| Description | VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ). |
| In vitro | It has also been found that VTX-27 has good selectivity to other PKC family members, especially the classic isoforms (except for PKCβI, >1000 times, 200 times) and atypical isoforms (>10000 times). As expected, it is more challenging to obtain selectivity for more closely related novel PKC family members, which is 200 times more selective than PKCδ. |
| In vivo | VTX-27 shows the best PK profile with low clearance (7 mL/min/kg), good oral bioavailability (65%), and long half-life (4.7 h). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose-dependent inhibition of IL-2 production. |
| Target activity | PKCα:356 nM (ki), PKCδ:16 nM (ki), PKCθ:0.08 nM (ki) |
| molecular weight | 418.9 |
| Molecular formula | C20H24ClFN6O |
| CAS | 1321924-70-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (298.40 mM), Sonication is recommended. |
| References | 1. Jimenez JM, et al. Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases. J Med Chem. 2013 Mar 14;56(5):1799-810. |