Pamapimod
Based on 1 publication(s) in Google Scholar
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
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- Pureté : 99.71%
- CAS No.: 449811-01-2
- Formule: C19H20F2N4O4
- Masse moléculaire:406.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Pamapimod
More
Activité biologique
Description
IC50 & Target
[1]|
p38α 14 nM (IC50) |
p38α 1.3 nM (Ki) |
p38β 480 (IC50) |
p38β 120 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
>30 μM
Compound: 5
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Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against HEK293 after 24 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 26704265] |
| THP-1 | IC50 |
0.025 μM
Compound: 2b, Pamapimod
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Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human THP1 cells after 2 hrs by ELISA
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[PMID: 21375264] |
| THP-1 | IC50 |
25 nM
Compound: 1
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Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA
Inhibition of LPS-induced TNFalpha production in human THP1 cells by ELISA
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[PMID: 19950901] |
In Vitro
Pamapimod binds to JNK kinases with Ki values of 190 nM, 16 nM and 19 nM for Jnk1, Jnk2 and Jnk3, respectively[1].
After lipopolysaccharide (LPS) stimulation of the human myelomonocytic cell line (THP-1), secretion of TNF-α is inhibited by Pamapimod, with an EC50 of 25 nM. Pamapimod suppresses TNF-α and IL-1β production in whole blood, with EC50 values of 0.40 and 0.10 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/1J female mice (8-10 weeks of age) induced murine collagen[1]
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Dosage:0 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg, 90 mg/kg, 150 mg/kg
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Administration:Oral gavage; once daily
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Result:Reduced inflammation and bone loss.
Chemical Information
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CAS No. 449811-01-2
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Appearance Solid
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Masse moléculaire 406.38
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Formule C19H20F2N4O4
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Color White to off-white
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SMILES
O=C1C(OC2=CC=C(F)C=C2F)=CC3=CN=C(NC(CCO)CCO)N=C3N1C
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Synonyms
Ro4402257; R1503
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
2025 May 23;16(1):4791. PMID: 40410189
Solvant et solubilité
In Vitro:
DMSO : ≥ 34 mg/mL (83.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.4608 mL | 12.3038 mL | 24.6075 mL | 61.5188 mL |
| 5 mM | 0.4922 mL | 2.4608 mL | 4.9215 mL | 12.3038 mL | |
| 10 mM | 0.2461 mL | 1.2304 mL | 2.4608 mL | 6.1519 mL | |
| 15 mM | 0.1641 mL | 0.8203 mL | 1.6405 mL | 4.1013 mL | |
| 20 mM | 0.1230 mL | 0.6152 mL | 1.2304 mL | 3.0759 mL | |
| 25 mM | 0.0984 mL | 0.4922 mL | 0.9843 mL | 2.4608 mL | |
| 30 mM | 0.0820 mL | 0.4101 mL | 0.8203 mL | 2.0506 mL | |
| 40 mM | 0.0615 mL | 0.3076 mL | 0.6152 mL | 1.5380 mL | |
| 50 mM | 0.0492 mL | 0.2461 mL | 0.4922 mL | 1.2304 mL | |
| 60 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0253 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3076 mL | 0.7690 mL |
Pamapimod Related Classifications
HY-10405 Related Classifications
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