MS8815 是 zeste 同源物2(EZH2)PROTAC降解剂，具有选择性。MS8815 对 EZH2 有抑制活性，IC50值为 8.6 nM。MS8815 可用于三阴性乳腺癌 (TNBC) 研究。
| 生物活性 | MS8815 is a selectiveenhancer of zeste homolog 2 (EZH2)PROTACdegrader. MS8815 has inhibition activity forEZH2with anIC50value of 8.6 nM. MS8815 can be used for the research of triple-negative breastcancer(TNBC)[1]. |
| IC50& Target | IC50: 8.6 nM (EZH2); 62 nM (EZH1)[1].
DC50: 140 nM (EZH2 in MDA-MB-453 cells)[1] |
体外研究
(In Vitro) | MS8815 shows potency in inhibiting the EZH2 and EZH1 methyltransferase activity with IC50values of 8.6 nM and 62 nM, respectively[1].
MS8815 (0.1-1 μM) degrades EZH2 with a DC50value of 140 nM in MDA-MB-453 cells[1].
MS8815 (1 μM; 48 h) induces robust EZH2 degradation in a concentration-, time-, and proteasome-dependent manner in TNBC cells[1].
MS8815 (0.1-10 μM; 5 days) effectively suppresses the cell growth in multiple TNBC cell lines and primary patient TNBC cells[1].
Western Blot Analysis[1] | Cell Line: | MDA-MB-453 cells and BT549 cells | | Concentration: | 0.3, 3 μM; 1μM | | Incubation Time: | 48 h; 24 h | | Result: | Induced nearly complete degradation of EZH2 and exhibited the most robust degradation at 0.3 μM.
Induced EZH2 degradation in a time-and concentration-dependent manner.
Induced EZH2 degradation through the UPS. |
Cell Proliferation Assay[1] | Cell Line: | BT549, MDA-MB-468, SUM159 and MDA-MB-453 cells | | Concentration: | 0.1-10 μM | | Incubation Time: | 5 days | | Result: | Showed superior cellular growth inhibition activity in a panel of TNBC cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 溶解性数据 | In Vitro: DMSO : 130 mg/mL(112.60 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.8662 mL | 4.3308 mL | 8.6617 mL | | 5 mM | 0.1732 mL | 0.8662 mL | 1.7323 mL | | 10 mM | 0.0866 mL | 0.4331 mL | 0.8662 mL |
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 3.25 mg/mL (2.82 mM); Clear solution
此方案可获得 ≥ 3.25 mg/mL (2.82 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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