γgt

γ-GT (H-GLA(PNA)-OH) is used as a synthetic substrate for gamma-glutamyltransferase (GGT) to determine GGT activity.

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

GT-653 is a PROTAC degrader targeting lysine-specific demethylase 5B (KDM5B). It induces the degradation of KDM5B via ubiquitin-proteasome pathways, achieving a degradation rate of 68.35% at a concentration of 10 μM. Additionally, GT-653 upregulates H3K4me3 levels and activates type I interferon signaling pathways in prostate cancer cells 22RV1.

GT-02216 is capable of binding allosterically to GCase, thereby enhancing its function. In primary human fibroblasts, it increases GCase activity and decreases Tau accumulation in mutant GBA1 fibroblasts. Additionally, GT-02216 offers protection to hippocampal primary neurons exposed to Tau oligomer in a rat model.

GT 2016 is a H3 receptor antagonist.

Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCPyV receptor. [2] Ganglioside GT1b decreases production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMCs) by 31.4, 30.5, 60, 59.5, and 58%, respectively, when used at a concentration of 10 μM [3] . Ganglioside GT1b mixture contains ganglioside GT1b molecular species with C18:1 and C20:1 sphingoid backbones.

GT-1 (LCB10-0200) is a siderophore-linked cephalosporin compound that effectively combats clinical isolates of various bacterial species, including P. aeruginosa, Klebsiella oxytoca, Proteus spp., Serratia marcescens, and Enterobacter aerogenes.

GT-055 (LCB18-055) is a novel inhibitor of broad-spectrum β-lactamase.

GT-11 is an inhibitor of dihydroceramides (DHCer) desaturase activity.

GT951 is a EAAT2 activator.

GT-2331 is a histamine H3 receptor antagonist.

GT-2394 is a histamine H3 receptor agonist.

GT-2227 is a histamine H3 receptor antagonist.

GT-0198 is a novel glycine transporter 2 inhibitor showed activity in a mouse model of neuropathic pain. GT-0198 inhibited the function of glycine transporter 2 (GlyT2) in human GlyT2-expressing HEK293 cells and did not bind various major transporters or receptors of neurotransmitters in a competitive manner. GT-0198 is considered to be a comparatively selective GlyT2 inhibitor. GT-0198 is a structurally novel GlyT2 inhibitor bearing a phenoxymethylbenzamide moiety with in vivo efficacy in behavioral models of neuropathic pain.

Thifensulfuron-methyl (Pinnacle) is a sulfonylurea (SU) herbicide, has an important role in the removal of broadleaf weeds.

Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorde

Proxalutamide is a potent antagonist of the androgen receptor (AR).

Deferitrin (GT-56-252) is an iron chelator. It potentially for the treatment of thalassemia and iron overload.

Ganglioside GT1b bovine trisodium is a trisialoganglioside that binds to botulinum toxin type A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively. It acts as a TLR2 agonist in spinal cord microglia, leading to microglial activation, increased expression of pro-inflammatory factors, and heightened pain sensitivity. Additionally, Ganglioside GT1b bovine trisodium reduces the production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMC). In neuronal cell models, it elevates extracellular glutamate levels. Ganglioside GT1b bovine trisodium is used in the research of immune and neurological disorders.

Cipralisant maleate is a potent, selective Histamine H3 receptor antagonist.

Indantadol HCl (CHF-3381) is a NMDA antagonist and nonselective MAO inhibitor.

NIBR-1282 is a CCR5 antagonist.

Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

CVS-1578 is a potent serine protease inhibitor, targeting the S2S3 thrombin and FXa subsites.