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active-site aspartates 32

" in MedChemExpress (MCE) Product Catalog:

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By Research Areas:	Cancer (93) Cardiovascular Disease (30) Endocrinology (4) Infection (63) Inflammation/Immunology (46) Metabolic Disease (40) Neurological Disease (39)
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313

Inhibitors & Agonists

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Inhibitory Antibodies

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Isotope-Labeled Compounds

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GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-Y1750

β-Aminopropionitrile Maximum Cited Publications 13 Publications Verification BAPN	Endogenous Metabolite Lysyl Oxidase	Neurological Disease Cancer
β-Aminopropionitrile (BAPN) is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes. β-Aminopropionitrile can be used for the study of obesity .

HY-158301

MY-1B 1 Publications Verification	DNA Methyltransferase RNA MTase	Others
MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC₅₀: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .

HY-15345A

Tetrahydrouridine 3 Publications Verification THU; NSC-112907	DNA/RNA Synthesis	Cancer
Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .

HY-137431

Asundexian 5 Publications Verification BAY-2433334	Factor Xa	Cardiovascular Disease
Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC₅₀ of 1 nM .

HY-103334

MAFP 5 Publications Verification Methyl Arachidonyl Fluorophosphonate	Phospholipase	Cardiovascular Disease Neurological Disease Metabolic Disease
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

HY-11107

PHA-665752 10+ Cited Publications	c-Met/HGFR Autophagy Apoptosis	Cancer
PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (K_i=4 nM; IC₅₀=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .

HY-120110

IOX4 5+ Cited Publications	HIF/HIF Prolyl-Hydroxylase	Neurological Disease Inflammation/Immunology
IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC₅₀ value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .

HY-12903

Macozinone 5 Publications Verification PBTZ169	Bacterial Antibiotic	Infection
Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect .

HY-A0068

Aurothioglucose 2 Publications Verification Gold thioglucose	NF-κB HIV Reactive Oxygen Species (ROS)	Infection Inflammation/Immunology Cancer
Aurothioglucose (Gold thioglucose), containing monovalent gold ion, is a potent active-site inhibitor of TrxR1 (thioredoxin reductase 1), with an IC₅₀ of 65 nM. Aurothioglucose inhibits the DNA binding of NF-κB in vitro. Aurothioglucose shows anti-HIV and anti-rheumatic activities .

HY-14617

Paradol 4 Publications Verification [6]-Gingerone; [6]-Paradol	COX	Cancer
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.

HY-N7136

α-Terpinyl acetate	Environmental Pollutants Cytochrome P450	Metabolic Disease
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a K_d value of 5.4 μM .

HY-W012658

2-Methylacetophenone O-Methylacetophenone	Xanthine Oxidase	Metabolic Disease Inflammation/Immunology
2-Methylacetophenone (O-Methylacetophenone), acetophenone derivative and acaricide, is a xanthine dehydrogenase (XDH) inhibitor. 2-Methylacetophenone competitively binds to the XDH active site, blocking the pathway for xanthine to be converted to uric acid. 2-Methylacetophenone can be used for the study of hyperuricemia and house dust .

HY-12062

PD318088 1 Publications Verification	MEK	Cancer
PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .

HY-102087

JPM-OEt 3 Publications Verification	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .

HY-138825

NCGC00188636	Pyk2	Metabolic Disease
NCGC00188636 is a novel covalent pyruvate kinase (PYK) inhibitor. NCGC00188636 blocks nucleotide binding to the active site of pyruvate kinase. NCGC00188636 can be used for the research of the metabolism of many organisms and cell types.

HY-P99283

Concizumab 1 Publications Verification NN 7415; mAb 2021; Anti-TFPI Recombinant Antibody	Factor Xa	Others
Concizumab is an anti-TFPI monoclonal antibody (IgG4 type) that binds to the Kunitz-type protease inhibitor (KPI) 2 structural domain of TFPI, thereby blocking the interaction of this structural domain with the FXa active site. Concizumab can be used in the study of haemophilia .

HY-P2463

Fequesetide	Arp2/3 Complex	Inflammation/Immunology
Fequesetide, a peptide segment, is the active site within the protein thymosin β₄ responsible for actin binding, cell migration and wound healing .

HY-15345

Tetrahydrouridine dihydrate 3 Publications Verification THU dihydrate; NSC-112907 dihydrate	DNA/RNA Synthesis	Cancer
Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.

HY-133154

Carboxyaminoimidazole ribotide CAIR; 4-Carboxy-AIR	Endogenous Metabolite	Infection
Carboxyaminoimidazole ribotide (CAIR) is a metabolite of E. coli. Carboxyaminoimidazole ribotide can be used to detect distinctive features of E. coli PurE active site and synthesis fungal de novo purine .

HY-108419

WHI-P258	JNK	Cancer
WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated K_i of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM .

HY-P2759

Thioredoxin reductase TrxR	TrxR	Infection Cardiovascular Disease Inflammation/Immunology Cancer
Thioredoxin reductase (TrxR) is a selenoprotein that plays a central role in cellular redox homeostasis by utilizing highly reactive selenocysteine (Sec) residues exposed to solvents at its active site. Thioredoxin reductase can be used for the study of diverse diseases, from rheumatoid arthritis and ischemia to cancer and parasitic infections .

HY-171036

GAPDH-IN-1	Endogenous Metabolite	Metabolic Disease
GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC₅₀ of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD ⁺, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .

HY-126031

(R)-KT109	DAGL	Inflammation/Immunology
(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC₅₀ values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .

HY-173593

Adenosine-3',5'-bisphosphate	Small Interfering RNA (siRNA)	Cancer
Adenosine-3',5'-bisphosphate is an exoribonuclease XRN1 inhibitor with an IC₅₀ of 36 nM, a K_D of 12 nM, and a K_D of 14 nM against human XRN2. Adenosine-3',5'-bisphosphate binds to the bimetallic active site of human XRN1, and also binds potently to human XRN2 via its conserved bimetallic active site. Adenosine-3',5'-bisphosphate can be used in research related to non-small cell lung cancer .

HY-Y1750A

β-Aminopropionitrile hydrochloride Maximum Cited Publications 13 Publications Verification BAPN hydrochloride	Monoamine Oxidase Endogenous Metabolite	Metabolic Disease Cancer
β-Aminopropionitrile (BAPN) hydrochloride is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile hydrochloride targets the active site of LOX or LOXL isoenzymes .

HY-148433

SpdSyn binder-1	Parasite	Infection Inflammation/Immunology
SpdSyn binder-1 is a weak binder, which binds in the active site of plasmodium falciparum spermidine synthase. SpdSyn binder-1 can be used for the research of malaria .

HY-161137

LQFM215	Amino acid Transporter iGluR	Neurological Disease
LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .

HY-119390

AA-CW236	DNA Methyltransferase	Cancer
AA-CW236 is a MGMT (O6-methylguanine DNA methyltransferase) inhibitor. AA-CW236 targets MGMT active site Cys145 for covalent modification .

HY-P99298

Lampalizumab RG 7417; TNX 234; Anti-CFD Recombinant Antibody	Complement System	Inflammation/Immunology
Lampalizumab (RG 7417) is a humanised monoclonal antibody targeting complement Factor D in the alternative complement pathway. Lampalizumab binds an exosite and sterically blocks Factor B access to the active site. Lampalizumab can be used for age-related macular degeneration (AMD) research .

HY-176892

Papaveroline	Src	Neurological Disease
Papaveroline is an orally active Fyn tyrosine kinase inhibitor. Papaveroline stably binds to the active site of Fyn tyrosine kinase via hydrogen bonding and hydrophobic interactions, thereby inhibiting kinase activity associated with the pathogenesis of Alzheimer's disease. Papaveroline can be used for the research of Alzheimer's disease .

HY-139031

ALDH1A2-IN-1	Aldehyde Dehydrogenase (ALDH)	Endocrinology
ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC₅₀=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions .

HY-116750

6-Hydroxykaempferol	Tyrosinase	Others
6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC₅₀ value of 124 μM. 6-Hydroxykaempferol has a K_i value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .

HY-129944

MJ33-OH	Phospholipase	Inflammation/Immunology
MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .

HY-175249

TKL-IN-2		Others
TKL-IN-2 is a herbicide and SvTKL inhibitor with an IC₅₀ of 0.11 mg/L. TKL-IN-2 binds to the SvTKL active site, interacts with key pocket residues, and inhibits enzyme activity. TKL-IN-2 can be used for the research of weed control in maize, wheat, soybean, and cotton fields .

HY-116188

HX1	Others	Inflammation/Immunology
HX1 is a potent reversible myeloperoxidase (MPO) inhibitor with an IC₅₀ value of 50 nM. HX1 is bound within the active site cavity above the heme and blocks the substrate channel. HX1 is promising for research of inflammatory diseases .

HY-158615

STING18 Stimulator of interferon genes 18	Others	Others
STING18 (Stimulator of interferon genes 18) is a compound that inhibits STING protein by utilizing a small molecule active site dimer, with good oral exposure, slow binding kinetics, and functional inhibitory activity on STING-mediated cytokine release.

HY-126055

Hadacidin	Adenylate Cyclase	Others
Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .

HY-P0266B

N-Acetyl-Ser-dAsp-Lys-Pro acetate Ac-SdKP acetate	Angiotensin-converting Enzyme (ACE)	Inflammation/Immunology
N-Acetyl-Ser-dAsp-Lys-Pro (Ac-SdKP) acetate is a specific substrate for the N-terminal active site of angiotensin-converting enzyme (ACE). N-Acetyl-Ser-dAsp-Lys-Pro acetate is a natural inhibitor of pluripotent hematopoietic stem cell proliferation. Anti-inflammatory and antifibrotic properties .

HY-W671129

Frenolicin B	Antibiotic Fungal	Infection
Frenolicin B is a covalent enzyme inhibitor and an orally active antiparasitic agent, with an IC₅₀ of 0.2 μM against human Prx1. Frenolicin B selectively inhibits Glutaredoxin 3 via covalent modification of the active-site cysteines Cys159/Cys261. Frenolicin B selectively inhibits Peroxiredoxin 1 via covalent modification of the active-site cysteines Cys83/Cys173. Frenolicin B can be used in research related to colon cancer, breast cancer, lung cancer and malaria .

HY-162785

XC219	CDK	Infection
XC219 (compound 43) is a cyclin-dependent kinase CDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research .

HY-Y1750R

β-Aminopropionitrile (Standard)	Reference Standards Monoamine Oxidase Endogenous Metabolite	Metabolic Disease Cancer
β-Aminopropionitrile (BAPN) is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes .

HY-139032

CM121	Aldehyde Dehydrogenase (ALDH)	Others
CM121 is an active site-directed reversible ALDH1A2 inhibitor (IC₅₀=0.54 μM；Kd=1.1 μM) with a variety of hydrophobic interactions .

HY-N1066

Xanthohumol D 1 Publications Verification	Others	Cancer
Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC₅₀ value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro .

HY-129944A

MJ33-OH lithium	Phospholipase	Inflammation/Immunology
MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .

HY-P10828

MAPI	Virus Protease	Infection Inflammation/Immunology
MAPI is a polypeptide irreversible 3C cysteine protease (SV3CP) inhibitor. MAPI inhibits SV3CP by covalently binding its C-terminal Michael-acceptor extension to the active site thiol of SV3CP Cys 139. MAPI is promising for research of noroviruses infection .

HY-12903R

Macozinone (Standard) PBTZ169 (Standard)	Reference Standards Bacterial Antibiotic	Infection
Macozinone (Standard) is the analytical standard of Macozinone. This product is intended for research and analytical applications. Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect[1][2].

HY-P4552

Hippuryl-Phe-Arg-OH	Angiotensin Receptor	Others
Hippuryl-Phe-Arg-OH is the *active site* on the cell surface of Angiotensin I converting enzyme (ACE) .

HY-130366

JG-365	HIV Protease	Others
JG-365 is an HIV-1 protease inhibitor that binds to the active site of HIV-1 protease.

HY-E70628

Aspartic acid proteinase	Biochemical Assay Reagents	Others
Aspartic acid proteinase is a type of proteolytic enzyme, which is characterized by its action via two critical aspartic acid residues in the active site, which facilitate the hydrolysis of peptide bonds in proteins .

HY-N11896A

10-Hydroxyaloin A	SARS-CoV	Infection Inflammation/Immunology
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor. 10-Hydroxyaloin A exhibits significant efficacy to bind SARS-Cov-2 M_pro active site .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-Y1750

β-Aminopropionitrile Maximum Cited Publications 13 Publications Verification BAPN	Structural Classification Natural Products Microorganisms Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification Cancer	Endogenous Metabolite Lysyl Oxidase
β-Aminopropionitrile (BAPN) is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes. β-Aminopropionitrile can be used for the study of obesity .

HY-W050154

Kojic acid 2 Publications Verification	Infection Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification	Parasite Tyrosinase NF-κB CDK
Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC₅₀ of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity .

HY-78726

Fosamprenavir 4 Publications Verification Amprenavir phosphate; GW 433908	Infection Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Drug Intermediate HIV HIV Protease
Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-14617

Paradol 4 Publications Verification [6]-Gingerone; [6]-Paradol	Zingiber officinale Roscoe Monophenols Classification of Application Fields Phenols Plants Disease Research Fields Source Classification Zingiberaceae Cancer	COX
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.

HY-N0419

Quercimeritrin 2 Publications Verification Quercetin-7-O-β-D-glucopyranoside	Flavonols Structural Classification Ginkgoaceae Classification of Application Fields Metabolic Disease Plants Compositae Endogenous metabolite Ginkgo biloba Human Gut Microbiota Metabolites Flavonoids Derris scandens Disease Research Fields Source Classification	Glycosidase c-Kit MMP VEGFR Aurora Kinase
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC₅₀ of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .

HY-I0096

Indole-2-carboxylic acid	Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	iGluR HIV HIV Integrase
Indole-2-carboxylic acid (I2CA) is a competitive antagonist of the glycine site of the NMDA receptor (K_i=15 μM, 5-fluoro-I2CA) and an inhibitor of HIV-1 integrase. Indole-2-carboxylic acid is selective for the glycine site of the NMDA receptor and blocks the enhancement of NMDA receptor by competitively inhibiting the binding of glycine to the NMDA receptor. Indole-2-carboxylic acid can also inhibit the strand transfer activity of HIV-1 integrase by chelating Mg ²⁺ at the active site of integrase and interacting with the hydrophobic cavity. Indole-2-carboxylic acid can be used in the study of neurological diseases (such as stroke, epilepsy) and HIV-1 infection .

HY-N7136

α-Terpinyl acetate	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Laurus nobilis L. Metabolic Disease Plants Lauraceae Disease Research Fields Source Classification	Environmental Pollutants Cytochrome P450
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a K_d value of 5.4 μM .

HY-W012658

2-Methylacetophenone O-Methylacetophenone	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Xanthine Oxidase
2-Methylacetophenone (O-Methylacetophenone), acetophenone derivative and acaricide, is a xanthine dehydrogenase (XDH) inhibitor. 2-Methylacetophenone competitively binds to the XDH active site, blocking the pathway for xanthine to be converted to uric acid. 2-Methylacetophenone can be used for the study of hyperuricemia and house dust .

HY-W012817

Methylhydroquinone	Structural Classification Natural Products Microorganisms Classification of Application Fields Other Diseases Disease Research Fields Source Classification	Environmental Pollutants COX
Methylhydroquinone is an orally active COX inhibitor with IC₅₀s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions .

HY-17431

Fosamprenavir Calcium Salt 4 Publications Verification GW433908G	Infection Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Drug Intermediate HIV HIV Protease
Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-15130

DL-O-Phosphoserine	Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
DL-O-Phosphoserine is a normal metabolite in human biofluids and is a mixture of phosphoserine with two stereochemical structures (D-type and L-type O-phospho-serine). O-phospho-L-serine is a competitive inhibitor of serine racemase and phagocytosis. O-phospho-L-serine inhibits the enzymatic reaction by competing with the active site of serine racemase, thereby affecting the production of D-serine. O-phospho-L-serine also mimics the phosphatidylserine head group, binds to the phosphatidylserine receptor, interferes with phagocytic signal transduction, and partially blocks the phagocytosis of apoptotic cells by cells. O-phospho-L-serin can be used in the research of retinal regeneration, bone repair, and insect growth and development .

HY-N7652

Terminolic acid	Triterpenes other families Classification of Application Fields Terpenoids Plants Inflammation/Immunology Disease Research Fields Source Classification	Bacterial Interleukin Related
Terminolic acid is a pentacyclic triterpene glycoside and antibacterial agent. Terminolic acid can be isolated from Combretum racemosum. Terminolic acid inhibits proinflammatory cytokines by binding to the receptor active sites of IL-1β and IL-6. Terminolic acid reduces IL-8. Terminolic acid has antibacterial activity against Staphylococcus aureus, Escherichia coli and Enterococcus faecalis with MICs ranging from 64 to 256 μg/mL. Terminolic acid is used in colon cancer research .

HY-133154

Carboxyaminoimidazole ribotide CAIR; 4-Carboxy-AIR	Infection Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
Carboxyaminoimidazole ribotide (CAIR) is a metabolite of E. coli. Carboxyaminoimidazole ribotide can be used to detect distinctive features of E. coli PurE active site and synthesis fungal de novo purine .

HY-N10686

Tanshinone IIA anhydride	Structural Classification Flavonoids Labiatae Samanea saman (Jacq.) Merr. Plants Other Flavonoids Source Classification	Carboxylesterase (CES)
Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a K_i value of 1.9 nM against hCE1 and a K_i value of 1.4 nM against hiCE. Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase, and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies .

HY-N0857

Deoxyandrographolide 1 Publications Verification	Structural Classification Acanthaceae Simsia foetida (Cav.) S.F.Blake Terpenoids Diterpenoids Plants Source Classification	GLUT HDAC Virus Protease PI3K AMPK Akt Histone Demethylase MDM-2/p53 IFNAR Reactive Oxygen Species (ROS)
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a K_D of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, γH2A.X, p53 and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection .

HY-N10423

Cubebin (-)-Cubebin	Structural Classification Classification of Application Fields Lignans Piperaceae Piper cubeba L.f. Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields Source Classification	Cholinesterase (ChE) Bacterial Fungal Parasite p38 MAPK
Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression .

HY-Y1750A

β-Aminopropionitrile hydrochloride Maximum Cited Publications 13 Publications Verification BAPN hydrochloride	Alkaloids Classification of Application Fields Other Alkaloids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification Cancer	Monoamine Oxidase Endogenous Metabolite
β-Aminopropionitrile (BAPN) hydrochloride is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile hydrochloride targets the active site of LOX or LOXL isoenzymes .

HY-116750

6-Hydroxykaempferol	Flavonols Flavonoids Trifolium repens Linn. Leguminosae Plants Source Classification	Tyrosinase
6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC₅₀ value of 124 μM. 6-Hydroxykaempferol has a K_i value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .

HY-N15159

Cladophorol A	Structural Classification Marine algae Marine natural products Phenols Polyphenols Source Classification	Cyclic GMP-AMP Synthase STING Parasite
Cladophorol A is a cyclic GMP-AMP synthase (cGAS) inhibitor. Cladophorol A binds to the conserved adenosine nucleobase binding site within the cGAS active site to inhibit its catalytic activity. Cladophorol A effectively inhibits the overactivation of the cGAS-STING pathway with an IC₅₀ of 370 nM. Cladophorol A inhibits asexual blood-stage Plasmodium falciparum with an EC₅₀ of 0.7 μg/mL. Cladophorol A can be used for the researches of inflammatory disease and malaria .

HY-126055

Hadacidin	Microorganisms Ketones, Aldehydes, Acids Source Classification	Adenylate Cyclase
Hadacidin is a competitive inhibitor of adenylate synthase. Hadacidin binds to the active site of adenylate synthase, competitively inhibiting L-aspartate binding. Hadacidin can be used in drug design, to help develop new inhibitors or activators to regulate adenylate synthase activity, and to play a role in the study of related diseases .

HY-W671129

Frenolicin B	Structural Classification Microorganisms Antibiotics Other Antibiotics Source Classification	Antibiotic Fungal
Frenolicin B is a covalent enzyme inhibitor and an orally active antiparasitic agent, with an IC₅₀ of 0.2 μM against human Prx1. Frenolicin B selectively inhibits Glutaredoxin 3 via covalent modification of the active-site cysteines Cys159/Cys261. Frenolicin B selectively inhibits Peroxiredoxin 1 via covalent modification of the active-site cysteines Cys83/Cys173. Frenolicin B can be used in research related to colon cancer, breast cancer, lung cancer and malaria .

HY-Y1750R

β-Aminopropionitrile (Standard)	Structural Classification Natural Products Microorganisms Endogenous metabolite Source Classification	Reference Standards Monoamine Oxidase Endogenous Metabolite
β-Aminopropionitrile (BAPN) is a specific, irreversible and orally active lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes .

HY-N1066

Xanthohumol D 1 Publications Verification	Chalcones Flavonoids Classification of Application Fields Humulus lupulus L. Phenols Polyphenols Plants Moraceae Disease Research Fields Source Classification Cancer	Others
Xanthohumol D, isolated from hops, is an inhibitor of quinone reductase-2 (QR-2) with the IC₅₀ value of 110 μM, and binds to the active site of QR-2. Xanthohumol D shows antiproliferative activity on human cancer cell lines in vitro .

HY-121020

Arcapillin	Structural Classification Flavonoids Flavones Plants Compositae Artemisia capillaris Thunb. Source Classification	SARS-CoV
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin induces dose-dependent relaxation of ileum and pulmonary artery smooth muscle, causes slight urinary bladder smooth muscle contraction at highest tested concentrations. Arcapillin binds to the active site of SARS-CoV-2 M_pro via interactions with Gln139, His163, and His164, exhibits antiviral activity against SARS-CoV-2 and MERS-CoV. Arcapillin can be used for the research of gastrointestinal disorders, COVID-19, and Middle East respiratory syndrome (MERS) .

HY-W050154R

Kojic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Parasite Tyrosinase NF-κB CDK
Kojic acid (Standard) is the analytical standard of Kojic acid. This product is intended for research and analytical applications. Kojic acid is a substance produced by Aspergillus oryzae, with various biological activities including antitumor, insecticidal, antibacterial, antioxidant, and radioprotective effects. Kojic acid exhibits tyrosinase inhibition activity by capturing copper ions that bind to the active site of tyrosinase, preventing its activation. Tyrosinase is a key enzyme in the biosynthesis of melanin, so kojic acid can block melanin production. Additionally, kojic acid shows potential inhibition of NF-κB activity in human keratinocytes, which may also be related to the anti-melanogenic effect induced by kojic acid. Kojic acid is effective when administered orally and can also be absorbed transdermally. Nano-carrier systems prepared with kojic acid demonstrate effective delivery of anticancer drugs. Kojic acid holds promise for research in cancer, infectious diseases, and skin whitening among other fields .

HY-N11896A

10-Hydroxyaloin A	Natural Products Liliaceae Aloe vera (L.) Burm. f. Plants Source Classification	SARS-CoV
10-10-Hydroxyaloin A is potent SARS-CoV-2 inhibitor. 10-Hydroxyaloin A exhibits significant efficacy to bind SARS-Cov-2 M_pro active site .

HY-N16415

Deoxyfunicone	Natural Products Microorganisms Source Classification	Phosphatase
Deoxyfunicone is a secondary fungal metabolite that inhibits PTP1B activity by binding to the active site of the enzyme with an IC₅₀ value of 24.3µM. Deoxyfunicone has anti-inflammatory activity .

HY-14617R

Paradol (Standard) [6]-Gingerone (Standard); [6]-Paradol (Standard)	Zingiber officinale Roscoe Structural Classification Monophenols Phenols Plants Source Classification Zingiberaceae	Reference Standards COX
Paradol (Standard) is the analytical standard of Paradol. This product is intended for research and analytical applications. Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.

HY-N7263

Galanthamine N-Oxide	Alkaloids other families Plants Source Classification	Cholinesterase (ChE)
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC₅₀ of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .

HY-W012658R

2-Methylacetophenone (Standard) O-Methylacetophenone (Standard)	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Xanthine Oxidase
2-Methylacetophenone (O-Methylacetophenone) (Standard) is the analytical standard of 2-Methylacetophenone (HY-W012658). This product is intended for research and analytical applications. 2-Methylacetophenone (O-Methylacetophenone), acetophenone derivative and acaricide, is a xanthine dehydrogenase (XDH) inhibitor. 2-Methylacetophenone competitively binds to the XDH active site, blocking the pathway for xanthine to be converted to uric acid. 2-Methylacetophenone can be used for the study of hyperuricemia and house dust .

HY-W012817R

Methylhydroquinone (Standard)	Natural Products Microorganisms Source Classification	COX Reference Standards
Methylhydroquinone (Standard) is the analytical standard of Methylhydroquinone. This product is intended for research and analytical applications. Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions[1][2].

HY-17431R

Fosamprenavir Calcium Salt (Standard) GW433908G (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Reference Standards Drug Intermediate HIV HIV Protease
Fosamprenavir Calcium Salt (GW433908G) (Standard) is the analytical standard of Fosamprenavir Calcium Salt (HY-17431R). This product is intended for research and analytical applications. Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-N11721

5-Hydroxyaloin A	Structural Classification Liliaceae Aloe microstigma Salm-Dyck Phenols Polyphenols Plants Source Classification	SOD Lipase
5-Hydroxyaloin A is a polyphenolic antioxidant agent. 5-Hydroxyaloin A forms hydrogen bonding interactions at lipase’s active site and SOD’s active site with low binding energy. 5-Hydroxyaloin A inhibits microsomal lipid peroxidation induced by ferrous-cysteine, reducing malondialdehyde production. 5-Hydroxyaloin A can be used for the research of obesity .

HY-118572

(S)-Allantoin	Structural Classification Caprifoliaceae Cordyceps bassiana Ketones, Aldehydes, Acids Plants Endogenous metabolite Source Classification	Drug Isomer
(S)-Allantoin is the S-isomer of Allantoin (HY-N0543). (S)-Allantoin binds selectively in the active site of urate oxidase. (S)-Allantoin can be converted to Allantoate by the action of allantoicase. (S)-Allantoin serves as a source of nitrogen in Arabidopsis thaliana .

HY-N18420

Citriniorl A	Structural Classification Natural Products Microorganisms Coumarins Phenylpropanoids Source Classification	Sirtuin
Citriniorl A is a SIRT1 enhancer with an EC₅₀ of 5.8 μM. Citriniorl A binds to key amino acid residues in the SIRT1 active site to stabilize binding and enhance SIRT1-mediated deacetylation. Citriniorl A can be used for the research of metabolic disorders .

HY-127083

Artecanin	Structural Classification Natural Products Laurus nobilis L. Plants Lauraceae Source Classification	SARS-CoV Virus Protease
Artecanin is a SARS-CoV-2 main protease (M ^pro) inhibitor with predicted high gastrointestinal absorption and oral bioavailability, and no predicted hepatotoxicity, carcinogenicity, mutagenicity or cytotoxicity. Artecanin interacts with His41 and Cys145, the key amino acid residues in the active site of M ^pro, blocks the cleavage and maturation of viral precursor proteins, and forms a stable complex with M ^pro. Artecanin blocks the invasion of SARS-CoV-2. Artecanin is applicable to the research of COVID-19 .

Cat. No.	Product Name	Chemical Structure

HY-78726S

Fosamprenavir-d4

Fosamprenavir-d₄ is the Deuterium-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-W050154S

Kojic acid-13C6

Kojic acid- ¹³C₆ is ¹³C labeled Kojic acid (HY-W050154). Kojic acid is a substance produced by Aspergillus oryzae that is orally effective and can also be absorbed transdermally. Kojic acid exhibits various biological activities, including anti-aging, anti-nematode, antimicrobial, antioxidant, and anti-inflammatory effects. Kojic acid is a Tyrosinase inhibitor with an Mushroom Tyrosinase IC50 of 182.7 μM. Kojic acid prevents melanin production by capturing copper ions that bind to the tyrosinase active site, thus inhibiting its activation. Kojic acid also suppresses the NF-κB and p21 signaling pathways in human keratinocytes. Kojic acid derivatives have anticancer activity .

HY-15345AS

Tetrahydrouridine-d3
Tetrahydrouridine-d₃ is the deuterium labeled Tetrahydrouridine . Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .

HY-137431S

Asundexian-d3
Asundexian-d₃ (BAY-2433334-d₃) is the deuterium labeled Asundexian (HY-137431). Asundexian (BAY 2433334) is an orally active coagulation factor Xia (FXIa) inhibitor. Asundexian binds directly, potently, and reversibly to the active site of FXIa and thereby inhibits its activity. Asundexian inhibits human FXIa in buffer with an IC₅₀ of 1 nM .

HY-W284558S

Sodium hexadecyl sulfate-d33

Sodium hexadecyl sulfate-d₃₃ is the deuterium labeled Sodium hexadecyl sulfate. Sodium hexadecyl sulfate is a long-chain anionic surfactant. Sodium hexadecyl sulfate can act as an interface-regulating substance to form a soft layer on the surface of carbon nanotubes, guide proteins to adsorb in the correct orientation with active sites facing outward through electrostatic interactions, and significantly enhance the activity of immobilized enzymes. Sodium hexadecyl sulfate can replace or supplement SDS (HY-Y0316) in capillary gel electrophoresis (CGE) .

HY-W740650

Migalastat hydrochloride-15N

Migalastat hydrochloride- ¹⁵N (GR181413A- ¹⁵N) is the ¹⁵N-labeled Migalastat hydrochloride (HY-14929A). Migalastat (GR181413A free base) hydrochloride is an orally active α-galactosidase A molecular chaperone, with an IC50 value of 0.04 μM for human α-Gal A. Migalastat binds to the active site of certain unstable mutant forms of α-galactosidase A, facilitating their transport to the lysosome. After dissociation in the acidic environment, Migalastat enables the mutant α-galactosidase A to exhibit biological activity .

HY-W728096

Migalastat-d5

Migalastat-d₅ (GR181413A-d₅ (free base)) is deuterium labeled Migalastat. Migalastat (GR181413A free base) is an orally active α-galactosidase A molecular chaperone, with an IC₅₀ value of 0.04 μM for human α-Gal A. Migalastat binds to the active site of certain unstable mutant forms of α-galactosidase A, facilitating their transport to the lysosome. After dissociation in the acidic environment, Migalastat enables the mutant α-galactosidase A to exhibit biological activity .

HY-78726S2

Fosamprenavir-13C6

Fosamprenavir- ¹³C₆ is the ¹³C-labeled Fosamprenavir (HY-78726). Fosamprenavir is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir can be used for the study of human immunodeficiency virus (HIV-1) infection .

HY-B1451S

Imidapril-d3 hydrochloride

Imidapril-d₃ hydrochloride (TA-6366-d₃) is the deuterium labeled Imidapril hydrochloride. Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .

HY-W000854S

3-Methoxybenzeneboronic acid-d3

3-Methoxybenzeneboronic acid-d₃ is the deuterium labeled 3-Methoxybenzeneboronic acid (HY-W000854). 3-Methoxybenzeneboronic acid (3-Methoxyphenylboronic acid) is a boronic acid derivative. 3-Methoxybenzeneboronic acid shows best suitable binding pattern at the active site by interacting non-covalently with amino acid residues of proteins. 3-Methoxybenzeneboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13642G

RG108	DNA Methyltransferase	Cancer
RG108 (GMP) is RG108 (HY-13642) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RG108 (N-Phthalyl-L-tryptophan) is a non-nucleoside DNA methyltransferases (DNMTs) inhibitor (IC₅₀=115 nM) that blocks the DNMTs active site. RG108 (N-Phthalyl-L-tryptophan) causes demethylation and reactivation of tumor suppressor genes, but it does not affect the methylation of centromeric satellite sequences .

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