Adezmapimod (SB203580)
别名: RWJ 64809, PB 203580
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Adezmapimod (SB203580, RWJ 64809, PB 203580) 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。SB203580 可诱导线粒体自噬和细胞自噬。
Adezmapimod (SB203580) Chemical Structure
CAS: 152121-47-6
产品质控
批次：
纯度：
99.98%
99.98
Adezmapimod (SB203580)相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| RAW 264.7 | Cytotoxic Assay | 12.5 μM | 12h | Blocks lethal toxin-mediated cytotoxicity | 17485504 |
| PC12 | Kinase Assay | 10 μM | 15 min | Inhibits p38 MAP kinase with IC50 of 0.6 μM | 7750577 |
| HCA2 | Function Assay | 2.5 μM | Inhibits p38 mediated MK2 activation | 17964780 | |
| PC12 | Function Assay | 10 μM | Activates Nrf2/ARE in rat PC12 cells assessed as HO-1 protein induction | 21345685 | |
| hESCs | Growth Inhibition Assay | 5 μM | Induces cardiomyogenic activity assessed as cell growth | 23602399 | |
| RAW264.7 | Function Assay | 10 μM | Induces antiinflammatory activity by inhibiting IL-1β release | 23791078 | |
| RAW264.7 | Function Assay | 10 μM | Induces antiinflammatory activity by inhibiting iNOS release | 23791078 | |
| RAW264.7 | Function Assay | 10 μM | Induces antiinflammatory activity by inhibiting NO release | 23791078 | |
| RAW264.7 | Function Assay | 10 μM | Inhibits LPS-induced p38 MAPK phosphorylation | 24016057 | |
| IEC-18 | Function Assay | 10 μM | Inhibits LPS-induced p38 MAPK phosphorylation | 23758110 | |
| whole blood cell | Function assay | 0.01 to 100 uM | Inhibition of p38-related IL1-beta release by whole blood cells at 10 e-4 to 10 e-8 M, IC50 = 0.35 μM. | 12852754 | |
| whole blood cell | Function assay | 0.01 to 100 uM | Inhibition of p38-related TNF-alpha release by whole blood cells at 10 e-4 to 10 e-8 M, IC50 = 0.94 μM. | 12852754 | |
| WS | Function assay | 2.5 uM | Inhibition of anisomycin-induced P38-alpha activation in human human TERT-immortalised WS cells assessed as HSP27 phosphorylation at 2.5 uM | 17659871 | |
| SW1353 | Function Assay | 1 h | Inhibits IL-6 production with IC50 of 0.05 μM | 11140741 | |
| PBMC | Function Assay | 15 min | Inhibits the release of interleukin-1-beta with IC50 of 0.037 μM | 12361396 | |
| Sf9 | Function assay | 30 mins | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay, IC50 = 0.01 μM. | 26455654 | |
| BMDC | Antiinflammatory assay | 1 hr | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 3.5 μM. | 24047259 | |
| BMDC | Antiinflammatory assay | 1 hr | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 5 μM. | 24047259 | |
| BMDC | Antiinflammatory assay | 1 hr | Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA, IC50 = 7.5 μM. | 24047259 | |
| macrophage-like cell | Antiinflammatory assay | 30 mins | Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA, IC50 = 8.6 μM. | 23811089 | |
| U937 | Function Assay | Inhibits JAK-mediated interferon-gamma/anisomycin-induced Stat1 phosphorylation | 18157122 | ||
| Hela | Function Assay | Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM | 18926711 | ||
| THP-1 | Function Assay | Inhibits LPS-induced TNFalpha production with IC50 of 0.16 μM | 18325768 | ||
| U937 | Function Assay | Inhibits JAK-mediated interferon-gamma/anisomycin-induced p38 phosphorylation | 18157122 | ||
| sf21 | Function assay | Binding affinity to wild type human biotin labelled p38 alpha (9 to 352 residues) expressed in sf21 insect cells SPR analysis, Kd = 0.0217 μM. | 28834431 | ||
| PBMC | Function assay | Inhibition of TNF-alpha production by lipopolysaccharide-stimulated human peripheral blood mononuclear cells, IC50 = 0.025 μM. | 9873730 | ||
| PBMC | Function assay | Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs), IC50 = 0.025 μM. | 9784093 | ||
| PBMC | Function assay | Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC), IC50 = 0.037 μM. | 12061876 | ||
| PBMC | Function assay | Inhibition of LPS-induced IL1-beta production in human peripheral blood mononuclear cells(PBMCs), IC50 = 0.048 μM. | 9784093 | ||
| SW1353 | Function assay | Compound was evaluated for its ability to inhibit IL-6 production in SW1353 cells treated with cytokines IL-1 and TNF, IC50 = 0.05 μM. | 10999467 | ||
| SW1353 | Function assay | Inhibition of TNF and IL-1 induced IL-6 production in human chondro-sarcoma SW 1353 cells, IC50 = 0.05 μM. | 10999468 | ||
| THP1 | Function assay | Inhibition of LPS-stimulated IL1 production in human THP1 cells, IC50 = 0.05 μM. | 18077363 | ||
| THP1 | Function assay | Inhibition of LPS-stimulated TNFalpha production in human THP1 cells, IC50 = 0.05 μM. | 18077363 | ||
| THP1 | Function assay | Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells, EC50 = 0.06 μM. | 12086485 | ||
| THP1 | Function assay | Inhibition of tumor necrosis factor alpha release by THP-1 cells, IC50 = 0.07 μM. | 15658855 | ||
| monocytic cell | Function assay | Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells, IC50 = 0.072 μM. | 12729637 | ||
| THP1 | Function assay | Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1), IC50 = 0.072 μM. | 15139749 | ||
| THP-1 | Function assay | Inhibitory activity against lipopolysaccharide stimulated TNF-alpha production in THP-1 cells (human monocytic cells), IC50 = 0.072 μM. | 15837310 | ||
| THP1 | Function assay | Inhibition of LPS-stimulated TNFalpha production in THP1 cells, IC50 = 0.072 μM. | 16750367 | ||
| PBMC | Function assay | Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs), IC50 = 0.16 μM. | 9784093 | ||
| PBMC | Function assay | Concentration required to inhibit lipopolysaccharide induced TNF-alpha release was determined in human peripheral blood mononuclear cells, IC50 = 0.19 μM. | 15454231 | ||
| Sf9 | Function assay | Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay, IC50 = 0.2 μM. | 26455654 | ||
| HEK293F | Function assay | Inhibition of sodium arsenate activated N-terminal GST-tagged Brugia malayi MPK1 expressed in HEK293F cells using FAM-p38tide as substrate by IMAP assay, IC50 = 0.22 μM. | 29541362 | ||
| HEK-293 | Function assay | Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion, IC50 = 0.25 μM. | 27109867 | ||
| PBMC | Function assay | Inhibition of p38 MAP kinase related TNF-alpha release from peripheral blood mononuclear cells (PBMC), IC50 = 0.59 μM. | 12061876 | ||
| PBMC | Function assay | Inhibition of the release of tumor necrosis factor alpha from peripheral blood mononuclear cells, IC50 = 0.59 μM. | 12361396 | ||
| PBMC | Function assay | Inhibitory activity against TNF-alpha release in PBM cells, IC50 = 0.59 μM. | 12852754 | ||
| HEK-293 | Function assay | Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion, IC50 = 6.31 μM. | 27109867 | ||
| WS | Function assay | Inhibition of MK2 mediated HSP27 phosphorylation in immortalised WS cells assessed as reduction in F-actin stress fibres | 17964780 | ||
| WS | Function assay | Inhibition of p38 mediated MK2 activation in WS cells | 17964780 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Adezmapimod (SB203580, RWJ 64809, PB 203580) 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。SB203580 可诱导线粒体自噬和细胞自噬。 | ||||
|---|---|---|---|---|---|
| 特性 | SB203580是第一个被报道的p38抑制剂。 | ||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 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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|---|---|---|---|---|
| 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-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。 | ||||
| 细胞实验 | 细胞系 | CT6细胞, BA/F3 F7细胞 | ||
| 浓度 | 0-30 μM | |||
| 孵育时间 | 1小时 | |||
| 方法 | 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | phospho-p38 / p38 p-ASK1 / ASK1 / P-JNK / p-MKK4 / p-ERK phospho-MK2(T334) / phospho-HSP27(S82) / phospho-Akt(T308) / phospho-Akt(S473) |
|
25747578 | |
| Immunofluorescence | dsRNA / hnRNP A1 |
|
25747578 | |
| Growth inhibition assay | Cell viability |
|
23001390 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 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] |
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|---|---|---|
| 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 |
| Dosages | 0.4mL/天 | |
| Administration | 口服处理 | |
化学信息&溶解度
| 分子量 | 377.43 | 分子式 | C21H16FN3OS |
| CAS号 | 152121-47-6 | SDF | Download Adezmapimod (SB203580) SDF |
| Smiles | CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F | ||
| 储存条件(自收到货起) | 3年 -20°C(避光) 粉状 | ||
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体外溶解度 |
DMSO : 38 mg/mL ( (100.68 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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