Name | VTX-27 |
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 demonstrates a superior PK profile characterized by low clearance (7 mL/min/kg), high oral bioavailability (65%), and a prolonged half-life (4.7 h). Following a single oral administration at doses of 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL), it effectively inhibits IL-2 production in a potent dose-dependent manner. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 125 mg/mL (298.40 mM), Sonication is recommended.
|
Keywords | VTX-27 | VTX27 | VTX 27 | Protein kinase C | PKC | Inhibitor | inhibit |
Inhibitors Related | Daphnetin | Darovasertib | Ellagic acid | α-Vitamin E | Ro-3306 | Staurosporine | Methyl-Hesperidin | N-Desmethyltamoxifen hydrochloride | Fasudil hydrochloride | Mitoxantrone dihydrochloride | Myricitrin | R59949 |
Related Compound Libraries | Bioactive Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | Cytoskeletal Signaling Pathway Compound Library | TGF-beta/Smad Compound Library |