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MRT67307

MRT67307

产品编号 T0097   CAS 1190378-57-4
别名: MRT67307 HCl

MRT67307 是一种IKKε和TBK-1的双抑制剂,IC50分别为 160 和 19 nM。它抑制细胞自噬,也可抑制ULK1和ULK2,IC50分别为 45 和 38 nM。

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MRT67307 Chemical Structure
MRT67307, CAS 1190378-57-4
规格 价格/CNY 货期 数量
1 mg ¥ 238 现货
5 mg ¥ 592 现货
10 mg ¥ 1,080 现货
25 mg ¥ 2,180 现货
50 mg ¥ 3,270 现货
100 mg ¥ 4,770 现货
1 mL * 10 mM (in DMSO) ¥ 666 现货
产品目录号及名称: MRT67307 (T0097)
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纯度: 99.79%
纯度: 99.25%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Through its effects on ULK1 and ULK2, MRT67307 blocks autophagy. MRT67307 prevents the phosphorylation of IRF3 and the production of IFN-β and increases toll-like receptor-induced IL-10 and IL-1ra secretion in macrophages. MRT67307 is a kinase inhibitor that has been shown to inhibit TBK1, MARK1-4, IKKε, and NUAK1 (IC50 values are 19, 27-52, 160, and 230 nM, respectively), the salt-inducible kinases (SIKs; IC50s =250, 67, and 430 nM for SIK1, SIK2, and SIK3, respectively) and ULK1 and ULK2 (IC50s = 45 and 38 nM, respectively).
靶点活性 TBK1:190 nM, IKKϵ:160 nM
体外活性 In macrophages, MRT67307 prevents the phosphorylation of IRF3 and the production of IFNβ. In wild-type MEFs, MRT67307 enhances the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536, and also enhances IL-1-stimulated activation of NF-κB-dependent gene transcription. [1] MRT67307 increases IL-10 production and suppresses proinflammatory cytokine production via a cAMP response element-Binding protein (CREB)-regulated transcriptional coactivator (CRTC) 3 Dependent Mechanism. [2] In addition, MRT67307 inhibit ULK and block autophagy in MEF cells. [3]
激酶实验 Substrates and kinases are diluted in 50?mM Tris/HCl (pH?7.5), 0.1% 2-mercaptoethanol, 0.1?mM EGTA and 10?mM magnesium acetate. Reactions are initiated with [γ-32P]ATP (2500 c.p.m./pmol) to a final concentration of 0.1?mM and terminated after 15?min at 30°C by the addition of SDS and EDTA (pH?7.0) to final concentrations of 1.0% (w/v) and 20?mM respectively. After heating for 5?min at 100°C and separation by SDS/PAGE, the phosphorylated proteins are detected by autoradiography.
细胞实验 Cells are rinsed in ice-cold PBS and extracted in lysis buffer (50 mM Tris·HCl at pH 7.4, 1 mM EDTA, 1 mM EGTA, 50 mM NaF, 5 mM sodium pyrophosphate, 10 mM sodium β-glycerol 1-phosphate, 1 mM DTT, 1 mM sodium orthovanadate, 0.27mol/Lsucrose, 1% (vol/vol) Triton X-100, 1 μg/mL aprotinin, 1 μg/ mL leupeptin, and 1 mM phenylmethylsulphonyl fluoride). Cell extracts are clarified by centrifugation at 14,000 × g for 10 min at 4°C, and protein concentrations are determined by using the Bradford assay. FLAG-CRTC3 is purified on anti-FLAG M2 agarose, whereas endogenous CRTC3 is immunoprecipitated from cell extracts by using anti-CRTC3 raised against the peptide CWKEEKHPGFR (S277D bleed 2) and coupled to Protein GSepharose. To detect proteins in cell lysates, 20 μg of protein extract is separated by SDS/PAGE. After transfer to PVDF membranes, proteins are detected by immunoblotting and visualized by treating the blots with ECL followed by autoradiography. The following antibodies are used for immunoblotting: pSer133 CREB, pSer171 CRTC2, total CRTC2, GAPDH, total STAT3, pTyr705 STAT3, FLAG (M2 clone), CRTC3, HA (3F10), and 14-3-3; and antibodies against pSer329 (S256D bleed 2) and pSer370 (S253D bleed 2) of CRTC3 are raised against the phosphopeptides GLQSSRpSNPSIQ and RLFSLpSNPSLST.
别名 MRT67307 HCl
分子量 464.6
分子式 C26H36N6O2
CAS No. 1190378-57-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 83 mg/mL(178.6 mM)

Ethanol: 83 mg/mL(178.6 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.1524 mL 10.7619 mL 21.5239 mL 53.8097 mL
5 mM 0.4305 mL 2.1524 mL 4.3048 mL 10.7619 mL
10 mM 0.2152 mL 1.0762 mL 2.1524 mL 5.381 mL
20 mM 0.1076 mL 0.5381 mL 1.0762 mL 2.6905 mL
50 mM 0.043 mL 0.2152 mL 0.4305 mL 1.0762 mL
100 mM 0.0215 mL 0.1076 mL 0.2152 mL 0.5381 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Clark K, et al. Biochem J. 2011, 434(1), 93-104. 2. Clark K, et al. Proc Natl Acad Sci U S A. 2012, 109(42), 161986-161991. 3. Petherick KJ, et al. J Biol Chem. 2015, 290(18), 11376-11383.
TBK1/IKKε-IN-1 Cyclo(L-Pro-L-Val) Bardoxolone Methyl Cudraflavone B Armepavine Protosappanin A Resveratrol Bay 65-1942 free base

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 自噬库 抗肝癌化合物库 激酶抑制剂库 抗抑郁症化合物库 经典已知活性库 抗乳腺癌化合物库 抑制剂库 NO PAINS 化合物库 抗卵巢癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

MRT67307 1190378-57-4 Autophagy NF-Κb IκB/IKK MRT 67307 Inhibitor ULK2 ULK IKKε MRT-67307 inhibit IKK MRT67307 HCl ULK1 cancer IκB kinase signal TBK-1 Unc-51 like kinase I kappa B kinase transduction inhibitor

 

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