Thieno[3,2-d]pyriMidine-6-carboxaMide, 4-[4-[2-[(2,2-diMethyl-1-oxopropyl)aMino]ethyl]-1-piperidinyl]-

Description

SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.

SIRT-IN-1 (compound 28) is one of the most potent truncated pan SIRT1/ 2/3 inhibitor, the IC50 values are 0.015, 0.010, 0.033 μM, respectively. SIRT-IN-1 (SIRT1/2/3 pan inhibitor) binds identically in the catalytic active site (RMS=0.29 ?), occupying the nicotinamide C-pocket and acetyl lysine substrate channel[1].

References

[1]. Disch JS, et al. Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3. J Med Chem. 2013 May 9;56(9):3666-79.