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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
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 No.: 285983-48-4
- 화학식: C31H37N5O3
- 분자량:527.66
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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
|
[PMID: 21888439] |
| PBMC | IC50 |
30 nM
Compound: BIRB-796
|
Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
Inhibition of LPS-stimulated TNFalpha release in human PBMC by ELISA
|
[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
|
Inhibition of LPS-induced TNFalpha production in human THP1 cells
Inhibition of LPS-induced TNFalpha production in human THP1 cells
|
[PMID: 18325768] |
| THP-1 | IC50 |
18 nM
Compound: 1, BIRB-796
|
Inhibition of LPS-induced TNFalpha production in human THP1 cells
Inhibition of LPS-induced TNFalpha production in human THP1 cells
|
[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
|
[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
|
[PMID: 26800309] |
Chemical Information
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CAS No. 285983-48-4
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분자량 527.66
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Doramapimod (GMP) Related Classifications
HY-10320G Related Classifications
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