Home MAPK p38 MAPK inhibitor - Autophagy activator - Apoptosis related inhibitor - Ferroptosis inhibitor SB202190 仅限科研使用

SB202190

别名: FHPI

SB202190是一种有效的p38 MAPK抑制剂，靶向作用于p38α/β，无细胞试验中IC50为50 nM/100 nM，有时用于代替SB 203580研究其在体内对SAPK2a/p38的潜在作用。SB202190 可通过诱导自噬和血红素氧化酶1来抑制内皮细胞的凋亡。SB202190可显著抑制Erastin依赖的铁死亡ferroptosis。

SB202190 Chemical Structure

SB202190 Chemical Structure

CAS: 152121-30-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1091.41 现货
25mg 1189.49 现货
100mg 3017.14 现货
1g 13677.3 现货
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SB202190相关产品

相关信号通路图

p38 MAPK Signaling Pathways

p38 MAPK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
MKN-45 Function Assay 10 µM 30 min significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression 24479681
AGS  Function Assay 10 µM 30 min significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression 24479681
MKN-45 Function Assay 10 µM 30 min attenuates IL-1β-induced GA cell migration and invasion 24479681
AGS  Function Assay 10 µM 30 min attenuates IL-1β-induced GA cell migration and invasion 24479681
MKN-45 Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 24479681
AGS  Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 24479681
HUVECs  Function Assay 10 µM 1 h inhibits TNF-α-induced CXCL1 production 24487964
MC3T3-E1 Function Assay 30 μM 1 h attenuates TNF-α-stimulated p38 MAPK phosphorylation 24502696
MC3T3-E1 Function Assay 0.3/3/30 μM 1 h attenuates TNF-α-induced MMP-9 expression in a concentration-dependent manner  24502696
H1703 Function Assay 10 µM 6 h significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
H520 Function Assay 10 µM 6 h significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
H1703 Function Assay 10 µM 12 h inhibits pemetrexed-elicited MSH2 protein stability 24530475
H520 Function Assay 10 µM 12 h inhibits pemetrexed-elicited MSH2 protein stability 24530475
H1703 Function Assay 10 µM 1 h decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
H520 Function Assay 10 µM 1 h decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
AGS Function Assay 5 μM 30 min suppresses 1-induced caspase-8 and caspase-3 activation 24547878
PDL  Function Assay 20 μM  30 min significantly inhibits the tensile force-mediated BMP-2 expression 24561081
macrophages Function Assay 1 μM 4.5 h completely inhibits MT-III-induced activation of NF-κB 24808633
MDDCs Function Assay 10 μM 3.5 h blocks EBOV GP, but not VSV G mediated entry into human MDDCs 24815087
MDDCs Function Assay 0-15 μM 48 h inhibits MIP-1a, MIP-1b and RANTES production 24815087
MDDCs Function Assay 0-15 μM 48 h suppresses IFN-α and IP-10 production  24815087
HSCs Apoptosis Assay 25 μM 24 h significantly attenuates TG-induced activated HSCs apoptosis 24961950
H9c2 Function Assay 50 μM  12 h reduces LDH release and MMP loss 25245818
HaCaT  Function Assay 40 μM 3-24 h reduces the accumulation of ZO-1 25435485
RAW 264.7 Function Assay 10 μM 30 min attenuates the effects of OPG on osteoclast retraction 25461399
RAW 264.7 Function Assay 10 μM 30 min induces characteristic vacuolation of OCs  25461399
WB Function Assay 20 μM  30 min decreases the LPS- or LTA-induced IL-6 and TNF-α production 25530682
THP-1 Function Assay 5 µM 2 h significantly attenuates secretion of IL-1α induced by 27OHChol plus FSL-1  25598661
K562  Function Assay 0.25-1 μM 24 h suppresses resveratrol-induced H2AX phosphorylation 25619392
BxPC-3 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
PANC-1 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
K562 Function Assay 10 μM 1 h inhibits quinacrine-induced p38 MAPK phosphorylation 25684043
HPAEpiCs Function Assay 1/3/10 μM 1 h inhibits S1P time-dependently stimulated c-Jun phosphorylation 25734900
HPAEpiCs Function Assay 1/3/10 μM 1 h inhibits S1P-stimulated Akt phosphorylation   25734900
HPAEpiCs  Function Assay 1/3/10 μM 1 h reduces S1P-induced ICAM-1 protein and mRNA expression and promoter activity 25734900
HaCaT  Function Assay 5 µM 24 h inhibits IFN-α-induced CCL22 production levels 25834353
HaCaT  Function Assay 5 µM 24 h inhibits IFN-γ-induced CCL22 production levels 25834353
SCC25 Function Assay 20 μM 24 h increases autophagy level 25834400
MH7A  Apoptosis Assay 25 μM 24 h reverses cell cycle arrest induced by XAN and caused apoptosis of cells via activation of JNK 25862966
SK-OV-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
OVCAR-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
HEY Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
AsPC-1 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
BxPC-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
MIA PaCa-2 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
MIA PaCa-2 Function Assay 20 μM 24 h enhances cleavage of PARP when combined with glucose analogs 25888489
AsPC-1 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
BxPC-3 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
MIA PaCa-2 Function Assay 20 μM 24 h results in a modest inhibition of HIF-1α protein accumulation 25888489
MIA PaCa-2 Function Assay 20 μM 24 h reduced lactate accumulation in combination with both 2-DG and D-allose  25888489
HTSMCs Function Assay 0.1/1/10 μM 1 h inhibited CORM-2-induced HO-1 protein levels and mRNA expression 25921464
MG63 Apoptosis Assay 10/20/30 μM 24 h significantly decreased the apoptosis rate of MG63 induced by CdCl2 25998312
MG63 Function Assay 10/20/30 μM 24 h significantly decreases the level of phosphorylated p38 induced by CdCl2 in a concentration -dependent manner 25998312
rBMSCs Function Assay 10 μM 2.5 h depresses the phosphorylation of ERK and p38 26053266
MDA-MB-231 Function Assay 2 μM 24 h lessenes CCL2 induction by TNFα 26100848
HCT-116 Function Assay 25 μM 30 min attenuates the mRNA and protein expression of hBD-2 in responsive to DA 26223251
DCs Function Assay 20 μM 1 h decreases IL-12 production 24434636
HUVEC  Function Assay 20 μm  5 h reduces cytokine expression levels in a concentration-dependent manner 24189062
A 549 Function Assay 50 μM 1 h decreases the level of IL-8  24179688
H520  Function Assay 5/10 μM 1 h decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H1703  Function Assay 5/10 μM 1 h decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H520  Function Assay 10 µM 12 h decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells 24138903
H1703  Function Assay 10 µM 12 h decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells 24138903
MCF-7  Growth Inhibition Assay 10 μM 24 h inhibits the CR108-induced cell death 24128853
HPAEpiCs Function Assay 0.1/1/10 μM 1 h inhibits TNF-α-induced cPLA2 protein and mRNA expression 24069158
podocytes Function Assay 10 μM 1 h inhibits TGFβ1-induced activation of p38MAPK and Erk1/2  24036212
MCF-7 Function Assay 10 μM 1 h reduces the WA-induced phosphorylated p38 MAPK 24019090
MCF-7 Function Assay 10 μM 24 h increases the WA-induced apoptosis 24019090
HAPI Function Assay 10/20/40 μM 1 h inhibits TCDD-induced p38/JNK MAPK phosphorylation 23969120
HAPI Function Assay 20 μM  1 h attenuates TCDD-induced activation of iNOS and production 23969120
HepG2 Function Assay 350 nM 24 h inhibits the deguelin-induced activation of p38MAPK 23933198
AGS  Function Assay 10 μM 30 min inhibits caspase-3 activation and inhibition of ERK 23850994
HepG2 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
BEL7404 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
HL7702 Growth Inhibition Assay 0-50 μM 48 h inhibits the proliferation in a dose dependent manner 23807508
HepG2 Function Assay 0-50 μM 24 h inhibits the phosphorylation of p38 downstream proteins MAPKAPK2, ATF2, MSK1 and HSP27 in a dose-dependent manner 23807508
BEAS-2B Growth Inhibition Assay 10 μM 30 min reverses the decrease of cell viability induced by HCI 23784034
BEAS-2B Cytotoxity Assay 10 μM 30 min inhibited the increase in LDH and IL-8 expression 23784034
BEAS-2B Function Assay 10 μM 30 min decreases the levels of caspase-3, Bad and fas 23784034
H9c2  Function Assay 0.01/0.1/1 μM 1 h attenuates TNF-α-induced MMP-9 expression, mRNA levels, and promoter activity 23774252
H9c2  Function Assay 1 μM 1 h reduces TNF-α directly stimulated p38 MAPK phosphorylation 23774252
U937 Function Assay 10 μM  1 h abrogates the caffeine effect on MKP-1 and PP2Acα mRNA transcriptional levels 23707387
U937 Function Assay 10 μM  1 h abrogates caffeine-induced MKP-1 down-regulation and PP2Acα up-regulation 23707387
U937 Function Assay 10 μM  1 h suppresses c-Jun and CREB phosphorylation in caffeine-treated cells  23707387
A549 Function Assay 0.3/3/30 μM 1 h significantly attenuates ATPγS-mediated COX-2 protein and mRNA expression and promoter activity  23680674
A549 Function Assay 10 μM  0-30 min inhibits ATPγS induced p42/p44 MAPK and p38 MAPK phosphorylation 23680674
A549 Function Assay 10 μM  1 h inhibits ATPγS induced NF-κB p65 subunit phosphorylation and NF-κB promoter activity 23680674
A549 Function Assay 10 μM  1 h reduces ATPγS-stimulated cPLA2 phosphorylation  23680674
A549 Function Assay 10 μM  1 h reduces ATPγS-enhanced enzymatic activity of cPLA2  23680674
PC12 Function Assay 10/20/40 μM 1 h inhibits JNK and p38 23584357
HK-2 Apoptosis Assay 20 μM 24 h inhibits ERK and p38MAPK 23543151
H9c2 Function Assay 1 μM 1 h reduces TNF-α-induced MMP-9 mRNA levels and promoter activity 23353699
H9c2 Function Assay 1 μM 1 h reduces TNF-α-enhanced AP-1 promoter activity 23353699
H1650  Function Assay 10 μM  1 h decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1703 Function Assay 10 μM  1 h decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1650  Growth Inhibition Assay 10 μM  1 h enhances paclitaxel-induced cytotoxicity 23228696
H1703 Growth Inhibition Assay 10 μM  1 h enhances paclitaxel-induced cytotoxicity 23228696
MDDCs Growth Inhibition Assay 72 h IC502.7μM 24815087
THP-1 Growth Inhibition Assay 72 h IC50=4.7μM 24815087
MH7A  Growth Inhibition Assay 24 h reinforces the inhibitory effects of XAN 25862966
RAW264.7 Antiinflammatory assay 10 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 10 mins prior to LPS-challenge measured after 18 hrs by Griess method, IC50 = 16 μM. 22831798
BL21(DE3) Function assay 60 mins Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as substrate after 60 mins by AlphaScreen assay, IC50 = 3.4 μM. 28195723
medulloblastoma cells Antiproliferative assay Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay, EC50 = 3.006 μM. 17417631
neural precursor cells Antiproliferative assay Antiproliferative activity against mouse neural precursor cells by MTT assay, EC50 = 8.063 μM. 17417631
RAW264.7 Function assay Protection against Bacillus anthracis protective antigen and lethal toxin-diphtheria toxin chimeric protein mediated cytotoxicity in mouse RAW264.7 cells assessed as cell viability 17485504
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 SB202190是一种有效的p38 MAPK抑制剂，靶向作用于p38α/β，无细胞试验中IC50为50 nM/100 nM，有时用于代替SB 203580研究其在体内对SAPK2a/p38的潜在作用。SB202190 可通过诱导自噬和血红素氧化酶1来抑制内皮细胞的凋亡。SB202190可显著抑制Erastin依赖的铁死亡ferroptosis。
特性 SB 202190 与SB 203580极为相似。
靶点
Ferroptosis [11] p38α [1]
(Cell-free assay)		 p38β [1]
(Cell-free assay)
50 nM 100 nM
体外研究(In Vitro)
体外研究活性

SB 202190显著抑制内源本底和和抗Fas抗体诱导的MAPKAPK 2活性，且抑制效果呈剂量依赖性。SB 202190本身就足以诱导Jurkat细胞和Hela细胞的死亡：通过激活CPP 32样半胱氨酸蛋白酶，可阻断Bcl - 2的表达。p38β可减轻而p38α可加剧由SB 202190诱导的细胞凋亡[2]。在HaCaT细胞中SB 202190强烈抑制由紫外线诱导的cox - 2蛋白表达和 mRNA水平[3]。用SB 202190处理肾小管上皮细胞（正常大鼠k肝脏-52E），可将由白蛋白引发的炎症（单核细胞趋化蛋白-1，MCP - 1）或肿瘤生长因子β-1（TGFβ-1）引发的原纤维化（原骨胶原I a1，procollagen-i alpha1）相关基因降低50%[4]。SB 202190处理A549细胞，可诱导JNK磷酸化（该磷酸化效应呈时间和剂量依赖性）、转录因子ATF - 2磷酸化，并增加AP – 1与DNA的结合[6]。SB 202190处理促进THP-1和MV4-11细胞的生长。SB 202190可提高c-Raf 和ERK（细胞外信号调节激酶）磷酸化，暗示由SB 202190诱导的白血病细胞增殖过程有Ras-Raf-MEK-mitogen激活的MAPK通路的参与[7]。
激酶实验 体外酶活检测
p38α 和 p38β 溶解在25mM的Tris - HCl缓冲液中，PH 7.5，含0.1mM EGTA，髓鞘碱性蛋白（0.33毫克/毫升）作为底物。人工操作条件用50μL [γ-33P]ATP于30 °C孵育10分钟；Biomek 2000自动化工作站用25μL [γ-33P]ATP在96孔板室温孵育40分钟。ATP和乙酸镁浓度分别为0.1mM和10mM。所有检测都用MgATP起始。人工检测将孵育液滴到磷酸纤维素纸上，浸泡在50mM磷酸中。用5μL磷酸终止反应，后将孵育液点滴在P30过滤垫上。滤膜在50mM磷酸中漂洗四次以去除ATP，在用丙酮（人工孵育）或甲醇（工作站孵育）处理后，干燥并用放射性计量。
细胞实验 细胞系 Jurkat, 和 HeLa细胞
浓度 溶解于DMSO, 终浓度~50 μM
孵育时间 24 小时
方法

细胞血清饥饿后，用不同浓度SB 202190处理24小时。用台盼蓝或PI染色后经流式细胞仪分析，以检测细胞活力。凋亡细胞核用H33258染色。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot pJNK1 / pJNK2 / JNK1 / JNK2 mTOR / p-S6K / S6K / p-S6 / p-AKT / p-MK2 18222647
Immunofluorescence p-p38 / MMP9 24479681
Growth inhibition assay Cell viability 26844273
体内研究(In Vivo)
体内研究活性

SB 202190通过抑制p38减弱了由人脊髓灰质炎IgG（PV-IgG）在被动转移小鼠模型中诱发的水泡形成[5]。在脓毒症内毒素模型中，与对照组相比，经SB 202190处理可显著提高存活率[8]。
动物实验 Animal Models C57BL/6J 小鼠皮内注射无菌的对照IgG或人脊髓灰质炎IgG做对比。
Dosages 12.5 μg
Administration 皮内注射

化学信息&溶解度

分子量 331.34 分子式

C20H14N3OF
CAS号 152121-30-7 SDF Download SB202190 SDF
Smiles C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 66 mg/mL ( (199.19 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 22 mg/mL (66.39 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

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

摩尔浓度计算器

质量 浓度 体积 分子量

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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