An SHMT1 and SHMT2 inhibitor
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)
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Cell experiment: |
For proliferation assays, HCT-116 cells are treated with SHIN1 (1, 10, 100, 1000, 10000 nM) for 24-72 hours. Cell number was counted directly using Trypan blue and the Countess system[1]. |
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参考文献: [1]. Ducker GS, et al. Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11404-11409. |
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