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Results for "

Reversible Inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adenosine Receptor (1) Apoptosis (6) Aurora Kinase (1) Bacterial (1) Btk (2) Carboxylesterase (1) Cholinesterase (ChE) (4) COMT (1) Deubiquitinase (2) Dipeptidyl Peptidase (1) DNA Methyltransferase (2) EGFR (1) Endogenous Metabolite (1) Fatty Acid Synthase (FASN) (1) Fungal (1) Glucosidase (1) Histone Demethylase (3) Histone Methyltransferase (2) HIV (1) Isotope-Labeled Compounds (2) Lipoxygenase (2) MAGL (2) Monoamine Oxidase (5) PAK (3) Parasite (2) Phosphodiesterase (PDE) (2) Potassium Channel (7) Proton Pump (1) Reactive Oxygen Species (2) Sodium Channel (7) YAP (1) γ-secretase (2)
By Research Areas:	Cancer (25) Cardiovascular Disease (8) Infection (4) Inflammation/Immunology (6) Metabolic Disease (5) Neurological Disease (19)

By Targets:

Adenosine Receptor (1)

Apoptosis (6)

Aurora Kinase (1)

Bacterial (1)

Btk (2)

Carboxylesterase (1)

Cholinesterase (ChE) (4)

COMT (1)

Deubiquitinase (2)

Dipeptidyl Peptidase (1)

DNA Methyltransferase (2)

EGFR (1)

Endogenous Metabolite (1)

Fatty Acid Synthase (FASN) (1)

Fungal (1)

Glucosidase (1)

Histone Demethylase (3)

Histone Methyltransferase (2)

HIV (1)

Isotope-Labeled Compounds (2)

Lipoxygenase (2)

MAGL (2)

Monoamine Oxidase (5)

PAK (3)

Parasite (2)

Phosphodiesterase (PDE) (2)

Potassium Channel (7)

Proton Pump (1)

Reactive Oxygen Species (2)

Sodium Channel (7)

YAP (1)

γ-secretase (2)

By Research Areas:

Cancer (25)

Cardiovascular Disease (8)

Infection (4)

Inflammation/Immunology (6)

Metabolic Disease (5)

Neurological Disease (19)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101578

2614W94	Monoamine Oxidase	Neurological Disease
2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC₅₀ of 5 nM and K_i of 1.6 nM with serotonin as substrate.

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-139603

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

HY-N3474

Isolicoflavonol	Carboxylesterase	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-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-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-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-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	Others	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-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 .

HY-17543

ML-323 Maximum Cited Publications 12 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-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-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-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-15958A

(S,R,R)-VBY-825	Others	Cancer
(S,R,R)-VBY-825 is the isomer of VBY-825 (HY-15958), and can be used as an experimental control. VBY-825 is a novel reversible inhibitor of cathepsin with high inhibition of cathepsin B, L, S and V.

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-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-139664

GSK-3685032 5 Publications Verification	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-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-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-129923

(R)-Omeprazole sodium	Others	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-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-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-100414

Soraprazan 1 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-B0563B

Ropivacaine hydrochloride 5 Publications Verification	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-B0563

Ropivacaine 5 Publications Verification	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-129388A

Pulrodemstat CC-90011; LSD1-IN-7	Histone Demethylase	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, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .

HY-14205

NW-1772	Monoamine Oxidase	Neurological Disease
NW-1772 (methanesulfonate) (compound 22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .

HY-113725

L 668411	Others	Others
L 668411 is a β-lactone inhibitor with activity against 3-hydroxy-3-methylglutaryl-CoA synthase and cholesterol biosynthesis. L 668411 inhibits rat liver cytosolic 3-hydroxy-3-methylglutaryl-CoA synthase and [14C] acetate incorporation into sterols in cultured Hep G2 cells, and the inhibition appears to be irreversible in cells but reversible in cultured cells and animals.

HY-155137

CHBO4	Monoamine Oxidase Reactive Oxygen Species	Neurological Disease
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC₅₀ value of 0.031 μM in CHBO subseries and an K_i value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research .

HY-B0563A

Ropivacaine hydrochloride monohydrate 5 Publications Verification	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-129388B

Pulrodemstat benzenesulfonate 2 Publications Verification CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate	Histone Demethylase	Cancer
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. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .

HY-139664B

(S)-GSK-3685032	Others	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-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-116973

L 738372	HIV	Infection
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (K_i) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .

HY-129388

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

HY-B0563C

Ropivacaine mesylate 5 Publications Verification	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1] . 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 .

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[1][2]. 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[3]. Ropivacaine is used for the research of neuropathic pain management[1].

HY-156078

α-Glucosidase-IN-32	Glucosidase	Metabolic Disease
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC₅₀ value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .

HY-B0563R

Ropivacaine (Standard)	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Ropivacaine (Standard) is the analytical standard of Ropivacaine. This product is intended for research and analytical applications. 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-B0563AR

Ropivacaine hydrochloride monohydrate (Standard)	Sodium Channel Potassium Channel	Cardiovascular Disease Neurological Disease Cancer
Ropivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Ropivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. 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-B0563BS

Ropivacaine-d7 hydrochloride	Isotope-Labeled Compounds	Neurological Disease
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 .

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-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-U00346A

TS-021	Dipeptidyl Peptidase	Metabolic Disease
TS-021 is a selective, orally active, reversible and long-acting DPP-IV inhibitor, and exhibits significant inhibition selectivity against DPP-8 (> 600 fold), DPP-9 (> 1200 fold) and other peptidases (> 15,000 fold). TS-021 inhibits DPP-IV activity in human plasma with an IC₅₀ value of 5.34 nM. TS-021 has long-term persistent plasma drug concentration and potent antihyperglycemic activity, and increases in the active form of GLP-1 .

HY-16731

Sembragiline EVT 302; RG1577; RO4602522	Monoamine Oxidase Reactive Oxygen Species	Neurological Disease
Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity .

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-110137

Furamidine dihydrochloride 2 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 .

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 .

HY-137409

Suc-AAA-pNA	Peptides	Others
Suc-AAA-pNA?is the substrate of analysis of the reversible inhibition of porcine pancreatic elastase (PPE) .

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[1][2]. 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[3]. Ropivacaine is used for the research of neuropathic pain management[1].

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 .

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