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420126

Sigma-Aldrich

JAK3 Inhibitor VI

The JAK3 Inhibitor VI, also referenced under CAS 856436-16-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

JAK3 Inhibitor VI

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About This Item

Empirical Formula (Hill Notation):
C18H13N3O · xCH4O3S
CAS Number:
Molecular Weight:
287.32 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

solid

potency

27 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

yellow

solubility

water: 1 mg/mL
DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C18H13N3O.CH4O3S/c22-18-16(10-14-4-2-8-20-14)15-9-12(5-6-17(15)21-18)13-3-1-7-19-11-13;1-5(2,3)4/h1-11,20H,(H,21,22);1H3,(H,2,3,4)/b16-10-;

InChI key

ZUDPNBZMAJGYTE-HYMQDMCPSA-N

General description

A cell-permeable 3′-pyridyl oxindole compound that acts as a potent and reversible inhibitor of JAK3 (IC50 = 27 nM)and displays ~16-fold greater selectivity over JAK2. Binds to the enzyme active site and prevents IL-2-induced cellular phosphorylation of JAK3 and STAT5. Inhibits IL-2-induced cell proliferation (IC50 = 760 and 250 nM for mouse CTLL and human T-cells, respectively) and alleviates oxazolone-induced ear odema in mouse with an efficacy comparable to that of Dexamethasone (Cat. No. 265005).
A cell-permeable, potent, and reversible inhibitor of Janus kinase 3 (JAK3) (IC50 = 27 nM). Reported to bind to the enzyme active site and prevent IL-2-induced phosphorylation of JAK3 and STAT5. Also reported to inhibit IL-2-induced cell proliferation (IC50 = 760 nM for murine CTLL cells and 250 nM for human T-cells). Shown to alleviate oxazolone-induced ear edema in mice with an efficacy comparable to Dexamethasone (Cat. No. 265005) and displays ~16-fold greater selectivity over JAK2.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
JAK-3
Product does not compete with ATP.
Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Chen, J., et al. 2006. Bioorg. Med. Chem. Lett. In press.
Adams, C., et al. 2003. Bioorg. Med. Chem. Lett.13, 3105.

Legal Information

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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