TPCA-1

TPCA-1 is a selective inhibitor of IkappaB kinase-2 (IC50s = 17.9 nM and 0.40 µM for IKK2 and IKK1, respectively). Furthermore, it displays greater than 550-fold selectivity over other kinases and enzymes including, p38, MAPK, COX, and JNK. TPCA-1 inhibits the production of LPS-induced TNF-alpha, IL-6, and IL-8 with IC50 values equal to 0.17, 0.29, and 0.32 µM, respectively. At 20 mg/kg, TPCA-1 has been used to reduce the severity and onset of collagen-induced arthritis in mice and at 30 mg/kg to block cytokine release in an antigen-driven rat model of lung inflammation.Formal Name: 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide. CAS Number: 507475-17-4. Synonyms: IKK2 Inhibitor IV. Molecular Formula: C12H10FN3O2S. Formula Weight: 279.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16.6 mg/ml, DMSO: 16.6 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 232, 312 nm. SMILES: FC1=CC=C(C2=CC(C(N)=O)=C(NC(N)=O)S2)C=C1. InChi Code: InChI=1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18). InChi Key: SAYGKHKXGCPTLX-UHFFFAOYSA-N.