Doramapimod is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 5 mg | In stock | $ 70 | |
| 10 mg | In stock | $ 133 | |
| 20 mg | In stock | $ 166 | |
| 50 mg | In stock | $ 354 | |
| 100 mg | In stock | $ 559 |
| Description | Doramapimod is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM), but weakly inhibits c-RAF, Fyn, Lck, ERK-1, SYK, IKK2, and ZAP-70. |
| Targets&IC50 | p38 MAPK:0.1 nM (Kd, cell free) |
| In vitro | Doramapimod (BIRB796) is a highly potent inhibitor of p38 MAPK (Kd: 0.1 nM) that blocks TNFα release in LPS-stimulated THP-1 cells (IC50: 18 nM) . BIRB796 also inhibits the activity and the activation of SAPK3/p38gamma. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97 . BIRB 796 inhibited Hsp27 phosphorylation induced by 17-AAG plus bortezomib, thereby enhancing cytotoxicity. In bone marrow stromal cells (BMSC), BIRB 796 inhibited phosphorylation of p38 MAPK and secretion of IL-6 and vascular endothelial growth factor triggered by either tumour necrosis factor-alpha or tumour growth factor-beta1. BIRB 796 also inhibited IL-6 secretion induced in BMSCs by adherence to MM cells, thereby inhibiting tumour cell proliferation . |
| In vivo | Systolic blood pressure of untreated dTGRs was 204 mm Hg, but partially reduced after BIRB796 (30 mg/kg per day) treatment (166 mm Hg), whereas Sprague-Dawley rats were normotensive. The beta-myosin heavy chain expression of BIRB796-treated hearts was significantly lower in BIRB796 compared with dTGRs. BIRB796 treatment significantly reduced cardiac fibrosis, connective tissue growth factor, tumor necrosis factor-alpha, interleukin-6, and macrophage infiltration . |
| Synonyms | BIRB 796 |
| CAS No. | 285983-48-4 |
| Chemical Formula | C31H37N5O3 |
| Molecular Weight | 527.669 |
| Solubility | Ethanol: 26.4 mg/mL (50 mM) DMSO: 52.8 mg/mL (100 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
In vivo Formulation Calculator (Clear solution)Calculatorbottom
