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Cat.No.S1077
| Related Targets | ERK K-Ras Raf JNK MEK Ras S6 Kinase MAP4K TAK1 Mixed Lineage Kinase |
|---|---|
| Other p38 MAPK Products | SB203580 (Adezmapimod) PH-797804 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate VX-702 Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | 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 | |||
| Click to View More Cell Line Experimental Data | ||||||
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In vitro |
DMSO
: 66 mg/mL
(199.19 mM)
Ethanol : 22 mg/mL Water : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 331.34 | Formula | C20H14N3OF |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 152121-30-7 | Download SDF | Storage of Stock Solutions |
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| Synonyms | FHPI | Smiles | C1=CC(=CC=C1C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F)O | ||
| 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. |
| 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.
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| 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. |
References |
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| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Western blot | mTOR / p-S6K / S6K / p-S6 / p-AKT / p-MK2 pJNK1 / pJNK2 / JNK1 / JNK2 |
|
26844273 |
| Immunofluorescence | p-p38 / MMP9 |
|
24479681 |
| Growth inhibition assay | Cell viability |
|
26844273 |
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