gpat

GPAT-IN-1 is a glycerol 3-phosphate acyltransferase (GPAT) inhibitor, which can be used to study obesity and diabetes.

FSG67 is a glycerol 3-phosphate acyltransferase (GPAT) and glycerol-3-phosphate acyltransferase, mitochondrial (GPAM) inhibitor that attenuates hepatic regeneration following acetaminophen overdose by altering GSK3β and Wnt/β-catenin signaling.

AGPAT4-IN-1 (Compound CL26) is a covalent AGPAT4 inhibitor with an IC50 of 795 nM. It binds covalently to the Cys228 site of AGPAT4, significantly inhibiting acyltransferase activity, the conversion of LPA to PA, and the downstream mTOR/S6K pathway. AGPAT4-IN-1 enhances the sensitivity of hepatocellular carcinoma (HCC) tumors to Sorafenib and significantly induces apoptosis through synergistic effects. This compound exhibits antitumor activity and reduces tumorigenicity and stem cell characteristics in a hepatocellular carcinoma xenograft mouse model.

LGE-899 (Sonidegib metabolite M48) is a main metabolite of Sonidegib which is an inhibitor of the hedgehog pathway. The Tmax of LGE-899(60 h) is much longer than Sonidegib.

Methyl-β-cyclodextrin (Methyl-beta-cyclodextrin) is a macrocyclic compound utilized as a solubilizer for hydrophobic substances in biological studies, and serves as a lipid raft inhibitor with cholesterol-lowering and potential antitumor activities.

AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2]. AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM.

Diazepinomicin is a secondary metabolite produced by Micromonospora sp. It inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. Diazepinomicin also is an anti-tumor agent for K-Ras mutant models.

PD 128042 (CI 976) is a potent, orally active, and selective ACAT inhibitor (IC50: 73 nM) as well as a lysophospholipid acyltransferase (LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

Ciliobrevin A (HPI-4) is an inhibitor of the hedgehog signaling pathway with an IC50 of less than 10 μM.

Saponin activator. Activates release of Prostaglandin E2 in vitro. Anti-inflammatory agent. Orally active. Active in vivo and in vitro.

RU.521 (RU3205217) is a selective cyclic GMP-AMP synthetase (cGAS) inhibitor (mouse: IC50=0.11 μM), (human: IC50=2.94 μM). RU.521 is an inhibitor of the receptor activated by dsDNA (IC50=700 nM). RU.521 inhibits cGAS-mediated interferon upregulation. RU.521 reduces constitutive interferon expression in macrophages derived from a mouse model of Aicardi-Goutieres syndrome.

Astin C (Asterin), a naturally occurring cyclic peptide that can be extracted from Aster tataricus, specifically blocks IRF3 recruitment at the STING signalosome inhibiting cGAS-STING signaling and innate inflammatory responses triggered by cytoplasmic dna, resulting in mice that are more susceptible to HSV-1 infection and significantly attenuating autoinflammatory responses.

Angoline (6-Methoxyldihydrochelerythrine) hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor(IC50 : 11.56 μM). It inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.