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Caco-2 cells

" in MedChemExpress (MCE) Product Catalog:

56

Inhibitors & Agonists

3

Fluorescent Dye

1

Biochemical Assay Reagents

7

Peptides

8

Natural
Products

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
    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-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-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-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
    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-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-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-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-N11680
    Microcystin-LF

    		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 .
    Microcystin-LF
  • 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
    (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-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-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-N2009
    3-O-Methylgallic acid

    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 .
    3-O-Methylgallic acid
  • 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-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-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-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-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-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-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-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
  • HY-155478
    Androgen receptor-IN-6

    		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-N3121
    Pachypodol

    		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) .
    Pachypodol
  • HY-156253
    Anticancer agent 166

    		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-15951
    ML167

    CID44968231; NCGC00188654

    		 CDK DYRK Cancer
    ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B .
    ML167
  • HY-160160
    BAY-5516

    		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
  • HY-A0032A
    Valganciclovir hydrochloride

    		CMV Infection Inflammation/Immunology
    Valganciclovir hydrochloride is an orally active antiviral agent. Valganciclovir hydrochloride can inhibit the growth of adenoviruses and have a protective effect on immunosuppressed hamsters. Valganciclovir hydrochloride can be used for the research of Cytomegalovirus .
    Valganciclovir hydrochloride
  • HY-145147A
    AAA-10 formic

    		Bacterial Infection
    AAA-10 formic is an orally active gut bacterial bile salt hydrolases (BSH) inhibitor, with IC50s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH, respectively .
    AAA-10 formic
  • HY-145147
    AAA-10

    		Bacterial Infection
    AAA-10 is an orally active gut bacterial bile salt hydrolases (BSH) inhibitor, with IC50s of 10 nM, 80 nM against B. theta rBSH and B. longum rBSH respectively .
    AAA-10
  • HY-151133
    Antiparasitic agent-9

    		Parasite Infection
    Antiparasitic agent-9 (compound 47) is an orally active and potent antiparasitic agent. Antiparasitic agent-9 shows antiparasitic activity against the human parasite .
    Antiparasitic agent-9
  • HY-163402
    EGFR-IN-108 chloride

    		EGFR Apoptosis Cancer
    EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
    EGFR-IN-108 chloride
  • HY-113099
    Indolelactic acid
    2 Publications Verification

    Indole-3-lactic acid

    		 Endogenous Metabolite Inflammation/Immunology
    Indolelactic acid (Indole-3-lactic acid) is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures. Indolelactic acid has anti-inflammation and potential anti-viral activity .
    Indolelactic acid
  • HY-149940
    SIMR3030

    		SARS-CoV Infection
    SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice .
    SIMR3030
  • HY-P0185
    Endomorphin 1
    1 Publications Verification

    		 Opioid Receptor Neurological Disease
    Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
    Endomorphin 1
  • HY-N6684
    Deoxynivalenol
    4 Publications Verification

    Vomitoxin

    		 Others Metabolic Disease
    Deoxynivalenol, an orally active mycotoxin of the trichothecenes family, crosses the intestinal mucosa by a paracellular pathway through the tight junctions. The Deoxynivalenol transport is not affected by P-glycoprotein (PgP) or multidrug resistance-associated proteins (MRPs) inhibitors .
    Deoxynivalenol

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