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Results for "

hERG protein

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) AAK1 (1) Arrestin (1) Autophagy (10) Bacterial (8) Beta-secretase (1) CCR (1) Cytochrome P450 (2) DNA/RNA Synthesis (3) Dopamine Receptor (1) Drug Derivative (1) Epigenetic Reader Domain (1) ERK (1) Eukaryotic Initiation Factor (eIF) (1) FAP (1) GLUT (1) Glycosidase (1) GPR68 (1) HBV (1) HMG-CoA Reductase (HMGCR) (10) HSP (4) Interleukin Related (1) Isotope-Labeled Compounds (2) Keap1-Nrf2 (1) Lipocalin Family (1) Opioid Receptor (1) p38 MAPK (1) Potassium Channel (27) Protein Arginine Deiminase (1) Reference Standards (6) SARS-CoV (1) Serotonin Transporter (2) Sodium Channel (5) Taste Receptor (3) Virus Protease (1) WDR5 (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (19) Infection (3) Inflammation/Immunology (9) Metabolic Disease (12) Neurological Disease (8)

By Targets:

5-HT Receptor (1)

AAK1 (1)

Arrestin (1)

Autophagy (10)

Bacterial (8)

Beta-secretase (1)

CCR (1)

Cytochrome P450 (2)

DNA/RNA Synthesis (3)

Dopamine Receptor (1)

Drug Derivative (1)

Epigenetic Reader Domain (1)

ERK (1)

Eukaryotic Initiation Factor (eIF) (1)

FAP (1)

GLUT (1)

Glycosidase (1)

GPR68 (1)

HBV (1)

HMG-CoA Reductase (HMGCR) (10)

HSP (4)

Interleukin Related (1)

Isotope-Labeled Compounds (2)

Keap1-Nrf2 (1)

Lipocalin Family (1)

Opioid Receptor (1)

p38 MAPK (1)

Potassium Channel (27)

Protein Arginine Deiminase (1)

Reference Standards (6)

SARS-CoV (1)

Serotonin Transporter (2)

Sodium Channel (5)

Taste Receptor (3)

Virus Protease (1)

WDR5 (1)

By Research Areas:

Cancer (17)

Cardiovascular Disease (19)

Infection (3)

Inflammation/Immunology (9)

Metabolic Disease (12)

Neurological Disease (8)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17504

Rosuvastatin Calcium Maximum Cited Publications 24 Publications Verification Rosuvastatin hemicalcium; ZD 4522 Calcium	HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504A

Rosuvastatin Maximum Cited Publications 24 Publications Verification ZD 4522	HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks *hERG* current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-19620

Branaplam 10+ Cited Publications LMI070; NVS-SM1	DNA/RNA Synthesis Potassium Channel	Cancer
Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC₅₀ of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC₅₀ of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .

HY-17504B

Rosuvastatin Sodium Maximum Cited Publications 24 Publications Verification ZD 4522 Sodium; X-Plended Sodium; Crestor Sodium	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-153714

Zefamenib BN-104; BNM-1192; Menin-MLL inhibitor 27	Epigenetic Reader Domain Potassium Channel	Cancer
Zefamenib (BN-104) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. Zefamenib is a weak *hERG* inhibitor, with an IC₅₀ greater than 100 μM. Zefamenib has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia .

HY-N1934

Dihydroberberine	Potassium Channel HSP	Cardiovascular Disease Inflammation/Immunology Cancer
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

HY-12533

Disopyramide 2 Publications Verification Dicorantil; SC-7031	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action .

HY-163387

CHI3L1-IN-1	Glycosidase Potassium Channel	Inflammation/Immunology Cancer
CHI3L1-IN-1 (Compound 30) is an inhibitor for Chitinase-3-like protein 1 (CHI3L1) (YKL-40) with IC₅₀ of 50 nM. CHI3L1-IN-1 inhibits hERG channel with an IC₅₀ of 2.3 μM .

HY-19620A

Branaplam hydrochloride 10+ Cited Publications LMI070 hydrochloride; NVS-SM1 hydrochloride	DNA/RNA Synthesis Potassium Channel	Cancer
Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC₅₀ of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC₅₀ of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .

HY-134494

MS48107 2 Publications Verification	GPR68	Neurological Disease
MS48107 is a potent and selective positive allosteric modulator of *G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68* over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .

HY-111747

TBAJ-587 3 Publications Verification	Bacterial	Infection Cardiovascular Disease
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC₉₀s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .

HY-12533A

Disopyramide phosphate 2 Publications Verification Dicorantil phosphate; SC-7031 phosphate	Potassium Channel Sodium Channel	Cardiovascular Disease
Disopyramide phosphate is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action .

HY-122351A

Advantame	Taste Receptor	Others
Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K ⁺ channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .

HY-136832

Noribogaine hydrochloride	Serotonin Transporter Potassium Channel Arrestin Opioid Receptor	Cardiovascular Disease Neurological Disease
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC₅₀=50-300 nM) and *hERG* channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits β-arrestin recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .

HY-175802

HBI-2375 HYBI-084	WDR5 Potassium Channel	Inflammation/Immunology Cancer
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC₅₀ of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 ⁺ cytotoxic T lymphocyte infiltration. HBI-2375 inhibits *hERG* with an IC₅₀ of 17 µM .

HY-17504R

Rosuvastatin Calcium (Standard) 10+ Cited Publications Rosuvastatin hemicalcium (Standard); ZD 4522 Calcium (Standard)	Reference Standards HMG-CoA Reductase (HMGCR) Autophagy Potassium Channel Bacterial	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin (Calcium) (Standard) is the analytical standard of Rosuvastatin (Calcium). This product is intended for research and analytical applications. Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Calcium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-131335

p38α inhibitor 2	p38 MAPK	Inflammation/Immunology
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC₅₀ of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC₅₀=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .

HY-17504AS1

Rosuvastatin-d6 ZD 4522-d₆	Isotope-Labeled Compounds Autophagy Bacterial HMG-CoA Reductase (HMGCR) Potassium Channel	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin-d₆ (ZD 4522-d₆) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks *hERG* current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504BS1

Rosuvastatin-d6 sodium	HMG-CoA Reductase (HMGCR) Autophagy	Cardiovascular Disease Metabolic Disease
Rosuvastatin-d₆ sodium is deuterium labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

HY-N1934R

Dihydroberberine (Standard)	Reference Standards Potassium Channel HSP	Cardiovascular Disease Inflammation/Immunology Cancer
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

HY-149431

NDNA4	HSP Potassium Channel	Cancer
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC₅₀: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC₅₀ >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .

HY-17504BR

Rosuvastatin Sodium (Standard) ZD 4522 Sodium (Standard); X-Plended Sodium (Standard); Crestor Sodium (Standard)	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy Bacterial Reference Standards	Cardiovascular Disease Metabolic Disease Cancer
Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504BS2

Rosuvastatin-13C,d3 sodium ZD 4522-13C,d3 sodium; X-Plended-13C,d3 sodium; Crestor-13C,d3 sodium	Autophagy Bacterial HMG-CoA Reductase (HMGCR) Potassium Channel Isotope-Labeled Compounds	Cardiovascular Disease Metabolic Disease
Rosuvastatin- ¹³C,d₃ sodium is ¹³C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks *hERG* current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504D

(3S,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC₅₀ of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504C

(3R,5R)-Rosuvastatin	HMG-CoA Reductase (HMGCR) Potassium Channel Autophagy	Cardiovascular Disease Metabolic Disease
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM . Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC₅₀ of 195 nM . Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-159931

HW161023	AAK1	Neurological Disease
HW161023 (compound 5) is an orally active *AP2-associated protein* kinase 1 (AAK1) inhibitor with IC₅₀ values of 5.4 nM and 11.9 μM aganist of AAK1and hERG**, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model .

HY-175258

PAD2/4-IN-1	Protein Arginine Deiminase Potassium Channel	Neurological Disease Inflammation/Immunology Cancer
PAD2/4-IN-1 (Compound 4f) is an orally active inhibitor of PAD2 and PAD4 with IC₅₀ values of 23 nM and 10 nM, respectively. PAD2/4-IN-1 can inhibit protein citrullination in neutrophils and reduce *hERG* channel liabilities. PAD2/4-IN-1 can be used in the research of autoimmune diseases, neurological disorders, and cancers .

HY-172350

WEHI-P8	SARS-CoV Virus Protease Interleukin Related	Infection
WEHI-P8 is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC₅₀ of 12 nM and a K_d of 9.0 nM. WEHI-P8 reduces viral load, body weight loss, pulmonary inflammation, immune cell infiltration and pro-inflammatory mediator levels in SARS-CoV-2-infected mice. WEHI-P8 prevents pulmonary hemorrhage, immune cell infiltration, fibrotic remodeling and neuroinflammation, and improves cognitive function in a mouse model of post-acute sequelae of SARS-CoV-2 infection (PASC). WEHI-P8 is applicable for the research of COVID-19 and PASC .

HY-157929

Keap1-Nrf2-IN-19	Keap1-Nrf2	Inflammation/Immunology Cancer
Keap1-Nrf2-IN-19 (compound 33) is an oral active *Keap1-Nrf2 protein–protein* interaction (PPI) inhibitor with the K_d** value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .

HY-12533B

Disopyramide hydrochloride Dicorantil hydrochloride; SC-7031 hydrochloride	Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide hydrochloride is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide hydrochloride blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide hydrochloride inhibits HERG encoded potassium channels. Disopyramide hydrochloride also exhibits complex protein binding, and has a potent negative inotropic action .

HY-103268

(Rac)-AZD3839	Potassium Channel	Neurological Disease
(Rac)-AZD3839 is an orally active beta-amyloid precursor protein cleaving enzyme (BACE1) inhibitor that is blood-brain barrier-permeable. (Rac)-AZD3839 has an affinity for the human ether-a-go-go related gene (hERG) ion channel. (Rac)-AZD3839 can be used in the research of Alzheimer's disease .

HY-130244

BACE1-IN-5	Beta-secretase	Neurological Disease
BACE1-IN-5 (Compound 15) is a *β-site amyloid precursor protein* cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC₅₀** of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .

HY-12533R

Disopyramide (Standard) Dicorantil (Standard); SC-7031 (Standard)	Reference Standards Sodium Channel Potassium Channel	Cardiovascular Disease
Disopyramide (Standard) is the analytical standard of Disopyramide. This product is intended for research and analytical applications. Disopyramide (Dicorantil) is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide inhibits HERG encoded potassium channels. Disopyramide also exhibits complex protein binding, and has a potent negative inotropic action .

HY-12533AR

Disopyramide phosphate (Standard) Dicorantil phosphate (Standard); SC-7031 phosphate (Standard)	Potassium Channel Sodium Channel Reference Standards	Cardiovascular Disease
Disopyramide (phosphate) (Standard) is the analytical standard of Disopyramide (phosphate). This product is intended for research and analytical applications. Disopyramide phosphate is a class IA antiarrhythmic agent with efficacy in ventricular and atrial arrhythmias. Disopyramide phosphate blocks the fast inward sodium current of cardiac muscle and prolongs the duration of cardiac action potentials. Disopyramide phosphate inhibits HERG encoded potassium channels. Disopyramide phosphate also exhibits complex protein binding, and has a potent negative inotropic action .

HY-149432

NDNA3	HSP Potassium Channel	Cancer
NDNA3 (compound 14) is a selective inhibitor of Hsp90α (IC₅₀: 0.51 μM). NDNA3 is a permanently charged analog with low membrane permeability and low toxicity to Ovcar-8 (IC₅₀: 12.66 μM) and MCF-10A (IC₅₀: 11.72 μM) cells. NDNA3 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .

HY-122351

Advantame free acid	Drug Derivative Taste Receptor	Others
Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K ⁺ channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .

HY-122351AR

Advantame (Standard)	Reference Standards Taste Receptor	Others
Advantame (Standard) is the analytical standard of Advantame. This product is intended for research and analytical applications. Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K ⁺ channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .

HY-182735

BMS-570520	CCR Cytochrome P450 5-HT Receptor Dopamine Receptor Serotonin Transporter	Inflammation/Immunology
BMS-570520 is an orally bioavailable CCR3 antagonist with an IC₅₀ of 1.9 nM against hCCR3 and an IC₅₀ of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the *hERG* potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis .

HY-182385

BPN-14136	Lipocalin Family	Metabolic Disease
BPN-14136 is an orally effective retinol-binding protein 4 (RBP4) inhibitor. BPN-14136 inhibits the binding of retinol to RBP4 with an IC₅₀ of 12.8 nM. BPN-14136 inhibits retinol-dependent RBP4-transthyretin interaction (IC₅₀ = 43.6 nM) and reduces circulating plasma RBP4 levels in vivo. BPN-14136 decreases the formation of cytotoxic bisretinoids in retinal pigment epithelial cells. BPN-14136 can be used for the research of atrophic age-related macular degeneration and Stargardt disease .

HY-124640

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

HY-182250

BR103354	FAP ERK GLUT	Metabolic Disease Inflammation/Immunology
BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis .

HY-181406

eIF2B activator-1	Eukaryotic Initiation Factor (eIF) Potassium Channel	Neurological Disease
eIF2B activator-1 (Compound 7a) is a eIF2B activator with a pEC₅₀ value of 7.3. eIF2B activator-1 exhibits significant hERG inhibitory activity, with a pIC₅₀ value of 5.7. eIF2B activator-1 can be used in research related to Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS).

HY-183260

HBV-IN-57	HBV Cytochrome P450	Infection
HBV-IN-57 is an orally active HBV inhibitor with pan-genotypic efficacy against HBV genotypes B/C. HBV-IN-57 inhibits HBV DNA replication and HBV capsid assembly. HBV-IN-57 can be used for the research of chronic hepatitis B .

Cat. No.	Product Name

HY-L923

Ion Channel Lead-like Compound Library	9000 compounds
Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields. MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Ion Channel Lead-like Compound Library

9000 compounds

Ion channels are key proteins on the cell membrane that regulate the flow of ions across membranes. They participate in nearly all physiological processes, including nerve conduction, muscle contraction, heart rhythm, and pain perception. Abnormalities in their function can lead to various serious diseases such as arrhythmia, epilepsy, hypertension, neuropathic pain, and cancer. Therefore, ion channels are highly valuable drug targets—over 15% of approved drugs target ion channels currently, demonstrating their irreplaceable therapeutic value in cardiovascular, neurological, and analgesic fields.

MCE has collected a library of over 5,000 reported ion channel-related bioactive compounds targeting major sites such as Na+ channels, K+ channels, Ca2+ channels, GABA receptors, iGluRs, and others. Using AI models, these compounds are characterized through both 2D representations (molecular fingerprints, pharmacophores) and 3D representations (3D conformation) to screen for a collection of lead-like compounds highly similar to known active molecules. Additionally, an hERG channel prediction algorithm integrating XGB and ISE mapping strategy is employed to assess and exclude potential cardiotoxicity in the library.. This step significantly reduces safety risks in subsequent screenings, particularly for ion channel drug development related to cardiovascular systems (e.g., Nav1.5, Cav1.2), effectively minimizing failures due to hERG inhibition and serving as a valuable tool for ion channel drug screening.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1934

Dihydroberberine	Cardiovascular Disease Alkaloids other families Classification of Application Fields Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields Source Classification	Potassium Channel HSP
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

HY-N1934R

Dihydroberberine (Standard)	Alkaloids Structural Classification other families Plants Isoquinoline Alkaloids Source Classification	Reference Standards Potassium Channel HSP
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .

Species:	Human (2)
Tag:	GFP (1) His (1)
Source:	HEK293 (2)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P701834

	hERG Protein, Human (HEK293, GFP, His) KCNH2; Potassium voltage-gated channel subfamily H member 2; Eag homolog; Ether-a-go-go-related gene potassium channel 1; ERG-1; Eag-related protein 1; Ether-a-go-go-related protein 1; H-ERG; hERG-1; hERG1; Voltage-gated potassium channel subunit Kv11.1	Human	HEK293
	The hERG protein is the α subunit of voltage-gated potassium channels and is critical for mediating cardiac delayed rectifier potassium current (IKr). It lacks individual channel activity but dynamically affects properties by forming heterotetramers with other isoforms. hERG Protein, Human (HEK293, GFP, His) is the recombinant human-derived hERG protein, expressed by HEK293 , with C-10*His, C-GFP labeled tag.

HY-P703937

	hERG Protein, Human (HEK293) Voltage-gated inwardly rectifying potassium channel KCNH2; Eag homolog; Ether-a-go-go-related gene potassium channel 1; ERG-1; Eag-related protein 1; Ether-a-go-go-related protein 1; H-ERG; hERG-1; hERG1; Potassium voltage-gated channel subfamily H member 2; Voltage-gated potassium channel subunit Kv11.1	Human	HEK293
	The hERG protein is the α subunit of voltage-gated potassium channels and is critical for mediating cardiac delayed rectifier potassium current (IKr). It lacks individual channel activity but dynamically affects properties by forming heterotetramers with other isoforms. hERG Protein, Human (HEK293) is the recombinant human-derived hERG protein, expressed by HEK293, with tag free.

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Cat. No.	Product Name	Chemical Structure

HY-17504AS1

Rosuvastatin-d6

Rosuvastatin-d₆ (ZD 4522-d₆) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC₅₀ of 11 nM. Rosuvastatin potently blocks hERG current with an IC₅₀ of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

HY-17504BS1

Rosuvastatin-d6 sodium

Rosuvastatin-d₆ sodium is deuterium labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.

HY-17504BS2

Rosuvastatin-13C,d3 sodium

Rosuvastatin- ¹³C,d₃ sodium is ¹³C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC₅₀ of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC₅₀ of 195 nM . Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels .

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