Doramapimod (GMP)
Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity.
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。
The Doramapimod (GMP) was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS 番号: 285983-48-4
- 分子式: C31H37N5O3
- 分子量:527.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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p38α 38 nM (IC50) |
p38β 65 nM (IC50) |
p38γ 200 nM (IC50) |
p38δ 520 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
15 nM
Compound: BIRB-796
|
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
Antiinflammatory activity in LPS-stimulated human isolated PBMC assessed as inhibition of TNFalpha production preincubated for 1 hr prior to LPS-challenge by ELISA
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[PMID: 21888439] |
| PBMC | IC50 |
30 nM
Compound: BIRB-796
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Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
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[PMID: 18602262] |
| THP-1 | EC50 |
18 nM
Compound: 45
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Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells
Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells
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[PMID: 12086485] |
| THP-1 | IC50 |
0.013 μM
Compound: BIRB-796
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Inhibition of LPS-induced TNFalpha production in human THP1 cells
Inhibition of LPS-induced TNFalpha production in human THP1 cells
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[PMID: 18325768] |
| THP-1 | IC50 |
18 nM
Compound: 1, BIRB-796
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Inhibition of LPS-induced TNFalpha production in human THP1 cells
Inhibition of LPS-induced TNFalpha production in human THP1 cells
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[PMID: 19356929] |
| THP-1 | IC50 |
18 nM
Compound: BIRB-796
|
Inhibition of LPS-induced TNFalpha production in THP1 cells
Inhibition of LPS-induced TNFalpha production in THP1 cells
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[PMID: 17560108] |
| THP-1 | IC50 |
18 nM
Compound: BIRB-796
|
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells
|
[PMID: 18462940] |
| U-937 | IC50 |
15 nM
Compound: 4; BIRB-796
|
Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control
Antiinflammatory activity in differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS-stimulation for 4 hrs by sandwich ELISA relative to vehicle-treated control
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[PMID: 26800309] |
化学情報
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CAS 番号 285983-48-4
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分子量 527.66
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分子式 C31H37N5O3
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SMILES
O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3
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別名
BIRB 796 (GMP)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Doramapimod (GMP) 関連分類
HY-10320G 関連分類
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