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MY-875
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
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MY-875 是一种竞争性的微管蛋白聚合 (microtubulin polymerization) 抑制剂, IC50 值为 0.92 μM。MY-875 通过靶向秋水仙碱结合位点抑制微管蛋白聚合,同时可以激活 Hippo 通路。MY-875 可以诱导细胞凋亡 (apoptosis),具有抗癌活性。
分子式C21H25NO6
分子量387.43
溶解度DMSO : ≥ 250 mg/mL (645.28 mM)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

MY-875 is a competitivemicrotubulin polymerizationinhibitor with anIC50value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 inducesapoptosisand has anticancer activity[1].

MY-875 (0-80 μM, 48 h) has significant anti-proliferative activity against cancer cells[1].
MY-875 (1-10 μM) can inhibit microtubule protein polymerization with an IC50value of 0.92 μM while inhibiting alkylation of β-tubulin and the formation of EBI-β-tubulin adduct bands in a dose-dependent manner[1].
MY-875 (0-45 nM, 48 h) can induce the phosphorylation state of MST (Ste20-like kinases) and LATS (large tumor suppressor kinases), leading to YAP (Yes-associated protein) degradation in a dose-dependent manner[1].
MY-875 (0-45 nM, 24 h) significantly inhibits cell colony-forming ability, arrests cells in the G2/M phase and induces cell apoptosis in a dose-dependent manner[1].

Cell Proliferation Assay[1]

Cell Line:MGC-803, HCT-116, KYSE450, HGC-27, SGC-7901cell lines
Concentration:0-80 μM
Incubation Time:48 hours
Result:Inhibited the proliferation of MGC-803, HCT-116, KYSE450, HGC-27 and SGC-7901 cells with the IC50values of 0.027, 0.055, 0.067, 0.033 and 0.025 μM, respectively.
Showed strong inhibitory effect on other tumor cell lines with the IC50values less than 0.1 μM, such as DU145, A549, MCF-7, etc.

Cell Cycle Analysis[1]

Cell Line:MGC-803, SGC-7901 cell lines
Concentration:0-45 nM
Incubation Time:24 hours
Result:Increased the percentage of cells in G2/M phase from 19.38% to 76.97% in MGC-803 cells and from 7.04% to 80.89% in SGC-7901 cells, respectively at 45 nM.

Apoptosis Analysis[1]

Cell Line:MGC-803, SGC-7901 cell lines
Concentration:0-45 nM
Incubation Time:48 hours
Result:Induced apoptotic cells from 21.96% to 76.08% in MGC-803 cells and from 9.28% to 63.51% in SGC-7901 cells, respectively at 45 nM.
Reduced expression of anti-apoptotic proteins c-IAP1, Bcl-xL and Mcl-1.

 
 
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