SB202190

ArtNr	S1077-10mM
Hersteller	Selleckchem
CAS-Nr.	152121-30-7
Menge	10 mM/1 ml
Kategorie	Oncology Neuroscience Neural Lineage Markers Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Colorectal Cancer Heart & Blood Cancer Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	p38alpha, p38beta;p38 MAPK
Similar products	SB
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Administration	Administered via i.d.
Animal Models	C57BL/6J mice injected i.d. with a sterile solution of either control IgG or PV IgG
Cell lines	Jurkat, and HeLa
Chemical Name	4-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)phenol
Concentrations	Dissolved in DMSO, final concentrations ca.50 uM
Description	SB 202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38alpha and p38beta with IC50 of 50 nM and 100 nM, respectively.
Dosages	12.5 ug
Formulation	Dissolved in DMSO, and diluted in saline
IC50	50 nM, 50 nM, 50 nM, 50 nM, 50 nM, 50 nM
In vitro	SB 202190 significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner. SB202190 by itself is sufficient to induce cell death in Jurkat and HeLa cells through activation of CPP32-like caspases, which can be blocked by expression of bcl-2. SB202190-induced apoptosis is attenuated by p38beta but augmented by p38alpha. [2] SB 202190 strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA. [3] SB 202190 treatment inhibits the expression of albumin-induced proinflammatory (monocyte chemoattractant protein-1) and transforming growth factor (TGF)-beta1-induced profibrotic (procollagen-Ialpha1) genes over 50% in renal tubular cells (normal rat kidney-52E). [4] SB 202190 treatment induces phosphorylation of JNK in a dose- and time- dependent manner in A549 cells, induces phosphorylation of ATF-2 transcription factor, and increases AP-1 DNA binding. [6] SB 202190 treatment enhances the growth of THP-1 and MV4-11 cells. SB 202190 increases the phosphorylation of c-Raf and ERK, suggesting that Ras-Raf-MEK-mitogen-activated protein kinase (MAPK) pathway activation is involved in the leukemia cell growth induced by SB 202190. [7]
In vivo	Inhibiting p38 by administration of SB 202190 inhibits PV IgG-induced blister formation in the passive transfer mouse model. [5] In the endotoxin model of sepsis, SB 202190 treatment produces a statistically significant survival benefit compared with control. [8]
Incubation Time	24 hours
Kinase Assay	In vitro kinase assays, The p38alpha and p38beta are assayed in 25 mM Tris-HCl, pH 7.5, containing 0.1 mM EGTA, with myelin basic protein (0.33 mg/mL) as substrate. Assays are performed either manually for 10 minutes at 30 C in 50 uL incubations using [gamma-33P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at ambient temperature in 25 uL incubations using [gamma-33P]ATP. The concentrations of ATP and magnesium acetate are 0.1 mM and 10 mM respectively. All assays are initiated with MgATP. Manual assays are terminated by spotting aliquots of incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays are terminated by the addition of 5 uL of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers are then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity.
Method	Cells are serum-starved and then treated with different concentration of SB 202190 for 24 hours. Cell viability is assayed by either trypan blue exclusion or propidium iodide exclusion followed by flow cytometry analysis. The apoptotic nuclei are visualized by H33258 staining.
Molecular Weight (MW)	331, 34
Picture ChemicalStructure Description	SB 202190 Chemical Structure
Picture Description 1	Data from [J Biol Chem , 2010, 285, 3282432833], SB 202190purchased from Selleck, C, Jurkat cells with SB202190 at 1, 5, and 10 M were tested, and a decreased SRP72 expression was found when using at 10 M (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 M at 240 versus 0 and 120 versus 0 min (p0.05).
Picture Description 2	Data from [J Biol Chem , 2010, 285, 3282432833], SB 202190purchased from Selleck, C, effect of SB202190 (1, 5, and 10 M) on SRP72 phosphorylation was tested. A decreased intensity of SRP72 expression when used at 1 M (240 min) and 5 and 10 M (120 and 240 min) was found. D, RUA illustrated obtaining significant results at concentration 5 and 10 M at 120 versus 0 and 240 versus 0 min. * indicates p0.05.
Solubility (25C)	DMSO 66 mg/mL, Water <1 mg/mL, Ethanol 32 mg/mL
Storage	2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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