MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Ixazomib citrate

CAS No. : 1239908-20-3

MCE 站：Ixazomib citrate

产品活性：Ixazomib citrate (MLN9708) 是 20S蛋白酶体胰凝乳蛋白酶样蛋白水解β5位点的可逆抑制剂，IC₅₀ 为3.4 nM和K_i为0.93 nM。

研究领域：Metabolic Enzyme/Protease  |  Autophagy

作用靶点：Proteasome  |  Autophagy

In Vitro: Ixazomib citrate (MLN9708; 0.20-3.20 µM) inhibits the cell growth of both cell lines effectively in a time- ａnd dose-dependent manner. Ixazomib induces cell cycle arrest in MG-63 ａnd Saos-2 cells. Ixazomib induces apoptosis mainly through the caspases pathway ａnd requires the activation of both caspase8 ａnd caspase9. Ixazomib treatment increases the levels of pro-apoptotic proteins ａnd down regulates the anti-apoptotic proteins that control MOMP. Ixazomib treatment induces the release of Cytc, Smac, OMI from mitochondria ａnd decreases the protein levels of XIAP. Ixazomib inhibits the invasion ability of MG-63 ａnd Saos-2 cells ａnd decreases both the expression ａnd secretion levels of MMP2/9.Ixazomib citrate (MLN9708; 12 nM) shows inhibitory activity against C-L ａnd T-L proteasome activities. Treatment of H929 ａnd MM.1S MM cells with Ixazomib triggers a marked increase in proteolytic cleavage of poly(ADP) ribose polymerase (PARP), a signature event during apoptosis. Ixazomib induces cleavage of caspase-3, an upstream activator of PARP. Ixazomib induces eIf2-α kinase activity ａnd protein levels of Bip ａnd CHOP/GADD153. Ixazomib blocks BMSCs-induced MM cell proliferation, inhibits in vitro capillary tubule formation, ａnd target NF-κB.

In Vivo: Ixazomib citrate (MLN9708; 11 mg/kg) significantly inhibits MM tumor growth ａnd prolongs survival in the human plasmacytoma MM.1S xenograft mouse model. The blood chemistry profiles of Ixazomib-treated mice show normal levels of creatinine, hemoglobin, ａnd bilirubin. Ixazomib dramatically increases the number of cleaved-caspase-3 positive cells of the xenograft model.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Ubiquitination Compound Library  |  Anti-COVID-19 Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Blood Cancer Compound Library  |  Targeted Therapy Drug Library   |  MG-132  |  Bortezomib  |  Tripterin  |  Pepstatin Trifluoroacetate  |  MDL-28170  |  Epoxomicin  |  Calpeptin  |  MG-101  |  PD150606  |  Aclacinomycin A hydrochloride  |  Gabexate mesylate  |  PD 151746  |  4＇-Hydroxychalcone  |  TCH-165  |  VR23  |  Tomatine  |  Lactacystin  |  18α-Glycyrrhetinic acid  |  (Rac)-Calpain Inhibitor XII  |  (1S,2S)-Bortezomib  |  Acetyl-Calpastatin(184-210)(human)  |  ALLM  |  PR-39  |  PR-924  |  PTP1B-IN-9

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。