GX

GX-585 is a sulfonamide analog that is a Nav 1.7 channel inhibitor with analgesic activity for the study of neuropathic pain and inflammation.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

GX-674 is a highly potent and selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 value of 0.1 nM measured at -40 mV for the study of inflammatory and neuropathic pain.

GX-936 (PF-05196233) is a selective Nav1.7 inhibitor that binds to the activated state of VSD4 (voltage-sensor domain IV), thereby opposing VSD4 inactivation and inhibiting Nav1.7. It can be used for pain perception research.

Glycinexylidide (GX), the active metabolite of the local anesthetic Lidocaine, exhibits properties significant in inhibiting sodium channels with complex voltage dependence and mitigates the proliferation and spread of gastric cancer cells. GX holds research promise in applications related to anesthesia, cancer, and cardiovascular disease [1].

Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.

Variegatic acid is a natural inhibitor of β-hexosaminidase release and tumor necrosis factor (TNF)-α secretion from rat basophilic leukemia (RBL 2H3) cells, with IC50 values of 10.4 μM and 16.8 μM, respectively, also inhibiting PKC β1 activity with an IC50 value of 36.2 μM.

GX-395 is a novel Nav1.7 inhibitor.

AMK-GX (Immobilized Penicillin G acylase) is a stabilized form of penicillin acylase with enhanced temperature and pH resistance. It exhibits high recovery rates and maintains most of its original activity even after 12 cycles of use. AMK-GX catalyzes the conversion of Penicillin G (PG) into 6-aminopenicillanic acid (6-APA) and 7-amino-desacetoxycephalosporanic acid, which are crucial intermediates in the production of β-lactam antibiotics.

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β/p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

RGX-202 (β-GPA) is a creatine analog that alters skeletal muscle energy expenditure. It reduces cellular ATP, creatine, and phosphocreatine levels and stimulates AMP-activated protein kinase (AMPK), activating PPARγ coactivator 1α (PGC-1α).

VGX-1027 (GIT 27) is an isoxazole compound with various immunomodulatory properties.

AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.

3-Methyl-chuangxinmycin, an antibiotic, inhibits the enzyme responsible for synthesizing tryptophan tRNA (TrpRS), thereby affecting the translation process in both bacteria and mammalian cells. Additionally, it downregulates genes associated with interferon, TNF, and inflammatory responses in RDEB_L1 cells.

Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.

SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.

TGX-155 is a selective PI3K inhibitor.

TGX-221, an effective, specific, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, is utilized for cancer treatment.

MrgX1-Activator-1 is a MrgX1 receptor activator.

NGX-267, a muscarinic M1 agonist, is used potentially for the treatment of Xerostomia, Alzheimer's disease and cognitive.

RGX-104 hydrochloride (SB742881) is a liver X receptor (LXR) agonist with potential immunomodulating and antineoplastic activities. It modulates innate immunity via transcriptional activation of the ApoE gene.

Mrgx2 antagonist-1 is a potent antagonist of Mrgx2 (Mas-related Gene X2) and can be used to study Mrgx2-mediated diseases and disorders.

SGX393 is an inhibitor of the CML mutant Bcr-AblT315I, thereby preempting in vitro resistance when combined with nilotinib or dasatinib.

GXH-II-052 is a potent bivalent inhibitor targeting the bromodomain and extraterminal domain (BET), exhibiting significant binding affinity to various BET proteins, including BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, and BRDT-T, with dissociation constants (Kd) of 28, 9.1, 4.8, 0.6, 8.4, and 2.6 nM, respectively. Additionally, GXH-II-052 demonstrates antiproliferative effects and reduces the expression of c-Myc [1].