SB 202190 | FHPI | p38 MAPK Inhibitor | AmBeed-信号通路专用抑制剂

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杀虫畏 /SB 202190 {[allProObj[0].p_purity_real_show]}

货号：A277214 同义名： FHPI

SB-202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase with IC50 values of 50 nM and 100 nM for p38α and p38β respectively; also shows slightly weaker activity for BRD4 (Kd=3.4 μM).

SB 202190 化学结构
CAS号：152121-30-7

SB 202190 3D分子结构
CAS号：152121-30-7

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SB 202190 纯度/质量文件产品仅供科研

货号：A277214 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

自噬亚型比较
p38 MAPK 亚型比较

产品名称	Autophagy ↓ ↑	其他靶点	纯度
SBI-0206965	+++ ULK1, IC50: 108 nM ULK2, IC50: 711 nM		97%
Hydroxychloroquine sulfate	✔		99%
Valproic acid sodium	✔	HDAC	97%
PFK-015	++ PFKFB3, IC50: 207 nM		99%+
MRT68921 hydrochloride	++++ ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM		99%+
ROC-325	✔		99%+
Autophinib	+++ Autophagy, IC50: 40 nM		97%
Lys05	✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	p38 MAPK ↓ ↑	p38α ↓ ↑	p38β ↓ ↑	其他靶点	纯度
BMS-582949	+++ p38 MAPK, IC50: 13 nM				98%
SB 203580					99%+
Pexmetinib	✔			Tie-2	99%+
Skepinone-L		++++ p38α, IC50: 5 nM			98%
Doramapimod		++++ p38α, IC50: 38 nM p38α, Kd: 0.1 nM			99%+
VX-702					99%+
Ralimetinib dimesylate		++++ p38α, IC50: 7 nM			98%
SB 202190		++ p38α, IC50: 50 nM	++ p38β, IC50: 100 nM		99%+
Losmapimod		++++ p38α, pKi: 8.1	+++ p38β, pKi: 7.6		99%+
Neflamapimod		+++ p38α, IC50: 10 nM	+ p38β, IC50: 220 nM		99%+
PH-797804		++ p38α, IC50: 26 nM	+ p38β, IC50: 102 nM		98%
TAK-715		++++ p38α, IC50: 7.1 nM	+ p38β, IC50: 0.20 μM		99%+
SB 239063		++ p38α, IC50: 44 nM	++ p38β, IC50: 44 nM		99%+
Pamapimod		+++ p38α, IC50: 0.014 μM	+ p38β, IC50: 0.48 μM		98%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

SB 202190 生物活性

靶点	p38β p38β, IC50:100 nM p38α p38α, IC50:50 nM
描述	Mitogen-activated protein kinase (MAPK) cascades regulate signal transduction involved in cell proliferation and death. SB-202190 is a potent cell-permeable inhibitor of p38 MAPK that inhibits p38 and p38β with IC50 values of 50 nM and 100 nM, respectively^[3]. SB-202190 at 5 μM inhibited the activation of p38 in HaCaT cells. The protein expression of COX-2 was almost completely blocked by 5 μM SB-202190 at 8 and 12 h post the exposure to UVB irradiation (250 J/m²). SB-202190 at the same concentration also significantly abrogated UVB induced cox-2mRNA in HaCaT cells. The inhibitory effect of SB-202190 on PGE₂ production after UVB was observed in HaCaT cells treated by 5 μM SB-202190 for one hour^[4]. Bull serum albumin induced the gene expression of the inflammation marker MCP-1 more than 30-fold in renal tubular cells, while pre-incubation with 10 μM SB-202190 decreased the gene expression to the basal level. In HK-2 cells, 10 μM SB202190 treatment significantly reduced TGF-β1-induced gene expression^[5]. Two doses of SB-202190 (6.25 μg/dose, i.d. administered) prevented the development of blisters and a positive Nikolsky’s skin induced by PV IgG injection (1.5 mg of IgG/g body weight) in neonatal mice. The PV IgG-mediated activation of phospho-p38MAPK immunoreactivity in the skin was abrogated in SB-202190-treated mice^[6].
作用机制	SB-202190 is a pyridinyl imidazole that inhibits p38 MAPK via competing with ATP^[7].

SB 202190 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A 549	50 μM	Function Assay	1 h	decreases the level of IL-8	24179688
A549	0.3/3/30 μM	Function Assay	1 h	significantly attenuates ATPγS-mediated COX-2 protein and mRNA expression and promoter activity	23680674
A549	10 μM	Function Assay	0-30 min	inhibits ATPγS induced p42/p44 MAPK and p38 MAPK phosphorylation	23680674
A549	10 μM	Function Assay	1 h	inhibits ATPγS induced NF-κB p65 subunit phosphorylation and NF-κB promoter activity	23680674

SB 202190 动物研究

Dose	Nude Mice: 5 mg/kg^[3] (i.p.), 25 μg/kg^[4] (i.p.) Mice: 20 mg/kg^[5] (i.p.)
Administration	i.p.

SB 202190 参考文献

[1]351(Pt 1):95-105.

[2]20(29):3921-6.

[3]Davies SP, 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.

[4]Chen W, Tang Q, Gonzales MS, Bowden GT. Role of p38 MAP kinases and ERK in mediating ultraviolet-B induced cyclooxygenase-2 gene expression in human keratinocytes. Oncogene. 2001 Jun 28;20(29):3921-6.

[5]Prakash J, Sandovici M, Saluja V, Lacombe M, Schaapveld RQ, de Borst MH, van Goor H, Henning RH, Proost JH, Moolenaar F, Këri G, Meijer DK, Poelstra K, Kok RJ. Intracellular delivery of the p38 mitogen-activated protein kinase inhibitor SB202190 [4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)1H-imidazole] in renal tubular cells: a novel strategy to treat renal fibrosis. J Pharmacol Exp Ther. 2006 Oct;319(1):8-19.

SB 202190 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.18mL

6.04mL

3.02mL

SB 202190 技术信息

CAS号	152121-30-7
分子式	C₂₀H₁₄FN₃O
分子量	331.343

别名	FHPI
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(316.89 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water 8 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A 549	50 μM	Function Assay	1 h	decreases the level of IL-8	24179688
A549	0.3/3/30 μM	Function Assay	1 h	significantly attenuates ATPγS-mediated COX-2 protein and mRNA expression and promoter activity	23680674
A549	10 μM	Function Assay	0-30 min	inhibits ATPγS induced p42/p44 MAPK and p38 MAPK phosphorylation	23680674
A549	10 μM	Function Assay	1 h	inhibits ATPγS induced NF-κB p65 subunit phosphorylation and NF-κB promoter activity	23680674
A549	10 μM	Function Assay	1 h	reduces ATPγS-stimulated cPLA2 phosphorylation	23680674
A549	10 μM	Function Assay	1 h	reduces ATPγS-enhanced enzymatic activity of cPLA2	23680674
AGS	5 μM	Function Assay	30 min	suppresses 1-induced caspase-8 and caspase-3 activation	24547878
AGS	10 µM	Function Assay	30 min	inhibits IL-1β-induced activation of p38	24479681
AGS	10 µM	Function Assay	30 min	attenuates IL-1β-induced GA cell migration and invasion	24479681
AGS	10 µM	Function Assay	30 min	significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression	24479681
AGS	10 μM	Function Assay	30 min	inhibits caspase-3 activation and inhibition of ERK	23850994
AsPC-1	20 μM	Function Assay	24 h	results in a modest inhibition of HIF-1α protein accumulation	25888489
AsPC-1	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
BEAS-2B	10 μM	Growth Inhibition Assay	30 min	reverses the decrease of cell viability induced by HCI	23784034
BEAS-2B	10 μM	Cytotoxity Assay	30 min	inhibited the increase in LDH and IL-8 expression	23784034
BEAS-2B	10 μM	Function Assay	30 min	decreases the levels of caspase-3, Bad and fas	23784034
BEL7404	0-50 μM	Growth Inhibition Assay	48 h	inhibits the proliferation in a dose dependent manner	23807508
BxPC-3	20 μM	Function Assay	24 h	results in a modest inhibition of HIF-1α protein accumulation	25888489
BxPC-3	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
BxPC-3	10 μM	Function Assay	1 h	enhances the autophagic effect	25632222
DCs	20 μM	Function Assay	1 h	decreases IL-12 production	24434636
H1650	10 μM	Function Assay	1 h	decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells	23228696
H1650	10 μM	Growth Inhibition Assay	1 h	enhances paclitaxel-induced cytotoxicity	23228696
H1703	10 µM	Function Assay	1 h	decreases the pemetrexed-induced MSH2 mRNA and protein levels	24530475
H1703	10 µM	Function Assay	12 h	inhibits pemetrexed-elicited MSH2 protein stability	24530475
H1703	10 µM	Function Assay	6 h	significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line	24530475
H1703	5/10 μM	Function Assay	1 h	decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell	24138903
H1703	10 µM	Function Assay	12 h	decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells	24138903
H1703	10 μM	Function Assay	1 h	decreases both protein and mRNA levels of ERCC1 in paclitaxel-exposed cells	23228696
H1703	10 μM	Growth Inhibition Assay	1 h	enhances paclitaxel-induced cytotoxicity	23228696
H520	10 µM	Function Assay	1 h	decreases the pemetrexed-induced MSH2 mRNA and protein levels	24530475
H520	10 µM	Function Assay	12 h	inhibits pemetrexed-elicited MSH2 protein stability	24530475
H520	10 µM	Function Assay	6 h	significantly increases the levels of ubiquitin-conjugated MSH2 in pemetrexed-treated cell line	24530475
H520	5/10 μM	Function Assay	1 h	decreases MSH2 protein as well as mRNA levels in gefitinib-exposed cell	24138903
H520	10 µM	Function Assay	12 h	decreases MSH2 mRNA and protein stability in gefitinib-treated NSCLC cells	24138903
H9c2	50 μM	Function Assay	12 h	reduces LDH release and MMP loss	25245818
H9c2	0.01/0.1/1 μM	Function Assay	1 h	attenuates TNF-α-induced MMP-9 expression, mRNA levels, and promoter activity	23774252
H9c2	1 μM	Function Assay	1 h	reduces TNF-α directly stimulated p38 MAPK phosphorylation	23774252
H9c2	1 μM	Function Assay	1 h	reduces TNF-α-induced MMP-9 mRNA levels and promoter activity	23353699
H9c2	1 μM	Function Assay	1 h	reduces TNF-α-enhanced AP-1 promoter activity	23353699
HaCaT	5 µM	Function Assay	24 h	inhibits IFN-γ-induced CCL22 production levels	25834353
HaCaT	5 µM	Function Assay	24 h	inhibits IFN-α-induced CCL22 production levels	25834353
HaCaT	40 μM	Function Assay	3-24 h	reduces the accumulation of ZO-1	25435485
HAPI	10/20/40 μM	Function Assay	1 h	inhibits TCDD-induced p38/JNK MAPK phosphorylation	23969120
HAPI	20 μM	Function Assay	1 h	attenuates TCDD-induced activation of iNOS and production	23969120
HCT-116	25 μM	Function Assay	30 min	attenuates the mRNA and protein expression of hBD-2 in responsive to DA	26223251
HepG2	350 nM	Function Assay	24 h	inhibits the deguelin-induced activation of p38MAPK	23933198
HepG2	0-50 μM	Growth Inhibition Assay	48 h	inhibits the proliferation in a dose dependent manner	23807508
HepG2	0-50 μM	Function Assay	24 h	inhibits the phosphorylation of p38 downstream proteins MAPKAPK2, ATF2, MSK1 and HSP27 in a dose-dependent manner	23807508
HEY	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
HK-2	20 μM	Apoptosis Assay	24 h	inhibits ERK and p38MAPK	23543151
HL7702	0-50 μM	Growth Inhibition Assay	48 h	inhibits the proliferation in a dose dependent manner	23807508
HPAEpiCs	1/3/10 μM	Function Assay	1 h	reduces S1P-induced ICAM-1 protein and mRNA expression and promoter activity	25734900
HPAEpiCs	1/3/10 μM	Function Assay	1 h	inhibits S1P-stimulated Akt phosphorylation	25734900
HPAEpiCs	1/3/10 μM	Function Assay	1 h	inhibits S1P time-dependently stimulated c-Jun phosphorylation	25734900
HPAEpiCs	0.1/1/10 μM	Function Assay	1 h	inhibits TNF-α-induced cPLA2 protein and mRNA expression	24069158
HSCs	25 μM	Apoptosis Assay	24 h	significantly attenuates TG-induced activated HSCs apoptosis	24961950
HTSMCs	0.1/1/10 μM	Function Assay	1 h	inhibited CORM-2-induced HO-1 protein levels and mRNA expression	25921464
HUVEC	20 μm	Function Assay	5 h	reduces cytokine expression levels in a concentration-dependent manner	24189062
HUVECs	10 µM	Function Assay	1 h	inhibits TNF-α-induced CXCL1 production	24487964
K562	10 μM	Function Assay	1 h	inhibits quinacrine-induced p38 MAPK phosphorylation	25684043
K562	0.25-1 μM	Function Assay	24 h	suppresses resveratrol-induced H2AX phosphorylation	25619392
macrophages	1 μM	Function Assay	4.5 h	completely inhibits MT-III-induced activation of NF-κB	24808633
MC3T3-E1	0.3/3/30 μM	Function Assay	1 h	attenuates TNF-α-induced MMP-9 expression in a concentration-dependent manner	24502696
MC3T3-E1	30 μM	Function Assay	1 h	attenuates TNF-α-stimulated p38 MAPK phosphorylation	24502696
MCF-7	10 μM	Growth Inhibition Assay	24 h	inhibits the CR108-induced cell death	24128853
MCF-7	10 μM	Function Assay	1 h	reduces the WA-induced phosphorylated p38 MAPK	24019090
MCF-7	10 μM	Function Assay	24 h	increases the WA-induced apoptosis	24019090
MDA-MB-231	2 μM	Function Assay	24 h	lessenes CCL2 induction by TNFα	26100848
MDDCs		Growth Inhibition Assay	72 h	IC502.7μM	24815087
MDDCs	0-15 μM	Function Assay	48 h	suppresses IFN-α and IP-10 production	24815087
MDDCs	0-15 μM	Function Assay	48 h	inhibits MIP-1a, MIP-1b and RANTES production	24815087
MDDCs	10 μM	Function Assay	3.5 h	blocks EBOV GP, but not VSV G mediated entry into human MDDCs	24815087
MG63	10/20/30 μM	Function Assay	24 h	significantly decreases the level of phosphorylated p38 induced by CdCl2 in a concentration -dependent manner	25998312
MG63	10/20/30 μM	Apoptosis Assay	24 h	significantly decreased the apoptosis rate of MG63 induced by CdCl2	25998312
MH7A		Growth Inhibition Assay	24 h	reinforces the inhibitory effects of XAN	25862966
MH7A	25 μM	Apoptosis Assay	24 h	reverses cell cycle arrest induced by XAN and caused apoptosis of cells via activation of JNK	25862966
MIA PaCa-2	20 μM	Function Assay	24 h	reduced lactate accumulation in combination with both 2-DG and D-allose	25888489
MIA PaCa-2	20 μM	Function Assay	24 h	results in a modest inhibition of HIF-1α protein accumulation	25888489
MIA PaCa-2	20 μM	Function Assay	24 h	enhances cleavage of PARP when combined with glucose analogs	25888489
MIA PaCa-2	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
MKN-45	10 µM	Function Assay	30 min	inhibits IL-1β-induced activation of p38	24479681
MKN-45	10 µM	Function Assay	30 min	attenuates IL-1β-induced GA cell migration and invasion	24479681
MKN-45	10 µM	Function Assay	30 min	significantly decreases Il-1β-induced MMP2 and MMP9 mRNA expression	24479681
OVCAR-3	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
PANC-1	10 μM	Function Assay	1 h	enhances the autophagic effect	25632222
PC12	10/20/40 μM	Function Assay	1 h	inhibits JNK and p38	23584357
PDL	20 μM	Function Assay	30 min	significantly inhibits the tensile force-mediated BMP-2 expression	24561081
podocytes	10 μM	Function Assay	1 h	inhibits TGFβ1-induced activation of p38MAPK and Erk1/2	24036212
RAW 264.7	10 μM	Function Assay	30 min	induces characteristic vacuolation of OCs	25461399
RAW 264.7	10 μM	Function Assay	30 min	attenuates the effects of OPG on osteoclast retraction	25461399
rBMSCs	10 μM	Function Assay	2.5 h	depresses the phosphorylation of ERK and p38	26053266
SCC25	20 μM	Function Assay	24 h	increases autophagy level	25834400
SK-OV-3	20 μM	Growth Inhibition Assay	2 h	sensitizes cell lines to treatment with 2-DG and D-allose	25888489
THP-1	5 µM	Function Assay	2 h	significantly attenuates secretion of IL-1α induced by 27OHChol plus FSL-1	25598661
THP-1		Growth Inhibition Assay	72 h	IC50=4.7μM	24815087
U937	10 μM	Function Assay	1 h	abrogates the caffeine effect on MKP-1 and PP2Acα mRNA transcriptional levels	23707387
U937	10 μM	Function Assay	1 h	abrogates caffeine-induced MKP-1 down-regulation and PP2Acα up-regulation	23707387
U937	10 μM	Function Assay	1 h	suppresses c-Jun and CREB phosphorylation in caffeine-treated cells	23707387
WB	20 μM	Function Assay	30 min	decreases the LPS- or LTA-induced IL-6 and TNF-α production	25530682

杀虫畏 /SB 202190 {[allProObj[0].p_purity_real_show]}

SB 202190 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

SB 202190 质控信息

SB 202190 生物活性

SB 202190 细胞研究

SB 202190 动物研究

SB 202190 参考文献

SB 202190 实验方案

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杀虫畏 /SB 202190 {[allProObj[0].p_purity_real_show]}

SB 202190 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

SB 202190 质控信息

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SB 202190 参考文献

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SB 202190 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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