TCS 21311

TCS 21311 is an inhibitor of JAK3 (IC50 = 8 nM in an enzyme assay). It is selective for JAK3 over JAK1, JAK2, and tyrosine kinase 2 (TYK2, IC50s = 1,017, 2,550, and 8,055 nM, respectively) but does inhibit glycogen synthase kinase 3beta (GSK-3beta), PKCalpha, and PKCtheta (IC50s = 13, 68, and 3 nM, respectively). TCS 21311 inhibits cytokine-induced STAT5 phosphorylation, a JAK3-dependent activity, in CTLL and M-07 cells (IC50s = 1,294 and 525 nM, respectively) and inhibits TCR/CD28-mediated T cell activation, a PCK-dependent activity, in Jurkat cells (IC50 = 689 nM). It also increases proliferation of mouse embryonic nephron progenitor cells (NPCs) and NPCs derived from human induced pluripotent stem cells (iPSCs) in the absence of bone morphogenic protein 7 (BMP7) when used at a concentration of 0.3 µM.Formal Name: 3-[5-[4-(2-hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione. CAS Number: 1260181-14-3. Synonyms: NIBR3049. Molecular Formula: C27H25F3N4O4. Formula Weight: 526.5. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50 mg/ml. lambdamax: 266 nm. SMILES: O=C(N1)C(C2=CNC3=CC=CC=C32)=C(C4=C(C(F)(F)F)C=CC(N5CCN(C(C(C)(O)C)=O)CC5)=C4)C1=O. InChi Code: InChI=1S/C27H25F3N4O4/c1-26(2,38)25(37)34-11-9-33(10-12-34)15-7-8-19(27(28,29)30)17(13-15)21-22(24(36)32-23(21)35)18-14-31-20-6-4-3-5-16(18)20/h3-8,13-14,31,38H,9-12H2,1-2H3,(H,32,35,36). InChi Key: CLGRAWDGLMENOD-UHFFFAOYSA-N.