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Merck
CN

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.

别名:

JAK3 Inhibitor VI

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关于此项目

经验公式（希尔记法）:
C18H13N3O · xCH4O3S
化学文摘社编号:
856436-16-3
分子量:
287.32 (free base basis)
MDL number:
MFCD09037543
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

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.

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

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

Quality Level

100

相关类别

Preparation Note

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

Legal Information

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

Biochem/physiol Actions

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

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

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.

Other Notes

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

Packaging

Packaged under inert gas

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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Satellite cells are the canonical muscle stem cells that regenerate damaged skeletal muscle. Loss of function of these cells has been linked to reduced muscle repair capacity and compromised muscle health in acute muscle injury and congenital neuromuscular diseases. To

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Pathways and Biomarkers of JAK/STAT Signaling

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JAK/STAT Signaling Research Focus

The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.

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