gt1

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.

BGT1-IN-1 (compound 9) is an effective inhibitor of BGT1, demonstrating IC50 values of 13.9 µM for hBGT1 and 58.3 µM for GAT3. It exhibits no cytotoxic effects and possesses neuroprotective activity.

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.

BGT1-IN-9 is an M1 muscarinic agonist.

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

UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity.

BPDBA is an effective, selective, and non-competitive inhibitor of the betaine/GABA transporter (BGT-1), displaying inhibitory activity against human BGT-1 and mouse GAT2, with IC50 values of 20 μM and 35 μM, respectively.

Deferiprone (Deferidone) is an Iron Chelator. The mechanism of action of deferiprone is as an Iron Chelating Activity.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Cremophor EL is a nonionic surfactant. cremophor EL inhibits cellular metabolism and suppresses UGT1A1-mediated rhodopsin glucuronidation.

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

MG-T-19, a TIM-3 inhibitor (KD=0.26 μM), significantly inhibited the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9, and increased the production of TNF-α and IFN-γ in PBMCs, which reactivated the tumor-attacking ability of T cells.

E2730 is an orally active, selective, and non-competitive GABA transporter 1 (GAT1) inhibitor with antiepileptic activity, used in neurological disease research.

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.

FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).

Ledipasvir D-tartrate (GS-5885 D-tartrate) is an HCV NS5A inhibitor that suppresses viral overphosphorylation and replication, and is used for the treatment of hepatitis C virus.

UK-157147 is a substrate for UGT1A1 (Km: 105 μM).

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Grazoprevir is a drug approved for the treatment of hepatitis C. Grazoprevir is a second-generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets.

LGT-1 is a PD-L1 ligand. The compound labeled with 18F shows exceptional specificity and uptake in B16-F10 tumor cells and demonstrates high tumor uptake with relatively low liver uptake in mouse models carrying B16-F10 tumors, while maintaining good stability. LGT-1 can be utilized as a radiotracer for PET imaging of tumor PD-L1 expression.

Grazoprevir, a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets, has good activity against a range of hepatitis C virus genotype variants, including some that are resistant to most currently used antiviral medic

Sergliflozin etabonate (KGT-1251) is an inhibitor of SGLT2 and can be used in studies about type 2 diabetes and obesity.