Western blot analysis of extracts from KARPAS 299 cells, untreated (-) or treated with WHI-P131 (50 μM, 1hr; +), using Phospho-Stat3 (Tyr705) (D3A7) XP® Rabbit mAb #9145 (upper), Stat3 (D3Z2G) Rabbit mAb #12640 (middle), or β-Actin (D6A8) Rabbit mAb #8457 (lower).
Chemical structure of WHI-P131.
WHI-P131 is supplied as a lyophilized powder. For a 15 mM stock, reconstitute 5 mg of powder in 998 μl of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.
Store lyophilized at 4ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 2 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
Molecular Weight: 333.8 g/mol
Molecular Formula: C16H15N3O3 • HCl
Solubility: Soluble in DMSO at 50 mg/ml.
WHI-P131 is a potent and selective inhibitor of Janus kinase 3 (Jak3) (IC50 = 78 μM) and glioblastoma cell adhesion and migration (1,2). This novel quinazoline derivative inhibits the enzymatic activity of constitutively active Jak3 without affecting Jak1, Jak2, or other family tyrosine kinases (1). WHI-P131 has also been shown to inhibit thrombin-induced tyrosine phosphorylation of Stat1 and Stat3. These properties make this compound useful when studying different diseases such as acute lymphoblastic leukemia, glioblastoma multiforme, and thromboembolism (1-3).
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