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Results for "17 dmag hsp90 Inhibitors" in MCE Product Catalog:

422

Inhibitors & Agonists

1

Screening Libraries

1

Dye Reagents

42

Peptides

58

Natural
Products

9

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-10389
    Alvespimycin

    17-dmag; NSC 707545

    HSP Cancer
    Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM.
  • HY-12024
    Alvespimycin hydrochloride

    17-dmag hydrochloride; KOS-1022; BMS 826476

    HSP Apoptosis Cancer
    Alvespimycin hydrochloride (17-DMAG hydrochloride; KOS-1022; BMS 826476) is a potent inhibitor of Hsp90, binding to Hsp90 with EC50 of 62±29 nM.
  • HY-111414
    Hsp90-Cdc37-IN-1

    HSP Cancer
    Hsp90-Cdc37-IN-1 is an Hsp90-Cdc37 interaction disruptor that inhibit cell migration and reverse drug resistance, with an IC50 of 140 nM.
  • HY-133570
    17-AEP-GA

    HSP ADC Cytotoxin Cancer
    17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
  • HY-130997
    17-GMB-APA-GA

    HSP ADC Cytotoxin Cancer Infection
    17-GMB-APA-GA is an ADC Cytotoxin. 17-GMB-APA-GA is a potent HSP90 inhibitor and used for latent T. gondii infection research.
  • HY-10211
    Tanespimycin

    17-AAG; NSC 330507; CP 127374

    HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic Cancer Infection
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
  • HY-106723
    AMP-PCP

    HSP Cancer
    AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90.
  • HY-106723A
    AMP-PCP disodium

    HSP Cancer
    AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90.
  • HY-13757AS
    Tamoxifen-​d5

    ICI 47699-​d5; (Z)-Tamoxifen-​d5; trans-Tamoxifen-​d5

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
  • HY-115499
    MPC-0767

    HSP Cancer
    MPC-0767 is a potent, selective, and orally active hsp90 inhibitor. MPC-0767 is an L-alanine ester prodrug of MPC-3100 with improved chemical stability.
  • HY-13757A
    Tamoxifen

    ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen activates autophagy and induces apoptosis.
  • HY-10212
    BIIB021

    CNF2024

    HSP Autophagy Cancer
    BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.
  • HY-13757
    Tamoxifen Citrate

    ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate

    Estrogen Receptor/ERR HSP Autophagy Apoptosis Cancer
    Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate activates autophagy and induces apoptosis.
  • HY-N3417
    Kongensin A

    HSP RIP kinase Apoptosis Cancer Inflammation/Immunology
    Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
  • HY-10210
    Retaspimycin Hydrochloride

    IPI-504

    HSP Cancer
    Retaspimycin Hydrochloride is a potent and water-soluble inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
  • HY-15263
    Retaspimycin

    HSP Cancer
    Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.
  • HY-N6769
    Radicicol

    Monorden

    HSP Bacterial Antibiotic Infection
    Radicicol is an inhibitor of Hsp90 with an IC50 value of 1 μM. Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients, leading to proteasomal degradation. Radicicol is an antifungal antibiotic with antimalarial activity, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB.
  • HY-130851
    HS-27

    HSP Cancer
    HS-27, a fluorescently-tethered Hsp90 inhibitor, assays surface Hsp90 expression on intact tissue specimens. HS-27 is made up of the core elements of SNX-5422, an Hsp90 inhibitor, tethered via a PEG linker to a fluorescein derivative (fluorescein isothiocyanate or FITC), that binds to ectopically expressed Hsp90. HS-27 has potential use in a see-and-treat paradigm in breast cancer.
  • HY-N1455
    Falcarinol

    Panaxynol; Carotatoxin

    HSP Cancer
    Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.
  • HY-133705
    Geldanamycin-FITC

    HSP Others
    Geldanamycin-FITC, a Geldanamycin fluorescent probe, can be used in a fluorescence polarization assay for HSP90 inhibitors. Geldanamycin-FITC also can be used for detection of cell surface HSP90.
  • HY-15986
    VER-49009

    CCT 129397

    HSP Cancer
    VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
  • HY-15984
    VER-50589

    HSP Apoptosis Cancer
    VER-50589 is a Hsp90 inhibitor, with an IC50 of 21 nM and a Kd of 4.5 nM.
  • HY-13313
    XL888

    HSP Cancer
    XL888 is a heat shock protein-90 (HSP90) inhibitor, with an IC50 of 24 nM.
  • HY-14463
    Onalespib

    AT13387

    HSP Cancer
    Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.
  • HY-10215
    Luminespib

    NVP-AUY922; VER-52296

    HSP Autophagy Apoptosis Cancer
    Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
  • HY-13469
    Debio 0932

    CUDC-305

    HSP Cancer
    Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
  • HY-15190
    NVP-HSP990

    hsp-990

    HSP Apoptosis Cancer
    NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
  • HY-108248
    KU-32

    HSP Metabolic Disease Neurological Disease Cardiovascular Disease
    KU-32 is a novel, novobiocin-based Hsp90 inhibitor that can protect against neuronal cell death.
  • HY-N1986
    Cucurbitacin D

    HSP Cancer
    Cucurbitacin D is an active component in Cucurbita texana, disrupts interactions between Hsp90 and two co-chaperones, Cdc37 and p23. Cucurbitacin D prevents Hsp90 client (Her2, Raf, Cdk6, pAkt) maturation without induction of the heat shock response. Anti-cancer activity.
  • HY-102007
    Gamitrinib TPP

    HSP Cancer
    Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
  • HY-114413
    YZ129

    HSP Apoptosis Cancer
    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. YZ129-induced GBM cell-cycle arrest at the G2/M phase promotes apoptosis and inhibited tumor cell proliferation and migration.
  • HY-B1425
    Ethoxyquin

    HSP Reactive Oxygen Species Cancer
    Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90).
  • HY-102007A
    Gamitrinib TPP hexafluorophosphate

    HSP Cancer
    Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
  • HY-15205
    Ganetespib

    STA-9090

    HSP Apoptosis Cancer
    Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
  • HY-P1750
    Shepherdin (79-87)

    HSP Survivin Cancer
    Shepherdin (79-87) is amino acids 79 to 87 fragment of Shepherdin. Shepherdin is a peptidomimetic antagonist of the complex between Hsp90 and Survivin. Anticancer activity.
  • HY-N0754
    Eupalinolide A

    HSP Inflammation/Immunology
    Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
  • HY-15785
    TAS-116

    HSP Cancer
    TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
  • HY-15230
    Geldanamycin

    HSP Bacterial Influenza Virus Antibiotic Cancer Infection Inflammation/Immunology
    Geldanamycin is a Hsp90 inhibitor with antimicrobial activity against many Gram-positive and some Gram-negative bacteria. Geldanamycin has anti-influenza virus H5N1 activities.
  • HY-10213A
    SNX-5422 Mesylate

    PF-04929113 (Mesylate)

    HSP Cancer
    SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37 nM.
  • HY-B0425A
    Novobiocin Sodium

    Albamycin; Cathomycin

    Bacterial Autophagy Antibiotic Infection Cancer
    Novobiocin Sodium (Albamycin; Cathomycin) is an orally active antibiotic compound derived from Streptomyces niveus and a potent DNA gyrase inhibitor by binding the ATP-binding site in the ATPase subunit. Novobiocin Sodium manifests strong anti-bacterial activities effectively against gram-positive pathogens and shows limited activity against gram-negative organisms due to LPS-containing outer membrane.Novobiocin Sodium binds to the C-terminus of Hsp90 and slightly induces degradation of Hsp90-dependent client proteins (IC50=700 µM).
  • HY-N6850
    Calenduloside E

    HSP Endogenous Metabolite
    Calenduloside E (CE) is a natural pentacyclic triterpenoid saponin extracted from Aralia elata. Calenduloside E (CE) has anti-apoptotic potent by targeting heat shock protein 90 (Hsp90).
  • 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-N1934
    Dihydroberberine

    Potassium Channel HSP Cancer Inflammation/Immunology Cardiovascular Disease
    Dihydroberberine inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces heat shock protein 90 (Hsp90) expression and its interaction with hERG. Dihydroberberine has anti-inflammatory, anti-atherosclerotic, hypolipidemic and antitumor activities.
  • HY-10942
    VER-82576

    NVP-BEP800

    HSP Cancer
    VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
  • HY-108486
    Herbimycin A

    Bacterial Antibiotic
    Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
  • HY-120548
    KBU2046

    Others Cancer
    KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
  • HY-121744
    PS10

    PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
  • HY-112910
    Grp94 Inhibitor-1

    HSP Cancer Infection
    Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
  • HY-13468
    KW-2478

    HSP Cancer
    KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
  • HY-B0891
    17-Hydroxyprogesterone

    17α-Hydroxyprogesterone; 17-OHP

    Progesterone Receptor Endogenous Metabolite Others
    17-Hydroxyprogesterone (17-OHP) is an endogenous progestogen as well as chemical intermediate in the biosynthesis of other steroid hormones, including the corticosteroids and the androgens and the estrogens.
  • HY-136239
    Beclomethasone 17-propionate

    Beclomethasone-17-monopropionate; 17-BMP

    Glucocorticoid Receptor Drug Metabolite Inflammation/Immunology
    Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages.
  • HY-113263
    17a-Hydroxypregnenolone

    Endogenous Metabolite Endocrinology
    17a-Hydroxypregnenolone is a pregnane steroid. 17a-Hydroxypregnenolone is a prohormone in the formation of dehydroepiandrosterone (DHEA).
  • HY-B0983
    Hydrocortisone 17-butyrate

    Cortisol 17-butyrate; Hydrocortisone butyrate

    Adrenergic Receptor Inflammation/Immunology Endocrinology
    Hydrocortisone 17-butyrate is an adrenocortico hormone
  • HY-N4132
    17-Hydroxyisolathyrol

    Others Infection Inflammation/Immunology
    17-Hydroxyisolathyrol is a macrocychc lathyrol derivative isolated from seeds of Euphorbla luthyrrs.
  • HY-101030A
    MBM-17S

    Apoptosis Cancer
    MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
  • HY-U00138
    Androstenediol 17-acetate

    Others Endocrinology
    Androstenediol 17-acetate is a synthetic anabolic-androgenic steroid and an androgen ester.
  • HY-B0708
    β-Estradiol 17-acetate

    1,3,5(10)-Estratriene-3,17β-diol 17-acetate

    Estrogen Receptor/ERR Endocrinology
    β-Estradiol 17-acetate is a metabolite of estradiol.
  • HY-P1484
    Bradykinin (1-7)

    Bradykinin Fragment 1-​7

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase.
  • HY-13331
    Clascoterone

    Cortexolone 17 alpha-propionate; Cortexolone 17α-propionate; CB-03-01

    Androgen Receptor Endocrinology
    Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
  • HY-13615A
    EC-17 disodium salt

    Others Cancer
    EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.
  • HY-101516
    CYP17-IN-1

    Cytochrome P450 Cancer
    CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM.
  • HY-U00161
    Betamethasone 17-benzoate

    Others Inflammation/Immunology
    Betamethasone 17-benzoate is a representative steroid, which can be used in the treatment of recurrent aphothous ulcers (RAU).
  • HY-B0742
    Hydroxyprogesterone caproate

    17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate

    Others Others
    Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17α-hydroxyprogesterone formed from caproic acid.
  • HY-P1066
    Apelin-17(human, bovine)

    HIV Infection
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-P1755
    p53 (17-26)

    MDM-2/p53 Cancer
    p53 (17-26) is amino acids 17 to 26 fragment of p53. p53 (17-26) is mdm-2-binding domain.
  • HY-B0491A
    Carbazochrome sodium sulfonate

    AC-17

    Adrenergic Receptor Cardiovascular Disease Endocrinology
    Carbazochrome (sodium sulfonate) (AC-17) is an antihemorrhagic agent.
  • HY-101030
    MBM-17

    Apoptosis Cancer
    MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
  • HY-P1204
    [Ala17]-MCH

    MCHR1 (GPR24) Metabolic Disease
    [Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
  • HY-141024
    Bis-PEG17-acid

    PROTAC Linker Cancer
    Bis-PEG17-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140502
    m-PEG17-acid

    PROTAC Linker Cancer
    m-PEG17-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-101915
    IL-17A antagonist 3

    Interleukin Related Inflammation/Immunology
    IL-17A antagonist 3 is an IL-17A antagonist, compound 3.
  • HY-130600
    HO-PEG17-OH

    PROTAC Linker Cancer
    HO-PEG17-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-133350
    m-PEG17-Hydrazide

    PROTAC Linker Cancer
    m-PEG17-Hydrazide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140062
    Propargyl-PEG17-methane

    PROTAC Linker Cancer
    Propargyl-PEG17-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-113368
    3b,17b-Dihydroxyetiocholane

    Endogenous Metabolite Metabolic Disease
    3b,17b-Dihydroxyetiocholane is known as androgens and derivatives.
  • HY-U00272
    Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)-

    Androst-4-ene-3β,17β-diol, dipropionate

    Androgen Receptor Metabolic Disease Neurological Disease
    Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- is the dipropanoate of 4-Androstenediol, a metabolite of testosterone.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-P1066A
    Apelin-17(human, bovine) TFA

    HIV Infection
    Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-123918
    JMS-17-2

    Others Cancer Endocrinology
    JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells.
  • HY-101929
    CU-CPT17e

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    CU-CPT17e is a potent multi-Toll-like receptor (TLR) agonist that activates TLR3, TLR8, and TLR9.
  • HY-P1545
    ACTH (1-17)

    α1-17-ACTH

    Melanocortin Receptor Cancer Neurological Disease Endocrinology
    ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-B0775
    Betamethasone-17-butyrate-21-propionate

    Others Inflammation/Immunology
    Betamethasone-17-butyrate-21-propionate is a topical corticosteroid with potential in the treatment of inflammatory skin diseases.
  • HY-101913
    IL-17A antagonist 1

    Interleukin Related Inflammation/Immunology
    IL-17A antagonist 1 (compound 1) is an IL-17A antagonist, with a Kd of 0.66 μM and an IC50 of 1.14 μM.
  • HY-P1204A
    [Ala17]-MCH TFA

    MCHR1 (GPR24) Metabolic Disease
    [Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
  • HY-B0727
    Betamethasone valerate

    Betamethasone 17-valerate

    Glucocorticoid Receptor Inflammation/Immunology
    Betamethasone valerate (Betamethasone 17-valerate), the 17-valerate ester of Betamethasone, is a topical corticosteroid with anti-inflammatory activity. Betamethasone valerate is used in the treatment of recurrent aphthous stomatitis. Betamethasone valerate inhibits the binding of the radiolabeled glucocorticoid dexamethasone ( 3H dexamethasone) to human epidermis and mouse skin with IC50s of 5 and 6 nM, respectively.
  • HY-133046
    VHL Ligand-Linker Conjugates 17

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.
  • HY-140042
    Bis-propargyl-O-PEG17

    PROTAC Linker Cancer
    Bis-propargyl-O-PEG17 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141108
    m-PEG17-NHS ester

    PROTAC Linker Cancer
    m-PEG17-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-A0095
    Flibanserin

    BIMT-17; BIMT-17BS

    5-HT Receptor Neurological Disease
    Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD).
  • HY-15665
    XMD17-109

    ERK Cancer
    XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC50 of 162 nM.
  • HY-130826
    Bis-PEG17-NHS ester

    ADC Linker Cancer
    Bis-PEG17-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-P1341
    OXA(17-33)

    Orexin Receptor (OX Receptor) Neurological Disease
    OXA(17-33) is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
  • HY-117291A
    XMD-17-51 Trifluoroacetate

    Others Others
    XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that is able to modulate protein kinases.
  • HY-123918A
    JMS-17-2 hydrochloride

    Others Cancer Endocrinology
    JMS-17-2 hydrochloride is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 hydrochloride impairs metastatic seeding and colonization of breast cancer cells.
  • HY-101097
    PD-1-IN-17

    PD-1/PD-L1 Cancer
    PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • 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-B0672
    Estradiol valerianate

    β-Estradiol 17-valerate

    Estrogen Receptor/ERR Endocrinology Cancer
    Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs.
  • HY-P1545A
    ACTH (1-17) (TFA)

    α1-17-ACTH TFA

    Melanocortin Receptor Cancer Neurological Disease Endocrinology
    ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
  • HY-B0216
    Ethynyl Estradiol

    17α-Ethynylestradiol; Ethynylestradiol

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Ethynyl Estradiol (17α-Ethynylestradiol;Ethynylestradiol) is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills.
  • HY-12403
    Angiotensin (1-7)

    Ang-(1-7)

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Inflammation/Immunology Cardiovascular Disease Endocrinology
    Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
  • HY-128918
    SIS17

    HDAC Others
    SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
  • HY-101097A
    PD-1-IN-17 (TFA)

    PD-1/PD-L1 Cancer
    PD-1-IN-17 TFA is a programmed cell death-1 (PD-1) inhibitor extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM.
  • HY-P1341A
    OXA(17-33) TFA

    Orexin Receptor (OX Receptor) Neurological Disease
    OXA(17-33) TFA is a potent and selective orexin-1 receptor (OX1) agonist. OXA(17-33) TFA shows a ∼23-fold selectivity for the OX1 (EC50=8.29 nM) over OX2 (187 nM).
  • HY-A0095S
    Flibanserin D4

    BIMT-17 D4; BIMT-17BS D4

    5-HT Receptor Neurological Disease
    Flibanserin D4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM).
  • HY-125875
    KRAS G12C inhibitor 17

    Ras Cancer
    KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM.
  • HY-P1772
    β-Amyloid (1-17)

    Amyloid-β Neurological Disease
    β-Amyloid (1-17) is a peptide of β-Amyloid, stabilizes the fibres and plays a role in Aβ fibre formation.
  • HY-P1791
    Lactoferrin (17-41)

    Lactoferricin B; Lfcin B

    Bacterial Fungal Apoptosis Cancer Infection
    Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities.
  • HY-N2116
    Ginkgolic acid C17:1

    PTEN Phosphatase Cancer
    Ginkgolic acid C17:1, extracted from Ginkgo biloba Leaves, suppresses constitutive and inducible STAT3 activation through induction of PTEN and SHP-1 tyrosine phosphatase. Ginkgolic acid C17:1 has anticancer effects.
  • HY-128976
    10β,17β-dihydroxyestra-1,4-dien-3-one

    DHED

    Estrogen Receptor/ERR Metabolic Disease
    10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.
  • HY-P1791B
    Lactoferrin (17-41) (acetate)

    Lactoferricin B acetate; Lfcin B acetate

    Bacterial Fungal Apoptosis Cancer Infection
    Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities.
  • HY-136092
    Androsta-1,4,6-triene-3,17-dione

    Aromatase Endocrinology Neurological Disease
    Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.
  • HY-P1757
    HIV p17 Gag (77-85)

    HIV Infection
    HIV p17 Gag (77-85) is an HLA-A*0201(A2)-restricted CTL epitope, used in the research of anti-HIV.
  • HY-W022240
    NH2-PEG5-C2-NH-Boc

    PROTAC Linker 17

    PROTAC Linker Cancer
    NH2-PEG5-C2-NH-Boc (PROTAC Linker 17) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-113463
    CE(20:5(5Z,8Z,11Z,14Z,17Z)

    Endogenous Metabolite Metabolic Disease
    CE(20:5(5Z,8Z,11Z,14Z,17Z) is an endogenous metabolite.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-103394
    TC HSD 21

    Others Cancer
    TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
  • HY-114464
    11-Beta-hydroxyandrostenedione

    4-Androsten-11β-ol-3,17-dione

    Endogenous Metabolite Endocrinology
    11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-70013
    Abiraterone

    CB-7598

    Cytochrome P450 Cancer
    Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
  • HY-G0018
    Norgestimate metabolite Norelgestromin

    17-Deacetyl norgestimate; 17-Deacylnorgestimate

    Drug Metabolite Others
    Norelgestromin is a metabolite of Norgestimate, which is a progestin or synthetic progestogen.
  • HY-12883B
    PF 05089771 tosylate

    Sodium Channel Neurological Disease
    PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-12883
    PF 05089771

    Sodium Channel Neurological Disease
    PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
  • HY-13985
    Nav1.7 inhibitor

    Sodium Channel Neurological Disease
    Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-130243
    RORγt Inverse agonist 6

    ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the treatment of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
  • HY-101871
    Trehalose 6-behenate

    Others Inflammation/Immunology
    Trehalose 6-behenate is a Th1/Th17 skewing vaccine adjuvant.
  • HY-18173
    AZD8329

    Others Metabolic Disease
    AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
  • HY-19958
    XEN907

    Sodium Channel Neurological Disease
    XEN907 is a novel spirooxindole NaV1.7 blocker, inhibits hNaV1.7 with IC50 of 3 nM.
  • HY-19366
    Nav1.7-IN-2

    Sodium Channel Neurological Disease
    Nav1.7-IN-2 is an inhibitor of voltage-gated sodium channels (Nav), in particular Nav 1.7, with IC50 of 80 nM.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-103623
    PF-05241328

    Sodium Channel Neurological Disease
    PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.
  • HY-119934
    NaV1.7 inhibitor-1

    Sodium Channel Neurological Disease
    NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC50 of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-B1643
    Ethyl Vanillate

    Fungal Infection
    Ethyl Vanillate is a fungicidal agent. Ethyl Vanillate inhibits 17β-HSD2 with an IC50 1.3 µM.
  • HY-128353
    ROR agonist-1

    ROR Inflammation/Immunology
    ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5.
  • HY-100727
    AM-2099

    Sodium Channel Neurological Disease
    AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.
  • HY-17461A
    Cortisone acetate

    Cortisone 21-acetate

    Glucocorticoid Receptor Endogenous Metabolite Apoptosis Cancer Endocrinology
    Cortisone acetate (17-hydroxy-11-dehydrocorticosterone), a 21-carbon steroid hormone, is one of the main hormones released by the adrenal gland in response to stress.
  • HY-U00190
    Deprodone propionate

    RD20000

    Others Inflammation/Immunology
    Deprodone propionate (RD20000) is a corticosteroid which is obtained by esterifying with propionic acid the 17-position of the prednisolone skeleton and deoxidating its 21-position.
  • HY-P1319
    Nociceptin(1-7)

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
  • HY-B0141
    Estradiol

    β-Estradiol; E2; 17β-Estradiol; 17β-Oestradiol

    Estrogen Receptor/ERR Endogenous Metabolite Endocrinology Cancer
    Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.
  • HY-131182
    DS-1971a

    Sodium Channel Neurological Disease
    DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
  • HY-P1319A
    Nociceptin(1-7) TFA

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
  • HY-126252
    A-9758

    ROR Interleukin Related Inflammation/Immunology
    A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
  • HY-15898
    Y-320

    Interleukin Related Inflammation/Immunology
    Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits IL-17 production by CD4 T cells stimulated with IL-15 with IC50 values of 20 to 60 nM.
  • HY-14908
    Vidofludimus

    4sc-101; SC12267

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Interleukin Related Inflammation/Immunology
    Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.
  • HY-W018392
    Phthalic acid mono-2-ethylhexyl ester

    MEHP

    Endogenous Metabolite Metabolic Disease
    Phthalic acid mono-2-ethylhexyl ester (MEHP) is a major bioactive metabolite of diethylhexyl phthalate (DEHP), which inhibits the 17, 20 lyase activity of CYP17.
  • HY-108425B
    (Rac)-AMG8379

    (Rac)-AMG8380

    Sodium Channel Neurological Disease
    (Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .
  • HY-102998
    Nav1.7-IN-6

    Sodium Channel Neurological Disease
    Nav1.7-IN-6 (example 346) is a Nav1.7 selective inhibitor, which is extracted from patent WO2015078374A1.
  • HY-N0102
    Isoliquiritigenin

    GU17; ISL; Isoliquiritigen

    Aldose Reductase Influenza Virus Autophagy Apoptosis Cancer Infection Inflammation/Immunology
    Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC50 of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC50 of 24.7 μM.
  • HY-101789
    Nav1.7-IN-3

    Sodium Channel Neurological Disease
    Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration.
  • 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-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-103637
    Vimirogant

    VTP-43742

    ROR Inflammation/Immunology
    Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.
  • HY-103637A
    Vimirogant hydrochloride

    VTP-43742 hydrochloride

    ROR Inflammation/Immunology
    Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
  • HY-12811
    PF-04856264

    Sodium Channel Neurological Disease
    PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect.
  • HY-P1586
    HIV-1 Rev 34-50

    HIV-1 rev Protein (34-50)

    HIV Infection
    HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
  • HY-P1485
    Substance P(1-7)

    Neurokinin Receptor Neurological Disease Endocrinology
    Substance P(1-7) is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
  • HY-50759
    Ispinesib

    SB-715992

    Kinesin Apoptosis Cancer
    Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.
  • HY-119366
    S18-000003

    ROR Inflammation/Immunology
    S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production.
  • HY-P1485A
    Substance P(1-7) TFA

    Neurokinin Receptor Neurological Disease Endocrinology
    Substance P(1-7) TFA is a fragment of the neuropeptide, substance P (SP). Substance P(1-7) TFA gives depressor and bradycardic effects when applied to the nucleus tractus solitarius.
  • HY-135619
    DHODH-IN-4

    Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis Infection Inflammation/Immunology
    DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC50 values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity.
  • HY-18075
    LPA2 antagonist 1

    LPL Receptor Cancer
    LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
  • HY-18099A
    S1RA hydrochloride

    E-52862 hydrochloride

    Sigma Receptor Neurological Disease
    S1RA hydrochloride (E-52862 hydrochloride) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
  • HY-12033
    2-Methoxyestradiol

    2-ME2; NSC-659853

    Apoptosis Microtubule/Tubulin 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.
  • HY-128573
    RORγt Inverse agonist 3

    ROR Neurological Disease
    RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively.
  • HY-108425
    AMG8379

    Sodium Channel Neurological Disease
    AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM.
  • HY-16723
    Funapide

    TV 45070; XEN402

    Sodium Channel Inflammation/Immunology
    Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
  • HY-13571
    Betamethasone dipropionate

    Betamethasone 17,21-dipropionate

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology Cancer
    Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities.
  • HY-B0469
    Medroxyprogesterone acetate

    Medroxyprogesterone 17-acetate; MPA

    Progesterone Receptor Androgen Receptor Glucocorticoid Receptor Endogenous Metabolite Endocrinology Cancer
    Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-18099
    S1RA

    E-52862

    Sigma Receptor Neurological Disease
    S1RA(E-52862) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).
  • HY-12426
    mAChR-IN-1

    mAChR Neurological Disease
    mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
  • HY-112279
    GNE-131

    Sodium Channel Neurological Disease
    GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
  • HY-100291
    SX-3228

    GABA Receptor Neurological Disease
    SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.
  • HY-P1228
    HAEGTFT

    Glucagon Receptor Metabolic Disease
    HAEGTFT is the first N-terminal 1-7 residues of GLP-1 peptide.
  • HY-P1293
    Conantokin G

    iGluR Neurological Disease
    Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
  • HY-15826
    SGC-CBP30

    Epigenetic Reader Domain Histone Acetyltransferase Cancer Inflammation/Immunology
    SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-133128
    FM26

    ROR Cancer
    FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
  • 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-15778A
    AVE 0991 sodium salt

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM.
  • HY-P1593
    Mini Gastrin I, human

    Cholecystokinin Receptor Cancer Endocrinology
    Mini Gastrin I, human is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • HY-U00146
    FR-188582

    COX Inflammation/Immunology
    FR-188582 is a highly selective inhibitor of cyclooxygenase (COX)-2, with an IC50 value of 17 nM.
  • HY-12277
    AZ191

    DYRK Cancer
    AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
  • HY-U00076
    MK-0249

    Histamine Receptor Neurological Disease Endocrinology
    MK-0249 is a potent histamine H3 receptor antagonist, with Ki of 1.7 nM for human H3.
  • HY-P1293A
    Conantokin G TFA

    iGluR Neurological Disease
    Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties.
  • HY-12426A
    mAChR-IN-1 hydrochloride

    mAChR Neurological Disease
    mAChR-IN-1 hydrochloride is a potent muscarinic cholinergic receptor (mAChR) antagonist, with an IC50 of 17 nM.
  • HY-18620
    DZ2002

    Others Inflammation/Immunology
    DZ2002 is a potent and reversible S-Adenosyl-L-homocysteine Hydrolase(SAHH; AdoHcy Hydrolase) inhibitor with Ki of 17.9 nM.
  • HY-P1593A
    Mini Gastrin I, human TFA

    Cholecystokinin Receptor Cancer Endocrinology
    Mini Gastrin I, human (TFA) is a shorter version of human gastrin, consists of amino acids 5-17 of the parent peptide.
  • HY-101601
    Bamirastine

    TAK-427

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
  • HY-18162
    JNJ-42153605

    mGluR Neurological Disease
    JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-17461
    Cortisone

    17-Hydroxy-11-dehydrocorticosterone; Kendall's compound E

    Glucocorticoid Receptor Endogenous Metabolite Inflammation/Immunology Endocrinology
    Cortisone is a 21-carbon steroid hormone.
  • HY-120689
    PF-04745637

    TRP Channel Inflammation/Immunology
    PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1.
  • HY-12796A
    Raxatrigine hydrochloride

    GSK-1014802 hydrochloride; CNV1014802 (hydrochloride)

    Sodium Channel Neurological Disease
    Raxatrigine hydrochloride (GSK-1014802 hydrochloride) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  • HY-109020
    Acrizanib

    VEGFR Others
    Acrizanib is a VEGFR-2 inhibitor, with an IC50 of 17.4 nM for BaF3-KDR.
  • HY-12796
    Raxatrigine

    GSK-1014802; CNV1014802

    Sodium Channel Neurological Disease
    Raxatrigine (GSK-1014802) is a novel small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor.
  • HY-B1853
    Simetryn

    Others Others
    Simetryn is a herbicide with the LC50 of 16.9-3.70 mg/L (79.3-17.4 microM.
  • HY-15536
    Cebranopadol

    GRT6005

    Opioid Receptor Neurological Disease
    Cebranopadol is an analgesic NOP and opioid receptor agonist with Kis/EC50s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.
  • HY-12059A
    AT7867 dihydrochloride

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-133552
    RORγt Inverse agonist 10

    ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
  • HY-P1221
    ProTx II

    Sodium Channel Neurological Disease
    ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors.
  • HY-12059
    AT7867

    Akt PKA Ribosomal S6 Kinase (RSK) Cancer
    AT7867 is a potent ATP-competitive inhibitor of Akt1/Akt2/Akt3 and p70S6K/PKA with IC50s of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively.
  • HY-135880A
    OMDM-4

    Endogenous Metabolite Neurological Disease
    OMDM-4 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki 17.7 μM.
  • HY-P0216
    A 779

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
  • HY-16904
    RI-2

    RAD51 Cancer
    RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
  • HY-15778
    AVE 0991

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    AVE 0991 is a nonpeptide and orally active angiotensin-(1-7) receptor agonist with an IC50 of 21 nM.
  • HY-13510
    Cutamesine dihydrochloride

    SA4503 dihydrochloride; AGY94806 dihydrochloride

    Sigma Receptor Neurological Disease
    Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a potent Sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes.
  • HY-12747
    DC_517

    DNA Methyltransferase Cancer
    DC_517 is a DNA methyltransferase 1 (DNMT1) inhibitor, with an IC50 and a Kd of 1.7 μM and 0.91 μM, respectively.
  • HY-50295
    CI-1040

    PD 184352

    MEK Apoptosis Cancer
    CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-75054
    Abiraterone acetate

    CB7630

    Cytochrome P450 Cancer
    Abiraterone acetate is an oral, potent, selective, and irreversible inhibitor of CYP17A1 with antiandrogen activity. Abiraterone acetate is a prodrug form of Abiraterone (CB7598).
  • HY-101921
    PI3Kδ-IN-1

    PI3K Inflammation/Immunology
    PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
  • HY-111463
    CDK8-IN-3

    CDK Cancer Metabolic Disease Inflammation/Immunology
    CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.
  • HY-136527
    BMS-986251

    ROR Interleukin Related Inflammation/Immunology
    BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-125079
    DSP-2230

    Sodium Channel Neurological Disease Cardiovascular Disease
    DSP-2230 is a selective Nav1.7/Nav1.8 blocker.
  • HY-70006
    Galeterone

    TOK-001; VN-124-1

    Cytochrome P450 Cancer
    Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
  • HY-17411
    Limonin

    Limonoic acid 3,19:16,17 dilactone

    HIV Apoptosis Endogenous Metabolite Infection Cancer
    Limonin is a triterpenoid enriched in citrus fruits, which has antivirus and antitumor ability.
  • HY-13295
    Vinpocetine

    Ethyl apovincaminate

    Sodium Channel IKK Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
    Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na + channels. The IC50 value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.
  • HY-N2284
    Sophoflavescenol

    AChE Beta-secretase Phosphodiesterase (PDE) Cancer
    Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
  • HY-111359
    GPR40 agonist 1

    GPR40 Metabolic Disease
    GPR40 agonist 1 is a potent and novel GPR40 full agonist with an EC50 of 2 nM and 17 nM for hGPR40 and rGPR40, respectively.
  • HY-119937
    ROCK inhibitor-2

    ROCK Inflammation/Immunology Cardiovascular Disease
    ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC50s of 17 nM and 2 nM, respectively.
  • HY-111421
    ODM-204

    Androgen Receptor Cytochrome P450 Cancer
    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
  • HY-101619
    Abaperidone

    Dopamine Receptor 5-HT Receptor Neurological Disease
    Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
  • HY-140323
    Tetraethyl heptane-1,7-diylbis(phosphonate)

    PROTAC Linker Cancer
    Tetraethyl heptane-1,7-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-U00431
    CCG 203769

    RGS Protein Neurological Disease
    CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
  • HY-19770
    GSK2981278

    ROR Inflammation/Immunology
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
  • HY-106266
    Chiglitazar

    PPAR Metabolic Disease
    Chiglitazar is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.
  • HY-18960
    CHZ868

    JAK Cancer
    CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
  • HY-13245
    PF-4136309

    INCB8761

    CCR Inflammation/Immunology Endocrinology
    PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
  • HY-13243
    Alvimopan

    ADL 8-2698; LY 246736

    Opioid Receptor Metabolic Disease
    Alvimopan(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  • HY-15277
    AM966

    LPL Receptor Inflammation/Immunology
    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).
  • HY-100155
    4-IBP

    Sigma Receptor Cancer
    4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
  • HY-76657A
    Alvimopan dihydrate

    ADL 8-2698 dihydrate; LY 246736 dihydrate

    Opioid Receptor Neurological Disease
    Alvimopan dihydrate (ADL 8-2698 dihydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  • HY-76657
    Alvimopan monohydrate

    ADL 8-2698 monohydrate; LY 246736 monohydrate

    Opioid Receptor Neurological Disease
    Alvimopan monohydrate (ADL 8-2698 monohydrate) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  • HY-111271A
    L 888607 Racemate

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    L 888607 Racemate is a selective prostaglandin D2 receptor subtype 1 (DP1) antagonist, with Kis of 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively.
  • HY-B1100
    Estradiol (cypionate)

    Estrogen Receptor/ERR Endocrinology Cancer
    Estradiol cypionate is a 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor IC50 value: Target: estrogen receptor Estradiol cypionate is a synthetic ester, is a estrogen.
  • HY-112433
    NIK SMI1

    NF-κB Inflammation/Immunology
    NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM.
  • HY-124625
    BI-4464

    FAK Ligand for Target Protein for PROTAC Cancer
    BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-B1618
    Corticosterone

    17-Deoxycortisol; 11β,21-Dihydroxyprogesterone; Kendall's compound B

    Glucocorticoid Receptor Endogenous Metabolite Neurological Disease Endocrinology
    Corticosterone is an adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid.
  • HY-N0933
    Androsterone

    5α-Androstan-3α-ol-17-one

    FXR Endogenous Metabolite Autophagy Metabolic Disease Neurological Disease
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • HY-B0648
    Medroxyprogesterone

    17α-Hydroxy-6α-methylprogesterone; U8840

    Progesterone Receptor Endocrinology
    Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
  • HY-120323
    DRI-C21045

    TNF Receptor Inflammation/Immunology
    DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
  • HY-107390A
    AX-024 hydrochloride

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-107390
    AX-024

    TNF Receptor Interleukin Related IFNAR Inflammation/Immunology
    AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
  • HY-N5006
    Guanfu base G

    Potassium Channel Cardiovascular Disease
    Guanfu base G is an antiarrhythmic alkaloid isolated from Aconitum coreanum. Guanfu base G inhibits HERG channel current with an IC50 of 17.9 μM.
  • HY-10497
    BMS-794833

    c-Met/HGFR VEGFR Cancer
    BMS-794833 is a VEGFR2 and Met inhibitor extracted from patent WO2009094417, compound example 1; has IC50s of 15 and 1.7 nM, respectively.
  • HY-103687
    Abiraterone metabolite 1

    3β-OH-5α-Abi

    Drug Metabolite Cancer
    Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
  • HY-N2279
    Kurarinone

    Others Inflammation/Immunology
    Kurarinone, a flavanoid derived from shrub Sophora flavescens, inhibits the process of experimental autoimmune encephalomyelitis via blocking Th1 and Th17 cell differentiation.
  • HY-111513
    4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine

    Amyloid-β Neurological Disease
    4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.
  • HY-10074
    TPCA-1

    IKK STAT Apoptosis Inflammation/Immunology Cancer
    TPCA-1 is a potent and selective inhibitor of IKK-2 with IC50 of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.
  • HY-103310
    MRS1845

    Calcium Channel CRAC Channel Cardiovascular Disease
    MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC50 of 1.7 μM. MRS1845 is an ORAI1 inhibitor.
  • HY-15797
    UNC2250

    TAM Receptor Cancer
    UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
  • HY-101454
    SR0987

    ROR Cancer Inflammation/Immunology
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.
  • HY-100208
    HC-067047

    TRP Channel Cancer
    HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively.
  • HY-W017829
    1,7-Bis-Boc-1,4,7-triazaheptane

    PROTAC Linker Cancer
    1,7-Bis-Boc-1,4,7-triazaheptane is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-101533
    AZD-5991

    Bcl-2 Family Cancer
    AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay.
  • HY-12776
    GSK805

    ROR Inflammation/Immunology
    GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
  • HY-13638
    GDC-0152

    IAP Cancer
    GDC-0152 is a potent IAPs inhibitor, and binds to the BIR3 domains of XIAP, cIAP1, cIAP2 and the BIR domain of ML-IAP with Ki values of 28 nM, 17 nM, 43 nM and 14 nM, respectively.
  • HY-15996B
    Seviteronel racemate

    VT-464 (racemate)

    Cytochrome P450 Cancer
    Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
  • HY-N6691
    Veratridine

    3-Veratroylveracevine

    Sodium Channel Neurological Disease
    Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM.
  • HY-124653
    HSP27 inhibitor J2

    J2

    HSP Cancer
    HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
  • HY-P1220
    Huwentoxin-IV

    Sodium Channel Neurological Disease
    Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-136301
    Acid secretion-IN-1

    Others Inflammation/Immunology
    Acid secretion-IN-1 is a polycyclic compound extracted from patent WO2018024188A1, Compound Example 17.4. Acid secretion-IN-1 is synthesized and used in the IDO inhibitor synthetic experiment.
  • HY-14470
    Sibutramine hydrochloride monohydrate

    BTS 54-524 hydrochloride monohydrate

    Serotonin Transporter Potassium Channel Metabolic Disease Neurological Disease
    Sibutramine hydrochloride monohydrate is a novel 5-HT (serotonin) and noradrenaline reuptake inhibitor (SNRI). The IC50 for Sibutramine block of voltage-gated K + channel (KV)4.3 is 17.3 μM.
  • HY-100655
    O-Desmethyl apixaban

    Drug Metabolite Cardiovascular Disease
    O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01). Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
  • HY-14111
    GSK189254A

    GSK189254

    Histamine Receptor Neurological Disease Endocrinology
    GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
  • HY-129111
    EACC

    Autophagy Infection Neurological Disease
    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  • HY-10805A
    Almorexant hydrochloride

    ACT-078573 hydrochloride

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Almorexant hydrochloride (ACT 078573 hydrochloride) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
  • HY-129749
    IDO-IN-13

    Indoleamine 2,3-Dioxygenase (IDO) Inflammation/Immunology
    IDO-IN-13 is a potent indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an EC50 of 17 nM, extracted from patent WO2019040102A1, example 43.
  • HY-10805
    Almorexant

    ACT 078573

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Almorexant (ACT 078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM, respectively.
  • HY-16657
    TAPI-1

    MMP Cancer Inflammation/Immunology
    TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor.
  • HY-12883A
    PF-05198007

    Sodium Channel Neurological Disease
    PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.
  • HY-N0163
    Magnolol

    RAR/RXR PPAR Autophagy Bacterial Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
    Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 µM and 17.7 µM, respectively.
  • HY-125872
    KRAS G12C inhibitor 14

    Ras Cancer
    KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC50 of 18 nM.
  • HY-135128
    Dot1L-IN-5

    Histone Methyltransferase Cancer
    Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 SPA DOT1L of 0.17 nM.
  • HY-15790
    Elobixibat

    A 3309; AZD 7806

    Others Metabolic Disease
    Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
  • HY-123230
    Trifloxystrobin

    CGA 279202

    Fungal Infection
    Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
  • HY-126290
    Tyk2-IN-8

    JAK Inflammation/Immunology
    Tyk2-IN-8 (compound 10) is a selective TYK2 inhibitor, which binds to TYK2 catalytically active JH1 domain with an IC50 of 17 nM, used in the treatment of psoriasis.
  • HY-128128
    ASN04421891

    Others Neurological Disease
    ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
  • HY-120086
    RO-5963

    MDM-2/p53 E1/E2/E3 Enzyme Cancer
    RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.
  • HY-P1220A
    Huwentoxin-IV TFA

    Sodium Channel Neurological Disease
    Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain.
  • HY-16780
    Gemilukast

    ONO-6950

    Leukotriene Receptor Inflammation/Immunology
    Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.
  • HY-19369
    L-685458

    L-685,458

    γ-secretase Apoptosis Neurological Disease Cancer
    L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.
  • HY-15529
    S0859

    Na+/HCO3- Cotransporter Cardiovascular Disease
    S0859 is a selective, high-affinity generic NBC inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
  • HY-10873
    N-Desethyl Sunitinib

    SU-11662

    Others Cancer
    N-Desethyl Sunitinib is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
  • HY-14649
    Retinoic acid

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM.
  • HY-125801
    3-Oxo-5β-cholanoic acid

    Dehydrolithocholic acid; 3-oxoLCA

    ROR Inflammation/Immunology
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
  • HY-11079
    A-803467

    Sodium Channel Neurological Disease
    A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
  • HY-128339
    Autogramin-1

    Autophagy Cancer
    Autogramin-1 potently inhibits autophagy induced by either starvation (IC50=0.17 μM) or mTORC1 inhibition (Rapamycin; IC50=0.44 μM).
  • HY-110000
    (+)-PD 128907 hydrochloride

    Dopamine Receptor Neurological Disease
    (+)-PD 128907 hydrochloride is a selective dopamine D2/D3 receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3 receptors, 179, 770 n M for human and rat D3 receptors, respectively.
  • HY-N7501
    Isoformononetin

    Others Metabolic Disease Inflammation/Immunology
    Isoformononetin is an analog of Daidzein (HY-N0019) and has immunoprotective effects. Isoformononetin inhibits the differentiation of Th17 and B-cells lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions.
  • HY-N2187
    Deoxyshikonin

    Bacterial HIF/HIF Prolyl-Hydroxylase Cancer Infection Cardiovascular Disease
    Deoxyshikonin is isolated from Lithospermum erythrorhizon Sieb with antitumor activity. Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF, indicates a prolymphangiogenesis as well as a proangiogenesis effect in vitro. Deoxyshikonin shows significant synergic antimicrobial activity against S. pneumonia (MIC=17 μg/mL), also shows significantly inhibitory activities against MRSA.
  • HY-10505
    Orteronel

    TAK-700

    Others Cancer
    Orteronel is a highly selective inhibitor of human 17,20-lyase with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.
  • HY-50667S
    Apixaban 13CD3

    BMS-562247-01 13CD3

    Factor Xa Cardiovascular Disease
    Apixaban 13CD3 (BMS-562247-01 13CD3) is a deuterium labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
  • HY-120530
    JNJ-46281222

    mGluR Neurological Disease
    JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).
  • HY-114405
    SJFδ

    PROTAC p38 MAPK Autophagy Cancer
    SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ.
  • HY-50667
    Apixaban

    BMS-562247-01

    Factor Xa Cardiovascular Disease
    Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively. Apixaban is in development for the prevention and treatment of various thromboembolic diseases.
  • HY-125012
    MAP4K4-IN-3

    MAP4K Metabolic Disease
    MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent.
  • HY-19327
    ACY-738

    HDAC Cancer
    ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50 of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
  • HY-N4291
    1,7-Dihydroxy-2,3-methylenedioxyxanthone

    Others Neurological Disease
    1,7-Dihydroxy-2,3-methylenedioxyxanthone is isolated from Polygala cyparissias which is a small herb found in Brazil, Argentina and Uruguay. Polygala cyparissias are used in folk medicine as an anaesthetic.
  • HY-126291
    GNE-616

    Sodium Channel Neurological Disease
    GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.
  • HY-P1324A
    [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA

    Neuropeptide Y Receptor Neurological Disease
    [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
  • HY-P1324
    [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide

    Neuropeptide Y Receptor Neurological Disease
    [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
  • HY-15996A
    Seviteronel R enantiomer

    VT-464 (R enantiomer)

    Others Cancer
    Seviteronel R enantiomer (VT-464 R enantiomer) is the R enantiomer of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM); Seviteronel (VT-464) R enantiomer's activity is unknown.
  • HY-16172
    DMAPT

    Dimethylamino Parthenolide

    NF-κB Cancer
    DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
  • HY-19316
    NU2058

    O6-(Cyclohexylmethyl)guanine

    CDK Cancer
    NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
  • HY-B0469S
    Medroxyprogesterone acetate D3

    Medroxyprogesterone 17-acetate D3; MPA D3

    Progesterone Receptor Androgen Receptor Glucocorticoid Receptor Cancer Endocrinology
    Medroxyprogesterone acetate D3 is deuterium labeled Medroxyprogesterone acetate. Medroxyprogesterone acetate is a widely used synthetic steroid by its interaction with progesterone, androgen and glucocorticoid receptors.
  • HY-117959
    TAK-615

    LPL Receptor Inflammation/Immunology
    TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
  • 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-130614
    PROTAC EED degrader-1

    PROTAC Histone Methyltransferase Cancer
    PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
  • HY-109619
    D4-abiraterone

    Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite

    Androgen Receptor Cytochrome P450 Cancer
    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  • HY-15996
    Seviteronel

    VT-464

    Cytochrome P450 Cancer
    Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
  • HY-112416
    AZD4320

    Bcl-2 Family Cancer
    AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
  • HY-N2185
    (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one

    Others Inflammation/Immunology
    (5R,6E)-5-Hydroxy-1,7-diphenyl-6-hepten-3-one is the methylene chloride extract of Alpinia nutans, has antioxidant activity.
  • HY-108015
    RO5263397

    Others Neurological Disease
    RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect.
  • HY-18947
    SKLB-23bb

    HDAC Cancer
    SKLB-23bb is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.
  • HY-128579
    DW14800

    Histone Methyltransferase Cancer
    DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
  • HY-101980
    AZD4635

    HTL1071

    Adenosine Receptor Cancer
    AZD4635 (HTL1071) is a potent, selective and orally active adenosine A2A receptor (A2AR) antagonist. AZD4635 binds to human A2AR with a Ki of 1.7 nM and shows >30-fold selectivity over other adenosine receptors.
  • HY-B0683
    Limaprost

    17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206

    PGE synthase Inflammation/Immunology Cardiovascular Disease
    Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.
  • HY-114300
    DSP-0565

    Others Neurological Disease
    DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic drug (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin.
  • HY-N1454
    Apigenin-7-glucuronide

    Apigenin 7-O-glucuronide

    MMP Cancer
    Apigenin-7-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 12.87, 22.39, 17.52, 0.27 μM for MMP-3, MMP-8, MMP-9, MMP-13, respectively.
  • HY-112708
    PF-06700841

    JAK Inflammation/Immunology
    PF-06700841 is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
  • HY-100653A
    AZD5153 6-Hydroxy-2-naphthoic acid

    AZD-5153 HNT salt

    Epigenetic Reader Domain Cancer
    AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-118916
    FTI-2148

    Farnesyl Transferase Cancer
    FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-136531
    XMU-MP-3

    Btk Apoptosis Cancer
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis.
  • HY-100986
    L-NIO dihydrochloride

    NO Synthase Cardiovascular Disease
    L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively. L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats.
  • HY-135871
    BMT-124110

    Others Neurological Disease
    BMT-124110 is a potent, selective AAK1 inhibitor with an IC50 of 0.9 nM. BMT-124110 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 17 and 99 nM, respectively.
  • HY-112708A
    PF-06700841 P-Tosylate

    JAK Inflammation/Immunology
    PF-06700841 P-Tosylate is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 P-Tosylate also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
  • HY-10410
    TG101209

    FLT3 JAK RET Autophagy Apoptosis Cancer
    TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
  • HY-118916A
    FTI-2148 diTFA

    Farnesyl Transferase Cancer
    FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
  • HY-N2435
    [8]-Shogaol

    COX Apoptosis Cancer
    [8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.
  • HY-135199
    Ubiquitination-IN-1

    E1/E2/E3 Enzyme Cancer
    Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
  • HY-140188
    Amino-PEG6-amido-C16-COOH

    17-(Amino-PEG6-ethylcarbamoyl)heptadecanoic acid

    PROTAC Linker Cancer
    Amino-PEG6-amido-C16-COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N0646
    Silydianin

    Phosphatase Cancer
    Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.
  • HY-14813
    Cutamesine

    SA4503; AGY 94806

    Sigma Receptor Neurological Disease
    Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
  • HY-129910
    FABP5-IN-1

    FABP Inflammation/Immunology
    FABP5-IN-1(Compounds 4j) is a selective and high affinity fatty acid binding protein 5 (FABP5) inhibitor with a Ki value of 1.7 μM, and does not bind to both FABP3 and FABP7. FABP5-IN-1 shows potent antinociceptive effects.
  • HY-128587
    SY-1365

    CDK Cancer
    SY-1365 is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. SY-1365 exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. SY-1365 possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
  • HY-19638A
    Cangrelor tetrasodium

    P2Y Receptor Inflammation/Immunology Cardiovascular Disease
    Cangrelor tetrasodium, an adenosine triphosphate analogue, is a reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor tetrasodium directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor tetrasodium is also a nonspecific GPR17 antagonist.
  • HY-112811
    PROTAC CDK9 degrader-2

    PROTAC CDK Cancer
    PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
  • HY-100675
    JTE-013

    LPL Receptor Apoptosis Cancer
    JTE-013 is a potent and specific S1P2 (Sphingosine-1-Phosphate 2; EDG-5) antagonist. JTE-013 inhibits the specific binding of radiolabeled S1P to human and rat S1P2 with IC50s of 17 nM and 22 nM, respectively.
  • HY-19928A
    Vactosertib Hydrochloride

    EW-7197 Hydrochloride; TEW-7197 Hydrochloride

    TGF-β Receptor Cancer
    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect.
  • HY-101698
    Alniditan

    Alnitidan

    5-HT Receptor Neurological Disease
    Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
  • HY-N0501
    11-oxo-mogroside V

    Reactive Oxygen Species Metabolic Disease
    11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2 -, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
  • HY-19928
    Vactosertib

    EW-7197; TEW-7197

    TGF-β Receptor Cancer
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect.
  • HY-N1463
    Luteolin 7-O-glucuronide

    Luteolin 7-glucuronide

    MMP Others
    Luteolin 7-O-glucuronide could inhibit Matrix Metalloproteinases (MMP) activities, with IC50s of 17.63, 7.99, 11.42, 12.85, 0.03 μM for MMP-1, MMP-3, MMP-8, MMP-9, MMP-13, respectively.
  • HY-108425A
    AMG8380

    Sodium Channel Neurological Disease
    AMG8380, an orally active and less active enantiomer of AMG8379, can serves as a negative control. AMG8380 inhibits human and mouse voltage-gated sodium channel NaV1.7 with IC50s of 0.907 and 0.387 μM, respectively. AMG8380 blocks Tetrodotoxin (TTX)-sensitive native channels with an IC50 of 2560 nM.
  • HY-126679
    Apoptolidin

    ATP Synthase Apoptosis Cancer
    Apoptolidin is a polyketide isolated from Nocardiopsis bacteria. Apoptolidin is a selective mitochondrial F1FO ATPase inhibitor. Apoptolidin is an apoptosis inducer and induces apoptotic cell death in cells transformed with the adenovirus type 12 oncogenes including ElA (IC50=10-17 ng/ml) but not in normal cells.
  • HY-P2244A
    YAP-TEAD-IN-1 TFA

    YAP Cancer
    YAP-TEAD-IN-1 TFA is a potent and competitive peptide inhibitor of YAP-TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 TFA is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd= 40 nM).
  • HY-10656
    SB-657510

    Urotensin Receptor Inflammation/Immunology
    SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells.
  • HY-100637
    Hydroxybupropion

    Adrenergic Receptor nAChR Neurological Disease
    Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonis tis more potent than Bupropion .
  • HY-P2244
    YAP-TEAD-IN-1

    YAP Cancer
    YAP-TEAD-IN-1 is a potent and competitive inhibitor of YAP–TEAD interaction (IC50=25 nM). YAP-TEAD-IN-1 is a 17mer peptide and shows a higher the binding affinity to TEAD1 (Kd=15 nM) than YAP (50-171) (Kd=40 nM).
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • 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-130602
    MS432

    PROTAC MEK Cancer
    MS432 is a first-in-class and highly selective PD0325901-based VHL-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
  • HY-114641A
    BIIL-260 hydrochloride

    Leukotriene Receptor Inflammation/Immunology
    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM.
  • HY-103195
    NKY80

    Adenylate Cyclase Metabolic Disease
    NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues.
  • HY-111422
    PLX51107

    Epigenetic Reader Domain Cancer
    PLX51107 is a potent and selective BET inhibitor, with Kds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (Kd, in the 100 nM range).
  • HY-10559
    Nelotanserin

    APD125

    5-HT Receptor Cancer Neurological Disease
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
  • HY-N2572
    Nepetin

    6-Methoxyluteolin

    Others Inflammation/Immunology
    Nepetin (6-Methoxyluteolin) is a natural flavonoid isolated from Eupatorium ballotaefolium HBK with potent anti-inflammatory activities. Nepetin inhibits IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43 μM, 3.42 μM and 4.17 μM, respectively in ARPE-19 cells.
  • HY-133551
    WF-47-JS03

    RET Cancer
    WF-47-JS03 is a potent RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, CCDC6-RET transfected LC-2/ad lung cancer cells, respectively.
  • HY-114237
    GDC-0276

    Sodium Channel Neurological Disease
    GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.
  • HY-10202A
    Tandutinib hydrochloride

    MLN518 hydrochloride; CT53518 hydrochloride

    FLT3 c-Kit PDGFR Apoptosis Cancer
    Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-P1726
    MSG606

    Melanocortin Receptor
    MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
  • HY-130246
    NF-56-EJ40

    Others Inflammation/Immunology
    NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.
  • HY-10202
    Tandutinib

    MLN518; CT53518

    FLT3 c-Kit PDGFR Apoptosis Cancer
    Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
  • HY-140791
    Azide-PEG9-amido-C16-Boc

    17-(Azide-PEG9-ethylcarbamoyl)heptadecanoic t-butyl ester

    PROTAC Linker Cancer
    Azide-PEG9-amido-C16-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140787
    Azide-PEG6-amido-C16-Boc

    17-(Azide-PEG6-ethylcarbamoyl)heptadecanoic t-butyl ester

    PROTAC Linker Cancer
    Azide-PEG6-amido-C16-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140201
    Amino-PEG6-amido-C16-Boc

    17-(Amino-PEG6-ethylcarbamoyl)heptadecanoic t-butyl ester

    PROTAC Linker Cancer
    Amino-PEG6-amido-C16-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-140202
    Amino-PEG9-amido-C16-Boc

    17-(Amino-PEG9-ethylcarbamoyl)heptadecanoic t-butyl ester

    PROTAC Linker Cancer
    Amino-PEG9-amido-C16-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-12995A
    (S)-BI 665915

    FLAP Inflammation/Immunology
    (S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
  • HY-75800
    Lomibuvir

    VX-222

    DNA/RNA Synthesis HCV Infection
    Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
  • HY-N6962
    α-Spinasterol

    TRP Channel COX Infection Neurological Disease
    α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
  • HY-106004
    Zamicastat

    BIA 5-1058

    Dopamine β-hydroxylase P-glycoprotein BCRP Cancer Cardiovascular Disease
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.
  • 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-114170
    ML604440

    Proteasome Inflammation/Immunology
    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
  • HY-128600
    ERD-308

    PROTAC Estrogen Receptor/ERR Cancer
    ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively).
  • HY-107422A
    PAT-1251 Hydrochloride

    Monoamine Oxidase Inflammation/Immunology
    PAT-1251 Hydrochloride is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 Hydrochloride is used in the research of fibrotic diseases.
  • HY-10200
    BMS-754807

    IGF-1R Insulin Receptor Cancer Endocrinology
    BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively.
  • HY-P1726A
    MSG606 TFA

    Melanocortin Receptor
    MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
  • HY-107422
    PAT-1251

    Monoamine Oxidase Inflammation/Immunology
    PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases.
  • HY-111875
    SNIPER(BRD)-1

    SNIPER Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively.
  • HY-107417
    Hypothemycin

    VEGFR MEK FLT3 PDGFR ERK Cancer
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
  • HY-124527
    HET0016

    Cytochrome P450 Cardiovascular Disease
    HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.
  • HY-N6732
    K-252a

    SF2370; Antibiotic K 252a; Antibiotic SF 2370

    PKC PKA CaMK Trk Receptor Autophagy Infection
    K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-N6953
    Garcinone D

    STAT Keap1-Nrf2 Reactive Oxygen Species Neurological Disease
    Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners.
  • HY-N2532
    Diphyllin

    HIV Proton Pump Influenza Virus Cancer Infection Inflammation/Immunology
    Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H +-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities.
  • HY-19974
    TAK-220

    CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
  • HY-128717A
    GSK3368715 dihydrochloride

    EPZ019997 dihydrochloride

    Histone Methyltransferase Cancer
    GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-13246
    Apitolisib

    GDC-0980; GNE 390; RG 7422

    PI3K mTOR Apoptosis Cancer
    Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a Ki of 17 nM for mTOR.
  • HY-18642
    CYP3cide

    PF-4981517

    Cytochrome P450 Others
    CYP3cide (PF-4981517) is a potent, selective and time-dependent inhibitor of cytochrome P4503A4 (CYP3A4). The IC50 values for Midazolam 1’-hydroxylase activity are 0.03 μM, 17 μM, and 71 μM for CYP3A4, CYP3A5, and CYP3A7, respectively. CYP3cide can be used to distinguish the contributions of CYP3A4 versus CYP3A5 on drug metabolism.
  • HY-128717
    GSK3368715

    EPZ019997

    Histone Methyltransferase Cancer
    GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
  • HY-N2348
    Tubulysin D

    Microtubule/Tubulin Cancer
    Tubulysin D is one of the most potent derivatives among the tubulysins isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin D is a novel tetrapeptide that displays potent antitumor activity and leads to cell cycle arrest and apoptosis by inhibiting tubulin polymerization with an IC50 of 1.7 μM. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range.
  • HY-123824
    GNE-0439

    Others Neurological Disease
    GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders.
  • HY-117482
    BPN-15606

    γ-secretase Neurological Disease
    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-100820
    Sarizotan

    EMD 128130

    5-HT Receptor Dopamine Receptor Neurological Disease
    Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
  • HY-100588
    VU0364770

    mGluR Neurological Disease
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • 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-112146
    MMG-11

    Toll-like Receptor (TLR) Inflammation/Immunology
    MMG-11 is a potent and selective human TLR2 antagonist with low cytotoxicity. MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with IC50s of 1.7 µM for Pam3CSK4-induced hTLR2/1 and 5.7 µM for Pam2CSK4-induced hTLR2/6 responses.
  • HY-117482A
    BPN-15606 besylate

    γ-secretase Neurological Disease
    BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
  • HY-100588A
    VU0364770 hydrochloride

    mGluR Neurological Disease
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively.
  • HY-106019C
    Liarozole dihydrochloride

    R75251 dihydrochloride

    Cytochrome P450 Cancer Inflammation/Immunology
    Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
  • HY-103286
    PD176252

    Bombesin Receptor Cancer
    PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
  • HY-15196
    TAK-285

    EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity. TAK-285 can cross the blood-brain barrier (BBB).
  • HY-101198
    Clobenpropit dihydrobromide

    Histamine Receptor Cancer Neurological Disease
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
  • HY-118607
    VU041

    Potassium Channel Infection
    VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.
  • HY-120000
    MS402

    Epigenetic Reader Domain Cancer Inflammation/Immunology
    MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice.
  • HY-114091
    PF-00356231 hydrochloride

    MMP Inflammation/Immunology
    PF-00356231 hydrochloride is a specific, non-peptidic, non-zinc chelating ligand and inhibitor of matrix metalloproteinase MMP-12 (IC50=1.4 μM). PF-00356231 hydrochloride binds to MMP-12 and forms PF-00356231/MMP-12 complex. PF-00356231 hydrochloride shows potency against MMP-13, MMP-8, MMP-9, MMP-3 with IC50s of 0.00065, 1.7, 0.98, 0.39 μM, respectively.
  • HY-12443
    PF-5006739

    Casein Kinase Neurological Disease
    PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid drug-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity.
  • HY-100839
    (RS)-(Tetrazol-5-yl)glycine

    D,L-(tetrazol-5-yl)glycine; LY 285265

    iGluR Neurological Disease
    (RS)-(Tetrazol-5-yl)glycine (D,L-(tetrazol-5-yl)glycine) is a highly potent and selective N-methyl-D-aspartate (NMDA) receptor agonist. (RS)-(Tetrazol-5-yl)glycine has EC50s of 99 nM, 1.7 μM for GluN1/GluN2D and GluN1/GluN2A, respectively. (RS)-(Tetrazol-5-yl)glycine induces seizure responses and Fos in mice.
  • 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-101995
    Ridaifen-B

    RID-B

    Estrogen Receptor/ERR Cannabinoid Receptor Cancer Metabolic Disease Inflammation/Immunology
    Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen derivative. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects.
  • HY-105285
    Piromelatine

    Neu-P11

    Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel Neurological Disease
    Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-N1992
    Theaflavin 3,3'-digallate

    TF3

    Akt NF-κB MEK ERK Cancer
    Theaflavin 3,3'-digallate (TF3), the typical pigment in black tea, is a good antitumor agent. Theaflavin 3,3'-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3'-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3'-digallate inhibits HCT116 cell growth with an IC50 of 17.26 μM.
  • HY-12379
    NS-2028

    Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.