SB203580

Catalog No.S1076 Synonyms: RWJ 64809, PB 203580

SB203580 Chemical Structure

Molecular Weight(MW): 377.43

SB203580 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.

Size Price Stock Quantity  
USD 147 In stock
USD 270 In stock
USD 370 In stock
USD 470 In stock

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

Cited by 48 Publications

3 Customer Reviews

  • A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).

     

     

    J Biol Chem 2010 285, 32824-32833. SB203580 purchased from Selleck.

    A, effect of p38 MAPK inhibitor SB203580 (1, 5, and 10 μM) on SRP72 phosphorylation was evaluated. Jurkat cells were stimulated with rhIL-1, harvested at 0, 120, and 240 min, lysed, and immunoprecipitated using anti-human SRP19 andWBusing anti-phosphoserine antibodies. A decreased intensity of SRP72 band was found when using the inhibitor at concentration of 1μM at 240 min and 5 and 10 μM at 120 and 240 min. B, results were analyzed and RUA illustrated, finding significant results at 1 μM 240 versus 120, 5, and 10 μM at 120 versus 0 and 240 versus 0 min *, p<0.05.

    J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.

  • We used real time RT-PCR to investigate the effects of SB203580 on SRP72 mRNA expression. All the samples were treated under the same experimental conditions used in protein tests done by WB, and phosphorylation was measured indirectly by IP-WB. The results did not show significant changes on the mRNA expression of SRP72 after the treatment with these inhibitors.

    J Biol Chem 2010 285, 32824–32833. SB203580 purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description SB203580 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.
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 NUfqb|dVU2mwYYPlJGF{e2G7 NFLVcW0yOCEQvF2= NUfFWVVjOTVibXnu MnnWTY5pcWKrdIOgdFM5KE2DUDDrbY5ie2Vid3n0bEBKSzVyIH;mJFAvPiEQvF2= M2LBd|c4PTB3N{e=
THP-1 MXXGeY5kfGmxbjDBd5NigQ>? MmjrTY5pcWKrdIOgUHBUNWmwZIXj[YQhXE6IYXzwbIEheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4yPiEQvF2= M2rFfFE5OzJ3N{[4
PBMC NEDQNI5HfW6ldHnvckBCe3OjeR?= MYSxOUBucW5? MnvSSG1UVw>? M2TzO2lvcGmkaYTzJJRp\SC{ZXzlZZNmKG:oIHnueIVzdGW3a3nuMVEu[mW2YTD3bZRpKEmFNUCgc4YhOC5yM{eg{txO NFTLb3oyOjN4MUO5Oi=>
SW1353 MkOySpVv[3Srb36gRZN{[Xl? NWfMOIF6OSCq M4HKRmROW09? M3vRfWlvcGmkaYTzJGlNNTZicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOC5yNTFOwG0> MWKxNVE1ODd2MR?=
Hela NHLYOIhHfW6ldHnvckBCe3OjeR?= NG\TNVZFVVOR NF73[ZdKdmirYnn0d{BV[XRvaX7keYNm\CCKSW[xJGxVWiC2cnHud4FkfGm4YYTpc44hcW5iaIXtZY4hUGWOYTDj[YxteyC5aYToJGlEPTBib3[gNE4yKM7:TR?= MVyxPFkzPjdzMR?=
PC12 MXvGeY5kfGmxbjDBd5NigQ>? MWexNEDPxE1? NUPqOY8zTE2VTx?= M13OfWFkfGm4YYTld{BPemZ{L1HSSUBqdiC{YYSgVGMyOiClZXzsd{Bie3Onc4Pl[EBieyCKTz2xJJBzd3SnaX6gbY5lfWO2aX;u NVvCbHJZOjF|NEW2PFU>
RAW 264.7 NV3j[GhmS3m2b4TvfIlkKEG|c3H5 MUixNk42KM7:TR?= MXixNog> Mkf4SG1UVw>? MWHCcI9kc3NibHX0bIFtKHSxeHnuMY1m\GmjdHXkJIN6fG:2b4jpZ4l1gQ>? NF2xc4cyPzR6NUWwOC=>
HCA2 MkPpSpVv[3Srb36gRZN{[Xl? M37CblIvPSEQvF2= NX\NbGFWUW6qaXLpeJMheDN6IH3l[IlifGWmIF3LNkBi[3SrdnH0bY9v M4HzdVE4QTZ2N{iw
U937 MVrGeY5kfGmxbjDBd5NigQ>? MVrJcohq[mm2czDKRWsudWWmaXH0[YQhcW62ZYLm[ZJwdi2pYX3tZU9idmm|b335Z4lvNWmwZIXj[YQhW3SjdEGgdIhwe3Cqb4L5cIF1cW:w MnrLNVgyPTdzMkK=
U937 M3nTc2Z2dmO2aX;uJGF{e2G7 NYTDcWV2UW6qaXLpeJMhUkGNLX3l[IlifGWmIHnueIVz\mW{b36t[4FudWFxYX7pd49ugWOrbj3pcoR2[2WmIICzPEBxcG:|cHjvdplt[XSrb36= M1TrZlE5OTV5MUKy
hESCs NVj6SWR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfTN2c2KM7:TR?= NIfnOYRFVVOR MoW1TY5lfWOnczDjZZJlcW:veX;n[Y5q[yCjY4Tpeol1gSCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bC=> NGTHcWEzOzZyMkO5PS=>
RAW264.7 NF7TVVJHfW6ldHnvckBCe3OjeR?= NWnrSFlQOTBizszN NYHtS4VGUW6mdXPld{BidnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIJ6KGmwaHnibZRqdmdiSVytNe6zKHKnbHXhd4U> NHn3VZozOzd7MUC3PC=>
RAW264.7 NXyzUYc4TnWwY4Tpc44hSXO|YYm= NH72SlUyOCEQvF2= M13NN2lv\HWlZYOgZY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDifUBqdmirYnn0bY5oKGmQT2OgdoVt\WG|ZR?= MU[yN|c6OTB5OB?=
RAW264.7 MV;GeY5kfGmxbjDBd5NigQ>? NWPSWHN4OTBizszN MX7JcoR2[2W|IHHueIlqdm[uYX3tZZRwenliYXP0bZZqfHliYomgbY5pcWKrdHnu[{BPVyC{ZXzlZZNm NHLXfJUzOzd7MUC3PC=>
RAW264.7 NEnzSlZHfW6ldHnvckBCe3OjeR?= MlO3NVAh|ryP NEi2ToFKdmirYnn0d{BNWFNvaX7keYNm\CCyM{igUWFRUyCyaH;zdIhwenmuYYTpc44> MUSyOFAyPjB3Nx?=
IEC-18 MlvnSpVv[3Srb36gRZN{[Xl? M33YTFExKM7:TR?= NFTJRmFKdmirYnn0d{BNWFNvaX7keYNm\CCyM{igUWFRUyCyaH;zdIhwenmuYYTpc44> NYTSclllOjN5NUixNVA>

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Systemic lupus erythematosus (SLE) are established in female MRL/lpr mice and female C57BL/6 mice
  • Formulation: Dissolved in drinking water (250 μM)
  • Dosages: 0.1 M/day
  • Administration: Orally administered
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 43 mg/mL (113.92 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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
Synonyms RWJ 64809, PB 203580

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 (g) = Concentration (mol/L) × Volume (L) × 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

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

Related p38 MAPK Products

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