CBL0137 (hydrochloride)

Curaxins are small molecules that simultaneously activate p53 and inhibit NF-kappaB without causing detectable genotoxicity. CBL0137 is a water soluble and metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-kappaB with an EC50 value of 0.47 µM. It functionally inactivates the facilitates chromatin transcription complex, driving the effects on p53 and NF-kappaB and promoting cancer cell death. CBL0137 has broad anticancer activity in mice when administered orally, eradicates drug-resistant cancer stem cells, and potentiates efficacy of gemcitabine (Cay-11690) in preclinical models of pancreatic cancer.Formal Name: 1,1'-[9-[2-[(1-methylethyl)imino]ethyl]-9H-carbazole-3,6-diyl]bis-ethanone, monohydrochloride. CAS Number: 1197397-89-9. Synonyms: CBLC137, Curaxin 137. Molecular Formula: C21H24N2O2 . HCl. Formula Weight: 372.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 25 mg/ml, PBS (pH 7.2): 1 mg/ml. lambdamax: 259, 290, 327 nm. SMILES: CC(C1=CC=C2C(C(C=C(C(C)=O)C=C3)=C3N2CCNC(C)C)=C1)=O.Cl. InChi Code: InChI=1S/C21H24N2O2.ClH/c1-13(2)22-9-10-23-20-7-5-16(14(3)24)11-18(20)19-12-17(15(4)25)6-8-21(19)23,/h5-8,11-13,22H,9-10H2,1-4H3,1H. InChi Key: IXRKBBVMDMKAEB-UHFFFAOYSA-N.