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。

Maritoclax

CAS No. : 1227962-62-0

MCE 站：Maritoclax

产品活性：Maritoclax (Marinopyrrole A) 是一种新颖的 Mcl-1 特异性抑制剂，IC₅₀ 值为 10.1 μM，对 BCL-xl 的 IC₅₀ 值 > 80 μM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vitro: Maritoclax (Marinopyrrole A) blocks the binding of Bim BH3 α-helix to Mcl-1 but not Bcl-XL. Maritoclax (Marinopyrrole A) markedly inhibits the viability of Mcl-1-IRES-BimEL cells (EC₅₀=1.6 μM) with a selectivity greater than 40-fold over Bcl-2-IRES-BimEL (EC₅₀=65.1 μM) and Bcl-XL-IRES-BimEL (EC₅₀=70.0 μM) cells. Maritoclax (Marinopyrrole A) induces cell death selectively in Mcl-1-dependent but not Bcl-2- or Bcl-XL-dependent leukemia cells. Maritoclax (Marinopyrrole A) induces proteasome-mediated Mcl-1 degradation without induction of Mcl-1 phosphorylation and Noxa expression. Maritoclax (Marinopyrrole A) inhibits Mcl-1 interaction with Bim in intact cells and triggers cytochrome c release from isolated mitochondria. Maritoclax (Marinopyrrole A) synergistically sensitizes lymphoma/leukemia cells to ABT-737. Maritoclax (Marinopyrrole A) shows activity against all tested S. aureus strains, including glycopeptide-intermediate and vancomycin-resistant MRSA, and has potent activities against other Gram-positive organisms. In addition, Maritoclax (Marinopyrrole A) is active against H. influenzae but is inactive against other tested Gram-negative strains. Maritoclax (Marinopyrrole A) displays substantial concentration-dependent killing against MRSA strain TCH1516 and is far more rapid in its antibiotic action than either vancomycin or linezolid. Maritoclax exhibits a favorable therapeutic index, with 50% inhibitory concentrations (IC₅₀) in excess of 20× above the MIC in each case: 32 to 64 μg/mL against HeLa cells and 8 to 32 μg/mL against L929 cells. Maritoclax (Marinopyrrole A) (3 μM) induced-cell death is associated with MCL1 decrease and translation inhibition. Maritoclax (Marinopyrrole A) induces a dephosphorylation of EIF4EBP1 concomitant to a decrease of EIF4E phosphorylation. Maritoclax (Marinopyrrole A) is much more effective against Bcl-2-dependent RS4;11 cells (IC₅₀: 2 μM) when compared to Mcl-1-dependent HeLa cells (IC₅₀: 20 μM).

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Anti-Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Venetoclax  |  BT2  |  Chelerythrine chloride  |  Bax inhibitor peptide V5  |  A-1210477  |  BAI1  |  Dehydrocorydaline chloride  |  Gambogic Acid  |  Gossypol  |  BI-3812  |  Clitocine  |  PROTAC Bcl2 degrader-1  |  (R)-(-)-Gossypol acetic acid  |  MIM1  |  TW-37  |  (E)-Ferulic acid  |  Jaceosidin  |  Paris saponin VII  |  Bz 423  |  Dihydrokaempferol  |  MSN-125  |  HA14-1  |  TCPOBOP  |  BH3I-1  |  Thevetiaflavone

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。