SB203580

For research use only.

Catalog No.S1076 Synonyms: RWJ 64809, PB 203580

567 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.

Size Price Stock Quantity  
10mM (1mL in DMSO) USD 191 In stock
USD 147 In stock
USD 270 In stock
USD 370 In stock
USD 470 In stock
USD 1170 In stock
Bulk Discount
Bulk Inquiry

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's SB203580 has been cited by 567 publications

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

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 NWSw[pdJU2mwYYPlJGF{e2G7 M{nHNlExKM7:TR?= M3;4N|E2KG2rbh?= MY\Jcohq[mm2czDwN|ghVUGSIHvpcoF{\SC5aYToJGlEPTBib3[gNE43KM7:TR?= NXm1Z4xwPzd3MEW3Oy=>
THP-1 MXjGeY5kfGmxbjDBd5NigQ>? NGX6[GVKdmirYnn0d{BNWFNvaX7keYNm\CCWTl\hcJBp[SCycn;keYN1cW:wIIfpeIghUUN3MDDv[kAxNjF4IN88US=> MY[xPFMzPTd4OB?=
PBMC NHPCWmtHfW6ldHnvckBCe3OjeR?= M3nNcFE2KG2rbh?= NEX3WVFFVVOR MW\Jcohq[mm2czD0bIUhemWuZXHz[UBw\iCrboTldoxmfWurbj2xMYJmfGFid3n0bEBKSzVyIH;mJFAvODN5IN88US=> MVOxNlM3OTN7Nh?=
SW1353 NXLTN21TTnWwY4Tpc44hSXO|YYm= NV[yTolIOSCq NHvibJhFVVOR NX;tR3hQUW6qaXLpeJMhUUxvNjDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iByLkC1JO69VQ>? MVGxNVE1ODd2MR?=
Hela MmrHSpVv[3Srb36gRZN{[Xl? MYjEUXNQ NULre4RMUW6qaXLpeJMhXGG2LXnu[JVk\WRiSFnWNUBNXFJidILhcpNi[3SrdnH0bY9vKGmwIHj1cYFvKEinTHGgZ4VtdHNid3n0bEBKSzVyIH;mJFAvOSEQvF2= MYexPFkzPjdzMR?=
PC12 MkDRSpVv[3Srb36gRZN{[Xl? NW\UfnZLOTBizszN MXnEUXNQ NH[xUG5C[3SrdnH0[ZMhVnKoMj;BVmUhcW5icnH0JHBEOTJiY3XscJMh[XO|ZYPz[YQh[XNiSF:tNUBxem:2ZXnuJIlv\HWldHnvci=> MnLqNlE{PDV4OEW=
RAW 264.7 M3HHRWN6fG:2b4jpZ{BCe3OjeR?= MWmxNk42KM7:TR?= M4HN[|EzcA>? NV\H[VF3TE2VTx?= M{\jfWJtd2OtczDs[ZRp[WxidH;4bY4udWWmaXH0[YQh[3m2b4TvfIlkcXS7 NF\USI8yPzR6NUWwOC=>
HCA2 MX7GeY5kfGmxbjDBd5NigQ>? NG\6d|kzNjVizszN MmnkTY5pcWKrdIOgdFM5KG2nZHnheIVlKE2NMjDhZ5RqfmG2aX;u NIfoVFkyPzl4NEe4NC=>
U937 MWLGeY5kfGmxbjDBd5NigQ>? M{LS[WlvcGmkaYTzJGpCUy2vZXTpZZRm\CCrboTldoZmem:wLXfhcY1iN2GwaYPvcZlkcW5vaX7keYNm\CCVdHH0NUBxcG:|cHjvdplt[XSrb36= NWi3elNQOThzNUexNlI>
U937 M{jLO2Z2dmO2aX;uJGF{e2G7 NUG2VHlEUW6qaXLpeJMhUkGNLX3l[IlifGWmIHnueIVz\mW{b36t[4FudWFxYX7pd49ugWOrbj3pcoR2[2WmIICzPEBxcG:|cHjvdplt[XSrb36= NFrxOHEyQDF3N{GyNi=>
hESCs MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXHOUDPxE1? M3TKdWROW09? MWnJcoR2[2W|IHPhdoRqd227b3flcolkKGGldHn2bZR6KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4To NYfESZhMOjN4MEKzPVk>
RAW264.7 M4DtbmZ2dmO2aX;uJGF{e2G7 NYe4TGcyOTBizszN M4qzemlv\HWlZYOgZY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDifUBqdmirYnn0bY5oKEmOLUJOtkBz\WynYYPl NUDTOlk5OjN5OUGwO|g>
RAW264.7 Mm[ySpVv[3Srb36gRZN{[Xl? NEnySlQyOCEQvF2= NFG4SmpKdmS3Y3XzJIFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZpkhcW6qaXLpeIlv\yCrTl;TJJJmdGWjc3W= NFfjSIIzOzd7MUC3PC=>
RAW264.7 MU\GeY5kfGmxbjDBd5NigQ>? MnXBNVAh|ryP MlW4TY5lfWOnczDhcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHL5JIlvcGmkaYTpcochVk9icnXs[YF{\Q>? MVuyN|c6OTB5OB?=
RAW264.7 MWPGeY5kfGmxbjDBd5NigQ>? MWKxNEDPxE1? NVOw[4ZrUW6qaXLpeJMhVFCVLXnu[JVk\WRicEO4JG1CWEticHjvd5Bpd3K7bHH0bY9v MXiyOFAyPjB3Nx?=
IEC-18 M2KybWZ2dmO2aX;uJGF{e2G7 NXLJdmZDOTBizszN MV7Jcohq[mm2czDMVHMucW6mdXPl[EBxOzhiTVHQT{BxcG:|cHjvdplt[XSrb36= NWTmPGdOOjN5NUixNVA>

... 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]
- Collapse

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]
- Collapse
  • 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]
- Collapse
  • 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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field
selleck catalog

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

  • Pan p38 MAPK Inhibitor

    SB202190 (FHPI) : Pan-p38α/β inhibitor, IC50=50 nM/100 nM.

  • Most Potent p38 MAPK Inhibitor

    Skepinone-L New : p38α-MAPK, IC50=5 nM.

  • p38 MAPK Inhibitor in Clinical Trial

    PH-797804 : Phase II for Chronic Obstructive Pulmonary Disease (COPD).

  • Newest p38 MAPK Inhibitor

    Skepinone-L New : Selective p38α-MAPK inhibitor with IC50 of 5 nM.

Related p38 MAPK Products

  • Pexmetinib (ARRY-614) New

    Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.

  • SB239063 New

    SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.

  • Ravoxertinib (GDC-0994) New

    Ravoxertinib (GDC-0994) is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.

  • Doramapimod (BIRB 796)

    Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

    Features:The first p38 MAPK inhibitor to be tested in a phase III clinical trial.

  • SB202190 (FHPI)

    SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.

  • Ralimetinib dimesylate

    Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.

  • Losmapimod (GW856553X)

    Losmapimod (GW856553X, GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively. P38 MAPKs are involved in cell differentiation, apoptosis and autophagy. Phase 3.

  • PH-797804

    PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.

  • VX-702

    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

    Features:Highly selective, orally active inhibitor of p38 MAPK.

  • TAK-715

    TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

Tags: buy SB203580 | SB203580 supplier | purchase SB203580 | SB203580 cost | SB203580 manufacturer | order SB203580 | SB203580 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID