产品
编 号：F762718
分子式：C20H20ClN5O2
分子量：397.86
分子式：C20H20ClN5O2
分子量：397.86
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规格
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CAS No: 2986747-52-6
产品详情
生物活性：
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC).
体外研究：
mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.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.mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone.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.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.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.
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC).
体外研究：
mTOR/HDAC6-IN-1 (compound 10g) (0-100 μM; 48 hours) has a medium anti-proliferation activity with IC50 of 8.4 μM, 10.6 μM and 14.3 μM in MDA-MB-231, MDA-MB-436 and MDA-MB-468 cells at 48h.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.mTOR/HDAC6-IN-1 (2.5, 5, 10 μM; 2 weeks) inhibits MDA-MB-231 cells form the clone.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.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.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.
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