Cas No.: | 2146095-85-2 |
Chemical Name: | SHIN1 |
Synonyms: | SHIN1; SHIN-1; SHIN 1; Serine hydroxymethyltranferase inhibitor 1 |
SMILES: | N#CC(C1(C2=CC(C3=CC=CC=C3)=CC(CO)=C2)C(C)C)=C(N)OC4=C1C(C)=NN4 |
Formula: | C24H24N4O2 |
M.Wt: | 400.48 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |
Target: | IC50: 5 nM (SHMT1), 13 nM (SHMT1)[1] |
In Vitro: | 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]. |
Cell Assay: | 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]. |
References: | [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. |