SB202190

製品コードS1077 バッチS107706

印刷

化学情報

Chemical Structure Synonyms FHPI Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H14N3OF
分子量 331.34 CAS No. 152121-30-7
Solubility (25°C)* 体外 DMSO 66 mg/mL (199.19 mM)
Ethanol 10 mg/mL (30.18 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
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.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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. [2] The chemical strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA. [3] 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). [4] 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. [6] 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. [7]
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, treatment with this compound produces a statistically significant survival benefit compared with control. [8]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 Jurkat, and HeLa
濃度 Dissolved in DMSO, final concentrations ~50 μM
反応時間 24 hours
実験の流れ

Cells are serum-starved and then treated with different concentration of SB 202190 for 24 hours. Cell viability is assayed by either trypan blue exclusion or propidium iodide exclusion followed by flow cytometry analysis. The apoptotic nuclei are visualized by H33258 staining.
動物実験 動物モデル C57BL/6J mice injected i.d. with a sterile solution of either control IgG or PV IgG
投薬量 12.5 μg
投与方法 Administered via i.d.

参考

  • https://pubmed.ncbi.nlm.nih.gov/10998351/
  • https://pubmed.ncbi.nlm.nih.gov/9632706/
  • https://pubmed.ncbi.nlm.nih.gov/11439356/
  • https://pubmed.ncbi.nlm.nih.gov/16807361/
  • https://pubmed.ncbi.nlm.nih.gov/16908851/
  • https://pubmed.ncbi.nlm.nih.gov/18222647/
  • https://pubmed.ncbi.nlm.nih.gov/18995898/
  • https://pubmed.ncbi.nlm.nih.gov/19027920/
  • https://pubmed.ncbi.nlm.nih.gov/21159664/
  • https://pubmed.ncbi.nlm.nih.gov/22053010/
  • https://pubmed.ncbi.nlm.nih.gov/28887319/

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Macropinocytosis maintains CAF subtype identity under metabolic stress in pancreatic cancer [ Cancer Cell, 2025, S1535-6108(25)00271-5] PubMed: 40712568
First-in-class ultralong-target-residence-time p38α inhibitors as a mitosis-targeted therapy for colorectal cancer [ Nat Cancer, 2025, 6(2):259-277] PubMed: 39820127
Fructose and glucose from sugary drinks enhance colorectal cancer metastasis via SORD [ Nat Metab, 2025, 7(10):2018-2032] PubMed: 40973819
Dual membrane receptor degradation via folate receptor targeting chimera [ Nat Commun, 2025, 16(1):8804] PubMed: 41038820
Multi-layer stratified oncology platform utilizing transcriptomics, prostate cancer organoids, and modeling of drug response [ J Exp Clin Cancer Res, 2025, 44(1):290] PubMed: 41094672
Aurantio-obtusin modulates Wilms Tumour 1 within the breast tumour microenvironment reducing immunosuppression and tumour growth [ Cell Commun Signal, 2025, 23(1):309] PubMed: 40598415
Comparison of characteristics and immune responses between paired human nasal and bronchial epithelial organoids [ Cell Biosci, 2025, 15(1):18] PubMed: 39920853
ERK1-mediated GLYCTK2 phosphorylation promotes fructolysis to sustain glioblastoma survival under glucose deprivation [ Cell Death Discov, 2025, 11(1):266] PubMed: 40467571
Single Low-Dose Ionizing Radiation Transiently Enhances Rat RIN-m5F Cell Function via the ROS/p38 MAPK Pathway Without Inducing Cell Damage [ Antioxidants (Basel), 2025, 14(2)120] PubMed: 40002307
Establishing Pancreatic Cancer Organoids from EUS-Guided Fine-Needle Biopsy Specimens [ Cancers (Basel), 2025, 17(4)692] PubMed: 40002285

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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