MRT 199665

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MRT 199665 是一种有效的盐诱导激酶 (SIK) 抑制剂，对 SIK1、2、3 的 IC50 分别为 110、12、43 nM。

MRT 199665 is a potent salt-inducible kinases (SIKs) inhibitor with IC50 of 110, 12, 43 nM for SIK1,2,3 respectively; also inhibits AMPKα1/α2 (both IC50=10 nM), MARK1/2/3/4 (both IC50=2 nM), NUAK1/2 (IC50=3/120 nM), and MELK (IC50=29 nM); elevates IL-10 production by inducing the dephosphorylation of CREB-regulated transcriptional coactivator 3 (CRTC3), increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion (IL-6, IL-12, and TNF) in macrophages.(In Vitro):MRT199665 (1 μM; pre-treated for 1 h) increases LPS (100 ng/mL; stimulated for up to 24 h)-stimulated IL-10 mRNA and Nurr77 mRNA production, and IL-10 secretion.MRT199665 (1 nM-100 μM; 48 hours) reduces leukemia growth.MRT199665 treatment can block MEF2C S222 phosphorylation in acute myeloid leukemias (AML) cells. MRT199665 (10 nM-1000 nM; 12 hours) leads to a dose-dependent reduction in total and pS222 MEF2C. MRT199665 also causes a decrease of total MEF2C protein.

Western Blot Analysis Cell Line:OCI-AML2 and MOLM-13 cells Concentration:10, 100, 500, and 1000 nMIncubation Time:12 hours Result:Led to a dose-dependent reduction in total and pS222 MEF2C, causing more than 40% reduction in MEF2C phosphorylation at 10 nM as compared to untreated cells.Cell Proliferation Assay Cell Line:Human AML cell lines OCI-AML2, MV4-11, MOLM-13 and Kasumi-1 with endogenous MEF2C phosphorylation; human AML cell lines NB-4, HEL, HL-60 and U937 lacking MEF2C Concentration:1 nM, 10 nM, 100n M, 1 μM, 10 μM, 100μM Incubation Time:48 hours Result: Human AML cell lines with endogenous MEF2C phosphorylation (OCI-AML2, MV4–11, MOLM-13 and Kasumi-1) were more sensitive as compared to cell lines lacking MEF2C (NB-4, HEL, HL-60 and U937), with mean IC50 of 26±13 versus 990±29 nM, respectively.

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MRT199665

Autophagy

SIK

SIK

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1456858-57-3

373.43

C18H19N3O4S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (266.20 mM)

O=C1C(C)(C)C2=CN=C(S(=O)(C)=O)N=C2N1[C@H]3CCC4=C3C=CC=C4O

7-[(1S)-4-Hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-(methylsulfonyl)-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

(-20℃)

With Ice Pack

≥ 2 years