JH-X-119-01 是一种有效的选择性白介素 1 受体相关激酶 1 (IRAK1) 抑制剂。JH-X-119-01 可改善 LPS 诱导的小鼠败血症。JH-X-119-01 抑制 IRAK1，IC₅₀ 为 9 nM，而在浓度高达 10 μM 时对 IRAK4 也没有抑制作用。

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC 50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM.

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IRAK-1 9 nM (IC50)

JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation.JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4.JH-X-119-01 shows moderate cell killing effects in a panel of Waldenstr?m’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only. Anima

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[1]. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597.
[2]. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243.

In Vitro: DMSO : 250 mg/mL (552.54 mM; Need ultrasonic)配制储备液