sgc

SGC-AAK1-1, a potent and selective inhibitor of AAK1 (AP2-associated kinase 1), has an IC50 of 270 nM and a Ki of 9 nM, and serves as a chemical probe.

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).

SGC3027 is an inhibitor of histone methyltransferase,also is a first potent, selective and cell active chemical probe for PRMT7.

SGC0946 is a highly effective and specific DOT1L methyltransferase inhibitor (IC50: 0.3 nM); selectively kill mixed lineage leukemia cells.

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

SGC-AAK1-1N is a potent and selective inhibitor of AAK1 (AP2 associated kinase 1), with an IC50 of 1.8 μM [1].

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 a

SGC-CK2-1 is a highly specific inhibitor of CK2, a inducer of insulin production and secretion in pancreatic β-cells, and can be used in the study of neurodegenerative diseases.

SGC-GAK-1 is a selective cyclin G-associated kinase (GAK) inhibitor (Ki: 3.1 nM).

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

SGC-STK17B-1 is a potent and selective inhibitor of STK17B/DRAK2 kinase.

SGC6870 is a novel potent, selective, and cell-active inhibitor of PRMT6 with IC50 of 77 ± 6 nM, being selective over all other PRMTs and 23 methyltransferases.

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

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.

NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor (IC50: 30 nM and 200 nM for basal and NO-stimulated enzyme activity) commonly used in nitric oxide signaling pathway research. It inhibits sGC activity in mouse cerebellum homogenates and neuronal NO synthase (IC50: 17 nM and 20 nM), inhibits 3-morpholino-sydnonimine (SIN-1)-elicited cyclic GMP formation in human cultured umbilical vein endothelial cells (IC50: 30 nM), and completely inhibits NO-dependent relaxant responses in non-vascular smooth muscle (1 μM). NS-2028 also decreases vascular endothelial growth factor-induced angiogenesis and permeability.

Ataciguat (HMR-1766) (HMR-1766) is a potent and specific soluble guanylate cyclase (sGC) activator.

BAY 41-8543 is a nitric oxide (NO)-independent stimulator of soluble guanylyl cyclase (sGC).

Lificiguat (YC-1) is an nitric oxide (NO)-independent activator of soluble guanylyl cyclase(sGC) and an inhibitor of Hypoxia-inducible factor-1alpha (HIF-1alpha).

Sertindole (Lu 23-174) is an atypical antipsychotic that binds to dopamine D2 receptors and serotonin (5-HT) receptor subtypes 5-HT1D, 5-HT2A, and 5-HT2C, with Kds of 2.7, 20, 0.14, and 6 nM, respectively.

SGC-CLK-1 is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. It effectively inhibits the growth of melanoma and glioblastoma cells.

sGC activator 2 (Compound 16a) acts as an activator of soluble guanylate cyclase (sGC), enhancing the production of cGMP and exhibiting vasoprotective and anti-inflammatory properties.

SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2) with an IC50 of 30 nM. It effectively inhibits AMPK phosphorylation in C4-2 cells, exhibiting an IC50 value of 1.6 µM.

SGC-NSP2hel-1 (RA-0188293) is a potent and selective oral inhibitor of the nsP2 helicase, with a CC50 greater than 250 µM and a selectivity index over 4000. It exhibits broad-spectrum activity against various alphaviruses. In preclinical small animal models of chikungunya virus (CHIKV) disease, SGC-NSP2hel-1 reduces viral replication and limits virus-induced pathology by forming a stable complex with nsP2 and ATP.

SGC-BRDVIII-NC (Compound 35) serves as a negative control for the SMARCA2/4 and PB1 bromodomain (BRD) inhibitors. The binding ability of the protein-ligand is completely eliminated in SGC-BRDVIII-NC through the methylation of the phenolic hydroxyl group. This compound is applicable for research in adipogenesis.