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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-MK256
MK256

Chemical Structure : MK256

CAS No.: 2271348-04-8

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MK256 (MK-256)

货号: PC-49444Not For Human Use, Lab Use Only.

MK256 (MK-256) is a potent, selective CDK8 inhibitor with IC50 of 2.5 nM and 3.3 nM against CDK8/cyclin C and CDK19/cyclin C, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    MK256 (MK-256) is a potent, selective CDK8 inhibitor with IC50 of 2.5 nM and 3.3 nM against CDK8/cyclin C and CDK19/cyclin C, respectively.
    MK256 does not inhibit other 13 CDKs at 200 nM, with exception of CDK9 (IC50=105 nM, 40-fold selectivity for CDK8).
    MK256 bonds in the ATP binding pocket of CDK8, two hydrogen bonds were formed between MK256 and hinge region residues Asp98 and Ala100.
    MK256 (50-500 nM) induces differentiation/maturation in CD34+/CD38- human leukemic cell line (TEX) cells.
    MK256 shows a wide range of sensitivity to a panel of AML cell lines, ranging from highly sensitive (<30 nM) to highly resistant (>5 uM).
    MK256 is sensitive to MV- 4-11 (IC50=23 nM) and MOLM-14 (IC50=24 nM), both of which harbor mixed lineage leukemia (MLL) fusions.
    MK256 also shows relatively potent growth inhibition against SKNO-1 (IC50=73 nM) and KG-1 (IC50=80 nM).
    MK256 downregulates phosphorylation of STAT1 and STAT5 in AML cell lines MV-4-11 and MOLM-14, also downregulates MCL-1 and CCL2 mRNA expression.
    MK256 (50 mg/kg, oral) showed great efficacy in MOLM-14 mice xenograft model, the combination of MK256 and venetoclax lowered the effective concentration for both compounds.

    物理化学性质&存储条件

    分子量 317.142
    分子式 C14H9BrN2O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    1-amino-5-bromobenzo[h]isoquinoline-8-carboxylic acid

    参考文献

    1. Jen-Chieh Lee, et al. Oncotarget. 2022 Nov 2;13:1217-1236.

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