WHI-P 154

Pricing Availability   Qty
Description: JAK3 kinase inhibitor. Also inhibits EGFR
Chemical Name: 2-Bromo-4-[(6,7-dimethoxy-4-quinazolinyl)amino]phenol
Purity: ≥99% (HPLC)
Pathways (1)

Biological Activity for WHI-P 154

WHI-P 154 is a JAK3 inhibitor (IC50 = 1.8 μM) that displays no activity at JAK1 or JAK2. Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. Also inhibits other common kinases including EGFR (IC50 = 4 nM), Src, Abl, VEGFR, MAPK and PI 3-K and induces apoptosis in human glioblastoma cell lines (IC50 = 158 μM). Induces differentiation of neural progenitor cells.

Technical Data for WHI-P 154

M. Wt 376.2
Formula C16H14BrN3O3
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 211555-04-3
PubChem ID 3795
Smiles OC(C=C3)=C(Br)C=C3NC2=NC=NC1=CC(OC)=C(OC)C=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WHI-P 154

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 37.62 100

Preparing Stock Solutions for WHI-P 154

The following data is based on the product molecular weight 376.2. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.66 mL 13.29 mL 26.58 mL
5 mM 0.53 mL 2.66 mL 5.32 mL
10 mM 0.27 mL 1.33 mL 2.66 mL
50 mM 0.05 mL 0.27 mL 0.53 mL

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References for WHI-P 154

References are publications that support the biological activity of the product.

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 PMID: 9626456

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 PMID: 18068105

Changelian et al (2008) The specificity of JAK3 kinase inhibitors. Blood 111 2155 PMID: 18094329

Kim et al (2010) Differential regulation of proliferation and differentiation in neural precursor cells by the Jak pathway. Stem Cells. 28 1816 PMID: 20979137

If you know of a relevant reference for WHI-P 154, please let us know.

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Citations for WHI-P 154

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Pathways for WHI-P 154

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.