PF-9366 (C005B-432400)

Biochem/physiol Actions

PF-9366 is a methionine adenosyltransferase 2A allosteric inhibitor (human Mat2A IC₅₀/K_d = 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 μM wihout vs. 0.86 μM 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.

UPC:

51112511

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

25

Unit of Measurement:

MG

MPN:

PZ0403-25MG

CAS:

72882-78-1