SB202190 (FHPI)
SB 202190 (CAS 152121-30-7) is a cell-permeable pyridinyl imidazole compound, functioning as a selective inhibitor of p38α and p38β2 mitogen-activated protein kinases (MAPKs) and exhibiting inhibitory activity against these enzymes in signal transduction pathways. Additionally, it binds to the ATP pocket of recombinant human active p38 kinase, interfering with downstream cellular signaling.
In in vitro biochemical assays, SB 202190 effectively blocks the phosphorylation of substrate proteins with an IC50 value of 50 nM for p38α and 100 nM for p38β2, tested against recombinant human kinases. It can also bind to the ATP-binding domain of p38 MAPK with a Kd value of 38 nM. SB 202190 has been observed to inhibit the activation of p38-dependent transcription factors and reduce the expression of pro-inflammatory cytokines in cultured cells. Furthermore, in cellular contexts, SB 202190 modulates cellular proliferation, promotes apoptosis in certain cancer cell lines, and affects memory-associated signaling pathways.
In research and preclinical application, SB 202190 is widely used for studies of MAPK signaling, investigation of inflammatory processes, and exploration of cancer therapeutics. It serves as a valuable tool for elucidating the role of p38 MAPK in cellular responses and disease models.
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 331.34 |
| Cas No. | 152121-30-7 |
| Formula | C20H14N3OF |
| Synonyms | SB 202190 |
| Solubility | insoluble in H2O; ≥22.47 mg/mL in EtOH; ≥57.7 mg/mL in DMSO |
| Chemical Name | 4-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)phenol |
| SDF | Download SDF |
| Canonical SMILES | Oc(cc1)ccc1-c1nc(-c(cc2)ccc2F)c(-c2ccncc2)[nH]1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment[1]: | |
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Cell lines |
THP-1 and MV4-11 leukemia cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37°C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
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Reacting condition |
72 h, 5 μM |
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Applications |
SB202190 is a specific inhibitor of p38ɑ and p38β through competition with ATP for the same binding site on p38. SB202190 potently activated the growth of THP-1 and MV4-11 cells. Furthermore, SB202190 increased the phosphorylation of C-Raf and ERK, suggesting that Raf–MEK–MAPK pathway activation is involved in the cell growth induced by SB202190. |
| Animal experiment [2]: | |
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Animal models |
Three-month specific pathogen-free (SPF) male Wistar rats |
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Dosage form |
5 μL of 10 μmol/L SB202190, ICV injection |
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Application |
One week after SB202190 treatment, p38 MAPK phosphorylation in hippocampus was higher in the model group than in the SB202190 group. Compared to the model group, the SB202190 group exhibited significantly shorter escape latencies in the Morris water maze hidden platform trials. The SB202190 group also showed higher Bcl-2 expression, lower caspase-3 expression and significantly decreased neuronal apoptosis in hippocampus. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Hirosawa M, Nakahara M, Otosaka R, et al. The p38 pathway inhibitor SB202190 activates MEK/MAPK to stimulate the growth of leukemia cells [J]. Leukemia research, 2009, 33 (5): 693-699. [2] Yang S, Zhou G, Liu H, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia [J]. BioMed research international, 2013, 2013: 215798. |
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| Description | SB202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinases with IC50 values of 50 nM and 100 nM for p38α and p38β, respectively. | |||||
| Targets | p38α MAPK | p38β MAPK | ||||
| IC50 | 50 nM | 100 nM | ||||
Quality Control & MSDS
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