SB202190 (FHPI)
SB202190 (FHPI; CAS 152121-30-7) is a selective MAPK inhibitor targeting specifically the p38 isoforms α and β, with reported IC50 values of approximately 50 nM and 100 nM, respectively. Through inhibition of p38 signaling, SB202190 has been observed to stimulate the proliferation of leukemia cell lines, including THP-1 and MV4-11, via activation of ERK and C-Raf phosphorylation pathways. Additionally, SB202190 modulates cellular responses to genotoxic stress, such as hydroxyurea-induced premature chromosome condensation, and influences histone acetylation status (Lys5 of histone H4) in plant systems. Such activities render SB202190 useful for investigating MAP kinase-dependent pathways in cell proliferation and stress responses.
References:
[1] Davies SP1, Reddy H, Caivano M, Cohen P. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1; 351 (Pt 1): 95-105.
[2] Hirosawa M1, Nakahara M, Otosaka R, Imoto A, Okazaki T, Takahashi S. The p38 pathway inhibitor SB202190 activates MEK/MAPK to stimulate the growth of leukemia cells. Leuk Res. 2009 May; 33 (5): 693-9.
[3] Winnicki K1, Maszewski J. SB202190 affects cell response to hydroxyurea-induced genotoxic stress in root meristems of Vicia faba. Plant Physiol Biochem. 2012 Nov; 60: 129-36.
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- 9. XiaoLi Jin, Jia Xu, et al. "Oridonin Attenuates Thioacetamide-Induced Osteoclastogenesis Through MAPK/NF-κB Pathway and Thioacetamide-Inhibited Osteoblastogenesis Through BMP-2/RUNX2 Pathway." Calcif Tissue Int. 2023 Jun;112(6):704-715. PMID: 37032340
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| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 331.34 |
| Cas No. | 152121-30-7 |
| Formula | C20H14N3OF |
| 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 | OC1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1 |
| 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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