mTOR/HDAC6-IN-1 是一种有效的哺乳动物雷帕霉素 (mTOR) 和组蛋白去乙酰酶 (HDAC6) 的双重抑制剂 (mTOR 和 HDAC6 的IC50s 分别为 133.7 nM 和 56 nM)。mTOR/HDAC6-IN-1 可诱导明显的细胞自噬 (autophagy)、细胞凋亡 (apoptosis)，以及抑制迁移。mTOR/HDAC6-IN-1 具有研究三阴性乳腺癌 (TNBC) 的潜力。
| 生物活性 | mTOR/HDAC6-IN-1 is a potentmTORandHDAC6dual inhibitor (IC50s of 133.7 nM and 56 nM formTORandHDAC6, respectively). mTOR/HDAC6-IN-1 can induce significantautophagy,apoptosisand suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breastcancer(TNBC)[1]. |
| IC50& Target[1] | mTOR 133.7 nM (IC50) | HDAC6 56 nM (IC50) |
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体外研究
(In Vitro) | mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h[1].
mTOR/HDAC6-IN-1 (10 μM; 6 hours) can significantly improve the thermal stability of HDAC6 in MDA-MB-231 cells, which indicates that mTOR/HDAC6-IN-1 has a selective inhibitory effect on HDAC6[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone[1].
mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 48 hours) induces obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 cells[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM) induces significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3[1].
mTOR/HDAC6-IN-1 (5, 10, 20 μM; 48 hours) inhibited MDA-MB-231 cells migration in a dose-dependent manner, and decreases the expression of MMP-2 as well as increases the expression of E-cadherin[1].
Cell Viability Assay | Cell Line: | MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells[1] | | Concentration: | 0, 20, 40, 60, 80 and 100 μM | | Incubation Time: | 48 hours | | Result: | Had a medium anti-proliferation activity with IC50of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h. |
Apoptosis Analysis | Cell Line: | MDA-MB-231[1] | | Concentration: | 5, 10, 20 μM | | Incubation Time: | | | Result: | Induced significant MDA-MB-231 apoptosis in a dose-dependent manner, also up-regulates the expression of Bax, down-regulates bcl-2, and promotes the cleavage of PARP and apoptotic executive protein caspase8 and caspase3. |
Cell Autophagy Assay | Cell Line: | MDA-MB-231[1] | | Concentration: | 2.5, 5, 10 μM | | Incubation Time: | 48 hours | | Result: | Induced obvious autophagy with the accumulation of LC3 puncta in MDA-MB-231 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. |
