gi

GI-560192 (RL-0070933) is a potent smo cilial modulator with an EC50 value of 0.02 µM. GI-560192 modulates the translocation and/or accumulation of smoothened to the primary cilia by hedgehog signaling pathway.

GI 181771 is an agonist of the cholecystokinin 1 receptor. GI 181771 can be used in studies about obesity.

α-Conotoxin GI acetate is a competitive antagonist of the muscle-type nicotinic acetylcholine receptors (nAChR).

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838

GI-129471 is a metalloproteinase inhibitor, specifically blocking TNF-alpha secretion both in vitro and in vivo.

GI254023X is a MMP9 and ADAM10 inhibitor with IC50 values ​​of 2.5 and 5.3 nM, respectively. GI254023X can also significantly inhibit the proliferation of Jurkat cells and induce apoptosis.

Farglitazar (GI-262570) is a PPAR-γ agonist and insulin sensitizer that inhibits stellate cell activation by activating receptor γ via oxidative enzymes proliferators and is used in the study of diabetes.

Dutasteride (GI 198745) is a 5-alpha-reductase inhibitor that inhibits both type-1 and type2 isoforms of the enzyme and is used to treat benign prostatic hyperplasia.

Ro 31-9790, a synthetic inhibitor of metalloproteinase (MMP), is designed to target and inhibit the action of MMP enzymes.

Lamivudine sulfoxide, (R)- is a metabolite of Lamivudine. Lamivudine is a potent nucleoside reverse transcriptase inhibitor and antiviral agent used for the treatment of chronic hepatitis B.

Lurtotecan (GI147211) is a semisynthetic Camptothecin analog. Lurtotecan is a topoisomerase I inhibitor with anticancer effects.

PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.

GI-Y2 is a GSDMD inhibitor that suppresses macrophage pyroptosis induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 dose-dependently reduces atherosclerotic plaques and decreases lesion size and fibrosis in the aortic root of ApoE-/- mice. GI-Y2 holds potential for research in pyroptosis and cardiovascular diseases, such as atherosclerosis.

GI261520A is a potent egfr/erbb2 dual inhibitor

Numidargistat dihydrochloride (CB-1158 dihydrochloride) is an orally active and highly effective arginase (ARG1) inhibitor, an immuno-oncology agent that inhibits TGF-β2-induced subcapsular cataract by reducing the proliferation of lens epithelial cells (LEC) and decreasing the expression of fibronectin, α-SMA, collagen 1A1, and vimentin.

Rezafungin (SP-3025) is a broad-spectrum and long-lasting echinocandin with potent antifungal activity against Candida, Aspergillus and Pneumocystis.

Fructose-arginine is a non-saponin molecule from Korean Red Ginseng that attenuates AIM2 inflammatory vesicle activation.

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

AGI-25696 is an inhibitor of methionine adenosyltransferase 2A (MATA2). AGI-25696 blocks the growth of MTAP-deleted tumors in vivo and can be used for studies about the treatment of cancer.

Giredestrant tartrate (Estrogen receptor antagonist 1) is a novel, orally active, selective and effective non-steroidal estrogen receptor antagonist. Giredestrant tartrate strongly binds to ER, resulting in the failure of ER to activate the transcription of targeted genes and promoting the degradation of ER protein. Giredestrant tartrate can be used to treat tumor diseases.