ホームページ MAPK p38 MAPK inhibitor - Autophagy activator - Apoptosis related inhibitor - Ferroptosis inhibitor SB202190 For research use only.

SB202190

別名：FHPI

SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.

SB202190化学構造

CAS No. 152121-30-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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SB202190関連製品

シグナル伝達経路

p38 MAPK Signaling Pathways

p38 MAPKシグナル伝達経路

p38 MAPK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 SB202190 is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.
Targets
Ferroptosis [11] p38α [1]
(Cell-free assay)		 p38β [1]
(Cell-free assay)
50 nM 100 nM
In Vitro
In vitro

SB 202190 significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner. SB202190 by itself is sufficient to induce cell death in Jurkat and HeLa cells through activation of CPP32-like caspases, which can be blocked by expression of bcl-2. SB202190-induced apoptosis is attenuated by p38β but augmented by p38α. [2] SB 202190 strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA. [3] SB 202190 treatment inhibits the expression of albumin-induced proinflammatory (monocyte chemoattractant protein-1) and transforming growth factor (TGF)-beta1-induced profibrotic (procollagen-Ialpha1) genes over 50% in renal tubular cells (normal rat kidney-52E). [4] SB 202190 treatment induces phosphorylation of JNK in a dose- and time- dependent manner in A549 cells, induces phosphorylation of ATF-2 transcription factor, and increases AP-1 DNA binding. [6] SB 202190 treatment enhances the growth of THP-1 and MV4-11 cells. SB 202190 increases the phosphorylation of c-Raf and ERK, suggesting that Ras-Raf-MEK-mitogen-activated protein kinase (MAPK) pathway activation is involved in the leukemia cell growth induced by SB 202190. [7]
Kinase Assay In vitro kinase assays
The p38α and p38β are assayed in 25 mM Tris-HCl, pH 7.5, containing 0.1 mM EGTA, with myelin basic protein (0.33 mg/mL) as substrate. Assays are performed either manually for 10 minutes at 30 °C in 50 μL incubations using [γ-33P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at ambient temperature in 25 μL incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate are 0.1 mM and 10 mM respectively. All assays are initiated with MgATP. Manual assays are terminated by spotting aliquots of incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays are terminated by the addition of 5 μL of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers are then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity.
細胞実験 細胞株 Jurkat, and HeLa
濃度 Dissolved in DMSO, final concentrations ~50 μM
反応時間 24 hours
実験の流れ

Cells are serum-starved and then treated with different concentration of SB 202190 for 24 hours. Cell viability is assayed by either trypan blue exclusion or propidium iodide exclusion followed by flow cytometry analysis. The apoptotic nuclei are visualized by H33258 staining.
実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo

Inhibiting p38 by administration of SB 202190 inhibits PV IgG-induced blister formation in the passive transfer mouse model. [5] In the endotoxin model of sepsis, SB 202190 treatment produces a statistically significant survival benefit compared with control. [8]
動物実験 動物モデル C57BL/6J mice injected i.d. with a sterile solution of either control IgG or PV IgG
投与量 12.5 μg
投与経路 Administered via i.d.

化学情報

分子量 331.34 化学式

C20H14N3OF
CAS No. 152121-30-7 SDF Download SB202190 SDFをダウンロードする
Smiles C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O
保管

In vitro
Batch:

DMSO : 66 mg/mL ( (199.19 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 22 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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