Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>SB202190 (FHPI)

SB202190 (FHPI)

Catalog No.GC13968

SB202190 (FHPI) is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively.

Products are for research use only. Not for human use. We do not sell to patients.

SB202190 (FHPI) Chemical Structure

Cas No.: 152121-30-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$38.00
In stock
10mg
$25.00
In stock
25mg
$40.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Kinase experiment[1]:

Preparation Method

The p38α and p38β 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℃ in 50 μL incubations using [γ-33P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at ambient temperature in 25 μL incubations using [γ-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 μL 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.

Applications

SB 202190 is a selective p38 MAPK inhibitor with IC50 of p38α and p38β2 at 50 nM and 100 nM, respectively.

Cell experiment [2]:

Cell lines

Jurkat and HeLa cells

Preparation 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.

Reaction Conditions

50 μM;24 hours

Applications

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.

Animal experiment [3]:

Animal models

C57BL/6J mice

Preparation Method

Neonatal C57BL/6J mice were injected i.d. with either PV IgG (1.5 mg of IgG/g body weight) or PV IgG (1.5 mg of IgG/g body weight) plus SB202190

Dosage form

12.5 μg; i.d.

Applications

SB 202190 attenuated blister formation induced by human poliomyelitis IgG(PV-IgG) in a passively transferred mouse model by inhibiting p38.

References:

[1]. Davies SP, Reddy H, et,al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095. PMID: 10998351; PMCID: PMC1221339.

[2].Nemoto S, Xiang J, et,al.Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20. doi: 10.1074/jbc.273.26.16415. PMID: 9632706.

[3]. Berkowitz P, Hu P, et,al. p38MAPK inhibition prevents disease in pemphigus vulgaris mice. Proc Natl Acad Sci U S A. 2006 Aug 22;103(34):12855-60. doi: 10.1073/pnas.0602973103. Epub 2006 Aug 14. PMID: 16908851; PMCID: PMC1568937.

Background

SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1,2]. SB202190 inhibits apoptosis of endothelial cells by inducing autophagy and heme oxidase 1 [3].

SB 202190(50 µM;24 hours) 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 p38β but augmented by p38α[4]. SB 202190 treatment(5/10 µM SB202190;4h) 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[5]. SB 202190(5µM;1h) strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA[6].

SB 202190(12.5 µg; i.d.) attenuated blister formation induced by human poliomyelitis IgG(PV-IgG) in a passively transferred mouse model by inhibiting p38[7]. Inhibition of P38-MAPK by SB-202190(2.5µM/kg;24d; s.c.) resulted in increased primary tumor growth in tumor-bearing Balb-c mice (4T-1 cells) [8].

References:
[1]. Davies SP, Reddy H, et,al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095. PMID: 10998351; PMCID: PMC1221339.
[2]. Schwartz M, BÖckmann S, et,al.SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. Oncotarget. 2018 May 1;9(33):23149-23163. doi: 10.18632/oncotarget.25234. PMID: 29796178; PMCID: PMC5955409.
[3]. Grossi V, Liuzzi M, et,al.Sorafenib inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81. doi: 10.4161/cbt.22254. Epub 2012 Sep 17. PMID: 22986232; PMCID: PMC3542239.
[4]. Nemoto S, Xiang J, et,al.Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20. doi: 10.1074/jbc.273.26.16415. PMID: 9632706.
[5]. Muniyappa H, Das KC. Activation of c-Jun N-terminal kinase (JNK) by widely used specific p38 MAPK inhibitors SB202190 and SB203580: a MLK-3-MKK7-dependent mechanism. Cell Signal. 2008 Apr;20(4):675-83. doi: 10.1016/j.cellsig.2007.12.003. Epub 2007 Dec 8. PMID: 18222647; PMCID: PMC2423944.
[6]. Chen W, Tang Q, et,al.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. doi: 10.1038/sj.onc.1204530. PMID: 11439356.
[7]. Berkowitz P, Hu P, et,al. p38MAPK inhibition prevents disease in pemphigus vulgaris mice. Proc Natl Acad Sci U S A. 2006 Aug 22;103(34):12855-60. doi: 10.1073/pnas.0602973103. Epub 2006 Aug 14. PMID: 16908851; PMCID: PMC1568937.
[8]. O'Sullivan AW, Wang JH, et,al. p38 MAP kinase inhibition promotes primary tumour growth via VEGF independent mechanism. World J Surg Oncol. 2009 Nov 15;7:89. doi: 10.1186/1477-7819-7-89. PMID: 19912664; PMCID: PMC2785811.

Chemical Properties

Cas No. 152121-30-7 SDF
Chemical Name 4-(4-(4-fluorophenyl)-5-(pyridin-4-yl)-1H-imidazol-2-yl)phenol
Canonical SMILES FC1=CC=C(C2=C(C3=CC=NC=C3)NC(C4=CC=C(O)C=C4)=N2)C=C1
Formula C20H14N3OF M.Wt 331.34
Solubility ≥ 57 mg/mL in DMSO, ≥ 22.47 mg/mL in EtOH Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.018 mL 15.0902 mL 30.1805 mL
5 mM 0.6036 mL 3.018 mL 6.0361 mL
10 mM 0.3018 mL 1.509 mL 3.018 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for SB202190 (FHPI)

Average Rating: 5 ★★★★★ (Based on Reviews and 8 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for SB202190 (FHPI)

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.