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Caco-2 cells

" in MedChemExpress (MCE) Product Catalog:

75

Inhibitors & Agonists

3

Fluorescent Dye

3

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8

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12

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5

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-14291B
    (2R)-Vildagliptin

    (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 .
    (2R)-Vildagliptin
  • HY-13749A
    Sitagliptin phosphate
    Maximum Cited Publications
    18 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
    18 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-13749
    Sitagliptin
    Maximum Cited Publications
    18 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-W009141
    1-Monopalmitin

    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-14291A
    Vildagliptin dihydrate

    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-14291R
    Vildagliptin (Standard)

    		Dipeptidyl Peptidase Ferroptosis Apoptosis Metabolic Disease
    Vildagliptin (Standard) is the analytical standard of Vildagliptin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-14291S2
    Vildagliptin-13C5,15N

    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 .
    Vildagliptin-13C5,15N
  • HY-138068
    L-Tryptophanylglycine

    		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-121598
    Actisomide

    SC-36602

    		 Apoptosis Cardiovascular Disease
    Actisomide (SC-36602) is an antiarrhythmic agent. Absorption of actisomide in rats and its in vitro uptake in CaCo-2 cells are pH-dependent .
    Actisomide
  • HY-N4236
    Angelol A

    		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
    Angelol B

    		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)-Sitagliptin phosphate

    (S)-MK-0431 phosphate

    		 Dipeptidyl Peptidase Autophagy Metabolic Disease
    (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)-Sitagliptin

    (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
    Sitagliptin-d4 phosphate

    		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
    1-Monopalmitolein

    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
    Sitagliptin-d4 hydrochloride

    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-13749BR
    Sitagliptin phosphate monohydrate (Standard)

    		Dipeptidyl Peptidase Autophagy Metabolic Disease
    Sitagliptin (phosphate monohydrate) (Standard) is the analytical standard of Sitagliptin (phosphate monohydrate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-W010162
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala)

    L-Alanyl-L-alanine; Ala-Ala

    		 Amino Acid Derivatives Others
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) is a nonpolar dipeptide that is absorbed by human intestinal Caco-2 cells. The transport of alanine (Ala), like proton/amino acid symport, can lead to cytoplasmic acidification .
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala)
  • HY-W009141R
    1-Monopalmitin (Standard)

    		P-glycoprotein Cancer
    1-Monopalmitin (Standard) is the analytical standard of 1-Monopalmitin. This product is intended for research and analytical applications. 1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells .
    1-Monopalmitin (Standard)
  • HY-20808
    Antioxidant agent-15

    		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-13749CR
    (S)-Sitagliptin phosphate (Standard)

    		Dipeptidyl Peptidase Autophagy Metabolic Disease
    (S)-Sitagliptin (phosphate) (Standard) is the analytical standard of (S)-Sitagliptin (phosphate). This product is intended for research and analytical applications. (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 (Standard)
  • HY-P4296
    H-Gly-Sar-Sar-OH

    		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 .
    H-Gly-Sar-Sar-OH
  • HY-14291S1
    Vildagliptin-d7

    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
    Vildagliptin-d3

    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
    MAOA-IN-1

    		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
    PHD-IN-1

    		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-111956
    D-Ala-Lys-AMCA

    		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 .
    D-Ala-Lys-AMCA
  • HY-111956B
    D-Ala-Lys-AMCA hydrochloride

    		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 .
    D-Ala-Lys-AMCA hydrochloride
  • HY-N2009
    3-O-Methylgallic acid

    3,4-Dihydroxy-5-methoxybenzoic acid

    		 Apoptosis Caspase Cancer
    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 .
    3-O-Methylgallic acid
  • HY-162239
    Anticancer agent 187

    		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-P5038
    Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)

    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-161845
    Anticancer agent 240

    		Others Cancer
    Anticancer agent 240 (compound 9b) is an 8-quinolinesulfonamide derivative with a cytotoxicity activity. Anticancer agent 240 shows inhibitory activity in Caco-2, SNB-19, A-549, and SKOV-3 cell line IC50 values of 0.26, 0.38, 0.40 and 4.16 μM .
    Anticancer agent 240
  • HY-111956A
    D-Ala-Lys-AMCA TFA

    		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 .
    D-Ala-Lys-AMCA TFA
  • HY-146078
    Antimicrobial agent-1

    		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-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 .
    Lipofermata
  • HY-131914B
    EST64454 maleate

    		Others Inflammation/Immunology
    EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
    EST64454 maleate
  • HY-155337
    eIF4E-IN-6

    		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-D0203
    Basic green 4
    1 Publications Verification

    Malachite green

    		 Fluorescent Dye Others
    Basic green 4 (Malachite green) is a cationic dye that is widely used as a bactericide in aquaculture and is also commonly used in laboratories for the determination of phosphates. Basic green 4 exhibits high cytotoxicity and carcinogenicity to mammalian cells, specifically shown by its IC50 values of 2.03 µM for HEp-2 human laryngeal cells and 13.8 µM for Caco-2 human colorectal adenocarcinoma cells, and it can promote the development of liver tumors. The maximum absorbance wavelength is 621 nm .
    Basic green 4
  • HY-N13063
    Anticancer agent 235

    		Apoptosis Reactive Oxygen Species PI3K Akt Cancer
    Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116 .
    Anticancer agent 235
  • HY-156965
    BAY-771

    		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-P10329
    KK14(R)

    		Fungal Infection
    KK14(R) is an analog of the de novo synthetic peptide KK14, which exhibits antifungal activity against Fusarium culmorum, Penicillium expansum and Aspergillus niger , with MICs of 6.25, 12.5 and 12.5 μg/mL, respecitvely. KK14(R) exhibits good heat- and pH-stability. KK14(R) exhibits cytotoxicity against cells Caco-2 and RAW264.7 .
    KK14(R)
  • HY-W010162R
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) (Standard)

    		Amino Acid Derivatives Others
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) (Standard) is the analytical standard of H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala). This product is intended for research and analytical applications. H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) is a nonpolar dipeptide that is absorbed by human intestinal Caco-2 cells. The transport of alanine (Ala), like proton/amino acid symport, can lead to cytoplasmic acidification .
    H-Ala-Ala-OH (L-Alanyl-L-alanine; Ala-Ala) (Standard)
  • HY-155328
    GK444

    		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-161628
    Tapcin

    		Topoisomerase Cancer
    Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
    Tapcin
  • HY-130418
    (-)-Domesticine

    		Others Cancer
    (-)-Domesticine is an anti-α-1D-adrenoceptor compound with cytotoxic activity. (-)-Domesticine showed activity in MTS cytotoxicity assays against human colon cancer cell lines HCT-116 and Caco-2. (-)-Domesticine tolerates alkoxy substituents and benzoate functional groups at the C1 position in modifications of its chemical structure. The most potent compounds of (-)-Domesticine have IC50 values in the range of 23-38 μM, similar to the known cytotoxic compound etoposide .
    (-)-Domesticine
  • HY-155027
    DPP-4-IN-8

    		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-169286
    [Au(L4)(CyJohnPhos)]SbF6

    		COX Reactive Oxygen Species Inflammation/Immunology Cancer
    [Au(L4)(CyJohnPhos)]SbF6 is a gold containing complex. [Au(L4)(CyJohnPhos)]SbF6 inhibits cyclooxygenase-1/2 (COX-1/2), inhibits the proliferation (IC50 is 0.98 μM) and induces apoptosis in colon cancer cell Caco2-/TC7. [Au(L4)(CyJohnPhos)]SbF6 is also an inhibitor for thioredoxin reductase (TrxR), thereby exhibits antioxidant activity by modulating ROS levels .
    [Au(L4)(CyJohnPhos)]SbF6
  • HY-157404
    Pim-1/2 kinase inhibitor 2

    		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-1/2 kinase inhibitor 2

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