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WHI-P97

  Cat. No.:  DC9494   Featured
Chemical Structure
211555-05-4
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More than 5000 active chemicals with high quality for research!
Field of application
WHI-P97 is a rationally designed potent inhibitor of JAK-3.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 211555-05-4
Synonyms: WHI-P-97;WHI P97
SMILES: BrC1=CC(NC2=NC=NC3=CC(OC)=C(OC)C=C32)=CC(Br)=C1O
Formula: C16H13Br2N3O3
M.Wt: 455.1007
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: WHI-P97 is a rationally designed potent inhibitor of JAK-3.Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.
Target: JAK3:11 μM (IC50)
References: [1]. Ji KA, Yang MS, Jou I, Shong MH, Joe EH.Thrombin induces expression of cytokine-induced SH2 protein (CIS) in rat brain astrocytes: involvement of phospholipase A2, cyclooxygenase, and lipoxygenase.Glia. 2004 Nov 1;48(2):102-11. [2]. Wong WS, Leong KP.Tyrosine kinase inhibitors: a new approach for asthma.Biochim Biophys Acta. 2004 Mar 11;1697(1-2):53-69. [3]. Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, Navara CS, Narla RK.Structure-based design of novel anticancer agents.Curr Cancer Drug Targets. 2001 May;1(1):59-71. [4]. Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.Clin Cancer Res. 1999 Jun;5(6):1569-82.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC72210 NDI-034858(Zasocitinib) NDI034858 is a TYK2 inhibitor, target TYK2 JH2 domain with binding constant Kd of <200 pM.
DC72043 VVD-118313 VVD-118313 (compound 5a) is a potent, selective JAK1 inhibitor. VVD-118313 targets an isoform-restricted allosteric cysteine to block JAK1-dependent trans-phosphorylation and cytokine signaling. VVD-118313 can be used for research of cancer.
DC70831 TD-1473 TD-1473 (Izencitinib, TD1473, JNJ 8398) is a potent, selective, oral gut-selective pan-JAK inhibitor with pKi of 10.0/10.0/8.8/9.5 for human recombinant JAK1, JAK2, JAK3 and TYK2.TD-1473 inhibited cytokine-induced phosphorylation of STAT1 in mouse primary colonic epithelial cells with pIC50 values for inhibition against IL-6, IFNα and IFNγ were 7.3, 6.8 and 7.0.TD-1473 demonstrated JAK inhibitory activity in ex vivo mouse colon and human IBD patient colonic tissue. TD-1473 (Izencitinib) is under development for the treatment of ulcerative colitis.
DC70233 AZD4604 AZD4604 (AZD-4604) is a potent, selective Janus-associated kinase 1 (JAK1) inhibitor with anti-inflammatory effect.
DC47591 JAK-IN-14 JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).
DC47132 JAK1-IN-8 JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.
DC47066 Ifidancitinib Ifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Ifidancitinib can be used in studies of allergies, asthma and autoimmune diseases.
DC47038 Fosifidancitinib Fosifidancitinib is a potent and selective inhibitor of JAK kinases 1/3. Fociatinib is used in studies of allergies, asthma and autoimmune diseases.
DC40513 BD750 BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
DC40459 FM-479 FM-479 is the negative control of FM-381 and has no activity on JAK3 or other kinases.
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