SHIN 1 is an inhibitor of serine hydroxymethyltransferase 1 (SHMT1) and SHMT2 (IC50s = 5 and 13 nM, respectively).1 It inhibits proliferation of H1299 non-small cell lung cancer (NSCLC) cells overexpressing the proto-oncogene FRAT1 (IC50 = 0.6 ?M). SHIN 1 decreases tumor volume in an NSCLC mouse xenograft model using FRAT1-overexpressing H1299 cells when administered at a dose of 100 mg/kg three times a week.
1.He, L., Endress, J., Cho, S., et al.Suppression of nuclear GSK3 signaling promotes serine/one-carbon metabolism and confers metabolic vulnerability in lung cancer cellsSci. Adv.8(20)eabm8786(2022)