caco-2

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.

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent DPP-IV inhibitor with an IC50 of 19 nM in Caco-2 cell extracts.

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.

Guanosine 5'-diphosphate (GDP) as Potential Iron Mobilizer, Preventing the Hepcidin-Ferroportin Interaction and Modulating the Interleukin-6 Stat-3 Pathway.

Guanosine 5'-diphosphate disodium salt (5'-GDP-Na2) is a nucleoside diphosphate, is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulating the interleukin-6 (IL-6) stat-3 pathway.

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Epieriocalyxin A can suppress Caco-2 colon cancer cell growth. It could be a potential drug for colon cancer therapy in the future.

Celiprolol hydrochloride (Selectrol) is a cardioselective beta-1 adrenergic antagonist that has intrinsic sympathomimetic activity. It is used in the management of ANGINA PECTORIS and HYPERTENSION.

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.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.

1. Oleandrin (Folinerin), the principal cardiac glycoside component of PBI-524, can quantitatively account for regulation of BDNF at both the protein and transcriptional levels. 2. Oleandrin are known to inhibit the Na, K-ATPase pump, resulting in a consequent increase in calcium influx in heart muscle. 3. Oleandrin has stronger anti-proliferative activity in undifferentiated CaCO-2 cells (IC50, 8.25 nM) , causes an autophagic cell death and altered ERK phosphorylation in undifferentiated.

3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) reduces cell proliferation in Caco-2 cells (IC50 = 24.1 μM) more effectively than anthocyanins and may offer protection against colon cancer after its formation in the gut. It inhibits transcription factors NF-κB, AP-1, STAT-1, and OCT-1, which are known to be activated in colorectal cancer.

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

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

(S)-Sitagliptin phosphate, the less active S-enantiomer of Sitagliptin phosphate, is a high-potency inhibitor of DPP4. It exhibits an IC50 of 19 nM in Caco-2 cell extracts.

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supplemented with α-ESA, apoptosis was induced via lipid peroxidation with an EC50 of 20 μM. It also inhibits DNA polymerases and topoisomerases with IC50s ranging from ~5-20 μM for different isoforms of the enzymes. α-ESA ethyl ester is a neutral, more lipid soluble form of the free acid.

Dodecanoic acid ingenol ester, a natural compound, shows moderate cytotoxicity with IC50 values being 35.59 μM (Caco-2), 24.04 μM (MCF-7), and 22.24 μM (MCF-7 ADM).

Valganciclovir, the L-valyl ester of ganciclovir, is a prodrug effectively converted to ganciclovir in the body, serving as an antiviral medication for cytomegalovirus (CMV) infections. In vitro studies demonstrate that valganciclovir inhibits glycylsarcosine transport mediated by PEPT1 and PEPT2 in Caco-2 and SKPT cells, respectively, with competitive inhibition K(i) values of 1.68±0.30 mM for PEPT1 and 0.043±0.005 mM for PEPT2. Clinical trials indicate valganciclovir's non-inferior efficacy to ganciclovir in pre-emptive therapy for CMV, exhibiting no significant difference in viral clearance rates or toxicity levels between the treatments. Specifically, 89.5% of patients treated with valganciclovir and 83% treated with ganciclovir achieved viral clearance at 28 days (P=0.030 for non-inferiority). Additionally, valganciclovir prophylaxis at 450 mg twice daily prevented CMV reactivation in patients on an alemtuzumab-containing regimen, with none of the 20 patients experiencing reactivation (P=0.004).

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

BMS-183920 is a diacid, potent angiotensin II receptor antagonist that improves Caco-2 cell permeability and in vivo oral absorption. The relative degree of hydrolysis (biological activation) and prodrug metabolism determines whether substantial improveme

Antioxidant agent-15 (Compound 4) demonstrates potent antioxidant inhibition activity with an IC50 value of 15.44 nM, and effectively inhibits tumor cell growth in Hela, Hep G2, and Caco-2 cells, with respective IC50 values of 395.26 nM, 400.4 nM, and 24.6 nM [1].

Compound 166, also referred to as compound 3, exhibits potent anticancer properties, demonstrating significant inhibitory activity against Caco-2 cells with an IC50 value of 9.6 nM [1].

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.

Pachypodol, a methoxyflavonoid isolated from Pogostemon cablin Bentham, has antioxidant and cytoprotective properties and inhibits the growth of CaCo 2 colon cancer cell lines in vitro.Pachypodol protects neonatal rats from anesthesia-induced apoptosis in the developing brain through modulation of the JNK ERK pathway.PDGFRα kinase inhibitory activity in macrophages exposed to STING agonists.

Vildagliptin-d7 is a deuterated compound of Vildagliptin. Vildagliptin has a CAS number of 274901-16-5. Vildagliptin 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.

Ganolucidic acid E effectively suppresses the proliferation of three human cancer cell lines: Caco-2 (colon cancer), HepG2 (hepatocellular carcinoma), and HeLa (cervical cancer).

MAOA-IN-1 (compound 15) is an orally-active monoamine oxidase A (MAOA) inhibitor with cytotoxic effects on prostate cancer cells. It exhibits Caco-2 permeability and reduced central nervous system (CNS) permeability, indicating potential utility in anti-cancer and anti-inflammatory research [1].

8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland microsomes (IC50= 31 μM).4 1.Crombie, L., and Holloway, S.J.The biosynthesis of calendic acid, octadeca-(8E,10E, 12Z)-trienoic, acid, by developing marigold seeds: origins of (E,E,Z) and (Z,E,Z) conjugated triene acids in higher plantsJ. Chem. Soc. Perk. T. 12425-2434(1985) 2.Yasui, Y., Hosokawa, M., Kohno, H., et al.Growth inhibition and apoptosis induction by all-trans-conjugated linolenic acids on human colon cancer cellsAnticancer Res.26(3A)1855-1860(2006) 3.Shinohara, N., Ito, J., Tsuduki, T., et al.Jacaric acid, a linolenic acid isomer with a conjugated triene system, reduces stearoyl-CoA desaturase expression in liver of miceJ. Oleo Sci.61(8)433-441(2012) 4.Nugteren, D.H., and Christ-Hazelhof, E.Naturally occurring conjugated octadecatrienoic acids are strong inhibitors of prostaglandin biosynthesisProstaglandins33(3)403-417(1987)

6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transporter substrate, across Caco-2 cell monolayers (IC50 = 0.7 μM). 6'7'-Epoxybergamottin also has insecticidal properties with a concentration of 5 μg/cm2 leading to 100% mortality of adult olive fruit flies.

Lucidumol A has relatively good effect against aldose reductase with IC50 of 19.1uM. Lucidumol A has cytotoxic activity, it reduced cell growth in three human carcinoma cells (Caco-2, HepG2, and HeLa cells) dose dependently with LC50s from 20.87 to 84.36

MC-70 hydrochloride is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively).

EST64454 is a σ1 receptor (σ1R) antagonist clinical candidate for the treatment of pain. EST64454 shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability.

PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.)

Anticanceragent 235 (Compound 49) functions as a modulator of the PI3K AKT mTOR signaling pathway, enhancing reactive oxygen species (ROS) production and reducing mitochondrial membrane potential, thereby inhibiting the proliferation of cancer cell lines HCT116, Caco-2, AGS, and SMMC-772 with IC50 values ranging from 0.35 to 26.9 μM. Additionally, it induces apoptosis and causes cell cycle arrest at the G2 M phase in HCT-116 cells.

DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM. It inhibits the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells and dose-dependently reduces the expression of chemokines such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) [1].

GK444 (Compound 15a), a selective HDAC1/2 inhibitor with IC50 values of 100 nM and 92 nM for HDAC1 and HDAC2 respectively, demonstrates an IC50 of 4.1 μM in Caco-2 cell inhibition. Additionally, GK444 attenuates TGF-β1-induced COL1A1 mRNA expression in primary normal human lung fibroblasts and mitigates Bleomycin-induced lung fibrosis in mice [1].

Vildagliptin dihydrate (LAF237 dihydrate) is a potent and stable dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells, exhibiting exceptional oral bioavailability and significant antihyperglycemic activity [1].

Antimicrobial Agent-1 (compound 6C) shows strong activity (MIC = 2 μg/mL) against TolC mutant E. coli. Additionally, it synergistically interacts with Colistin to exhibit enhanced activity against Gram-negative bacteria. Importantly, Antimicrobial Agent-1 exhibits no cytotoxic effects on mammalian cell lines. Its MIC values on Caco-2 and Vero cell lines are greater than 128 μg/mL [1].

IWP-051 is a potent, orally active sGC stimulator (EC50 = 290nM). IWP-051 showed >99% plasma protein binding, high metabolic stability, high permeability, and no efflux in a Caco-2 model of intestinal absorption. IWP-051 achieves good alignment of pote

Compound 5b, designated as Pim-1 2 kinase inhibitor 2, acts as a competitive inhibitor of both PIM-1 and PIM-2 kinases, demonstrating IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits potent in-vitro anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2), while showing low cytotoxicity to the normal human lung fibroblast Wi-38 cell line [1].

Anticanceragent 240 (compound 9b) is an 8-quinolinesulfonamide derivative with cytotoxic activity. It exhibits inhibitory effects on the Caco-2, SNB-19, A-549, and SKOV-3 cell lines, with IC50 values of 0.26, 0.38, 0.40, and 4.16 μM, respectively.

Microcystin-LF, a phenylalanine variant of Microcystin-LR, is a bacterial metabolite that exhibits cellular toxicity in Caco-2 cells [1] [2].

9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces apoptosis in T24 bladder cancer cells via production of reactive oxygen species. It also inhibits bacterial fatty acid dioxygenase with a Ki value of 49 nM in vitro.

1-Palmitoleoyl glycerol is a bioactive monoacylglycerol that inhibits P-glycoprotein in Caco-2 cells and induces thymocyte apoptosis.

The absorption and transport of angelol A and Angelol B are passive diffusion as the dominating process in Caco-2 cell monolayer model.

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

Indolelactic acid is a metabolite of tryptophan in Azotobacter vinelandii cultures.