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420146

JAK3 Inhibitor VIII, NSC114792

Name: JAK3 Inhibitor VIII, NSC114792
Brand: MM

The JAK3 Inhibitor VIII, NSC114792 controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

JAK3 Inhibitor VIII, NSC114792, 10,13-Dimethyl-17-(2-(6-sulfanylidene-3H-purin-9-yl)acetyl)-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one, Dimethyl-sulfanylidene-purinyl-acetyl-dodecahydrocyclopenta[a]phenanthren-3-one

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About This Item

Empirical Formula (Hill Notation):

C₂₆H₃₂N₄O₂S

CAS Number:

17392-79-9

Molecular Weight:

464.62

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥99% (HPLC)

Form:

powder

Storage condition:

OK to freeze, protect from light

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Properties

Quality Segment

100

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

yellow-white

solubility

DMSO: 10 mg/mL

shipped in

wet ice

storage temp.

2-8°C

SMILES string

O=C1CCC2(C)C(CCC3C2CCC4(C)C3CCC4C(CN5C(NC=NC6=S)=C6N=C5)=O)=C1

Description

General description

A cell-permeable steroidal-purinethione compound that targets JAK3 kinase domain and selectively inhibits JAK3, but not JAK1, JAK2, or TYK2, activity in cell-free immuncomplex kinase assays, and effectively blocks the constitutive Jak3 and STAT5 phosphorylations (complete inhibition at 10 µM) in BaF3-JAK3^V674A and BLNK^-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3^WT, BaF3-JAK3^V674A, and BLNK^-/- BKO84 cells in a time- and dose-dependent manner (by 40%, 50%, 57%, and 85%, respectively, after 72 h incubation with 20 µM inhibitor), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures.

A cell-permeable steroidal-purinethione that targets JAK3 kinase domain and selectively inhibits JAK3, but not JAK1, JAK2, or TYK2, activity and effectively blocks the constitutive Jak3 and STAT5 phosphorylations (complete inhibition at 10 µM) in BaF3-JAK3^V674A and BLNK^-/- BKO84 culltures. Shown to prevent the JAK3-dependent survival of L540, BaF3-JAK3^WT, BaF3-JAK3^V674A, and BLNK^-/- BKO84 cells (by 40%, 50%, 57%, and 85%, respectively; 20 µM; 72 h), while exhibiting no effect against the JAK3-independent growth in DU145, HDLM-2, and MDA-MB-468 cultures.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Kim, B.H., et al. 2010. Mol. Cancer9, 36.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c