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。

TW-37

CAS No. : 877877-35-5

MCE 国际站：TW-37

产品活性：TW-37 是一种有效的 Bcl-2 抑制剂，作用于 Mcl-1，Bcl-2 和 Bcl-xL，K_i 值分别为 260，290 和 1110 nM。

研究领域：Apoptosis

作用靶点：Bcl-2 Family

In Vitro: TW-37 (TW37) is a novel nonpeptide small-molecule inhibitor designed using a structure-based design strategy. TW-37 targets the BH3-binding groove in Bcl-2 where proapoptotic Bcl-2 proteins, such as Bak, Bax, and Bid bind. In fluorescence polarization-based binding assays using recombinant Bcl-2 and Bcl-xL proteins, TW-37 binds to Bcl-2 and Bcl-xL with K_i values of 290 and 1110 nM, respectively. TW-37 has an IC₅₀ of 1.8 μM for endothelial cells but shows no cytotoxic effects for fibroblasts at concentrations up to 50 μM. The mechanism of TW-37-induced endothelial cell death is apoptosis, in a process mediated by mitochondrial depolarization and activation of caspase-9 and caspase-3. The effect of TW-37 on endothelial cell apoptosis is not prevented by coexposure to the growth factor milieu secreted by tumor cells. Inhibition of the angiogenic potential of endothelial cells (i.e., migration and capillary sprouting assays) and expression of the angiogenic chemokines CXCL1 and CXCL8 are accomplished at subapoptotic TW-37 concentrations (0.005-0.05 μM). TW-37 is a potent Bcl-2 and Mcl-1 inhibitor. In fluorescence polarization-based binding assays using recombinant Bcl-2, Bcl-xL, and Mcl-1 proteins, TW-37 binds to Bcl-2, Bcl-xL, and Mcl-1 with K_i values of 290, 1,110 and 260 nM, respectively.

In Vivo: A murine model of humanized vasculature is used to investigate the biological effect of TW-37 (TW37) on human microvascular endothelial cell in vivo. Using this model, a significant decrease is observed in total blood vessel number (P<0.05) comparing both 3 and 30 mg/kg TW-37 against vehicle control. In addition to reduction in total number of blood vessels, an unusual number of occluded vessels are occurring in the treated groups. The levels of vessel occlusion are assessed by counting completely blocked vessels and determining their number as a percentage of total vessel number. TW-37 concentration mediates a significant increase in the number of occluded vessels when compared with control.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Anti-Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  F1324  |  Pyridoclax  |  Lobaplatin  |  Bcl-2-IN-10  |  Bim BH3, Peptide IV TFA  |  Amantadine-d₆  |  PROTAC Bcl-xL ligand-1  |  Anticancer agent 64  |  Bcl-2-IN-2  |  BPA-B9  |  Bcl-2-IN-8  |  PUMA BH3 TFA  |  Amantadine  |  MCL-1/BCL-2-IN-2  |  STAT3-IN-13  |  Murizatoclax  |  (E)-Ferulic acid  |  Lometrexol  |  Oxychlororaphine  |  BRD4 Inhibitor-15  |  Bim-IN-1  |  (S)-Gossypol (acetic acid)  |  S65487 sulfate  |  Pelcitoclax  |  Lobetyol  |  Carteolol  |  Antitumor agent-55  |  BT2

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 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；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   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 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。