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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
under inert gas
顏色
off-white
溶解度
DMSO: ≥4 mg/mL
儲存溫度
2-8°C
SMILES 字串
Cl[H].CCOc1ccc(cc1)C=C2SC(=O)N(CCN)C2=O
InChI
1S/C14H16N2O3S.ClH/c1-2-19-11-5-3-10(4-6-11)9-12-13(17)16(8-7-15)14(18)20-12;/h3-6,9H,2,7-8,15H2,1H3;1H/b12-9+;
InChI 密鑰
PQVLWVGMXJPJLG-NBYYMMLRSA-N
應用
3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is an extracellular signal-regulated kinase (ERK) docking domain inhibitor. ERK inhibitors have been used to study traumatic brain injuries.
生化/生理作用
3-(2-Aminoethyl)-5-((4-ethoxyphenyl)methylene)-2,4-thiazolidinedione is extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells. Currently, no specific inhibitors of the ERK proteins exist. Preferentially binds to ERK2 with a Kd of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1, but exhibits little effect on ERK1/2 phosphorylation by MEK1/2.
Extracellular signal-regulated kinase (ERK) docking domain inhibitor. Inhibits ERK binding rather then ERK activity at the ATP domain. IC50 = 25 μM in HeLa, A549, and SUM-159 tumor cells.
特點和優勢
This compound is featured on the MAPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
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The mitogen-activated protein kinase (MAPK) family consists of both stress activated (SAPK) and mitogen-activated (MAPK) protein kinases. They form a network of signal transduction cascades that mediate cellular responses to a diverse range of stimuli, including growth factors, chemical or osmotic stress, irradiation, bacterial infection and proinflammatory cytokines.
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