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CAS No.: 152121-47-6

SB 203580 Catalog No. CSN11899

Synonyms: RWJ 64809;PB-203580;AdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimod

SB-203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 p38 MAPK

IC50:0.3-0.5μM
描述The stress-activated protein kinase (SAPK) p38 isoforms are mitogen-activated protein kinase (MAPK) family members. MAPKs act as an integration point for multiple biochemical signals, and are involved in a wide variety of cellular processes such as proliferation, differentiation, transcription regulation and development.
SB 203580 is a p38 MAPK inhibitor. SB 203580 inhibited the ATPase activity of non-phosphorylated p38 MAPK with a K_m of 9.6 mM. SB 203580 was competitive with ATP with a K_i of 21 nM, detected in a kinetic study of yeast expressed active p38 MAPK^[3]. 24h treatment of SB 203580 dose-dependently inhibited IL-1β-induced PGE₂ release with an EC₅₀ of 0.18 μM^[4].
SB 203580 was dissolved in drinking water at the concentration of 250 μM and orally administrated 0.4 ml/day to MRL/lpr mice aged from 14 to 22 weeks. SB203580 improved renal function by decreasing the levels of proteinuria and serum BUN, ameliorating the pathologic changes of kidney and reducing Ig and C3 depositions in the kidney. Moreover, hepatocytes necrosis, recruitment and proliferation of leucocytes in liver and spleen were found to be inhibited by administration of SB203580^[5].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HCA2	2.5 μM	Function Assay	-	Inhibits p38 mediated MK2 activation	17964780
Hela	-	Function Assay	-	Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM	18926711
hESCs	5 μM	Growth Inhibition Assay	-	Induces cardiomyogenic activity assessed as cell growth	23602399

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6495 mL
- 13.2473 mL
- 26.4946 mL
- 5 mM
- 0.5299 mL
- 2.6495 mL
- 5.2989 mL
- 10 mM
- 0.2649 mL
- 1.3247 mL
- 2.6495 mL

技术信息

CAS号

152121-47-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H16FN3OS

运输

蓝冰

分子量

377.43

别名

RWJ 64809;PB-203580;AdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimodAdezmapimod;SB-203850;SB 203580

溶解度

DMSO	100.0 mg/mL (264.9 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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HCA2	2.5 μM	Function Assay	-	Inhibits p38 mediated MK2 activation	17964780
Hela	-	Function Assay	-	Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM	18926711
hESCs	5 μM	Growth Inhibition Assay	-	Induces cardiomyogenic activity assessed as cell growth	23602399
IEC-18	10 μM	Function Assay	-	Inhibits LPS-induced p38 MAPK phosphorylation	23758110
PBMC	-	Function Assay	15 min	Inhibits the release of interleukin-1-beta with IC50 of 0.037 μM	12361396
PC12	10 μM	Kinase Assay	15 min	Inhibits p38 MAP kinase with IC50 of 0.6 μM	7750577
PC12	10 μM	Function Assay	-	Activates Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction	21345685
RAW 264.7	12.5 μM	Cytotoxic Assay	12h	Blocks lethal toxin-mediated cytotoxicity	17485504
RAW264.7	10 μM	Function Assay	-	Induces antiinflammatory activity by inhibiting IL-1β release	23791078
RAW264.7	10 μM	Function Assay	-	Induces antiinflammatory activity by inhibiting iNOS release	23791078
RAW264.7	10 μM	Function Assay	-	Induces antiinflammatory activity by inhibiting NO release	23791078
RAW264.7	10 μM	Function Assay	-	Inhibits LPS-induced p38 MAPK phosphorylation	24016057
SW1353	-	Function Assay	1 h	Inhibits IL-6 production with IC50 of 0.05 μM	11140741
THP-1	-	Function Assay	-	Inhibits LPS-induced TNFalpha production with IC50 of 0.16 μM	18325768
U937	-	Function Assay	-	Inhibits JAK-mediated interferon-gamma/anisomycin-induced Stat1 phosphorylation	18157122
U937	-	Function Assay	-	Inhibits JAK-mediated interferon-gamma/anisomycin-induced p38 phosphorylation	18157122

SB 203580 Catalog No. CSN11899

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