化合物Ixazomib Citrate T2016

Product Introduction
Bioactivity


英文名: MLN9708

描述: MLN9708 (Ixazomib Citrate) 抑制 20S 蛋白酶体的糜蛋白酶样蛋白水解 (β5) 位点 (Ki50=0.93 nM, IC50=3.4 nM/)。 MLN9708 的生物活性形式是水溶液或血浆中的 MLN2238。

细胞实验: Calu-6 cells are cultured in MEM containing 10% FBS and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. For IC50 determinations, cells are treated with varying concentrations of Bortezomib or MLN2238 in DMSO (0.5% final, v/v) for 1 hour at 37 °C. For reversibility experiments, cells are treated with either 1 μM Bortezomib or MLN2238 for 30 minutes at 37 °C and then washed thrice in medium to remove the Bortezomib or MLN2238. Cells are incubated for an additional 4 hours at 37 °C, after which the medium is removed and replaced with fresh medium. (Only for Reference)

激酶实验: Kinase assay: Calu-6 cells are cultured in MEM containing 10% fetal bovine serum and 1% penicillin/streptomycin and plated 1 day before the start of the experiment at 1 × 104 cells per well in a 384-well plate. Proteasome activity is assessed by monitoring hydrolysis of the chymotrypsin-like substrate Suc-LLVY-aminoluciferin in the presence of luciferase using the Proteasome-Glo assay reagents according to the manufacturer's instructions. Luminescence is measured using a LEADseeker instrument.

体外活性: 在多种实体瘤和血液移植瘤中,MLN9708有抗癌活性.

体内活性: MLN9708与水溶液和血浆接触后, MLN9708快速水解为具有生物活性的MLN2238。MLN2238抑制20S蛋白酶体的糜蛋白酶类水解位点（IC50=3.4 nM,Ki=0.93 nM）。MLN2238也抑制20S蛋白酶体的caspase类水解的位点（IC50=31 nM）和胰蛋白酶类水解的位点（IC50=3.5 μM）。

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

溶解度: DMSO : 93 mg/mL (179.8 mM)


关键字: MLN 9708 | MLN-9708 | MLN9708

相关产品: Z-LLF-CHO | Proteasome-IN-5 | Teneligliptin hydrobromide | PD 151746 | KZR-504 | Talabostat mesylate | Davelizomib | Gly-Pro-pNA hydrochloride | N-alpha-Tosyl-L-lysine chloromethyl ketone hydrochloride | 20S Proteasome activator 1

相关库: Drug Repurposing Compound Library | HIF-1 Signaling Pathway Compound Library | Drug-induced Liver Injury (DILI) Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Ubiquitination Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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