基本信息

技术规格

物性(参考值)

相关法规

基本信息

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。

靶点（IC50 & Targe）

p38 MAPK,0.3μM-0.5μM

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]

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]

激酶实验

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-32PATP，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。

细胞实验

Cell lines: CT6细胞, BA/F3 F7细胞

Concentrations: 0-30 μM

Incubation Time: 1小时

Method:CT6细胞和BA/F3 F7细胞在RPMI培养基中冲洗三次，然后培养在含5%胎牛血清，生长因子，抗生素，β-巯基乙醇的RPMI培养基中。2-5×106个CT6细胞悬浮在含5%胎牛血清的2 ml RPMI培养基上, 用SB203580预处理。然后加入20 ng/ml重组人类IL-2，在37 oC下刺激细胞5分钟，离心30秒，溶解于合适buffer中。稳定表达IL-2受体β链缺失突变的BA/F3细胞维持在含谷氨酸，5%胎牛血清和0.2 μg/mL G418的RPMI培养基中。大规模冲洗细胞，过夜处理，在用IL-2激活前再次冲洗。通过测定[3H]胸苷的渗透率，进行细胞增殖实验。

(Only for Reference)

动物实验

Animal Models: 携带系统性红斑狼疮的雌性MRL/lpr鼠和雌性C57BL/6鼠

Formulation: 溶在饮用水中(250 μM)

Dosages: 0.4mL/天

Administration: 口服处理

(Only for Reference)

参考文献

[1] Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.

[2] Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.

[3] Zhang H, et al. Apoptosis, 2011

[4] Barancik M, et al. J Cardiovasc Pharmacol, 2000, 35(3), 474-83.

[5] Jin N, et al. Int Immunopharmacol, 2011, 11(9):1319-26.

安全信息

图形或危害标志
提示语	Danger
危险说明	H302 H318
防范说明	P280 P305+P351+P338
WGK	3
RTECS	UT3967600

产品说明

应用

使用SB 203580处理MDCK细胞以研究MAPK信号转导在诱导细胞膜的高渗性和钾耗竭中的作用。¹⁶ 它被用于抑制小鼠皮层神经元¹⁷和人肝细胞癌细胞系中的MAPK信号转导。¹⁸

包装

1 mg in glass bottle

生化/生理作用

SB 203580是一种吡啶基咪唑，可抑制MAPKAP激酶-2的活化，以及在体内抑制热休克蛋白(HSP)27对IL-1、细胞应激和细菌内毒素的反应磷酸化。它不可抑制JNK或p42 MAP激酶，因此可用于研究p38 MAPK和MAPKAP激酶-2的生理作用和靶点。已有研究显示它可诱导丝氨酸/苏氨酸激酶Raf-1的活化，并且据报道其可抑制细胞因子的产生。

特点和优势

该化合物是激酶磷酸酶生物学研究的推荐产品。点击此处，了解更多精选激酶磷酸酶生物学产品。了解更多有关用于其他研究领域的生物活性小分子的信息，请访问 sigma.com/discover-bsm。
该化合物在受体分类和信号转导手册中 MAPKs 页面中进行了详细介绍。想要浏览手册的其他页面， 请单击此处。

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H302 - H318
预防措施声明	P264 - P270 - P280 - P301 + P312 - P305 + P351 + P338 - P501
危险分类	Acute Tox. 4 Oral - Eye Dam. 1
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	dust mask type N95 (US), Eyeshields, Gloves

产品说明

一般描述

Reduces epirubicin-induced cell injury and caspase-3/7 activity. A highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 kinase (IC₅₀ = 34 nM in vitro, 600 nM in cells). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC₅₀ = 50-100 nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.
Reduces epirubicin-induced cell injury and caspase-3/7 activity. A highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC₅₀ = 34 nM in vitro, 600 nM in cells). Does not significantly inhibit the JNK and p42 MAP kinase at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC₅₀ = 50-100 nM). Inhibits bone morphogenetic protein-2-induced neurite outgrowth in PC12 cells. Also inhibits platelet aggregation caused by collagen (IC₅₀ = 0.2-1.0 µM) or the thromboxane analog U-46619 (Cat. No. 538944). A 1 mg/ml solution of SB 203580 (Cat. No. 559398) in anhydrous DMSO is also available.

包装

1 mg in Plastic ampoule
5, 10 mg in Glass bottle

生化/生理作用

Cell permeable: yes
Target IC₅₀: 34 nM against p38 MAP kinase in vitro, 600 nM in cells; 50-100 nM against IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1; 0.2-1.0 µM against platelet aggregation caused by collagen
Product competes with ATP.
Reversible: yes

警告

Toxicity: Irritant (B)

其他说明

Yamada. T., et al. 2012. Free Radic. Biol. Med. (In press)
Powell, D.J., et al. 2003. Mol. Cell Biol.23, 7794.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Iwasaki, S., et al. 1999. J. Biol. Chem.274, 26503.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.
Hazzalin, C.A., et al. 1996. Curr. Biol.6, 1028.
Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.
Saklatvala, J., et al. 1996. J. Biol. Chem. 271, 6586.
Cuenda, A., et al. 1995. FEBS Lett.364, 229.
Gallagher, T.F., et al. 1995. Bioorg. Med. Chem. Lett. 5, 1171.
Lee, J.C., et al. 1994. Nature 372, 739.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

象形图
警示用语：	Danger
危险声明	H302 - H318
预防措施声明	P264 - P270 - P280 - P301 + P312 - P305 + P351 + P338 - P501
危险分类	Acute Tox. 4 Oral - Eye Dam. 1
储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H332: Harmful if inhaled. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .