MRT67307 hydrochloride

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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。

MRT67307 hydrochloride 

MRT67307 hydrochloride 是 IKKε 和 TBK-1 的双抑制剂，IC50 分别为 160 和 19 nM。MRT67307 hydrochloride 也可抑制 ULK1 和 ULK2，IC50 分别为 45 和 38 nM。MRT67307 hydrochloride 还抑制细胞自噬 (autophagy)。

MRT67307 hydrochloride

MRT67307 hydrochloride Chemical Structure

CAS No. : 2095432-39-4

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MRT67307 hydrochloride 的其他形式现货产品:

MRT67307

生物活性

MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells[2].

IC50 & Target[1][2]

TBK1

19 nM (IC50, at 0.1 mM ATP)

IKKε

160 nM (IC50, at 0.1 mM ATP)

ULK2

38 nM (IC50)

ULK1

45 nM (IC50)

Autophagy

 

体外研究
(In Vitro)

MRT67307 inhibits IKKϵ and TBK1 with IC50 values of 160 and 19 nM when assayed at 0.1 mM ATP in vitro, but did not inhibit IKKα or IKKβ even at 10 μM[1].
MRT67307 (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT67307 (2 μM) dose not suppresse the activation of JNK or p38 MAPK by poly(I:C)[1].
MRT67307 (1 nM-10 μM) prevents the production of IFNβ in macrophages[1].
MRT67307 (10 μM) is sufficient to reduce phospho-ATG13 to control levels[2].
MRT67307 (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs)[2].
MRT67307 (5 µM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells[3].

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.

Western Blot Analysis[3]

Cell Line: 293T cells
Concentration: 5 µM
Incubation Time: 4 hours
Result: Abrogated TBK1/IKKε-induced CYLD phosphorylation.

分子量

501.06

Formula

C26H37ClN6O2
CAS 号

2095432-39-4
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]. Clark K, et al. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104.

    [2]. Petherick KJ, et al. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem. 2015 May 1;290(18):11376-83.

    [3]. Zhu Z, et al. Inhibition of KRAS-driven tumorigenicity by interruption of an autocrine cytokine circuit. 26.37Cancer Discov. 2014 Apr;4(4):452-65.

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