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SB 242235

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 193746-75-7
  • 分子式: C19H20FN5O
  • 分子量: 353.4
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
S655955-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 SB 242235
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。
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)

关联靶点(人)

HSPB1 Tchem 热休克蛋白β-1(Heat shock protein beta-1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CSNK1D Tchem 酪蛋白激酶 I 异构体 delta(Casein kinase I isoform delta) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PRKCB Tchem 蛋白激酶Cβ型(Protein kinase C beta type) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MAPK14 Tchem 丝裂原活化蛋白激酶 14(Mitogen-activated protein kinase 14) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES COC1=NC=CC(=N1)C2=C(N=CN2C3CCNCC3)C4=CC=C(C=C4)F
关联CAS 193746-75-7
PubChem CID 9863367
MeSH Entry Terms SB 242235;SB-242235;SB242235
分子量 353.4

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