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Results for "

Enzymatic Inhibitors

" in MCE Product Catalog:

72

Inhibitors & Agonists

1

Fluorescent Dye

1

Biochemical Assay Reagents

1

Peptides

2

Inhibitory Antibodies

5

Natural
Products

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-112261
    CDK12-IN-3

    CDK Cancer
    CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.
  • HY-130240
    GCN2-IN-6

    Eukaryotic Initiation Factor (eIF) Cancer
    GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
  • HY-131068
    BACE-1 inhibitor 2

    Beta-secretase Neurological Disease
    BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.
  • HY-111789
    Subasumstat

    TAK-981

    E1/E2/E3 Enzyme Cancer Inflammation/Immunology
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
  • HY-B0866
    Ametryn

    Others Metabolic Disease
    Ametryn, a member of the Triazine chemical family, is a herbicide which inhibits photosynthesis and other enzymatic processes. Ametryn is effective against annual broadleaf weeds and grasses.
  • HY-Y1269
    Ammonium chloride

    Autophagy Cancer
    Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor.
  • HY-125130
    Hesperetin 7-O-glucoside

    HMG-CoA Reductase (HMGCR) Bacterial Infection Metabolic Disease
    Hesperetin 7-O-glucoside is produced by the enzymatic conversion of Hesperidin. Hesperetin 7-O-glucoside is a potent human HMG-CoA reductase inhibitor and also effectively inhibits the growth of Helicobacter pylori. Antihypertensive effect.
  • HY-131903
    HS271

    IRAK Inflammation/Immunology
    HS271 is a highly potent, orally active and selective IRAK4 inhibitor, with an IC50 of 7.2 μM. HS271 exhibits superior enzymatic and cellular activities, as well as excellent pharmacokinetic properties.
  • HY-144092
    HPK1-IN-25

    MAP4K Cancer
    HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research.
  • HY-112711
    LV-320

    Autophagy Cathepsin Cancer
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
  • HY-101549
    MRX-2843

    UNC2371

    FLT3 Cancer
    MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-119933
    RIPK1-IN-7

    RIP kinase Cancer
    RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
  • HY-139884
    EGFR-IN-18

    EGFR Cancer
    EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
  • HY-143448
    Tyrosinase-IN-1

    Tyrosinase Others
    Tyrosinase-IN-1 (compound 90) is a potent inhibitor of tyrosinase. Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. Tyrosinase-IN-1 has the potential for the research of skin whitening agents and food preservatives.
  • HY-143450
    Tyrosinase-IN-3

    Tyrosinase Others
    Tyrosinase-IN-3 (compound 54) is a potent inhibitor of tyrosinase. Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. Tyrosinase-IN-3 has the potential for the research of skin whitening agents and food preservatives.
  • HY-143451
    Tyrosinase-IN-4

    Tyrosinase Others
    Tyrosinase-IN-4 (compound 34) is a potent inhibitor of tyrosinase. Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. Tyrosinase-IN-4 has the potential for the research of skin whitening agents and food preservatives.
  • HY-143449
    Tyrosinase-IN-2

    Tyrosinase Others
    Tyrosinase-IN-2 (compound 67) is a potent inhibitor of tyrosinase. Tyrosinase is a copper-containing metalloenzyme that is responsible for the rate-limiting catalytic step in the melanin biosynthesis and enzymatic browning. Tyrosinase-IN-2 has the potential for the research of skin whitening agents and food preservatives.
  • HY-103347
    M50054

    Apoptosis Inflammation/Immunology
    M50054 is a potent inhibitor of apoptosis. M50054 inhibits Etoposide-induced caspase-3 activation of U937 cells with an IC50 of 79 μg/mL. M50054 does not directly inhibit the enzymatic activity of caspase-3. M50054 can be used for the research anti-Fas-antibody-induced hepatitis and chemotherapy-induced alopecia.
  • HY-D0162
    Malachite green oxalate

    IKK NF-κB Apoptosis Cancer
    Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
  • HY-15148
    Tipranavir

    PNU-140690

    HIV Protease HIV SARS-CoV Infection
    Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-108702
    ML-792

    E1/E2/E3 Enzyme Cancer
    ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50 values of 32 μM and >100 μM, respectively).
  • HY-147841
    HIV-1 inhibitor-41

    HIV Reverse Transcriptase Infection
    HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity.
  • HY-115747
    Namoline

    Histone Demethylase Cancer
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research.
  • HY-141508
    Flazin

    Xanthine Oxidase NO Synthase Metabolic Disease Inflammation/Immunology Neurological Disease
    Flazin is a non-enzymatic protein glycation inhibitor, also inhibits peroxynitrite (ONOO -), with an IC50 value of 85.31 μM for bovine serum albumin (BSA) glycation and an EC50 value of 71.99 μM for ONOO -. Flazin can be used for researching diabetes and neuronal disorders. Flazin also can used as a lipid droplet (LD) regulator against lipid disorders, and a xanthine oxidase (XOD) inhibitor.
  • HY-N0814
    Phytic acid

    Inositol hexaphosphate

    Xanthine Oxidase Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Phytic acid (Inositol hexaphosphate) is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
  • HY-109127A
    Berotralstat dihydrochloride

    Ser/Thr Protease Others
    Berotralstat dihydrochloride is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat dihydrochloride works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-N0814B
    Phytic acid hexasodium

    Inositol hexaphosphate hexasodium

    Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Phytic acid (Inositol hexaphosphate) hexasodium is a phosphorus storage compound of seeds and cereal grains. Phytic acid hexasodium has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid hexasodium inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
  • HY-137742
    SBP-7455

    ULK Autophagy Cancer
    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.
  • HY-N0814A
    Phytic acid dodecasodium hydrate

    Inositol hexaphosphate dodecasodium hydrate

    Xanthine Oxidase Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Phytic acid (Inositol hexaphosphate) dodecasodium hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
  • HY-145953
    VY-3-135

    Others Cancer
    VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer.
  • HY-16910
    WIKI4

    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
  • HY-Z0816
    Dehydronitrosonisoldipine

    Calcium Channel Others
    Dehydronitrosonisoldipine, a derivative of Nisoldipine (HY-17402), is an irreversible and cell-permeant sterile alpha and TIR motif-containing 1 (SARM1) inhibitor. Dehydronitrosonisoldipine acts mainly by blocking SARM1 activation but not its enzymatic activities. Dehydronitrosonisoldipine inhibits SARM1 and axon degenration (AxD) by covalently modifying cysteines, also inhibits the Vincristine-activated cADPR production in neurons. Dehydronitrosonisoldipine can be used for researching neurodegenerative disorders.
  • HY-117359
    UCD38B hydrochloride

    PAI-1 Apoptosis Cancer
    UCD38B hydrochloride is a cell permeant, competitive enzymatic uPA inhibitor with an IC50 value of 7 μM. UCD38B hydrochloride targets intracellular uPA causing mistrafficking of uPA into perinuclear mitochondria, reducing the mitochondrial membrane potential, and followed by the release of apoptotic inducible factor (AIF). UCD38B hydrochloride induces apoptosis.
  • HY-109127
    Berotralstat

    Ser/Thr Protease Others
    Berotralstat (BCX7353) is a low toxicity, effective, highly specific, second-generation, synthetic and orally active plasma kallikrein inhibitor used for the research of hereditary angioedema (HAE) attacks. Berotralstat works by blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.
  • HY-115929
    DENV-IN-4

    DNA/RNA Synthesis Infection
    DENV-IN-4 is a potent DENV inhibitor (DENV EC50=4.79 μM, Vero CC50>100 μM, SI>20.9). DENV-IN-4 can inhibit the expression level of DENV2 with concentration-dependence and reduce RNA-dependent RNA polymerase (RdRp) enzymatic activity. DENV-IN-4 has antiviral effect.
  • HY-142685
    Pyruvate Carboxylase-IN-2

    Others Cancer
    Pyruvate Carboxylase-IN-2 (compound 29) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.065 and 0.097 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-2 is a natural analog of erianin. Pyruvate Carboxylase-IN-2 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC).
  • HY-142684
    Pyruvate Carboxylase-IN-1

    Others Cancer
    Pyruvate Carboxylase-IN-1 (compound 37) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.204 and 0.104 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-1 is a natural analog of erianin. Pyruvate Carboxylase-IN-1 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC).
  • HY-116804
    ZLD1039

    Histone Methyltransferase Cancer
    ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis.
  • HY-114286
    PXS-5153A

    Monoamine Oxidase Inflammation/Immunology
    PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
  • HY-146213
    CDK4/6-IN-12

    CDK Cancer
    CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. CDK4/6-IN-12 has enzymatic inhibitory activity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer.
  • HY-144732
    TRK/ALK-IN-1

    Trk Receptor Anaplastic lymphoma kinase (ALK) Cancer
    TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases.
  • HY-B0091A
    Adapalene sodium salt

    CD 271 sodium salt

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity.
  • HY-114286A
    PXS-5153A monohydrochloride

    Monoamine Oxidase Inflammation/Immunology
    PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
  • HY-129388A
    Pulrodemstat

    CC-90011; LSD1-IN-7

    Histone Demethylase Cancer
    Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-143900
    BTK-IN-7

    Btk Apoptosis Cancer Inflammation/Immunology
    BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels(ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity.
  • HY-B0091
    Adapalene

    CD271

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.
  • HY-15148S
    Tipranavir-d4

    HIV Protease HIV SARS-CoV Infection
    Tipranavir-d4 (PNU-140690-d4) is the deuterium labeled Tipranavir. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM. Tipranavir inhibits SARS-CoV-2 3CL pro activity.
  • HY-101117
    EED226

    Histone Methyltransferase Cancer
    EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
  • HY-151988
    SARS-CoV-2-IN-36

    SARS-CoV Infection
    SARS-CoV-2-IN-36 is a potent SARS-CoV-2 Mpro (SARS-CoV) inhibitor with an IC50 of 2.37 μM and a Kd of 1.19 μM in enzymatic assays. SARS-CoV-2-IN-36 shows antiviral activity against UC-1074, RG2674, and NVDBB-2220 SARS-CoV-2 variants in Vero cells.
  • HY-129388B
    Pulrodemstat benzenesulfonate

    CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate

    Histone Demethylase Cancer
    CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-138298A
    Trastuzumab deruxtecan

    DS-8201; DS-8201a

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
  • HY-124825
    iGOT1-01

    Others Cancer
    iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity.
  • HY-114778
    Fluzoparib

    SHR3162; Fuzuloparib

    PARP Cancer
    Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell‐free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)‐deficient cells, and sensitizes both HR‐deficient and HR‐proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research.
  • HY-129388
    Pulrodemstat Methylbenzenesulfonate

    CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate

    Histone Demethylase Cancer
    CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
  • HY-138298
    Trastuzumab deruxtecan (solution)

    DS-8201 (solution); DS-8201a (solution)

    Antibody-Drug Conjugates (ADCs) EGFR Cancer
    Trastuzumab deruxtecan (DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan (solution) is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan (solution) can be used for the research of HER2-positive breast cancer and gastric cancer.
  • HY-144123
    HIV-1 inhibitor-16

    HIV Infection
    HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity.
  • HY-128333
    PI3K/mTOR Inhibitor-4

    PI3K mTOR Cancer
    PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.
  • HY-150701
    INCB13739

    Glucocorticoid Receptor Mineralocorticoid Receptor 11β-HSD Metabolic Disease
    INCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research.
  • HY-15823
    CAY10566

    Stearoyl-CoA Desaturase (SCD) Cancer
    CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).
  • HY-12473
    Vps34-IN-2

    PI3K SARS-CoV Cancer
    Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively. Vps34-IN-2 shows antiviral activity against SARS-CoV-2 (IC50 of 3.1 μM), HCoV-229E (IC50 of 0.7 μM) and HCoV-OC43.
  • HY-B0091S
    Adapalene-d3

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.
  • HY-138831
    AES-350

    HDAC Apoptosis Cancer
    AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.
  • HY-B0091S1
    Adapalene-d6 Methyl Ester

    RAR/RXR Autophagy Apoptosis Cancer Inflammation/Immunology Neurological Disease
    Adapalene-d6 Methyl Ester is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity.
  • HY-117724
    AZ3976

    PAI-1 Cardiovascular Disease
    AZ3976 is a potent plasminogen activator inhibitor type 1 (PAI-1) inhibitor with an IC50 value of 26 μM in an enzymatic chromogenic assay. AZ3976 is active with an IC50 of 16 μM in a plasma clot lysis assay. AZ3976 does not bind to active PAI-1 but bound reversibly to latent PAI-1. AZ3976 inhibits PAI-1 by enhancing the latency transition of active PAI-1. AZ3976 displays profibrinolytic activities in a human plasma clot lysis assay.
  • HY-146408
    ALK-IN-21

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-21 (Compound B10), a potent ALK inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC50 values of 4.59 nM, 2.07 nM and 5.95 nM toward ALK WT, ALK L1196M and ALK G1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC50 values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma.
  • HY-148333
    MS177

    PROTACs Histone Methyltransferase Apoptosis Cancer
    MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12 nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest.
  • HY-145685
    RECQL5-IN-1

    Others Cancer
    RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.
  • HY-B1455
    Clindamycin

    Bacterial Antibiotic Parasite Infection Cancer
    Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria.
  • HY-B1455S
    Clindamycin-d3 hydrochloride

    Bacterial Antibiotic Parasite Infection
    Clindamycin-d3 hydrochloride is the deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria.
  • HY-124346
    T-3364366

    Others Metabolic Disease
    T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay.
  • HY-B1455S1
    Clindamycin-13C,d3

    Bacterial Antibiotic Parasite Infection
    Clindamycin-13C,d3 is the 13C- and deuterium labeled Clindamycin. Clindamycin is an orally active and broad-spectrum bacteriostatic lincosamide antibiotic. Clindamycin can inhibit bacterial protein synthesis, possessing the ability to suppress the expression of virulence factors in Staphylococcus aureus at sub-inhibitory concentrations (sub-MICs). Clindamycin resistance results from enzymatic methylation of the antibiotic binding site in the 50S ribosomal subunit (23S rRNA). Clindamycin decreases the production of Panton-Valentine leucocidin (PVL), toxic-shock-staphylococcal toxin (TSST-1) or alpha-haemolysin (Hla). Clindamycin also can be used for researching malaria.