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Catalog Number | orb692134 |
---|---|
Category | Small Molecules |
Description | Casein Kinase inhibitor A51 (CKIα inhibitor A51) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=0.5-20 nM, CKIα Kd=5.3 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at < 160 nM, in correlation to the capacity to stabilize p53; 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, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models. |
CAS Number | [2079068-74-7] |
MW | 360.89 |
SMILES | [C@@H](NC1=NC=C(Cl)C(C2=C(CC3CC3)N(C)N=C2)=N1)1CC[C@H](N)CC1 |
Formula | C18H25ClN6 |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |
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