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.
|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|
|Animal models||Male Crlj:CD1(ICR)mice|
|Dosages||250, 500 or 1000 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 100 mg/mL|
Role of p38 mitogen-activated protein kinase in posttraumatic immunosuppression in mice.
Ding et al. J Trauma Acute Care Surg. 2012 Aug 20. PMID: 22914078.
A possible mechanism for hepatotoxicity induced by BIRB-796, an orally active p38 mitogen-activated protein kinase inhibitor.
Iwano et al. J Appl Toxicol. 2011 Oct;31(7):671-7. PMID: 21328587.
X-ray crystal structure of JNK2 complexed with the p38alpha inhibitor BIRB796: insights into the rational design of DFG-out binding MAP kinase inhibitors.
Kuglstatter et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5217-20. PMID: 20655210.
|Related p38 MAPK Products|
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Losmapimod (GW856553) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.
VX-745 is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
Skepinone-L is a selective p38α-MAPK inhibitor with IC50 of 5 nM.
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