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TCS 21311

Names

[ CAS No. ]:
1260181-14-3

[ Name ]:
TCS 21311

[Synonym ]:
NIBR-3049

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]:

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C27H25F3N4O4

[ Molecular Weight ]:
526.50700

[ Exact Mass ]:
526.18300

[ PSA ]:
109.23000

[ LogP ]:
3.45220

Related Compounds