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Results for "

Reversible Inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adenosine Receptor (1) Apoptosis (8) Aurora Kinase (1) Bacterial (2) Btk (3) Carboxylesterase (CES) (1) Cholinesterase (ChE) (4) Complement System (1) COMT (2) Cytochrome P450 (1) Deubiquitinase (2) Dipeptidyl Peptidase (2) DNA Methyltransferase (3) EGFR (2) Endogenous Metabolite (4) Fatty Acid Synthase (FASN) (1) Fungal (1) Glycosidase (1) HBV (1) HDAC (1) Histone Demethylase (4) Histone Methyltransferase (3) HIV (1) HMG-CoA Reductase (HMGCR) (1) Interleukin Related (1) IPK Superfamily (1) Isotope-Labeled Compounds (2) JAK (1) Lipoxygenase (2) MAGL (3) mGluR (1) Monoamine Oxidase (7) Na+/K+ ATPase (1) NO Synthase (1) PAK (3) Parasite (4) Phosphodiesterase (PDE) (3) Potassium Channel (8) Prostaglandin Receptor (1) Proteasome (1) Proton Pump (2) Reactive Oxygen Species (ROS) (2) Reference Standards (9) RIP kinase (1) Ser/Thr Protease (1) Sodium Channel (8) Src (1) YAP (2) γ-secretase (3)
By Research Areas:	Cancer (35) Cardiovascular Disease (9) Endocrinology (1) Infection (6) Inflammation/Immunology (14) Metabolic Disease (11) Neurological Disease (23)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-139664

GSK-3685032 10+ Cited Publications	DNA Methyltransferase	Cancer
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-15185

Nirogacestat 10+ Cited Publications PF-3084014	γ-secretase Apoptosis	Cancer
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .

HY-13007

PF-3758309 5+ Cited Publications PF-03758309	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-129388B

Pulrodemstat benzenesulfonate 4 Publications Verification CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate	Histone Demethylase	Inflammation/Immunology Cancer
Pulrodemstat (CC-90011) benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .

HY-17543

ML-323 Maximum Cited Publications 17 Publications Verification	Deubiquitinase	Cancer
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC₅₀ of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (K_i) is 68 nM.

HY-B0563

Ropivacaine 5+ Cited Publications	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .

HY-B0563B

Ropivacaine hydrochloride 5+ Cited Publications	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .

HY-100414

Soraprazan 2 Publications Verification BYK61359	Proton Pump	Metabolic Disease
Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (K_i=6.4 nM), with an IC₅₀ of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases .

HY-110137

Furamidine dihydrochloride 3 Publications Verification DB75 dihydrochloride; NSC 305831 dihydrochloride	Histone Methyltransferase Phosphodiesterase (PDE) Parasite	Infection Inflammation/Immunology Cancer
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .

HY-15185B

Nirogacestat dihydrobromide 10+ Cited Publications PF-3084014 dihydrobromide; PF-03084014 dihydrobromide	γ-secretase Apoptosis	Cancer
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .

HY-N0313

Euphol	MAGL Endogenous Metabolite	Inflammation/Immunology
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC₅₀=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .

HY-117769

GSK837149A	Fatty Acid Synthase (FASN)	Metabolic Disease
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (K_i=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .

HY-B0563A

Ropivacaine hydrochloride monohydrate 5+ Cited Publications	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .

HY-B0563S1

Ropivacaine-d7	Isotope-Labeled Compounds Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease
Ropivacaine-d₇ is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain?management .

HY-152846

Flizasertib GDC-8264	RIP kinase Interleukin Related	Cardiovascular Disease Inflammation/Immunology Endocrinology
Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with K_i ^app values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury .

HY-110079

TNP	IPK Superfamily	Cancer
TNP is a competitive, reversible inhibitor of IP6K1 and IP3K, with IC₅₀s of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP competitively binds to the ATP binding site of IP6K, inhibits the generation of 5-IP7, and thus relieves the inhibition of 5-IP7 on the AKT signaling pathway. TNP can enhance insulin sensitivity and promote thermogenesis in adipose tissue. TNP cannot effectively pass through the blood-brain barrier and is mainly used in the study of obesity, type 2 diabetes, and metabolic syndrome. However, TNP also inhibits CYP3A4 and may need further optimization[1][2][3].

HY-139603

MYF-01-37 1 Publications Verification	YAP	Cancer
MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction .

HY-176542

TD034	HDAC YAP	Cancer
TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC₅₀ of 5.1 nM and a K_i of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer .

HY-N3474

Isolicoflavonol	Carboxylesterase (CES)	Others
Isolicoflavonol potently inhibits hCES2A (Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM .

HY-106405

Nebicapone BIA 3-202	COMT	Metabolic Disease
Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease .

HY-132310

MAGL-IN-4	MAGL	Neurological Disease
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC₅₀ of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .

HY-139664A

(R)-GSK-3685032	DNA Methyltransferase	Cancer
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-117853

Atreleuton ABT-761; VIA-2291	Lipoxygenase	Cardiovascular Disease
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation . Atreleuton is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-132808

Atuzabrutinib SAR 444727; PRN473	Btk	Inflammation/Immunology
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .

HY-129388A

Pulrodemstat 4 Publications Verification CC-90011; LSD1-IN-7	Histone Demethylase	Inflammation/Immunology Cancer
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .

HY-129923

(R)-Omeprazole sodium	Cytochrome P450	Neurological Disease
(R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .

HY-P5272

Histatin-3 TFA	Bacterial	Inflammation/Immunology
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant K_i of 1.98 μM .

HY-110137A

Furamidine DB75; NSC 305831	Histone Methyltransferase Phosphodiesterase (PDE) Parasite	Infection Inflammation/Immunology Cancer
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .

HY-162837

AURKA against 1	Aurora Kinase	Cancer
AURKA against 1 is an inhibitor of AURKA (IC₅₀ less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3 .

HY-123129

RS 2232	5-HT Receptor Monoamine Oxidase	Neurological Disease
RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a K_i of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research .

HY-116866

Sclerotiorin	Lipoxygenase Fungal	Infection Inflammation/Immunology
Sclerotiorin is a reversible and uncompetitive inhibitor against soybean lipoxygenase-1 (LOX-1) (IC₅₀: 4.2 μM). Sclerotiorin also shows antioxidant activity by scavenging free radical (ED₅₀: 0.12 μM), and nonenzymatic lipid peroxidation inhibition activity. Sclerotiorin has antifungal activity, and also inhibits platelet aggregation. Sclerotiorin can be purified from the fermented broth of Penicillium frequentans .

HY-N0313R

Euphol (Standard)	MAGL Endogenous Metabolite Reference Standards	Inflammation/Immunology
Euphol (Standard) is the analytical standard of Euphol. This product is intended for research and analytical applications. Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .

HY-120826

A2AAR/hMAO-B-IN-1	Monoamine Oxidase Adenosine Receptor	Neurological Disease
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC₅₀: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .

HY-165498

AU-461	Na+/K+ ATPase	Metabolic Disease
AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers .

HY-13007A

PF-3758309 hydrochloride PF-03758309 hydrochloride	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-13007B

PF-3758309 dihydrochloride PF-03758309 dihydrochloride	PAK Apoptosis	Cancer
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .

HY-101578

2614W94	Monoamine Oxidase	Neurological Disease
2614W94 is a selective, reversible and orally active monoamine oxidase-A (MAO-A) inhibitor with an IC₅₀ of 5 nM and a K_i of 1.6 nM. 2614W94 shows no significant inhibition of MAO-B. 2614W94 has antidepressant and anxiolytic effects .

HY-157472

ACT-1014-6470	Complement System	Inflammation/Immunology
ACT-1014-6470 is an orally active, potent, reversible, and selective C5aR1 antagonist. ACT-1014-6470 demonstrates potent inhibition of C5aR1 activation. ACT-1014-6470 can be used in the research of inflammatory diseases .

HY-15185R

Nirogacestat (Standard) PF-3084014 (Standard)	γ-secretase Apoptosis Reference Standards	Cancer
Nirogacestat (Standard) is the analytical standard of Nirogacestat. This product is intended for research and analytical applications. Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .

HY-129388C

Pulrodemstat hydrochloride CC-90011 hydrochloride; LSD1-IN-7 hydrochloride	Histone Demethylase	Inflammation/Immunology Cancer
Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC₅₀ value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .

HY-139664B

(S)-GSK-3685032	DNA Methyltransferase	Cancer
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC₅₀ of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .

HY-164002

PF-303	Btk	Others
PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC₅₀=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .

HY-162633

USP1-IN-9	Deubiquitinase	Cancer
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC₅₀ of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .

HY-19651A

Zanapezil TAK-147	Cholinesterase (ChE)	Neurological Disease
Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .

HY-19651B

Zanapezil fumarate TAK-147 fumarate	Cholinesterase (ChE)	Neurological Disease
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .

HY-163052

Ciproquazone SL-573	Prostaglandin Receptor	Others
Ciproquazone (SL-573) is a compound that inhibits prostaglandin biosynthesis. Its relative inhibitory potency is between that of indomethacin and aspirin, and its inhibition of prostaglandin biosynthesis is reversible.

HY-19651

Zanapezil free base TAK-147 free base	Cholinesterase (ChE)	Neurological Disease
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC₅₀=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with K_i values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .

HY-172764

L-ENIPO hydrochloride	NO Synthase	Metabolic Disease
L-ENIPO (hydrochloride) is an inhibitor of iNOS, nNOS, and eNOS with K_i values of 17, 10.3, and 58.2 μM. L-ENIPO (hydrochloride) exerts reversible tight binding inhibition selective for iNOS with longer incubation time .

HY-103562

DMeOB 3,3'-Dimethoxybenzaldazine	mGluR	Neurological Disease
DMeOB (3,3'-Dimethoxybenzaldazine) is a mGluR5 receptor negative allosteric modulator with an IC₅₀ of 3 μM. DMeOB displays reversible non-competitive inhibition of mGlu5-mediated responses .

HY-144689

BChE-IN-3	Cholinesterase (ChE)	Neurological Disease
BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC₅₀ of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE .

Cat. No.	Product Name

HY-LD004

DEL Covalent Library

14 million compounds

DEL technology enables the simultaneous screening of millions or billions of compounds in a single tube by covalently linking each small molecule with a unique DNA sequence. Traditional DEL screening primarily focuses on identifying non-covalent binding molecules, where interactions with the target are reversible. In contrast, DNA‑encoded covalent library is an ultra‑high‑throughput screening library developed on the basis of conventional DNA‑encoded library technology. It incorporates controllable electrophilic covalent warheads capable of forming irreversible covalent bonds with amino acid residues at the active sites of target proteins, including Cys, Lys, Ser, Tyr, and others. This covalent binding enhances binding affinity, prolongs residence time at the target site, and has the potential to overcome challenges associated with traditional non-covalent inhibitors, such as drug resistance or off-target effects.

Each compound in the library contains both a binding domain and an electrophilic warhead. It first recognizes and binds to the target through non covalent interactions, and then forms a stable covalent bond with key amino acid residues to achieve irreversible inhibition. This library is specifically designed for the discovery of potent, long lasting, and highly selective covalent inhibitors, particularly for undruggable targets such as kinases, GPCRs, proteases, and mutant oncoproteins. Each molecule is uniquely labeled with a DNA barcode for molecular identification and sequencing decoding.

This library is an advanced and highly diverse collection, consists of 35 independent sub-libraries with a total scaleof 14 million compounds, It incorporates over 14 experimentally validated covalent warheads capable of targeting cysteine, lysine, arginine, aspartic acid and glutamic acid. This library is constructed with diverse drug like core scaffolds and integrated controllable covalent warheads, it features structural diversity, reaction spec

Cat. No.	Product Name	Target	Research Area

HY-P5272

Histatin-3 TFA	Bacterial	Inflammation/Immunology
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant K_i of 1.98 μM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0313

Euphol	Triterpenes Classification of Application Fields Terpenoids Euphorbiaceae Plants Inflammation/Immunology Disease Research Fields	MAGL Endogenous Metabolite
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC₅₀=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .

HY-N3474

Isolicoflavonol	Flavonols Flavonoids other families Classification of Application Fields Other Diseases Phenols Polyphenols Plants Disease Research Fields Source Classification	Carboxylesterase (CES)
Isolicoflavonol potently inhibits hCES2A (Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM .

HY-116866

Sclerotiorin	Structural Classification Natural Products Microorganisms Source Classification	Lipoxygenase Fungal
Sclerotiorin is a reversible and uncompetitive inhibitor against soybean lipoxygenase-1 (LOX-1) (IC₅₀: 4.2 μM). Sclerotiorin also shows antioxidant activity by scavenging free radical (ED₅₀: 0.12 μM), and nonenzymatic lipid peroxidation inhibition activity. Sclerotiorin has antifungal activity, and also inhibits platelet aggregation. Sclerotiorin can be purified from the fermented broth of Penicillium frequentans .

HY-N0313R

Euphol (Standard)	Triterpenes Structural Classification Terpenoids Euphorbiaceae Plants	MAGL Endogenous Metabolite Reference Standards
Euphol (Standard) is the analytical standard of Euphol. This product is intended for research and analytical applications. Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .

HY-N13917

Argyrin B	Natural Products Microorganisms Source Classification	Proteasome Bacterial
Argyrin B, a natural product cyclic peptide, is a reversible, non-competitive immunoproteasome inhibitor. Argyrin B shows selective inhibition of the β5i and β1i sites of the immunoproteasome over the β5c and β1c sites of the constitutive proteasome with nearly 20-fold selective inhibition of β1i over the homologous β1c. Argyrin B has antibacterial effects .

Cat. No.	Product Name	Chemical Structure

HY-B0563S1

Ropivacaine-d7

Ropivacaine-d₇ is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain?management .

HY-B0563BS

Ropivacaine-d7 hydrochloride

Ropivacaine-d₇ hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K_2P (two-pore domain potassium channel) TREK-1 with an IC₅₀ of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .

Cat. No.	Product Name		Classification

HY-181268

MAO-B-IN-53		Alkynes
MAO-B-IN-53 is a human monoamine oxidase B (hMAO-B) inhibitor with an IC₅₀ of 0.066 μM. MAO-B-IN-53 exhibits mixed reversible inhibition, binds stably to the hMAO-B active site, and shows high selectivity over hMAO-A. MAO-B-IN-53 acts as a neuroprotective agent, protects against 6-OHDA-induced damage, and exhibits low neurotoxicity in neuroblastoma cells. MAO-B-IN-53 can be used for the research of Parkinson's disease .

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