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ATP-binding region

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112299
    Zipalertinib
    3 Publications Verification

    TAS6417; CLN-081

    EGFR Apoptosis Cancer
    Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
    Zipalertinib
  • HY-12062
    PD318088
    1 Publications Verification

    MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
    PD318088
  • HY-112373

    Aurora Kinase Others
    Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
    Aurora kinase inhibitor-3
  • HY-147259

    c-Met/HGFR Cancer
    Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
    Dalmelitinib
  • HY-164523

    Checkpoint Kinase (Chk) Cancer
    PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .
    PV1162
  • HY-116882

    PI3K Inflammation/Immunology
    PIK-39 is a selective PI3Kδ inhibitor with an IC50 of 0.30 μM. PIK-39 has a propeller-like structure that induces conformational changes in the ATP-binding region of its target. PIK-39 is applicable to the research of autoimmune diseases .
    PIK-39
  • HY-182281

    FLT3 STAT Akt ERK Apoptosis Cancer
    FLT3-IN-41 is a highly potent FLT3 inhibitor. The IC50 values of FLT3-IN-41 against human FLT3-ITD and FLT3-WT are 3.16 nM and 294.7 nM, respectively. By binding to the ATP-binding pockets of FLT3-ITD and FLT3-WT and forming hydrogen bonds with hinge region residues and Phe830, FLT3-IN-41 inhibits the STAT5, Akt and Erk signaling pathways. FLT3-IN-41 induces G2/M phase arrest and promotes apoptosis in FLT3-ITD-positive acute myeloid leukemia cells, exhibiting significant antiproliferative activity. FLT3-IN-41 serves as a valuable tool for the study of acute myeloid leukemia .
    FLT3-IN-41
  • HY-182764A

    CDK Cancer
    CDK11-IN-1 hydrochloride is a potent, highly selective, and orally active CDK11 inhibitor with an IC50 of 4 nM, showing 32.5-fold and 2700-fold selectivity over CDK7 and CDK9, respectively. CDK11-IN-1 hydrochloride binds competitively to the ATP-binding pocket of CDK11 and forms a hydrogen bond with the hinge region residue Val163. It inhibits tumor cell proliferation and exhibits antitumor activity in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for studies on the pathophysiology of CDK11-mediated tumors, as well as research on malignant tumors such as lung cancer .
    CDK11-IN-1 hydrochloride
  • HY-123726

    EGFR Cancer
    ErbB-1/ErbB-2 tyrosine kinase-IN-1 is a dual ErbB-1/ErbB-2 tyrosine kinase inhibitor with IC50 values of 0.027 μM and 0.026 μM. ErbB-1/ErbB-2 tyrosine kinase-IN-1 targets the ATP binding region of ErbB-1 and ErbB-2 tyrosine kinases. ErbB-1/ErbB-2 tyrosine kinase-IN-1 inhibits cancer cells proliferation .
    ErbB-1/ErbB-2 tyrosine kinase-IN-1
  • HY-181169

    Cyclin G-associated Kinase (GAK) Cancer
    GAK-IN-3 is a cyclin G-associated kinase (GAK) inhibitor with an IC50 of 207 nM and a Ki of 66 nM. GAK-IN-3 inhibits kinase activity in the nanomolar range by binding to GAK’s ATP-binding site. GAK-IN-3 acts as a cytotoxic agent that reduces viability of Ewing sarcoma cells. GAK-IN-3 can be used for the research of ewing sarcoma .
    GAK-IN-3

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