BAY-888

BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP) . BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways[1][2][3].

Product Specifications

CAS Number

[2468783-75-5]

Product Name Alternative

BRD5846

UNSPSC

12352005

Target

Casein Kinase

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bay-888.html

Purity

98.27

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C1C2=C(NC(C3=CC=NC(NC([C@@H](C)C4=CC=C(F)C=C4)=O)=C3)=C2NC5=CC=CC=C5)CCN1C

Molecular Formula

C28H26FN5O2

Molecular Weight

483.54

References & Citations

[1]Preparation of 3-amino-2-[2- (acylamino) pyridin-4-yl]-1,5,6,7-tetrahydro-4H-pyrrolo[3,2-C]pyridin-4-ones as CSNK1 inhibitors. World Intellectual Property Organization, WO2020161257 A1 2020-08-13.|[2]Steven M. Corsello, et al Abstract 3588: Discovery of potent and selective CSNK1A1 inhibitors for solid tumor therapy. Cancer Res 15 June 2022; 82 (12_Supplement) : 3588.|[3]Huang L, et al. Development of Oral, Potent, and Selective CK1α Degraders for AML Therapy. JACS Au. 2024 Nov 8;4 (11) :4423-4434.