A JAK3 inhibitor (IC50 = 8 nM); selective for JAK3 over JAK1

TCS 21311 – 5 mg

Brand:
Cayman
CAS:
1260181-14-3
Storage:
-20
UN-No:
Non-Hazardous - /

TCS 21311 is an inhibitor of JAK3 (IC50 = 8 nM in an enzyme assay).{53897} 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 3β (GSK-3β), PKCα, and PKCθ (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.{53898}  

 

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SKU: 30063 - 5 mg Category:

Description

A JAK3 inhibitor (IC50 = 8 nM); selective for JAK3 over JAK1, JAK2, and TYK2 (IC50s = 1,017, 2,550, and 8,055 nM, respectively) but does inhibit GSK-3β, PKCα, and PKCθ (IC50s = 13, 68, and 3 nM, respectively); inhibits cytokine-induced STAT5 phosphorylation in CTLL and M-07 cells (IC50s = 1,294 and 525 nM, respectively) and TCR/CD28-mediated T cell activation in Jurkat cells (IC50 = 689 nM); increases proliferation of mouse embryonic NPCs and human iPSC-derived NPCs in the absence of BMP7 at 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

Synonyms:  NIBR3049

Molecular weight: 526.5

CAS: 1260181-14-3

Purity: ≥95%

Formulation: A solid

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