SML1753
XMD17-109
≥98% (HPLC)
别名:
11-Cyclopentyl-2-((2-ethoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)-phenyl)amino)-5-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one, ERK5-IN-1
SMILES string
N7(CCN(CC7)C)C1CCN(CC1)C(=O)c2cc(c(cc2)Nc3nc4[n](c6c([c]([n](c4cn3)C)=O)cccc6)C5CCCC5)OCC
InChI
1S/C36H46N8O3/c1-4-47-32-23-25(34(45)43-17-15-26(16-18-43)42-21-19-40(2)20-22-42)13-14-29(32)38-36-37-24-31-33(39-36)44(27-9-5-6-10-27)30-12-8-7-11-28(30)35(46)41(31)3/h7-8,11-14,23-24,26-27H,4-6,9-10,15-22H2,1-3H3,(H,37,38,39)
InChI key
XVBGRTMNFNMINE-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 20 mg/mL, clear
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
XMD17-109 is a cell-permeable, non-cytotoxic ATP site-targeting pyrimido-diazepinone derivative that acts as a potent inhibitor against ERK5 (MAPK7, BMK1) kinase activity in cell-free assay, and EGF-induced ERK5 autophosphorylation in HeLa cells.
XMD17-109 is a cell-permeable, non-cytotoxic ATP site-targeting pyrimido-diazepinone derivative that acts as potent inhibitor against ERK5 (MAPK7, BMK1) kinase activity in cell-free assay (IC50 = 162 nM; [ATP] = 50 μM) and EGF-induced ERK5 autophosphorylation in HeLa cells (IC50 = 90 nM). XMD17-109 displayed excellent target selectivity on a 442-kinase panel. XMD17-109 effectively inhibits inflammatory stimuli-induced IL-6 and IL-8 production from human endothelial cells in vitro and protects mice from LPS-induced mortality and systemic inflammation & coagulopathy in vivo with good pharmacokinetics.
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持