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MRT199665

CAT: 0804-HY-120877-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-120877-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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[1]. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells[2]. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370[3].
CAS Number
1456858-57-3
UNSPSC
12352005
Target
AMPK; Apoptosis; MARK; Salt-inducible Kinase (SIK)
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Immunology/Inflammation; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/mrt199665.html
Concentration
10mM
Purity
99.74
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C1C(C)(C)C2=CN=C(NC3=CC=CC(CN4CCCC4)=C3)N=C2N1[C@H]5CCC6=C5C=CC=C6O
Molecular Formula
C28H31N5O2
Molecular Weight
469.58
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
NUAK1; NUAK2; SIK1; SIK2; SIK3

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CatalogName
MBS5769546MRT199665

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