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Merck

420101

JAK3 Inhibitor I

The JAK3 Inhibitor I, also referenced under CAS 202475-60-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

JAK3 Inhibitor I, 4-(4ʹ-Hydroxyphenyl)amino-6,7-dimethoxyquinazoline, WHI-P131

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About This Item

Empirical Formula (Hill Notation):
C16H15N3O3
CAS Number:
Molecular Weight:
297.31
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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SMILES string

N(c3ccc(cc3)O)c1ncnc2c1cc(c(c2)OC)OC

InChI

1S/C16H15N3O3/c1-21-14-7-12-13(8-15(14)22-2)17-9-18-16(12)19-10-3-5-11(20)6-4-10/h3-9,20H,1-2H3,(H,17,18,19)

InChI key

HOZUXBLMYUPGPZ-UHFFFAOYSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to off-white

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Janus family kinase 3
Product competes with ATP.
Reversible: yes
Target IC50: 78 µM against Janus family kinase 3

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3; IC50 = 78 µM). Has no effect on JAK1, JAK2, or Zap/Syk or Src tyrosine kinases. Acts as a potent inhibitor of glioblastoma cell adhesion and migration. Also reported to block thrombin-induced platelet aggregation.

Other Notes

Tibbles, H.E., et al. 2001. J. Biol. Chem.276, 17815.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res.5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin. Cancer Res. 4, 2463.

Packaging

Packaged under inert gas

Legal Information

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

Storage Class

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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Related Content

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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