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WHI-P154

SKU: orb1306845

Description

WHI-P154 is a potent and selective small molecule inhibitor of Janus kinase 3 (JAK3). It is a valuable research tool for studying JAK-STAT signaling in immunology and oncology, with utility in both cellular assays and in vivo models of inflammation and immune function.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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WHI-P154

Key Properties

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CAS Number211555-04-3
MW376.2
Purity98.00% (May vary between batches)
FormulaC16H14BrN3O3
SMILESCOc1cc2ncnc(Nc3ccc(O)c(Br)c3)c2cc1OC
TargetSrc,JAK,EGFR,VEGFR,Apoptosis
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.32 mM);DMSO:50 mg/mL (132.91 mM)

Bioactivity

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Target IC50
Src:100 nM|JAK3:1.8 μM|EGFR:4 nM|VEGFR:100 nM
In Vivo
The in vitro anti-glioblastoma activity of WHI-P154 was amplified > 200-fold and was selective by binding to recombinant human-derived epidermal growth factor. WHI-P154 inhibited STAT1 activation, iNOS expression and NO production in macrophages in vitro. WHI-P154 was shown to inhibit other common kinases, including EGFR, Src, Abl, VEGFR, MAPK and PI3-K, and induced apoptosis in human glioblastoma cell lines.WHI-P154 inhibited the adhesion and migration of glioblastoma cells in the ECM. WHI-P154 was significantly cytotoxic to human malignant glioma cell lines U373 and U87, causing apoptotic cell death at micromolar concentrations.
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In Vitro
The in vitro anti-glioblastoma activity of WHI-P154 was amplified > 200-fold and was selective by binding to recombinant human-derived epidermal growth factor. WHI-P154 inhibited STAT1 activation, iNOS expression and NO production in macrophages in vitro. WHI-P154 was shown to inhibit other common kinases, including EGFR, Src, Abl, VEGFR, MAPK and PI3-K, and induced apoptosis in human glioblastoma cell lines.WHI-P154 inhibited the adhesion and migration of glioblastoma cells in the ECM. WHI-P154 was significantly cytotoxic to human malignant glioma cell lines U373 and U87, causing apoptotic cell death at micromolar concentrations.
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Cell Research
Cells are seeded into a 96-well plate at a density of 2.5×104 cells/well and incubated for 36 h at 37 ℃ before drug exposure. On the day of treatment, culture medium is carefully aspirated from the wells and replaced with fresh medium containing the quinazoline compounds WHI-P154 at concentrations ranging from 0.1 μM to 250 μM. Triplicate wells are used for each treatment. The cells are incubated with the compound for 24hours to 36hours at 37 ℃ in a humidified 5% CO2 atmosphere. To each well, 10 μL of MTT (final concentration, 0.5 mg/mL) is added, and the plate are incubated at 37 ℃ for 4 h. Than solubilized overnight at 37 ℃ in a solution containing 10% SDS in 0.01 M HCL. The absorbance of each well is measured in a microplate reader at 570 nm.(Only for Reference)
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Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Apoptosis, inhibit, JAK3, Jak3 inhibitor ii, Janus kinase, JAK, Inhibitor, HER1, EGFR, Epidermal growth factor receptor, ErbB-1, WHI P154, WHI-P 154, WHIP154, WHI-P154, WHI-P-154, Src, VEGFR

Similar Products

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  • WHI-P154

    WHI-P154 [orb1225686]

    >98% (HPLC)

    211555-04-3

    376.2

    C16H14BrN3O3

    2 mg, 5 mg, 10 mg, 1 g, 500 mg, 200 mg, 25 mg, 50 mg, 100 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
3795 ↗

Key Properties

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No computed properties available.

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WHI-P154 (orb1306845)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
¥ 1,040.00
1 ml x 10 mM (in DMSO)
¥ 1,300.00
5 mg
¥ 1,300.00
10 mg
¥ 1,690.00
25 mg
¥ 2,990.00
50 mg
¥ 4,420.00
100 mg
¥ 6,240.00
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