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CAS No. : 2173556-69-7
MCE 国际站:PK68
产品活性:PK68 是一种高效、特异性的受体相互作用激酶 1 (RIPK1) 的 II 型抑制剂,具有口服活性。其 IC50 值约 90 nM,可抑制 RIPK1 依赖性坏死。PK68 对 TNF 诱导的全身炎症反应综合征有较强的改善作用,可用于炎症紊乱和肿瘤转移的研究。
研究领域:Apoptosis
作用靶点:RIP kinase
In Vitro: PK68 has highly potent inhibition of TNF-induced necroptosis with EC50 values of 23 nM and 13 nM in human and mouse cells, respectively.
PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC50 value of 90 nM.
PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation.
In Vivo: PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice.
PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome.
PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis.
相关产品:Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | NF-κB Signaling Compound Library | Anti-Cancer Compound Library | Orally Active Compound Library | Protein-protein Interaction Inhibitor Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | RIPA-56 | RIPK1-IN-3 | RIP1 kinase inhibitor 1 | Desmethyl-WEHI-345 analog | RIP2 kinase inhibitor 2 | PROTAC RIPK degrader-6 | TP-030-1 | RIPK1-IN-4 | MLKL-IN-4 | NecroIr2 | RIPK1-IN-14 | Oditrasertib | cRIPGBM chloride | KWCN-41 | GSK963 | AV123 | RIP2 Kinase Inhibitor 4 | Necrostatin 2 | RIPK1-IN-11 | RIP1 kinase inhibitor 5 | ICCB-19 hydrochloride | RIPK3-IN-2 | GSK2983559 active metabolite | OD36 | RIP2 kinase inhibitor 1 | GSK840 | RIPK1-IN-15 | Necroptosis-IN-1
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货号: HY-128348
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