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。
| 生物活性 | MY-875 is a competitivemicrotubulin polymerizationinhibitor with anIC50value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates theHippopathway. MY-875 inducesapoptosisand has anticancer activity[1]. |
体外研究
(In Vitro) | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : ≥ 250 mg/mL(645.28 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.5811 mL | 12.9056 mL | 25.8111 mL | | 5 mM | 0.5162 mL | 2.5811 mL | 5.1622 mL | | 10 mM | 0.2581 mL | 1.2906 mL | 2.5811 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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