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
  • HY-103436
    NSC624206

    E1/E2/E3 Enzyme Cancer
    NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation.
  • HY-B0182
    Carmofur

    HCFU

    Nucleoside Antimetabolite/Analog SARS-CoV Virus Protease Cancer
    Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC50 of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC50 of  24.3  μM.
  • HY-118773
    MreB Perturbing Compound A22 hydrochloride

    A22 hydrochloride

    Bacterial Inflammation/Immunology
    MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
  • HY-19622
    PF-9184

    PGE synthase Inflammation/Immunology
    PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
  • HY-131262
    Hydroxychloroquine Impurity E

    4-[(7-Chloro-4-quinolinyl)amino]-1-pentanol

    Others Others
    Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
  • HY-19831A
    (Z)-4EGI-1

    Eukaryotic Initiation Factor (eIF) Cancer
    (Z)-4EGI-1 is the Z-isomer of 4EGI-1 and is an inhibitor of eIF4E/eIF4G interaction and of translation initiation. (Z)-4EGI-1 effectively binds to eIF4E with an IC50 of 43.5 μM and a Kd value of 8.74 μM. (Z)-4EGI-1 has anticancer activity.
  • HY-16023
    Acolbifene hydrochloride

    EM-652 hydrochloride; SCH 57068 hydrochloride

    Estrogen Receptor/ERR Cancer
    Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
  • HY-150044
    Type II topoisomerase inhibitor 1

    DNA/RNA Synthesis Topoisomerase Bacterial Infection
    Type II topoisomerase inhibitor 1 is a potent and selective E. coli DNA gyrase inhibitor (IC50: 1.7 nM), and forms hydrogen bonds with Asp73 residue. Type II topoisomerase inhibitor 1 inhibits topoisomerase IV activity (IC50: 0.98 μM). Type II topoisomerase inhibitor 1 can be used in the research of antibacterial area.
  • HY-105309
    GSK-626616

    DYRK Cardiovascular Disease
    GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
  • HY-138067
    SSAA09E2

    SARS-CoV Inflammation/Immunology
    SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
  • HY-146983
    hCAIX-IN-3

    Carbonic Anhydrase Cancer
    hCAII-IN-3 (compound 7e) is a potent and selective inhibitor of carbonic anhydrase (CA II/IX) with Kis of 124.2 and 30.5 nM, respectively. hCAII-IN-3 has the potential for the research of cancer diseases.
  • HY-126681
    SC-VC-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    SC-VC-PAB-MMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB.
  • HY-147416
    Vipoglanstat

    BI 1029539; GS-248; OX-MPI

    PGE synthase Infection
    Vipoglanstat (BI 1029539), a carboxamide, is a potent and selective, non-peptide and orally active small molecular inhibitor of human prostaglandin E synthase 1 (mPGES-1). Vipoglanstat also has anti-inflammatory activity.
  • HY-15575
    VcMMAE

    MC-Val-Cit-PAB-MMAE; mc-vc-PAB-MMAE

    Drug-Linker Conjugates for ADC Microtubule/Tubulin Cancer
    VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
  • HY-14566S1
    Donepezil-d5

    E2020-d5

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d5 is deuterium labeled Donepezil. Donepezil (E2020 free base) is a specific and potent AChE inhibitor with IC50s of 8.12 nM and 11.6 nM for bovine AChE and human AChE, respectively.
  • HY-150557
    CYP1B1-IN-1

    Cytochrome P450 Cancer
    CYP1B1-IN-1 (Compound 9e) is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 0.49 nM.
  • HY-12418
    E7449

    PARP Cancer
    E7449 is a potent PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively, using 32P-NAD + as substrate.
  • HY-125415
    PF-4693627

    PGE synthase Inflammation/Immunology
    PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
  • HY-B1123
    Auranofin

    SKF-39162

    Bacterial SARS-CoV Cancer Infection Inflammation/Immunology
    Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.
  • HY-141432
    Cbl-b-IN-3

    E1/E2/E3 Enzyme Cancer
    Cbl-b-IN-3 (Compound 23) is a casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 of < 1 nM. Cbl-b is an E3 ubiquitin ligase that negatively regulates T-cell activation.
  • HY-B0034
    Donepezil Hydrochloride

    E2020

    Cholinesterase (ChE) Neurological Disease
    Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-131232
    Desmorpholinyl Navitoclax-NH-Me

    Desmorpholinyl ABT-263-NH-Me

    Bcl-2 Family Ligands for Target Protein for PROTAC Cancer
    Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557).
  • HY-N10226
    Thielavin B

    Prostaglandin Receptor Endocrinology Cardiovascular Disease
    Thielavin B is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin B effectively influences the prostaglandin E2 synthesis from the endoperoxide. Thielavin B is significantly effective on carrageenan-induced oedema of rats when administered intravenously.
  • HY-111012
    DBCO-(PEG)3-VC-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    DBCO-(PEG)3-VC-PAB-MMAE is made by MMAE conjugated to DBCO-(PEG)3-vc-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
  • HY-146617
    GLS1 Inhibitor-4

    Glutaminase Apoptosis Cancer
    GLS1 Inhibitor-4 (compound 41e) is a potent GLS1 inhibitor with an IC50 of 11.86 nM. GLS1 Inhibitor-4 shows antiproliferative activity, good metabolic stability, robust GLS1 binding affinity. GLS1 Inhibitor-4 blocks the glutamine metabolism and induce the production of ROS. GLS1 Inhibitor-4 induces apoptosis and shows antitumor activity.
  • HY-51424S
    PLX-4720-d7

    Raf Cancer
    PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-Raf V600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
  • HY-N2463
    Kushenol E

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity.
  • HY-146359
    Influenza A virus-IN-5

    Influenza Virus DNA/RNA Synthesis Infection
    Influenza A virus-IN-5 (Compound 16e) is a potent, orally active anti-influenza A virus (IAV) agent with an IC50 of 1.29 μM. Influenza A virus-IN-5 inhibits the transcription and replication of viral RNA with acceptable cytotoxicity.
  • HY-108372
    Boc-C5-O-C5-O-C6-Cl

    PROTAC Linker 2

    PROTAC Linkers Cancer
    Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  • HY-137772
    Captopril EP Impurity E

    Others Others
    Captopril EP Impurity E is an impurity of Captopril. Captopril (SQ-14534), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC50=0.025 μM).
  • HY-N1407
    Polygalaxanthone III

    Cytochrome P450 Inflammation/Immunology
    Polygalaxanthone III is extracted from polygala tenuifolia wild, has inhibitory effect towards CYP450 enzyme. Polygalaxanthone III inhibits chlorzoxazone 6-hydroxylation catalyzed by CYP2E1 with an IC50 of 50.56 μM.
  • HY-N8085
    Icariside F2

    NF-κB Inflammation/Immunology
    Icariside F2 is a potent NF-κB inhibitor with an IC50 value of 16.25 μM. Icariside F2 is an aromatic glycoside isolated from the leaves of E. ulmoides Oliver. Icariside F2 has anti-inflammatory activity.
  • HY-B0876
    Fomepizole

    4-Methylpyrazole

    Cytochrome P450 Metabolic Disease
    Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.
  • HY-147980
    Aβ-IN-5

    Amyloid-β Cholinesterase (ChE) Neurological Disease
    Aβ-IN-5 (Compound e12) is an orally active Aβ aggregation inhibitor. Aβ-IN-5 also inhibits AChE and BuChE with IC50 values of 21.29 μM and 1.32 μM, respectively. Aβ-IN-5 shows excellent neuroprotective effects and low neurotoxicity.
  • HY-146541
    FGFR4-IN-10

    FGFR Cancer
    FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3.
  • HY-144279
    MsbA-IN-1

    Bacterial Infection
    MsbA-IN-1 is a highly potent MsbA inhibitor with IC50 of 4 nM. MsbA-IN-1 has activity against wild-type E. coli with MIC of 79 μM. MsbA-IN-1 possesses sufficient permeability across the fully intact outer membrane of Gram-negative bacteria to inhibit MsbA.
  • HY-110204
    Heclin

    E1/E2/E3 Enzyme Others
    Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits several HECT ligases in tissue culture cells (IC50s=6.8, 6.3, and 6.9 μM for Smurf2, Nedd4, and WWP1 HECT ligase domains, respectively).
  • HY-107411
    Bromoenol lactone

    (6E)-Bromoenol lactone

    Phospholipase Inflammation/Immunology
    Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx.
  • HY-44432
    Navitoclax-piperazine

    ABT-263-piperazine

    Bcl-2 Family Ligands for Target Protein for PROTAC Cancer
    Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604).
  • HY-145881
    Elongation factor P-IN-2

    Bacterial Infection
    Elongation factor P-IN-2 is a potent inhibitor elongation factor P (EFP). Elongation factor P-IN-2 is a β-lysine derivative compound. Elongation factor P-IN-2 affects the proliferation rates of E. coli.
  • HY-118827
    Vedaprofen

    Quadrisol; CERM 10202; PM 150

    COX Inflammation/Immunology
    Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory drug (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM.
  • HY-128842
    PROTAC MDM2 Degrader-3

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-128843
    PROTAC MDM2 Degrader-4

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-147960
    Glycosyltransferase-IN-1

    Bacterial Infection
    Glycosyltransferase-IN-1 (compound 5m) is a potent glycosyltransferase inhibitor, with an IC50 of 82.8 μM. Glycosyltransferase-IN-1 shows antibacterial activity, with MIC values of 6 μg/mL for MSSA, MRSA, B. subtilis and 12 μg/mL for E. coli.
  • HY-126686
    Mal-Phe-C4-VC-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    Mal-Phe-C4-VC-PAB-MMAE is made by MMAE conjugated to Mal-Phe-C4-VC-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
  • HY-128840
    PROTAC MDM2 Degrader-1

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-101445A
    (R)-Trolox

    Tyrosinase Cancer
    (R)-Trolox is a vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM. The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM).
  • HY-147237
    LpxC-IN-10

    Bacterial Infection
    LpxC-IN-10 (Compound A) is a high selectivity inhibitor of LpxC. LpxC-IN-10 exhibits MIC values of 0.5 μg/mL against E. coli and K. pneumoniae. LpxC-IN-10 (Compound A) can be used for the research of bacterial infection.
  • HY-128841
    PROTAC MDM2 Degrader-2

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-145880
    Elongation factor P-IN-1

    Bacterial Infection
    Elongation factor P-IN-1 is a potent inhibitor elongation factor P (EFP). Elongation factor P-IN-1 is a β-lysine derivative compound. Elongation factor P-IN-1 affects the proliferation rates of E. coli.
  • HY-101257B
    YKL-5-124 TFA

    CDK Cancer
    YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-101257
    YKL-5-124

    CDK Cancer
    YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.
  • HY-N6954
    Garcinone C

    ATM/ATR STAT CDK Cancer
    Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
  • 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-147841
    HIV-1 inhibitor-41

    HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity.
  • HY-130794
    ALK/ROS1-IN-1

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-12057
    Vemurafenib

    PLX4032; RG7204; RO5185426

    Raf Autophagy Cancer
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-151160
    LasR-IN-1

    Bacterial Infection
    LasR-IN-1 (compound 9g) is a potent LasR inhibitor. LasR-IN-1 has good efficacy toward E. coli. LasR-IN-1 shows anti-bacterial activity, with a MIC of 28.13 μM against P. aeruginosa.
  • HY-142779
    Lp-PLA2-IN-11

    Phospholipase Metabolic Disease Neurological Disease
    Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).
  • HY-B0876A
    Fomepizole hydrochloride

    4-Methylpyrazole hydrochloride

    Cytochrome P450 Metabolic Disease
    Fomepizole (4-Methylpyrazole) hydrochloride is a potent and orally active cytochrome P450 (CYP2E1) inhibitor. Fomepizole hydrochloride is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole hydrochloride blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole hydrochloride has the potential for an antidote for ethylene glycol or methanol poisoning.
  • HY-B0497
    Niclosamide

    BAY2353

    STAT Parasite Antibiotic Infection Cancer
    Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells.
  • HY-B0497A
    Niclosamide sodium

    BAY2353 sodium

    Antibiotic STAT Parasite Cancer Infection
    Niclosamide (BAY2353) sodium is an orally active antihelminthic agent used in parasitic infection research. Niclosamide sodium is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide sodium has biological activities against cancer, and inhibits DNA replication in Vero E6 cells.
  • HY-N4110
    Friedelin

    Cytochrome P450 Metabolic Disease
    Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79  μM and 6.16  μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54  μM and 18.02 μM, respectively.
  • HY-14596S
    Genistein-d4

    NPI 031L-d4

    EGFR Autophagy Apoptosis Endogenous Metabolite Cancer
    Genistein-d4 (NPI 031L-d4) is the deuterium labeled Genistein. Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
  • HY-B0497B
    Niclosamide monohydrate

    BAY2353 monohydrate

    STAT Antibiotic Parasite Cancer Infection
    Niclosamide (BAY2353) monohydrate is an orally active antihelminthic agent used in parasitic infection research. Niclosamide monohydrate is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide monohydrate has biological activities against cancer, and inhibits DNA replication in Vero E6 cells.
  • HY-N7148
    γ-Tocopherol

    D-γ-Tocopherol; (+)-γ-Tocopherol

    COX Cancer Inflammation/Immunology
    γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
  • HY-129105
    Clomethiazole

    GABA Receptor Cytochrome P450 Neurological Disease
    Chlormethiazole is an potent and orally active GABAA agonist. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus.
  • HY-101466A
    E7090 succinate

    FGFR Cancer
    E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively.
  • HY-151104
    Neuraminidase-IN-11

    Influenza Virus Infection
    Neuraminidase-IN-11 (15e) is a potent and selective neuraminidase (NA) inhibitor with the IC50 values of 4.7 nM, 8.46 nM and 1.5 nM against H1N1, H5N1 and H5N8 NAs respectively.
  • HY-106139A
    Bimosiamose disodium

    TBC-1269Z

    Others Inflammation/Immunology
    Bimosiamose disodium (TBC-1269Z) is a nonoligosaccharide pan-selectin inhibitor with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose disodium has anti-inflammatory effects.
  • HY-128773
    MRL-494

    Bacterial Infection
    MRL-494, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.
  • HY-12828A
    KH-CB20

    CDK DYRK Infection Neurological Disease
    KH-CB20, an E/Z mixture, is a potent and selective inhibitor of CLK1 and the closely related isoform CLK4, with an IC50 of 16.5 nM for CLK1. KH-CB20 can also inhibit DYRK1A (IC50=57.8 nM) and CLK3 (IC50=488 nM).
  • HY-128773A
    MRL-494 hydrochloride

    Bacterial Infection
    MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.
  • HY-B0497C
    Niclosamide olamine

    BAY2353 olamine

    STAT Parasite Antibiotic Cancer Infection
    Niclosamide (BAY2353) olamine is an orally active antihelminthic agent used in parasitic infection research. Niclosamide olamin is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide olamin has biological activities against cancer, and inhibits DNA replication in Vero E6 cells.
  • HY-101466
    E7090

    FGFR Cancer
    E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively.
  • HY-N3513
    Mulberrin

    Kuwanon C

    Others Cardiovascular Disease
    Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
  • HY-130626
    RSV/IAV-IN-1

    RSV Influenza Virus Infection
    RSV/IAV-IN-1 (compound 14e) is a potent and dual inhibitor of RSV/IAV. RSV/IAV-IN-1 has lesser cytotoxicity than the clinical drug, Ribavirin. RSV/IAV-IN-1 has the potential for the research of RSV and/or IAV infections.
  • HY-146061
    KRAS G12C inhibitor 48

    Ras Cancer
    KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively.
  • HY-133680
    β-Tocopherol

    Tyrosinase Metabolic Disease
    β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
  • HY-14660S
    Dabrafenib-d9

    GSK2118436A-d9; GSK2118436-d9

    Raf Cancer
    Dabrafenib-d9 (GSK2118436A-d9) is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
  • HY-147818
    DNA Gyrase-IN-2

    Bacterial DNA/RNA Synthesis Infection
    DNA Gyrase-IN-2 (Compound 22a) is a bacterial DNA gyrase B inhibitor with IC50s of 3.29-10.49 and 4.41-5.61 µM for E. coli DNA gyrase and M. tuberculosis DNA gyrase. Anti-tubercular and antibacterial activity.
  • HY-18299A
    Purvalanol A

    NG-60

    CDK Autophagy Apoptosis Cancer
    Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
  • HY-100859
    LSD1-IN-5

    Histone Demethylase Cancer
    LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1.
  • HY-B0034S
    Donepezil-d5 hydrochloride

    E2020-d5

    Cholinesterase (ChE) Neurological Disease
    Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity.
  • HY-146133
    LA-Bac8c

    Bacterial Antibiotic Infection
    LA-Bac8c is a Lipoic acid modified antimicrobial peptide with enhanced antimicrobial properties. LA-Bac8c inhibits S. aureus, MRSA, S. epidermidis, E. coli, and P. aeruginosa with MICs of 1, 4, 8, 8, and 8 μg/mL.
  • HY-125810
    4'-Ethynyl-2'-deoxyadenosine

    HIV Reverse Transcriptase Infection Inflammation/Immunology
    4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.
  • HY-W190943
    Azido-PEG4-Val-Cit-PAB-MMAE

    Drug-Linker Conjugates for ADC Cancer
    Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH.
  • HY-139909
    CL2E-SN38

    Drug-Linker Conjugates for ADC Cancer
    CL2E-SN-38, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
  • HY-125176
    G907

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-126690
    DBCO-(PEG2-VC-PAB-MMAE)2

    Drug-Linker Conjugates for ADC Cancer
    DBCO-(PEG2-VC-PAB-MMAE)2 is made by MMAE conjugated to the cleavable DBCO-(PEG2-VC-PAB)2 linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
  • 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-124322
    NB-360

    Beta-secretase Inflammation/Immunology Neurological Disease
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E.
  • HY-W412264
    Pim-1/2 kinase inhibitor 1

    Pim Cancer
    Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer.
  • HY-139909A
    CL2E-SN38 TFA

    Drug-Linker Conjugates for ADC Cancer
    CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
  • HY-126298
    RAF mutant-IN-1

    Raf Cancer
    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively.
  • HY-109785A
    (R)-Gyramide A hydrochloride

    Bacterial Infection
    (R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
  • HY-151168
    3-Chlorogentisyl alcohol

    Bacterial Cancer Inflammation/Immunology
    3-Chlorogentisyl alcohol is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.74 µM, an Ki value of 0.58 µM. 3-Chlorogentisyl alcohol shows antiproliferative activity. 3-Chlorogentisyl alcohol has the potential for the research of anti-cancer and anti-inflammatory therapies.
  • HY-12057S1
    Vemurafenib-d7

    PLX4032-d7; RG7204-d7; RO5185426-d7

    Raf Autophagy Cancer
    Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-147977
    ALR1/2-IN-1

    Aldose Reductase Cancer
    ALR1/2-IN-1 (Compound 6e) is an aldehyde reductase (ALR1) and aldose reductase (ALR2) inhibitor with IC50 values of 3.26 μM and 3.06 μM against ALR1 and ALR2, respectively. ALR1/2-IN-1 shows anticancer activity.
  • HY-146371
    COX-2-IN-13

    COX Inflammation/Immunology
    COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study.
  • HY-10014
    R547

    CDK GSK-3 Apoptosis Cancer
    R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
  • HY-118827S
    Vedaprofen-d3

    COX Inflammation/Immunology
    Vedaprofen-d3 is the deuterium labeled Vedaprofen. Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory drug (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM.
  • HY-143289
    NTPDase-IN-3

    Phosphatase Cancer Cardiovascular Disease
    NTPDase-IN-3 (Compound 5e) is a NTPDase inhibitor, with IC50 values of: 0.38 μM (NTPDase3), 0.05 μM (NTPDase8), 0.21 μM (NTPDase1), and 1.07 μM (NTPDase2). NTPDase-IN-3 can be used in the research of cancers and thrombosis.
  • HY-12291
    HG6-64-1

    HMSL 10017-101-1

    Raf Cancer
    HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
  • HY-124819
    D13-9001

    Bacterial Infection
    D13-9001 is a potent AcrB (AcrAB-TolC efflux pump subunit) and MexB (MexAB-OprM efflux pump subunit) inhibitor with the KD values of 1.15 μM and 3.57 μM in E. coli and P. aeruginosa, respectively. D13-9001 exhibits antibiotic activities.
  • HY-144878
    VPC-70619

    c-Myc Cancer
    VPC-70619 is a potent, orally active N-Myc inhibitor. VPC-70619 blocks the N-Myc-Max heterocomplex from binding to DNA E-boxes and demonstrated strong inhibition activity against N-Myc-dependent cell lines as well as high bioavailability in both oral and intraperitoneal administration.
  • HY-101647
    Intoplicine

    RP 60475

    Topoisomerase Cancer
    Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
  • HY-114324
    PROTAC PARP1 degrader

    PROTACs PARP Cancer
    PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
  • HY-144122
    HIV-1 inhibitor-15

    HIV Infection
    HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability.
  • HY-123967
    RNF5 inhibitor inh-02

    Others Inflammation/Immunology
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
  • HY-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.
  • HY-150612
    (R)-STU104

    p38 MAPK Cancer
    (R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis.
  • HY-117273
    AZ304

    Raf Autophagy Cancer
    AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity.
  • HY-107779
    BI-882370

    Raf Cancer
    BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases.
  • HY-110354
    UCM05

    G28UCM

    Fatty Acid Synthase (FASN) Bacterial Antibiotic Cancer Infection
    UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
  • HY-128382
    Brilliant Black BN

    E 151

    Enterovirus Infection
    Brilliant black BN (E151) is an azo dye and a food colorant. Brilliant black BN is a promising antiviral agent against EV71 infection via inhibiting the interaction between EV71 and its cellular uncoating factor cyclophilin A. Brilliant black BN has the potential for the investigation of contagious disease.
  • HY-N2106
    Dehydroevodiamine

    NF-κB COX PGE synthase NO Synthase Inflammation/Immunology
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
  • HY-139279
    TPX-0131

    Anaplastic lymphoma kinase (ALK) Cancer
    TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
  • HY-14658S
    Thalidomide D4

    Ligands for E3 Ligase Molecular Glues Autophagy Apoptosis Cancer Inflammation/Immunology
    Thalidomide D4 is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.
  • HY-113068
    (rel)-β-Tocopherol

    Tyrosinase Metabolic Disease
    (rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
  • HY-151357
    MraY-IN-3

    Bacterial Infection
    MraY-IN-3 (12a) is a potent bacterial translocase MraY inhibitor with an IC50 value of 140 µM. MraY-IN-3 acts on E. coli K12, B. subtilis W23 and P. fluorescens Pf-5 with the MIC50 values of 7 µg/mL, 12 µg/mL, and 46 µg/mL, respectively.
  • HY-144096
    EZH2-IN-11

    Others Cancer
    EZH2-IN-11 is a potent inhibitor of E2HZ. The oncogenic activities of EZH2 have been shown by a number of studies in various different cancer types. EZH2-IN-11 has the potential for the research of cancer diseases (extracted from patent WO2019204490A1, compound 17).
  • HY-101647A
    Intoplicine dimesylate

    RP 60475 dimesylate

    Topoisomerase Cancer
    Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
  • HY-131295
    PD0325901-O-C2-dioxolane

    MEK Ligands for Target Protein for PROTAC Cancer
    PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.
  • HY-135194
    Risperidone E-oxime

    Others Others
    Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
  • HY-115933
    EGFR/BRAF-IN-1

    EGFR Raf Cancer
    EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAF V600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM). EGFR/BRAF-IN-1 shows good antioxidant activity.
  • HY-110287
    Apcin

    APC Cancer
    Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis.
  • HY-115959
    Anticancer agent 34

    Bacterial Cancer Inflammation/Immunology
    Anticancer agent 34 (compound 9), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 34 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/ml. Anticancer agent 34 inhibits A549, PC3 cell growth with IC50s of 8.4 µg/ml, 7.8 µg/ml, respectively.
  • HY-115961
    Anticancer agent 36

    Bacterial Cancer Inflammation/Immunology
    Anticancer agent 36 (compound 11), a sulfonylurea derivative, is a potent antimicrobial and anticancer agent. Anticancer agent 36 inhibits the microbial growth of B. mycoides, E. coli, and C. albicans with a MIC between 0.156 and 0.039 mg/L. Anticancer agent 36 inhibits A549, PC3 cell growth with IC50s of 19.7 µg/mL, 11.9 µg/mL, respectively.
  • HY-147513
    AKT-IN-12

    Akt Apoptosis Cancer
    AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia.
  • HY-144675A
    LSD1-IN-13 hydrochloride

    Histone Demethylase Cancer
    LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines.
  • HY-N7626
    Eleutherol

    Fungal Glucosidase Infection
    Eleutherol is a naphthalene isolated from E. americana with antifungal activities. Eleutherol is against yeasts Candida albicans, C. tropicalis, Saccharomyces cerevisiae and Cryptococcus neoformans with MIC values between 7.8 µg/mL and 250 µg/mL. Eleutherol inhibits α-glucosidase function with an IC50>1.00 mM.
  • HY-108705
    BI-3802

    Bcl-2 Family Cancer
    BI-3802 is a highly potent BCL6 degrader and inhibits the Bric-à-brac (BTB) domain of BCL6 with an IC50 of ≤3 nM. BI-3802 induces the polymerization of BCL6 and promotes BCL6 degration depended on E3 ligase SIAH1. BI-3802 has antitumor activity.
  • HY-137315S
    TML-6-d3

    NF-κB mTOR Keap1-Nrf2 Amyloid-β Neurological Disease
    TML-6-d3 is the deuterium labeled TML-6. 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-
  • HY-W020790
    Sialyl-Lewis X

    sLeX

    Others Inflammation/Immunology
    Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation.
  • HY-16952
    Bepridil

    (±)-Bepridil; Org 5730

    Calcium Channel Sodium Channel SARS-CoV Infection Cardiovascular Disease
    Bepridil ((±)-Bepridil) is a calcium channel blocking agent used as antiarrhythmic agent. Bepridil inhibits both calcium and sodium currents, has research potential in certain ischemia-induced ventricular arrhythmias. Bepridil also has strong inhibition of SARS-CoV-2 from entry and replication inside Vero E6 and A549 cells.
  • HY-15605S
    Encorafenib-13C,d3

    LGX818-13C,d3

    Raf Cancer
    Encorafenib-13C,d3 (LGX818-13C,d3) is the 13C- and deuterium labeled Encorafenib. Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
  • HY-151166
    β-Glucuronidase-IN-2

    Bacterial Cancer
    β-Glucuronidase-IN-2 is a potent E. coli β-glucuronidase inhibitor with an IC50 value of 0.24 µM, an Ki value of 1.09 µM. β-Glucuronidase-IN-2 shows antiproliferative activity. β-Glucuronidase-IN-2 has the potential for the research of anti-cancer and anti-inflammatory therapies.
  • HY-16772
    EPI-743

    α-Tocotrienol quinone; PTC-743; Vatiquinone; NCT04378075

    Mitochondrial Metabolism Ferroptosis Neurological Disease
    EPI-743 (Vatiquinone; α-Tocotrienol quinone; PTC-743; NCT04378075) is a potent cellular oxidative stress protectant, inhibits ferroptosis in cells, which could be used for the study for mitochondrial diseases. EPI-743 is a synthetic analog of vitamin E with oral activity, targets repletion of reduced intracellular glutathione.
  • HY-15610
    GDC-0623

    RG 7421; MEK inhibitor 1

    MEK Apoptosis Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
  • HY-144675
    LSD1-IN-13

    Histone Demethylase Cancer
    LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines.
  • HY-12847
    CCT241161

    Raf Src Apoptosis Cancer
    CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.
  • HY-132998
    HDAC6 degrader-1

    PROTACs Others
    HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation.
  • HY-17624
    Framycetin

    Neomycin B; Fradiomycin B

    Bacterial Antibiotic Infection
    Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-127146
    Platensimycin

    Antibiotic Bacterial
    Platensimycin is an antibiotic produced by S. platensis that inhibits gram-positive bacteria by selectively inhibiting cellular lipid biosynthesis (IC50=0.1 μM). Platensimycin targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s=48 nM and 160 nM for S.aureus and E.coli enzymes, respectively). Platensimycin is a promising agent for overcoming antibiotic resistance.
  • HY-125789
    PF-04753299

    Bacterial Infection
    PF-04753299 is a potent and selective UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase (LpxC) inhibitor. PF-04753299 is bactericidal for the gonococcal isolates. PF-04753299 inhibits E. coli, P. aeruginosa and K. pneumoniae strains with MIC90 values of 2 μg/ml, 4 μg/ml and 16 μg/ml, respectively. PF-04753299 is used for the study of gram-negative bacteria infection.
  • HY-17624A
    Framycetin sulfate

    Neomycin B sulfate; Fradiomycin B sulfate

    Antibiotic Bacterial Infection
    Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
  • HY-P99107
    Brentuximab vedotin

    Antibody-Drug Conjugates (ADCs) Apoptosis TNF Receptor Cancer
    Brentuximab vedotin (cAC10-vcMMAE) is an antibody-drug conjugate (ADC) comprising an anti- CD30 antibody and the cytotoxic agent Monomethyl auristatin E (MMAE). Brentuximab vedotin inhibits CD30-positive cells with an IC50 of 2.5 ng/mL. Brentuximab vedotin can be used for the research of relapsed and refractory Hodgkin lymphoma.
  • HY-103046
    UbcH5c-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-100864
    mPGES1-IN-3

    PGE synthase Inflammation/Immunology
    mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
  • HY-147742
    Thi-DPPY

    JAK Inflammation/Immunology
    Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
  • HY-N4237
    Saikogenin D

    Prostaglandin Receptor Potassium Channel Inflammation/Immunology
    Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
  • HY-12304
    IOX1

    Histone Demethylase Cancer
    IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC50 values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.
  • HY-144123
    HIV-1 inhibitor-16

    HIV Infection
    HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity.
  • HY-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-10581A
    Gatifloxacin hydrochloride

    AM-1155 hydrochloride; BMS-206584 hydrochloride; PD135432 hydrochloride

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
  • HY-116788
    Lipofermata

    Bacterial Infection
    Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM.
  • HY-10581B
    Gatifloxacin mesylate

    AM-1155 mesylate; BMS-206584 mesylate; PD135432 mesylate

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin mesylate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin mesylate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin mesylate can be used to treat bacterial conjunctivitis in vivo.
  • HY-130854
    Thalidomide-NH-C6-NH-Boc

    E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
  • HY-147405
    Tinlorafenib

    PF-07284890; ARRY-461

    Raf Cancer
    Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAF V600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies.
  • HY-113068S
    β-Tocopherol-d3

    Tyrosinase Metabolic Disease
    β-Tocopherol-d3 is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol can also prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
  • HY-115672
    KS15

    Others Cancer
    KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity.
  • HY-12057S
    Vemurafenib-d5

    Raf Autophagy Cancer
    Vemurafenib-d5 (PLX4032-d5) is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
  • HY-132296
    GSK215

    FAK PROTACs Cancer
    GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect.
  • HY-144307
    Aurora A/PKC-IN-1

    Aurora Kinase PKC Cancer
    Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity.
  • HY-143898
    PIM1-IN-4

    Pim Cancer
    PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases.
  • HY-135969
    Glycol chitosan

    Bacterial Infection
    Glycol chitosan is a chitosan derivative with ethylene glycol branches. Glycol chitosan enhances membrane permeability and leadkage in Glycine max Harosoy 63W cells. Glycol chitosan is biocompatible and biodegradable. Glycol chitosan inhibits E. coli, S. aureus and S. enteritidis growths with MIC values of 4 μg/mL, 32 μg/mL and <0.5 μg/mL, respectively.
  • HY-N2278
    Kushenol A

    Leachianone E

    Tyrosinase Glucosidase Cancer
    Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
  • HY-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-13811
    NSC697923

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-B0132S
    Norfloxacin-d5

    Bacterial Antibiotic Infection
    Norfloxacin-d5 is a deuterium labeled Norfloxacin. Norfloxacin is a fluoroquinolone antibiotic that inhibits the growth of Gram-positive and Gram-negative bacteria (MICs = 4 μg/mL and 1 μg/mL for S. aureus and P. aeruginosa, respectively). Norfloxacin also inhibits the growth S. pseudintermedius, S. aureus, E. coli, Pasturella, and S. canis isolates from dogs (mean MIC50s = 0.25 μg/mL, 1 μg/mL, 0.03 μg/mL, 1 μg/mL, and 1 μg/mL, respectively).
  • 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-12033
    2-Methoxyestradiol

    2-ME2; NSC-659853

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-119271
    CMLD010509

    SDS-1-021

    c-Myc Apoptosis Cancer
    CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism.
  • HY-12302
    Kenpaullone

    9-Bromopaullone; NSC-664704

    CDK GSK-3 Cancer
    Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
  • HY-131907
    LpxC-IN-5

    Bacterial Infection
    LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively.
  • HY-146977
    LDHA/PDKs-IN-1

    PDK-1 Cancer
    LDHA/PDKs-IN-1 (compound 20e) is a potent and dual inhibitor of PDKs and LDHA with IC50s of 0.8 and 0.15 μM, respectively. LDHA/PDKs-IN-1 reduces A549 cell proliferation with an EC50 of 13.2 μM and decreases the lactate formation, and increases oxygen consumption. LDHA/PDKs-IN-1 has the potential for the research of cancer diseases.
  • HY-10581
    Gatifloxacin

    AM-1155; BMS-206584; PD135432

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50=0.109 μg/ml). Gatifloxacin can be used to treat bacterial conjunctivitis in vivo.
  • HY-N0074
    Byakangelicol

    COX Inflammation/Immunology
    Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
  • HY-144736
    NS2B/NS3-IN-4

    Virus Protease Infection
    NS2B/NS3-IN-4 (Compound 34e) is an allosteric DENV2 and ZIKV NS2B/NS3 protease inhibitor with IC50 values of 0.69 µM and 1.04 µM against DENV2 and ZIKV NS2B/NS3 proteases, respectively.
  • HY-W037817
    Dimethyl L-glutamate

    Dimethyl glutamate

    Potassium Channel Bacterial Infection Metabolic Disease
    Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism.
  • HY-10424
    Milciclib

    PHA-848125

    CDK Autophagy Cancer
    Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC50s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.
  • HY-N7148S1
    γ-Tocopherol-d4

    COX Cancer Inflammation/Immunology
    γ-Tocopherol-d4 (D-γ-Tocopherol-d4) is the deuterium labeled γ-Tocopherol. γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
  • HY-10581C
    Gatifloxacin sesquihydrate

    AM-1155 sesquihydrate; BMS-206584 sesquihydrate; PD135432 sesquihydrate

    Bacterial Topoisomerase Antibiotic Infection Inflammation/Immunology
    Gatifloxacin sesquihydrate (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin sesquihydrate inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin sesquihydrate can be used to treat bacterial conjunctivitis in vivo.
  • HY-148044
    UNC10201652

    Bacterial Infection
    UNC10201652 is a potent Loop 1 (L1)-specific gut bacterial β-glucuronidase (GUSs) inhibitor with an IC50 value of 0.117 μM for E. coli GUS. UNC10201652 can block SN-38 glucuronide (HY-126373) processing only in individuals whose fecal gut microbiota is highly abundant in L1 GUS enzymes.
  • HY-128686
    KAG-308

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    KAG-308 is a potent selective and orally active agonist of EP4 receptor (a prostaglandin E2 receptor subtype), suppresses colitis and promotes histological mucosal healing, potently inhibits TNF-α production. KAG-308 shows a Ki and an EC50 of 2.57 nM and 17 nM for human EP4 receptor, respectively, more selective over EP1, EP2, EP3 and IP receptor.
  • HY-141431
    Cbl-b-IN-2

    E3 Ligase Ligand-Linker Conjugates Cancer Inflammation/Immunology
    Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
  • HY-12843
    Bohemine

    CDK ERK Cancer
    Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
  • HY-125877
    PROTAC Mcl1 degrader-1

    PROTACs Bcl-2 Family Cancer
    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC50 of 0.78 μM. PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity.
  • HY-107573
    KDM2/7-IN-1

    Histone Demethylase Cancer
    KDM2/7-IN-1 (TC-E 5002) is a selective histone demethylase KDM2/7 subfamily inhibitor (IC50 values are 0.2, 1.2, 6.8, 55, 83, >100 and >120 μM for KDM7A, KDM7B, KDM2A, KDM5A, KDM4C, KDM6A and KDM4A respectively). KDM2/7-IN-1 inhibits growth of HeLa and KYSE-150 cancer cells in vitro.
  • HY-147947
    Tubulin polymerization-IN-30

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM.
  • HY-146492
    VEGFR-2/BRAF-IN-2

    VEGFR Raf Apoptosis Cancer
    VEGFR-2/BRAF-IN-2 (Compound 4a) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.111, 0.089 and 0.071 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-2 induces apoptosis and arrests the cell cycle mainly in the G1 phase.
  • HY-108467
    GGsTop

    Nahlsgen

    Others Cardiovascular Disease
    GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ−glutamyl transpeptidase (GGT) inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150±10 and 51±3 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model.
  • HY-139328
    CDK12-IN-5

    CDK Cancer
    CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-10581AS
    Gatifloxacin-d3 hydrochloride

    AM-1155-d3 hydrochloride; BMS-206584-d3 hydrochloride; PD135432-d3 hydrochloride

    Bacterial Topoisomerase Antibiotic Infection
    Gatifloxacin-d3 (hydrochloride) is the deuterium labeled Gatifloxacin (hydrochloride). Gatifloxacin hydrochloride (AM-1155; BMS-206584; PD135432) is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases (IC50=13.8 μg/ml for S. aureus topoisomerase IV) and E. coli DNA gyrase (IC50 = 0.109 μg/ml). Gatifloxacin hydrochloride can be used to treat bacterial conjunctivitis in vivo.
  • HY-125728
    Micrococcin P1

    Bacterial Parasite HCV Infection
    Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC50 range of 0.1-0.5 μM. Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against S. aureus 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively. Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum.
  • HY-18299
    Purvalanol B

    NG 95

    CDK Parasite Cancer Infection
    Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum.
  • HY-111546
    BI-3663

    PROTACs FAK Cancer
    BI-3663 is a highly selective PTK2/FAK PROTAC (DC50=30 nM), with Cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC50 of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.
  • HY-144323
    YF135

    PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway.
  • HY-111140
    YS121

    PGE synthase Lipoxygenase Inflammation/Immunology
    YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells.
  • HY-146491
    VEGFR-2/BRAF-IN-1

    VEGFR Raf Apoptosis Cancer
    VEGFR-2/BRAF-IN-1 (Compound 4b) is a dual VEGFR-2 and BRAF kinases inhibitor with IC50 values of 0.049, 0.063 and 0.005 µM against VEGFR-2, BRAF V600E and BRAF WT, respectively. VEGFR-2/BRAF-IN-1 induces apoptosis and arrests the cell cycle mainly in the G1/S phase.
  • HY-139329
    CDK12-IN-6

    CDK Cancer
    CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-117026
    LKY-047

    Cytochrome P450 Metabolic Disease Inflammation/Immunology
    LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A.
  • HY-136055
    (S,R,S)-AHPC-C5-COOH

    VH032-C5-COOH

    E3 Ligase Ligand-Linker Conjugates HIF/HIF Prolyl-Hydroxylase Cancer
    (S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases.
  • HY-125876
    PROTAC Bcl2 degrader-1

    PROTACs Bcl-2 Family Cancer
    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
  • HY-100022
    Tomivosertib

    eFT508

    MNK PD-1/PD-L1 Cancer
    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.
  • HY-139327
    CDK12-IN-4

    CDK Cancer
    CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1).
  • HY-N6979
    Crustecdysone

    20-Hydroxyecdysone

    Caspase Autophagy Endogenous Metabolite Cardiovascular Disease
    Crustecdysone (20-Hydroxyecdysone) is a naturally occurring ecdysteroid hormone isolated from Cyanotis arachnoides C.B.Clarke which controls the ecdysis (moulting) and metamorphosis of arthropods, it inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP. Crustecdysone exhibits regulatory or protective roles in the cardiovascular system. Crustecdysone is an active metabolite of Ecdysone (α-Ecdysone; HY-N0179)
  • HY-146019A
    HIV-1 inhibitor-25

    HIV Infection
    HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS.
  • HY-134807
    Indophagolin

    P2X Receptor 5-HT Receptor Autophagy Cancer
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
  • HY-134903
    (32-Carbonyl)-RMC-5552

    mTOR Cancer
    (32-Carbonyl)-RMC-5552 is a potent mTOR inhibitor. (32-Carbonyl)-RMC-5552 inhibits mTORC1 and mTORC2 substrate (p-P70S6K-(T389), p-4E-BP1-(T37/36), AND p-AKT1/2/3-(S473)) phosphorylation with pIC50s of > 9, >9 and between 8 and 9, respectively (patent WO2019212990A1, example 2).
  • HY-12033S2
    2-Methoxyestradiol-d5

    2-ME2-d5; NSC-659853-d5

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite
    2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-W011428
    Olomoucine

    CDK Others
    Olomoucine is an ATP competitive inhibitor of CDKs. Olomoucine is a purine (HY-34431) derivative and inhibits CDC2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E (both IC50=7 µM), CDK/p35 kinase (IC50=3 µM) and ERK1/p44 MAP kinase (IC50=25 µM). Olomoucine regulates cell cycle and shows anti-melanin tumor activity.
  • HY-144269
    SHR902275

    Raf Cancer
    SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively.
  • HY-17639
    Navamepent

    RX-10045

    Others Inflammation/Immunology
    Navamepent is an analog of naturally occurring resolvin E1 (a major dietary omega-3 polyunsaturated fatty-acid metabolite) with potent anti-inflammatory and cell survival benefits. Navamepent is highly effective against dry eye and goblet cell loss thereby accelerating tear production. Also, Navamepent can reduce corneal inflammation, epithelial damage, and accelerate corneal tissue repair. In addition, Navamepent can inhibit the release of several key proinflammatory mediators from corneal epithelial cells.
  • HY-103636
    PROTAC Sirt2 Degrader-1

    Sirtuin PROTACs Cancer
    PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
  • HY-A0003B
    Lenalidomide hemihydrate

    CC-5013 hemihydrate

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-130122
    MG-277

    PROTACs Apoptosis Cancer
    MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
  • HY-12892
    SKI-178

    SphK Apoptosis Cancer
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
  • HY-W019806
    Lacto-N-fucopentaose I

    LNFP I

    Endogenous Metabolite CDK Reactive Oxygen Species Apoptosis Enterovirus Bacterial Infection Inflammation/Immunology
    Lacto-N-fucopentaose I (LNFPI) is a human milk oligosaccharide (HMO), possessing antiviral and antibacterial activity. Lacto-N-fucopentaose I can reduce capsid protein VP1 to block virus adsorption, promote CDK2 and reduce cyclin E to recover cell cycle S phase block. Lacto-N-fucopentaose I inhibits ROS production and apoptosis in virus-infected cells. Lacto-N-fucopentaose I can also regulate intestinal microbiota to affect immune system development.
  • HY-46531
    Thalidomide-5-NH2-CH2-COOH

    Ligands for E3 Ligase Cancer Inflammation/Immunology
    Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1).
  • HY-144730
    gp120-IN-1

    HIV Inflammation/Immunology
    gp120-IN-1 (compound 4e) is a potent HIV-1 gp120 inhibitor with an IC50 of 2.2 µM and CC50 of 100.90 µM. gp120-IN-1 shows anti-HIV-1 activity. gp120-IN-1 shows cytotoxicity in a dose dependent manner in SUP-T1 cells. gp120-IN-1 shows inhibition of gp120-mediated virus enter into cells.
  • HY-130241
    Reverse transcriptase-IN-1

    HIV Infection
    Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme.
  • HY-A0003
    Lenalidomide

    CC-5013

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer Inflammation/Immunology
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-150596
    CT1-3

    Apoptosis Bcl-2 Family JNK Cancer
    CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity.
  • HY-129619
    SNIPER(ER)-87

    SNIPERs Estrogen Receptor/ERR Cancer
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
  • HY-144749
    AKR1C3-IN-5

    Others Cancer
    AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells.
  • HY-A0003A
    Lenalidomide hydrochloride

    CC-5013 hydrochloride

    Ligands for E3 Ligase Molecular Glues Cancer Inflammation/Immunology
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-12033S
    2-Methoxyestradiol-13C,d3

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol-13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-147518
    p38-α MAPK-IN-5

    p38 MAPK Inflammation/Immunology
    p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research.
  • HY-130422
    Tos-PEG4-t-butyl ester

    Tos-PEG4-Boc

    PROTAC Linkers Cancer
    Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC50 of 18 nM.
  • HY-144688
    HIV-1 protease-IN-1

    HIV Infection
    HIV-1 protease-IN-1 (Compound 1e) is a potent inhibitor of HIV-1 protease with an IC50 of 90 pM. HIV-1 protease-IN-1 demonstrates antiviral activity with EC50 value of 89 nM against B-HIV. HIV-1 protease-IN-1 exhibits activity with EC50 value of 13.59 nM against C-HIV strain ZM246. HIV-1 protease-IN-1 shows remarkable activity with EC50 value of 8.23 nM against C-HIV strain Indie[1].
  • HY-111932
    Indirubin-5-sulfonate

    CDK GSK-3 Cancer
    Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
  • HY-A0003S
    Lenalidomide-d5

    CC-5013-d5

    Ligands for E3 Ligase Molecular Glues Apoptosis Cancer Inflammation/Immunology
    Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-146001
    Influenza virus-IN-4

    Influenza Virus Inflammation/Immunology
    Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidase inhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitory activity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice.
  • HY-12033S1
    2-Methoxyestradiol-13C6

    2-ME2-13C6; NSC-659853-13C6

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol-13C6 (2-ME2-13C6) is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-126251
    CDK9-IN-7

    CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-108359
    Alsterpaullone

    9-Nitropaullone; NSC 705701

    CDK GSK-3 Apoptosis Cancer
    Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.
  • HY-129602
    SD-36

    PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-107738
    Guggulsterone

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
  • HY-147898
    PI3K-IN-33

    PI3K Apoptosis Cancer
    PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research.
  • HY-144451
    TRK-IN-12

    Trk Receptor Cancer
    TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control drug LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line.
  • HY-11080A
    PKI-179 hydrochloride

    PI3K mTOR Cancer
    PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo.
  • HY-131187
    BMS-1166-N-piperidine-COOH

    Ligands for Target Protein for PROTAC Cancer
    BMS-1166-N-piperidine-COOH, the BMS-1166-based moiety, binds to E3 ligase ligand via a linker to form PROTAC PD-1/PD-L1 degrader-1 (HY-131183) to degrade PD-1/PD-L1. BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
  • HY-11080
    PKI-179

    PI3K mTOR Cancer
    PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo.
  • HY-18340
    (R)​-​CR8

    CR8, (R)-Isomer

    CDK Apoptosis Cancer Neurological Disease
    (R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.
  • HY-18340A
    (R)-CR8 trihydrochloride

    CR8, (R)-Isomer trihydrochloride

    CDK Apoptosis Cancer Neurological Disease
    (R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.
  • HY-112363
    Aloisine A

    RP107

    CDK GSK-3 ERK JNK CFTR Cancer Inflammation/Immunology
    Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 µM) and GSK-3β (IC50=1.5 µM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research.
  • HY-131183
    PROTAC PD-1/PD-L1 degrader-1

    PROTACs PD-1/PD-L1 Inflammation/Immunology
    PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.