2468783-75-5
Chemical Structure
BAY-888
Synonym(s): BRD5846
- CAS. Nr.: 2468783-75-5
- Formula:C28H26FN5O2
- Molecular Weight:483.54
IUPAC Name: (S)-2-(4-fluorophenyl)-N-(4-(5-methyl-4-oxo-3-(phenylamino)-4,5,6,7-tetrahydro-1H-pyrrolo[3,2-c]pyridin-2-yl)pyridin-2-yl)propanamide
InChIKey: UYAQWCZWVIFRCN-KRWDZBQOSA-N
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
Biological Activity: 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].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
BAY-888 | 98.27% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [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. [Content Brief]
