MRT67307 hydrochloride

Modify Date: 2024-01-24 12:48:23

MRT67307 hydrochloride Structure
MRT67307 hydrochloride structure
Common Name MRT67307 hydrochloride
CAS Number 2095432-39-4 Molecular Weight 501.06
Density N/A Boiling Point N/A
Molecular Formula C26H37ClN6O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of MRT67307 hydrochloride


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].

 Names

Name MRT67307 hydrochloride

 MRT67307 hydrochloride Biological Activity

Description 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].
Related Catalog
Target

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

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]. Western Blot Analysis[3] Cell Line: 293T cells Concentration: 5 µM Incubation Time: 4 hours Result: Abrogated TBK1/IKKε-induced CYLD phosphorylation.
References

[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.

 Chemical & Physical Properties

Molecular Formula C26H37ClN6O2
Molecular Weight 501.06