pancreatic β

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.

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Glipizide (CP 28720) is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

Imeglimin (EMD 387008) is an orally available antidiabetic compound that enhances mitochondrial function, enhances insulin secretion, promotes β-cell proliferation and improves pancreatic β-cell survival in mice.

1. Gypsogenin-3-O-glucuronide (Methyl gypsogenin 3-O-beta-D-glucuronopy) shows inhibitory activity toward pancreatic lipase with IC5 value of .29 mM, and the free carboxylic acid groups in position 28 within its chemical structures are required for enhancement of pancreatic lipase inhibition.

RH01687 is a potent β-cell protector , exhibits β-cell-protective activities against endoplasmic reticulum (ER) stress.

Dorzagliatin (HMS5552) is a dual-acting glucokinase (GK) activator. It also improves glycaemic control and pancreatic β-cell function in type 2 diabetes.

Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability.

Mahanimbine is found in the roots, leaves and stems of Murraya koenigii and is an orally active alkaloid extracted from Murraya koenigii. Bifidobacterium bifidum leaves on histopathological changes in pancreatic beta cells of streptozotocin-induced diabetic rats.

LY2090314, an effective GSK-3α β inhibitor (IC50: 1.5 nM 0.9 nM), may improve the efficacy of platinum-based chemotherapy regimens. LY2090314 has been used in trials studying the treatment of Leukemia, Advanced Cancer, and Pancreatic Cancer.

IHMT-MST1-39 is an orally effective MST kinase inhibitor with IC50 values of 42 nM for MST1 and 109 nM for MST2. It activates the AMPK signaling pathway in hepatocytes and inhibits apoptosis in pancreatic β cells. Additionally, IHMT-MST1-39 improves type 1 diabetes in mice induced by Streptozotocin.

Semaglutide is a glucagon-like peptide-1 (GLP-1) receptor agonist. This compound mimics GLP-1 to lower blood glucose levels and stimulates the growth of pancreatic β-cells responsible for insulin production and release. Additionally, Semaglutide inhibits the production of glucagon, a hormone that enhances glycogenolysis [the release of liver-stored carbohydrates] and gluconeogenesis [the synthesis of new glucose]. By reducing appetite and slowing gastric emptying, it also helps decrease food intake and aids in reducing body fat.

WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.

8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac), which are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. It specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2].

Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

Linogliride fumarate is the fumarate salt of Linogliride. Linogliride is a guanidine-based inhibitor of insulin secretion and a structural analog of pirogliride with hypoglycemic activity. It blocks ATP-sensitive potassium channels in the pancreatic beta cell membrane, thereby stimulating insulin secretion and improving glucose tolerance.

BRD0476 is a suppressor of pancreatic β-cell apoptosis. BRD0476 inhibits interferon-gamma (IFN-γ)-induced Janus kinase 2 (JAK2) and signal transducer and activation of transcription 1 (STAT1) signaling to promote β-cell survival. BRD0476 inhibits JAK-STAT

KM10103 exhibits β-cell-protective activities against ER stress, which plays an important role in the decline in pancreatic β cell function and mass observed in type 2 diabetes.

Nephrin is a cell surface signaling receptor protein that regulates podocyte function and plays a role in β-cell survival signaling; it is a protein necessary for the proper functioning of the renal filtration barrier. Nephrin belongs to a family of highl

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-