TCS 21311

Modify Date: 2024-01-04 18:24:08

TCS 21311 Structure
TCS 21311 structure
Common Name TCS 21311
CAS Number 1260181-14-3 Molecular Weight 526.50700
Density N/A Boiling Point N/A
Molecular Formula C27H25F3N4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of TCS 21311


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].

 Names

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

 TCS 21311 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C27H25F3N4O4
Molecular Weight 526.50700
Exact Mass 526.18300
PSA 109.23000
LogP 3.45220

 Synonyms

NIBR-3049
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