caco-2 cells

ML167 (CID44968231) is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor.

Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Remdesivir (GS-5734) is a nucleoside analog, a broad-spectrum antiviral compound that exerts its activity by inhibiting the RNA-dependent RNA polymerase of viruses. Remdesivir is active against Ebola, SARS, and MERS viruses, and is potentially therapeutic against COVID-19.

Acarbose (BAY g 5421) is a hypoglycemic agent that is an inhibitor of orally active alpha-glucosidase (IC50=11 nM). Acarbose enhances the hypoglycemic effect of sulfonylureas or insulin.

Chenodeoxycholic acid (CDCA) is a bile acid that inhibits 11β-HSD2 with an IC50 value of 22 mM. Chenodeoxycholic acid acts as a detergent to dissolve fat for intestinal absorption and is reabsorbed by the small intestine. Chenodeoxycholic acid is used as a choledocholithiasis, choledocholithiasis and laxative, as well as to prevent or dissolve gallstones.

Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Chlorogenic acid is a natural phenol found in honeysuckle. Chlorogenic acid has a wide range of biological activities including anti-inflammatory, antioxidant, antitumor, antimicrobial, and neuroprotective.

Palmitic acid (Cetylic acid) is a natural product, a common saturated fatty acid found in animals, plants and microorganisms. Palmitic acid has antitumor activity.

Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein serine/threonine calmodulin phosphatases (IC50=21 μM), enhances transferrin receptor-mediated transcytosis in Caco-2 cells, and increases the hypoglycemic effect of oral insulin-transferrin. hypoglycemic effect.

Levofloxacin ((-)-Ofloxacin) is a synthetic fluoroquinolone antibiotic that inhibits the superhelical activity of bacterial DNA rotamase and prevents DNA replication. Levofloxacin is a broad-spectrum antibiotic used for the treatment of a wide range of bacterial infections.

Mitoxantrone (mitozantrone) is an anthracenedione antibiotic with antineoplastic activity. Mitoxantrone intercalates into and crosslinks DNA, thereby disrupting DNA and RNA replication. This agent also binds to topoisomerase II, resulting in DNA strand breaks and inhibition of DNA repair. Mitoxantrone is less cardiotoxic compared to doxorubicin.

Urolithin A is a natural product, a metabolite of ellagic acid, which inhibits DNA synthesis and induces apoptosis and autophagy. Urolithin A exhibits antioxidant, anti-inflammatory and antitumor activities.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Cucurbitacin I 2-glucoside is a natural product with cytotoxic effects on HSC-T6, Caco-2, and HEPG2 cells.

D-Ala-Lys-AMCA hydrochloride, a known substrate of proton-coupled oligopeptide transporter 1 (PEPT1), emits blue fluorescence and may be transported into Caco-2 cells and liver cancer cells.

Antibacterialagent 256 (Compound C09) is an inhibitor of Type I signal peptidase (SPase I). It targets Gram-positive bacteria, effectively inhibiting S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1, and S. suis P1 7, with MIC values ranging from 1-16 μg mL. In cancer cells HEp-2 and Caco-2, Antibacterialagent 256 exhibits cytotoxicity with CC50 values of 14.65 μg mL and 21.93 μg mL, respectively. Additionally, it shows hemolytic activity on mouse red blood cells with an HC50 of 13.29 μg mL and can improve MRSA skin infections in mouse models.

VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.

GSK-3β inhibitor23 (Compound 11726169) is an inhibitor of glycogen synthase kinase 3 (GSK-3), effectively inhibiting GSK-3β and GSK-3α with IC50 values of 12.1 nM and 18.8 nM, respectively. It demonstrates antiviral activity against HIV1 and exhibits good metabolic stability in mouse and human liver microsomes and plasma, although it has poor permeability in Caco-2 cells, indicating potentially low oral bioavailability.

ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 μM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.

Anticanceragent 271 (compound 5C) exhibits antiproliferative activity against lung cancer (A549), colon cancer (Caco-2) cell lines, and human lung fibroblasts (WI38), with an IC50 value of 9.18 μM for A549 cells. This compound can downregulate PI3K and mTOR gene expression and is applicable in cancer research.

Digitonin is a natural product of the glycoside family and is a detergent. Digitonin has antitumor activity, binds to cholesterol molecules to increase the permeability of cell membranes, and is active in the cleavage of cell membranes in a wide range of cells.