Home MAPK p38 MAPK inhibitor SB202190

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SB202190 p38 MAPK inhibitor

Cat. No.: S1077

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. This compound inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. It significantly suppresses Erastin‐dependent ferroptosis.
SB202190 p38 MAPK inhibitor Chemical Structure

Estructura química

Peso molecular: 331.34

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.99%
99.99

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
HCT-116 Function Assay 25 μM 30 min DMSO  attenuates the mRNA and protein expression of hBD-2 in responsive to DA 26223251
MDA-MB-231 Function Assay 2 μM 24 h lessenes CCL2 induction by TNFα 26100848
rBMSCs Function Assay 10 μM 2.5 h depresses the phosphorylation of ERK and p38 26053266
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
MG63 Apoptosis Assay 10/20/30 μM 24 h significantly decreased the apoptosis rate of MG63 induced by CdCl2 25998312
HTSMCs Function Assay 0.1/1/10 μM 1 h inhibited CORM-2-induced HO-1 protein levels and mRNA expression 25921464
MIA PaCa-2 Function Assay 20 μM 24 h reduced lactate accumulation in combination with both 2-DG and D-allose  25888489
MIA PaCa-2 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
AsPC-1 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 enhances cleavage of PARP when combined with glucose analogs 25888489
MIA PaCa-2 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
AsPC-1 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
OVCAR-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
SK-OV-3 Growth Inhibition Assay 20 μM 2 h sensitizes cell lines to treatment with 2-DG and D-allose 25888489
MH7A  Growth Inhibition Assay 24 h reinforces the inhibitory effects of XAN 25862966
MH7A  Apoptosis Assay 25 μM 24 h reverses cell cycle arrest induced by XAN and caused apoptosis of cells via activation of JNK 25862966
SCC25 Function Assay 20 μM 24 h increases autophagy level 25834400
HaCaT  Function Assay 5 µM 24 h inhibits IFN-γ-induced CCL22 production levels 25834353
HaCaT  Function Assay 5 µM 24 h inhibits IFN-α-induced CCL22 production levels 25834353
HPAEpiCs  Function Assay 1/3/10 μM 1 h reduces S1P-induced ICAM-1 protein and mRNA expression and promoter activity 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 inhibits S1P time-dependently stimulated c-Jun phosphorylation 25734900
K562 Function Assay 10 μM 1 h DMSO inhibits quinacrine-induced p38 MAPK phosphorylation 25684043
PANC-1 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
BxPC-3 Function Assay 10 μM 1 h enhances the autophagic effect  25632222
K562  Function Assay 0.25-1 μM 24 h suppresses resveratrol-induced H2AX phosphorylation 25619392
THP-1 Function Assay 5 µM 2 h significantly attenuates secretion of IL-1α induced by 27OHChol plus FSL-1  25598661
WB Function Assay 20 μM  30 min decreases the LPS- or LTA-induced IL-6 and TNF-α production 25530682
RAW 264.7 Function Assay 10 μM 30 min induces characteristic vacuolation of OCs  25461399
RAW 264.7 Function Assay 10 μM 30 min attenuates the effects of OPG on osteoclast retraction 25461399
HaCaT  Function Assay 40 μM 3-24 h DMSO reduces the accumulation of ZO-1 25435485
H9c2 Function Assay 50 μM  12 h reduces LDH release and MMP loss 25245818
HSCs Apoptosis Assay 25 μM 24 h significantly attenuates TG-induced activated HSCs apoptosis 24961950
THP-1 Growth Inhibition Assay 72 h DMSO IC50=4.7μM 24815087
MDDCs Growth Inhibition Assay 72 h DMSO IC502.7μM 24815087
MDDCs Function Assay 0-15 μM 48 h DMSO suppresses IFN-α and IP-10 production  24815087
MDDCs Function Assay 0-15 μM 48 h DMSO inhibits MIP-1a, MIP-1b and RANTES production 24815087
MDDCs Function Assay 10 μM 3.5 h DMSO blocks EBOV GP, but not VSV G mediated entry into human MDDCs 24815087
macrophages Function Assay 1 μM 4.5 h completely inhibits MT-III-induced activation of NF-κB 24808633
PDL  Function Assay 20 μM  30 min DMSO significantly inhibits the tensile force-mediated BMP-2 expression 24561081
AGS Function Assay 5 μM 30 min suppresses 1-induced caspase-8 and caspase-3 activation 24547878
H520 Function Assay 10 µM 1 h DMSO decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
H1703 Function Assay 10 µM 1 h DMSO decreases the pemetrexed-induced MSH2 mRNA and protein levels 24530475
H520 Function Assay 10 µM 12 h DMSO inhibits pemetrexed-elicited MSH2 protein stability 24530475
H1703 Function Assay 10 µM 12 h DMSO inhibits pemetrexed-elicited MSH2 protein stability 24530475
H520 Function Assay 10 µM 6 h DMSO significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
H1703 Function Assay 10 µM 6 h DMSO significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line 24530475
MC3T3-E1 Function Assay 0.3/3/30 μM 1 h attenuates TNF-α-induced MMP-9 expression in a concentration-dependent manner  24502696
MC3T3-E1 Function Assay 30 μM 1 h attenuates TNF-α-stimulated p38 MAPK phosphorylation 24502696
HUVECs  Function Assay 10 µM 1 h inhibits TNF-α-induced CXCL1 production 24487964
AGS  Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 24479681
MKN-45 Function Assay 10 µM 30 min inhibits IL-1β-induced activation of p38 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 attenuates IL-1β-induced GA cell migration and invasion 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 significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression 24479681
DCs Function Assay 20 μM 1 h decreases IL-12 production 24434636
HUVEC  Function Assay 20 μm  5 h DMSO 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 DMSO decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H1703  Function Assay 5/10 μM 1 h DMSO decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell 24138903
H520  Function Assay 10 µM 12 h DMSO decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells 24138903
H1703  Function Assay 10 µM 12 h DMSO 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 DMSO reduces the WA-induced phosphorylated p38 MAPK 24019090
MCF-7 Function Assay 10 μM 24 h DMSO 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 DMSO 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 DMSO decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1703 Function Assay 10 μM  1 h DMSO decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells 23228696
H1650  Growth Inhibition Assay 10 μM  1 h DMSO enhances paclitaxel-induced cytotoxicity 23228696
H1703 Growth Inhibition Assay 10 μM  1 h DMSO enhances paclitaxel-induced cytotoxicity 23228696
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 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
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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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 331.34 Fórmula

C20H14N3OF

 Almacenamiento (Desde la fecha de recepción)
Nº CAS 152121-30-7 Descargar SDF Almacenamiento de soluciones madre

Sinónimos FHPI Smiles C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 66 mg/mL (199.19 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 22 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa Concentración Volumen Peso molecular
Calculadora de Dilución Calculadora de Peso Molecular

In vivo
Lote:

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

mg/kg g μL

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH2O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC50/Ki
Ferroptosis
p38α
(Cell-free assay)
50 nM
p38β
(Cell-free assay)
100 nM
In vitro

SB 202190 significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner. This compound 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. Its apoptosis is attenuated by p38β but augmented by p38α. The chemical strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA. Treatment with this inhibitor 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). It 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. This agent enhances the growth of THP-1 and MV4-11 cells. It 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 this compound.

Ensayo de quinasa
Ensayos de quinasas in vitro
Las p38α y p38β se ensayan en 25 mM Tris-HCl, pH 7.5, que contiene 0.1 mM EGTA, con proteína básica de mielina (0.33 mg/mL) como sustrato. Los ensayos se realizan manualmente durante 10 minutos a 30 °C en incubaciones de 50 μL usando [γ-33P]ATP, o con una estación de trabajo de automatización de laboratorio Biomek 2000 en un formato de 96 pocillos durante 40 minutos a temperatura ambiente en incubaciones de 25 μL usando [γ-33P]ATP. Las concentraciones de ATP y acetato de magnesio son 0.1 mM y 10 mM respectivamente. Todos los ensayos se inician con MgATP. Los ensayos manuales se terminan colocando alícuotas de incubación sobre papel de fosfocelulosa, seguido de inmersión en 50 mM de ácido fosfórico. Los ensayos robóticos se terminan mediante la adición de 5 μL de ácido fosfórico 0.5 M antes de colocar las alícuotas sobre esteras de filtro P30. Todos los papeles se lavan luego cuatro veces en 50 mM de ácido fosfórico para eliminar el ATP, una vez en acetona (incubaciones manuales) o metanol (incubaciones robóticas), y luego se secan y se cuentan para la radioactividad.
In vivo

Inhibiting p38 by administration of SB 202190 inhibits PV IgG-induced blister formation in the passive transfer mouse model. In the endotoxin model of sepsis, treatment with this compound produces a statistically significant survival benefit compared with control.

Referencias
  • [4] https://pubmed.ncbi.nlm.nih.gov/16807361/
  • [5] https://pubmed.ncbi.nlm.nih.gov/16908851/
  • [6] https://pubmed.ncbi.nlm.nih.gov/18222647/
  • [7] https://pubmed.ncbi.nlm.nih.gov/18995898/
  • [8] https://pubmed.ncbi.nlm.nih.gov/19027920/
  • [9] https://pubmed.ncbi.nlm.nih.gov/21159664/
  • [10] https://pubmed.ncbi.nlm.nih.gov/22053010/
  • [11] https://pubmed.ncbi.nlm.nih.gov/22053010/

Aplicaciones (Applications)

Métodos Biomarcadores Imágenes PMID
Western blot pJNK1 / pJNK2 / JNK1 / JNK2 mTOR / p-S6K / S6K / p-S6 / p-AKT / p-MK2
S1077-WB2
18222647
Immunofluorescence p-p38 / MMP9
S1077-IF1
24479681
Growth inhibition assay Cell viability
S1077-viability1
26844273