SHIN 1

SHIN1 is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

IC50: 5 nM (SHMT1), 13 nM (SHMT1)[1]

SHIN1 inhibits human SHIN1 SHMT1/2 with IC50s of 5 and 13 nM, respectively in an in vitro assay. SHIN1 inhibits the growth of SHMT2 deletion HCT-116 cells with an IC50 of 10 nM. SHIN1 inhibits SHMT1/2 in HCT-116 cells. SHIN1 is particularly active against B-cell malignancies. SHIN1 blocks cell growth through a progressive depletion of purines, leading to loss of nucleotide triphosphates[1].

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].

[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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