2. MAPK/ERK Pathway
  3. p38 MAPK
  4. 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.

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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.

Doramapimod (GMP)

Doramapimod (GMP) Estructura química

No. CAS : 285983-48-4

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Doramapimod (GMP) Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas p38 MAPK:

Ver todas las isoformas
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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Descripciòn

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[1].

IC50 & Target

p38α

38 nM (IC50)

p38β

65 nM (IC50)

p38γ

200 nM (IC50)

p38δ

520 nM (IC50)

Cellular Effect
Cell Line 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
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
[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]
Peso molecular

527.66

Fòrmula

C31H37N5O3
No. CAS
SMILES

O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=C(C)C=C2)NC3=C4C=CC=CC4=C(OCCN5CCOCC5)C=C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
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Doramapimod (GMP) Related Classifications

  • Calculadora de molaridad

  • Calculadora de dilución

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Doramapimod (GMP)285983-48-4BIRB 796 (GMP)p38 MAPKorally activemultiple myelomaoral epidermoid carcinomacervical cancerInhibitorinhibitorinhibit

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Nombre del producto:
Doramapimod (GMP)
Cat. No.:
HY-10320G
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