Synonyms: 7-Chloro-N,N-dimethyl-5-phenyl-[1,2,4]triazolo[4,3-a]quinoline-1-ethanamine; PF 9366; PF9366
Molecular Formula: C20H19ClN4
Molecular Weight: 350.84
Linear Structural Formula: C20H19ClN4
MDL Number: MFCD31630724
Purity: >=98% (HPLC)
Storage: room temp
Biochem Physiol Actions: PF-9366 is a methionine adenosyltransferase 2A allosteric inhibitor (human Mat2A IC50/Kd = 420 nM/170 nM) whose binding site overlaps with that of the Mat2A regulator, Mat2B. PF-9366 inhibits cellular SAM production in a Mat2B-competitive manner (IC50 post 6-hr treatment = 1.2 muM wihout vs. 0.86 muM with Mat2B knockdown; H520 lung carcinoma cells) without antiproliferation efficacy in cancer cultures due to an induction of Mat2A upregulation upon allosteric inhibition. Similar to Mat2B, PF-9366 allosteric binding alters Mat2A active site, causing increased substrate affinity and decreased enzyme turnover.
Legal Information: Sold for research purposes under agreement from Pfizer Inc.