MRT199665

COA

级别和纯度:

≥99%

CAS编号: 1456858-57-3
分子式: C₂₈H₃₁N₅O₂
分子量: 469.58
PubChem编号: 71725150

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货号 (SKU)	包装规格	是否现货
M646396-5mg	5mg	期货
M646396-10mg	10mg	期货
M646396-25mg	25mg	期货
M646396-50mg	50mg	期货

查看相关系列

AMPK (94) Apoptosis (7108) Cell Cycle (7376) DNA Methylation (633) Immunology/Inflammation (1938) PI3K/Akt/mTOR (764) Salt-inducible Kinase (SIK) (15) 表观遗传学 (1497)

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基本描述

规格或纯度	≥99%
英文名称	MRT199665
生化机理	MRT199665 是一种强效的 ATP 竞争性、选择性 MARK / SIK / AMPK 抑制剂，对 MARK1/MARK2/MARK3/MARK14 、AMPKα1/AMPKα2 和 SIK1/SIK2/SIK3 的 IC 50 s 分别为 2/2/3/2、10/10 nM 和 110/12/43 nM。MRT199665 在 ME 中导致细胞凋亡
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	抑制剂
产品介绍	MRT199665 is a potent and ATP-competitive, selective MARK / SIK / AMPK inhibitor with IC 50 s 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 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.\nMRT199665 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: OCI-AML2 and MOLM-13 cells Concentration: 10, 100, 500, and 1000 nM Incubation 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 AssayCell 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 IC 50 of 26±13 versus 990±29 nM, respectively. Form:Solid IC50& Target:MARK1 2 nM (IC 50 ) MARK2 2 nM (IC 50 ) MARK3 3 nM (IC 50 ) MARK4 2 nM (IC 50 ) SIK1 110 nM (IC 50 ) SIK2 12 nM (IC 50 ) SIK3 43 nM (IC 50 ) NUAK1 3 nM (IC 50 ) NUAK2 120 nM (IC 50 ) AMPKα1 10 nM (IC 50 ) AMPKα2 10 nM (IC 50 ) MELK 29 nM (IC 50 ) TBK1 5400 nM (IC 50 ) IKKε 7700 nM (IC 50 ) BRSK2 10000 nM (IC 50 )
纯度	≥99%

名称和识别符

IIUPAC Name	7-[(1S)-4-hydroxy-2,3-dihydro-1H-inden-1-yl]-5,5-dimethyl-2-[3-(pyrrolidin-1-ylmethyl)anilino]pyrrolo[2,3-d]pyrimidin-6-one
INCHI	1S/C28H31N5O2/c1-28(2)22-16-29-27(30-19-8-5-7-18(15-19)17-32-13-3-4-14-32)31-25(22)33(26(28)35)23-12-11-21-20(23)9-6-10-24(21)34/h5-10,15-16,23,34H,3-4,11-14,17H2,1-2H3,(H,29,30,31)/t23-/m0/s1
InChi Key	OFIFLUFVENTCNZ-QHCPKHFHSA-N
Smiles	CC1(C2=CN=C(N=C2N(C1=O)C3CCC4=C3C=CC=C4O)NC5=CC=CC(=C5)CN6CCCC6)C
Isomeric SMILES	CC1(C2=CN=C(N=C2N(C1=O)[C@H]3CCC4=C3C=CC=C4O)NC5=CC=CC(=C5)CN6CCCC6)C
PubChem CID	71725150
MeSH Entry Terms	MRT199665
分子量	469.58

化学和物理性质

溶解性	DMSO : 125 mg/mL (266.20 mM; Need ultrasonic)
分子量	469.600 g/mol
XLogP3	4.300
氢键供体数Hydrogen Bond Donor Count	2
氢键受体数Hydrogen Bond Acceptor Count	6
可旋转键计数Rotatable Bond Count	5
精确质量Exact Mass	469.248 Da
单同位素质量Monoisotopic Mass	469.248 Da
拓扑极表面积Topological Polar Surface Area	81.600 Å²
重原子数Heavy Atom Count	35
形式电荷Formal Charge	0
复杂度Complexity	770.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	1
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

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