869185-85-3|SB 203580 hydrochloride，≥98%|Medlife|Medlife为MCE，Selleck，麦克林，阿拉丁试剂，罗恩试剂，Sigma，安耐吉试剂，泰坦等同类产品品牌，上海现货，高性价比小分子化合物

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SB 203580 hydrochloride

p38-MAPK特异性抑制剂,SB 203580 hydrochloride是一种广泛使用的 p38 MAPK 抑制剂， IC50 介于 0.3-0.5 μM 之间。对 p38 MAPK 的选择性比 PKB, LCK, 和 GSK-3β高100倍

目录号: PC11782 纯度: ≥98%

CAS No. :869185-85-3

商品编号	规格	价格	会员价
PC11782-25mg	25mg	¥617.40	请登录
PC11782-50mg	50mg	¥823.20	请登录
PC11782-100mg	100mg	¥1430.80	请登录
PC11782-250mg	250mg	¥2763.60	请登录
PC11782-10mM (in 1mL DMSO)	10mM(in1mLDMSO)	¥490.00	请登录

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中文名称	SB 203580 hydrochloride
中文别名	SB 203580氢氯化物;SB 203580 (hydrochloride)
英文名称	SB 203580 hydrochloride
英文别名	SB 203580 hydrochloride;SB 203580 (hydrochloride);RWJ 64809 hydrochloride;SB-203580 hydrochloride;SB203580 hydrochloride;SB 2035850;SB 203580, Hydrochloride;PubChem24446;sb203580-hydrochloride;C21H16FN3OS.ClH;BCP29070;4024AH;4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole, HCl;RWJ 64809 hydrochloride;RWJ64809 HCl;SB203580 HCl;RWJ 64809 hydrochloride;SB203580 hydrochloride;SB
Cas No.	869185-85-3
分子式	C₂₁H₁₇ClFN₃Os
分子量	413.90
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator.

性状

Solid

IC50 & Target[1][2]

p38

50 nM (IC₅₀)

p38β2

500 nM (IC₅₀)

体外研究(In Vitro)

Adezmapimod hydrochloride (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.
Adezmapimod hydrochloride blocks PKB phosphorylation (IC₅₀ 3-5 μM). Adezmapimod hydrochloride inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.

Western Blot Analysis

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究(In Vivo)

Adezmapimod hydrochloride (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10). ?

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Information]

[2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitoge [Information]

[3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (241.60 mM; Need ultrasonic)

H₂O : 8.43 mg/mL (20.37 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4160 mL	12.0802 mL	24.1604 mL
5 mM	0.4832 mL	2.4160 mL	4.8321 mL
10 mM	0.2416 mL	1.2080 mL	2.4160 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.04 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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