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

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Caco-2 cell monolayers

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amino Acid Derivatives (1) Angiotensin-converting Enzyme (ACE) (1) Biochemical Assay Reagents (2) Cytochrome P450 (2) DNA/RNA Synthesis (1) Drug Intermediate (1) Drug Metabolite (1) Endogenous Metabolite (2) Ephrin Receptor (1) Eukaryotic Initiation Factor (eIF) (1) FAK (1) FGFR (1) Interleukin Related (1) Kisspeptin Receptor (1) nAChR (1) NOD-like Receptor (NLR) (1) Parasite (1) PDGFR (1) RABV (1) SARS-CoV (1) Thyroid Hormone Receptor (1) VEGFR (1) Virus Protease (1)
By Research Areas:	Cancer (6) Endocrinology (1) Infection (2) Inflammation/Immunology (4) Metabolic Disease (4) Neurological Disease (5)

By Targets:

Amino Acid Derivatives (1)

Angiotensin-converting Enzyme (ACE) (1)

Biochemical Assay Reagents (2)

Cytochrome P450 (2)

DNA/RNA Synthesis (1)

Drug Intermediate (1)

Drug Metabolite (1)

Endogenous Metabolite (2)

Ephrin Receptor (1)

Eukaryotic Initiation Factor (eIF) (1)

FAK (1)

FGFR (1)

Interleukin Related (1)

Kisspeptin Receptor (1)

nAChR (1)

NOD-like Receptor (NLR) (1)

Parasite (1)

PDGFR (1)

RABV (1)

SARS-CoV (1)

Thyroid Hormone Receptor (1)

VEGFR (1)

Virus Protease (1)

By Research Areas:

Cancer (6)

Endocrinology (1)

Infection (2)

Inflammation/Immunology (4)

Metabolic Disease (4)

Neurological Disease (5)

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

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-W096638A

Glycerophosphocholine (S)-Glycerolphosphocholine	Endogenous Metabolite	Neurological Disease Metabolic Disease Cancer
Glycerophosphocholine ((S)-Glycerolphosphocholine) is an orally active metabolite that crosses the blood-brain barrier. Glycerophosphocholine acts as a precursor of acetylcholine, a specific marker for phosphatidylcholine breakdown, a major water-soluble storage form of choline, and an intermediate in phosphatidylcholine metabolism. Glycerophosphocholine is specifically elevated in the cerebrospinal fluid of Alzheimer's disease models, and it also promotes growth hormone secretion and fat oxidation. Glycerophosphocholine is also a potential biomarker for breast cancer .

HY-168046

ALG-055009	Thyroid Hormone Receptor	Metabolic Disease
ALG-055009 is a selective and orally active Thyroid Hormone Receptor Beta (THR-β) agonist with an EC₅₀ of 0.063 μM. ALG-055009 binds to the T3 hormone pocket of human THR-β, forming polar interactions with protein residues. ALG-055009 can lower total cholesterol levels in rats on a high-fat diet. ALG-055009 exhibits high metabolic stability, good permeability, a long in vivo half-life, and limited drug-drug interaction liability. ALG-055009 can be used in studies related to metabolic dysfunction-associated fatty liver disease .

HY-W040203

Decyl β-D-maltopyranoside	Biochemical Assay Reagents	Others
Decyl β-D-maltopyranoside is an epithelial permeability enhancer. Decyl β-D-maltopyranoside regulates the paracellular transport pathway and increases the permeability of molecules and proteins transported via the paracellular route. Decyl β-D-maltopyranoside enhances the transepithelial paracellular permeability of EPO across cell monolayers .

HY-138068

L-Tryptophanylglycine	Endogenous Metabolite	Metabolic Disease
L-Tryptophanylglycine is a dipeptide. L-Tryptophanylglycine exerts its function through competitive substrate interaction with intestinal dipeptide transporters .

HY-148447

eIF4A-IN-3	Eukaryotic Initiation Factor (eIF)	Cancer
eIF4A-IN-3, Silvestrol (HY-13251) analogue, is an eIF4A inhibitor. eIF4A-IN-3 blocks protein translation initiation by interfering with eIF4F complex assembly, preferentially inhibiting translation of mRNAs with long, highly structured 5'-untranslated regions. eIF4A-IN-3 inhibits proliferation of human breast cancer cells. eIF4A-IN-3 has moderate apical to basolateral permeability in intestinal cell monolayers and a low efflux ratio .

HY-P4086

Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R)	RABV nAChR	Neurological Disease Cancer
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) is a cell-penetrating peptide that is synthesized by adding nona-arginine motif to the carboxy terminus of RVG (rabies virus glycoprotein). Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) binds to nAChR on neuronal cells to mediate receptor-mediated endocytosis and targeted siRNA delivery. Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) protects complexed siRNA from degradation, enhances transcellular siRNA delivery in neuronal cells, and promotes efficient, pecific gene silencing. Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) can be used for the researches of neurological disease and cancer .

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-W1113135

Carboxymethyl-β-cyclodextrin sodium salt	Biochemical Assay Reagents	Others
Carboxymethyl-β-cyclodextrin sodium salt is a negatively charged β-cyclodextrin derivative, as well as a metal ion chelator and solubilizing reagent. Carboxymethyl-β-cyclodextrin sodium salt forms stable aqueous complexes with Ba ²⁺, Ca ²⁺, Cd ²⁺, Ni ²⁺, Pb ²⁺, Sr ²⁺, and Zn ²⁺ ions. Carboxymethyl-β-cyclodextrin sodium salt derived hydrogel carriers support oral insulin delivery via paracellular permeation across Caco-2 monolayers and produce sustained hypoglycemic effects in diabetic mice. Carboxymethyl-β-cyclodextrin sodium salt can be conjugated onto folate-modified BSA nanoparticles to boost folate receptor-mediated endocytosis, elevate intracellular anticancer drug uptake and trigger cell apoptosis. Carboxymethyl-β-cyclodextrin sodium salt can be utilized for chiral separation in capillary electrophoresis, development of nanoscale drug carriers and nucleic acid transfection research .

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-147681

SUN13837	FGFR	Neurological Disease
SUN13837 is an orally active, blood-brain barrier permeable FGFR modulator and neuroprotective agent. SUN13837 mimics the activity of basic fibroblast growth factor, stimulates intracellular tyrosine phosphorylation of FGFR and signal transduction in neuronal cells, induces neurite outgrowth, and inhibits glutamate-induced neuronal death. SUN13837 can be used in research related to acute cervical spinal cord injury and severe spinal cord injury .

HY-W344531

Indomethacin glucuronide	Drug Metabolite	Inflammation/Immunology
Indomethacin glucuronide is a glucuronide metabolite of Indomethacin (HY-14397) .

HY-P11740

VYPFPGPIHN	Angiotensin-converting Enzyme (ACE) Drug Intermediate	Others
VYPFPGPIHN is a precursor peptide of β-casomorphin (HY-P0179) and also an ACE inhibitor (IC₅₀ = 123 μM). VYPFPGPIHN resists hydrolysis by peptidases associated with intestinal cell monolayers, maintaining structural integrity and ACE inhibitory activity. VYPFPGPIHN is not extensively taken up or transported by differentiated intestinal cell monolayers .

HY-W099633

2-Aminodecanoic acid	Amino Acid Derivatives	Neurological Disease
2-Aminodecanoic acid is a lipophilic α-amino acid with an aliphatic side chain of 10 carbon atoms. 2-Aminodecanoic acid modifies the N-terminus of endogenous opioid peptide endomorphin-1 to enhance metabolic stability and membrane permeability. 2-Aminodecanoic acid can be used for the research of neuropathic pain .

HY-181487

FAK activator-1	FAK	Inflammation/Immunology
FAK activator-1 is a FAK activator and mucosal healing inducer.FAK activator-1 increases FAK phosphorylation at Tyr-397, promoting FAK activation.FAK activator-1 promotes mucosal healing.FAK activator-1 can be used for the research of nsaid-associated gastrointestinal mucosal injury .

HY-183752

CG-0988	SARS-CoV Virus Protease	Infection
CG-0988 is a selective SARS-CoV-2 3C-like protease (3CL ^pro) inhibitor with an IC₅₀ of 8.5 nM. CG-0988 functionally inhibits SARS-CoV-2 3CL ^pro, blocks SARS-CoV-2 replication, and exerts antiviral activity against SARS-CoV-2 variants. CG-0988 can be used in research related to coronavirus disease 2019 (COVID-19) .

HY-W663179

DNDI-VL-2098	Parasite Cytochrome P450	Infection
DNDI-VL-2098 is an orally active antileishmanial agent. DNDI-VL-2098 exhibits high permeability, in vitro metabolic stability, and selective inhibition of CYP2C19 (IC₅₀=0.47 μM). DNDI-VL-2098 does not affect the activities of other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6 and CYP3A4) at concentrations up to 12.5 μM. It shows favorable pharmacokinetic properties in multiple animal models including mice, hamsters, rats and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding and can be used for the research of visceral leishmaniasis .

HY-16265A

JI-101 hydrochloride	Ephrin Receptor PDGFR VEGFR	Cancer
JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .

HY-182421

GPR54 antagonist-1	Kisspeptin Receptor	Endocrinology Cancer
GPR54 antagonist‑1 is a GPR54 antagonist with IC₅₀ values of 3.6 nM and 15 nM against human and rat GPR54, respectively. GPR54 antagonist‑1 shows blood‑brain barrier penetration. GPR54 antagonist‑1 blocks the function of human and rat GPR54 receptors. GPR54 antagonist‑1 suppresses plasma luteinizing hormone levels in castrated male rats. GPR54 antagonist‑1 can be used for the study of prostate cancer and endometriosis .

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 .

Decyl β-D-maltopyranoside	Biochemical Assay Reagents
Decyl β-D-maltopyranoside is an epithelial permeability enhancer. Decyl β-D-maltopyranoside regulates the paracellular transport pathway and increases the permeability of molecules and proteins transported via the paracellular route. Decyl β-D-maltopyranoside enhances the transepithelial paracellular permeability of EPO across cell monolayers .

Cat. No.	Product Name	Target	Research Area

HY-P4086

Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R)	RABV nAChR	Neurological Disease Cancer
Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) is a cell-penetrating peptide that is synthesized by adding nona-arginine motif to the carboxy terminus of RVG (rabies virus glycoprotein). Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) binds to nAChR on neuronal cells to mediate receptor-mediated endocytosis and targeted siRNA delivery. Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) protects complexed siRNA from degradation, enhances transcellular siRNA delivery in neuronal cells, and promotes efficient, pecific gene silencing. Chimeric Rabies Virus Glycoprotein Fragment (RVG-9R) can be used for the researches of neurological disease and cancer .

HY-P11740

VYPFPGPIHN	Angiotensin-converting Enzyme (ACE) Drug Intermediate	Others
VYPFPGPIHN is a precursor peptide of β-casomorphin (HY-P0179) and also an ACE inhibitor (IC₅₀ = 123 μM). VYPFPGPIHN resists hydrolysis by peptidases associated with intestinal cell monolayers, maintaining structural integrity and ACE inhibitory activity. VYPFPGPIHN is not extensively taken up or transported by differentiated intestinal cell monolayers .

Glycerophosphocholine (S)-Glycerolphosphocholine	Structural Classification Human Gut Microbiota Metabolites Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Endogenous Metabolite
Glycerophosphocholine ((S)-Glycerolphosphocholine) is an orally active metabolite that crosses the blood-brain barrier. Glycerophosphocholine acts as a precursor of acetylcholine, a specific marker for phosphatidylcholine breakdown, a major water-soluble storage form of choline, and an intermediate in phosphatidylcholine metabolism. Glycerophosphocholine is specifically elevated in the cerebrospinal fluid of Alzheimer's disease models, and it also promotes growth hormone secretion and fat oxidation. Glycerophosphocholine is also a potential biomarker for breast cancer .

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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