BTX-A51 | CK1α inhibitor, CDK7/9 inhibitor | Probechem Biochemicals

Chemical Structure : BTX-A51

CAS No.: 2079068-74-7

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BTX-A51 (CKIα inhibitor A51)

货号: PC-35627Not For Human Use, Lab Use Only.

BTX-A51 (CK1α inhibitor A51) is a novel pan-specific CK1 (CSNK1) inhibitor (Kd=0.5-20 nM, CK1α Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19.

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10 mg	￥5280	In stock
25 mg	￥8980	In stock
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生物&药学活性

BTX-A51 (CK1α inhibitor A51) is a novel pan-specific CK1 (CSNK1) inhibitor (Kd=0.5-20 nM, CK1α Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19.
BTX-A51 targest both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53.
BTX-A51 shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs.
Blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprives leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1.
BTX-A51 demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.

物理化学性质&存储条件

分子量	360.89
分子式	C18H25ClN6
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	(1r,4r)-N1-(5-chloro-4-(5-(cyclopropylmethyl)-1-methyl-1H-pyrazol-4-yl)pyrimidin-2-yl)cyclohexane-1,4-diamine

参考文献

1. Minzel W, et al. Cell. 2018 Aug 20. pii: S0092-8674(18)30973-5. doi: 10.1016/j.cell.2018.07.045.

BTX-A51 (CKIα inhibitor A51)

生物&药学活性

物理化学性质&存储条件

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BTX-A51 (CKIα inhibitor A51)

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