1. Stem Cell/Wnt MAPK/ERK Pathway Autophagy
  2. Organoid p38 MAPK Autophagy Mitophagy
  3. Adezmapimod

Adezmapimod  (Synonyms: SB 203580; RWJ 64809)

Cat. No.: HY-10256 Purity: 99.96%
COA Handling Instructions

SB 203580 (RWJ 64809) est un inhibiteur sélectif et ATP-compétitif de p38 MAPK avec des IC50 de 50 nM et 500 nM pour SAPK2a/p38 et SAPK2b/p38β2, respectivement. SB 203580 inhibe les LCK, GSK3β et PKBα avec des IC50 de 100 à 500 fois plus élevées que celles de SAPK2a/p38. SB 203580 ne perturbe pas l'activité de JNK et SB 203580 est un activateur de l'autophagie et de la mitophagie.

Adezmapimod (SB 203580) ist ein selektiver und ATP-kompetitiver p38 MAPK-Inhibitor mit IC50 von 50 nM und 500 nM für SAPK2a/p38 and SAPK2b/p38β2. Adezmapimod hemmt LCK, GSK3β und PKBα mit IC50s von 100-500-fach höher als die für SAPK2a/p38. Adezmapimod stört die JNK-Aktivität nicht und ist ein autophagy- und mitophagy-Aktivator.

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.

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

Adezmapimod Chemical Structure

Adezmapimod Chemical Structure

CAS No. : 152121-47-6

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Customer Review

Based on 488 publication(s) in Google Scholar

Other Forms of Adezmapimod:

Top Publications Citing Use of Products

454 Publications Citing Use of MCE Adezmapimod

IF
WB
IHC

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomaterials. 2018 Aug;175:19-29.  [Abstract]

    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).

    Adezmapimod purchased from MedChemExpress. Usage Cited in: PLoS Biol. 2018 May 11;16(5):e2004225.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Dec 7;9:2854.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Acta Physiol (Oxf). 2018 Feb;222(2).  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Am J Physiol Cell Physiol. 2018 Aug 1;315(2):C225-C235.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5450-5467.  [Abstract]

    Treatment with SB203580 significantly abolishes siPlectin-stimulated p38 activation.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Feb;33(2):2435-2450.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Endod. 2018 May;44(5):751-758.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Nov;119(10):8450-8459.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Cell Biochem. 2018 Dec 2.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: BMC Pulm Med. 2018 Nov 27;18(1):178.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.  [Abstract]

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

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2017 Nov;112:49-59.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Hum Mol Genet. 2017 Sep 15;26(18):3553-3563.  [Abstract]

    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).

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biochem Cell Biol. 2017 Feb;95(1):64-68.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

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

    Adezmapimod purchased from MedChemExpress. 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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

    The Western blot analysis of HOG1 and Phospho-HOG1.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Oct 19;8(60):101965-101983.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    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.

    Adezmapimod purchased from MedChemExpress. 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.

    Adezmapimod purchased from MedChemExpress. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    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.

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator[1].

    IC50 & Target[1]

    p38

    50 nM (IC50)

    p38β2

    500 nM (IC50)

    In Vitro

    Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents 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[1].
    SB203580 blocks PKB phosphorylation (IC50 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[1].

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

    Cell Proliferation Assay[1]

    Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
    Result: Prevented 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.

    Western Blot Analysis[1]

    Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells
    Concentration: 0-30 μM
    Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
    Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.
    In Vivo

    Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[1].

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

    Animal Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors[1]
    Dosage: 5 mg/kg/day
    Administration: Intra peritoneal injected daily for 16 consecutive days
    Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).
    Molecular Weight

    377.43

    Formula

    C21H16FN3OS

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    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.

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

    DMSO : 20 mg/mL (52.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

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

    • Protocol 2

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

      Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (26.49 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6495 mL 13.2475 mL 26.4950 mL 66.2374 mL
    5 mM 0.5299 mL 2.6495 mL 5.2990 mL 13.2475 mL
    10 mM 0.2649 mL 1.3247 mL 2.6495 mL 6.6237 mL
    15 mM 0.1766 mL 0.8832 mL 1.7663 mL 4.4158 mL
    20 mM 0.1325 mL 0.6624 mL 1.3247 mL 3.3119 mL
    25 mM 0.1060 mL 0.5299 mL 1.0598 mL 2.6495 mL
    30 mM 0.0883 mL 0.4416 mL 0.8832 mL 2.2079 mL
    40 mM 0.0662 mL 0.3312 mL 0.6624 mL 1.6559 mL
    50 mM 0.0530 mL 0.2649 mL 0.5299 mL 1.3247 mL
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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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