化合物ONX0914 T6029

Product Introduction
Bioactivity


英文名: ONX-0914

描述: ONX-0914 (PR-957) 是选择性的低分子量多肽-7(LMP7)的抑制剂，LMP7 是免疫蛋白酶体的类糜蛋白酶亚单位。它是分枝杆菌蛋白酶体的非竞争性不可逆抑制剂，Ki 值为5.2 μM。它通过 HSF-1 介导的 p-TEFb 活化激活潜伏的 HIV-1。

激酶实验: 20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.

体外活性: Selective inhibition of LMP7 by PR-957 blocked production of interleukin-23 (IL-23) by activated monocytes and interferon-gamma and IL-2 by T cells.

体内活性: 在类风湿性关节炎和红斑狼疮的小鼠模型中，ONX-0914的最大耐受剂量(MTD)为每千克体重30 mg/kg。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 35 mg/mL


关键字: HIV | Inhibitor | Proteasome | inhibit | Bacterial | ONX-0914 | PR957 | PR 957 | Human immunodeficiency virus

相关产品: RA375 | NDMC101 | Teneligliptin hydrobromide | DD1 | Z-GGF-CMK | PR 39 (porcine) acetate | Epoxomicin | TCH-165 | VR23 | Alloxan monohydrate

相关库: Anti-COVID-19 Compound Library | Inhibitor Library | Anti-Cancer Active Compound Library | Protease Inhibitor Library | Preclinical Compound Library | NO PAINS Compound Library | Anti-Viral Compound Library | Covalent Inhibitor Library | Nonsteroidal Anti-Inflammatory Compound Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途