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SB202190 (FHPI)

现货
Catalog No.
A1632
P38 MAPK抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
100mg
¥ 1,000.00
现货

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Background

SB202190 (FHPI) is a potent p38 MAPK inhibitor that specifically inhibits p38α and p38β with IC50 values of 50 and 100 nM, respectively [1].

SB202190 has been reported to potently enhance the growth of leukemia cell lines THP-1 and MV4-11. SB202190 activates the phosphorylation ERK and C-Raf. Studies have shown that the ED50 values of U0126 and FPT inhibitor II were significantly decreased in the presence of SB202190 [2].

SB202190 triggers changes in cell cycle profiles both during HU treatment and caffeine-induced PCC (premature chromosome condensation) in plants. Moreover, SB202190 and caffeine decrease independently HU-induced histone H4 Lys5 acetylation [3].

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.

文献引用

1. 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
2. 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
3. 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
4. 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
5. 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

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt331.34
Cas No.152121-30-7
FormulaC20H14N3OF
Solubility≥57 mg/mL in DMSO, ≥22.47 mg/mL in EtOH, <1.71 mg/mL in H2O
Chemical Name4-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)phenol
SDFDownload SDF
Canonical SMILESOC1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。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。

试验操作

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.

生物活性

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

化学结构

SB202190 (FHPI)

相关生物数据

SB202190 (FHPI)

相关生物数据

SB202190 (FHPI)

相关生物数据

SB202190 (FHPI)

相关生物数据

SB202190 (FHPI)