420126
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)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
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
SMILES string
[S](=O)(=O)(O)C.[nH]1c(ccc1)\C=C2\c3c(ccc(c3)c4cnccc4)NC\2=O
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
JAK-3
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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.
Adams, C., et al. 2003. Bioorg. Med. Chem. Lett.13, 3105.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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