nur für Forschungszwecke
Kat.-Nr.S1077
| Verwandte Ziele | ERK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Weitere p38 MAPK Inhibitoren | SB203580 (Adezmapimod) PH-797804 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate VX-702 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | 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 | |||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 331.34 | Formel | C20H14N3OF |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 152121-30-7 | SDF herunterladen | Lagerung von Stammlösungen |
|
|
| Synonyme | FHPI | Smiles | C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O | ||
|
In vitro |
DMSO
: 66 mg/mL
(199.19 mM)
Ethanol : 22 mg/mL Water : Insoluble |
|
In vivo |
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Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
| Targets/IC50/Ki |
Ferroptosis
p38α
(Cell-free assay) 50 nM
p38β
(Cell-free assay) 100 nM
|
|---|---|
| In vitro |
SB 202190 hemmt sowohl die basale als auch die durch Anti-Fas-Antikörper induzierte MAPKAPK 2-Aktivität dosisabhängig. Diese Verbindung allein reicht aus, um den Zelltod in Jurkat- und HeLa-Zellen durch Aktivierung von CPP32-ähnlichen Caspasen zu induzieren, was durch die Expression von bcl-2 blockiert werden kann. Seine Apoptose wird durch p38β abgeschwächt, aber durch p38α verstärkt. Die Chemikalie hemmt stark die UVB-induzierte COX-2-Proteinexpression in HaCaT-Zellen und hemmt deutlich die UVB-induzierte cox-2-mRNA. Die Behandlung mit diesem Inhibitor hemmt die Expression von Albumin-induzierten proinflammatorischen (Monozyten-Chemoattraktionsprotein-1) und Transforming Growth Factor (TGF)-beta1-induzierten profibrotischen (Prokollagen-Ialpha1) Genen um über 50% in Nierentubuluszellen (normale Rattenniere-52E). Es induziert die Phosphorylierung von JNK dosis- und zeitabhängig in A549-Zellen, induziert die Phosphorylierung des ATF-2-Transkriptionsfaktors und erhöht die AP-1-DNA-Bindung. Dieses Mittel verbessert das Wachstum von THP-1- und MV4-11-Zellen. Es erhöht die Phosphorylierung von c-Raf und ERK, was darauf hindeutet, dass die Aktivierung des Ras-Raf-MEK-Mitogen-aktivierten Proteinkinase (MAPK)-Signalwegs am Leukämiezellwachstum beteiligt ist, das durch diese Verbindung induziert wird. |
| Kinase-Assay |
In-vitro-Kinase-Assays
|
|
Die p38α und p38β werden in 25 mM Tris-HCl, pH 7,5, das 0,1 mM EGTA enthält, mit Myelin-Basischem Protein (0,33 mg/mL) als Substrat getestet. Die Assays werden entweder manuell für 10 Minuten bei 30 °C in 50 μL Inkubationen unter Verwendung von [γ-33P]ATP durchgeführt, oder mit einer Biomek 2000 Laborautomatisierungs-Workstation in einem 96-Well-Format für 40 Minuten bei Umgebungstemperatur in 25 μL Inkubationen unter Verwendung von [γ-33P]ATP. Die Konzentrationen von ATP und Magnesiumacetat betragen jeweils 0,1 mM und 10 mM. Alle Assays werden mit MgATP initiiert. Manuelle Assays werden durch Auftragen von Inkubationsaliquots auf Phosphozellulosepapier und anschließendes Eintauchen in 50 mM Phosphorsäure beendet. Robotergestützte Assays werden durch Zugabe von 5 μL 0,5 M Phosphorsäure beendet, bevor Aliquots auf P30-Filtermatten aufgetragen werden. Alle Papiere werden dann viermal in 50 mM Phosphorsäure gewaschen, um ATP zu entfernen, einmal in Aceton (manuelle Inkubationen) oder Methanol (robotergestützte Inkubationen), und dann getrocknet und auf Radioaktivität gezählt.
|
|
| In vivo |
Die Hemmung von p38 durch die Verabreichung von SB 202190 hemmt die PV-IgG-induzierte Blasenbildung im passiven Transfer-Mausmodell. Im Endotoxinmodell der Sepsis führt die Behandlung mit dieser Verbindung zu einem statistisch signifikanten Überlebensvorteil im Vergleich zur Kontrolle. |
Literatur |
|
| Methoden | Biomarker | Bilder | 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 |
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