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Pathways Recommended:	Stem Cell/Wnt Cell Cycle/DNA Damage

Results for "

Caco-2 cell model

" in MedChemExpress (MCE) Product Catalog:

By Targets:	NAMPT (1) Akt (1) Apoptosis (2) Bacterial (2) c-Kit (1) CDK (1) Collagen (1) Cytochrome P450 (1) DNA/RNA Synthesis (3) Drug Intermediate (1) FLT3 (1) Heme Oxygenase (HO) (1) HIF/HIF Prolyl-Hydroxylase (1) Hippo (MST) (1) Interleukin Related (3) JAK (2) Keap1-Nrf2 (1) Methylenetetrahydrofolate Dehydrogenase (MTHFD) (1) mTOR (1) NF-κB (1) NOD-like Receptor (NLR) (1) p38 MAPK (1) PD-1/PD-L1 (1) PDGFR (1) Phosphatase (1) Phosphodiesterase (PDE) (1) PI3K (1) Reactive Oxygen Species (ROS) (1) STAT (1) STING (1) TGF-beta/Smad (1) Toll-like Receptor (TLR) (1) Topoisomerase (1) VD/VDR (1)
By Research Areas:	Cancer (9) Infection (2) Inflammation/Immunology (5) Metabolic Disease (3) Neurological Disease (2)

By Targets:

NAMPT (1)

Akt (1)

Apoptosis (2)

Bacterial (2)

c-Kit (1)

CDK (1)

Collagen (1)

Cytochrome P450 (1)

DNA/RNA Synthesis (3)

Drug Intermediate (1)

FLT3 (1)

Heme Oxygenase (HO) (1)

HIF/HIF Prolyl-Hydroxylase (1)

Hippo (MST) (1)

Interleukin Related (3)

JAK (2)

Keap1-Nrf2 (1)

Methylenetetrahydrofolate Dehydrogenase (MTHFD) (1)

mTOR (1)

NF-κB (1)

NOD-like Receptor (NLR) (1)

p38 MAPK (1)

PD-1/PD-L1 (1)

PDGFR (1)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

PI3K (1)

Reactive Oxygen Species (ROS) (1)

STAT (1)

STING (1)

TGF-beta/Smad (1)

Toll-like Receptor (TLR) (1)

Topoisomerase (1)

VD/VDR (1)

By Research Areas:

Cancer (9)

Infection (2)

Inflammation/Immunology (5)

Metabolic Disease (3)

Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Targets Recommended: Programmed Cell Death 4 (PDCD4) Itk TOPK NAMPT ALCAM/CD166 GDNF Receptor BCL6 Tim3 VISTA BMI1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15163

Zotiraciclib 2 Publications Verification TG02; SB1317	JAK CDK FLT3	Cancer
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC₅₀ values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, *B-cell* lymphoma**, advanced leukemia, acute leukemia and multiple myeloma .

HY-N2217

Rotundic acid	Akt mTOR p38 MAPK Apoptosis Phosphatase Interleukin Related NF-κB PI3K Keap1-Nrf2 Heme Oxygenase (HO) Toll-like Receptor (TLR) Reactive Oxygen Species (ROS)	Metabolic Disease Inflammation/Immunology Cancer
Rotundic acid is an orally effective triterpenoid with a K_d value of 51.3 µM for PTP1B. Rotundic acid downregulates the AKT/mTOR pro-survival pathway and modulates the MAPK pathway. Rotundic acid induces cell cycle S-phase arrest, DNA damage and apoptosis; it inhibits migration, invasion, angiogenesis and proliferation of cancer cells. Rotundic acid improves leptin sensitivity, regulates gut microbiota and reduces cellular senescence. Rotundic acid can be used in research related to hepatocellular carcinoma, obesity, aging, acute lung injury and type 2 diabetes .

HY-170522

ISM012-042	HIF/HIF Prolyl-Hydroxylase	Inflammation/Immunology
ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC₅₀ values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases .

HY-158346

RP-2119	DNA/RNA Synthesis	Cancer
RP-2119 is an orally bioactive Polymerase Theta (Polθ) inhibitor, with an IC₅₀ of 0.7 nM against human Polθ ATPase. RP-2119 reduces Polθ activity and exerts antiproliferative effects in BRCA2-deficient cancer cells. RP-2119 exhibits antitumor activity in BRCA2-deficient cancer cell xenograft mouse models . RP-2119 can be used for the research of cancer and homologous recombination-deficient cancers, including brca1/brca2-mutant cancers and shld2-mutant cancers .

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 .

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 .

HY-162239

Anticancer agent 187	Drug Intermediate	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 .

HY-172826

Anti-MRSA agent 26	Bacterial	Infection
Anti-MRSA agent 26 is a potent anti-MRSA agent with MIC <0.015 μg/mL. Anti-MRSA agent 26 has superior activity against a broad range of Gram-positive pathogens and shows no cytotoxicity in three mammalian cell lines (Caco-2, DU-145 and MDCKII MDR1 cells) at 10 μM. Anti-MRSA agent 26 has a robust TAP pharmacophore and an excellent antibacterial activity in Staphylococcus aureus skin infection mice model .

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 .

HY-168491

Enpp-1-IN-25	Phosphodiesterase (PDE) STING PD-1/PD-L1	Cancer
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC₅₀ of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .

HY-168729

Antibacterial agent 256	Bacterial	Infection
Antibacterial agent 256 (Compound C09) is an inhibitor for type I signal peptidase (SPase I). Antibacterial agent 256 inhibits gram-positive bacteria, that inhibits S. aureus ATCC 29213, E. faecium QF31, E. faecalis SF23-1 and S. suis P1/7, with MIC of 1-16 μg/mL. Antibacterial agent 256 exhibits cytotoxicity in cancer cell HEp-2 and Caco-2 with CC₅₀ of 14.65 μg/mL and 21.93 μg/mL. Antibacterial agent 256 exhibits a hemolytic activity on mouse RBCs, with an HC₅₀ of 13.29 μg/mL. Antibacterial agent 256 ameliorates the MRSA skin infection in mouse model .

HY-182356

MTHFD1/2-IN-1	Methylenetetrahydrofolate Dehydrogenase (MTHFD)	Cancer
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC₅₀ values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable *Caco-2* permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .

HY-182043

BLU-654	c-Kit PDGFR	Cancer
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT ^V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT ^V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .

HY-181863

Nampt-IN-18	NAMPT DNA/RNA Synthesis Apoptosis	Cancer
Nampt-IN-18 (Compound Q24) is an orally active NAMPT inhibitor with an IC₅₀ of 8.0 nM against hNAMPT. Nampt-IN-18 inhibits NAMPT enzymatic activity. Nampt-IN-18 inhibits DNA synthesis and induces Apoptosis. Nampt-IN-18 exhibits anticancer activity against gastric cancer and colorectal cancer. Nampt-IN-18 can be used for the research of gastrointestinal cancers .

HY-124640

SMN2 modulator-1	DNA/RNA Synthesis	Neurological Disease
SMN2 modulator-1 is a brain-penetrant survival motor neuron (SMN) modulator. SMN2 modulator-1 post-translationally stabilizes SMN protein and increases SMN protein levels independent of SMN2 transcription. SMN2 modulator-1 can be used for the research of spinal muscular atrophy^[1].

HY-182038

TGF-β1/Smad3-IN-2	VD/VDR TGF-beta/Smad Collagen Hippo (MST)	Metabolic Disease
TGF-β1/Smad3-IN-2 is an orally active antifibrotic agent. TGF-β1/Smad3-IN-2 has high affinity for VDR and can inhibit the TGFβ/SMAD3 signaling pathway. TGF-β1/Smad3-IN-2 inhibits hepatic stellate cell activation, reduces extracellular matrix deposition, and alleviates liver fibrosis in a bile duct ligation mouse model. TGF-β1/Smad3-IN-2 can be used for the research of liver fibrosis .

HY-183370

JAK2/STAT3-IN-2	JAK STAT Interleukin Related	Inflammation/Immunology
JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis .

HY-186072

NT-0527	NOD-like Receptor (NLR) Interleukin Related Cytochrome P450	Neurological Disease Metabolic Disease Inflammation/Immunology
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .

Rotundic acid	Cardiovascular Disease Triterpenes Structural Classification Classification of Application Fields Plants Aquifoliaceae Microorganisms other families Terpenoids Parameria laevigata (Juss.) Moldenke Inflammation/Immunology Disease Research Fields Source Classification Cancer	Akt mTOR p38 MAPK Apoptosis Phosphatase Interleukin Related NF-κB PI3K Keap1-Nrf2 Heme Oxygenase (HO) Toll-like Receptor (TLR) Reactive Oxygen Species (ROS)
Rotundic acid is an orally effective triterpenoid with a K_d value of 51.3 µM for PTP1B. Rotundic acid downregulates the AKT/mTOR pro-survival pathway and modulates the MAPK pathway. Rotundic acid induces cell cycle S-phase arrest, DNA damage and apoptosis; it inhibits migration, invasion, angiogenesis and proliferation of cancer cells. Rotundic acid improves leptin sensitivity, regulates gut microbiota and reduces cellular senescence. Rotundic acid can be used in research related to hepatocellular carcinoma, obesity, aging, acute lung injury and type 2 diabetes .

Angelol A	Structural Classification Classification of Application Fields Other Diseases Coumarins Phenylpropanoids Umbelliferae Plants Seriphidium transiliense Disease Research Fields Source Classification	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 B	Classification of Application Fields Coumarins Phenylpropanoids Plants Umbelliferae Seriphidium transiliense Disease Research Fields Inflammation/Immunology Source Classification	Others
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 .

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Caco-2 cell model

Inhibitors & Agonists

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