Epigenetics

SIRT-IN-1 is a potent SIRT1/2/3 inhibitor(IC50s of 15, 10, 33 μM, respectively).

Sirt2-IN-1 is a inhibitor of sirtuin 2 (Sirt2)(IC50 of 163 nM).

SIRT1-IN-1 is a selective inhibitor of SIRT1 with an IC50 of 205 nM. SIRT1-IN-1 is an inhibitor of cytomegalovirus (CMV) with antiviral activity.

SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.

Sinefungin is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7/9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.

Sinapic acid protects the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid with antioxidant role protects cardiac cells and its functions from I/R induced oxidative stress. Sinapic acid is a potentially useful agent for the protection against liver fibrosis and cirrhosis. Sinapic acid prevents the alterations in the levels of lipids and lipoproteins by virtue of its anti-lipidaemic effect in isoproterenol induced myocardial infarcted rats. Sinapic acid ameliorates hyperglycemia through PLC-PKC signals to enhance the glucose utilization in diabetic rats.

Shizukaol D exerts a growth inhibition effect on liver cancer cells in a dose- and time-dependent manner by modulating wnt signalling pathway. Shizukaol D may be used to treat metabolic syndrome, it induces mitochondrial dysfunction by depolarizing the mitochondrial membrane and suppressing energy production, which may result in AMPK activation.

SGC-SMARCA-BRDVIII is a potent and selective inhibitor of SMARCA2, SMARCA4, PB1(2), PB1(3) and PB1(5) with Kds of 35 nM, 36 nM, 3.7 μM, 2.0 μM and 13 nM, respectively.

SGC-iMLLT is a potent and selective MLLT1/3-histone interactions inhibitor(IC50 = 0.26 μM),and is a first-in-class chemical probe displaying cellular target engagement of MLLT1(Kd = 0.129 μM) and MLLT3(Kd = 0.077 μM).

SGC-CBP30 is an effective CREBBP/EP300 inhibitor (IC50: 21/38 nM).

SGC707 is a potent, selective, and cell-active allosteric inhibitor of PRMT3.

SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).

SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

SF2523 is a highly selective and potent inhibitor.

SETDB1-TTD-IN-1 is a potent, selective and endogenous binder competitive inhibitor of SETDB1-TTD with a Kd of 88 nM.

Senaparib is a novel highly potent and selective oral PARP1/2 inhibitor with strong antitumor activity.

Selisistat S-enantiomer is an effective and specific SIRT1 inhibitor (IC50 = 98 nM) and shows >200-fold selectivity against SIRT2/3.

Selisistat R-enantiomer is a SIRT1 inhibitor with much less activity than the R-enantiomer of Selisistat (IC50 of SIRT1 > 100 μM).

Seclidemstat is an effective LSD1 inhibitor, with a mean IC50 of 127 nM.

Scopolin formation is increased by the enhanced activity of PAL. Scopolin can reduce the clinical symptoms of rat AIA by inhibiting inflammation and angiogenesis, and this compound may be a potent agent for angiogenesis related diseases and can serve as a structural base for screening more potent synthetic analogs.