1. MAPK/ERK Pathway
    PI3K/Akt/mTOR
    Autophagy
  2. p38 MAPK
    Akt
    Autophagy
    Mitophagy

SB 203580 (Synonyms: RWJ 64809)

Cat. No.: HY-10256 Purity: 99.54%
Handling Instructions

SB 203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM, also blocks PKB phosphorylation with IC50 of 3-5 μM.

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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10 mM * 1 mL in DMSO USD 66 In-stock
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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

Other Forms of SB 203580:

Customer Validation

    SB 203580 purchased from MCE. Usage Cited in: Mol Immunol. 2017 May 4;87:161-170.

    Effect of TLR2 on autophagy activation via p38 signaling pathway in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA is then infected with MG for 30 min prior to SB203580. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot. The GAPDH level is used as the internal standard.

    SB 203580 purchased from MCE. Usage Cited in: Mol Immunol. 2017 May 4;87:161-170.

    Effect of TLR2 on autophagy activation via ERK1/2 signaling pathway activation in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA is then infected with MG for 30 min prior to PD98059. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot.

    SB 203580 purchased from MCE. Usage Cited in: Mol Immunol. 2017 May 4;87:161-170.

    Effect of TLR2 on autophagy activation via ERK signaling pathway in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA are infected with MG for 30 min prior to SP600125. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot. The GAPDH level was used as the internal standard.

    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: Elife. 2016 Apr 11;5. pii: e14087.

    Fbxo21-/- RAW264.7 cells are transfected with indicated amounts (0, 1 or 5 μg) Fbxo21-Myc and equal amounts of K29O-Ub-HA vectors for 48 hr, and then infected with VSV (MOI = 1) or HSV-1 (MOI = 5) for 2 hr in the presence or absence of MLN-4924 (10 nM). Then polyubiquitinated ASK1 is examined by immunoblot (IB) against HA after immuneprecipitations (IP).

    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 Jan, 23(1).

    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 U0126 (an ERK1/2 inhibitor, 10 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: 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 SP600125 (a JNK 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: 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: Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128.

    Osthole attenuates the phosphorylation of p38 in TNBS-induced colitis. Mice receive Osthole intraperitoneally at 100 mg/kg once daily starting at three days before being exposed to TNBS treatments and until the end of the experiments. Colitis is induced by infusing a 100 μL enema of TNBS (2.8 mg) in 50% ethanol into the colonic lumen. Western blot analysis of the colonic mucosa homogenates is performed 2 d after the initial rectal TNBS administration.

    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 Jul 9;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: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    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: Phytomedicine. 2018 Mar 15;42:152-163.

    Cells are pretreated with SP600125 (20μM), SB203580 (20μM) or U0126 (20μM) in presence or absence of Khayandirobilide A (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: Cell Physiol Biochem. 2018 Apr 25;46(5):1779-1792.

    Western blot and quantitative analysis of the expressions of ZO-1, Claudin-1, and Occludin. Apoptosis inhibitor Z-VAD(OMe)-FMK is used.

    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: 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: Int J Cancer. 2018 Aug 1;143(3):645-656.

    Evaluation of protein expression change of Notch receptors response to the treatment of 10 μM Enzalutamide as an androgen receptor (AR) antagonist.

    SB 203580 purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656.

    Evaluation of expression change of Notch downstream under the androgen-deprived condition with or without the treatment of DAPT by western blot assay.

    SB 203580 purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Jul 16.

    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 Sep 4.

    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. 2018 Sep 27:fj201800935RR.

    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 Sep 6.

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SB 203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM, also blocks PKB phosphorylation with IC50 of 3-5 μM.

    IC50 & Target[1]

    p38 MAP kinase

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

    PKB

    3-5 μM (IC50, in IL-2-stimulated T cells)

    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. SB 203580 at 10 μM enhances phosphorylation of ERK1/2 and JNK[1].

    In Vivo

    SB 203580 decreases protein concentrations of IL-1β from 106.49±10.93 to 67.85±7.39 pg/mL and TNF-α from 462.54±50.16 to 252.71±44.03 pg/mL. Similarly, the protein levels of MMP-2 and MMP-9 are significantly lower in the SB 203580 than the EM group. After treatment with SB 203580, the protein levels of MMP-2 and MMP-9 decreases from 2.70±0.14 to 1.74±0.26 ng/mL and from 3.17±0.31 to 1.98±0.24 ng/mL, respectively[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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 33 mg/mL (87.43 mM)

    *"≥" means soluble, but saturation unknown.

    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.

      SB 203580 is dissolved in 1% DMSO at 1 mg/mL[5].

    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]
    Thirty female BALB/c mice with experimentally induced EM are randomly divided into two groups. The first group is designated as the study group (SB 203580 group, n=15), which is injected i.p. with SB 203580 at a dose of 1 μg/mg on a daily basis (this dose is established in a pre-test). The second group is the positive control group (EM group, n=15), which received no medication except i.p. injection of isotonic saline solution (volume equal to that of SB 203580). The sham-operated mice served as the negative controls (sham-operated group, n=15), which received no medication but did have an i.p. injection of isotonic saline solution (volume equal to that of SB 203580). The injection of vehicle or SB 203580 started 3 days before injection of the endometrial fragments (in SB 203580 and EM groups) or the PBS (in sham-operated group) and lasted for 24 days. Then, the mice are sacrificed by cervical dislocation on the day of the last injection and surgical procedures are performed under aseptic conditions.

    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.54%

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

    Cat. No.: HY-10256