mTOR/HDAC-IN-1

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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/HDAC-IN-1 

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。

mTOR/HDAC-IN-1

mTOR/HDAC-IN-1 Chemical Structure

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生物活性

mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC50 values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent[1].

IC50 & Target

mTOR

0.49 nM (IC50)

HDAC1

0.91 nM (IC50)

HDAC6

86 nM (IC50)

HDAC8

27 nM (IC50)

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 IC50 values 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 values 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.

分子量

501.50

Formula

C23H23N11O3
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]. Mingming Zhang, et al. Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy. Bioorg Med Chem Lett. 2021 Oct 1;49:128286.

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