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Product details

名称

SB 242235

分子类型

小分子

英文名称

SB 242235

货号

S655955-1ml

包装规格

1ml

浓度

10mM in DMSO

储存温度

-80℃储存

运输条件

超低温冰袋运输

产品介绍

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC 50 of 1.0 μM in primary human chondrocytes In Vitro SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 of 1.0 μM in human chondrocytes stimulated with IL-1β. SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Human chondrocytes Concentration: 0 μM,0.01 μM,0.1 μM,1 μM,10 μM Incubation Time: 15 minutes Result: Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM. In Vivo SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation. SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2. SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female SKH-1 hairless mice (4–6 weeks)Dosage: 100 mg/kg Administration: Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation Result: Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation. IC50& Target:IC50: 1.0 μM (p38 MAPK, primary human chondrocytes)

生化机理

SB-242235 是一种强效的选择性 p38 MAP 激酶抑制剂，在原代人类软骨细胞中的 IC 50 为 1.0u3000μM。

CAS号

193746-75-7(DMSO)

分子式

C19H20FN5O

分子量

353.4 g/mol

Smiles

COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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「No related articles yet」

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