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Caco-2

" in MedChemExpress (MCE) Product Catalog:

82

Inhibitors & Agonists

3

Fluorescent Dye

2

Biochemical Assay Reagents

8

Peptides

2

Inhibitory Antibodies

14

Natural
Products

9

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-W009141

    Glyceryl palmitate

    P-glycoprotein Cancer
    1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells .
    1-Monopalmitin
  • HY-14291
    Vildagliptin
    4 Publications Verification

    LAF237; NVP-LAF 237

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
    Vildagliptin
  • HY-156253

    Others Cancer
    Anticancer agent 166 (compound 3) is an anticancer agent with an excellent inhibition activity against Caco-2 (IC50 = 9.6 nM) .
    Anticancer agent 166
  • HY-N11680

    Others Cancer
    Microcystin-LF is a bacterial metabolite. Microcystin-LF is a phenylalanine variant of Microcystin-LR. Microcystin-LF has cellular toxicity on Caco-2 cells [2].
    Microcystin-LF
  • HY-14291A

    LAF237 dihydrate; NVP-LAF 237 dihydrate

    Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity .
    Vildagliptin dihydrate
  • HY-20808

    COX Cancer
    Antioxidant agent-15 (Compound 4) is a potent antioxidant inhibition activity, with the IC50 of 15.44 nM. Antioxidant agent-15 inhibits tumor cell growth in Hela, Hep G2 and Caco-2 cells, with the IC50 of 395.26, 400.4 and 24.6 nM, respectively .
    Antioxidant agent-15
  • HY-14291B

    (2R)-LAF237; (2R)-NVP-LAF 237

    Others Metabolic Disease
    (2R)-Vildagliptin is the isomer of Vildagliptin (HY-14291), and can be used as an experimental control. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity .
    (<em>2</em>R)-Vildagliptin
  • HY-155337

    Others Cancer
    eIF4E-IN-6(compound 4b) is a GMP analogs synthesized to targeteIF4Eand restrain its binding to cap mRNA.eIF4E-IN-6shows cell cytotoxicity against Caco-2, HepG-2,and MCF-7 cells, withIC50values of 31, 27, and 21 μM, respectively .
    eIF4E-IN-6
  • HY-155027

    Dipeptidyl Peptidase TNF Receptor Interleukin Related Inflammation/Immunology Cancer
    DPP-4-IN-8 (compound 27) is a potent and selective DPP4 (dipeptidyl peptidase 4) inhibitor, with a Ki of 0.96 μM. DPP-4-IN-8 blocks the dipeptidase activity of DPP4 in both Caco-2 and HepG-2 cells. DPP-4-IN-8 also dose-dependently suppresses the expression levels of the chemokines tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) .
    DPP-4-IN-8
  • HY-111956

    Fluorescent Dye Cancer
    D-Ala-Lys-AMCA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA can be used for characterizing PEPT1-specific substrates or inhibitors [2].
    D-Ala-Lys-AMCA
  • HY-111956B

    Fluorescent Dye Cancer
    D-Ala-Lys-AMCA hydrochloride is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA hydrochloride may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA hydrochloride can be used for characterizing PEPT1-specific substrates or inhibitors [2].
    D-Ala-Lys-AMCA hydrochloride
  • HY-111956A

    Fluorescent Dye Cancer
    D-Ala-Lys-AMCA TFA is a known proton-coupled oligopeptide transporter 1 (PEPT1) substrate that emits blue fluorescence. D-Ala-Lys-AMCA TFA may be transported into liver cancer cells and Caco-2 cells based on fluorescence analysis. D-Ala-Lys-AMCA TFA can be used for characterizing PEPT1-specific substrates or inhibitors [2].
    D-Ala-Lys-AMCA TFA
  • HY-13749A
    Sitagliptin phosphate
    Maximum Cited Publications
    14 Publications Verification

    MK-0431 phosphate

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    Sitagliptin phosphate
  • HY-13749B
    Sitagliptin phosphate monohydrate
    Maximum Cited Publications
    14 Publications Verification

    MK-0431 phosphate monohydrate

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    Sitagliptin phosphate monohydrate
  • HY-138068

    Others Metabolic Disease
    L-Tryptophanylglycine (Trp-gly) is a dipeptide that can inhibit Ceronapril uptake by Caco-2 cells, with a Ki of 7.19 mM .
    L-Tryptophanylglycine
  • HY-146078

    Bacterial Infection
    Antimicrobial agent-1 (compound 6C) possesses potent activity against TolC mutant E. coli with an MIC value of 2 μg/mL. Antimicrobial agent-1 and Colistin exhibit synergistic activity against Gram-negative bacteria. Antimicrobial agent-1 has no cytotoxicity on mammalian cell lines, with MICs > 128 μg/mL in Caco-2 and Vero cell lines .
    Antimicrobial agent-1
  • HY-13749
    Sitagliptin
    Maximum Cited Publications
    14 Publications Verification

    MK-0431

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin (MK-0431) is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    Sitagliptin
  • HY-14291S2

    LAF237-13C5,15N; NVP-LAF 237-13C5,15N

    Isotope-Labeled Compounds Metabolic Disease
    Vildagliptin- 13C5, 15N (LAF237- 13C5, 15N; NVP-LAF 237- 13C5, 15N) is a 13C- and 15N-labeled Vildagliptin (HY-14291). Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity [2].
    Vildagliptin-13C5,15N
  • HY-N4236

    Others Others
    Angelol A is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model .
    Angelol A
  • HY-N4235

    Others Inflammation/Immunology
    Angelol B is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model .
    Angelol B
  • HY-13749C

    (S)-MK-0431 phosphate

    (S)-Sitagliptin phosphate is the less active S-enantiomer of Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    (S)-Sitagliptin phosphate
  • HY-13749D

    (Rac)-MK-0431

    Autophagy Dipeptidyl Peptidase Metabolic Disease
    (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts .
    (Rac)-Sitagliptin
  • HY-13749AS

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin-d4 (phosphate) is the deuterium labeled Sitagliptin phosphate. Sitagliptin phosphate (MK-0431 phosphate) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[1][2].
    Sitagliptin-d4 phosphate
  • HY-133948

    Glyceryl palmitoleate

    Biochemical Assay Reagents Others
    1-Palmitoleoyl glycerol is a biologically active monoacylglycerol. It increases daunomycin accumulation, shown to inhibit P-glycoprotein in Caco-2 cells. 1-Palmitoleoyl glycerol induces thymocyte apoptosis.
    1-Monopalmitolein
  • HY-13749S1

    MK-0431-d4 hydrochloride

    Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin-d4 (hydrochloride) is the deuterium labeled Sitagliptin[1]. Sitagliptin (MK-0431) is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts[2].
    Sitagliptin-d4 hydrochloride
  • HY-N3197

    (+)-Neostenine

    P-glycoprotein Cancer
    Neostenine is a stenine-type Stemona alkaloid, with antitussive activity. Neostenine is also a substrate of P-glycoprotein with high absorptive permeability in Caco-2 monolayer model. Neostenine also shows oral activity for intestinal application [2].
    Neostenine
  • HY-163042

    Bacterial Infection
    HSGN-218 is an antibacterial agent with low Caco-2 permeability. HSGN-218 efficiently inhibits the growth of different C. difficile species with MIC values ranging from 0.007 μM to 0.07 μM.
    HSGN-218
  • HY-P4296

    Amino Acid Derivatives Others
    H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation [2] .
    H-Gly-Sar-Sar-OH
  • HY-14291S1

    LAF237-d7; NVP-LAF 237-d7

    Isotope-Labeled Compounds Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d7 is deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1].
    Vildagliptin-d7
  • HY-14291S

    LAF237-d3; NVP-LAF 237-d3

    Isotope-Labeled Compounds Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin-d3 is the deuterium labeled Vildagliptin. Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity[1][2].
    Vildagliptin-d3
  • HY-149408

    Monoamine Oxidase Cancer
    MAOA-IN-1 (compound 15) is an orally active MAOA inhibitor with cytotoxicity against prostate cancer cells. MAOA-IN-1 has Caco-2 permeability and lower CNS permeability. MAOA-IN-1 can be further used in the research of anti-cancer and anti-inflammatory indications .
    MAOA-IN-1
  • HY-156526

    HIF/HIF Prolyl-Hydroxylase Others
    PHD-IN-1 (compound 80) is a potent inhibitor of PHD2,with an IC50 value of ≤5 nM. PHD-IN-1 shows EC50s of 2.5 μM in EPO Elisa assay both in Caco2-HIFla-HiBiT-clone-1 cells and Hep3B cells,respectively .
    PHD-IN-1
  • HY-P5038

    c(GRGDSP)

    Integrin Cancer
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)
  • HY-116788
    Lipofermata
    2 Publications Verification

    Bacterial Infection
    Lipofermata is a fatty acid transport protein 2 (FATP2) inhibitor. Lipofermata shows fatty acid transport inhibition with an IC50 of 4.84 μM in Caco-2 cells. Lipofermata, an analog of spiro-indoline-thadiazole, shows zinc-specific suppression of antibacterial activity. Lipofermata perturbs zinc homeostasis in E. coli K-12 with a MIC of 16 μM [2] .
    Lipofermata
  • HY-N2009

    3,4-Dihydroxy-5-methoxybenzoic acid

    3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects [2].
    3-O-Methylgallic acid
  • HY-147397

    Pyruvate Kinase Cancer
    PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
    (AC50: the concentration which gives 50% activation of enzyme.)
    PKM<em>2</em> activator 3
  • HY-162239

    Others Cancer
    Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
    Anticancer agent 187
  • HY-156965

    Others Metabolic Disease Cancer
    BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitory activity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
    BAY-771
  • HY-155328

    HDAC Inflammation/Immunology
    GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice .
    GK444
  • HY-162313

    SARS-CoV Infection
    NIP-22c is a novel coronavirus 3CLpro inhibitor. The EC50 for Verona, Calu3, Caco2 and HBTEC-ALI were 4.6, 1.1, 0.1 and 0.6 μM, respectively. NIP-22c has antiviral activity .
    NIP-22c
  • HY-155478

    Androgen Receptor Cancer
    Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
    Androgen receptor-IN-6
  • HY-157404

    Pim Cancer
    Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
    Pim-1/<em>2</em> kinase inhibitor <em>2</em>
  • HY-N3121

    Others Cancer
    Pachypodol exerts antioxidant and cytoprotective effects in HepG2 cells .Pachypodol inhibits the growth of CaCo 2 colon cancer cell line in vitro(IC50 = 185.6 mM) [2].
    Pachypodol
  • HY-152748

    Apoptosis Caspase Cancer
    Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
    Caspase-3/7 activator 1
  • HY-152756

    Apoptosis Caspase Cancer
    Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
    Caspase-3/7 activator <em>2</em>
  • HY-152758

    Apoptosis Caspase Cancer
    Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability .
    Caspase-3/7 activator 3
  • HY-155099

    Dopamine Receptor Arrestin G Protein-coupled Receptor Kinase (GRK) Neurological Disease
    FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin .
    FGH31
  • HY-155186

    SARS-CoV Infection
    SARS-CoV-2 3CLpro-IN-19 (Compound C5a) is a non-covalent, non-peptide SARS-CoV-2 3CLpro inhibitor (IC50s: 0.7 μM). SARS-CoV-2 3CLpro-IN-19 has broad-spectrum activity against Omicron subvariants (BA.5, BQ.1.1, and XBB.1.5) infection in human cells, with EC50 values between 30-69 nM .
    SARS-CoV-<em>2</em> 3CLpro-IN-19
  • HY-161049

    Fungal Infection
    Antifungal agent 89 (compound 28) is a antifungal agent against Cryptococcus neoformans with minimum inhibitory concentration value ranging from 0.8 to 52.17 μM .
    Antifungal agent 89
  • HY-160160

    PPAR Cancer
    BAY-5516 is a inverse-agonist o PPARG, with the IC50 value of 6.1±3.6 nM that has anti-tumor effect .
    BAY-5516

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