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SB 202190

产品编号 T2301 CAS 152121-30-7

别名: FHPI, SB202190

SB 202190 (FHPI) 是一种 p38 MAPK 抑制剂，可以抑制 p38α 和 p38β2 (IC50=50/100 nM)，具有选择性和细胞渗透性。SB 202190 具有抗肿瘤活性，还可以诱导人胚胎干细胞向心肌细胞分化。

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SB 202190, CAS 152121-30-7

规格	价格/CNY	货期
10 mg	￥ 467	现货
25 mg	￥ 839	现货
50 mg	￥ 997	现货
100 mg	￥ 1,675	现货
200 mg	￥ 2,683	现货
1 mL * 10 mM (in DMSO)	￥ 333	现货

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其他形式的 SB 202190:

SB 202190 hydrochloride
询价

选择批次

纯度: 99.84%

纯度: 99.73%

纯度: 99.67%

纯度: 99.66%

纯度: 99.55%

纯度: 99.21%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	SB 202190 (FHPI) is a p38 MAPK inhibitor that inhibits p38α and p38β2 (IC50=50/100 nM) selectively and cell-permeably. SB 202190 has antitumor activity and also induces the differentiation of human embryonic stem cells into cardiomyocytes.
靶点活性	p38β:100 nM (cell free), p38α:50 nM (cell free)
体外活性	方法：人 Tenon 成纤维细胞用 SB 202190 (5-50 μM) 处理，使用 MTT assay 检测细胞活力。结果：SB 202190 对细胞有毒性，IC50 为 17.2 μM。[1] 方法：人脐静脉内皮细胞 HUVEC 用 SB 202190 (0.1-10 μM) 处理 6-48 h，使用 Western Blot 方法检测靶点蛋白表达水平。结果：SB 202190 孵育 24 小时后，LC3A/B-I 转化为 PE 偶联的 LC3A/B-II 以浓度依赖的方式增加。[2]
体内活性	方法：为研究 p38 MAPK 在急性内毒素血症小鼠中的作用，将 SB 202190 (2 mg/kg) 腹腔注射给 C57BL/6 小鼠，30 min 后注射 LPS (10 mg/kg)。结果：SB 202190 预处理可降低 TNF-α水平，显著逆转 LPS 诱导的左心室抑制，降低 LPS 诱导的死亡率。[3] 方法：为检测体内抗肿瘤活性，将 SB 202190 (5 mg/kg) 和 OSI-027 (10 mg/kg) 腹腔注射给携带人 CRC 肿瘤 SW620 的 BALB/c 小鼠，每天一次，持续十天。结果：单独使用 SB 202190 增强了 SW620 异种移植物的肿瘤增殖和肿瘤负荷。SB 202190 和 OSI-027 的联合显著减弱了异种移植物肿瘤的生长。[4]
激酶实验	All protein kinase activities were linear with respect to time in every incubation. Assays were performed either manually for 10 min at 30 °C in 50 μl incubations using [γ-32P]ATP or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 min at ambient temperature in 25 μl incubations using [γ-32P]ATP. The concentrations of ATP and magnesium acetate were 0.1 mM and 10 mM respectively, unless stated otherwise. This concentration of ATP is 5–10-fold higher than the Km for ATP of most of the protein kinases studied in the present paper, but lower than the normal intracellular concentration, which is in the millimolar range. All assays were initiated with MgATP. Manual assays were terminated by spotting aliquots of each incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays were terminated by the addition of 5 μl of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers were then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity [1].
细胞实验	For transfection, A549 cells were seeded in 6-well plates to obtain 30% confluence at the time of transfection. Xtreme siRNA transfection reagent was used to transfect siRNA to a final concentration of 100 nM. Inhibition of gene expression by siRNA was determined after 48 hours by Western analysis. Cells were harvested, and the nuclear extract or total cell lysate was assayed for AP-1 DNA binding or Western blotting, respectively. HEK293T cells were cultured in complete DMEM. phCMV2-HA-MLK3 was transfected into HEK293T cells using genejammer transfection reagent using manufacturer's instructions. After 48 hours, cells were either untreated or treated with 5 or 10 μM SB202190 or SB203580 for 4 hours. Following treatment cell lysates were prepared using lysis buffer (50 mM Tris-HCl at pH 7.5, 5 mM EDTA, 150 mM NaCl, 1% Triton X-100, 50 mM NaF, 10 mM sodium pyrophosphate, 25 mM β- glycerophosphate, 1 mM PMSF, 30 μL/mL aprotinin, and 1 mM Na3VO4). 500 μg of total protein was immunoprecipitated with anti-HA-agarose conjugate. Phospho-MLK3 (Thr277/Ser281) was detected in western blotting using phosphospecific antibodies. The expression vector was transfected into HEK293T cells using Genejammer as stated earlier. After 48 hours, cell lysates was prepared and Flag-MKK7 was immunoprecipitated using anti-Flag-agarose conjugate. The Flag-MKK7 was used as a substrate for MLK3 kinase assay [3].
动物实验	The pharmacological efficacy of SB-ULS-LZM was evaluated in the unilateral ischemia-reperfusion (I/R) rat model. At 2 h before the ischemia procedure, rats were injected with SB-ULS-LZM (32 mg/kg. conjugate, equivalent to 752 g/kg SB202190), vehicle (5% glucose), or free SB202190 (800 g/kg). SB-ULS-LZM was dissolved in 5% glucose, whereas SB202190 was dissolved in 20% hydroxypropyl-β-cyclodextrin solution with 5% dimethyl sulfoxide as described earlier. Compounds were administered i.v. via the penis vein as described above. Animals were allowed to recover and placed back into the cages until the induction of renal ischemia. Rats were operated, and the renal artery and vein were clamped under microscope to stop renal blood flow. After 45 min, clamps were removed, and reperfusion of the kidney was observed before closing of the wound. Sham-operated animals (n 3) received the same surgical procedure, with the exception of ischemia, and were included as a control group. After 4 days, animals were sacrificed, and blood samples were collected from the abdominal aorta. Kidneys were isolated after gently flushing the organs with saline and preserved in 4% formalin for preparation of paraffin-embedded sections or frozen in ice-cold isopentane for preparation of cryosections [2].

别名	FHPI, SB202190
化合物与蛋白结合的复合物	Crystal structure of the first bromodomain of human BRD4 in complex with SB 202190
分子量	331.34
分子式	C20H14FN3O
CAS No.	152121-30-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33.1 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.018 mL	15.0902 mL	30.1805 mL	75.4512 mL
	5 mM	0.6036 mL	3.018 mL	6.0361 mL	15.0902 mL
	10 mM	0.3018 mL	1.509 mL	3.018 mL	7.5451 mL
	20 mM	0.1509 mL	0.7545 mL	1.509 mL	3.7726 mL
	50 mM	0.0604 mL	0.3018 mL	0.6036 mL	1.509 mL
	100 mM	0.0302 mL	0.1509 mL	0.3018 mL	0.7545 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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浓度

容积

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浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Nassar K, et al. A p38 MAPK inhibitor improves outcome after glaucoma filtration surgery. J Glaucoma. 2015 Feb;24(2):165-78. 2. Schwartz M, et al. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. Oncotarget. 2018 May 1;9(33):23149-23163. 3. Peng T, et al. Inhibition of p38 MAPK decreases myocardial TNF-alpha expression and improves myocardial function and survival in endotoxemia. Cardiovasc Res. 2003 Oct 1;59(4):893-900. 4. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56. 5. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798. 6. Yang C W, Hsu H Y, Chang H Y, et al. Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis[J]. Biochemical Pharmacology. 2020: 114122.

文献引用

1. Yang S, Yang S, Zhang H, et al. Targeting Na+/K+‐ATPase by berbamine and ouabain synergizes with sorafenib to inhibit hepatocellular carcinoma. British Journal of Pharmacology. 2021 2. Chen H, He A, Li H, et al. TSSK4 upregulation in alveolar epithelial type-II cells facilitates pulmonary fibrosis through HSP90-AKT signaling restriction and AT-II apoptosis. Cell Death & Disease. 2021, 12(10): 1-1 3. Hu H, Jiang H, Zhang K, et al. Memantine nitrate MN-08 suppresses NLRP3 inflammasome activation to protect against sepsis-induced acute lung injury in mice. Biomedicine & Pharmacotherapy. 2022, 156: 113804 4. Yang C W, Hsu H Y, Chang H Y, et al. Natural cardenolides suppress coronaviral replication by downregulating JAK1 via a Na+/K+-ATPase independent proteolysis. Biochemical Pharmacology. 2020: 114122. 5. Zou X, Zeng M, Zheng Y, et al.Comparative Study of Hydroxytyrosol Acetate and Hydroxytyrosol in Activating Phase II Enzymes.Antioxidants.2023, 12(10): 1834. 6. Ouyang P, Tao Y, Wei W, et al.Spring Viremia of Carp Virus Infection Induces Carp IL-10 Expression, Both In Vitro and In Vivo.Microorganisms.2023, 11(11): 2812. 7. Feng L, Wang C, Zhang C, et al.p38 MAPK inhibitor SB202190 suppresses ferroptosis in the glutamate-induced retinal excitotoxicity glaucoma model.Neural Regeneration Research.10.4103.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

SB 202190 152121-30-7 Apoptosis Autophagy MAPK p38 MAPK colorectal inhibit Inhibitor memory ATP anti-cancer learning SB-202190 FHPI SB202190 pocket spatial deficits inhibitor

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SB 202190

存储

溶解度

溶液配制表

计算器

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参考文献

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剂量换算

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