- 抑制劑
- 研究領(lǐng)域
- PI3K/Akt/mTOR信號(hào)通路
- 表觀遺傳
- 甲基化
- 免疫&炎癥
- 酪氨酸蛋白激酶
- 血管生成
- 凋亡
- 自噬
- 內(nèi)質(zhì)網(wǎng)應(yīng)激&UPR響應(yīng)
- JAK/STAT信號(hào)通路
- MAPK信號(hào)通路
- 細(xì)胞骨架
- 細(xì)胞周期
- TGF-beta/Smad信號(hào)通路
- DNA損傷/DNA修復(fù)
- 化合物庫(kù)
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 動(dòng)物實(shí)驗(yàn)
- 鼠尾直接PCR試劑盒(快速基因型鑒定)
- 小鼠CD3+ T細(xì)胞分選試劑盒
- 小鼠CD4+ T細(xì)胞分選試劑盒
- 小鼠CD8+ T細(xì)胞分選試劑盒
- 新產(chǎn)品
- 聯(lián)系我們
Adezmapimod (SB203580)
別名: RWJ 64809, PB 203580
此產(chǎn)品請(qǐng)避光密封保存。
Adezmapimod (SB203580, RWJ 64809, PB 203580) 是一種p38 MAPK抑制劑，在THP-1細(xì)胞中IC50為0.3-0.5 μM，對(duì)SAPK3(106T)和SAPK4(106T)選擇性低10倍，且阻斷PKB磷酸化，IC50為3-5 μM。SB203580 可誘導(dǎo)線粒體自噬和細(xì)胞自噬。
Adezmapimod (SB203580) Chemical Structure
CAS: 152121-47-6
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
Adezmapimod (SB203580)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | p38α p38β | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)產(chǎn)品 | SB202190 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate PH-797804 VX-702 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L Asiatic Acid TAK-715 Pamapimod Pexmetinib SD 0006 R1487 PD 169316 | 點(diǎn)擊展開(kāi) |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) MAPK抑制劑庫(kù) 細(xì)胞周期化合物庫(kù) TGF-beta/Smad信號(hào)通路庫(kù) 抗阿爾茨海默病化合物庫(kù) | 點(diǎn)擊展開(kāi) |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Adezmapimod (SB203580, RWJ 64809, PB 203580) 是一種p38 MAPK抑制劑，在THP-1細(xì)胞中IC50為0.3-0.5 μM，對(duì)SAPK3(106T)和SAPK4(106T)選擇性低10倍，且阻斷PKB磷酸化，IC50為3-5 μM。SB203580 可誘導(dǎo)線粒體自噬和細(xì)胞自噬。 | ||||
|---|---|---|---|---|---|
| 特性 | SB203580是第一個(gè)被報(bào)道的p38抑制劑。 | ||||
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | SB203580作用于人類T細(xì)胞,鼠CT6 T細(xì)胞, 或BAF F7 B細(xì)胞，抑制IL-2誘導(dǎo)的增殖，IC50為3-5 μM。SB203580也抑制IL-2誘導(dǎo)的p70S6K激活, IC50 > 10 μM。SB203580也抑制PDK1活性，IC50為3-10 μM，這種抑制存在劑量依賴性。[1]SB203580抑制MAPKAPK2中p38-MAPK的刺激，IC50 為0.07 μM, 然而抑制完整SAPK/JNK活性時(shí)，IC50為3-10 μM。SB203580 高濃度時(shí)激活ERK通路,隨后增強(qiáng)NF-κB轉(zhuǎn)錄活性。[2]SB203580作用于人類肝癌細(xì)胞(HCC)，誘導(dǎo)自體吞噬。[3] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 細(xì)胞受體激酶磷酸化實(shí)驗(yàn) | |||
| 4 μg羊PKBα抗體固定在25 μL蛋白G-親和層析柱上過(guò)夜(或1.5 小時(shí)) ，用Buffer A (50 mM Tris, pH 為7.5, 1 mM EDTA, 1 mM EGTA, 0.5 mM Na3VO4, 0.1% β-巰基乙醇，1% Triton X-100, 50 mM NaF, 5 mM焦磷酸鈉, 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)沖洗。固定的PKB抗體和0.5 ml細(xì)胞溶解物溫育1.5小時(shí)，用含0.5 M NaCl的0.5 mL Buffer A沖洗三次, 再用0.5 mL Buffer B (含50 mM Tris-HCl, pH為7.5, 0.03% (w/v) Brij-35, 0.1 mM EGTA, 及 0.1% β-巰基乙醇)沖洗二次,最后用100 μL實(shí)驗(yàn)稀釋buffer沖洗二次; 5×實(shí)驗(yàn)稀釋buffer包含100 mM MOPS, pH為7.2, 125 mM β-甘油磷酸, 25 mM EGTA, 5 mM原釩酸鈉, 及5 mM DTT。10 μL實(shí)驗(yàn)稀釋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酶免疫復(fù)合物中。反應(yīng)在室溫下震蕩溫育20分鐘，40 μL反應(yīng)物轉(zhuǎn)移到其他試管中，加入20 μL 40%三氯乙酸，終止反應(yīng)。在室溫下混合，溫育5分鐘，40 μL轉(zhuǎn)移到P81磷酸纖維素紙上，親和處理30秒 。P81紙?jiān)?.75%磷酸中洗三次，然后在室溫下加到丙酮中。 使用閃爍計(jì)數(shù)器測(cè)量γ-32P 滲透率。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | CT6細(xì)胞, BA/F3 F7細(xì)胞 | ||
| 濃度 | 0-30 μM | |||
| 孵育時(shí)間 | 1小時(shí) | |||
| 方法 | CT6細(xì)胞和BA/F3 F7細(xì)胞在RPMI培養(yǎng)基中沖洗三次，然后培養(yǎng)在含5%胎牛血清，生長(zhǎng)因子，抗生素，β-巰基乙醇的RPMI培養(yǎng)基中。2-5×106個(gè)CT6細(xì)胞懸浮在含5%胎牛血清的2 ml RPMI培養(yǎng)基上, 用SB203580預(yù)處理。然后加入20 ng/ml重組人類IL-2，在37 oC下刺激細(xì)胞5分鐘，離心30秒，溶解于合適buffer中。穩(wěn)定表達(dá)IL-2受體β鏈缺失突變的BA/F3細(xì)胞維持在含谷氨酸，5%胎牛血清和0.2 μg/mL G418的RPMI培養(yǎng)基中。大規(guī)模沖洗細(xì)胞，過(guò)夜處理，在用IL-2激活前再次沖洗。通過(guò)測(cè)定[3H]胸苷的滲透率，進(jìn)行細(xì)胞增殖實(shí)驗(yàn)。 |
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| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | 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 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | SB203580作用于缺血性損傷，保護(hù)豬的心肌層。[4] SB203580有效保護(hù)攜帶系統(tǒng)性紅斑狼瘡的MRL/lpr鼠和治療疾病。[5] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | 攜帶系統(tǒng)性紅斑狼瘡的雌性MRL/lpr鼠和雌性C57BL/6鼠 |
| Dosages | 0.4mL/天 | |
| Administration | 口服處理 | |
化學(xué)信息&溶解度
| 分子量 | 377.43 | 分子式 | C21H16FN3OS |
| CAS號(hào) | 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 | ||
| 儲(chǔ)存條件(自收到貨起) | 3年 -20°C(避光) 粉狀 | ||
|
體外溶解度 |
DMSO : 38 mg/mL ( (100.68 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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