SB203580

Catalog No.S1076

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.

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SB203580 Chemical Structure

SB203580 Chemical Structure
Molecular Weight: 377.43

Validation & Quality Control

Cited by 48 publications:

3 customer reviews :

Quality Control & MSDS

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Product Information

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  • Research Area
  • Inhibition Profile
  • SB203580 Mechanism

Product Description

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.
Targets p38 MAPK [1]
(THP-1 cells)
PKB [1]
(THP-1 cells)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
PC12Mlf3T4lv[XOnIFHzd4F6MXexNEDPxE1?NUjXUVJTOTVibXnuM{fFO2lvcGmkaYTzJJA{QCCPQWCgb4lv[XOnIIfpeIghUUN3MDDv[kAxNjZizszNMVe3O|UxPTd5
THP-1MUHGeY5kfGmxbjDBd5NigQ>?NVvGcW5LUW6qaXLpeJMhVFCVLXnu[JVk\WRiVF7GZYxxcGFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOC5zNjFOwG0>MUKxPFMzPTd4OB?=
PBMCM2nGNmZ2dmO2aX;uJGF{e2G7NEPMdpEyPSCvaX6=MVvEUXNQMoXrTY5pcWKrdIOgeIhmKHKnbHXhd4Uhd2ZiaX70[ZJt\XWtaX6tNU1j\XSjIIfpeIghUUN3MDDv[kAxNjB|NzFOwG0>NVXzUVNpOTJ|NkGzPVY>
SW1353NWr1TXdQTnWwY4Tpc44hSXO|YYm=MmrNNUBpMUnEUXNQMn[0TY5pcWKrdIOgTWwuPiCycn;keYN1cW:wIIfpeIghUUN3MDDv[kAxNjB3IN88US=>MV[xNVE1ODd2MR?=
HelaM4jOeGZ2dmO2aX;uJGF{e2G7MW\EUXNQNUD4foxqUW6qaXLpeJMhXGG2LXnu[JVk\WRiSFnWNUBNXFJidILhcpNi[3SrdnH0bY9vKGmwIHj1cYFvKEinTHGgZ4VtdHNid3n0bEBKSzVyIH;mJFAvOSEQvF2=Mn3SNVg6OjZ5MUG=
PC12MVHGeY5kfGmxbjDBd5NigQ>?MlvTNVAh|ryPMUPEUXNQMmTQRYN1cX[jdHXzJG5z\jJxQWLFJIlvKHKjdDDQR|EzKGOnbHzzJIF{e2W|c3XkJIF{KEiRLUGgdJJwfGWrbjDpcoR2[3Srb36=M4LYNFIyOzR3Nki1
RAW 264.7Mo\vR5l1d3SxeHnjJGF{e2G7MkHENVIvPSEQvF2=NUHHXm1EOTKqNUfx[IlzTE2VTx?=M2fHeWJtd2OtczDs[ZRp[WxidH;4bY4udWWmaXH0[YQh[3m2b4TvfIlkcXS7M4LReVE4PDh3NUC0
HCA2Mn;nSpVv[3Srb36gRZN{[Xl?MnfKNk42KM7:TR?=MVLJcohq[mm2czDwN|ghdWWmaXH0[YQhVUt{IHHjeIl3[XSrb36=M3j6TFE4QTZ2N{iw
U937NEHJXlZHfW6ldHnvckBCe3OjeR?=MXfJcohq[mm2czDKRWsudWWmaXH0[YQhcW62ZYLm[ZJwdi2pYX3tZU9idmm|b335Z4lvNWmwZIXj[YQhW3SjdEGgdIhwe3Cqb4L5cIF1cW:wMUOxPFE2PzF{Mh?=
U937M2LO[WZ2dmO2aX;uJGF{e2G7MYPJcohq[mm2czDKRWsudWWmaXH0[YQhcW62ZYLm[ZJwdi2pYX3tZU9idmm|b335Z4lvNWmwZIXj[YQheDN6IIDoc5NxcG:{eXzheIlwdg>?NGHVUG0yQDF3N{GyNi=>
hESCsMWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUnObHljPSEQvF2=NHvPOmdFVVORNEXo[JJKdmS3Y3XzJINiemSrb335c4dmdmmlIHHjeIl3cXS7IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpM1;xN|I{PjB{M{m5
RAW264.7M4SzVGZ2dmO2aX;uJGF{e2G7NUfK[HZ1OTBizszNNHTqT2tKdmS3Y3XzJIFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZpkhcW6qaXLpeIlv\yCLTD2x{tIhemWuZXHz[S=>M{nJVVI{PzlzMEe4
RAW264.7NFPRPG5HfW6ldHnvckBCe3OjeR?=M3j5dlExKM7:TR?=MkDZTY5lfWOnczDhcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHL5JIlvcGmkaYTpcochcU6RUzDy[Yxm[XOnNVe0THZoOjN5OUGwO|g>
RAW264.7NGCxTVFHfW6ldHnvckBCe3OjeR?=MXmxNEDPxE1?NHXzNZBKdmS3Y3XzJIFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZpkhcW6qaXLpeIlv\yCQTzDy[Yxm[XOnM2P3O|I{PzlzMEe4
RAW264.7NXzPU3JwTnWwY4Tpc44hSXO|YYm=MV2xNEDPxE1?NUSxcIw6UW6qaXLpeJMhVFCVLXnu[JVk\WRicEO4JG1CWEticHjvd5Bpd3K7bHH0bY9vMXqyOFAyPjB3Nx?=
IEC-18MYjGeY5kfGmxbjDBd5NigQ>?NUTCOGJ[OTBizszNNHPDNXRKdmirYnn0d{BNWFNvaX7keYNm\CCyM{igUWFRUyCyaH;zdIhwenmuYYTpc44>NWPxV25JOjN5NUixNVA>

... 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]
Features First reported p38 inhibitor.

Protocol(Only for Reference)

Kinase Assay:

[1]

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 Assay:

[1]

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.

Animal Study:

[5]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.

[2] Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.

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Chemical Information

Download SB203580 SDF
Molecular Weight (MW) 377.43
Formula

C21H16FN3OS

CAS No. 152121-47-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms RWJ 64809, PB 203580
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 Name 4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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