MRT199665

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 .


Cat. No.: EX-A10309	Purity: >98%

	Chemical structure of MRT199665

For research only, Do not use for Human!

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CAS No.	1456858-57-3
Purity	>98%
Formula	C28H31N5O2
Mol Weight	469.578
Color	off-white to light yellow
State	solid
Solubility	Soluble in DMSO
Shelf Life	>3 years if stored properly
Storage	Powder 4℃, protect from light, 2 years; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91. [2]. Brown FC, et al. MEF2C Phosphorylation Is Required for Chemotherapy Resistance in Acute Myeloid Leukemia. Cancer Discov. 2018 Apr;8(4):478-497. [3]. Hutchinson LD, et al. Salt-inducible kinases (SIKs) regulate TGFβ-mediated transcriptional and apoptotic responses.Cell Death Dis. 2020 Jan 22;11(1):49.
CoA	CoA of MRT199665

Smiles:	O=C1C(C)(C)C2=CN=C(NC3=CC=CC(CN4CCCC4)=C3)N=C2N1[C@H]5CCC6=C5C=CC=C6O


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