产品说明书

MRT67307

Print
Chemical Structure| 1190378-57-4 同义名 : IKKε/TBK1 Inhibitor II
CAS号 : 1190378-57-4
货号 : A608717
分子式 : C26H36N6O2
纯度 : 99%+
分子量 : 464.603
MDL号 : MFCD19443643
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(226 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Members of the IKK {IκB [inhibitor of NF-κB (nuclear factor κB)] kinase} family play a central role in innate immunity by inducing NF-κB- and IRF [IFN (interferon) regulatory factor]-dependent gene transcription programmes required for the production of pro-inflammatory cytokines and IFNs[3]. MRT67307 is a dual inhibitor of the IKKε and TBK-1 (TANK-binding Kinase 1) with IC50s of 19 and 160 nM in vitro[3]. In IKKα−/−MEFs (mouse embryonic fibroblasts), MRT67307 enhanced the IL-1-stimulated phosphorylation of RelA at Ser468. Similarly, in wild type MEFs, MRT67307 enhanced the IL-1-stimulated phosphorylation of p105 at Ser933 and RelA at both Ser468 and Ser536. MRT67307 also enhanced IL-1-stimulated activation of NF-κB -dependent gene transcription in wild type MEFs. Treatment of macrophages with MRT67307 enhanced the poly(I:C)-stimulated phosphorylation of TBK1 at Ser172 and enhanced the catalytic activity of IKK and TBK1. Additionally, Treatment of macrophages with MRT67307 led to an increase in the poly(I:C) and LPS-stimulated phosphorylation of p105 and RelA and enhanced NF-κB transcriptional activity[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.52mL

4.30mL

2.15mL
参考文献

[1]Petherick KJ, Conway OJ, 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.

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

[3]Clark K, Peggie M, Plater L, Sorcek RJ, Young ER, Madwed JB, Hough J, McIver EG, Cohen P. Novel cross-talk within the IKK family controls innate immunity. Biochem J. 2011 Feb 15;434(1):93-104. doi: 10.1042/BJ20101701. PMID: 21138416.