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Formula | C20H14N3OF |
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Molecular Weight | 331.34 | CAS No. | 152121-30-7 | |
Solubility (25°C)* | In vitro | DMSO | 66 mg/mL (199.19 mM) | |
Ethanol | 12 mg/mL (36.21 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | ||||||
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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] |
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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. [5] In the endotoxin model of sepsis, SB 202190 treatment produces a statistically significant survival benefit compared with control. [8] |
Kinase Assay: |
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Data from [J Biol Chem, 2010, 285, 32824–32833]
Data from [J Biol Chem, 2010, 285, 32824–32833]
Data from [J Biol Chem, 2010, 285, 32824–32833]
Targeting EMSY-mediated methionine metabolism is a potential therapeutic strategy for triple-negative breast cancer [ Cell Rep Med, 2024, 5(2):101396] | PubMed: 38290515 |
The DNA-dependent protein kinase catalytic subunit exacerbates endotoxemia-induced myocardial microvascular injury by disrupting the MOTS-c/JNK pathway and inducing profilin-mediated lamellipodia degradation [ Theranostics, 2024, 14(4):1561-1582] | PubMed: 38389837 |
LRPPRC promotes glycolysis by stabilising LDHA mRNA and its knockdown plus glutamine inhibitor induces synthetic lethality via m6 A modification in triple-negative breast cancer [ Clin Transl Med, 2024, 14(2):e1583] | PubMed: 38372449 |
Cancer-associated DNA Hypermethylation of Polycomb Targets Requires DNMT3A Dual Recognition of Histone H2AK119 Ubiquitination and the Nucleosome Acidic Patch [ bioRxiv, 2024, 2024.03.18.585588] | PubMed: 38562823 |
Dynamic interplay between IL-1 and WNT pathways in regulating dermal adipocyte lineage cells during skin development and wound regeneration [ Cell Rep, 2023, 42(6):112647] | PubMed: 37330908 |
Feedback activation of EGFR/wild-type RAS signaling axis limits KRASG12D inhibitor efficacy in KRASG12D-mutated colorectal cancer [ Oncogene, 2023, 10.1038/s41388-023-02676-9 10.3322/caac.21660 10.1001/jama.2021.6021 10.1038/nrdp.2015.65 10.1038/s41575-019-0189-8 10.1038/nature11252 10.1038/s41392] | PubMed: 37020035 |
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.07.012] | PubMed: 37562653 |
Hypoxia Primes Human ISCs for Interleukin-Dependent Rescue of Stem Cell Activity [ Cell Mol Gastroenterol Hepatol, 2023, 16(5):823-846] | PubMed: 37562653 |
SB202190 Predicts BRAF-Activating Mutations in Primary Colorectal Cancer Organoids via Erk1-2 Modulation [ Cells, 2023, 12(4)664] | PubMed: 36831331 |
Phosphorylation-Assisted Luciferase Complementation Assay Designed to Monitor Kinase Activity and Kinase-Domain-Mediated Protein-Protein Binding [ Int J Mol Sci, 2023, 24(19)14854] | PubMed: 37834301 |
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