|4-(4-(4-氟苯基)-5-(吡啶-4-基)-1H-咪唑-2-基)苯酚|CsnPharm

CAS No.: 152121-30-7

SB 202190/杀虫畏 Catalog No. CSN12267

Synonyms: 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).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 4

Kd:3.4μM p38 MAPKα

IC50:50nM p38 MAPKβ

IC50:100nM
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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Nude Mice: 5 mg/kg^[3] (i.p.), 25 μg/kg^[4] (i.p.) Mice: 20 mg/kg^[5] (i.p.)

给药途径
i.p.

动物研究
剂量	Nude Mice: 5 mg/kg^[3] (i.p.), 25 μg/kg^[4] (i.p.) Mice: 20 mg/kg^[5] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0180 mL
- 15.0901 mL
- 30.1802 mL
- 5 mM
- 0.6036 mL
- 3.0180 mL
- 6.0360 mL
- 10 mM
- 0.3018 mL
- 1.5090 mL
- 3.0180 mL

技术信息

CAS号

152121-30-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H14FN3O

运输

蓝冰

分子量

331.34

别名

FHPI

溶解度

DMSO	66.0 mg/mL (199.2 mM)
Water	Insoluble
Ethanol	12.0 mg/mL (36.2 mM)

动物实验配方

5%DMSO+40%PEG300+5%Tween80+50%water

8 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

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

靶点	Description	IC50
Bromodomain 4		Kd:3.4μM
p38 MAPKα		IC50:50nM
p38 MAPKβ		IC50:100nM

SB 202190/杀虫畏 Catalog No. CSN12267

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