Home Tools

Adezmapimod

Catalog No. T1764 CAS 152121-47-6

Synonyms: PB 203580, RWJ 64809, SB203580

Adezmapimod (SB 203580) is a p38 MAPK inhibitor (IC50=0.3-0.5 μM) that is selective and ATP-competitive. Adezmapimod possesses autophagy and mitochondrial autophagy activating activity. Adezmapimod displays more than 100-fold higher selectivity than PKB, LCK, and GSK-3β.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Adezmapimod, CAS 152121-47-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
50 mg	In stock	$ 64.00
100 mg	In stock	$ 100.00
200 mg	In stock	$ 173.00
500 mg	In stock	$ 292.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

Bulk Inquiry

Select Batch

Purity: 99.87%

Purity: 99.79%

Purity: 99.59%

Purity: 99.42%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Adezmapimod (SB 203580) is a p38 MAPK inhibitor (IC50=0.3-0.5 μM) that is selective and ATP-competitive. Adezmapimod possesses autophagy and mitochondrial autophagy activating activity. Adezmapimod displays more than 100-fold higher selectivity than PKB, LCK, and GSK-3β.
Targets&IC50	PKB:3-5 μM (THP-1 cells), p38 MAPK:0.3-0.5 μM (THP-1 cells)
In vitro	METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Adezmapimod (0.1-20 μM) for 30 min, and the expression levels of target proteins were detected by Western Blot. RESULTS: Adezmapimod dose-dependently activated ERK but not p38 and JNK, and the maximum activation of ERK was between 1-10 μM. [1] METHODS: CD4+ T cells were treated with Adezmapimod (1-25 μM) for 72 h. The proliferation of Tregs was analyzed by Flow Cytometry. RESULTS: Adezmapimod inhibited TNF-induced proliferation of Tregs in a dose-dependent manner, with inhibition rates ranging from 32.0-73.2%. Adezmapimod treatment also significantly reduced the proportion of Foxp3+ Tregs in cultured CD4+ T cells, with inhibition rates ranging from 24.9-47.05%. [2]
In vivo	METHODS: To examine the in vivo activity, Adezmapimod (25 mg/kg in 4% DMSO+30% PEG 300+5% Tween 80+61% ddH2O) was administered to LPS-treated C57BL/6J mice by a single intraperitoneal injection, and then the mice were killed 24 and 72 h later. RESULTS: The LPS-induced up-regulation of Ki-67 and TNFR2 expression on Tregs was completely eliminated by Adezmapimod treatment. The inhibitory effect of Adezmapimod on the proliferation of Tregs in LPS-treated mice lasted for at least 72 h. [2] METHODS: To detect the effects on endometriosis (EM) development, Adezmapimod (1 μg/mg) was injected intraperitoneally into EM-induced BALB/c mice once daily for twenty-four days. RESULTS: Adezmapimod reduced the weight and size of endometriotic lesions in mice. Levels of IL-1β, TNF-α, MMP-2, and MMP-9 were reduced in peritoneal cells in the Adezmapimod group compared to the EM group. p38 MAPK phosphorylation levels were elevated in the EM group, and Adezmapimod down-regulated phosphorylation levels. [3]
Kinase Assay	Cells were lysed in Buffer A for Western blotting and PKB kinase assays. Kinase assays were performed according to the manufacturer's instructions. Briefly, 4 μg of sheep anti-PKBα was immobilized on 25 μl of protein G-Sepharose overnight (or 1.5 h) and washed in Buffer A (50 mM Tris, pH 7.5, 1 mM EDTA, 1 mMEGTA, 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 was then incubated with 0.5 ml of lysate (from 5 × 10^6 cells) for 1.5 h 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 mMβ-glycerophosphate, 25 mM EGTA, 5 mM sodium orthovanadate, 5 mM DTT. To the PKB enzyme immune complex was 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 was incubated for 20 min at room temperature with shaking, then samples were pulse spun, and 40 μl of reaction volume were removed into another tube to which was added 20 μl of 40% trichloroacetic acid to stop the reaction. This was mixed and incubated for 5 min at room temperature, and 40 μl was transferred onto P81 phosphocellulose paper and allowed to bind for 30 s. The P81 pieces were washed three times in 0.75% phosphoric acid then in acetone at room temperature. γ-32P incorporation was then measured by scintillation counting [1].
Cell Research	The luciferase reporter plasmid pIL6luc(-122) and the CAT reporter plasmid p(TRE)5CAT were transfected into TF-1 cell line by means of electroporation. Prior to transfection, cells were cultured for 16?h at a density of 0.5×10^6 cells/ml in the appropriate medium, washed twice and resuspended in RPMI 1640 at a density of 10×10^6 in 200?μl. When transfected with a single plasmid, 25?μg of DNA was added and the mixture was left at room temperature for 15?min. Cotransfections were performed with 15?μg of the reporter plasmid pIL6luc(-122) together with 15?μg of the dominant-negative expression plasmids (pRSV-MKK3(Ala), pcDNA3-MKK6(K82A), pRSV-NΔRaf1, pcDNA3-MKK4(Ala), pcDNA3-Flag-JNK1, or pcDNA3 (empty vector). Cotransfections of pGAL4tkluc (5?μg) with either pGAL4p65 (5?μg) or pGAL4dbd (5?μg) were performed under similar conditions. In addition, cells were cotransfected with 2?μg of a CMV-CAT plasmid, to normalize for transfection efficiency. Electroporation, in 0.4?cm electroporation cuvettes, was performed at 240?V and 960?μF with Gene Pulser electroporator. After electroporation, the cells were replated in RPMI 1640 containing 2% FBS. Six hours after transfection cells were stimulated for 24?h with medium or OA (30?ng/ml) or SB203580 for 30?min prior to OA stimulation. The cells were then harvested and lysed by commercially available luciferase lysis buffer. One-hundred μl of lysis product was added to 100?μl of luciferase assay reagents and luciferase activity was measured with the Anthos Lucy1 luminometer. CAT reporter activity of 100?μl lysis product plus 100?μl CAT dilution buffer was determined with a commercially available CAT Elisa kit [3].
Animal Research	In survival studies, C57BL/6J mice weighing 20 g to 30 g were briefly anesthetized with isoflurane and challenged with 0.05 mL of IT normal saline (NS, noninfected controls) or E. coli (15 × 10^9 CFU/kg) as previously described. One hour before NS challenge, mice (n = 24) received either intraperitoneal SB203580 (100 mg/kg in 0.25 mL) or diluent only (placebo). Infected animals received 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). All animals received ceftriaxone (100 mg/kg in 0.1 mL, subcutaneously) for 4 days and NS (0.5 mL, subcutaneously) for 1 day beginning 4 hours after challenge. Animals were 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). Sequential weekly experiments with 24 animals each compared either two to three doses of SB203580 versus placebo administered at similar times or similar doses of SB203580 versus placebo at differing treatment times. Study groups in each experiment were of equivalent sample size (i.e., 6 – 8 per group) [5].

Synonyms	PB 203580, RWJ 64809, SB203580
Molecular Weight	377.43
Formula	C21H16FN3OS
CAS No.	152121-47-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (132.47 mM)

1eq. HCl: 37.7 mg/mL (100 mM)

References and Literature

1. Henklova P, et al. SB203580, a pharmacological inhibitor of p38 MAP kinase transduction pathway activates ERK and JNK MAP kinases in primary cultures of human hepatocytes. Eur J Pharmacol. 2008 Sep 28;593(1-3):16-23. 2. He T, et al. The p38 MAPK Inhibitor SB203580 Abrogates Tumor Necrosis Factor-Induced Proliferative Expansion of Mouse CD4+Foxp3+ Regulatory T Cells. Front Immunol. 2018 Jul 9;9:1556. 3. Zhou WD, et al. SB203580, a p38 mitogen-activated protein kinase inhibitor, suppresses the development of endometriosis by down-regulating proinflammatory cytokines and proteolytic factors in a mouse model. Hum Reprod. 2010 Dec;25(12):3110-6. 4. Jin N, et al. The selective p38 mitogen-activated protein kinase inhibitor, SB203580, improves renal disease in MRL/lpr mouse model of systemic lupus. Int Immunopharmacol. 2011 Sep;11(9):1319-26. 5. Su J, et al. SB203580, a p38 inhibitor, improved cardiac function but worsened lung injury and survival during Escherichia coli pneumonia in mice. J Trauma. 2010 Jun;68(6):1317-27. 7. Liu J, Lv L, Gong J, et al. Overexpression of F-box only protein 31 predicts poor prognosis and deregulates p38α- and JNK-mediated apoptosis in esophageal squamous cell carcinoma [J]. International journal of cancer. 2018 Jan 1;142(1):145-155. 8. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma[J]. Theranostics. 2020, 10(14): 6530. 9. Hu S, Zhu L, Song Y, et al. Radiation-induced abscopal reproductive effect is driven by TNF-α/p38 MAPK/Rac1 axis in Sertoli cells[J]. Theranostics. 2021, 11(12): 5742.

Citations

1. Zhao Y, Li Y, Zhu R, et al.RPS15 interacted with IGF2BP1 to promote esophageal squamous cell carcinoma development via recognizing m6A modification.Signal Transduction and Targeted Therapy.2023, 8(1): 224. 2. Jiang Y, Zhao X, Chen J, et al.PM2. 5 induces cardiac malformations via PI3K/akt2/mTORC1 signaling pathway in zebrafish larvae.Environmental Pollution.2023: 121306. 3. Sui A, Yao C, Chen Y, et al.Polystyrene nanoplastics inhibit StAR expression by activating HIF-1α via ERK1/2 MAPK and AKT pathways in TM3 Leydig cells and testicular tissues of mice.Food and Chemical Toxicology.2023: 113634. 4. Liang Y, Qian Y, Tang J, et al.Arsenic trioxide promotes ERK1/2-mediated phosphorylation and degradation of BIMEL to attenuate apoptosis in BEAS-2B cells.Chemico-Biological Interactions.2022: 110304. 5. Yu Y, Wu T, Zhang X, et al.Regorafenib activates oxidative stress by inhibiting SELENOS and potentiates oxaliplatin-induced cell death in colon cancer cells.European Journal of Pharmacology.2023: 175986. 6. Lin X, Wang Y, Guo X, et al.Shikonin promotes rat periodontal bone defect repair and osteogenic differentiation of BMSCs by p38 MAPK pathway.Odontology.2022: 1-9. 7. Zhu Y, Xiao Y, Kong D, et al. Down-Regulation of miR-378d Increased Rab10 Expression to Help Clearance of Mycobacterium tuberculosis in Macrophages. Frontiers in cellular and infection microbiology. 2020, 10: 108. 8. Chang Y H, Chiang C Y, Fu E, et al. Staphylococcus aureus enhances gelatinase activities in monocytic U937 cells and in human gingival fibroblasts. Journal of Dental Sciences. 2022 9. Kong L, Huang H, Luan S, et al. Inhibition of ASIC1a-Mediated ERS Improves the Activation of HSCs and Copper Transport Under Copper Load. Frontiers in Pharmacology. 2021, 12: 1348. 10. Shao S, Xia H, Hu M, et al. Isotalatizidine, a C19-diterpenoid alkaloid, attenuates chronic neuropathic pain through stimulating ERK/CREB signaling pathway-mediated microglial dynorphin A expression. Journal of Neuroinflammation. 2020, 17(1): 1-11

11. Li Z J, Hou Y J, Hao G P, et al. CUDC-907 enhances TRAIL-induced apoptosis through upregulation of DR5 in breast cancer cells. Journal of Cell Communication and Signaling. 2020: 1-11. 12. Lyu L, Hu Y, Yin S, et al. Autophagy inhibition enhances anti‐pituitary adenoma effect of tetrandrine. Phytotherapy Research. 2021, 35(7): 4007-4021. 13. Zhang H, Wei Q, Gao Z, et al. G protein-coupled receptor 30 mediates meiosis resumption and gap junction communications downregulation in goat cumulus-oocyte complexes by 17β-estradio. Journal of Steroid Biochemistry and Molecular Biology. 2019, 187: 58-67 14. Hu S, Zhu L, Song Y, et al. Radiation-induced abscopal reproductive effect is driven by TNF-α/p38 MAPK/Rac1 axis in Sertoli cells. Theranostics. 2021 Mar 31;11(12):5742-5758. doi: 10.7150/thno.56853. eCollection 2021. 15. Zhou B, Yan J, Guo L, et al. Hepatoma cell-intrinsic TLR9 activation induces immune escape through PD-L1 upregulation in hepatocellular carcinoma. Theranostics. 2020, 10(14): 6530. 16. Li Z J, Hou Y J, Hao G P, et al. CUDC-907 enhances TRAIL-induced apoptosis through upregulation of DR5 in breast cancer cells. Journal of Cell Communication and Signaling. 2020: 1-11. 17. Cen W J, Feng Y, Li S S, et al. Iron overload induces G1 phase arrest and autophagy in murine preosteoblast cells. Journal of cellular physiology. 2018, 233(9): 6779-6789. 18. Tang J, Yao C, Liu Y, et al. Arsenic trioxide induces expression of BCL-2 expression via NF-κB and p38 MAPK signaling pathways in BEAS-2B cells during apoptosis. Ecotoxicology and Environmental Safety. 2021, 222: 112531. 19. Wang D, Wang H, Yan Y, et al.Coating 3D-printed bioceramics with histatin promotes adhesion and osteogenesis of stem cells.Tissue Engineering.2023 (ja). 20. Du T, Yan Z, Zhu S, et al. QKI deficiency leads to osteoporosis by promoting RANKL-inducedosteoclastogenesis and disrupting bone metabolism. Cell Death and Disease. 2020 21. Wen Y, Peng D, Li C, et al. A new polysaccharide isolated from Morchella importuna fruiting bodies and its immunoregulatory mechanism. International Journal of Biological Macromolecules. 2019, 137: 8-19. 22. Yuan J, Yao C, Tang J, et al. Enhanced GRP78 protein expression via the IRE1α/ASK1/p38 MAPK pathway during As2O3-induced endoplasmic reticulum stress in BEAS-2B cells. Toxicology. 2021, 462: 152962. 23. Hu Q, Du H, Ma G, et al. Purification, identification and functional characterization of an immunomodulatory protein from Pleurotus eryngii. Food & Function. 2018, 9(7): 3764-3775 24. Zhu N, Xiang Y, Zhao X, et al. Thymoquinone suppresses platelet‐derived growth factor‐BB–induced vascular smooth muscle cell proliferation, migration and neointimal formation. Journal of Cellular and Molecular Medicine. 2019 25. Xie D, Ge X, Ma Y, et al. Clemastine improves hypomyelination in rats with hypoxic–ischemic brain injury by reducing microglia-derived IL-1β via P38 signaling pathway. Journal of neuroinflammation. 2020, 17(1): 1-17. 26. Liu Y, Tang J, Yuan J, et al. Arsenite-induced downregulation of occludin in mouse lungs and BEAS-2B cells via the ROS/ERK/ELK1/MLCK and ROS/p38 MAPK signaling pathways. Toxicology Letters. 2020, 332: 146-154 27. Da Q, Yan Z, Li Z, et al. TAK1 is involved in sodium L-lactate-stimulated p38 signaling and promotes apoptosis. Molecular and Cellular Biochemistry. 2020: 1-10 28. Lu D, Zhang H, Zhang Y, et al. Secreted MbovP0145 Promotes IL-8 Expression through Its Interactive β-Actin and MAPK Activation and Contributes to Neutrophil Migration. Pathogens. 2021, 10(12): 1628. 29. Zhao M, Zheng Z, Yin Z, et al.DEL-1 deficiency aggravates pressure overload-induced heart failure by promoting neutrophil infiltration and neutrophil extracellular traps formation.Biochemical Pharmacology.2023: 115912. 30. Cui S, Suo N, Yang Y, et al.The aminosteroid U73122 promotes oligodendrocytes generation and myelin formation.Acta Pharmacologica Sinica.2023: 1-12. 31. Zhang X, Wang J, Wang M, et al.IFN-β Pretreatment Alleviates Allogeneic Renal Tubular Epithelial Cell–Induced NK Cell Responses via the IRF7/HLA-E/NKG2A Axis.The Journal of Immunology.2023 32. Ni L, Zhu X, Zhao Q, et al.Dihydroartemisinin, a potential PTGS1 inhibitor, potentiated cisplatin-induced cell death in non-small cell lung cancer through activating ROS-mediated multiple signaling pathways.Neoplasia.2024, 51: 100991.

See More... Hide

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Anti-Cancer Active Compound Library Preclinical Compound Library Anti-Prostate Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library Cancer Cell Differentiation Compound Library Bioactive Compounds Library Max Neural Regeneration Compound Library HIF-1 Signaling Pathway Compound Library

Related Products

Related compounds with same targets

Oxidopamine hydrobromide 5-Aminolevulinic acid hydrochloride D-glutamine Deferoxamine Mesylate Simvastatin Torkinib Sulfosuccinimidyl oleate Curcumin

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

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 n 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.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Adezmapimod 152121-47-6 Autophagy MAPK Mitophagy p38 MAPK Inhibitor PKBα PB 203580 inhibit SAPK2a GSK3β RWJ 64809 Mitochondrial Autophagy SB-203580 PB-203580 SB203580 SB 203580 RWJ64809 PB203580 LCK SAPK2b RWJ-64809 ATP-competitive inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.