pancreatic α

Carbidopa monohydrate (S(-)-Carbidopa) is an inhibitor of DOPA decarboxylase, preventing the conversion of levodopa to dopamine.

Carbidopa (Lodosyn) is an aromatic-L-amino-acid decarboxylase inhibitor (IC50: 29±2 μM). It is used in PARKINSON DISEASE to reduce peripheral adverse effects of LEVODOPA.

PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.

ABzOH is a benzoic acid derivative, similar in structure to non-steroidal anti-inflammatory drugs such as aspirin, with anti-inflammatory, anti-tumor and anti-proliferative effects. ABzOH can not only inhibit the expression of tumor necrosis factor-α (TNF-a), interleukin-1β (IL-1β), interleukin-6 (IL-6) and other pro-inflammatory cytokines, but also inhibit breast cancer, lung cancer and pancreatic cancer.

1. Ethyl trans-caffeate (Caffeic Acid Ethyl Ester) has anti-inflammatory activity. 2. Ethyl trans-caffeate may as a promising natural compound for future application in chronic liver disease. 3. Ethyl trans-caffeate is a potent chemopreventive compound against skin carcinogenesis caused by solar UV exposure. 4. Ethyl trans-caffeate is the high-resolution structures of representative inhibitors in complex with human pancreatic α-amylase. 5. Ethyl trans-caffeate strongly inhibits neoplastic transformation of JB6 Cl41 cells without toxicity. PI3K, ERK1 2, and p38 kinase activities were suppressed by direct binding with HOEC in vitro.

Sanggenon C is a flavanone Diels-Alder adduct compound isolated from the root bark of Morus alba. Sanggenon C can inhibit NF-κB activity, inhibit the expression of inducible nitric oxide synthase in RAW264.7 cells, and inhibit tumor necrosis factor-α-stimulated cell adhesion and vascular cell adhesion molecule-1 expression; Sanggenon C also has antioxidant and anti-inflammatory effects, and also has the effect of inhibiting pancreatic lipase. [1,2]

Glucagon (1-29), bovine, human, porcine is a hormone produced by pancreatic α-cells with glucagon activity, which promotes glycogenolysis and gluconeogenesis, and is used in the study of obesity and diabetes.

Glucagon (1-29), bovine, human, porcine hydrochloride (Porcine glucagon hydrochloride) is a peptide hormone produced by pancreatic α-cells that activates HNF4α, increases HNF4α phosphorylation, and stimulates gluconeogenesis.

WB403 is a TGR5 activator. WB403 significantly decreases fasting blood glucose, postprandial blood glucose and HbA1c, improves glucose tolerance in type 2 diabetic mice. WB403 increases pancreatic β-cells and restores the normal distribution pattern of α-

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr-/-) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

Rhein-13C4 is intended for use as an internal standard for the quantification of rhein by GC- or LC-MS. Rhein is an anti-inflammatory anthraquinone found in rhubarb and is the bioactive derivative of its prodrug diacerein . At 10 μM, rhein inhibits IL-1β signaling, suppressing signaling through NF-κB, and reduces the expression of the matrix metalloproteases MMP-1 and MMP-13.1 It inhibits IKKβ (IC50 = 11.8 μM), decreasing iNOS and IL-6 expression in LPS-stimulated macrophages but paradoxically increasing TNF-α, IL-1β, and HMBG1 expression.2 Rhein shows efficacy against pancreatic fibrosis, chronic pancreatitis, and hyperglycemia-induced pancreatic β-cell apoptosis.3,4 It also inhibits angiogenesis of breast cancer cells under normoxic and hypoxic conditions.5

G3-CNP is a substrate for α-amylase and the hydrolysis product is 2-chloro-4-nitrophenol, which can be used to determine the enzyme activity by colorimetric assay at 405 nm.

Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg ml, respectively) but does not inhibit fatty acid amide hydrolase (FAAH) or KIAA1363 (IC50s = >100 µM for both). Orlistat decreases ionomycin-induced production of the endocannabinoid 2-arachidonoyl glycerol (2-AG) in N18TG2 murine neuroblastoma cells when used at a concentration of 1 µM. It also inhibits fatty acid synthase (FASN; Kiapp = ~0.1 µM for the human enzyme) and the proliferation of PC3 prostate cancer cells in a concentration-dependent manner. Orlistat (10 mg kg) decreases serum cholesterol levels and total bod......

Rosolic Acid serves as an Nrf2 activator and influences its downstream targets, enhancing angiogenic factor levels while reducing inflammation (TNF-α and IL-1β) and apoptotic markers (CXCL10 and CCL2). This compound not only facilitates the restoration of pancreatic cell function but also shields endothelial cells (ECs) from endoplasmic reticulum stress.

HPA-IN-1 (Compound 1) is a potent and selective inhibitor of human pancreatic α-amylase (HPA), with IC50 values of 12.0 μM for HPA and 410.4 μM for α-glucosidase [1].

Certepetide (CEND-1), also known as iRGD, is a bifunctional cyclic peptide that enhances tumor penetration. By interacting with alphav-integrins through its RGD motif and activating NRP-1, it transforms the solid tumor microenvironment into a temporary conduit for therapeutic agents. This property facilitates Certepetide's accumulation in tumors, making it a valuable tool in researching pancreatic cancer and other solid tumors [1] [2] [3].

α-Thevetin B (Compound 24), a cardiac glycoside extracted from Thevetia peruviana, has applications in research concerning lung, gastric, and pancreatic cancers [1].

5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8), extracted from Dendrobium infundibulum (D. infundibulum), shows no inhibitory effects on α-glucosidase and pancreatic lipase [1].

Glucagon, a peptide hormone derived from proglucagon in pancreatic α cells, regulates glucose metabolism. It stimulates glucose production in rat hepatocytes ex vivo and enhances glucose output from perfused rat livers through elevated gluconeogenesis and glycogenolysis, while reducing glycolysis, and raises plasma glucose levels in rats. Glucagon secretion decreases following food intake in healthy rats and humans, yet remains unchanged or increases in individuals with type 2 diabetes.