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SB202190 p38 MAPK remmer

Name: SB202190
Brand: Selleck Chemicals
SKU: S1077
Rating: 5 (215 reviews)

Cat.Nr.S1077

SB202190 is een krachtige p38 MAPK-remmer die zich richt op p38α/β met een IC50 van 50 nM/100 nM in celvrije assays, soms gebruikt in plaats van SB 203580 om mogelijke rollen van SAPK2a/p38 in vivo te onderzoeken. Deze verbinding remt endotheelcel Apoptosis via inductie van Autophagy en heemoxygenase-1. Het onderdrukt significant Erastin-afhankelijke Ferroptosis.

SB202190 p38 MAPK remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 331.34

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	ERK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Overige p38 MAPK Inhibitoren	SB203580 (Adezmapimod) PH-797804 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate VX-702 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	331.34	Formule	C₂₀H₁₄N₃OF	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	152121-30-7	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	FHPI			Smiles	C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O

Oplosbaarheid

In vitro
Batch:

DMSO : 66 mg/mL (199.19 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	8.000mg/ml (24.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	Ferroptosis p38α (Cell-free assay) 50 nM p38β (Cell-free assay) 100 nM
In vitro	SB202190 remt significant zowel de basale als de anti-Fas antilichaam-geïnduceerde MAPKAPK 2 activiteit op een dosisafhankelijke manier. Deze verbinding alleen is voldoende om celdood te induceren in Jurkat en HeLa cellen door activering van CPP32-achtige caspasen, wat geblokkeerd kan worden door expressie van bcl-2. De Apoptosis related wordt afgezwakt door p38β maar versterkt door p38α. De chemische stof remt sterk UVB-geïnduceerde COX-2 eiwitexpressie in HaCaT cellen, en remt aanzienlijk UVB-geïnduceerd cox-2 mRNA. Behandeling met deze remmer remt de expressie van albumine-geïnduceerde pro-inflammatoire (monocyt chemoattractant proteïne-1) en transforming growth factor (TGF)-beta1-geïnduceerde profibrotische (procollageen-Ialpha1) genen met meer dan 50% in renale tubulaire cellen (normale rattennier-52E). Het induceert fosforylering van JNK op een dosis- en tijdsafhankelijke manier in A549 cellen, induceert fosforylering van ATF-2 transcriptiefactor, en verhoogt AP-1 DNA-binding. Dit middel versterkt de groei van THP-1 en MV4-11 cellen. Het verhoogt de fosforylering van c-Raf en ERK, wat suggereert dat Ras-Raf-MEK-mitogen-activated protein kinase (MAPK) pathway activering betrokken is bij de leukemie celgroei geïnduceerd door deze verbinding.
Kinase Assay	In vitro kinase testen
Kinase Assay	De p38α en p38β worden geanalyseerd in 25 mM Tris-HCl, pH 7.5, met 0.1 mM EGTA, en myeline basisch proteïne (0.33 mg/mL) als substraat. De analyses worden handmatig uitgevoerd gedurende 10 minuten bij 30 °C in incubaties van 50 μL met [γ-³³P]ATP, of met een Biomek 2000 Laboratory Automation Workstation in een 96-well formaat gedurende 40 minuten bij kamertemperatuur in incubaties van 25 μL met [γ-³³P]ATP. De concentraties van ATP en magnesiumacetaat zijn respectievelijk 0.1 mM en 10 mM. Alle analyses worden gestart met MgATP. Handmatige analyses worden beëindigd door aliquots van de incubatie op fosfocellulosepapier te druppelen, gevolgd door onderdompeling in 50 mM fosforzuur. Robotanalyses worden beëindigd door de toevoeging van 5 μL 0.5 M fosforzuur voordat aliquots op P30-filtermatten worden gedruppeld. Alle papieren worden vervolgens vier keer gewassen in 50 mM fosforzuur om ATP te verwijderen, eenmaal in aceton (handmatige incubaties) of methanol (robotincubaties), en daarna gedroogd en geteld op radioactiviteit.
In vivo	Het remmen van p38 door toediening van SB202190 remt PV IgG-geïnduceerde blaarvorming in het passieve transfer muismodel. In het endotoxinemodel van sepsis leidt behandeling met deze verbinding tot een statistisch significant overlevingsvoordeel in vergelijking met de controle.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/10998351/ [2] https://pubmed.ncbi.nlm.nih.gov/9632706/ [3] https://pubmed.ncbi.nlm.nih.gov/11439356/ [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/

Toepassingen

Methoden	Biomarkers	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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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