SB203580
目录号：S1076 别名： RWJ 64809, PB 203580
Molecular Weight(MW): 377.43
SB203580是一种p38 MAPK抑制剂，在THP-1细胞中IC50为0.3-0.5 μM，对SAPK3(106T)和SAPK4(106T)选择性低10倍，且阻断PKB磷酸化，IC50为3-5 μM。
客户使用该产品的5个实验数据：
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C57BL/6 male mice (8 weeks, Harlan) were pretreated with by intravenous injections with PERY or SCR peptides (15 mg/kg) or DMSO. The following day, mice were treated with 1.5% dextran sodium sulfate (DSS) in drinking water for 7 days followed by 3 days of normal drinking water. During DSS administration, mice were treated every other day (total of five intravenous injections). Control groups included nontreated mice (no DSS, no treatment) and mice receiving PERY peptide with normal drinking water (PERY only, no DSS). Mice were then euthanized and analyzed. Colitis was evaluated using (C) hematoxylin and eosin (H&E) histological sections of the colons (top) and their magnifications (bottom). Scale bar, 2 mm.
Science, 2018, 11(525), doi: 10.1126/scisignal.aao3428. SB203580 purchased from Selleck.
A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
J Biol Chem 2010 285, 32824-32833. SB203580 purchased from Selleck.
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A, effect of p38 MAPK inhibitor SB203580 (1, 5, and 10 μM) on SRP72 phosphorylation was evaluated. Jurkat cells were stimulated with rhIL-1, harvested at 0, 120, and 240 min, lysed, and immunoprecipitated using anti-human SRP19 andWBusing anti-phosphoserine antibodies. A decreased intensity of SRP72 band was found when using the inhibitor at concentration of 1μM at 240 min and 5 and 10 μM at 120 and 240 min. B, results were analyzed and RUA illustrated, finding significant results at 1 μM 240 versus 120, 5, and 10 μM at 120 versus 0 and 240 versus 0 min *, p<0.05.
J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.
We used real time RT-PCR to investigate the effects of SB203580 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.
J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.
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Strain-induced BMMSC migration was mediated by p38 activity in vitro. The mechanical strain (static, 6%) significantly promoted BMMSC migration, and this effect was abolished by inhibition of p38 phosphorylation.
Arch Oral Biol, 2017, 76:55-60. SB203580 purchased from Selleck.
产品安全说明书
p38 MAPK抑制剂选择性比较
生物活性
| 产品描述 | SB203580是一种p38 MAPK抑制剂，在THP-1细胞中IC50为0.3-0.5 μM，对SAPK3(106T)和SAPK4(106T)选择性低10倍，且阻断PKB磷酸化，IC50为3-5 μM。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 特性 | SB203580是第一个被报道的p38抑制剂。 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 体外研究 |
SB203580作用于人类T细胞,鼠CT6 T细胞, 或BAF F7 B细胞，抑制IL-2诱导的增殖，IC50为3-5 μM。SB203580也抑制IL-2诱导的p70S6K激活, IC50 > 10 μM。SB203580也抑制PDK1活性，IC50为3-10 μM，这种抑制存在剂量依赖性。[1]SB203580抑制MAPKAPK2中p38-MAPK的刺激，IC50 为0.07 μM, 然而抑制完整SAPK/JNK活性时，IC50为3-10 μM。SB203580 高浓度时激活ERK通路,随后增强NF-κB转录活性。[2]SB203580作用于人类肝癌细胞(HCC)，诱导自体吞噬。[3] |
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| 体内研究 | SB203580作用于缺血性损伤，保护猪的心肌层。[4] SB203580有效保护携带系统性红斑狼疮的MRL/lpr鼠和治疗疾病。[5] |
推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)
| 激酶实验： |
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细胞受体激酶磷酸化实验 : 4 μg羊PKBα抗体固定在25 μL蛋白G-亲和层析柱上过夜(或1.5 小时) ，用Buffer A (50 mM Tris, pH 为7.5, 1 mM EDTA, 1 mM EGTA, 0.5 mM Na3VO4, 0.1% β-巯基乙醇，1% Triton X-100, 50 mM NaF, 5 mM焦磷酸钠, 0.1 mM苯甲磺酰氟, 1 μg/mL抑蛋白酶肽, 抑肽素, 亮抑酶肽,及1 μM微囊藻素)冲洗。固定的PKB抗体和0.5 ml细胞溶解物温育1.5小时，用含0.5 M NaCl的0.5 mL Buffer A冲洗三次, 再用0.5 mL Buffer B (含50 mM Tris-HCl, pH为7.5, 0.03% (w/v) Brij-35, 0.1 mM EGTA, 及 0.1% β-巯基乙醇)冲洗二次,最后用100 μL实验稀释buffer冲洗二次; 5×实验稀释buffer包含100 mM MOPS, pH为7.2, 125 mM β-甘油磷酸, 25 mM EGTA, 5 mM原钒酸钠, 及5 mM DTT。10 μL实验稀释buffer，40 μM蛋白激酶A抑制肽, 100 μM PKB-特定底物肽,及10 μCi [γ-32P]ATP，加到PKB酶免疫复合物中。反应在室温下震荡温育20分钟，40 μL反应物转移到其他试管中，加入20 μL 40%三氯乙酸，终止反应。在室温下混合，温育5分钟，40 μL转移到P81磷酸纤维素纸上，亲和处理30秒 。P81纸在0.75%磷酸中洗三次，然后在室温下加到丙酮中。 使用闪烁计数器测量γ-32P 渗透率。 |
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| 细胞实验： |
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| 动物实验： |
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溶解度 (25°C)
| 体外 | DMSO | 43 mg/mL (113.92 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| 体内 |
从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 4% DMSO+30% PEG 300+5% Tween 80+ddH2O |
5mg/mL |
* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。
化学数据
| 分子量 | 377.43 |
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| 化学式 | C21H16FN3OS |
| CAS号 | 152121-47-6 |
| 稳定性 | powder |
| in solvent | |
| 别名 | RWJ 64809, PB 203580 |
计算器
摩尔浓度计算器
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。
稀释计算器
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )
在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
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