a 274

A 274 is a highly aromatic, monosubstituted phenol antioxidant generated during differentiation of neuroblastoma cells.

HIV gp120 254-274, a conserved fragment of the envelope glycoprotein gp120 from the human immunodeficiency virus (HIV), displays immunosilent activity [1].

NCX-274 is a ROCK inhibitor and NO-donating anti-glaucoma agent

ABI-274 is a novel potent colchicine binding site inhibitor (CBSI) and tubulin inhibitor.

GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.

FD274 is a potent dual PI3K/mTOR inhibitor with inhibitory effects on PI3Kα/β/γ/δ and mTOR, with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM, respectively. FD274 showed significant antiproliferative activity in AML cell line antiproliferative assays. FD274 exhibited dose-dependent pit tumor growth activity in an HL-60 xenograft model. FD274 has potential for use in acute myeloid leukemia studies.

D-threo-PPMP is a glucosylceramide (GlyCer) synthetase inhibitor.1,2It is the active enanantiomer and enzymatic inhibitory component of the racemic DL-threo-PPMP . In MDCK kidney epithelial cells, D-threo-PPMP induces a 70% reduction in cell growthin vitroat 20 μM and significantly inhibits DNA synthesis at 3 μM.3[Matreya, LLC. Catalog No. 1865] 1.Shen, W., Henry, A.G., Paumier, K.L., et al.Inhibition of glucosylceramide synthase stimulates autophagy flux in neuronsJ. Neurochem.129(5)884-894(2014) 2.Lee, L., Abe, A., and Shayman, J.A.Improved inhibitors of glucosylceramide synthaseJ. Biol. Chem.274(21)14662-14669(1999) 3.Abe, A., Inokuchi, J.-i., Jimbo, M., et al.Improved inhibitors of glucosylceramide synthaseJ. Biochem.111(2)191-196(1992)

Enpp-1-IN-17 (example 274) is a potent inhibitor of ENPP1, with inhibition constants (Ki values) ranging from 100 nM to 1 μM for cGAMP hydrolysis and greater than 1 μM for ATP hydrolysis, demonstrating a selectivity ratio of over 6.4 favoring cGAMP hydrolysis inhibition [1].