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HEK

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) 5-HT Receptor (14) Adrenergic Receptor (1) AMPK (1) Amylases (1) Amyloid-β (1) Androgen Receptor (2) Antibiotic (3) Apelin Receptor (APJ) (5) Apoptosis (14) ASCT (4) ATP Synthase (1) Aurora Kinase (4) Autophagy (12) AUTOTACs (2) Bacterial (15) Bcl-2 Family (1) BCRP (2) BMI1 (2) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (1) c-Fms (1) Calcium Channel (4) CaMK (1) Casein Kinase (1) CaSR (2) CDK (1) CFTR (1) Cholinesterase (ChE) (1) CMV (2) Cytochrome P450 (2) DNA/RNA Synthesis (3) Dopamine Receptor (4) Dopamine Transporter (3) Drug Metabolite (1) EAAT (1) EGFR (2) Endogenous Metabolite (15) Enolase (2) Epigenetic Reader Domain (1) ERK (7) Estrogen Receptor/ERR (2) FAP (1) FKBP (3) Fluorescent Dye (1) Fungal (2) FXR (1) G Protein-coupled Receptor Kinase (GRK) (1) GABA Receptor (3) GHSR (1) GLP Receptor (4) Glucosidase (1) GPR119 (1) GPR35 (1) GPR55 (1) GPR88 (1) GSK-3 (1) Guanylate Cyclase (3) HIF/HIF Prolyl-Hydroxylase (2) Histone Methyltransferase (2) HIV (7) HMG-CoA Reductase (HMGCR) (6) HPV (2) IAP (1) iGluR (3) Indoleamine 2,3-Dioxygenase (IDO) (6) Influenza Virus (1) Interleukin Related (2) IRAK (2) Isotope-Labeled Compounds (6) Itk (2) JAK (1) LPL Receptor (1) mAChR (6) MAGL (2) MDM-2/p53 (1) Melanocortin Receptor (1) Melatonin Receptor (7) mGluR (6) Microtubule/Tubulin (5) Monoamine Oxidase (1) Motilin Receptor (1) mTOR (4) MyD88 (1) nAChR (2) NADPH Oxidase (2) NOD-like Receptor (NLR) (2) OAT (2) Opioid Receptor (1) Orexin Receptor (OX Receptor) (1) P-glycoprotein (3) P2X Receptor (1) p38 MAPK (1) p62 (1) Parasite (7) PARP (1) PD-1/PD-L1 (1) PERK (1) Phosphatase (1) PI4K (1) Piezo Channel (1) PKG (1) Potassium Channel (6) PPAR (2) Prostaglandin Receptor (3) PROTACs (2) Protease Activated Receptor (PAR) (1) Proteasome (1) Pyroptosis (1) Raf (1) Reactive Oxygen Species (11) ROR (3) RXFP Receptor (8) SARS-CoV (2) Serotonin Transporter (1) Sirtuin (1) Sodium Channel (3) STAT (3) Thyroid Hormone Receptor (1) TNF Receptor (1) Toll-like Receptor (TLR) (8) TRP Channel (7) TSH Receptor (1) URAT1 (1) Urotensin Receptor (1) VEGFR (1) Virus Protease (4) Wnt (1) Xanthine Oxidase (1) β-catenin (1) γ-secretase (1)
By Research Areas:	Cancer (75) Cardiovascular Disease (35) Endocrinology (5) Infection (31) Inflammation/Immunology (47) Metabolic Disease (40) Neurological Disease (63)
Click Chemistry:	Alkynes (1)
Oligonucleotides:	Aptamers (2)

240

Inhibitors & Agonists

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6589

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Isotope-Labeled Compounds

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Click Chemistry

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19608

GSK1016790A 20+ Cited Publications	TRP Channel Calcium Channel	Cardiovascular Disease Metabolic Disease
GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca ²⁺ influx and elevate intracellular Ca ²⁺ in HEK cells .

HY-126010

Dooku1 5+ Cited Publications	Piezo Channel	Others
Dooku1 is a reversibly Yoda1 antagonist with IC₅₀ value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca ²⁺ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .

HY-P1066

Apelin-17(human, bovine)	Apelin Receptor (APJ) HIV	Infection
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC₅₀=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .

HY-N125722

Venturicidin A Aabomycin A1	ATP Synthase Antibiotic	Infection
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.

HY-135783

AT 1001	nAChR	Neurological Disease
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (K_i=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .

HY-157503

Photosensitizer-3	Others	Cancer
Photosensitizer-3 is a photosensitizer that exhibits powerful selective killing effects on transfected HEK cells and affibody-targeted A431 cancer cells when exposed to near-infrared light excitation .

HY-146299

Mt KARI-IN-2	Bacterial	Infection
Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a K_i value of 2.02 μM. Mt KARI-IN-2 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC₅₀ > 86 μg/mL) .

HY-146300

Mt KARI-IN-4	Bacterial	Infection
Mt KARI-IN-4 (compound 5c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a K_i value of 5.48 μM. Mt KARI-IN-4 has inhibitory activity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC₅₀ > 72 μg/mL) .

HY-146301

Mt KARI-IN-5	Bacterial	Infection
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI) inhibitor with a K_i value of 4.72 μM. Mt KARI-IN-5 has inhibitory activity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC₅₀ > 64 μg/mL)

HY-P1066A

Apelin-17(human, bovine) TFA	HIV Apelin Receptor (APJ)	Infection
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC₅₀=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .

HY-19774

GNE-0946	ROR	Inflammation/Immunology
GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC₅₀ value of 4 nM for HEK-293 cell.

HY-148939

MPX-004	iGluR	Neurological Disease
MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC₅₀ of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research .

HY-P1064

Apelin-36(human)	Apelin Receptor (APJ) HIV	Infection Cardiovascular Disease Metabolic Disease
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC₅₀ of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC₅₀=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .

HY-P1064A

Apelin-36(human) TFA	HIV Apelin Receptor (APJ)	Infection Cardiovascular Disease Metabolic Disease
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC₅₀ of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC5₅₀=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .

HY-169136

U 101958	Dopamine Receptor	Neurological Disease
U 101958 is full Dopamine D4 receptor agonist, with a pEC₅₀ of 8.7 in HEK293/D₄ cells .

HY-132934

Ac32Az19 1 Publications Verification	BCRP	Cancer
Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC₅₀ value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.

HY-120538

CPG-52364	Toll-like Receptor (TLR)	Inflammation/Immunology
CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC₅₀ value of 4.6 nM .

HY-153132

mGluR3 modulator-1	mGluR	Metabolic Disease
mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC₅₀ of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay .

HY-109039

Praliciguat IW-1973	Guanylate Cyclase	Cardiovascular Disease
Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC₅₀ of 197 nM .

HY-19775

GNE-6468	ROR	Inflammation/Immunology
GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC₅₀ value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC₅₀ of 30 nM for IL-17 PBMC .

HY-160811

hVEGF-IN-3	VEGFR	Cancer
hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC₅₀s of 61, 142, and 114 μM .

HY-108682

EMPA 5+ Cited Publications	Orexin Receptor (OX Receptor)	Neurological Disease
EMPA is a high-affinity, reversible and selective orexin OX₂ receptor antagonist. [ ³H]EMPA binds to human and rat OX₂-HEK293 membranes with K_D values of 1.1 and 1.4 nM respectively .

HY-101560

Linrodostat 4 Publications Verification BMS-986205; ONO-7701	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC₅₀ value of 1.1 nM in *IDO1*-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .

HY-12805

ML171 15+ Cited Publications 2-Acetylphenothiazine; 2-APT	NADPH Oxidase	Cardiovascular Disease
ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC₅₀ of 0.25 μM in HEK293-Nox1 confirmatory assay.

HY-101560A

Linrodostat mesylate BMS-986205 mesylate; ONO-7701 mesylate	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
Linrodostat (BMS-986205) mesylate is a selective irreversible inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), which effectively inhibits IDO1-HEK293 mesylate cells with an IC₅₀ value of 1.1 nM. Linrodostat mesylate demonstrates good pharmacological activity in advanced cancer .

HY-134988

EDP-305	FXR Phosphatase Cytochrome P450	Inflammation/Immunology
EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC₅₀ values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .

HY-123663

U-101958 maleate PNU-101958 maleate	Dopamine Receptor	Neurological Disease
U-101958 (PNU-101958) maleate is a highly selective ligand and antagonist for dopamine D4 receptor, with an IC₅₀ of 2.7 nM. U-101958 maleate behaves as an agonist in HEK-293 cells expressing the human recombinant D4.4 receptor. U-101958 maleate is an antipsychotic .

HY-120006A

(rel)-AR234960 1 Publications Verification	ERK	Cardiovascular Disease
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts .

HY-136555

GSK717 5+ Cited Publications	NOD-like Receptor (NLR)	Inflammation/Immunology
GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC₅₀ of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells .

HY-139848

WS-898	P-glycoprotein	Cancer
WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC₅₀ = 5.0, 3.67, and 3.68 nM, respectively).

HY-157935

17β-HSD10-IN-3	Endogenous Metabolite	Neurological Disease
17β-HSD10-IN-3 (compound 23) is a 17β-HSD10 inhibitor with the IC₅₀ of 5.59 μM. 17β-HSD10-IN-3 shows no cell cytotoxicity toward the HEK-293 cell line up to 20 μM .

HY-100360

MS049	Histone Methyltransferase	Cancer
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC₅₀s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .

HY-112683

V-9302 10+ Cited Publications	ASCT	Cancer
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC₅₀=9.6 µM) in HEK-293 cells .

HY-112683A

V-9302 hydrochloride 10+ Cited Publications	ASCT	Cancer
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC₅₀=9.6 µM) in HEK-293 cells .

HY-100360A

MS049 dihydrochloride	Histone Methyltransferase	Cancer
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC₅₀s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells .

HY-131891

JHU37152	mAChR	Neurological Disease
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC₅₀s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ ³H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .

HY-161074

PNT6555	FAP	Cancer
PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .

HY-117443

IWP-051	Guanylate Cyclase	Cardiovascular Disease
IWP-051 is an agonist for soluble guanylate cyclase with an EC₅₀ of 290 nM. IWP-051 stimulates the generation of cGMP, and exhibits the synergistic effect with NO. IWP-051 exhibits good pharmacokinetic characteristics in rats .

HY-131881

JHU37160 1 Publications Verification	mAChR	Neurological Disease
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC₅₀s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ ³H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .

HY-153460

TLR7/8/9 antagonist 2	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC₅₀ values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .

HY-136583

28-Epirapamycin	Drug Metabolite	Others
28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells .

HY-120170

BMS-466442	ASCT Adrenergic Receptor Dopamine Transporter	Neurological Disease
BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC₅₀ of 11 nM. BMS-466442 inhibits [ ³H] D-serine uptake into rat brain synaptosomes, with an IC₅₀ of 400 nM. BMS-466442 can be used for schizophrenia research .

HY-18332A

Amitifadine hydrochloride DOV-21947 hydrochloride; EB-1010 hydrochloride	Serotonin Transporter Dopamine Transporter	Neurological Disease
Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC₅₀s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.

HY-100013C

2-PCCA hydrochloride	GPR88	Neurological Disease
2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC₅₀ of 116 nM in HEK293 cells.

HY-118368

L-742001 hydrochloride	Influenza Virus	Infection Inflammation/Immunology
L-742001 hydrochloride is an influenza virus PA endonuclease inhibitor, with an EC₉₀ of 4.3 μM for vRNP activity in HEK293T cells .

HY-150766

KPC-2-IN-1	Bacterial	Infection
KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with K_i of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics .

HY-50883

BMS 299897	γ-secretase	Neurological Disease
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC₅₀ of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).

HY-108576

Linopirdine dihydrochloride DuP 996 dihydrochloride	TRP Channel	Neurological Disease
Linopirdine dihydrochloride is a agonist of capsaicin receptor TRPV1. Linopirdine increases the intracellular calcium concentration in HEK293 cells. Linopirdine dihydrochloride exerts an excitatory action on mammalian nociceptors .

HY-101698B

Alniditan dihydrochloride Alnitidan dihydrochloride	5-HT Receptor	Neurological Disease Inflammation/Immunology
Alniditan (Alnitidan) dihydrochloride is a potent 5-HT_1B and 5-HT_1D receptors agonist, with IC₅₀s of 1.7 nM and 1.3 nM for h5-HT_1B and h5-HT_1D receptors in HEK?293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects .

HY-114962

S-22153	Melatonin Receptor	Neurological Disease
S-22153 is a potent melatonin receptor antagonist with EC₅₀ values of 19 nM, 4.6 nM for hMT₁ and hMT₂ melatonin receptor, respectively. S-22153 has K_i values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT₁, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT₂. S-22153 is a specific ligand of MT₁ and MT₂ melatonin receptors subtypes .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N125722

Venturicidin A Aabomycin A1	Infection Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Source classification Antibacterial Disease Research Disease Research Fields	ATP Synthase Antibiotic
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.

HY-100801

L-threo-3-Hydroxyaspartic acid	Human Gut Microbiota Metabolites Microorganisms Source classification Endogenous metabolite	EAAT
L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor with K_is of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3, respectively in HEK293 cell lines .

HY-17038

Agomelatine 4 Publications Verification S-20098	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-17038A

Agomelatine hydrochloride 4 Publications Verification S-20098 hydrochloride	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-22024

5-Hydroxyflavone	Flavonoids Monophenols other families Classification of Application Fields Flavones Source classification Phenols Plants Disease Research Fields Cancer	Others
5-Hydroxyflavone, a flavonoid ligand, shows no cytotoxic activity against MCF-7, FaDU, MDA-MB-435S, U87, RPE-1, and HEK293 cells .

HY-17038B

Agomelatine (L(+)-Tartaric acid) 4 Publications Verification S-20098 L(+)-Tartaric acid	Structural Classification Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-10219

Rapamycin Maximum Cited Publications 850 Publications Verification Sirolimus; AY-22989	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Classification of Application Fields Antibiotics Anti-aging Source classification Disease Research Disease Research Fields Cancer	mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial
Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-B1167

Ajmaline Cardiorythmine; (+)-Ajmaline	Apocynaceae Cardiovascular Disease Alkaloids Piperidine Alkaloids Structural Classification Rauvolfia serpentina Classification of Application Fields Source classification Plants Disease Research Fields Indole Alkaloids	Sodium Channel
Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .

HY-101795

Larixyl acetate 2 Publications Verification	Infection Structural Classification Natural Products Neurological Disease Classification of Application Fields Pinaceae Source classification Larch resin Plants Disease Research Fields	TRP Channel HPV
Larixyl acetate is a potent and selective TRPC6 inhibitor with IC₅₀ values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction .

HY-17038R

Agomelatine (Standard)	Structural Classification Alkaloids Other Alkaloids Source classification Endogenous metabolite	Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-101795R

Larixyl acetate (Standard)	Structural Classification Natural Products Pinaceae Source classification Larch resin Plants	TRP Channel HPV
Larixyl acetate (Standard) is the analytical standard of Larixyl acetate. This product is intended for research and analytical applications. Larixyl acetate is a potent and selective TRPC6 inhibitor with IC₅₀ values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction .

HY-119695A

Simvastatin acid ammonium Tenivastatin ammonium	Cardiovascular Disease Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields	HMG-CoA Reductase (HMGCR) Reactive Oxygen Species
Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .

HY-10219R

Rapamycin (Standard)	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Antibiotics Source classification Disease Research Endogenous metabolite	mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial
Rapamycin (Standard) is the analytical standard of Rapamycin. This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-B1167R

Ajmaline (Standard)	Apocynaceae Alkaloids Piperidine Alkaloids Structural Classification Rauvolfia serpentina Source classification Plants Indole Alkaloids	Sodium Channel
Ajmaline (Standard) is the analytical standard of Ajmaline. This product is intended for research and analytical applications. Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC₅₀ of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia .

HY-N12007

OAT1/3-IN-1	Quinones Structural Classification Cassia obtusifolia L. Anthraquinones Source classification Caesalpiniaceae Plants	OAT
OAT1/3-IN-1 (compound 7) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-1 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-1 can be used to study mercury-induced kidney damage .

HY-N12008

OAT1/3-IN-2	Quinones Structural Classification Cassia obtusifolia L. Anthraquinones Source classification Caesalpiniaceae Plants	OAT
OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3. OAT1/3-IN-2 can reverse the toxicity of Cys-Hg on HEK-OAT1 cells (10 μM) and has a potential protective effect on the kidneys. OAT1/3-IN-2 can be used to study mercury-induced kidney damage .

HY-119695AR

Simvastatin acid ammonium (Standard)	Structural Classification Ketones, Aldehydes, Acids Source classification Endogenous metabolite	HMG-CoA Reductase (HMGCR) Reactive Oxygen Species
Simvastatin acid (ammonium) (Standard) is the analytical standard of Simvastatin acid (ammonium). This product is intended for research and analytical applications. Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .

HY-12033

2-Methoxyestradiol 20+ Cited Publications 2-ME2; NSC-659853	Structural Classification Monophenols Classification of Application Fields Source classification Disease markers Phenols Endocrine diseases Endogenous metabolite Disease Research Fields Steroids Cancer	Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa .

HY-N0930B

Galegine hydrochloride	Alkaloids Classification of Application Fields Leguminosae Source classification Metabolic Disease Plants Disease Research Fields Galega officinalis Linn.	AMPK Bacterial
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .

HY-122416

6,8-Diprenylnaringenin Lonchocarpol A; Senegalensin	Structural Classification Classification of Application Fields Erythrinasenegalensis DC. Source classification Metabolic Disease Plants Moraceae Flavonoids Leguminosae Humulus lupulus L. Flavonones Phenols Polyphenols Disease Research Fields Cancer	BCRP
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and ³H-Methotrexate transport (IC₅₀=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .

HY-P99499

Cetrelimab JNJ 63723283; JNJ 3283	Classification of Application Fields Disease Research Fields Cancer	PD-1/PD-L1 Interleukin Related TNF Receptor
Cetrelimab (JNJ 63723283; JNJ 3283) is a human IgG4κ mAb targeting PD-1. Cetrelimab binds PD-1 (K_d=1.72 nM, HEK293) to block the interaction of PD-1 with PD-L1 and PD-L2 (IC₅₀s=111.7 ng/mL and 138.6 ng/mL, respectively). Cetrelimab stimulates peripheral T cells, increases IFN-γ, IL-2, TNF-α level and inhibits tumor growth in vivo .

HY-N0110

Palmatine chloride 5+ Cited Publications	Structural Classification Alkaloids Phellodendron amurense Rupr. Classification of Application Fields Rutaceae Plants Isoquinoline Alkaloids Disease Research Fields Cancer	mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-N0110A

Palmatine	Alkaloids Structural Classification Phellodendron amurense Rupr. Classification of Application Fields Source classification Rutaceae Plants Isoquinoline Alkaloids Inflammation/Immunology Disease Research Fields	mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
Palmatine is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-N0110B

Palmatine hydroxide 5+ Cited Publications	Alkaloids Phellodendron amurense Rupr. Other Alkaloids Source classification Rutaceae Plants	mAChR Indoleamine 2,3-Dioxygenase (IDO) Virus Protease Aurora Kinase Apoptosis Bacterial Parasite
Palmatine hydroxide is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-N0110R

Palmatine chloride (Standard)	Structural Classification Alkaloids Phellodendron amurense Rupr. Classification of Application Fields Source classification Rutaceae Plants Isoquinoline Alkaloids Disease Research Fields Cancer	Apoptosis Virus Protease Indoleamine 2,3-Dioxygenase (IDO) Parasite Bacterial Aurora Kinase mAChR
Palmatine (chloride) (Standard) is the analytical standard of Palmatine (chloride). This product is intended for research and analytical applications. Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC₅₀s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC₅₀ of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .

HY-B1167A

Ajmaline hydrochloride Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride	Rauvolfia verticillata (Lour.) Baill. Apocynaceae Structural Classification Natural Products Source classification Plants	Others
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.

Cat. No.	Product Name	Chemical Structure

HY-17038S2

Agomelatin-d3
Agomelatin-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-10219S

Rapamycin-d3
Rapamycin-d₃ is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .

HY-10219S1

Rapamycin-13C,d3

Rapamycin- ¹³C,d₃ (Sirolimus- ¹³C,d₃; AY-22989- ¹³C,d₃) is the ¹³C and deuterium labeled Rapamycin (HY-10219) . Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-12033S2

2-Methoxyestradiol-d5

2-Methoxyestradiol-d₅ is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].

HY-17038S1

Agomelatine-d4
Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-119695AS1

Simvastatin acid-d9 ammonium

Simvastatin acid-d₉ ammonium is deuterated labeled Simvastatin acid ammonium (HY-119695A). Simvastatin acid (Tenivastatin) ammonium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid ammonium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid ammonium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .

HY-119695AS

Simvastatin acid-d6 ammonium

Simvastatin acid-d₆ (ammonium)mis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene[1].

HY-12033S

2-Methoxyestradiol-13C,d3

2-Methoxyestradiol- ¹³C,d₃ is the ¹³C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].

HY-12033S1

2-Methoxyestradiol-13C6

2-Methoxyestradiol- ¹³C₆ is the ¹³C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6].

HY-163816

Antiproliferative agent-53-d3

Antiproliferative agent-53-d3 (Compound C1) is an inhibitor for theta-mediated end joining (TMEJ) in HEK293 cell with an IC₅₀ of 0.14 µM. Antiproliferative agent-53-d3 is the inhibitor for CYP2C19 and CYP2C9 with IC₅₀ of 0.77 and 3.1 µM. Antiproliferative agent-53-d3 inhibits the proliferation of DNA repair-compromised cells, with IC₅₀ of 8.1 µM for BRCA2 ^-/- DLD-1. Antiproliferative agent-53-d3 exhibits good pharmacokinetic characteristics in CD-1 mice .

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