CB-5083

CB-5083 is an orally bioavailable inhibitor of p97 (IC50 = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP). It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083 causes accumulation of poly-ubiquitinated proteins, retention of endoplasmic reticulum-associated degradation (ERAD) substrates, and activation of the apoptotic arm of the unfolded protein response.Formal Name: 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide. CAS Number: 1542705-92-9. Molecular Formula: C24H23N5O2. Formula Weight: 413.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. lambdamax: 245, 301 nm. SMILES: CC1=CC2=C(C=CC=C2C(N)=O)N1C3=NC(CCOC4)=C4C(NCC5=CC=CC=C5)=N3. InChi Code: InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28). InChi Key: RDALZZCKQFLGJP-UHFFFAOYSA-N.