SB202190 (FHPI)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SB202190（FHPI）是一种有效的MAPK抑制剂，可特异地抑制p38α和p38β，IC50值分别为50 nM和100 nM[1]。
SB202190可有效促进白血病细胞系THP-1和MV4-11的生长。SB202190可激活ERK和C-Raf的磷酸化作用。研究表明，SB202190存在时，U0126和FPT抑制剂II的ED50值显著降低[2]。
在植物中，SB202190可在HU处理和咖啡因诱导的PCC（早熟染色体凝集）中诱发细胞周期发生变化。此外，SB202190和咖啡因分别减少HU诱导的组蛋白H4 Lys5乙酰化[3]。
参考文献：
[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.
- 1. Jingchun Du, Yougui Xiang, et al. "RIPK1 dephosphorylation and kinase activation by PPP1R3G/PP1γ promote apoptosis and necroptosis." Nat Commun. 2021 Dec 3;12(1):7067. PMID: 34862394
- 2. Bas Ponsioen, Jasmin B Post, et al. "Quantifying single-cell ERK dynamics in colorectal cancer organoids reveals EGFR as an amplifier of oncogenic MAPK pathway signalling." Nat Cell Biol. 2021 Apr;23(4):377-390. PMID: 33795873
- 3. Tong Wang, Qi Sun, et al. "A1 Reactive Astrocytes Activated by 2-chloroethanol Modulate M1 Microglia Polarization through Upregulating IL-1β and TNF-α." Research Square. April 13th, 2021
- 4. Tong Wang, Qi Sun, et al. "A1 astrocytes activated by 2-Chloroethanol via the ROS-induced p38 MAPK/NF-κB and AP-1 pathways modulate microglia polarization." Research Square. April 12th, 2021.
- 5. Shuxian Wang, Qiwei Chen, et al. "Omega-3 polyunsaturated fatty acids alleviate hydrogen sulfide-induced blood-testis barrier disruption in the testes of adult mice." Reprod Toxicol. 2020 Oct 14;S0890-6238(20)30233-1. PMID: 33068716
- 6. Post JB, Hami N, et al. "CRISPR-induced RASGAP deficiencies in colorectal cancer organoids reveal that only loss of NF1 promotes resistance to EGFR inhibition." Oncotarget. 2019 Feb 15;10(14):1440-1457. PMID: 30858928
- 7. van der Waals LM, Laoukili J, et al. "Differential anti-tumour effects of MTH1 inhibitors in patient-derived 3D colorectal cancer cultures." Sci Rep. 2019 Jan 28;9(1):819. PMID: 30692572
- 8. Ramos-Alvarez I, Lee L, et al. "Cyclic AMP-dependent protein kinase A and EPAC mediate VIP and secretin stimulation of PAK4 and activation of Na(+),K(+)-ATPase in pancreatic acinar cells." Am J Physiol Gastrointest Liver Physiol. 2019 Feb 1;316(2):G263-G277. PMID: 30520694
- 9. Ramos-Alvarez I, Jensen RT. "P21-activated kinase 4 in pancreatic acinar cells is activated by numerous gastrointestinal hormones/neurotransmitters and growth factors by novel signaling, and its activation stimulates secretory/growth cascades." Am J Physiol Gastrointest Liver Physiol. 2018 Aug 1;315(2):G302-G317. PMID: 29672153
- 10. Verissimo CS, Overmeer RM, et al. "Targeting mutant RAS in patient-derived colorectal cancer organoids by combinatorial drug screening." Elife. 2016 Nov 15;5. pii: e18489. PMID: 27845624
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
白血病THP-1和MV4-11细胞 |
|
溶解方法 |
在DMSO中的溶解度大于10 mM。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
72 h，5 μM |
|
应用 |
SB202190是p38ɑ和p38β的特异性抑制剂，可以与ATP竞争结合p38上的同一位点。SB202190可以有效地激活THP-1和MV4-11细胞的生长，SB202190能够增加C-Raf和ERK的磷酸化，表明Raf–MEK–MAPK通路的激活参与SB202190诱导的细胞生长。 |
| 动物实验[2]: | |
|
动物模型 |
三个月无特定病原体（SPF）雄性Wistar大鼠 |
|
剂量 |
脑室内注射5 μL的10 μmol/L SB202190 |
|
应用 |
SB202190处理一周后，模型组海马内p38 MAPK的磷酸化高于SB202190处理组。在Morris水迷宫隐藏平台试验中，和模型组相比，SB202190组逃避潜伏期显著缩短。SB202190组的海马组织还具有高的Bcl-2表达和低的caspase-3表达，以及显著减少的神经细胞凋亡。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
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是一种高选择性的、细胞通透性的和有效的p38 MAP激酶抑制剂，对于p38和p38β的IC50值分别为50 nM和100 nM。 | |||||
| 靶点 | p38α MAPK | p38β MAPK | ||||
| IC50 | 50 nM | 100 nM | ||||
质量控制和MSDS
- 批次:
化学结构
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