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首页-小分子抑制剂&激动剂-Autophagy-ULK-MRT67307
MRT67307

Chemical Structure : MRT67307

CAS No.: 1190378-57-4

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MRT67307 (MRT 67307, MRT-67307)

货号: PC-43328Not For Human Use, Lab Use Only.

MRT67307 is a potent, dual inhibitor of IKKε and TBK-1 with IC50 of 160 and 19 nM at 0.1 mM ATP in vitro, also potently inhibit ULK1 and ULK2 in vitro (IC50=45 and 38 nM) and block autophagy in cells.

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5 mg ￥580 In stock
10 mg ￥880 In stock
25 mg ￥1380 In stock
50 mg ￥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MRT67307 is a potent, dual inhibitor of IKKε and TBK-1 with IC50 of 160 and 19 nM at 0.1 mM ATP in vitro, also potently inhibit ULK1 and ULK2 in vitro (IC50=45 and 38 nM) and block autophagy in cells.
The autophagy-inhibiting capacity of MRT67307 is specifically through ULK1, results in accumulation of stalled early autophagosomal structures in treated cells。
MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production in macrophages, increases CREB-dependent gene transcription by promoting the dephosphorylation of CRTC3。
MRT67307 also inhibits MARK, NUAK and SIK isoforms in vitro with comparable potency to the IKK-related kinases.

物理化学性质&存储条件

分子量 464.603
分子式 C26H36N6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Cyclobutanecarboxamide, N-[3-[[5-cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]-

参考文献

1. Clark K, et al. Biochem J. 2011 Feb 15;434(1):93-104.

2. Clark K, et al. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91.

3. Petherick KJ, et al. J Biol Chem. 2015 May 1;290(18):11376-83.

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