Preferred Label : CK1 Alpha Degrader CC-91633;
NCIt synonyms : CK1a Degrader CC-91633; CK1 Alpha Degrader BMS986397;
NCIt definition : An orally bioavailable degrader of casein kinase 1 alpha (CK1alpha; CK1a), with potential
antineoplastic activity. Upon oral administration, CK1a degrader CC-91633 binds to
and degrades CK1a, thereby inhibits the activity of CK1a. This prevents the enhanced
binding of murine double minute X (MDMX) to p53, reduces the formation of CK1a and
MDM2 complex, and prevents the interaction of MDM2 with p53. This prevents the inhibition
of p53 and increases p53 activity. This induces p53-mediated cell cycle arrest, thereby
inhibiting tumor cell proliferation. CK1a, a serine/threonine kinase and a leukemic
stem cell target, acts as a tumor suppressor in several cancers through the negative
regulation of Wnt/beta-catenin signaling and p53. It negatively regulates p53 by phosphorylating
MDMX, thus enhancing binding of MDMX to p53, as well as by forming a complex with
MDM2.;
Molecule name : CC-91633; BMS-986397; CC 91633; BMS 986397;
NCI Metathesaurus CUI : CL1778256;
Origin ID : C185875;
UMLS CUI : C5667041;
Semantic type(s)
- chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
