WHI-P 154 A JAK3 inhibitor which inhibits other common kinases

WHI-P 154 (CAS 211555-04-3)

WHI-P 154 | CAS 211555-04-3 is rated 5.0 out of 5 by 1.
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Synonym: 2-Bromo-4-[(6,7-dimethoxy-4-quinazo linyl)amino]phenol
Application: A JAK3 inhibitor which inhibits other common kinases
CAS Number: 211555-04-3
Molecular Weight: 376.2
Molecular Formula: C16H14BrN3O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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WHI-P 154 is a JAK3 inhibitor (IC50 = 1.8 μM) that displays no activity at JAK1 or JAK2. WHI-P 154 inhibits STAT1 activation, iNOS expression, and NO production in macrophages in vitro. WHI-P 154 induces apoptosis in human glioblastoma cell lines (IC50 = 158 μM). WHI-P 154 inhibits other common kinases including EGFR (IC50 = 4 nM), SRC, c-Abl, VEGFR, MAPK and PI 3-kinase.


References

Narla et al (1998) 4-(3'-bromo-4'hydroxylphenyl)-amino-6,7-dimethoxyquinazoline: a novel quinazoline derivative with potent cytotoxic activity against human glioblastoma cells. Clin.Cancer Res. 4 1405. Sareila et al (2008) Janus kinase 3 inhibitor WHI-P154 in macrophages activated by bacterial endotoxin: differential effects on the expression of iNOS, COX-2 and TNF-α. Int.Immunopharmacol. 8 100. Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM).
Storage :
Store at room temperature
IC50 :
JAK3: IC50 = 1.8 µM; EGFR: IC50 = 4 nM; induces apoptosis: IC50 = 158 µM (human glioblastoma cell lines); Tyrosine-protein kinase JAK2: IC50 = >10 µM (human); Tyrosine-protein kinase JAK1: IC50 = >10 µM (human); HFF : IC50 = 6.34 µM (human)
pK Values :
pKa: 8.57, pKb: 5.53
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
3795
MDL Number :
MFCD02179366
SMILES :
COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)O)Br)OC

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Certificate of Analysis

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Rated 5 out of 5 by from Various publications cite the use of WHI Various publications cite the use of WHI-P 154 due to its ability to interact with JAK3 and not JAK1 or JAK2. -SCBT Publication Review
Date published: 2015-04-16
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