Referencia número: HY-11068

SB 239063

31 Cited Publications

Revisión del cliente

Based on 31 publication(s) in Google Scholar

SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC₅₀ of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD. SB 239063 can penetrate the blood brain barrier (BBB).

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 99.15%
No. CAS: 193551-21-2
Fòrmula: C₂₀H₂₁FN₄O₂
Peso molecular:368.40

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SB 239063 Chemical Structure

No. CAS: 193551-21-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (31)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

IC50: 44 nM (Human p38α)^[1]

Ver todos los productos específicos de isoformas p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	IC₅₀	120 nM Compound: K00570a, SB-239063	Inhibition of LPS-stimulated IL1 production in human THP1 cells Inhibition of LPS-stimulated IL1 production in human THP1 cells	[PMID: 18077363]
THP-1	IC₅₀	120 nM Compound: K00570a, SB-239063	Inhibition of LPS-stimulated TNFalpha production in human THP1 cells Inhibition of LPS-stimulated TNFalpha production in human THP1 cells	[PMID: 18077363]

In Vitro

SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards^[1].
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC₅₀ values of 120 nM and 350 nM, respectively^[1].

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

Apoptosis Analysis^[1]

Cell Line:

Eosinophils (guinea pig BALs)
Concentration:

0.1μM, 1μM, 10μM
Incubation Time:

29 hours, 47 hours
Result:

Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.

In Vivo

SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia^[1].
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation^[1].
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC₅₀ of 5.8 mg/kg (2.8–10.3; 95% CL)^[1].

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

Animal Model:

Male BALB/c mice (18–20 g)^[1]
Dosage:

12 mg/kg
Administration:

Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days
Result:

Significantly inhibited the resultant antigen-induced airway eosinophilia.

Chemical Information

No. CAS 193551-21-2
Appearance Solid
Peso molecular 368.40
Fòrmula C₂₀H₂₁FN₄O₂
Color White to yellow
SMILES

COC1=NC=CC(C2=C(N=CN2[C@H]3CC[C@H](O)CC3)C4=CC=C(F)C=C4)=N1
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (31)

All IFWB

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Journal Impact Factor

Microbiome

RhoB affects colitis through modulating cell signaling and intestinal microbiome. [Abstract]

2022 Sep 16;10(1):149. PMID: 36114582
Acta Pharm Sin B

A novel mesenchymal stem cell-based regimen for acute myeloid leukemia differentiation therapy. [Abstract]

2023 Jul;13(7):3027-3042. PMID: 37521858
J Exp Clin Cancer Res

Supervillin promotes epithelial-mesenchymal transition and metastasis of hepatocellular carcinoma in hypoxia via activation of the RhoA/ROCK-ERK/p38 pathway. [Abstract]

2018 Jun 28;37(1):128. PMID: 29954442

SB 239063 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 28;37(1):128. [Abstract]

MHCC-97H cells are transfected with control or supervillin-specific siRNA for 48 h, exposed to hypoxia for 16 h, and lysates are assayed for the relative amounts of GTP-loaded (activated) Rac1, Cdc42, and RhoA. Cells that have been transfected with control RNAi are treated with a PD0325901 or SB239063 before assaying for GTP-Rac1, Cdc42, and RhoA levels.
Carbohydr Polym

Inhibition of dextran sodium sulfate-induced colitis in mice by baker's yeast polysaccharides. [Abstract]

2019 Mar 1;207:371-381. PMID: 30600019
Research (Wash D C)

Gene Signature-Based Drug Screening Reveals Ponatinib Enhances Immunotherapy Efficacy in Triple-Negative Breast Cancer by Reversing MDSC-Mediated Immunosuppressive Tumor Microenvironment. [Abstract]

2025 Oct 9:8:0915. PMID: 41079672
Cell Death Dis

Dynasore suppresses cell proliferation, migration, and invasion and enhances the antitumor capacity of cisplatin via STAT3 pathway in osteosarcoma. [Abstract]

2019 Sep 18;10(10):687. PMID: 31534119
Cell Death Discov

TGR5-HNF4α axis contributes to bile acid-induced gastric intestinal metaplasia markers expression. [Abstract]

2020 Jul 6;6:56. PMID: 32655894
Int J Biol Macromol

Camellia sinensis polysaccharide attenuates inflammatory responses via the ROS-mediated pathway by endocytosis. [Abstract]

2024 May;267(Pt 2):131674. PMID: 38641285
Int J Biol Macromol

Polysaccharide isolated from Sarcodon aspratus induces RAW264.7 activity via TLR4-mediated NF-κB and MAPK signaling pathways. [Abstract]

2018 Dec;120(Pt A):1039-1047. PMID: 30171950
Cell Mol Neurobiol

Geniposide Alleviates Traumatic Brain Injury in Rats Via Anti-Inflammatory Effect and MAPK/NF-kB Inhibition. [Abstract]

2020 May;40(4):511-520. PMID: 31677006
CNS Neurosci Ther

NFAT1 Signaling Contributes to Bone Cancer Pain by Regulating IL-18 Expression in Spinal Microglia. [Abstract]

2025 Feb;31(2):e70222. PMID: 39957627
Cells

Search for Synergistic Drug Combinations to Treat Chronic Lymphocytic Leukemia. [Abstract]

2022 Nov 18;11(22):3671. PMID: 36429097
Cells

Blood Serum Stimulates p38-Mediated Proliferation and Changes in Global Gene Expression of Adult Human Cardiac Stem Cells. [Abstract]

2020 Jun 16;9(6):1472. PMID: 32560212
Int Immunopharmacol

Administration of SB239063, a potent p38 MAPK inhibitor, alleviates acute lung injury induced by intestinal ischemia reperfusion in rats associated with AQP4 downregulation. [Abstract]

2016 Sep:38:54-60. PMID: 27236300

SB 239063 purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2016 Sep:38:54-60. [Abstract]

The protective role of p38 MAPK inhibition in II/R-induced ALI and regulation of AQP4 in rats. HE staining and Lung wet/dry weight ratio show obvious evidences of ALI and lung edema. Western blot and immunofluorescent staining confirm the increased expression levels of AQP4 and P-p38 MAPK protein in the lung tissues. Then, the p38 MAPK inhibitor is administrated intraperitoneally. Results show that p38 MAPK inhibition downregulates AQP4 expression in the lungs and protected lung from acute injur
Front Pharmacol

Andrographolide Protects against Aortic Banding-Induced Experimental Cardiac Hypertrophy by Inhibiting MAPKs Signaling. [Abstract]

2017 Nov 14:8:808. PMID: 29184496

SB 239063 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2017 Nov 14:8:808. [Abstract]

Immunofluorescence staining of α-actinin and the cell surface area of cardiomyocytes in the indicated groups (n=5 samples and n=100+cells per group).
Sci Rep

PTPRK promotes resiniferatoxin-induced postherpetic neuralgia via activating DUSP1/p38 MAPK signaling pathway in dorsal root ganglia. [Abstract]

2025 Nov 18;15(1):40630. PMID: 41253902
Journal of Pharmaceutical Investigation

2021 Apr.
Journal of Pharmaceutical Investigation

2021 Mar 31.
FASEB J

ALOX15-Derived Oxylipins Attenuate Macrophage Inflammatory Signaling Via a Gαq-PLC-PKC Pathway. [Abstract]

2026 Mar 31;40(6):e71696. PMID: 41847922
Cell Biol Int

Bcl6 knockdown aggravates hypoxia injury in cardiomyocytes via the P38 pathway. [Abstract]

2019 Feb;43(2):108-116. PMID: 29972264
R Soc Open Sci

Ultra-performance liquid chromatography-tandem mass spectrometric method for quantitation of the recently Food and Drug Administration approved combination of vaborbactam and meropenem in human plasma. [Abstract]

2020 Jul 8;7(7):200635. PMID: 32874656
Scand J Immunol

Saturated fatty acids activate the inflammatory signalling pathway in Schwann cells: Implication in sciatic nerve injury. [Abstract]

2020 Aug;92(2):e12896. PMID: 32557749
Biomed Pharmacother

Homoharringtonine (omacetaxine mepesuccinate) limits the angiogenic capacity of endothelial cells and reorganises filamentous actin. [Abstract]

2025 Apr 3:186:118025. PMID: 40184838
SSRN

27 Sep 2022.
Oxid Med Cell Longev

Cholecystokinin Octapeptide Promotes ANP Secretion through Activation of NOX4-PGC-1 α-PPAR α/PPAR γ Signaling in Isolated Beating Rat Atria. [Abstract]

2022 Jun 20;2022:5905374. PMID: 35770043
Patent

US20190248778A1.
China Biotechnology

2017, 37(12): 40-48.

SB 239063 purchased from MedChemExpress. Usage Cited in: China Biotechnology. 2017, 37(12): 40-48.

The Western blot analysis of HOG1 and Phospho-HOG1.
Patent

US20160368910A1.
Patent

US20140309249A1.
Patent

US20120245188A1.
Chem Biol

Discovery of potent and selective covalent inhibitors of JNK. [Abstract]

2012 Jan 27;19(1):140-54. PMID: 22284361

Solvente y solubilidad

In Vitro:

DMSO : 33.33 mg/mL (90.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7144 mL

13.5722 mL

27.1444 mL

5 mM

0.5429 mL

2.7144 mL

5.4289 mL

10 mM

0.2714 mL

1.3572 mL

2.7144 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Underwood DC, et al. SB 239063, a potent p38 MAP kinase inhibitor, reduces inflammatory cytokine production, airways eosinophil infiltration, and persistence. J Pharmacol Exp Ther. 2000 Apr;293(1):281-8. [Content Brief]

[2]. Matthew Huentelman, et al. Methods of treating memory loss and enhancing memory performance. US 20120245188 A1.

[3]. Katherine L. Gibbs, et al. Inhibiting p38 MAPK alpha rescues axonal retrograde transport defects in a mouse model of ALS. cell death & disease. 596 (2018).

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.7144 mL	13.5722 mL	27.1444 mL	67.8610 mL
	5 mM	0.5429 mL	2.7144 mL	5.4289 mL	13.5722 mL
	10 mM	0.2714 mL	1.3572 mL	2.7144 mL	6.7861 mL
	15 mM	0.1810 mL	0.9048 mL	1.8096 mL	4.5241 mL
	20 mM	0.1357 mL	0.6786 mL	1.3572 mL	3.3931 mL
	25 mM	0.1086 mL	0.5429 mL	1.0858 mL	2.7144 mL
	30 mM	0.0905 mL	0.4524 mL	0.9048 mL	2.2620 mL
	40 mM	0.0679 mL	0.3393 mL	0.6786 mL	1.6965 mL
	50 mM	0.0543 mL	0.2714 mL	0.5429 mL	1.3572 mL
	60 mM	0.0452 mL	0.2262 mL	0.4524 mL	1.1310 mL
	80 mM	0.0339 mL	0.1697 mL	0.3393 mL	0.8483 mL

Keywords

SB 239063

31 Cited Publications

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SB 239063

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) SB 239063

Ver todos los productos específicos de isoformas p38 MAPK

Actividad biológica

Chemical Information

Publications (31)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

SB 239063 Related Classifications

HY-11068 Related Classifications