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hERG activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (9) Akt (1) Antibiotic (6) Apoptosis (3) Autophagy (7) Bacterial (11) Calcium Channel (3) CCR (1) CDK (1) CRAC Channel (1) CXCR (1) Cytochrome P450 (11) Dopamine Receptor (3) Drug Derivative (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (1) Eukaryotic Initiation Factor (eIF) (1) FGFR (1) GLP Receptor (1) Glucocorticoid Receptor (2) HBV (1) HCV (1) HCV Protease (2) Histamine Receptor (5) Histone Demethylase (1) HIV (1) HSP (2) IDE (1) iGluR (4) Isotope-Labeled Compounds (4) LRRK2 (1) METTL3 (1) MNK (1) Opioid Receptor (2) P-glycoprotein (1) Parasite (4) Phosphatase (1) Phosphorylase (1) PI4K (1) Pim (1) Potassium Channel (28) Proteolytic Enzyme (1) Ras (1) Reference Standards (9) Reverse Transcriptase (1) Ser/Thr Protease (1) Sigma Receptor (1) SOS1 (1) Taste Receptor (3) TGF-β Receptor (1) Topoisomerase (1) TRP Channel (3)
By Research Areas:	Cancer (19) Cardiovascular Disease (8) Endocrinology (6) Infection (19) Inflammation/Immunology (14) Metabolic Disease (4) Neurological Disease (24)

By Targets:

5-HT Receptor (9)

Akt (1)

Antibiotic (6)

Apoptosis (3)

Autophagy (7)

Bacterial (11)

Calcium Channel (3)

CCR (1)

CDK (1)

CRAC Channel (1)

CXCR (1)

Cytochrome P450 (11)

Dopamine Receptor (3)

Drug Derivative (1)

Endogenous Metabolite (1)

Epigenetic Reader Domain (1)

Estrogen Receptor/ERR (1)

Eukaryotic Initiation Factor (eIF) (1)

FGFR (1)

GLP Receptor (1)

Glucocorticoid Receptor (2)

HBV (1)

HCV (1)

HCV Protease (2)

Histamine Receptor (5)

Histone Demethylase (1)

HIV (1)

HSP (2)

IDE (1)

iGluR (4)

Isotope-Labeled Compounds (4)

LRRK2 (1)

METTL3 (1)

MNK (1)

Opioid Receptor (2)

P-glycoprotein (1)

Parasite (4)

Phosphatase (1)

Phosphorylase (1)

PI4K (1)

Pim (1)

Potassium Channel (28)

Proteolytic Enzyme (1)

Ras (1)

Reference Standards (9)

Reverse Transcriptase (1)

Ser/Thr Protease (1)

Sigma Receptor (1)

SOS1 (1)

Taste Receptor (3)

TGF-β Receptor (1)

Topoisomerase (1)

TRP Channel (3)

By Research Areas:

Cancer (19)

Cardiovascular Disease (8)

Endocrinology (6)

Infection (19)

Inflammation/Immunology (14)

Metabolic Disease (4)

Neurological Disease (24)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124702

ICA-105574 1 Publications Verification	Potassium Channel	Cardiovascular Disease
ICA-105574 is a potent and efficacious *hERG* channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC₅₀ value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2 .

HY-17508

Clarithromycin 15+ Cited Publications	Bacterial Cytochrome P450 Autophagy Antibiotic	Infection Cancer
Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-17508R

Clarithromycin (Standard) 15+ Cited Publications	Reference Standards Bacterial Cytochrome P450 Autophagy Antibiotic	Infection Cancer
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-17508S1

Clarithromycin-d3	Isotope-Labeled Compounds Bacterial Antibiotic Autophagy Cytochrome P450	Others
Clarithromycin-d₃ is the deuterium labeled Clarithromycin (HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-14149

Cisapride 1 Publications Verification R 51619; (±)-Cisaprid	5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-149013

Anti-MRSA agent 5	Bacterial	Infection
Anti-MRSA agent 5 (B14) is a potent MRSA agent with MIC₅₀ values of 0.38 μg/mL and has low hERG activity with an IC₅₀ values of >40 μM. Anti-MRSA agent 5 (B14) also has low cytotoxicity to mammal cells and unlikely to acquire bacterial resistance .

HY-146158

Fudapirine WX-081	Bacterial Potassium Channel Antibiotic	Infection
Fudapirine, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. Fudapirine exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. Fudapirine also inhibits hERG channel with the IC50 of 1.89 μM.

HY-120713

MK-8325 dihydrochloride	HCV	Infection
MK-8325 (dihydrochloride) is an inhibitor of HCV NS5A with oral activity. MK-8325 exhibits minimal inhibition on hERG at the concentration of 30 mM .

HY-103399R

Trovafloxacin mesylate (Standard)	Reference Standards Bacterial Topoisomerase Antibiotic	Infection
Clarithromycin (Standard) is the analytical standard of Clarithromycin. This product is intended for research and analytical applications. Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-153240

ACT-672125	CXCR	Inflammation/Immunology
ACT-672125 is a potent CXCR3 antagonist with IC₅₀ value of 239 nM in human blood. ACT-672125 has activity for hERG with IC₅₀ value of 18μM. ACT-672125 can be used for the research of autoimmune diseases .

HY-173278

AIC263282	HBV Potassium Channel	Infection
AIC263282 is a potent Hepatitis B Virus (HBV) capsid assembly modulator with an EC₅₀ of 3.8 nM. AIC263282 shows an IC₅₀ of 61 nM for *hERG. AIC263282 exhibits activity* against viral replication and hepatitis B surface antigen (HBsAG) on primary human hepatocytes .

HY-116838

TAM-16	Bacterial	Infection
TAM-16 is a potent and orally active polyketide synthase 13 (Pks13) inhibitor with an IC₅₀ value of 0.32 μM. TAM-16 has promising activity against Mycobacterium tuberculosis. TAM-16 inhibits hERG cardiac ion channel .

HY-172953

Insecticidal agent 24	Parasite	Infection
Insecticidal agent 24 is an orally active pyridylspiroindoline frontrunner. Insecticidal agent 24 has antiplasmodial activity (Pf NF54 IC₅₀: 0.08 μM). Insecticidal agent 24 inhibits hERG activity (IC₅₀: 6.5 μM). Insecticidal agent 24 reduces parasitemia in a humanized immunodeficient NSG mouse Plasmodium falciparum infection model .

HY-W157689

IDE-IN-2	Proteolytic Enzyme IDE	Infection Metabolic Disease Cancer
IDE-IN-3 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-3 is predicted to have CYP3A4, CYP2C19, hERG, NADP+, HIF1α and histidine kinase inhibitory activities, and has potential biological activity in anti-diabetic, anti-tumor, anti-bacterial aspects, according to the in silico prediction .

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-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-14356

ADL5859	Opioid Receptor Potassium Channel Cytochrome P450	Neurological Disease Inflammation/Immunology
ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an K_i and an EC₅₀ value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 can be used for the research of pain .

HY-12532

Astemizole 5+ Cited Publications R 43512	Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K ⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-13044

ADL-5859 hydrochloride 1 Publications Verification	Opioid Receptor Potassium Channel Cytochrome P450	Neurological Disease Inflammation/Immunology
ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an K_i and an EC₅₀ value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitory activity to hERG channel with an IC₅₀ value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain .

HY-12962

NMDA-IN-1	iGluR	Neurological Disease
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.

HY-144341

DprE1-IN-1	Bacterial	Infection
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.

HY-14149A

Cisapride monohydrate R 51619 monohydrate; (±)-Cisaprid monohydrate	5-HT Receptor	Neurological Disease Metabolic Disease
Cisapride monohydrate is an orally and potent 5-HT₄ receptor agonist and *hERG* inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .

HY-14149R

Cisapride (Standard) R 51619 (Standard); (±)-Cisaprid (Standard)	Reference Standards 5-HT Receptor Potassium Channel	Neurological Disease
Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

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-12532S

Astemizole-d3	Isotope-Labeled Compounds Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole-d₃ is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-156759

METTL3-IN-5	METTL3	Cancer
METTL3-IN-5 (Compound 13) is a METTL3 inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC₅₀ less than 2 μM. METTL3-IN-5 has weak hERG inhibitory activity (IC₅₀ >30 μM). METTL3-IN-5 can be used for AML research .

HY-14149S

Cisapride-d6 R51619-d₆; (±)-Cisaprid-d₆	Isotope-Labeled Compounds 5-HT Receptor Potassium Channel	Neurological Disease
Cisapride-d₆ (R51619-d₆) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-107708

threo-Ifenprodil hemitartrate	iGluR Sigma Receptor Potassium Channel	Neurological Disease
threo Ifenprodil hemitartrate is a σ receptor agonist, with K_is of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC₅₀=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC ₅₀ of 88 nM, showing antiarrhythmic activity .

HY-12532R

Astemizole (Standard) R 43512 (Standard)	Reference Standards Histamine Receptor Potassium Channel	Inflammation/Immunology Endocrinology
Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K ⁺ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-111552

PIM1-IN-1	Pim	Cancer
PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC₅₀s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC₅₀ of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity .

HY-153219A

P-CAB agent 2	Potassium Channel	Endocrinology
P-CAB agent 2 is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 inhibits H ⁺/K ⁺-ATPase activity with an IC₅₀ value of <100 nM. P-CAB agent 2 inhibits the hERG potassium channel with an IC₅₀ value of 18.69 M. P-CAB agent 2 shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .

HY-153219

P-CAB agent 2 hydrochloride	Potassium Channel	Endocrinology
P-CAB agent 2 hydrochloride is a potent and orally active potassium-competitive acid blocker and a gastric acid secretion inhibitor. P-CAB agent 2 hydrochloride inhibits H ⁺/K ⁺-ATPase activity with an IC₅₀ value of <100 nM. P-CAB agent 2 hydrochloride inhibits the hERG potassium channel with an IC₅₀ value of 18.69 M. P-CAB agent 2 hydrochloride shows no acute toxicity and inhibits histamine (HY-B1204)-induced gastric acid secretion .

HY-121495

BKI-1369	Parasite	Infection
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC₅₀ of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .

HY-133012

GFB-8438	TRP Channel	Neurological Disease
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model .

HY-158365

LRRK2-IN-14	LRRK2	Neurological Disease
LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC₅₀ of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on *hERG* (IC₅₀=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .

HY-W777120

Cisapride-13C,d3 R 51619-13C,d3; (±)-Cisaprid-_{13_{C_,d₃}}	Isotope-Labeled Compounds 5-HT Receptor Potassium Channel	Neurological Disease
Cisapride- ¹³C,d₃ (R 51619- ¹³C,d₃) is the deuteriumand ¹³C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a hERG blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-172090

MASP-2-IN-1	Ser/Thr Protease Potassium Channel	Inflammation/Immunology
MASP-2-IN-1 (Compound 77) is the inhibitor for mannan-binding lectin-associated serine protease (MASP), that inhibits MASP2 and MASP3 with IC₅₀ of 11.4 nM and 13.2 µM. MASP-2-IN-1 exhibits a weak inhibitory activity against *hERG* with an IC₅₀ of 175 µM. MASP-2-IN-1 reveals a poor stability in mouse plasma with a half-life of 4.4 hours .

HY-163479

MNK1/2-IN-7	Eukaryotic Initiation Factor (eIF) MNK	Cancer
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970) .

HY-109968A

Irdabisant hydrochloride CEP-26401 hydrochloride	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .

HY-109968

Irdabisant CEP-26401	Histamine Receptor	Neurological Disease
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .

HY-119101

AZD-5672 1 Publications Verification	CCR Potassium Channel P-glycoprotein	Inflammation/Immunology
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC₅₀=0.32 nM). AZD-5672 shows moderate activity against the *hERG* ion channel (binding IC₅₀=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC₅₀=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .

HY-17442

Azathramycin Azaerythromycin A; Desmethyl Azithromycin	Bacterial Antibiotic	Infection
Azathramycin (Desmethyl Azithromycin) is a macrolide antibiotic. Azathramycin is a derivative of the anti-ribosomal antibiotic Azithromycin (HY-17506). Azathramycin exerts its antibacterial activity by binding to ribosomes and inhibiting bacterial protein synthesis. Azathramycin can selectively target and kill human senescent fibroblasts and is expected to be used in anti-aging research. Azathramycin affects multiple ion channels such as SCN5A, hERG, KCNQ1 + KCNE1, L-type Ca ⁺⁺ and K_ir2.1 .

HY-144437

ALK5-IN-9	TGF-β Receptor	Cancer
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC₅₀ values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .

HY-150562

CDK9-IN-19	CDK	Cancer
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .

HY-100001

SKF-96365 hydrochloride 20+ Cited Publications	TRP Channel CRAC Channel Potassium Channel Autophagy Apoptosis	Cardiovascular Disease Cancer
SKF-96365 hydrochloride is a potent TRP channel blocker and a store-operated Ca ²⁺ entry (SOCE) inhibitor. SKF-96365 hydrochloride significantly inhibits hERG, hKCNQ1/hKCNE1, hKir2.1 and hKv4.3 current, and significantly prolongs the QTc interval in isolated guinea pig hearts. SKF-96365 hydrochloride exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal cancer cells .

HY-B1467

Domiphen bromide 1 Publications Verification	Potassium Channel Bacterial Parasite Phosphatase	Infection Inflammation/Immunology
Domiphen bromide is a cationic active quaternary ammonium salt and also an inhibitor of *HERG* channels (IC₅₀: 9 nM), aminopeptidase-like enzymes, Escherichia coli alkaline phosphatase, and α-chymotrypsin. Domiphen bromide has multiple activities such as antibacterial, antimalarial, and disinfectant properties, and it is also a synergist of Colistin (HY-113678). Domiphen bromide can be used as a chemical preservative and a cationic surfactant, and it can also be used in the research of bacterial infectious diseases such as pharyngitis, thrush, and oral ulcers .

HY-157425

5-HT2CR agonist 1	5-HT Receptor	Neurological Disease
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT_2CR partial agonist (E_max=71.09%) with an EC₅₀ value of 121.5 nM and no observed activity toward 5-HT_2AR or 5-HT_2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .

HY-12946

BI 653048	Glucocorticoid Receptor Cytochrome P450 HCV Protease	Infection Inflammation/Immunology
BI 653048 is a selective and orally active nonsteroidal glucocorticoid (GC) agonist with an IC₅₀ value of 55 nM . BI 653048 inhibits CP1A2, CYP2D6, CYP2C9, CYP2C19 and CYP3A4 isoforms’ activity and reduces affinity for the hERG ion channel (IC₅₀>30 μM) . BI 653048 (Compound 103) is also a HCV NS3 protease inhibitor that can reduce viral loads infected with the hepatitis C virus .

HY-103309A

ML218 hydrochloride	Calcium Channel	Neurological Disease
ML218 hydrochloride is a potent, selective and orally active T-type Ca ²⁺ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier .

HY-103309

ML218 2 Publications Verification	Calcium Channel	Neurological Disease
ML218 is a potent, selective and orally active T-type Ca ²⁺ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, K_ATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1934

Dihydroberberine	Cardiovascular Disease Alkaloids Structural Classification other families Classification of Application Fields Source classification Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields	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 Source classification Plants Isoquinoline Alkaloids	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 .

HY-W041470R

4-Methyl-1-phenyl-2-pentanone (Standard)	Structural Classification Ketones, Aldehydes, Acids Source classification Endogenous metabolite	Reference Standards Endogenous Metabolite
Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .

Cat. No.	Product Name	Chemical Structure

HY-17508S1

Clarithromycin-d3

Clarithromycin-d₃ is the deuterium labeled Clarithromycin (HY-17508) . Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC₅₀ (K_i) value of 56 (43) μM . Clarithromycin significantly inhibits the HERG potassium current .Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K .

HY-12532S

Astemizole-d3
Astemizole-d₃ is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC₅₀ of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC₅₀ of 0.9 nM. Astemizole has antipruritic effects .

HY-14149S

Cisapride-d6
Cisapride-d₆ (R51619-d₆) is deuterium labeled Cisapride. Cisapride (R 51619) is an orally active 5-HT₄ receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a *hERG* blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-W777120

Cisapride-13C,d3
Cisapride- ¹³C,d₃ (R 51619- ¹³C,d₃) is the deuteriumand ¹³C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC₅₀ value of 140 nM. Cisapride is a hERG blocker with an IC₅₀ value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity .

HY-103309S

ML218-d9

ML218-d₉ is the deuterium labeled ML218. ML218 is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC₅₀s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 can penetrate the blood-brain barrier .

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