1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
    Mitophagy
  3. SB 203580

SB 203580 (Synonyms: RWJ 64809)

Cat. No.: HY-10256 Purity: 99.92%
Handling Instructions

SB 203580 (RWJ 64809) is a widely used p38 MAPK inhibitor with an IC50 of 0.3-0.5 μM. SB 203580 (RWJ 64809) shows more than 100-fold selectivity over Akt (PKB), LCK, and GSK-3β.

For research use only. We do not sell to patients.

SB 203580 Chemical Structure

SB 203580 Chemical Structure

CAS No. : 152121-47-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
50 mg USD 96 In-stock
Estimated Time of Arrival: December 31
100 mg USD 144 In-stock
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Customer Review

Based on 110 publication(s) in Google Scholar

Other Forms of SB 203580:

Top Publications Citing Use of Products

Customer Validation

    SB 203580 purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    SB 203580 purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.

    LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

    SB 203580 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    SB 203580 purchased from MCE. Usage Cited in: Chin Arch Otolaryngol Head Neck Surg. 2016,23(01):49-52.

    Effect of p38MAPK inhibitor on the soft palate reconstruction of the rats with chronic intermittent hypoxia.

    SB 203580 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SB203580 (a P38 inhibitor, 20 μM) for 1 h, followed by exposure to CPS (100 ng/mL) or MO (MOI = 30) for 48 h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    SB 203580 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    SB 203580 purchased from MCE. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.

    Immunofluorescence analysis for expression of the I-cell marker ΔNP63 on proximal sections of ureters explanted from E12.5 wildtype (control) embryos and cultured for 6 d in the presence of solvent (DMSO) (A), the AKT inhibitor (AKT-i) MK2206 (B), the P38 inhibitor (P38-i) SB203580 (C), the ERK1/2 inhibitor (ERK1/2-i) PD98059 (D) or combinations as indicated (E and F).

    SB 203580 purchased from MCE. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68.

    The involvement of the p38 MAPK signaling pathways in lactoferrin-induced differentiation of HaCaT keratinocytes. HaCaT cells are differentiated in the presence or absence of 10 μM bovine Lactoferrin for 5 days. PD98059 (40 μM), SB203580 (10 μM), or LY294002 (10 μM) are added at the same time. Cell differentiation is evaluated by the expression levels of Involucrin and Filaggrin. GAPDH is used as a loading control.

    SB 203580 purchased from MCE. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2).

    P38 inhibitor SB203580 pretreatment also decreases p-HSP27 and MMP9 levels induced by MICAL2-overexpression.

    SB 203580 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.

    Cells are pre-treated with ERK (U1026) and p38 (SB203580) inhibitors, followed by GL-V9 treatment for 24 h. Western blot is performed to analyze NAG-1 expression.

    SB 203580 purchased from MCE. Usage Cited in: Int J Clin Exp Med. 2017;10(9):13542-13549.

    SB203580 decreases the expression ratio of p-p38 and p38 to inhibit activation of p38 MARK pathway.

    SB 203580 purchased from MCE. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983.

    Representative western blot analysis of P-gp, p38 MAPK and phospho-p38 MAPK expression in MCF-7/MDR and K562/MDR cells treated with 10 μM SB203580 for 48 hr.

    SB 203580 purchased from MCE. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    SB 203580 purchased from MCE. Usage Cited in: J Endod. 2018 May;44(5):751-758.

    p38 MAPK inhibition enhances DPC-Exos–induced tube formation. (A) p38 MAPK activity is measured by detecting Phospho-p38 MAPK. The ratio between Phospho-p38 MAPK and the p38 MAPK band is used for quantification. (B) The effects of VEGF-A and KDR expression after p38 MAPK inhibitor SB203580 treatment on DPC-Exos-stimulated HUVECs.

    SB 203580 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018 Apr 25;46(5):1779-1792.

    Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

    SB 203580 purchased from MCE. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235.

    Western blot analysis shows that inhibiting MAPK cannot completely reverse increased expression of RNF2 and CDDP resistance of OC cells.

    SB 203580 purchased from MCE. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225.

    Representative western blots of p-CREB (Ser133) and UCP-1 in iWAT from C57BL/6J mice after 4 wk of SB203580 treatment. These mice are exposed to cold for 2 d before analysis.

    SB 203580 purchased from MCE. Usage Cited in: Biomaterials. 2018 Aug;175:19-29.

    Western blotting analysis showing the related protein expression (MHC, MyoD, p38α, phospho-p38α) of C2C12 myoblasts after incubated for 6 days in DM containing 40 μg/mL AuNPs and Au-AgNPs in the presence or absence of SB203580 (SB).

    SB 203580 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459.

    Western blot results show a reduction in phosphorylated p38 MAPK in ADSCs after treatment with 20 μM SB203580, 20 μM SP600125, or 20 μM PD98059 for 1 hour.

    SB 203580 purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.

    HepG2 cells are pre-incubated with 20 µM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20µM) for 24 h.

    SB 203580 purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.

    Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

    SB 203580 purchased from MCE. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450.

    Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

    SB 203580 purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467.

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

    SB 203580 purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    SB 203580 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    SB 203580 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SB 203580 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    SB 203580 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SB 203580 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SB 203580 purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    SB 203580 purchased from MCE. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.

    P-p38 and P-Hsp27 are detected by western blotting with the treatment of LPS, SB203580 and SB203580+ LPS.

    SB 203580 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Dec 2.

    Western analysis of protein expression in the treatment of miR-543 and SB 203580.

    SB 203580 purchased from MCE. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.

    Neutrophils are pretreated with inhibitor of p38 MAPK (SB203580) and ERK1/2 (U0126), and the cells are then incubated with either SS2 ZY05719 or PMA for 3 h. Immunofluorescence is performed.

    SB 203580 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SB 203580 (RWJ 64809) is a widely used p38 MAPK inhibitor with an IC50 of 0.3-0.5 μM. SB 203580 (RWJ 64809) shows more than 100-fold selectivity over Akt (PKB), LCK, and GSK-3β.

    IC50 & Target[1]

    p38 MAP kinase

    0.3-0.5 μM (IC50, in IL-2-stimulated T cells)

    PKB

    3-5 μM (IC50)

    Autophagy

     

    Mitophagy

     

    In Vitro

    SB 203580 inhibits IL-2-driven T cell proliferation with an IC50 of 3-5 μM, SB 203580 is able to inhibit the activity of PDK1 in a dose-dependent manner with an IC50 in the 3-10 μM range[1].
    SB 203580 at a concentration of 1 μM is sufficient for inhibiting p38 kinase activity in TF-1 cells. SB 203580 at 5 and 10 μM enhances NF-κB-mediated gene transcription independently of phosphorylation on the transactivation domains of the p65 subunit. SB203580-mediated increase in NF-κB transcriptional activity is associated with enhanced phosphorylation of ERK1/2 and c-Jun N-terminal kinase (JNK), but not p38 kinase[2].
    SB203580 treatment does not decrease the phosphorylation of p38 MAPK, but it significantly reduces the phosphorylation of MAPKAPK2, HSP27, and ATF2[4].

    In Vivo

    All animals challenged with NS (noninfected controls) and treated with either SB203580 or placebo survive. Compared with placebo, pretreatment with the highest dose of SB203580 (100 mg/kg) 1 hour before E. coli increases the hazards ratio of death. With E. coli, compared with placebo, at 48 hours, but not 24 hours, low and high dose SB203580 decrease phosphorylated p38 MAPK and the ratio of phosphorylated to total p38. High dose SB203580 decreases lung neutrophils on histology at 24 hours in a trend approaching significance (p = 0.09) and increases them significantly at 48 hours (p = 0.01) in patterns different over time[3]. SB 203580 is evaluated in several models of cytokine inhibition and inflammatory disease. It is demonstrated clearly to be a potent inhibitor of inflammatory cytokine production in both mice and rats with IC50 values of 15 to 25 mg/kg[4].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (264.95 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6495 mL 13.2475 mL 26.4950 mL
    5 mM 0.5299 mL 2.6495 mL 5.2990 mL
    10 mM 0.2649 mL 1.3247 mL 2.6495 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    Phosphorylation of p38, JNK1/2, and ERK1/2 is analysed by Western blotting. Briefly, TF-1 cells are cultured for 16 h in RPMI 1640 containing 0.1% FBS and subsequently stimulated for various periods of time with medium or OA (30 ng/mL) or SB 203580(1 μM, 5 μM, 10 μM) plus OA. After harvesting, total cell extracts are prepared by resuspending the cells in 500 μL 1× sample buffer (containing 2% SDS, 10% glycerol, 2% β-mercaptoethanol, 60 mM Tris-HCl (pH 6.8) and bromophenol blue) and lysing the cells by passing them through a 23G1 needle (three times). Cell extracts are directly boiled for 10 min and stored at -20°C. Before loading, samples are again boiled for 5 min and cell extracts are resolved by running 1/10th volume on a SDS/12.5%PAGE gel (acryla-mide:bisacrylamide is 173:1) and transferred to cellulosenitrate membrane. Immunoblotting with the antibodies is performed by standard procedures and detection is performed[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3]

    Mice[3]
    In survival studies, C57BL/6J mice weighing 20 g to 30 g are challenged with 0.05 mL of IT normal saline (NS, noninfected controls) or E. coli (15 × 109 CFU/kg). One hour before NS challenge, mice (n = 24) receive either intraperitoneal SB203580 (100 mg/kg in 0.25 mL) or diluent only (placebo).
    Infected animals receive SB203580 in doses of 100, 10, 1, or 0.1 mg/kg or placebo 1 hour before IT E. coli (n = 241); SB203580 100 or 0.1 mg/kg or placebo 1 hour after E. coli (n = 121); or SB203580 100 mg/kg or placebo 12 hours after E. coli (n = 72). Animals are observed every 2 hours for the initial 48 hours, every 4 hours from 48 hours to 72 hours, every 8 hours from 72 hours to 96 hours, and then twice daily until study completion (168 hours)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    377.43

    Formula

    C₂₁H₁₆FN₃OS

    CAS No.

    152121-47-6

    SMILES

    O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C

    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.92%

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    Product Name:
    SB 203580
    Cat. No.:
    HY-10256
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    SB 203580

    Cat. No.: HY-10256