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质量水平
方案
≥98% (HPLC)
表单
powder
储存条件
desiccated
under inert gas
颜色
off-white
溶解性
DMSO: ≥4 mg/mL
储存温度
2-8°C
SMILES字符串
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 key
PQVLWVGMXJPJLG-NBYYMMLRSA-N
应用
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.
特点和优势
This compound is featured on the MAPKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
E Guerra et al.
Oncogene, 32(12), 1594-1600 (2012-05-09)
Our findings show that upregulation of a wild-type Trop-2 has a key controlling role in human cancer growth, and that tumour development is quantitatively driven by Trop-2 expression levels. However, little is known about the regulation of expression of the
Dexmedetomidine is neuroprotective in an in vitro model for traumatic brain injury
Schoeler, M., et al.
BMC Neurology, doi: 10-doi: 10 (2012)
Tony E Walshe et al.
Arteriosclerosis, thrombosis, and vascular biology, 29(8), 1185-1192 (2009-05-23)
Motivated by the central roles that vascular endothelial growth factor (VEGF) and transforming growth factor (TGF)-beta play in the assembly and maintenance of the vasculature, we examined the impact of systemic VEGF or TGF-beta signal inhibition on endothelial activation as
Yiming Zhang et al.
The Journal of biological chemistry, 287(22), 18562-18572 (2012-04-12)
Although neuromedin U (NMU) has been implicated in analgesia, the detailed mechanisms still remain unclear. In this study, we identify a novel functional role of NMU type 1 receptor (NMUR1) in regulating the transient outward K(+) currents (I(A)) in small
Mikihito Kajiya et al.
Molecular pharmacology, 82(1), 115-124 (2012-04-19)
Muscarinic type 3 receptor (M3R) plays a pivotal role in the induction of glandular fluid secretions. Although M3R is often the target of autoantibodies in Sjögren's syndrome (SjS), chemical agonists for M3R are clinically used to stimulate saliva secretion in
商品
丝裂原活化蛋白激酶(MAPK)家族由应激激活(SAPK)和丝裂原活化(MAPK)的蛋白激酶组成。了解它们介导细胞多种刺激反应的信号转导级联网络。
The mitogen-activated protein kinase (MAPK) family consists of stress-activated (SAPK) and MAPKs. Learn about their network of signal transduction cascades that mediate cellular responses to a diverse range of stimuli.
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