mTOR/HDAC6-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

mTOR/HDAC6-IN-1 

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。

mTOR/HDAC6-IN-1

mTOR/HDAC6-IN-1 Chemical Structure

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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)[1].

IC50 & Target[1]

mTOR

133.7 nM (IC50)

HDAC6

56 nM (IC50)

体外研究
(In Vitro)

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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 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.

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

分子量

397.86

Formula

C20H20ClN5O2

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.

参考文献
  • [1]. Yao D, et al. Design, synthesis and biological evaluation of dual mTOR/HDAC6 inhibitors in MDA-MB-231 cells. Bioorg Med Chem Lett. 2021;47:128204.

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