BAY-888

• Description :

  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 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, sealed storage, away from moisture and light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [2468783-75-5]