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MRT199665 

Cat. No. M28491

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MRT199665  Structure

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Quality Control & Documentation
Biological Activity

MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.

Chemical Information
Molecular Weight 469.58
Formula C28H31N5O2
CAS Number 1456858-57-3
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Mingsong Shi, et al. Phys Chem Chem Phys. Exploring the stability of inhibitor binding to SIK2 using molecular dynamics simulation and binding free energy calculation

[2] Luke D Hutchinson, et al. Cell Death Dis. Salt-inducible kinases (SIKs) regulate TGFβ-mediated transcriptional and apoptotic responses

[3] Fiona C Brown, et al. Cancer Discov. MEF2C Phosphorylation Is Required for Chemotherapy Resistance in Acute Myeloid Leukemia

[4] Fiona A Ross, et al. Cell Chem Biol. Mechanisms of Paradoxical Activation of AMPK by the Kinase Inhibitors SU6656 and Sorafenib

[5] Nicola J Darling, et al. Biochem J. Inhibition of SIK2 and SIK3 during differentiation enhances the anti-inflammatory phenotype of macrophages

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  Catalog
Abmole Inhibitor Catalog




Keywords: MRT199665  supplier, Salt-inducible Kinase, inhibitors, activators

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