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MRT 67307 dihydrochloride

Catalog No. T36994 CAS 1781882-89-0

MRT 67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks Autophagy in cells.

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MRT 67307 dihydrochloride, CAS 1781882-89-0

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Purity: 98%

Biological Description

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Description

In vitro

MRT 67307 dihydrochloride inhibits IKKϵ and TBK1 with IC50 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]. MRT 67307 dihydrochloride (2 μM) prevents the phosphorylation of IRF3 in bone-marrow-derived macrophages (BMDMs). MRT 67307 dihydrochloride (2 μM) dose not suppresse the activation of JNK or p38 MAPK by poly(I:C)[1]. MRT 67307 dihydrochloride (1 nM-10 μM) prevents the production of IFNβ in macrophages[1]. MRT 67307 dihydrochloride (10 μM) is sufficient to reduce phospho-ATG13 to control levels[2]. MRT 67307 dihydrochloride (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs)[2]. MRT 67307 dihydrochloride (5 µM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells[3].

Molecular Weight	537.53
Formula	C26H38Cl2N6O2
CAS No.	1781882-89-0

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 82.8mg/mL (154mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Clark et al (2012) Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc.Natl.Acad.Sci.U.S.A. 109 16986 2. Clark et al (2011) Novel cross-talk within the IKK family controls innate immunity. Biochem.J. 434 93 3. Smith et al (2011) The role of TBK1 and IKKe in the expression and activation of Pellino 1. Biochem.J. 434 537 4. Galluzzi et al (2017) Pharmacological modulation of autophagy: therapeutic potential and persisting obstacles. Nat.Rev.Drug.Discov.

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Keywords

MRT 67307 dihydrochloride 1781882-89-0 PI3K/Akt/mTOR signaling SIK Inhibitor inhibitor inhibit

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