mTOR/HDAC-IN-1 (Compound 50) 是一个具有选择性的mTOR和HDAC双重抑制剂，对mTOR和HDAC1的IC50分别为0.49和0.91 nM。 mTOR/HDAC-IN-1 可作为抗癌药物 （anti-cancer） 进行研究。
| 生物活性 | mTOR/HDAC-IN-1 (Compound 50) is a selectivemTORandHDACdual inhibitor withIC50values of 0.49 and 0.91 nM againstmTORandHDAC1, respectively. mTOR/HDAC-IN-1 can be studied as ananti-canceragent[1]. |
| IC50& Target | mTOR 0.49 nM (IC50) | HDAC1 0.91 nM (IC50) | HDAC6 86 nM (IC50) | HDAC8 27 nM (IC50) |
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体外研究
(In Vitro) | mTOR/HDAC-IN-1 (Compound 50) (0-10 μM, 72 h) shows remarkable anti-proliferative activity against A549, HCT116, and MV4-11 cells[1].
mTOR/HDAC-IN-1 (0-3 μM, 6 h) simultaneous modulates mTOR signaling and HDAC catalytic activity at cellular level[1].
mTOR/HDAC-IN-1 displays excellent specificity over both HDAC6 and HDAC11 (with IC50values of 0.91, 86, 27, and >1000 against HDAC1, HDAC6, HDAC8 and HDAC11)[1].
mTOR/HDAC-IN-1 maintains the interaction of MLN0128 with the ATP-binding site in mTOR and binds with the catalytic channel in HDAC[1].
Cell Proliferation Assay[1] | Cell Line: | A549, HCT116, and MV4-11 | | Concentration: | 0-10 μM | | Incubation Time: | At 70 h post-compound treatment, to each well was added CCK-8, and the mixture was incubated for additional 2 h. | | Result: | Showed anti-proliferative activity with IC50values of 2.16, 3.85, and 1.74 μM against A549, HCT116, and MV4-11 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | MV4-11 | | Concentration: | 0.3, 1.0, and 3.0 μM | | Incubation Time: | 6 h | | Result: | Downregulated the levels of Phos-S6 (Ser235/Ser236) and Phos-AKT (Ser473), and elevated the levels of Ac-H3 (K9) and Acα-tubulin (Lys40) in a concentration-dependent manner. |
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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. |
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