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420148

JAK3/GSK-3β/PKCα Inhibitor

Name: JAK3/GSK-3β/PKCα Inhibitor
Brand: MM

The JAK3/GSK-3β/PKCα Inhibitor, also referenced under CAS 1260181-14-3, controls the biological activity of JAK3/GSK-3β/PKCα. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

JAK3/GSK-3β/PKCα Inhibitor, 3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione, JAK3 Inhibitor XII, NIBR3049, JAK3 Inhibitor XII, NIBR3049, 3-(5-(4-(2-Hydroxy-2-methyl-propionyl)-piperazin-1-yl)-2-trifluoromethyl-phenyl)-4-(1H-indol-3-yl)-pyrrole-2,5-dione

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About This Item

Empirical Formula (Hill Notation):

C₂₇H₂₅F₃N₄O₄

CAS Number:

1260181-14-3

Molecular Weight:

526.51

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD19380092

Assay:

≥95% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Properties

Quality Segment

100

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: soluble

shipped in

ambient

storage temp.

2-8°C

SMILES string

O=C1NC(C(C2=CNC3=C2C=CC=C3)=C1C4=CC(N5CCN(C(C(C)(C)O)=O)CC5)=CC=C4C(F)(F)F)=O

InChI

1S/C27H25F3N4O4/c1-26(2,38)25(37)34-11-9-33(10-12-34)15-7-8-19(27(28,29)30)17(13-15)21-22(24(36)32-23(21)35)18-14-31-20-6-4-3-5-16(18)20/h3-8,13-14,31,38H,9-12H2,1-2H3,(H,32,35,36)

InChI key

CLGRAWDGLMENOD-UHFFFAOYSA-N

Description

General description

A cell-permeable phenyl-indolyl maleimide compound that acts as a potent, ATP-binding site targeting and reversible inhibitor of GSK-3β, JAK3, PKCα and PKCθ (IC₅₀ = 3, 8, 13 and 68 nM, respectively) with excellent selectivity over 40-kinases, including JAK1, JAK2 and Tyk2 (IC₅₀ = 1.017, 2.55 and 8.055 µM, respectively). Shown to efficiently block interleukin stimulated STAT5 phosphorylation and T cell costimulation (IC₅₀ = 0.525, 1.294 and 0.689 µM in IL15-MO7, IL2-CTLL and TCR/CD28-Jurkat cells, respectively).

Packaging

Packaged under inert gas

Other Notes

Haan, C., et al. 2011. Chem. Biol.18, 314.
Thoma, G., et al. 2011. J. Med. Chem.54, 284.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c