计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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概述
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)
规格
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。
储存条件
-80℃储存
运输条件
特低温运输
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
PubChem CID
MeSH Entry Terms
SB 242235;SB-242235;SB242235
分子量
353.4
高级数据
关联靶点（人）
HSPB1
Tchem
热休克蛋白β-1(Heat shock protein beta-1)
(1 活性数据)
CSNK1D
Tchem
酪蛋白激酶 I 异构体 delta(Casein kinase I isoform delta)
(1 活性数据)
PRKCB
Tchem
蛋白激酶Cβ型(Protein kinase C beta type)
(1 活性数据)
MAPK14
Tchem
丝裂原活化蛋白激酶 14(Mitogen-activated protein kinase 14)
(1 活性数据)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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危险品化学品经营许可证（带存储）