Chemical Structure : MRT67307
CAS No.: 1190378-57-4
Catalog No.: 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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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.
M.Wt | 464.603 | |
Formula | C26H36N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Cyclobutanecarboxamide, N-[3-[[5-cyclopropyl-2-[[3-(4-morpholinylmethyl)phenyl]amino]-4-pyrimidinyl]amino]propyl]- |
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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