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.
Para uso exclusivo en investigación. No vendemos a pacientes.
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.
- No. CAS: 285983-48-4
- Fòrmula: C31H37N5O3
- Peso molecular:527.66
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
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p38α 38 nM (IC50) |
p38β 65 nM (IC50) |
p38γ 200 nM (IC50) |
p38δ 520 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PBMC | IC50 |
15 nM
Compound: BIRB-796
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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
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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
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Inhibition of LPS-stimulated TNFalpha production in human THP1 cells
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells
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[PMID: 18462940] |
| U-937 | IC50 |
15 nM
Compound: 4; BIRB-796
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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] |
Chemical Information
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No. CAS 285983-48-4
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Peso molecular 527.66
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Fòrmula 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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Synonyms
BIRB 796 (GMP)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Doramapimod (GMP) Related Classifications
HY-10320G Related Classifications
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