PS-1145

PS-1145 is an IkappaB kinase beta (IKKbeta) inhibitor (IC50 = 88 nM). It selectively inhibits IKKbeta over a panel of 14 kinases (IC50s = >100 nM for all). PS-1145 also inhibits the IKK complex (IC50 = 100 nM). It inhibits the proliferation of MM.1S, U266, and RPMI-8226 myeloma cells when used at concentrations ranging from 1.5 to 50 µM. PS-1145 inhibits TNF-alpha-induced activation of NF-kappaB in MM.1S cells in a concentration-dependent manner. It inhibits RANKL-induced differentiation of RAW 264.7 cells into osteoclasts when used at concentrations of 5 and 10 µM. PS-1145 (10 µM) inhibits RANKL-induced phosphorylation of IkappaBalpha, ERK, and JNK in RAW 264.7 cells.Formal Name: N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)-3-pyridinecarboxamide. CAS Number: 431898-65-6. Synonyms: IKK Inhibitor X. Molecular Formula: C17H11ClN4O. Formula Weight: 322.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 10 mg/ml. lambdamax: 239, 293, 364 nm. SMILES: O=C(NC1=CC(Cl)=CC2=C1NC3=C2C=CN=C3)C4=CN=CC=C4. InChi Code: InChI=1S/C17H11ClN4O/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10/h1-9,21H,(H,22,23). InChi Key: JZRMBDHPALEPDM-UHFFFAOYSA-N.