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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.71%
- CAS 番号: 449811-01-2
- 分子式: C19H20F2N4O4
- 分子量:406.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
MedChemExpress(MCE)の使用を引用している文献 Pamapimod
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生物活性
製品説明
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 |
|---|---|---|---|---|
| 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
|
[PMID: 19950901] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 449811-01-2
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性状 Solid
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分子量 406.38
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分子式 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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別名
Ro4402257; R1503
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 | 2.4608 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 |