SB203580

For research use only.

Catalog No.S1076 Synonyms: RWJ 64809, PB 203580

470 publications

SB203580 Chemical Structure

CAS No. 152121-47-6

SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

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Selleck's SB203580 has been cited by 470 publications

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Biological Activity

Description SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.
Features First reported p38 inhibitor.
Targets
p38 MAPK [1]
(THP-1 cells)		 PKB [1]
(THP-1 cells)
0.3 μM-0.5 μM 3 μM-5 μM
In vitro

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. [1] SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. [2] SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC12 NGnXclFMcW6jc3WgRZN{[Xl? M4PPXFExKM7:TR?= NIjMcIYyPSCvaX6= NISyVZlKdmirYnn0d{BxOzhiTVHQJItqdmG|ZTD3bZRpKEmFNUCgc4YhOC54IN88US=> MVK3O|UxPTd5
THP-1 MXTGeY5kfGmxbjDBd5NigQ>? NWHnfoViUW6qaXLpeJMhVFCVLXnu[JVk\WRiVF7GZYxxcGFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOC5zNjFOwG0> NEjTXpAyQDN{NUe2PC=>
PBMC NVLUWJhOTnWwY4Tpc44hSXO|YYm= M3TlfFE2KG2rbh?= M2e1[mROW09? NV;Xd29jUW6qaXLpeJMhfGinIILlcIVie2Vib3[gbY51\XKuZYXrbY4uOS2kZYThJJdqfGhiSVO1NEBw\iByLkCzO{DPxE1? NVHKZoF4OTJ|NkGzPVY>
SW1353 NV74U2poTnWwY4Tpc44hSXO|YYm= MUexJIg> MmTISG1UVw>? NHrJcHhKdmirYnn0d{BKVC14IIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDBwMEWg{txO MlG1NVEyPDB5NEG=
Hela Mn7ySpVv[3Srb36gRZN{[Xl? NVPYcWRZTE2VTx?= MUTJcohq[mm2czDUZZQucW6mdXPl[EBJUVZzIFzUVkB1emGwc3HjeIl3[XSrb36gbY4hcHWvYX6gTIVN[SClZXzsd{B4cXSqIFnDOVAhd2ZiMD6xJO69VQ>? Mmr4NVg6OjZ5MUG=
PC12 MmHSSpVv[3Srb36gRZN{[Xl? MVSxNEDPxE1? NWjPSotITE2VTx?= MlHJRYN1cX[jdHXzJG5z\jJxQWLFJIlvKHKjdDDQR|EzKGOnbHzzJIF{e2W|c3XkJIF{KEiRLUGgdJJwfGWrbjDpcoR2[3Srb36= MkKxNlE{PDV4OEW=
RAW 264.7 Mnf6R5l1d3SxeHnjJGF{e2G7 NGjQTXAyOi53IN88US=> NIfvNlAyOmh? M3raU2ROW09? MYnCcI9kc3NibHX0bIFtKHSxeHnuMY1m\GmjdHXkJIN6fG:2b4jpZ4l1gQ>? M{nKNlE4PDh3NUC0
HCA2 NWmzNmx6TnWwY4Tpc44hSXO|YYm= MV[yMlUh|ryP MkXKTY5pcWKrdIOgdFM5KG2nZHnheIVlKE2NMjDhZ5RqfmG2aX;u NUPITm9YOTd7NkS3PFA>
U937 MoPDSpVv[3Srb36gRZN{[Xl? NVvXVVN5UW6qaXLpeJMhUkGNLX3l[IlifGWmIHnueIVz\mW{b36t[4FudWFxYX7pd49ugWOrbj3pcoR2[2WmIGP0ZZQyKHCqb4PwbI9zgWyjdHnvci=> MUmxPFE2PzF{Mh?=
U937 NFuzR2RHfW6ldHnvckBCe3OjeR?= NXjySI95UW6qaXLpeJMhUkGNLX3l[IlifGWmIHnueIVz\mW{b36t[4FudWFxYX7pd49ugWOrbj3pcoR2[2WmIICzPEBxcG:|cHjvdplt[XSrb36= NW\MdZRSOThzNUexNlI>
hESCs NYHaV2VrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLFOUDPxE1? NF;CPY5FVVOR MlvwTY5lfWOnczDjZZJlcW:veX;n[Y5q[yCjY4Tpeol1gSCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bC=> Mn33NlM3ODJ|OUm=
RAW264.7 M4nLUmZ2dmO2aX;uJGF{e2G7 NX7sOnZVOTBizszN NGfrN|hKdmS3Y3XzJIFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZpkhcW6qaXLpeIlv\yCLTD2x{tIhemWuZXHz[S=> M{L0O|I{PzlzMEe4
RAW264.7 MXTGeY5kfGmxbjDBd5NigQ>? MkXGNVAh|ryP NYm0RndXUW6mdXPld{BidnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIJ6KGmwaHnibZRqdmdiaV7PV{Bz\WynYYPl NGTzbJgzOzd7MUC3PC=>
RAW264.7 MmPNSpVv[3Srb36gRZN{[Xl? MWOxNEDPxE1? Ml;WTY5lfWOnczDhcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHL5JIlvcGmkaYTpcochVk9icnXs[YF{\Q>? NFH5Z2gzOzd7MUC3PC=>
RAW264.7 MX7GeY5kfGmxbjDBd5NigQ>? NEjqbncyOCEQvF2= M3PlZ2lvcGmkaYTzJGxRWy2rbnT1Z4VlKHB|ODDNRXBMKHCqb4PwbI9zgWyjdHnvci=> MkK2NlQxOTZyNUe=
IEC-18 NEfMU5dHfW6ldHnvckBCe3OjeR?= NWTBN|N1OTBizszN M17PNmlvcGmkaYTzJGxRWy2rbnT1Z4VlKHB|ODDNRXBMKHCqb4PwbI9zgWyjdHnvci=> M12yTFI{PzV6MUGw

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
phospho-p38 / p38; 

PubMed: 25747578     


Mock-infected RD cells were treated with SB203580 at different concentrations (10, 25, 50 and 100μM) or 1.0% DMSO (negative control) and cell lysates were harvested for Western blotting at 6h post-treatment. β-actin was included as a loading control. 

p-ASK1 / ASK1 / P-JNK / p-MKK4 / p-ERK; 

PubMed: 24082073     


(B) AGS cells were infected with ASK1-HA-expressing adenoviruses for 24 h, pretreated with vehicle (DMSO) or 10 μM SB203580, and stimulated with or without H. pylori for 3 h. Immunoblots of the indicated proteins are shown. (C) AGS cells were transfected with NC or ASK1 siRNA for 48 h and treated with vehicle (DMSO) or 10 μM SB203580 for 4 h. Immunoblots of the indicated proteins are shown.

phospho-MK2(T334) / phospho-HSP27(S82) / phospho-Akt(T308) / phospho-Akt(S473); 

PubMed: 21737674     


Lysates from wild-type MEFs pretreated with or without SB203580 (10 μM, 30 min) and exposed to H2O2 (100 μM) for the indicated duration were analyzed by immunoblotting with the indicated antibodies.

25747578 24082073 21737674
Immunofluorescence
dsRNA / hnRNP A1; 

PubMed: 25747578     


RD cells were subjected to infection with EV71 and post-treated with SB203580 (p38 MAPK inhibitor) for 8h. SB203580-treated cells were fixed and the subcellular localisation of hnRNP A1 (red) was investigated by indirect immunofluorescence assay. Mock-infected and DMSO-treated cells were included as infection and solvent control, respectively. The images were taken at 100X magnification. Colocalisation quantification was based on the MOC using WCIF ImageJ software and represented as percent colocalisation at the respective drug concentrations. Error bars represent the standard deviation of duplicate data.

25747578
Growth inhibition assay
Cell viability ; 

PubMed: 23001390     


B16F10 cells were treated with a concentrations of SB203580 as indicated in figure a.

23001390
In vivo SB203580 protects pig myocardium against ischemic injury in an in vivo model. [4]SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE). [5]

Protocol

Kinase Assay:

[1]
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Cellular receptor kinase phosphorylation assay :

4 μg of sheep anti-PKBα is immobilized on 25 μL of protein G-Sepharose overnight (or 1.5 hours) and washed in Buffer A (50 mm Tris, pH 7.5, 1 mm EDTA, 1 mm EGTA, 0.5 mm Na3VO4, 0.1% β-mercaptoethanol, 1% Triton X-100, 50 mm sodium fluoride, 5 mm sodium pyrophosphate, 0.1 mm phenylmethylsulfonyl fluoride, 1 μg/mL aprotinin, pepstatin, leupeptin, and 1 μm microcystin). The immobilized anti-PKB is then incubated with 0.5 ml of lysate (from 5 × 106 cells) for 1.5 hours and washed three times in 0.5 mL of Buffer A supplemented with 0.5 m NaCl, two times in 0.5 mL of Buffer B (50 mm Tris-HCl, pH 7.5, 0.03% (w/v) Brij-35, 0.1 mm EGTA, and 0.1% β-mercaptoethanol), and twice with 100 μl of assay dilution buffer; 5× assay dilution buffer is 100 mm MOPS, pH 7.2, 125 mm β-glycerophosphate, 25 mm EGTA, 5 mm sodium orthovanadate, 5 mm DTT. To the PKB enzyme immune complex is added 10 μL of assay dilution buffer, 40 μm protein kinase A inhibitor peptide, 100 μm PKB-specific substrate peptide, and 10 μCi of [γ-32P]ATP, all made up in assay dilution buffer. The reaction is incubated for 20 minutes at room temperature with shaking, then samples are pulse spun, and 40 μL of reaction volume are removed into another tube to which is added 20 μL of 40% trichloroacetic acid to stop the reaction. This is mixed and incubated for 5 minutes at room temperature, and 40 μL is transferred onto P81 phosphocellulose paper and allowed to bind for 30 seconds. The P81 piece is washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation is then measured by scintillation counting.
Cell Research:

[1]
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  • Cell lines: CT6 cell , BA/F3 F7 cell
  • Concentrations: 0–30 μM
  • Incubation Time: 1 hour
  • Method:

    CT6 cell and BA/F3 F7 cell are rested by washing three times in RPMI and culturing overnight in RPMI, 5% fetal calf serum in the absence of growth factor, antibiotics, or β-mercaptoethanol supplements. 2–5 × 106 rested CT6 cells are resuspended in 2 mL of RPMI, 5% fetal calf serum and preincubated with SB203580 or vehicle control as indicated in figure legends. Cells are then stimulated with 20 ng/ml recombinant human IL-2 for 5 minutes at 37  °C and pelleted in a minifuge for 30 seconds, medium is aspirated, and the pellet is lysed in the appropriate buffer. BA/F3 cells stably expressing deletion mutants of IL-2 receptor β chain are maintained in glutamine containing RPMI further supplemented with 5% fetal calf serum and 0.2 μg/mL G418. The cells are then washed extensively, rested overnight, and washed again before activating with IL-2; such cell preparations are >90% T cells. Cellular proliferation assays are performed by measurement of [3H]thymidine incorporation.


    (Only for Reference)
Animal Research:

[5]
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  • Animal Models: Systemic lupus erythematosus (SLE) are established in female MRL/lpr mice and female C57BL/6 mice
  • Dosages: 0.1 M/day
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 43 mg/mL (113.92 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 377.43
Formula

C21H16FN3OS
CAS No. 152121-47-6
Storage powder
in solvent
Synonyms RWJ 64809, PB 203580
Smiles CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID