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CIN

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38

Inhibitors & Agonists

2

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1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132809

    CIN-107

    Mineralocorticoid Receptor Metabolic Disease
    Baxdrostat is a aldosterone synthase inhibitor .
    Baxdrostat
  • HY-12682
    Glutaminase C-IN-1
    Maximum Cited Publications
    11 Publications Verification

    Compound 968

    Glutaminase Cancer
    Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts .
    Glutaminase C-IN-1
  • HY-153066

    KIF18A-IN-7

    Kinesin Microtubule/Tubulin Apoptosis Cancer
    VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
    VLS-1272
  • HY-173522

    Kinesin Microtubule/Tubulin Cancer
    KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (Ex/Em = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015) .
    KIF2C-IN-1
  • HY-162275

    Histone Demethylase Histone Methyltransferase STAT Cancer
    JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
    JMJD1C-IN-1
  • HY-146584

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity .
    Cathepsin C-IN-5
  • HY-146148
    KDM4C-IN-1
    2 Publications Verification

    Histone Demethylase Cancer
    KDM4C-IN-1 (Compound 4d) is a potent KDM4C inhibitor with an IC50 of 8 nM. KDM4C-IN-1 inhibits the growth of HepG2 and A549 cells with IC50s of 0.8 µM and 1.1 µM, respectively .
    KDM4C-IN-1
  • HY-132809A

    (S)-CIN-107

    Mineralocorticoid Receptor Endocrinology
    (S)-Baxdrostat is the S-enantiomer of Baxdrostat. Baxdrostat is an aldosterone synthase inhibitor .
    (S)-Baxdrostat
  • HY-163476

    PI4P5K Inflammation/Immunology Cancer
    PIP5K1C-IN-1 (Compound 30) is a potent PIP5K1C inhibitor, with an IC50 of 0.80 nM. PIP5K1C-IN-1 exhibits low total clearance in mice and high levels of kinase selectivity. PIP5K1C-IN-1 can be used for the research of cancer and chronic pain .
    PIP5K1C-IN-1
  • HY-153880

    LYTACs Ras Cancer
    KRAS degrader-1 is a potent KRAS degrader. KRAS degrader-1 targets specific proteins for degradation via the autophagy-lysosomal degradation pathway. KRAS degrader-1 is suitable for use in cancer research. (Blue: KRAS G12C-IN-72 (HY-128414); Black: Linker (HY-175587); Pink: 5-Iodoindolin-2-one (HY-76986); Blue + Black: KRAS ligand-Linker Conjugate 7 (HY-175586)) .
    KRAS degrader-1
  • HY-132809B

    (Rac)-CIN-107

    Drug Isomer Endocrinology
    (Rac)-Baxdrostat is the isomer of Baxdrostat (HY-132809), and can be used as an experimental control. Baxdrostat is a aldosterone synthase inhibitor .
    (Rac)-Baxdrostat
  • HY-103046

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent .
    UbcH5c-IN-1
  • HY-108420
    INK4C-IN-2
    1 Publications Verification

    CDK Cancer
    INK4C-IN-2 is a p18 INK4C inhibitor. NK4C-IN-2 promotes hematopoietic stem cells (HSCs) division by inhibiting INK4C and activating CDK4/6, with an ED50 of 5.21 nM. INK4C-IN-2 shows no cytotoxic to normal 32D cells, HSCs, leukemia cell lines and myeloma cell lines .
    INK4C-IN-2
  • HY-128771

    Ras Cancer
    K-Ras G12C-IN-4, compound 1, is a potent Covalent Inhibitor of KRAS G12C .
    K-Ras G12C-IN-4
  • HY-146581

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively .
    Cathepsin C-IN-4
  • HY-146580

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively .
    Cathepsin C-IN-3
  • HY-18606

    Ras Cancer
    K-Ras G12C-IN-3 (Compound VI-5) is an irreversible small molecule inhibitor of mutant K-Ras G12C. K-Ras G12C-IN-3 can be used in the research of cancers .
    K-Ras G12C-IN-3
  • HY-155611

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsin C with anti-inflammatory activity. Cathepsin C-IN-6 inhibts activation of neutrophil elastase,exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.,chronic obstructive pulmonary disease) .
    Cathepsin C-IN-6
  • HY-18604
    K-Ras G12C-IN-1
    1 Publications Verification

    Ras Cancer
    K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
    K-Ras G12C-IN-1
  • HY-RS10298

    Small Interfering RNA (siRNA) Others

    PDXP Human Pre-designed siRNA Set A contains three designed siRNAs for PDXP gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PDXP Human Pre-designed siRNA Set A
    PDXP Human Pre-designed siRNA Set A
  • HY-149602

    Glutaminase Reactive Oxygen Species (ROS) Cancer
    Glutaminase C-IN-2 (compound 11) is glutaminase C (GAC) allosteric inhibitor with an IC50 of 10.64 nM. Glutaminase C-IN-2 regulates the cellular metabolite, thereby increasing reactive oxygen species (ROS) by blocking glutamine metabolism. Glutaminase C-IN-2 has anticancer effects .
    Glutaminase C-IN-2
  • HY-174851

    Ras Cancer
    KRAS G12C-IN-70 is a selective KRAS G12C mutant inhibitor. KRAS G12C-IN-70 blocks KRAS G12C-mediated downstream signaling pathways (e.g., RAF-MEK-ERK) and inhibits tumor cell proliferation. KRAS G12C-IN-70 is promising for research of KRAS G12C mutation-related tumors (such as non-small cell lung cancer, colorectal cancer) .
    KRAS G12C-IN-70
  • HY-18605

    Ras Cancer
    K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
    K-Ras G12C-IN-2
  • HY-P2004

    MMP Cancer
    FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
    FFAGLDD
  • HY-P2004A

    MMP Cancer
    FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release .
    FFAGLDD TFA
  • HY-163477

    PI4P5K Cancer
    PIP5K1C-IN-2 (compound 33) is a potent and selective 4-phosphate 5-kinases 1 C (PIP5K1C) inhibitor with an IC50 value of 0.0059 µM .
    PIP5K1C-IN-2
  • HY-180241

    Glutaminase Reactive Oxygen Species (ROS) Cancer
    Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC) .
    Glutaminase C-IN-3
  • HY-177408

    Cathepsin Cancer
    Cathepsin C-IN-7 (Page 68) is a Cathepsin C inhibitor. Cathepsin C-IN-7 can be used in research related to primary cancers and cancer metastases .
    Cathepsin C-IN-7
  • HY-181913

    Ras ERK Cancer
    KRAS G12C-IN-76 (Compound 39) is an orally active KRAS G12C inhibitor. KRAS G12C-IN-76 inhibits the phosphorylation of ERK. KRAS G12C-IN-76 exhibits anticancer activity against pancreatic cancer .
    KRAS G12C-IN-76
  • HY-128414

    Ligands for Target Protein for PROTAC Ras Cancer
    KRAS G12C-IN-72 (Example 571) is a KRAS G12C inhibitor. KRAS G12C-IN-72 can be used as a target protein ligand to synthesize PROTACs, such as KRAS degrader-1 (HY-153880). KRAS G12C-IN-72 can be used in cancer research .
    KRAS G12C-IN-72
  • HY-183645

    Ras Cancer
    KRAS G12C-IN-79 is a KRAS G12C inhibitor with an IC50 of 1.9 nM. KRAS G12C-IN-79 functionally inhibits the activity of the GDP-bound form of KRAS G12C. KRAS G12C-IN-79 can be used for the research of nonsmall cell lung cancer, colon cancer, pancreatic cancer .
    KRAS G12C-IN-79
  • HY-180298

    Ras Cancer
    KRAS G12C-IN-71 (Compound 11) is a covalent G12C KRAS inhibitor with a Ki of 380 nM. KRAS G12C-IN-71 can be used in the research of non-small cell lung cancer .
    KRAS G12C-IN-71
  • HY-116796

    Histone Demethylase Inflammation/Immunology Cancer
    KDM4C-IN-2 is a histone lysine demethylase KDM4C (JMJD2C) inhibitor with an IC50 of 147 μM and a Ki of 51 μM. KDM4C-IN-2 can be used for the research of cancer, such as prostate and breast cancer .
    KDM4C-IN-2
  • HY-181889

    Ras Cancer
    KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
    KRAS G12C-IN-75
  • HY-181716

    Ras Apoptosis Cancer
    KRAS G12C-IN-74 is an orally active, selective KRAS G12C inhibitor with a target IC50 of 43.18 nM. KRAS G12C-IN-74 induces G0/G1 cell cycle arrest and apoptosis in KRAS G12C-mutant cancer cells. KRAS G12C-IN-74 is applicable for the research of KRAS G12C-mutant pancreatic cancer, colorectal cancer and lung cancer .
    KRAS G12C-IN-74
  • HY-181965

    Ras ERK p38 MAPK Cancer
    KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
    KRAS G12C-IN-78
  • HY-181570

    Cancer
    KRAS G12C-IN-73 (Page 21) is a KRAS G12C inhibitor, a derivative of Divarasib (HY-145928), which is applicable for cancer research .
    KRAS G12C-IN-73
  • HY-181964

    Cancer
    KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
    KRAS G12C-IN-77

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