Thieno[2,3-d]pyrimidin-4-amine, 5,6-dimethyl-N-[1-(phenylmethyl)-3-pyrrolidinyl]-

Description

Fasnall (CAS 929978-58-5) is a potent and selective fatty acid synthase (FASN) inhibitor acting via interfering with cofactor binding.1?IC50s = 147 and 213 nM respectively for inhibition of acetate and glucose incorporation into total lipids in HepG2 cells. IC50=5.84 μM in an isolated enzyme assay. Displays potent antitumor activity in the MMTV-Neu HER2+ breast cancer model.1?Reduces HIV-1 virion production by 90% (EC50=213 nM).2

Definition

ChEBI: Fasnall is a racemate comprising equimolar amounts of (R)- and (S)-Fasnall. Both enantiomers act as fatty acid synthase inhibitors, although the (S)-enantiomer was found to be more than 4 times as active as the (R)-enantiomer. It has a role as a fatty acid synthesis inhibitor, an EC 2.3.1.85 (fatty acid synthase) inhibitor, an apoptosis inducer and an anti-HIV agent. It contains a (R)-Fasnall and a (S)-Fasnall.

References

1) Alwarawrah et al. (2016) Fasnall, a Selective FASN Inhibitor, Shows Potent Anti-tumor Activity in the MMTV-Neu Model of HER2(+) Breast Cancer, Cell Chem. Biol., 23 678 2) Kulkarni et al. (2017), Cellular fatty acid synthase is required for late stages of HIV-1 replication; Retrovirology, 14 45