MRT 67307 dihydrochloride

SKU: orb1693260

Description

MRT67307 dihydrochloride is a potent dual inhibitor of IKKε (IC50=160 nM) and TBK1 (IC50=19 nM), and also inhibits ULK1/2, thereby blocking autophagy. This compound is a valuable research tool for studying innate immunity, autophagy signaling, and their roles in cancer and inflammatory diseases in cellular models.

Research Area

Cell Biology, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1781882-89-0
MW	537.53
Purity	99.75% (May vary between batches)
Formula	C₂₆H₃₈Cl₂N₆O₂
SMILES	O=C(C1CCC1)NCCCNC2=NC(NC3=CC=CC(CN4CCOCC4)=C3)=NC=C2C5CC5.Cl.Cl
Target	IκB/IKK,SIK,Autophagy
Solubility	DMSO:82.8 mg/mL (154.04 mM)

Bioactivity

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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. 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). MRT 67307 dihydrochloride (1 nM-10 μM) prevents the production of IFNβ in macrophages. MRT 67307 dihydrochloride (10 μM) is sufficient to reduce phospho-ATG13 to control levels. MRT 67307 dihydrochloride (10 μM) blocks autophagy in mouse embryonic fibroblasts (MEFs). MRT 67307 dihydrochloride (5 µM; 4 h) abrogates TBK1/IKKε-induced CYLD phosphorylation in 293T cells.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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MRT 67307, MRT 67307 Dihydrochloride, MRT 67307 dihydrochloride, MRT67307, MRT-67307, MRT67307 Dihydrochloride, MRT-67307 Dihydrochloride, Salt-inducible Kinase (SIK)

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Compound Identifiers

PubChem CID

90489013 ↗

Key Properties

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No computed properties available.

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