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Results for "productlist/G" in MCE Product Catalog:

337

Inhibitors & Agonists

7

Screening Libraries

6

Dye Reagents

2

Biochemical Assay Reagents

46

Peptides

2

MCE Kits

2

Inhibitory Antibodies

84

Natural
Products

8

Recombinant Proteins

Cat. No. Product Name Target Research Area
  • HY-N7120
    Penicillin G Procaine

    PGP

    Bacterial Infection
    Penicillin G Procaine(PGP), a β-lactam antibiotic, is a crystalline complex produced by chemically combining penicillin G with procaine.
  • HY-102036
    G-744

    Btk Inflammation/Immunology
    G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.
  • HY-107216
    G-1

    Estrogen Receptor/ERR Cancer
    G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a Ki of 11 nM.
  • HY-103449
    G15

    Estrogen Receptor/ERR Cancer
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  • HY-124658
    G0507

    Bacterial Infection
    G0507, a pyrrolopyrimidinedione compound, is a potent LolCDE ABC Transporter inhibitor. G0507 is a inhibitor of Escherichia coli growth and induces the extracytoplasmic σE stress response. G0507 acts as a chemical probe to dissect lipoprotein trafficking in Gram-negative bacteria.
  • HY-N6698
    Aflatoxin G2

    Others Cancer
    Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-19635A
    G-5555 hydrochloride

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
  • HY-P1592
    G3-C12

    Galectin Cancer
    G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
  • HY-100996
    10074-G5

    c-Myc Autophagy Cancer
    10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
  • HY-N0855
    Alisol G

    Alisol-G; 25-Anhydroalisol A

    Others Others
    Alisol G is a natural product extracted from Rhizoma Alismatis.
  • HY-N2103
    Tenacissoside G

    Others Cancer
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
  • HY-19635
    G-5555

    PAK Cancer
    G-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
  • HY-N4216
    Saikosaponin G

    Others Others
    Saikosaponin G is a triterpene glycoside isolated from Bupleuri Radix.
  • HY-12438
    G007-LK

    PARP Cancer
    G007-LK is a potent and selective inhibitor of TNKS1 and TNKS2, with IC50s of 46 nM and 25 nM, respectively.
  • HY-128771
    K-Ras G12C-IN-4

    Ras Others
    K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C.
  • HY-116304
    1G244

    Dipeptidyl Peptidase Apoptosis Cancer
    1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
  • HY-18605
    K-Ras G12C-IN-2

    Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
  • HY-N0817
    Polyphyllin G

    Apoptosis Autophagy Bacterial Cancer Inflammation/Immunology
    Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs). Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy.
  • HY-125176
    G907

    Bacterial Infection
    G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC50 of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.
  • HY-N4247
    Kuwanon G

    Bombesin Receptor Bacterial Infection
    Kuwanon G is a flavonoid isolated from Morus alba, acts as a bombesin receptor antagonist, with potential antimicrobial activity.
  • HY-N2291
    Rebaudioside G

    Others Others
    Rebaudioside G is the minor constituent isolated from the leaves of Stevia rebaudiana Bertoni, used for sweeteners research.
  • HY-12588
    Thiamet G

    Autophagy Cancer
    Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA), which acts to remove O-GlcNAc from modified proteins, with Ki of 20 nM for human OGA.
  • HY-N2242
    Hosenkoside G

    Others Cancer
    Hosenkoside G, a baccharane glycoside isolated from the seeds of Impatiens Balsamina L., possesses anti-tumor activity.
  • HY-17561
    G-418 disulfate

    Geneticin sulfate; Antibiotic G-418 sulfate

    Bacterial Others
    G-418 (disulfate) is an aminoglycoside antibiotic similar in structure to gentamicin B1, which blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells.
  • 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-112197
    PKG drug G1

    Others Cardiovascular Disease
    PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
  • HY-18606
    K-Ras G12C-IN-3

    Ras Cancer
    K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
  • HY-P1592A
    G3-C12 TFA

    Galectin Cancer
    G3-C12 (TFA) is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity.
  • HY-18604
    K-Ras G12C-IN-1

    Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
  • HY-N7018
    20-Hydroxyganoderic Acid G

    Others Inflammation/Immunology
    20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
  • HY-N1231
    Sophoraflavanone G

    Kushenol F

    Apoptosis Cancer
    Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties.  Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.
  • HY-N6983
    Licoricesaponin G2

    Others Others
    Licoricesaponin G2 is a pentacyclic triterpenoid isolated from Glycyrrhiza aspera.
  • HY-N2458
    Ganoderic acid G

    Others Others
    Ganoderic acid G is a triterpene isolated from the surface part of gills of Ganoderma lucidum.
  • HY-12333
    G-749

    Apoptosis FLT3 Cancer
    G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.
  • HY-N7050
    Tubulysin G

    Microtubule/Tubulin Apoptosis Cancer
    Tubulysin G is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin G is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
  • HY-128583
    G150

    Others Inflammation/Immunology
    G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
  • HY-N0858
    Gomisin G

    HIV Infection
    Gomisin G is an ethanolic extract of the stems of Kadsura interior; exhibits potent anti-HIV activity with EC50 and therapeutic index (TI) values of 0.006 microgram/mL and 300, respectively.
  • HY-N3521
    Platycoside G1

    Deapi-platycoside E

    Others Others
    Platycoside G1, a natural product found in Platycodon grandiflorum, is a triterpenoid saponin. Platycoside G1 has potent antioxidant activities.
  • HY-B1463
    Penicillin G sodium salt

    Benzylpenicillin sodium salt

    Bacterial Infection
    Penicillin G sodium salt is a typical β-lactam antibiotic.
  • HY-19711
    STING agonist-1

    G10

    Virus Protease STING Infection
    STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
  • HY-17591
    Penicillin G potassium

    Benzylpenicillin potassium

    Bacterial Infection
    Penicillin G potassium is a fast-acting antibiotic; used to treat bacterial infections that affect the blood, heart, lungs, joints, and genital areas.
  • HY-N7139A
    Penicillin G benzathine

    Benzathine benzylpenicillin

    Bacterial Infection
    Penicillin G benzathine (Benzathine benzylpenicillin) is an antibiotic against many bacterial infections.
  • HY-123962
    G6PD activator AG1

    Others Others
    G6PD activator AG1 is a glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ, extracted from patent WO2019023264A1, compound AG1.
  • HY-112494
    KRas G12C inhibitor 4

    Ras Cancer
    KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-112491
    KRas G12C inhibitor 1

    Ras Cancer
    KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-112493
    KRas G12C inhibitor 3

    Ras Cancer
    KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-112492
    KRas G12C inhibitor 2

    Ras Cancer
    KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
  • HY-70003
    Carboxypeptidase G2 (CPG2) Inhibitor

    CPG2 Inhibitor

    Carboxypeptidase Cancer
    Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
  • HY-I0408
    Sofosbuvir impurity G

    HCV Infection
    Sofosbuvir impurity G, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
  • HY-130547
    BS2G Crosslinker disodium

    ADC Linker Cancer
    BS2G Crosslinker (disodium) is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-114168
    KRAS G12C inhibitor 5

    Ras Cancer
    KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.
  • HY-126292
    KRAS G12C inhibitor 13

    Ras Cancer
    KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
  • HY-18707
    K-Ras(G12C) inhibitor 12

    Apoptosis Ras Cancer
    K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.
  • HY-125873
    KRAS G12C inhibitor 15

    Ras Cancer
    KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 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-125874
    KRAS G12C inhibitor 16

    Ras Cancer
    KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM.
  • 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-N6697
    Aflatoxin G1

    Others Cancer
    Aflatoxin G1 is one type of aflatoxins occuring in nature. It is produced by molds, such as Aspergillus flavus and Aspergillus parasiticus. Aflatoxins are hepatogenic, teratogenic, imunosuppressive, and carcinogenic fungal metabolites found in feeds, nuts, wine-grapes, spices, and other grain crops.
  • HY-17431
    Fosamprenavir Calcium Salt

    GW433908G

    HIV Infection
    Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
  • HY-N2153
    Apigenin-7-O-(2G-rhamnosyl)gentiobioside

    Others Others
    Apigenin-7-O-(2G-rhamnosyl)gentiobioside is a flavone glycosides from Lonicera gracilipes var. glandulosa.
  • HY-112272
    Lerociclib

    G1T38

    CDK Cancer
    Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
  • HY-112272A
    Lerociclib dihydrochloride

    G1T38 dihydrochloride

    CDK Cancer
    Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.
  • HY-N6882
    Genistein 8-c-glucoside

    G8CG

    Mitochondrial Metabolism Apoptosis Cancer
    Genistein 8-c-glucoside (G8CG) is a natural glucoside isolated from flowers of Lupinus luteus L. Genistein 8-c-glucoside induces mitochondrial membrane depolarization and induces apoptosis.
  • HY-N2148
    Cytosporone B

    Csn-B; Dothiorelone G

    Others Cancer
    Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
  • HY-103007
    TC-G-1008

    GPR39-C3

    GHSR Metabolic Disease Endocrinology
    TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-B0089
    Acarbose

    BAY g 5421

    Others Metabolic Disease
    Acarbose is an inhibitor of alpha glucosidase, an anti-diabetic drug.
  • HY-44234A
    Fmoc-Gly-Gly-D-Phe-OtBu

    ADC Linker Cancer
    Fmoc-Gly-Gly-D-Phe-OtBu is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Fmoc-Gly-Gly-D-Phe-OtBu is the R-isomer of Fmoc-Gly-Gly-Phe-OtBu (HY-44234).
  • HY-N2298
    Camellianin A

    Apoptosis Cancer
    Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
  • HY-120897
    NS-3-008 hydrochloride

    Others Inflammation/Immunology
    NS-3-008 hydrochloride is an orally active transcriptional inhibitor of G0/G1 switch 2 (G0s2) with an IC50 of 2.25 μM. NS-3-008 hydrochloride can be used for chronic kidney disease.
  • HY-P1449
    Boc-Gly-Gly-Phe-Gly-OH

    GGFG

    ADC Linker Cancer
    Boc-Gly-Gly-Phe-Gly-OH, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
  • HY-P1449A
    Boc-Gly-Gly-Phe-Gly-OH TFA

    ADC Linker Cancer
    Boc-Gly-Gly-Phe-Gly-OH TFA, a self-assembly of N- and C-protected tetrapeptide, is a protease cleavable linker used for the antibody-drug conjugate (ADC).
  • HY-B0089A
    Acarbose sulfate

    Bay-g 5421 sulfate

    Others Metabolic Disease
    Acarbose sulfate is an inhibitor of alpha glucosidase, an anti-diabetic drug.
  • HY-N0711
    Carvacrol

    Notch Fungal Apoptosis Cancer Inflammation/Immunology
    Carvacrol is a monoterpenoid phenol isolated from Lamiaceae family plants, with antioxidant, anti-inflammatory and anticancer properties. Carvacrol causes cell cycle arrest in G0/G1, downregulates Notch-1, and Jagged-1, and induces apoptosis.
  • HY-133234
    BMVC-8C3O

    G-quadruplex Others
    BMVC-8C3O is a DNA G-quadruplexe (G4) ligand which can induce topological conversion of non-parallel to parallel forms in human telomeric DNA G4s.
  • HY-126688
    Mal-C2-Gly3-EDA-PNU-159682

    Drug-Linker Conjugates for ADC Cancer
    Mal-C2-Gly3-EDA-PNU-159682, a drug-linker conjugate for ADC, consists a cleavable ADC linker Mal-C2-Gly3-EDA and a potent ADC cytotoxin PNU-159682.
  • HY-P0295
    Gly-Arg-Gly-Asp-Ser

    Integrin Others
    Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
  • HY-126673
    Mal-C2-Gly3-EDA

    ADC Linker Cancer
    Mal-C2-Gly3-EDA is a cleavable ADC linker containing a Maleimide group. Mal-C2-Gly3-EDA is used for making antibody-drug conjugate.
  • HY-P0295A
    Gly-Arg-Gly-Asp-Ser (TFA)

    Integrin Others
    Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM.
  • HY-140309
    Gly-Gly-Gly-PEG4-DBCO

    ADC Linker Cancer
    Gly-Gly-Gly-PEG4-DBCO is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-141190
    Gly-Gly-Gly-PEG3-TCO

    ADC Linker Cancer
    Gly-Gly-Gly-PEG3-TCO is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-141284
    Gly-Gly-Gly-PEG4-methyltetrazine

    ADC Linker Cancer
    Gly-Gly-Gly-PEG4-methyltetrazine is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • HY-44234
    Fmoc-Gly-Gly-Phe-OtBu

    ADC Linker Cancer
    Fmoc-Gly-Gly-Phe-OtBu is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-P0073
    Tyr-Gly-Gly-Phe-Met-OH

    Met-Enkephalin; Methionine enkephalin

    Opioid Receptor Neurological Disease Cancer
    Tyr-Gly-Gly-Phe-Met-OH regulates human immune function and inhibits tumor growth via binding to the opioid receptor.
  • HY-44235
    MC-Gly-Gly-Phe

    ADC Linker Cancer
    MC-Gly-Gly-Phe is a cleavable linker used for antibody-drug conjugates (ADC).
  • HY-13627
    Estramustine phosphate sodium

    Microtubule/Tubulin Cancer
    Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
  • HY-135889
    CPFX2090

    Bacterial Infection
    CPFX2090 is a cephalosporin antibacterial compound extracted from patent WO2013052568A1, Compound Example 16g.
  • HY-15595
    360A

    G-quadruplex Telomerase Cancer
    360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
  • HY-13980
    UNC0642

    Histone Methyltransferase Cancer
    UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
  • HY-101467
    Trilaciclib

    G1T28

    CDK Cancer
    Trilaciclib is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
  • HY-B0918
    Chlorindione

    Chlophenadione; Indaliton; G-25766

    Others Cardiovascular Disease
    Chlophenadione is a potent anticoagulant compound.
  • HY-B0542
    Ouabain Octahydrate

    Acocantherine; G-Strophanthin

    Na+/K+ ATPase Autophagy Cardiovascular Disease Cancer
    Ouabain Octahydrate is an inhibitor of Na +/K +-ATPase, used for the treatment of congestive heart failure.
  • HY-15176
    Pyridostatin

    RR82

    G-quadruplex Cancer
    Pyridostatin is a G-quadruplexe stabilizer, with a Kd of 490 nM.
  • HY-15595A
    360A iodide

    360 A iodide

    G-quadruplex Telomerase Cancer
    360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
  • HY-135776
    BMVC2

    o-BMVC

    G-quadruplex Cancer
    BMVC2 (o-BMVC) is a bisubstitute carbazole derivative of BMVC. BMVC2 is a G-quadruplex (G4) stabilizer.
  • HY-100733
    4E2RCat

    Eukaryotic Initiation Factor (eIF) Virus Protease Autophagy Neurological Disease
    4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.
  • HY-135775
    BMVC

    G-quadruplex Telomerase DNA/RNA Synthesis Cancer
    BMVC is a potent G-quadruplex (G4) stabilizer and a selective telomerase inhibitor with an IC50 of ~0.2 μM. BMVC inhibits Taq DNA polymerase with an IC50 of ~2.5 μM. BMVC increases the melting temperature of G4 structure of telomere and accelerates telomere length shortening. Anticancer activities.
  • HY-15176A
    Pyridostatin hydrochloride

    RR82 hydrochloride

    G-quadruplex Cancer
    Pyridostatin hydrochloride (RR82 hydrochloride) is a G-quadruplexe stabilizer, with a Kd of 490 nM.
  • HY-101801
    Ac-Gly-BoroPro

    Others Cancer
    Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
  • HY-N6696
    Aflatoxin B2

    Others Cancer
    Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-17408
    Mevastatin

    Compactin; ML236B

    HMG-CoA Reductase (HMGCR) Apoptosis Autophagy Cancer Metabolic Disease Neurological Disease Cardiovascular Disease
    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.
  • HY-N6700
    Aflatoxin M2

    Others Cancer
    Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-N6791
    KT5823

    PKA PKC Apoptosis Others
    KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
  • HY-114277
    AMG-510

    Ras Cancer
    AMG-510 is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. AMG-510 irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. AMG-510 is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors.
  • HY-130616
    EGFR-IN-11

    EGFR Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
  • HY-N6699
    Aflatoxin M1

    Others Cancer
    Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
  • HY-114414
    HDACs/mTOR Inhibitor 1

    HDAC mTOR Apoptosis Cancer
    HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
  • HY-N1150
    Thymidine

    DThyd; NSC 21548

    DNA/RNA Synthesis Endogenous Metabolite Others
    Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
  • HY-13017
    Ivacaftor

    VX-770

    CFTR Autophagy Endocrinology
    Ivacaftor is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
  • HY-N2369
    Chelidonine

    Apoptosis Cancer Infection
    Chelidonine is an isoquinoline alkaloid isolated from Chelidonium majus L., causes G2/M arrest and induces caspase-dependent and caspase-independent apoptosis, with anticancer and antiviral activity.
  • HY-14403
    ERK5-IN-1

    ERK Cancer
    ERK5-IN-1 is a potent ERK5 inhibitor with an IC50 of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC50 of 26 nM.
  • HY-15594
    Phen-DC3

    DNA/RNA Synthesis Others
    Phen-DC3 is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
  • HY-15594A
    Phen-DC3 Trifluoromethanesulfonate

    Phen-DC3 Triflate

    G-quadruplex Cancer
    Phen-DC3 Trifluoromethanesulfonate is a G-quadruplex (G4) specific ligand which can inhibit FANCJ and DinG helicases with IC50s of 65±6 and 50±10 nM, respectively.
  • HY-112607
    Tubulin inhibitor 1

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
  • HY-135337
    Ethyl tosylcarbamate

    Potassium Channel Metabolic Disease
    Ethyl tosylcarbamate is an intermediate in the synthesis of Gliclazide (G409877). Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
  • HY-10222
    Ixabepilone

    Azaepothilone B; BMS 247550; BMS 247550-1

    Microtubule/Tubulin Apoptosis Cancer
    Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
  • HY-19831
    4EGI-1

    Eukaryotic Initiation Factor (eIF) Apoptosis Autophagy Cancer
    4EGI-1 is an inhibitor of eIF4E/eIF4G interaction, with a Kd of 25 μM against eIF4E binding.
  • HY-114146
    CID 1375606

    Others Metabolic Disease Neurological Disease
    CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
  • HY-14987
    AX20017

    Bacterial Infection
    AX20017 is a small-molecule protein kinase G (PknG) inhibitor with an IC50 of 0.39 μM.
  • HY-10499
    PH-064

    BIM-46187

    Others Neurological Disease
    PH-064 (BIM-46187) is an inhibitor of heterotrimeric G-protein complex.
  • HY-70075
    CCG-63808

    RGS Protein Cancer
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-101467A
    Trilaciclib hydrochloride

    G1T28 hydrochloride

    CDK Cancer
    Trilaciclib hydrochloride is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.
  • HY-B1960
    Canthaxanthin

    E 161g; all-trans-Canthaxanthin

    Reactive Oxygen Species Cancer Inflammation/Immunology
    Canthaxanthin is a red-orange carotenoid with various biological activities, such as antioxidant, antitumor properties.
  • HY-101925
    CM-272

    Histone Methyltransferase DNA Methyltransferase Apoptosis Cancer
    CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing interferon-stimulated genes and immunogenic cell death. Anti-tumour Activity.
  • HY-13488
    HG-10-102-01

    LRRK2 Neurological Disease
    HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM) IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1] Target: LRRK2 HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2.
  • HY-111544
    EML741

    Histone Methyltransferase Cancer
    EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
  • HY-13650
    Indisulam

    E 7070

    Carbonic Anhydrase Cancer
    Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15.
  • HY-13807
    UNC0646

    Histone Methyltransferase Cancer
    UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
  • HY-117421A
    CM-579 trihydrochloride

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-N0816
    Polyphyllin VI

    Apoptosis Cancer
    Polyphyllin VI, an active saponin mainly isolated from traditional medicinal plant Paris polyphylla, possess anti-cancer activities. Polyphyllin VI induces G2/M cell cycle arrest and triggers apoptosis.
  • HY-B0294
    Flubendazole

    Parasite Microtubule/Tubulin Apoptosis Cancer Infection
    Flubendazole is a safe and efficacious anthelmintic drug, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle.
  • HY-117421
    CM-579

    Histone Methyltransferase DNA Methyltransferase Cancer
    CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells.
  • HY-N2374
    Eupatorin

    Others Cancer
    Eupatorin, a naturally occurring flavone, arrests cells at the G2-M phase of the cell cycle and induces apoptotic cell death involving activation of multiple caspases, mitochondrial release of cytochrome c and poly(ADP-ribose) polymerase cleavage.
  • HY-130149
    MRTX849

    Ras Cancer
    MRTX849 is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.
  • HY-103353
    SID 26681509

    Cathepsin Parasite Cancer Infection
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
  • HY-111425
    SSE15206

    Apoptosis Microtubule/Tubulin Cancer
    SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
  • HY-N6011
    9-Methoxycamptothecin

    Topoisomerase Apoptosis Cancer
    9-Methoxycamptothecin (MCPT), isolated from Nothapodytes foetida, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
  • HY-12290A
    Arg-Gly-Asp-Ser (TFA)

    RGDS peptide (TFA); Fibronectin tetrapeptide (TFA)

    Integrin Inflammation/Immunology
    Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
  • HY-100761
    SS28

    Microtubule/Tubulin Apoptosis Cancer
    SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.
  • HY-N6576
    Hellebrigenin

    Apoptosis Cancer
    Hellebrigenin, one of bufadienolides belonging to cardioactive steroids, is isolated from traditional Chinese medicine Venenum Bufonis. Hellebrigenin induces DNA damage and cell cycle G2/M arrest. Hellebrigenin triggers mitochondria-mediated apoptosis.
  • HY-18990
    GSK180736A

    ROCK Cardiovascular Disease
    GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  • HY-N2234
    Ganolactone B

    Others Others
    Ganolactone B is a lanostane-type triterpene isolated from the fruiting bodies of G. sinense.
  • HY-14832
    Ataluren

    PTC124

    CFTR Autophagy Metabolic Disease
    Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
  • HY-W016887
    H-Gly-Pro-OH

    Endogenous Metabolite Metabolic Disease
    H-Gly-Pro-OH is an end product of collagen metabolism that is further cleaved by prolidase.
  • HY-114165
    DJ-V-159

    Androgen Receptor Metabolic Disease
    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  • HY-B0355
    Ginkgolide A

    BN-52020

    GABA Receptor Inflammation/Immunology
    Ginkgolide A (BN-52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist.
  • HY-U00418
    ARS-1620

    Ras Cancer
    ARS-1620 is an atropisomeric selective KRAS G12C inhibitor with desirable pharmacokinetics.
  • HY-50162
    GPR120 modulator 1

    GPR120 Metabolic Disease
    GPR120 modulator 1 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • 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-12408A
    6H05 (TFA)

    Ras Cancer
    6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-16518
    Voreloxin Hydrochloride

    SNS-595 Hydrochloride; Vosaroxin Hydrochloride; AG 7352 Hydrochloride

    Topoisomerase Apoptosis Cancer
    Voreloxin Hydrochloride is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
  • HY-50172
    GPR120 modulator 2

    GPR120 Metabolic Disease
    GPR120 modulator 2 is useful for modulating G protein-coupled receptor 120 (GPR120).
  • HY-N2221
    Ganoderal A

    Others Metabolic Disease
    Ganoderal A, an oxygenated sterol from G. lucidum, is a cholesterol synthesis inhibitor.
  • HY-B1511
    Cyclic AMP

    Cyclic adenosine monophosphate; Adenosine cyclic 3', 5'-monophosphate; cAMP

    Endogenous Metabolite Others
    Cyclic AMP (cAMP) is a mitogenic messenger and promotes the G1 to S phase transition in the cell cycle.
  • HY-112680A
    Carboxy pyridostatin trifluoroacetate salt

    Others Others
    Carboxy pyridostatin trifluoroacetate salt has the peculiarity to exhibit high molecular specificity for RNA over DNA G4s.
  • HY-15291
    MBX-2982

    GPR119 Metabolic Disease
    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
  • HY-70074
    CCG-63802

    RGS Protein Cancer
    CCG-63802 is a reversible inhibitor of regulator of G-protein signaling (RGS) protein; with greatest potency at RGS4.
  • HY-B0412
    Estriol

    Oestriol

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-10010
    Ko 143

    BCRP Cancer
    Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2; BCRP) inhibitor.
  • HY-P1613A
    Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA

    Integrin Cancer
    Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
  • HY-12583
    A-366

    Histone Methyltransferase Cancer
    A-366 is a potent histone methyltransferase G9a inhibitor with an IC50 of 3.3 nM.
  • HY-128927
    Mc-Leu-Gly-Arg

    ADC Linker Cancer
    Mc-Leu-Gly-Arg is a cleavable ether linker for antibody-drug conjugates (ADC) design.
  • HY-U00004
    OSIP-486823

    OSIP 486823; OSIP486823; CP248

    Microtubule/Tubulin Cancer
    OSIP-486823 is a novel microtubule-interfering agent with distinct biological effects on both protein kinase G (PKG) and microtubules.
  • HY-19863
    F-15599

    NLX-101

    5-HT Receptor Neurological Disease
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
  • HY-P0195
    Bombesin

    Bombesin Receptor Metabolic Disease Neurological Disease
    Bombesin is a tetradecapeptide originally isolated from frog skin; plays an important role in the release of gastrin and the activation of G-protein receptors.
  • HY-12408
    6H05

    Ras Cancer
    6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
  • HY-B0550
    Bismuth Subsalicylate

    Bismuth oxysalicylate; Bismuth(III) salicylate basic

    PGE synthase Neurological Disease
    Bismuth Subsalicylate is the active ingredient in Pepto-Bismol and inhibits prostaglandin G/H Synthase 1/2.
  • HY-10587
    BIX-01294

    Histone Methyltransferase Autophagy Cancer
    BIX-01294 is an inhibitor of G9a Histone Methyltransferase with an IC50 of 1.9 μM.
  • HY-N0835
    (20S)-Protopanaxatriol

    20(S)-APPT; g-PPT

    Glucocorticoid Receptor Estrogen Receptor/ERR Apoptosis LXR Cardiovascular Disease Endocrinology
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
  • HY-12695B
    5'-GTP trisodium salt hydrate

    Guanosine 5'-triphosphate trisodium salt hydrate

    Others Others
    5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.
  • HY-114392
    Gly-β-MCA

    FXR Autophagy Metabolic Disease
    Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
  • HY-135864
    KRAS inhibitor-6

    Ras Cancer
    KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
  • HY-19560
    SBI-0640756

    SBI-756

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    SBI-0640756 (SBI-756) is a water soluble inhibitor of eIF4G1 and disrupts the eIF4F complex.
  • HY-135866
    KRAS inhibitor-8

    Ras Cancer
    KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
  • HY-U00416
    ARS-1323

    Ras Cancer
    ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
  • HY-140244
    Gly-PEG3-amine

    ADC Linker Cancer
    Gly-PEG3-amine is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-N0593
    Deoxycholic acid

    Cholanoic Acid; Desoxycholic acid

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • 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-141123
    SPDP-C6-Gly-Leu-NHS ester

    ADC Linker Cancer
    SPDP-C6-Gly-Leu-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-16642A
    LY2828360

    Cannabinoid Receptor Neurological Disease
    LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
  • HY-N2268
    Gymnemagenin

    Others Infection Metabolic Disease
    Gymnemagenin is a triterpenoid isolated from G. sylvestre. Gymnemagenin is an agent for diabetes and obesity and also possesses antiviral properties.
  • HY-15273
    UNC0638

    Histone Methyltransferase Autophagy Cancer
    UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively.
  • HY-140080
    Gly-PEG3-endo-BCN

    PROTAC Linker Cancer
    Gly-PEG3-endo-BCN is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-N0593A
    Deoxycholic acid sodium salt

    Sodium deoxycholate

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-113338
    8-Hydroxyguanine

    Endogenous Metabolite Others
    8-Hydroxyguanine is a major pre-mutagenic lesion generated from reactive oxygen species. It causes G-T and A-C substitutions.
  • HY-101777
    TC-O 9311

    GPR139 Neurological Disease
    TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
  • HY-111099
    GLPG1837

    ABBV-974

    CFTR Autophagy Others
    GLPG1837 is a potent and reversible CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
  • HY-124622
    NNC-0640

    Glucagon Receptor Metabolic Disease
    NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM.
  • HY-135865
    KRAS inhibitor-7

    Ras Cancer
    KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
  • HY-130801
    5-Hydroxy-2'-deoxyuridine

    5-OHdU

    Endogenous Metabolite Others
    5-Hydroxy-2'-deoxyuridine (5-OHdU) is a major stable oxidation product of 2'-Deoxycytidine. 5-Hydroxy-2'-deoxyuridine can be incorporated into DNA in vitro by DNA polymerase.
  • HY-125845
    (S,R,S)-AHPC

    MDK7526; VH032-NH2; VHL ligand 1

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC (MDK7526) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC (MDK7526) can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-13721
    Phenoxodiol

    Idronoxil; Dehydroequol; Haginin E

    Caspase Apoptosis Topoisomerase Cancer
    Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
  • HY-N2416
    Taccalonolide A

    Microtubule/Tubulin Apoptosis Cancer
    Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
  • HY-103080
    CMF019

    Others Cardiovascular Disease
    CMF019 is a potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents. Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin.
  • HY-N6682
    Cytochalasin D

    Zygosporin A; NSC 209835

    Arp2/3 Complex Others
    Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.
  • HY-15149
    Romidepsin

    FK 228; FR 901228; NSC 630176

    HDAC Apoptosis Cancer
    Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
  • HY-140081
    Boc-gly-PEG3-endo-BCN

    PROTAC Linker ADC Linker Cancer
    Boc-gly-PEG3-endo-BCN is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Boc-gly-PEG3-endo-BCN is also a cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-101763A
    (S,R,S)-AHPC hydrochloride

    MDK7526 hydrochloride; VH032-NH2 hydrochloride; VHL ligand 1 hydrochloride

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC hydrochloride (MDK7526 hydrochloride) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC hydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-12037A
    Rigosertib

    ON-01910

    Polo-like Kinase (PLK) Apoptosis PI3K Cancer
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-16936
    JH-II-127

    LRRK2 Neurological Disease
    JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
  • HY-P0165
    Taspoglutide

    ITM077; R1583; BIM51077

    Glucagon Receptor Metabolic Disease
    Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist developed for treatment of type 2 diabetes, with an EC50 value of 0.06 nM. Sequence: His-{Aib}-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-Ile-Ala-Trp-Leu-Val-Lys-{Aib}-Arg-NH2.
  • HY-B0011
    Docetaxel

    RP-56976

    Apoptosis Microtubule/Tubulin Cancer
    Docetaxel (RP-56976) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel (RP-56976) is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel (RP-56976) arrests the cell cycle at G2/M and leads to cell apoptosis.
  • HY-126246
    CDC25B-IN-1

    Phosphatase Cancer
    CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
  • HY-B0011A
    Docetaxel Trihydrate

    RP-56976 Trihydrate

    Microtubule/Tubulin Apoptosis Cancer
    Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis.
  • 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-125905
    VH032-cyclopropane-F

    VHL ligand 3; E3 ligase Ligand 19

    Ligand for E3 Ligase Cancer
    VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4。
  • HY-N0047
    Polyphyllin I

    JNK mTOR Akt PDK-1 Autophagy Apoptosis Cancer
    Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
  • HY-N2447
    Amarogentin

    AMPK Apoptosis Cancer Metabolic Disease
    Amarogentin is a secoiridoid glycoside that is mainly extracted from Swertia and Gentiana roots. Amarogentin exhibits many biological effects, including anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin exerts hepatoprotective and immunomodulatory effects. Amarogentin promotes apoptosis, arrests G2/M cell cycle and downregulates of PI3K/Akt/mTOR signalling pathways. Amarogentin exerts beneficial vasculo-metabolic effect by activating AMPK.
  • HY-A0004
    Decitabine

    NSC 127716; 5-Aza-2'-deoxycytidine

    Nucleoside Antimetabolite/Analog DNA Methyltransferase Apoptosis Cancer
    Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
  • HY-16350
    NKP-1339

    IT-139; KP-1339

    DNA/RNA Synthesis Apoptosis Cancer
    NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
  • HY-12037
    Rigosertib sodium

    ON-01910 sodium

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
  • HY-114436
    MRTX-1257

    Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
  • HY-12290
    Arg-Gly-Asp-Ser

    RGDS peptide; Fibronectin tetrapeptide

    Integrin Inflammation/Immunology
    Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
  • HY-19540
    GSK864

    Isocitrate Dehydrogenase (IDH) Cancer
    GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
  • HY-12695
    5'-GTP trisodium salt

    Guanosine 5'-triphosphate trisodium salt

    Endogenous Metabolite Others
    5'-GTP trisodium salt (Guanosine 5'-triphosphate trisodium salt) is an activator of the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades.
  • HY-141292
    Oleoyl-Gly-Lys-N-(m-PEG11)

    ADC Linker Cancer
    Oleoyl-Gly-Lys-N-(m-PEG11) is a cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-18175
    CCT244747

    Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
  • HY-140237
    Boc-Gly-amido-C-PEG3-C3-amine

    PROTAC Linker Cancer
    Boc-Gly-amido-C-PEG3-C3-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
  • HY-141146
    Mal-amido-PEG8-val-gly-PAB-OH

    ADC Linker Cancer
    Mal-amido-PEG8-val-gly-PAB-OH is a cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-15800
    CZC-25146 hydrochloride

    LRRK2 Neurological Disease
    CZC-25146 Hcl is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.
  • HY-114309
    URAT1 inhibitor 1

    URAT1 Inflammation/Immunology
    URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.
  • HY-100757
    CPUY074020

    Histone Methyltransferase Cancer
    CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
  • HY-10957
    L-692429

    MK-0751

    Others Metabolic Disease
    L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.
  • HY-10534
    Voreloxin

    SNS-595; Vosaroxin; AG 7352

    Topoisomerase Apoptosis Cancer
    Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis.
  • HY-B0792
    CZC-54252

    LRRK2 Neurological Disease
    CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.
  • HY-122186
    SGC-GAK-1

    Others Cancer
    SGC-GAK-1 is a potent, selective cyclin G-associated kinase (GAK) inhibitor with a Ki of 3.1 nM. SGC-GAK-1 is a chemical probe for GAK.
  • HY-13237
    GSK2578215A

    LRRK2 Autophagy Mitophagy Neurological Disease
    GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.
  • HY-130118
    MRGPRX1 agonist 1

    Others Neurological Disease
    MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect.
  • HY-N4171
    Dihydrocucurbitacin B

    Others Inflammation/Immunology
    Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
  • HY-128522
    ARS-1323-alkyne

    Ras Cancer
    ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
  • HY-100762
    Mcl1-IN-11

    Bcl-2 Family Cancer
    Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.
  • HY-15647
    BRD9539

    Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1.
  • HY-108477
    TMPyP4 tosylate

    TMP 1363

    G-quadruplex Telomerase Cancer
    TMPyP4 tosylate (TMP 1363) is a quadruplex-specific ligand, which inhibits the interaction between G-quadruplexes and IGF-1. TMPyP4 tosylate (TMP 1363) is a telomerase inhibitor with antitumor effects in osteosarcoma cell lines.
  • HY-N0800
    Protosappanin B

    (-)-Protosappanin B

    Apoptosis Cancer
    Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells.
  • HY-10875
    LRRK2-IN-1

    Apoptosis LRRK2 Neurological Disease Cancer
    LRRK2-IN-1 is a potent and selective LRRK2 inhibitor with IC50 of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.
  • HY-N0336
    3-Butylidenephthalide

    Butylidenephthalide

    Others Others
    3-Butylidenephthalide (Butylidenephthalide) is a phthalic anhydride derivative identified in Ligusticum chuanxiong Hort, and has larvicidal activity (LC50 of 1.56 mg/g for Spodoptera litura larvae).
  • HY-U00417
    ARS-1630

    Ras Cancer
    ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
  • HY-10863
    Anandamide

    (5Z,8Z,11Z,14Z)-N-(2-Hydroxyethyl)icosa-5,8,11,14-tetraenamide

    Cannabinoid Receptor GPR55 Endogenous Metabolite Inflammation/Immunology
    Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., GPR18/GPR55).
  • HY-114277A
    AMG-510 racemate

    Ras Cancer
    AMG-510 racemate is the less active racemate of AMG-510. AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
  • HY-135303
    GLPG1205

    GPR84 Inflammation/Immunology
    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
  • HY-15800A
    CZC-25146

    LRRK2 Neurological Disease
    CZC-25146 is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM/6.87 nM for wild type LRRK2 and G2019S LRRK2 respectively.
  • HY-N7273
    Soyasaponin III

    Apoptosis Cancer
    Soyasaponin III, a monodesmodic oleanane triterpenoid, is one of the main potentially bioactive saponins found in soy (Glycine max) and related products. Soyasaponin III can induce apoptosis in Hep-G2 cells.
  • HY-100551
    meso-Erythritol

    Endogenous Metabolite Others
    meso-Erythritol is a sugar alcohol that occurs naturally in a variety of foods (e.g., pear, watermelon), is 60-80% as sweet as sucrose, and is an approved low-calorie sweetener food additive.
  • HY-14596
    Genistein

    NPI 031L

    EGFR Autophagy Apoptosis Cancer
    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
  • HY-I0736
    Isonicotinic acid

    Drug Metabolite Others
    Isonicotinic acid is a metabolite of Isoniazid. Isoniazid is converted to Isonicotinic acid by hydrazinolysis, with the Isoniazid to Isonicotinic acid biotransformation also to be catalyzed by cytochrome P450 (CYP) enzymes, e.g., CYP2C.
  • HY-13238A
    Dolutegravir sodium

    S/GSK1349572 sodium

    HIV Integrase HIV Infection
    Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-13238
    Dolutegravir

    S/GSK1349572

    HIV Integrase HIV Infection
    Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM).
  • HY-18174B
    Prexasertib Mesylate Hydrate

    LY2606368 Mesylate Hydrate; LY2940930

    Checkpoint Kinase (Chk) Cancer
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a potent, selective, ATP competitive CHK1 and CHK2 inhibitor, with a Ki of 0.9 nM for CHK1 and IC50s of <1 nM, 8 nM for CHK1 and CHK2, respectively. Prexasertib Mesylate Hydrate inhibits HT-29 CHK1 autophosphorylation (S296) and HT-29 CHK2 autophosphorylation (S516). Prexasertib Mesylate Hydrate shows potent anti-tumor activity, significantly abrogates the G2/M checkpoint in p53 deficient HeLa cells with an EC50 of 9 nM.
  • HY-130709
    PROTAC CDK2/9 Degrader-1

    PROTAC CDK Cancer
    PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
  • HY-103369
    PG01

    CFTR Endocrinology
    PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin.
  • HY-110402
    (S,R,S)-AHPC TFA

    MDK7526 TFA; VH032-NH2 TFA; VHL ligand 1 TFA

    Ligand for E3 Ligase Cancer
    (S,R,S)-AHPC TFA (MDK7526 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA (MDK7526 TFA) can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  • HY-11101
    Alendronate sodium hydrate

    Alendronate; MK 217; G-704650 Adronat

    Others Cancer
    Alendronate (sodium hydrate) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM.
  • HY-D0254
    Gallein

    Pyrogallol phthalein

    Others Cancer
    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.
  • HY-N1990
    Gypenoside XLIX

    PPAR Inflammation/Immunology Cardiovascular Disease
    Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
  • HY-106376A
    L-Buthionine-(S,R)-sulfoximine

    L-Buthionine sulfoximine

    Ferroptosis Cancer
    L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
  • HY-N2255
    Crebanine

    Akt Apoptosis Cancer Inflammation/Immunology Cardiovascular Disease
    Crebanine, an alkaloid from Stephania venosa, induces G1 arrest and apoptosis in human cancer cells. Crebanine exhibits anti-inflammatory activity via suppressing MAPKs and Akt signaling. Crebanine also possesses antiarrhythmic effect.
  • HY-16929
    Latrunculin A

    LAT-A

    Arp2/3 Complex Others
    Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
  • HY-N7043
    Isosilybin A

    Apoptosis Cancer
    Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
  • HY-13808
    UNC 0631

    Histone Methyltransferase Cancer
    UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
  • HY-16291
    APTO-253

    LOR-253; LT-253

    c-Myc KLF Apoptosis Cancer
    APTO-253 is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor.
  • HY-101033
    GPR35 agonist 1

    CXCR Cancer Endocrinology
    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
  • HY-N6725
    Sterigmatocystine

    DNA/RNA Synthesis Apoptosis Cancer
    Sterigmatocystine is a precursor of aflatoxins and a mycotoxin produced by common mold strains from Aspergillus versicolor. Sterigmatocystine, a inhibitor of G1 Phase and DNA synthesis, is used to inhibit p21 activity. Sterigmatocystine has teratogenic, and carcinogenic effects in animals.
  • HY-106224
    Orexin A (human, rat, mouse)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-19805
    STO-609

    CaMK AMPK Autophagy Metabolic Disease
    STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
  • HY-P9920
    Ramucirumab

    VEGFR Cancer
    Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D.
  • HY-B1816
    Zaprinast

    M&B 22948

    Phosphodiesterase (PDE) CXCR Neurological Disease Cardiovascular Disease Endocrinology
    Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
  • HY-112140
    JH-VIII-157-02

    ALK Cancer
    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
  • HY-N2100
    6'-O-beta-D-Glucosylgentiopicroside

    Others Others
    6'-O-beta-D-Glucosylgentiopicroside is a secoiridoid isolated from the roots of G. straminea. 6'-O-beta-D-Glucosylgentiopicroside strongly suppresses N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation.
  • HY-114370
    Selpercatinib

    LOXO-292

    RET Cancer
    Selpercatinib (LOXO-292) is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.
  • HY-112950
    RET-IN-1

    RET Cancer
    RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
  • HY-P1525
    Melanin Concentrating Hormone, salmon

    MCH (salmon)

    MCHR1 (GPR24) Metabolic Disease Neurological Disease Cardiovascular Disease Endocrinology
    Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
  • HY-120006
    AR234960

    Others Cardiovascular Disease
    AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  • HY-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-N7045
    Isosilybin B

    Androgen Receptor Apoptosis Cancer
    Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
  • HY-19706
    ARS-853

    Apoptosis Ras Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation.
  • HY-N6615
    Aflatoxin B1

    Others Cancer
    Aflatoxin B1 (AFB1) is a Class 1A carcinogen, which is a secondary metabolite of Aspergillus flavus and A. parasiticus. Aflatoxin B1 (AFB1) mainly induces the transversion of G-->T in the third position of codon 249 of the p53 tumor suppressor gene, resulting in mutation.
  • HY-101483
    Dihydromunduletone

    DHM

    Others Cancer Neurological Disease
    Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
  • HY-13913
    NS-398

    COX Inflammation/Immunology Cancer
    NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM.
  • HY-12745A
    Nalfurafine hydrochloride

    TRK-820 hydrochloride

    Opioid Receptor Neurological Disease
    Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-124386
    DBCO-NHCO-PEG4-amine

    ADC Linker Cancer
    DBCO-NHCO-PEG4-amine is a cleavable ADC linker used to conjugate MMAE (HY-15162) and antibody (e.g., DBCO-VCpAB−MMAE and DBCO-TRX−MMAE with EC50s of 280 nM and 22 nM in SKBR3 cells, respectively).
  • HY-N1196
    Suberosin

    NF-κB Inflammation/Immunology
    Suberosin, isolated from Plumbago zeylanica, exhibits anti-inflammatory and anticoagulant activity. Suberosin suppresses PHA-induced PBMC proliferation and arrested cell cycle progression from the G1 transition to the S phase through the modulation of the transcription factors NF-AT and NF-κB.
  • HY-101290
    BMT-090605

    Others Neurological Disease
    BMT-090605 is a potent, selective AAK1 inhibitor, with an IC50 of 0.6 nM. BMT-090605 shows antinociceptive activity. BMT-090605 inhibits BMP-2-inducible protein kinase (BIKE) and Cyclin G-associated kinase (GAK) with IC50s of 45 and 60 nM, respectively.
  • HY-108699
    TM-N1324

    GHSR Neurological Disease Endocrinology
    TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn 2+, and 280 nM/180 nM in the absence of Zn 2+ for human/murine GPR39.
  • HY-14650
    DHEA

    Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone

    Androgen Receptor Endogenous Metabolite Endocrinology Cancer
    DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
  • HY-18991
    CCG215022

    PKA Cancer
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
  • HY-101379A
    8-Bromo-cGMP sodium

    Calcium Channel Neurological Disease
    8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator and significantly inhibits Ca 2+ macroscopic currents and impairs insulin release stimulated with high K +. 8-Bromo-cGMP sodium has antinociceptive effects.
  • HY-14776
    Quarfloxin

    CX-3543

    DNA/RNA Synthesis Cancer
    Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
  • HY-105309
    GSK-626616

    DYRK Cardiovascular Disease
    GSK-626616 is a potent, orally bioavailable inhibitor of DYRK3 (IC50=0.7 nM). GSK-626616 inhibits other members of the DYRK family (e.g., DYRK1A and DYRK2) with similar potency, which is a potential therapy for the treatment of anemia.
  • HY-12745
    Nalfurafine

    TRK-820

    Opioid Receptor Neurological Disease
    Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-101029
    MBM-55

    Apoptosis Cancer
    MBM-55 (compound 42g) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 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-P1525A
    Melanin Concentrating Hormone, salmon TFA

    MCH (salmon) (TFA)

    MCHR1 (GPR24) Metabolic Disease Neurological Disease Cardiovascular Disease Endocrinology
    Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
  • HY-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-109562A
    GRK2-IN-1 hydrochloride

    Others Cardiovascular Disease
    GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-16438
    RRx-001

    Apoptosis Parasite Cancer Infection Inflammation/Immunology
    RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes drug resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.
  • HY-130407
    Lipoamido-PEG3-OH

    PROTAC Linker Cancer
    Lipoamido-PEG3-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Lipoamido-PEG3-OH (compound TA-TEG-G2CN) can be used in the formation of a highly stable, dendronized gold nanoparticle (AuNP)-based drug delivery platform.
  • HY-15237
    SL 0101-1

    SL0101

    Ribosomal S6 Kinase (RSK) Cancer
    SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM. Shows proliferation inhibition in human breast cancer cell line MCF-7 and produces a cell cycle block in G1 phase.
  • HY-15971A
    AMD 3465

    GENZ-644494

    CXCR HIV Infection Endocrinology
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-N0904
    Ginsenoside C-K

    Ginsenoside compound K; Ginsenoside K

    COX NO Synthase Cytochrome P450 Inflammation/Immunology
    Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
  • HY-N2198
    Podocarpusflavone A

    Topoisomerase Apoptosis Cancer
    Podocarpusflavone A is a DNA topoisomerase I inhibitor, have moderated anti-proliferative activity induce cell apoptosis in MCF-7, is developing anti-tumor drugs target: DNA topoisomerase I In vitro: podocarpusflavone-A show significant inhibitions against DLD, KB, MCF-7, HEp-2 tumor cell lines (ED50 4.56-16.24 μg/mL) and induce cell apoptosis in MCF-7 via mainly sub-G1/S phase arrest.
  • HY-N6009
    8-Deoxygartanin

    Parasite NF-κB Infection
    8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE). 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM.
  • HY-112705
    VU0529331

    Potassium Channel Neurological Disease
    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  • HY-12700
    RO5256390

    Others Neurological Disease
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
  • HY-15589
    GW9508

    GPR40 Potassium Channel Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-N1401
    20(R)-Ginsenoside Rh2

    MMP Apoptosis Cancer Inflammation/Immunology
    20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity.
  • HY-N0930B
    Galegine hydrochloride

    AMPK Bacterial Infection Metabolic Disease
    Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-12455
    Duocarmycin A

    ADC Cytotoxin Apoptosis Caspase Cancer
    Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
  • HY-A0098
    Tunicamycin

    Bacterial Fungal Influenza Virus Cancer Infection Inflammation/Immunology
    Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-105685
    SRX246

    Vasopressin Receptor Neurological Disease
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-12649
    Y16

    Ras Cancer
    Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
  • HY-106224A
    Orexin A (human, rat, mouse) (TFA)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-19835
    LY2922470

    GPR40 Metabolic Disease
    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-P0172
    ATI-2341

    CXCR Inflammation/Immunology Endocrinology Cancer
    ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
  • HY-19269
    FK706

    Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
  • HY-109562
    GRK2-IN-1

    Others Cardiovascular Disease
    GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-130269
    β-Naphthoflavone-CH2-OH

    β-NF-CH2-OH

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins .
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-10930
    UNC0321

    Histone Methyltransferase Cancer
    UNC0321 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 63 pM and with assay-dependent IC50 values of 6-9 nM. UNC0321 also inhibits GLP with assay-dependent IC50 values of 15-23 nM. UNC0321 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-15610
    GDC-0623

    RG 7421; MEK inhibitor 1

    Apoptosis MEK Cancer
    GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
  • HY-117163
    FzM1.8

    Wnt β-catenin Cancer
    FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-15971
    AMD 3465 hexahydrobromide

    GENZ-644494 hexahydrobromide

    CXCR HIV Infection Endocrinology
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12 AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-112099
    Mc-Val-Cit-PAB-Cl

    ADC Linker Cancer
    Mc-Val-Cit-PAB-Cl is a cleavable ADC linker. Mc-Val-Cit-PAB-Cl can be used to conjugate MMAE and antibody to form antibody-MC-vc-MMAE (e.g., anti-CD22-MC-VC-PABC-MMAE with IC50s of 3.3 and 0.95 nM for BJAB and WSU cell lines in cytotoxicity assay).
  • HY-10929
    UNC0224

    Histone Methyltransferase Cancer
    UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E.
  • HY-17371
    Oxaliplatin

    DNA Alkylator/Crosslinker Autophagy Cancer
    Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
  • HY-120179
    LP-922761

    Others Neurological Disease
    LP-922761 is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with an in vitro IC50 of 4.8 nM and a cellular IC50 of 7.6 nM. LP-922761 also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 exhibits no significant activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors.
  • HY-111557
    YM-254890

    P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
  • HY-13509
    CCG-50014

    RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-N6818
    5,​7,​4'-​Trimethoxyflavone

    Apoptosis Caspase PARP Cancer
    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  • HY-126251
    CDK9-IN-7

    CDK Apoptosis Cancer
    CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC.
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • HY-103022
    Repotrectinib

    TPX-0005

    ROS Trk Receptor ALK Cancer
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. Repotrectinib (TPX-0005) potently inhibits WT ALK (1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). It also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (1.04, 1.66, 5.3, and 6.96 nM, respectively) .
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-16705
    BRD4770

    Histone Methyltransferase Cancer
    BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 µM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
  • HY-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.