HomeNew Casein Kinase Inhibitors

New Casein Kinase Inhibitors

Catalog No. Product Name Information
E1455 BTX-A51 BTX-A51 (Casein Kinase inhibitor A51) is a first-in-class oral and potent inhibitor of casein kinase 1α (CK1α) and cyclin dependent kinase (CDK7/9) with an IC50 of 17 nM for CK1α and Kd of 1.3 nM and 4 nM for CDK7 and CDK9, respectively. It induces apoptosis of leukemic cells by activating p53 and inhibiting expression of Mcl1 and can be used in Acute myeloid leukemia (AML) cancer research.
E4725 BMS-986397 BMS-986397 (CC-91633) is a potent and selective thalidomide-derived molecular glue degrader of CK1α and a modulator of CRBN E3 ubiquitin ligase. As a first-in-class CELMoD agent, it exhibits strong anti-leukemic activity in AML (Acute Myeloid Leukemia) and HR-MDS (High-Risk Myelodysplastic Syndrome) models, with enhanced efficacy and potency for hematologic malignancies and immunomodulation.
E1927 PF-05251749（CK1-IN-2） PF-05251749 (CK1-IN-2, Compound Nr.4) is a potent, selective, brain-penetrant inhibitor of Casein Kinase 1 (CK1) in a concentration-dependent manner, with IC50 values of 33.1 nM for CK1d and 51.6 nM for CK1e. It also functions as an inducer of CYP3A, with the potential to treat circadian rhythm disruptions in Alzheimer's and Parkinson's diseases.
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