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BIRB796

Cat. No. M1675
BIRB796 Structure
Synonym:

Doramapimod

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 65  USD65 In stock
5mg USD 35  USD35 In stock
10mg USD 45  USD45 In stock
50mg USD 105  USD105 In stock
100mg USD 140  USD140 In stock
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Quality Control & Documentation
Biological Activity

BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK. BIRB 796 (Doramapimod) has high picomolar affinity (Kd = 100 pM) for p38 MAP kinase and low nanomolar inhibitory activity (IC50 = 18 nM) against TNFα in THP-1 cell culture. The p38 inhibitor BIRB 796 (Doramapimod) binds tightly (Kd = 40 nM) to ABL (T315I) and inhibits the BMS-354825- and imatinib-resistant ABL (T315I) kinase.

Product Citations
Customer Product Validations & Biological Datas
Source PLoS One (2013). Figure 4. BIRB796
Method Western blot
Cell Lines MDR cells
Concentrations 10 μM
Incubation Time 72 h
Results These data indicated that BIRB796 mediated the reversal of MDR by inhibiting the function of ABCB1, and not due to inhibition of ABCB1 expression.
Protocol (for reference only)
Cell Experiment
Cell lines MM derived cell line
Preparation method Growth inhibition assay. The growth inhibitory effect of BIRB 796 on MM cell line growth was assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT, Sigma Chem-ical) dye absorbance, as previously described (Yasui et al,2005a)
Concentrations 0, 100, 400nM
Incubation time 72h
Animal Experiment
Animal models Male Crlj:CD1(ICR)mice
Formulation saline
Dosages 250, 500 or 1000 mg/kg
Administration oral
Chemical Information
Molecular Weight 527.66
Formula C31H37N5O3
CAS Number 285983-48-4
Solubility (25°C) DMSO 66 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ding et al. J Trauma Acute Care Surg. Role of p38 mitogen-activated protein kinase in posttraumatic immunosuppression in mice.

[2] Iwano et al. J Appl Toxicol. A possible mechanism for hepatotoxicity induced by BIRB-796, an orally active p38 mitogen-activated protein kinase inhibitor.

[3] Kuglstatter et al. Bioorg Med Chem Lett. X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.

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Keywords: BIRB796, Doramapimod supplier, p38 MAPK, inhibitors, activators


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