Drug intelligence / Profile preview

TCS21311

Development stage
Unknown
Modality
Small Molecules
01

Overview

TCS21311 (also known as NIBR3049) is a potent, highly selective small molecule inhibitor of Janus kinase 3 (JAK3) with an IC50 of 8 nM. It exhibits greater than 100-fold selectivity for JAK3 over other JAK family kinases, including JAK1, JAK2, and TYK2. Additionally, TCS21311 inhibits glycogen synthase kinase 3 beta (GSK-3β) and protein kinase C (PKC) isoforms, specifically PKCα and PKCθ. Originally developed by Novartis, TCS21311 has been utilized in research settings to study JAK/STAT signaling and T-cell activation. In regenerative medicine research, TCS21311 has been shown to replace bone morphogenetic protein 7 (BMP7) in expansion cultures, facilitating the proliferation of mouse embryonic and human induced pluripotent stem cell (iPSC)-derived nephron progenitor cells (NPCs) via the JAK3-STAT3 pathway.

Other names
3-[5-[4-(2-hydroxy-2-methyl-1-oxopropyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione3-[5-[4-(2-hydroxy-2-methylpropanoyl)-1-piperazinyl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
02

Targets

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