Adezmapimod (SB203580) 是一种p38 MAPK抑制剂,IC50为0.3-0.5 μM,与SAPK3(106T)和SAPK4(106T)相比选择性低10倍,且抑制PKB磷酸化,IC50为3-5 μM。Adezmapimod 不抑制 JNK 活性,是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。
别名:RWJ 64809; PB 203580; Adezmapimod
Adezmapimod (SB203580) 是一种p38 MAPK抑制剂,IC50为0.3-0.5 μM,与SAPK3(106T)和SAPK4(106T)相比选择性低10倍,且抑制PKB磷酸化,IC50为3-5 μM。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。Adezmapimod 不抑制 JNK 活性,是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。
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体外实验* | |
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细胞系 | CT6 cells,BA/F3 cells and PBMC/T cells |
方法 | 2–5 × 106 rested CT6 cells were resuspended in 2 ml of RPMI, 5% fetal calf serum and preincubated with inhibitors or vehicle control as indicated in figure legends. Cells were then stimulated with 20 ng/ml recombinant human IL-2 for 5 min at 37 °C and pelleted in a minifuge for 30 s, medium was aspirated, and the pellet was lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain (a generous gift from Professor T. Taniguchi, Tokyo, Japan) were maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/ml G418 (Calbiochem-Novabiochem) as described previously. Human peripheral blood mononuclear cells were prepared from buffy coat leukophoresis residues (North London Blood Transfusion Service, Colindale, London UK) and activated with 50 ng/ml OKT3 for 48 h. The cells were then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations were >90% T cells . Cellular proliferation assays were performed by measurement of [3H]thymidine incorporation as described previously. |
浓度 | 0~30 µm |
处理时间 | 24 h |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | Systemic lupus erythematosus (SLE) model (female MRL/lpr mice and female C57BL/6 mice) |
配制 | Dissolved in drinking water (250 μM) |
剂量 | 0.1 M/day |
给药处理 | orally |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 377.43 |
分子式 | C21H16FN3OS |
CAS号 | 152121-47-6 |
溶解性(25°C) | DMSO 20 mg/mL (ultrasonic and warming) |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.6495 mL | 13.2475 mL | 26.495 mL |
5 mM | 0.5299 mL | 2.6495 mL | 5.299 mL |
10 mM | 0.2649 mL | 1.3247 mL | 2.6495 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
其他相关的p38 MAPK产品 |
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HWY336
HWY336 is a selective, non-ATP competitive dual MKK4 and MKK7 inhibitor with IC50 values of 6 µM on MKK4 and 10 µM on MKK7 in vitro. HWY336 inhibits the phosphorylation of MKK4/MKK7 inside the activation loop or hinders the substrate to access the kinase. |
BSJ-04-122
BSJ-04-122 是一种共价 MKK4/7 双重抑制剂。BSJ-04-122 抑制 MKK4 和 MKK7,IC50 值分别为 4 nM 和 181 nM。 |
OVA-E1 peptide TFA
OVA-E1 peptide TFA 是SIINFEKL [OVA (257-264)拮抗突变体。 |
MBP MAPK Substrate
MBP MAPK Substrate 可以用作 MAPK 的外源底物。 |
OVA-E1 peptide
OVA-E1 peptide 是SIINFEKL [OVA (257-264)拮抗突变体。 |
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