1260181-14-3

1260181-14-3 structure

Name: TCS 21311
Chemical Name: 3-[5-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
CAS Number: 1260181-14-3
Molecular Formula: C₂₇H₂₅F₃N₄O₄
Molecular Weight: 526.50700
Catalog: Signaling Pathways Epigenetics JAK
Create Date: 2016-11-15 04:07:47
Modify Date: 2025-08-25 07:53:56
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively[1].

Name	3-[5-[4-(2-hydroxy-2-methylpropanoyl)piperazin-1-yl]-2-(trifluoromethyl)phenyl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
Synonyms	NIBR-3049

Description	TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively[1].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Signaling Pathways >> Stem Cell/Wnt >> GSK-3 Signaling Pathways >> JAK/STAT Signaling >> JAK Signaling Pathways >> Epigenetics >> JAK Signaling Pathways >> Stem Cell/Wnt >> JAK Research Areas >> Others Signaling Pathways >> TGF-beta/Smad >> PKC Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3
Target	JAK3:8 nM (IC50) JAK2:2.55 μM (IC50) JAK1:1.017 μM (IC50) PKCα:13 nM (IC50) PKCθ:68 nM (IC50) GSK-3β:3 nM (IC50)
In Vitro	TCS 21311 (NIBR3049) exhibits IC50 values of 1.017, 2.550 and 8.055 μM for JAK1, JAK2 and TYK2, respectively in a enzymatic Jak assay[1]. TCS 21311 (NIBR3049) shows moderate activity in this cellular assay (IC50=689 nM, Jurkat cells), which is in good agreement with its enzymatic Pkc activity[1].
References	[1]. Thoma G, et al. Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.J Med Chem. 2011 Jan 13;54(1):284-8.