Search Result

Results for "

selective activator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	11β-HSD (1) 17β-HSD (3) 5-HT Receptor (28) Acetyl-CoA Carboxylase (1) Ack1 (1) Acyltransferase (1) ADC Linker (1) ADC Payload (1) Adenosine Kinase (1) Adenosine Receptor (9) Adenylate Cyclase (6) Adhesion G Protein-coupled Receptors (AGPCRs) (1) Adrenergic Receptor (32) Akt (53) Aldehyde Dehydrogenase (ALDH) (4) Aldose Reductase (2) Amino Acid Derivatives (1) Aminopeptidase (1) AMPK (45) Amylases (1) Amylin Receptor (2) Amyloid-β (15) Androgen Receptor (8) Angiotensin Receptor (6) Annexin A (1) Antibiotic (4) AP-1 (9) APC (2) Apelin Receptor (APJ) (1) Apoptosis (281) Aquaporin (1) Arf Family GTPase (1) Arp2/3 Complex (2) Arrestin (8) Aryl Hydrocarbon Receptor (4) ASCT (1) ASK1 (1) ATF6 (3) Atg4 (1) Atg8/LC3 (2) ATM/ATR (6) ATP Synthase (2) Aurora Kinase (2) Autophagy (86) Bacterial (46) Bcl-2 Family (34) BCL6 (1) Bcr-Abl (2) Beclin1 (1) Biochemical Assay Reagents (9) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (4) c-Kit (5) c-Met/HGFR (4) c-Myc (5) Cadherin (3) Calcineurin (1) Calcium Channel (24) Calmodulin (4) CaMK (6) Cannabinoid Receptor (4) Carbonic Anhydrase (3) Casein Kinase (3) Caspase (68) CaSR (3) Cathepsin (1) CCR (5) CD19 (1) CD276/B7-H3 (1) CD28 (2) CD38 (1) CD73 (1) Cdc42-binding kinase (1) CDK (23) Ceramidase (1) CFTR (1) CGRP Receptor (2) Checkpoint Kinase (Chk) (3) Chloride Channel (11) Cholinesterase (ChE) (3) ClpP (4) Collagen (3) Complement System (9) Constitutive Androstane Receptor (2) COX (17) CRFR (4) CRM1 (1) CTLA-4 (1) CXCR (6) Cyclic GMP-AMP Synthase (7) Cyclin G-associated Kinase (GAK) (1) Cytochrome P450 (12) DAGL (1) Dengue Virus (2) Deubiquitinase (4) DGK (6) Dipeptidyl Peptidase (12) Discoidin Domain Receptor (1) DNA Alkylator/Crosslinker (5) DNA Glycosylase (2) DNA Methyltransferase (7) DNA/RNA Synthesis (22) Dopamine Receptor (29) Drug Derivative (8) Drug Intermediate (2) Drug Isomer (2) Drug Metabolite (16) Dynamin (2) E1/E2/E3 Enzyme (7) Early 2 Factor (E2F) (1) EBI2/GPR183 (1) EBV (2) EGFR (17) Endogenous Metabolite (48) Endonuclease (1) Endoplasmic Reticulum Oxidoreductase 1 (ERO1) (1) Endothelin Receptor (3) Enolase (1) Environmental Pollutants (8) Ephrin Receptor (4) Epigenetic Reader Domain (9) Epoxide Hydrolase (6) ERK (71) Erythropoietin Receptor (EpoR) (1) Estrogen Receptor/ERR (29) Eukaryotic Initiation Factor (eIF) (10) Factor Xa (4) Factor XI (2) FAK (3) FAP (9) Farnesyl Transferase (2) Fatty Acid Synthase (FASN) (2) Fc Receptor (FcR) (2) Ferroptosis (19) FGFR (6) FLAP (9) Flavivirus (2) FLT3 (4) Fluorescent Dye (14) Formyl Peptide Receptor (FPR) (9) FOXO (1) Free Fatty Acid Receptor (5) Fungal (1) Furin (2) FXR (10) G protein-coupled Bile Acid Receptor 1 (2) G Protein-coupled Receptor Kinase (GRK) (2) G-quadruplex (2) G2A (GPR132) (1) GABA Receptor (7) GCGR (1) GLP Receptor (24) Glucocorticoid Receptor (8) Glucokinase (4) GLUT (5) Glutathione Peroxidase (3) Glutathione S-transferase (2) Glycine Receptor (GlyR) (1) Glycosidase (1) GPR109A (1) GPR119 (1) GPR35 (1) GPR39 (1) GPR55 (1) GPR65 (1) GPR84 (3) GPR88 (2) GSK-3 (11) Guanylate Cyclase (6) HBV (1) HCN Channel (4) HDAC (22) Hedgehog (2) Herbicide (1) HIF/HIF Prolyl-Hydroxylase (1) Histamine Receptor (14) Histone Acetyltransferase (4) Histone Demethylase (2) Histone Methyltransferase (9) HIV (10) HIV Integrase (1) HIV Protease (4) HSP (15) IAP (6) IFNAR (17) iGluR (13) IKK (7) IKZF Family (1) Indoleamine 2,3-Dioxygenase (IDO) (2) Influenza Virus (1) Insecticide (3) Insulin Receptor (10) Integrin (6) Interleukin Related (79) IRAK (4) IRE1 (4) Isotope-Labeled Compounds (58) Itk (1) JAK (18) JNK (21) Kallikrein (2) Keap1-Nrf2 (11) Kinesin (2) Large Tumor Suppressor (LATS) (2) LDLR (1) Leukotriene Receptor (3) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (2) Lipase (2) Liposome (3) Lipoxygenase (1) LPL Receptor (12) LXR (5) mAChR (14) MAGL (2) MAP3K (3) MAP4K (4) MAPKAPK2 (MK2) (3) MARK (2) Mas-related G-protein-coupled Receptor (MRGPR) (3) MCHR1 (GPR24) (1) MDM-2/p53 (17) MEK (12) Melanocortin Receptor (3) Melatonin Receptor (5) mGluR (16) MHC (2) Microtubule/Tubulin (6) Mitochondrial Metabolism (19) Mitophagy (11) Mitosis (2) Mixed Lineage Kinase (5) MMP (23) Molecular Glues (2) Monoamine Oxidase (5) mTOR (22) MyD88 (2) Myosin (8) Na+/Ca2+ Exchanger (3) Na+/K+ ATPase (3) nAChR (19) NADPH Oxidase (3) Necroptosis (3) NEDD8-activating Enzyme (8) NEKs (1) Neprilysin (1) Neurokinin Receptor (5) Neuromedin U Receptor (NMUR) (1) Neuropeptide Y Receptor (4) NF-κB (80) NKCC (1) NO Synthase (13) NOD-like Receptor (NLR) (34) NTPDase (1) Nuclear Factor of activated T Cells (NFAT) (6) Nuclear Hormone Receptor 4A/NR4A (4) Nucleoside Antimetabolite/Analog (1) Opioid Receptor (25) Orexin Receptor (OX Receptor) (2) Organoid (16) Orphan GPCR (2) Orphan Nuclear Receptor (1) Orthopoxvirus (1) Oxidative Phosphorylation (2) Oxytocin Receptor (1) P-glycoprotein (10) P-selectin (1) P2X Receptor (5) P2Y Receptor (14) p38 MAPK (78) p62 (5) PAI-1 (8) PAK (3) PANK (1) PANoptosis (2) Parasite (29) PARP (16) PD-1/PD-L1 (5) PDGFR (5) PDK-1 (4) PERK (9) PGC-1α (1) PGE synthase (3) Phosphatase (20) Phosphodiesterase (PDE) (25) Phospholipase (10) Photosensitizer (1) PI3K (23) PI5P4K (1) Piezo Channel (3) PIKfyve (1) PIN1 (1) PKA (33) PKC (17) PKG (3) Platelet-activating Factor Receptor (PAFR) (11) Poly(ADP-ribose) Glycohydrolase (PARG) (1) Porcupine (1) Potassium Channel (68) PPAR (67) Pregnane X Receptor (PXR) (4) Progesterone Receptor (3) Prolyl Endopeptidase (PREP) (3) Prostaglandin Receptor (16) PROTACs (27) Protease Activated Receptor (PAR) (36) Proteasome (5) PTEN (1) PTHR (3) Pyk2 (1) Pyroptosis (6) Pyruvate Kinase (7) Quinone Reductase (4) Raf (4) RANKL/RANK (1) RAR/RXR (12) Ras (23) Reactive Oxygen Species (ROS) (41) Reference Standards (141) RET (3) Reverse Transcriptase (2) Ribosomal S6 Kinase (RSK) (3) RIP kinase (10) ROCK (1) ROR (4) ROS Kinase (2) RSV (1) RXFP Receptor (3) Salt-inducible Kinase (SIK) (2) SARS-CoV (5) Ser/Thr Kinase (1) Ser/Thr Protease (11) Serpin (1) SGK (2) SGLT (3) SHP1 (1) SHP2 (2) Sigma Receptor (9) Sirtuin (17) Smo (3) Sodium Channel (21) SOS1 (4) Src (4) STAT (26) Steroid Sulfatase (1) STING (17) Succinate Dehydrogenase (1) Survivin (2) Syk (4) TAM Receptor (1) Tau Protein (2) TGF-beta/Smad (6) TGF-β Receptor (12) Thrombin (8) Thyroid Hormone Receptor (2) Tie (3) TNF Receptor (36) Toll-like Receptor (TLR) (22) TOPK (2) Topoisomerase (1) Trace Amine-associated Receptor (TAAR) (1) Transferrin Receptor (1) Transmembrane Glycoprotein (5) TREM receptor (1) Trk Receptor (11) TRP Channel (42) TrxR (1) TSH Receptor (2) UGT (1) Vasopressin Receptor (1) VD/VDR (5) VDAC (1) VEGFR (13) Wnt (17) YAP (4) α-synuclein (8) β-catenin (12) β-glucuronidase (1)
By Research Areas:	Cancer (645) Cardiovascular Disease (186) Endocrinology (61) Infection (81) Inflammation/Immunology (449) Metabolic Disease (245) Neurological Disease (445)
Click Chemistry:	Tetrazine (1)
Oligonucleotides:	Pegylated Lipids (3) Nucleotide Analogs (1) CpG ODNs (1) Phospholipids (1) Adenine Nucleotide (1)

1567

Inhibitors & Agonists

Screening Libraries

Fluorescent Dye

Biochemical Assay Reagents

100

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Oligonucleotides

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18723

Yoda 1 95+ Cited Publications	Piezo Channel Akt ERK Potassium Channel	Cardiovascular Disease
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca ²⁺ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .

HY-111789

Subasumstat 30+ Cited Publications TAK-981	E1/E2/E3 Enzyme	Inflammation/Immunology Cancer
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .

HY-16985

Darolutamide 5+ Cited Publications ODM-201; BAY-1841788	Androgen Receptor	Cancer
Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a K_i of 11 nM for rat wild-type AR (wtAR) and IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-P10798

Eloralintide LY-3841136	Amylin Receptor	Metabolic Disease
Eloralintide is an amylin receptor (AMYR) activator and long-acting peptide. Eloralintide selectively activates amylin receptors. Eloralintide is modified with a C20 fatty diacid moiety that binds to amylin receptors while retaining selectivity from calcitonin receptors. Eloralintide induces decreased appetite.Eloralintide reduces body weight. Eloralintide can be used for the research of obesity .

HY-100407

JNJ16259685 3 Publications Verification	mGluR	Neurological Disease
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC₅₀ of 19 nM.

HY-P0256

Apamin 5+ Cited Publications Apamine	Potassium Channel	Neurological Disease Inflammation/Immunology
Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca ²⁺-activated K ⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity .

HY-101346

ZD7288 5+ Cited Publications ICI D7288	HCN Channel	Neurological Disease
ZD7288 (ICI D7288) is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker .

HY-B1816

Zaprinast 3 Publications Verification M&B 22948	Phosphodiesterase (PDE) GPR35	Cardiovascular Disease Neurological Disease Endocrinology
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .

HY-103683

PF-06409577 1 Publications Verification	AMPK	Metabolic Disease
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.

HY-117793

I-191 1 Publications Verification	Protease Activated Receptor (PAR)	Cancer
I-191 is a potent, selective *protease-activated* receptor 2 (PAR2)** antagonist .

HY-15577

GSK3787 15+ Cited Publications	PPAR	Cancer
GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC₅₀ of 6.6.

HY-P1026

NFAT Inhibitor-1 10+ Cited Publications VIVIT peptide	Nuclear Factor of activated T Cells (NFAT)	Inflammation/Immunology
NFAT Inhibitor (VIVIT peptide) is an inhibitor of *nuclear factor of activated* Tcells (NFAT)** that selectively inhibits calcineurin-mediated dephosphorylation of NFAT .

HY-14233

Omecamtiv mecarbil 4 Publications Verification CK-1827452	Myosin	Cardiovascular Disease
Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.

HY-13519

TRAM-34 25+ Cited Publications	Potassium Channel	Neurological Disease
TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K ⁺ channel (IKCa1) (K_d=20 nM).

HY-134570

ZINC40099027 3 Publications Verification	FAK	Metabolic Disease Inflammation/Immunology
ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research .

HY-15416

NS309	Potassium Channel	Cardiovascular Disease Neurological Disease
NS309 is a potent and selective activator of the *Ca ²⁺-activated* SK/IK potassium channels**, but displays no activity at BK channels .

HY-109121

Reldesemtiv 2 Publications Verification CK-2127107	Calcium Channel	Cardiovascular Disease
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC₅₀ of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model .

HY-15300

Skepinone-L 2 Publications Verification CBS3830	p38 MAPK Autophagy	Inflammation/Immunology
Skepinone-L (CBS3830), a chemical probe, is a selective p38 mitogen-activated protein kinase inhibitor.

HY-59047

Tolimidone 4 Publications Verification MLR-1023	Src	Metabolic Disease
Tolimidone is a potent and selective allosteric activator of Lyn kinase with an EC₅₀ of 63 nM.

HY-103368

Eact 1 Publications Verification	Chloride Channel	Neurological Disease
Eact is a selective and potent activator of TMEM16A, directly activates the TRPV1 channels in sensory nociceptors and produces itch, acute nociception and thermal hypersensitivity .

HY-104005

ML335 2 Publications Verification	Potassium Channel	Neurological Disease
ML335 is a selective activator of both TREK-1 and TREK-2.

HY-117755

PF-739	AMPK	Metabolic Disease
PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes .

HY-132247

ErSO	Estrogen Receptor/ERR	Cancer
ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer .

HY-137455

Terevalefim ANG-3777	c-Met/HGFR	Inflammation/Immunology
Terevalefim (ANG-3777), an hepatocyte growth factor (HGF) mimetic, selectively activates the c-Met receptor .

HY-139553

Zunsemetinib ATI-450; CDD-450	MAPKAPK2 (MK2)	Inflammation/Immunology
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .

HY-138936

SSK1 2 Publications Verification	p38 MAPK Apoptosis	Inflammation/Immunology
SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted proagent attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis .

HY-111098

GSK1702934A 2 Publications Verification	TRP Channel	Cardiovascular Disease
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3 .

HY-107988

MK-3903 3 Publications Verification	AMPK	Metabolic Disease
MK-3903 is a potent and selective *AMP-activated* protein kinase (AMPK*) activator* with an EC₅₀ of 8 nM.

HY-15341

BAM7 2 Publications Verification	Bcl-2 Family	Cancer
BAM7 is a direct and selective activator of proapoptotic BAX with an IC₅₀ of 3.3 μM.

HY-148802

Taplucainium chloride	Sodium Channel	Inflammation/Immunology
Taplucainium chloride is a sodium channel blocker. Taplucainium chloride selectively inhibits nociceptors in an activated or inflammatory state. Taplucainium chloride may be used in research on chronic cough .

HY-P2518

Protease-Activated Receptor-1, PAR-1 Agonist	Protease Activated Receptor (PAR)	Inflammation/Immunology
Protease-Activated Receptor-1, PAR-1 Agonist is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor .

HY-136172

ESI-08 1 Publications Verification	Ras	Cardiovascular Disease Metabolic Disease Cancer
ESI-08 is a potent and selective EPAC antagonist, which can completely inhibit both EPAC1 and EPAC2 (IC₅₀ of 8.4 μM) activity. ESI-08 selectively blocks cAMP-induced EPAC activation, but does not inhibit cAMP-mediated PKA activation .

HY-161928

GPX4 activator 1	Glutathione Peroxidase Ferroptosis	Cancer
GPX4 activator 1 (Compound A9) is a allosteric activator of GPX4 (K_d = 5.86 μM, EC₅₀ = 19.19 μM). GPX4 activator 1 can selectively act on ferroptosis and prevent the accumulation of intracellular lipid peroxides caused by ferroptosis inducers .

HY-143510

RMC-4627	mTOR	Cancer
RMC-4627 is a selective mTORC1 inhibitor that activates 4EBP1 and inhibits tumor growth.

HY-15530

CID-2858522	NF-κB	Inflammation/Immunology Cancer
CID-2858522 is a highly potent and selective antigen receptor-mediated NF-κB activation inhibitor with an IC₅₀ of 70 nM.

HY-158162

SIRT3 activator 1 1 Publications Verification	Sirtuin	Cardiovascular Disease
SIRT3 activator 1 (Compound 5v) is a SIRT3 activator. SIRT3 activator 1 selectively elevates SIRT3 expression, leading to the upregulation of SOD2 and OPA1 expression, effectively preventing mitochondrial dysfunction, mitigating oxidative stress, and preserving cardiomyocyte viability. SIRT3 activator 1 can be used for research of cardiovascular diseases .

HY-101918

DS-1040 Tosylate	Thrombin	Cardiovascular Disease
DS-1040 Tosylate is an orally active, selective inhibitor of activated *thrombin-activatable* fibrinolysis inhibitor (TAFIa) with IC₅₀**s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases .

HY-102066

Utatrectinib AZD-7451	Trk Receptor	Cancer
Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .

HY-152264

CFTR activator 1	CFTR	Inflammation/Immunology
CFTR activator 1 is a potent and selective CFTR activator, with an EC₅₀ of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease .

HY-19635A

G-5555 hydrochloride 5+ Cited Publications	PAK	Cancer
G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a K_i of 3.7 nM.

HY-131334

AMPK activator 4	AMPK	Metabolic Disease
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect .

HY-157485

Ebio1	Potassium Channel	Others
Ebio1 is a selective voltage-gated potassium channel KCNQ2 activator. Ebio1 activates KCNQ2 by generating an extended channel gate with greater conductance at a saturation voltage (+50 mV) .

HY-P0190A

Iberiotoxin TFA 2 Publications Verification	Potassium Channel	Others
Iberiotoxin (TFA) is a selective high conductance high conductance *Ca ²⁺-activated* K ⁺ channel inhibitor with a K_d** of ~1 nM. Iberiotoxin (TFA) does not block other types of voltage-dependent ion channels .

HY-112125A

KRN2 bromide 4 Publications Verification	Nuclear Factor of activated T Cells (NFAT)	Inflammation/Immunology
KRN2 (bromide) is a selective inhibitor of *nuclear factor of activated* T cells (NFAT5), with an IC₅₀** of 0.1 μM.

HY-128205

BTD	TRP Channel	Neurological Disease
BTD is a selective transient receptor potential canonical 5 (TRPC5) activator. BTD can be used for the research of neurological disease .

HY-14351

AC-264613	Protease Activated Receptor (PAR)	Inflammation/Immunology
AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC₅₀ of 7.5 .

HY-162965

Immunoproteasome activator 1	Proteasome	Cancer
Immunoproteasome activator 1 (compound A) is a selective immunoproteasome activator that increases the presentation of individual MHC-I–bound peptides by over 100-fold. Immunoproteasome activator 1 binds to the proteasome structural subunit PSMA1 and promotes the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes .

HY-117393

Bisindolylmaleimide III 1 Publications Verification	PKC	Cancer
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .

HY-16985S

Darolutamide-d4 ODM-201-d₄; BAY-1841788-d₄	Isotope-Labeled Compounds Androgen Receptor	Cancer
Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-112968

Human protein C	APC	Cardiovascular Disease
Human Protein C is activated by α-thrombin or α-thrombin/thrombomodulin complex to a serine protease, namely activated protein C (APC). Human Protein C can selectively inactivate factors Va and VIIIa and is a potent anticoagulant .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13434

Ionomycin 115+ Cited Publications SQ23377	Infection Microorganisms Classification of Application Fields Antibiotics Disease Research Anticancer Disease Research Fields Other Antibiotics Source Classification	Calcium Channel PKC Bacterial Apoptosis Antibiotic
Ionomycin (SQ23377) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin (SQ23377) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin also induces the activation of protein kinase C (PKC) .

HY-B0075

Melatonin Maximum Cited Publications 137 Publications Verification N-Acetyl-5-methoxytryptamine	Structural Classification Natural Products Other disease Neurological Disease Classification of Application Fields Anti-aging Disease markers Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification Cancer	Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Apoptosis PANoptosis
Melatonin is a hormone made by the pineal gland that can activate melatonin receptor and inhibit PANoptosis. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .

HY-13434A

Ionomycin calcium 115+ Cited Publications SQ23377 calcium	Infection Microorganisms Classification of Application Fields Antibiotics Disease Research Anticancer Disease Research Fields Other Antibiotics Source Classification	Calcium Channel PKC Bacterial Apoptosis Antibiotic
Ionomycin calcium (SQ23377 calcium) is a potent, selective calcium ionophore and an antibiotic produced by Streptomyces conglobatus. Ionomycin calcium (SQ23377 calcium) is highly specific for divalent cations (Ca>Mg>Sr=Ba). Ionomycin (SQ23377) promotes apoptosis. Ionomycin calcium (SQ23377 calcium) also induces the activation of protein kinase C (PKC) .

HY-100354

C16-Ceramide (d18:1/16:0) 5+ Cited Publications C16-Ceramide	Structural Classification Alkaloids Classification of Application Fields Other Alkaloids Endogenous metabolite Disease Research Fields Source Classification Cancer	MDM-2/p53 Apoptosis Endogenous Metabolite
C16-Ceramide (d18:1/16:0) is a natural small molecule activating p53 through the direct and selective binding .

HY-113134

25-Hydroxycholesterol 25+ Cited Publications 25-OHC	Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Steroids Source Classification	Endogenous Metabolite
25-Hydroxycholesterol (25-OHC) is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC₅₀≈65 nM) and selective suppressor of IgA production by B cells.

HY-B1247

Protoporphyrin IX 20+ Cited Publications PPIX	Structural Classification Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .

HY-N0305

5-Aminolevulinic acid hydrochloride 15+ Cited Publications 5-ALA hydrochloride; δ-Aminolevulinic acid hydrochloride; 5-Amino-4-oxopentanoic acid hydrochloride	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Cancer	Reactive Oxygen Species (ROS)
5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) hydrochloride is an orally active heme precursor. 5-Aminolevulinic acid hydrochloride promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid hydrochloride enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid hydrochloride selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid hydrochloride can be applied to the research of septic shock, melanoma, and cancer radiotherapy .

HY-N0377

Liquiritigenin 10+ Cited Publications 4',7-Dihydroxyflavanone	Neurological Disease Classification of Application Fields Plants Flavonoids Microorganisms Leguminosae Flavonones Phenols Polyphenols Inflammation/Immunology Disease Research Fields Glycyrrhiza uralensis Fisch. Source Classification	Estrogen Receptor/ERR
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC₅₀ of 36.5 nM for activation of the ERE tk-Luc.

HY-19356

Rocaglamide 25+ Cited Publications Roc-A	Alkaloids Classification of Application Fields Other Alkaloids Plants Meliaceae Disease Research Fields Aglaia elliptifolia Source Classification Cancer	NF-κB HSP Eukaryotic Initiation Factor (eIF)
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC₅₀ of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia .

HY-N0143

Phlorizin 10+ Cited Publications Floridzin	Structural Classification Flavonoids Classification of Application Fields Malus pumila Mill. Rosaceae Phenols Polyphenols Metabolic Disease Plants Dihydrochalcones Disease Research Fields Source Classification	Caspase JAK GLUT STAT Apoptosis Bacterial SGLT mTOR Akt NF-κB PI3K DNA/RNA Synthesis
Phlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities .

HY-113962

7α,25-Dihydroxycholesterol 3 Publications Verification 7α,25-OHC	Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Steroids Source Classification	EBI2/GPR183 Endogenous Metabolite
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC₅₀=140 pM; K_d=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-N7075

Inulin 4 Publications Verification	Structural Classification Human Gut Microbiota Metabolites Polysaccharides Classification of Application Fields Metabolic Disease Plants Compositae Endogenous metabolite Disease Research Fields Saccharides Sophora tomentosa L. Source Classification	Endogenous Metabolite
Inulin is an orally active prebiotic targeting the intestinal microbiota, selectively promoting the proliferation and activity of beneficial bacteria such as bifidobacteria and lactic acid bacteria, and playing a role in regulating the intestinal microecology. The functions of Inulin include: Fermentation by probiotics in the colon to produce short-chain fatty acids (such as butyrate and propionate), lowering the intestinal pH and inhibiting the overgrowth of harmful bacteria; Enhancing the intestinal barrier function and reducing endotoxin translocation; Directly scavenging free radicals (such as superoxide free radicals, hydroxyl free radicals) and activating antioxidant enzymes (SOD, CAT) to reduce oxidative stress. Inulin can also be used in the study of intestinal diseases (constipation, IBD), metabolic syndrome (diabetes, obesity) and liver damage by regulating glucose and lipid metabolism (such as reducing triglycerides, improving insulin sensitivity) and immune response (enhancing NK cell activity, inhibiting inflammatory factors)[1][2][3][4].

HY-B1614

Clenbuterol hydrochloride 5+ Cited Publications NAB-365 hydrochloride	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Endocrinology Source Classification	Adrenergic Receptor
Clenbuterol (NAB-365) hydrochloride, a selective β2-adrenergic agonist, enhances skeletal muscle strength and hypertrophy. Clenbuterol hydrochloride induces growth factor mRNA, activates astrocytes, and protects rat brain tissue against ischemic damage .

HY-W000450

5-Aminolevulinic acid 15+ Cited Publications 5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid	Cardiovascular Disease Structural Classification Classification of Application Fields Amino acids Endogenous metabolite Human Gut Microbiota Metabolites Immune System Disorder Microorganisms Ketones, Aldehydes, Acids Disease markers Disease Research Fields Source Classification Cancer	Reactive Oxygen Species (ROS)
5-Aminolevulinic acid (5-ALA; δ-Aminolevulinic acid; 5-Amino-4-oxopentanoic acid) is an orally active heme precursor. 5-Aminolevulinic acid promotes aerobic energy metabolism and increases ATP levels by enhancing the activity of cytochrome c oxidase. 5-Aminolevulinic acid enhances LPS-induced proinflammatory cytokine production and gene activation, and restores the phagocytic activity and ROS generation capacity of neutrophils. 5-Aminolevulinic acid selectively accumulates protoporphyrin IX in tumor cells; as a photosensitizer and radiosensitizer, it induces ROS burst upon light or X-ray irradiation to inhibit tumor growth. 5-Aminolevulinic acid can be applied to the research of septic shock, melanoma, and cancer radiotherapy .

HY-126585

SAICAR 4 Publications Verification	Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Disease Research Fields Source Classification Cancer	Endogenous Metabolite
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC₅₀ of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .

HY-110252

Salvinorin B	Terpenoids Labiatae Encelia stenophylla Greene Diterpenoids Plants Source Classification	Opioid Receptor
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC₅₀ of 248 nM and K_i of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .

HY-N2037

Higenamine 5+ Cited Publications Norcoclaurine; Demethyl-Coclaurine	Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Disease Research Fields Endocrinology Source Classification	MAP3K MDM-2/p53 Adrenergic Receptor ROS Kinase Apoptosis
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .

HY-P0190

Iberiotoxin 2 Publications Verification	Cardiovascular Disease Natural Products Animals Classification of Application Fields Disease Research Fields Source Classification	Potassium Channel
Iberiotoxin is a toxin isolated from Buthus tamulus scorpion venom. Iberiotoxin is a selective high conductance high conductance *Ca ²⁺-activated* K ⁺ channel inhibitor with a K_d** of ~1 nM. Iberiotoxin does not block other types of voltage-dependent ion channels .

HY-133168

Englerin A 1 Publications Verification	Structural Classification other families Classification of Application Fields Terpenoids Sesquiterpenes Plants Disease Research Fields Source Classification Cancer	TRP Channel
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC₅₀s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca ²⁺ influx and Ca ²⁺ cell overload .

HY-116330A

Hyperforin dicyclohexylammonium salt 3 Publications Verification Hyperforin DCHA	Natural Products Guttiferae Hyperlcurn perforatum L. Plants Source Classification	TRP Channel Calcium Channel
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca ²⁺ levels by activating Ca ²⁺-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .

HY-N0632

Esculentoside A 2 Publications Verification	Triterpenes Classification of Application Fields Terpenoids Phytolacca acinosa Roxb. Plants Inflammation/Immunology Disease Research Fields Phytolaccaceae Source Classification	COX NF-κB
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta . Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitory activity towards cyclooxygenase-2 (COX-2) . Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .

HY-18252

Avanafil 1 Publications Verification TA1790	Cardiovascular Disease Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology Source Classification	Phosphodiesterase (PDE) NO Synthase Endogenous Metabolite
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .

HY-12316

20(S)-Hydroxycholesterol 3 Publications Verification 20α-Hydroxycholesterol	Classification of Application Fields Endogenous metabolite Disease Research Fields Steroids Source Classification Cancer	Smo Endogenous Metabolite
20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) is an allosteric activator that selectively targets the Smoothened (Smo) of the Hedgehog pathway with an EC₅₀ of ~30 μM (Hedgehog). 20(S)-Hydroxycholesterol binds to the extracellular cysteine-rich domain (CRD) of Smo in a stereoselective manner, activating downstream Gli transcription factors (without inducing transcription of receptor genes in the Wnt pathway). 20(S)-Hydroxycholesterol enhances osteogenic differentiation of bone marrow stromal cells and synergistically activates the Raf/MEK/ERK pathway with Simvastatin (HY-17502) to promote bone regeneration. 20(S)-Hydroxycholesterol can be used to study the mechanisms of developmental biology, oncology, bone, and angiogenesis .

HY-N1163

Tetrahydroalstonine (-)-Tetrahydroalstonine	Apocynaceae Alkaloids Plants Indole Alkaloids Catharanthus roseus (L.) G. Don Source Classification	Adrenergic Receptor Atg8/LC3 Akt mTOR
Tetrahydroalstonine ((-)-Tetrahydroalstonine) is an indole alkaloid and a selective α₂-adrenergic receptor antagonist. Tetrahydroalstonine exhibits certain neuroprotective effects. Tetrahydroalstonine can regulate autophagy-lysosomal function by activating the Akt/mTOR pathway, significantly reducing OGD/R-induced primary cortical neuronal injury .

HY-I1070

D-Isoleucine (R)-Isoleucine	Microorganisms Source Classification	ASCT
D-Isoleucine is a selective competitive activator of the Asc-1 antiporter (Ki=0.98 mM). D-Isoleucine promotes the release of D-serine and glycine by binding to the Asc-1 protein on the neuronal cell membrane, and enhances NMDA receptor-dependent synaptic plasticity. D-Isoleucine can be used in the study of neurodegenerative diseases (such as Alzheimer's disease and schizophrenia). D-Isoleucine also acts as a non-classical D-amino acid, interferes with bacterial peptidoglycan synthesis, and inhibits the formation of Staphylococcus aureus biofilm, and has potential antibacterial application value[1][2].

HY-N2909

Aurantiamide	Alkaloids Classification of Application Fields Other Alkaloids Umbelliferae Plants Inflammation/Immunology Disease Research Fields Carphephorus corymbosus (Nutt.) Torr. & A.Gray Source Classification	NF-κB RIP kinase Mixed Lineage Kinase
Aurantiamide is a non-covalent, orally active, blood-brain-permeable GRPR selective antagonist with anti-inflammatory and neuroprotective effects. Aurantiamide reduces inflammation and oxidative stress in renal tissue by inhibiting GRPR-mediated renal necrosis pathways (such as RIPK3/MLKL signaling) and NF-κB inflammatory pathways, exerting anti-acute kidney injury and endothelial function activities. Aurantiamide also inhibits the M1 polarization of microglia and inhibits NLRP3 activation, thereby improving AD mouse models. Aurantiamide has in vivo inhibitory efficacy in acute kidney injury models such as ischemia/reperfusion, sepsis, and hypertension models .

HY-N0059

D-Arabinose	Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Saccharides Source Classification	Parasite Bacterial AMPK PPAR
D-Arabinose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-Arabinose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-Arabinose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-Arabinose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-Arabinose is the ring-opened form of the aldopentose D-?Arabinose (HY-N7082) .

HY-N6985

Baccatin III 2 Publications Verification	Structural Classification Classification of Application Fields Terpenoids Taxaceae Diterpenoids Plants Disease Research Fields Taxus chinensis (Pilger) Rehd. Source Classification Cancer	Others
Baccatin III is an orally available, selective inhibitor of the TGF-β1 signaling pathway and myeloid-derived suppressor cell (MDSC) activation. Baccatin III targets the AKT/STAT6 and Smad2/3 pathways, blocking TGF-β1-induced fibroblast differentiation and MDSC-mediated immunosuppression. Baccatin III exerts anti-inflammatory and anti-fibrotic effects by inhibiting macrophage activation and extracellular matrix deposition, and shows potential in the treatment of pulmonary fibrosis and cancer in terms of regulating the tumor immune microenvironment .

HY-N2424

Flavone 2-Phenyl-4-chromone	Flavonoids Classification of Application Fields Flavones Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	CDK Apoptosis Caspase
Flavone is an anti-tumor compound that targets cell cycle regulatory proteins (such as cyclin B1) and apoptosis-related factors (such as p21_waf1, PIG3). Flavone selectively induces mitochondrial-mediated apoptosis pathways in tumor cells, inhibits cyclin B1 protein expression, upregulates p21_waf1, and activates p63/p73 proteins. Flavone has immunomodulatory functions that enhance natural killer cell (NK cell) activity and lymphocyte proliferation. Flavone is used in cancer research, especially for its inhibitory potential in solid tumor models such as esophageal cancer and liver cancer .

HY-N8264

Moringin 1 Publications Verification	Structural Classification Natural Products Neurological Disease Classification of Application Fields Moringa oleifera Lam. Moringaceae Plants Inflammation/Immunology Disease Research Fields Source Classification	TRP Channel
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC₅₀ of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. Moringin has hypoglycemic, antimicrobial, anti-inflammatory, anticancer and neuroprotection activities .

HY-134356

AICA-riboside, 5′-phosphate AICAR-5'-MP	Human Gut Microbiota Metabolites Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .

HY-N1431

Tabersonine 3 Publications Verification	Apocynaceae Alkaloids Structural Classification Plants Indole Alkaloids Catharanthus roseus (L.) G. Don Source Classification	NOD-like Receptor (NLR) Apoptosis Cytochrome P450 NF-κB PI3K Akt CDK Caspase Interleukin Related p38 MAPK
Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer .

HY-N0467

Rebaudioside C Dulcoside B	Trifolium hybridum L. Classification of Application Fields Terpenoids Other Diseases Diterpenoids Plants Compositae Endogenous metabolite Disease Research Fields Sweeteners Source Classification Food Research	Endogenous Metabolite
Rebaudioside C (Dulcoside B) is an orally effective natural sweetener that cannot pass the blood-brain barrier and selectively binds to human sweet taste receptors (TAS1R2/TAS1R3). The sweetness of Rebaudioside C is about 20-30 times that of sucrose, and its sweetness activity depends on the C-16/C-17 double bond structure and specific aglycones. The glycoside structure in the Rebaudioside C molecule can bind to the sweet taste receptor, activate the taste signal transduction pathway, and produce sweetness perception .

HY-N3945

Glaucine O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396	Infection Alkaloids other families Classification of Application Fields Plants Isoquinoline Alkaloids Glaucium flavum Inflammation/Immunology Disease Research Fields Papaveraceae Source Classification	Phosphodiesterase (PDE) Calcium Channel MMP NF-κB
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a K_i of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .

HY-W010451

1,2,4-Trihydroxybenzene Hydroxyhydroquinone	Cardiovascular Disease Microorganisms Classification of Application Fields Phenols Polyphenols Disease Research Fields Source Classification	PERK Eukaryotic Initiation Factor (eIF) Potassium Channel Apoptosis
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone) is an ER stress inducer that targets proteins such as PKR-like ER kinase PERK to induce cytotoxicity. 1,2,4-Trihydroxybenzene selectively activates eIF2α phosphorylation, activates the PERK-eIF2α signaling pathway and induces stress granule formation. 1,2,4-Trihydroxybenzene subsequently exacerbates oxidative stress and causes DNA double-strand breaks, destroying organelles such as mitochondria and ER, and inducing cell death. 1,2,4-Trihydroxybenzene also has the potential to exhibit anti-tumor effect, increase blood pressure, and relieve spasm .

HY-N10361

Drupanin	Monophenols Animals Classification of Application Fields Phenols Disease Research Fields Source Classification Cancer	RAR/RXR PPAR Aldose Reductase
Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC₅₀ value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .

HY-B0075R

Melatonin (standard) Maximum Cited Publications 137 Publications Verification N-Acetyl-5-methoxytryptamine (standard); Melatonin	Structural Classification Natural Products Microorganisms Other disease Disease markers Endogenous metabolite Source Classification	Reference Standards Melatonin Receptor Autophagy Mitophagy Endogenous Metabolite Apoptosis
Melatonin (Standard) is the analytical standard of Melatonin. This product is intended for research and analytical applications. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .

HY-N7082

D-Arabinopyranose	Infection Microorganisms Classification of Application Fields Disease Research Fields Saccharides Monosaccharides Source Classification	Parasite Bacterial AMPK PPAR
D-Arabinopyranose is a rare aldehyde pentose, and its ring-opened form is D-arabinose (HY-N0059). D-arabinose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-arabinose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-arabinose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-arabinose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-arabinose is the ring-opened form of the aldopentose D-?Arabinose (HY-N7082) .

HY-116330

Hyperforin	Anti-inflammation/Immunoregulatory Antibiotics Guttiferae Hyperlcurn perforatum L. Disease Research Plants Anticancer Source Classification	Calcium Channel TRP Channel
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca ²⁺ levels by activating Ca ²⁺-conducting non-selective canonical TRPC6 channels and triggers adipose tissue thermogenesis via the Dlat-AMPK signaling axis to suppress obesity. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .

HY-N4205

Tetrahydropiperine	Alkaloids Piperidine Alkaloids Classification of Application Fields Piperaceae Plants Disease Research Fields Piper nigrum Linn. Source Classification Cancer	Cytochrome P450
Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs<、b>, and an activator of the PI3K/Akt/mTOR<、b> pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke .

HY-133178

Urolithin D 3,4,8,9-Tetrahydroxy urolithin	Microorganisms Classification of Application Fields Phenols Polyphenols Disease Research Fields Source Classification Cancer	Ephrin Receptor PPAR AMPK
Urolithin D (3,4,8,9-Tetrahydroxy urolithin) is a colonic metabolite of Ellagitannins and a competitive, reversible, and selective antagonist of the EphA receptor. Urolithin D inhibits EphA2-ephrin-A1 binding with an IC₅₀ of 0.9 μM. Urolithin D is also a potent antioxidant that scavenges free radicals and repairs oxidized DNA damage. Additionally, Urolithin D suppresses triglyceride accumulation and promotes fatty acid oxidation by activating the AMPK signaling pathway. Urolithin D can be used for research on tumors, metabolic, and inflammatory diseases .

HY-B1173

(+)-Camphor 1 Publications Verification D-(+)-Camphor; (1R)-(+)-Camphor	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Other Diseases Plants Lauraceae Cinnamomum camphora Disease Research Fields Source Classification	Environmental Pollutants Bacterial
(+)-Camphor (D-(+)-Camphor; (1R)-(+)-Camphor) is an isomer of Camphor. Camphor is an agonist of monoterpenoid transient receptor potential (TRP) channels (such as TRPV1, TRPV3, TRPM8) and an inhibitor of TRPA1 channels. Camphor's derivatives have multiple biological activities, including antibacterial, antiviral, antioxidant, analgesic and anticancer. Camphor can selectively activate cold-sensitive TRP channels and inhibit TRPA1-mediated nociceptive signals. Camphor stimulates the cold-sensing nerve endings in the skin and regulates the activity of ion channels to exert analgesic, anti-inflammatory and anti-itching effects. It also has anti-proliferative and anti-mutagenic activities on tumor cells, which may be related to inhibiting ribosome function or inducing cell apoptosis. Camphor can be absorbed through the skin and (+)-Camphor can be used in the study of muscle and joint pain and inflammation .

HY-N1180

Tanshinlactone	Structural Classification Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants Source Classification	SARS-CoV Keap1-Nrf2
Tanshinlactone is a compound found in Salvia miltiorrhiza with anti-coronavirus (CoV) and anti-tumor activities. Tanshinlactone induces methuocytic cell death (methuosis) by activating the NRF2 pathway, and selectively kills ER ⁺, HER2 ⁺/EGFR ⁺ breast cancer cells. Tanshinlactone is applicable to research related to breast cancer and coronavirus infections .

HY-N6009

8-Deoxygartanin	Infection other families Xanthones Classification of Application Fields Phenols Polyphenols Plants Disease Research Fields Source Classification	Parasite NF-κB
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE) . 8-Deoxygartanin exhibits antiplasmodial activity with an IC₅₀ of 11.8 μM for the W2 strain of Plasmodium falciparum . 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC₅₀ of 11.3 μM .

HY-125938

Cycloartenyl ferulate 1 Publications Verification Cycloartenol ferulate; Cycloartenol ferulic acid ester	Triterpenes Monophenols other families Classification of Application Fields Terpenoids Phenols Plants Inflammation/Immunology Disease Research Fields Source Classification	Drug Derivative Apoptosis Reactive Oxygen Species (ROS) JAK STAT
Cycloartenyl ferulate (Cycloartenol ferulate; Cycloartenol ferulic acid ester) is a derivative of γ-oryzanol (HY-B2194) with multiple biological activities including antioxidant, anti-inflammatory, and anti-tumor properties. Cycloartenyl ferulate selectively binds to IFNγR1 (binding affinity K_d = 0.5 μM) to activate the canonical JAK1/2-STAT1 signaling pathway. Cycloartenyl ferulate inhibits paraquat (PQ)-triggered apoptosis and ROS in HK2 cells. Cycloartenyl ferulate enhances the activation and cytolytic activity of natural killer (NK) cells by upregulating the expression of NK cell activation receptors (NKG2D, NKp30, NKp44) and the release of cytotoxic molecules and cytokine IFNγ. Cycloartenyl ferulate exerts anti-cancer effects in tumor mice models. Cycloartenyl ferulate can be used for the study of cancer and allergic inflammation intervention .

HY-B1247R

Protoporphyrin IX (Standard) PPIX (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
Protoporphyrin IX (Standard) is the analytical standard of Protoporphyrin IX. This product is intended for research and analytical applications. Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .

HY-N6576

Hellebrigenin	Animals Classification of Application Fields Disease Research Fields Steroids Source Classification Cancer	p38 MAPK ERK JNK IAP PARP Apoptosis Caspase
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .

HY-N7536

Voacangine	Alkaloids other families Classification of Application Fields Other Diseases Plants Disease Research Fields Indole Alkaloids Source Classification	TRP Channel
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC₅₀=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC₅₀=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC₅₀=9 μM) and it shows noncompetitive inhibition against icilin (IC₅₀=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .

HY-N16409

Berkeleyamide C	Natural Products Microorganisms Source Classification	MMP Caspase
Berkeleyamide C is a selective matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide C blocks MMP-3-mediated tumor cell invasion and metastasis, as well as the abnormal activation of inflammation and apoptosis related to caspase-1. Berkeleyamide C is promising for research of cancers and inflammation-related diseases .

Cat. No.	Product Name	Chemical Structure

HY-117287

Deucravacitinib

30+ Cited Publications

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC₅₀=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis .

HY-B0075S

Melatonin-d4
Melatonin-d₄ is deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Antioxidative and anti-inflammatory properties . Melatonin is a selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation .

HY-114118S3

Semaglutide-13C6,15N TFA

Semaglutide- ¹³C₆, ¹⁵N TFA is the ¹³C- and ¹⁵N-labeled Semaglutide TFA (HY-114118A). Semaglutide TFA is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide TFA promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide TFA also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide TFA has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide TFA can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer .

HY-B0075S1

Melatonin-d3

Melatonin-d₃ is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .

HY-114118S

Semaglutide-d8

Semaglutide-d₈ is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer .

HY-114118S1

Semaglutide-d8 tetraTFA

Semaglutide-d₈ tetraTFA is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer .

HY-101064S3

Fmoc-leucine-d10
Fmoc-leucine-d₁₀ is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .

HY-13757AS

Tamoxifen-d5
Tamoxifen-d₅ is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity .

HY-113134S

25-Hydroxycholesterol-d6
25-Hydroxycholesterol-d₆ (25-OHC-d₆) is the deuterium labeled 25-Hydroxycholesterol. 25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC₅₀≈65 nM) and selective suppressor of IgA production by B cells .

HY-101064S2

Fmoc-leucine-d3
Fmoc-leucine-d₃ is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .

HY-B0075S2

Melatonin-d7

Melatonin-d₇ is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .

HY-13749AS

Sitagliptin-d4 phosphate

Sitagliptin-d₄ phosphate (MK-0431-d₄) is the deuterium labeled Sitagliptin phosphate (HY-13749A). Sitagliptin phosphate is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes.

HY-16985S

Darolutamide-d4

Darolutamide-d₄ (ODM-201-d₄) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a K_i of 11 nM for rat wild-type AR (wtAR) and an IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .

HY-14233S

Omecamtiv mecarbil-d8
Omecamtiv mecarbil-d₈ is the deuterium labeled Omecamtiv mecarbil. Omecamtiv mecarbil (CK-1827452) is a selective cardiac myosin activator.

HY-101064S1

Fmoc-leucine-13C6,15N
Fmoc-leucine- ¹³C₆, ¹⁵N is a ¹⁵N-labeled and ¹³C-labled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity

HY-17386S1

Rosiglitazone-d4
Rosiglitazone-d₄ is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer .

HY-13749S1

Sitagliptin-d4 hydrochloride

Sitagliptin-d₄ hydrochloride is the deuterium labeled Sitagliptin hydrochloride (HY-13749E). Sitagliptin hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC₅₀ value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes.

HY-G0017S

N-Desmethyl imatinib-d8

N-Desmethyl imatinib-d₈ is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .

HY-17386S

Rosiglitazone-d3
Rosiglitazone-d₃ is the deuterium labeled Rosiglitazone. Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC₅₀=~30 μM) and an inhibitor of TRPM3 .

HY-15332

Alfacalcidol-d6
Alfacalcidol-d₆ is the deuterium labeled Alfacalcidol. Alfacalcidol is a non-selective VDR activator.

HY-126585S

SAICAR-d3
SAICAR-d₃ is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC₅₀ of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .

HY-10003S

Alfacalcidol-d7
Alfacalcidol-d₇ is the deuterium labeled Alfacalcidol. Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis .

HY-109128S

Danicamtiv-d6
Danicamtiv-d₆ (MYK-491-d₆) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .

HY-13757S

Tamoxifen-d3 hydrochloride

Tamoxifen-d₃ hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .

HY-W754911

Avapritinib-d3

Avapritinib-d₃ (BLU-285-d₃) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

HY-14300AS

Vilanterol-d4 trifenatate

Vilanterol-d₄ (trifenatate) is deuterium labeled Vilanterol (trifenatate).Vilanterol (GW642444) acetate is a long-acting β₂ adrenergic receptor agonist. Vilanterol acetate has pEC₅₀ values for β₂-AR, β₁-AR, and β₃-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β₂ adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research.

HY-B0197AS

Naratriptan-d3 hydrochloride

Naratriptan-d₃ (GR-85548A-d₃) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC₅₀=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms .

HY-N0059S1

D-Arabinose-13C-1

D-Arabinose- ¹³C-1 is the ¹³C labeled D-Arabinose (HY-N0059). D-Arabinose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-Arabinose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-Arabinose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-Arabinose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-Arabinose is the ring-opened form of the aldopentose D-?Arabinose (HY-N7082) .

HY-N0059S3

D-Arabinose-13C-3

D-Arabinose- ¹³C-3 is the ¹³C labeled D-Arabinose (HY-N0059). D-Arabinose is is an orally active antidepressant and a growth inhibitor of C. elegans (IC₅₀ is 7.5 mM). D-Arabinose can penetrate the blood-brain barrier, selectively interfere with the metabolism of D-ribose and D-fructose, and inhibit the growth of nematodes. D-Arabinose can also inhibit the synthesis of cell biofilm and exert antibacterial activity. D-Arabinose activates the ACSS2-PPARγ/TFEB-CRTC1 axis through the lysosomal AXIN-LKB1-AMPK pathway, inducing CRTC1 transcription, exerts antidepressant-like activity. D-Arabinose is the ring-opened form of the aldopentose D-?Arabinose (HY-N7082) .

HY-10119S

Vorapaxar-d5
Vorapaxar-d₅ is deuterated labeled Vorapaxar (HY-10119). Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor *protease-activated* receptor (PAR-1) antagonist (K_i*=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating* peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .

HY-B1221S1

Flufenamic acid-13C6

Flufenamic acid- ¹³C₆ is the ¹³C₆ labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca ²⁺ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

HY-B1221S

Flufenamic acid-d4

Flufenamic acid-d₄ is deuterium labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca ²⁺ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.

HY-109128S1

Danicamtiv-d3
Danicamtiv-d₃ (MYK-491-d₃) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .

HY-13757AS1

Tamoxifen-d3

Tamoxifen-d₃ is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .

HY-109128S2

Danicamtiv-d3-1
Danicamtiv-d₃-1 (MYK-491-d₃-1) is a deuterated labeled Danicamtiv (HY-109128). Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency .

HY-W778408

Tamoxifen-13C6

Tamoxifen- ¹³C₆ (ICI 47699- ¹³C₆) is the ¹³C-labeled Tamoxifen (HY-13757A). Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .

HY-137813S

PERK-IN-4-d3
PERK-IN-4-d₃ is the deuterium labeled PERK-IN-4. PERK-IN-4 is a potent and selective PERK (protein kinase R (PKR)-like endoplasmic reticulum kinase) inhibitor with an IC₅₀ of 0.3 nM. PERK is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states .

HY-121538S

CUDA-d11
CUDA-d₁₁ is deuterium labeled CUDA (HY-121538). CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC₅₀s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively . CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease .

HY-W721606

Chlorantraniliprole-d6
Chlorantraniliprole-d₆ is the deuterium labeled Chlorantraniliprole (HY-112820). Chlorantraniliprole is an insecticide that potently and selectively activates insect ryanodine receptor, with EC₅₀s of 40 nM and 50 nM for Drosophila melanogaster and H. virescens ryanodine receptor, and ～300-fold more potent than that in the mouse myoblast cell line, C2C12 (EC₅₀, 14 μM).

HY-B1794S

Thiethylperazine-d3
Thiethylperazine-d₃ is the deuterium labeled Thiethylperazinee (HY-B1794). Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects .

HY-W774926

Permethrin-d6

Permethrin-d₆ (NRDC-143-d₆) is deuterium labeled Permethrin. Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes) .

HY-12383S

Pelubiprofen-13C,d3

Pelubiprofen- ¹³C,d₃ is the ¹³C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects .

HY-10569S

Ponesimod-d4

Ponesimod-d₄ (ACT-128800-d₄) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .

HY-B0689S1

Indinavir-13C4,15N

Indinavir- ¹³C₄, ¹⁵N (MK-639 (free base)- ¹³C₄, ¹⁵N) is ¹³C and ¹⁵N labeled Indinavir. Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a K_i of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CL ^pro inhibitor .

HY-W748582

Clozapine N-oxide-d8

Clozapine N-oxide-d₈ is the deuterium labeled Clozapine N-oxide (HY-17366). Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

HY-135582S1

Raloxifene 4'-glucuronide-d4 lithium

Raloxifene 4'-glucuronide-d₄ (lithium) is deuterium labeled Raloxifene 4'-glucuronide. Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC₅₀ of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .

HY-135581S1

Raloxifene 6-glucuronide-d4 lithium

Raloxifene 6-glucuronide-d₄ (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC₅₀ of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .

HY-10569S1

Ponesimod-d7

Ponesimod-d₇ (ACT-128800-d₇) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d₇ (ACT-128800) is a potent, selective and orally active agonist of S1P₁, with an IC₅₀ of 6 nM in a radioligand binding assay. Ponesimod-d₇ activates S1P₁-mediated signal transduction with high potency (EC₅₀=5.7 nM). Ponesimod-d₇ can protect against lymphocyte-mediated tissue inflammation .

HY-135582S

Raloxifene 4'-glucuronide-d4

Raloxifene 4'-glucuronide-d₄ is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC₅₀ of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .

HY-B1272AS

Desipramine-d4

Desipramine-d₄ is the deuterium labeled Desipramine (HY-B1272A). Desipramine is a first-generation tricyclic antidepressant. Desipramine selectively binds to norepinephrine transporter and blocks neuronal norepinephrine reuptake. Desipramine activates MAPK signaling via ERK1/2, JNK, and p38, represses NF-κB and AP-1 activity, and induces apoptosis via ROS elevation, mitochondrial membrane potential reduction, and intracellular calcium increase. Desipramine also shows anyi-inflammatory activity, inhibiting TNF-α production. Desipramine can be used for the research of hepatocellular cancer, inflammation, and neurological diseases .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B0764G

Bucladesine sodium Dibutyryl cAMP sodium; DBcAMP sodium	PKA Reactive Oxygen Species (ROS) Apoptosis	Neurological Disease Inflammation/Immunology Cancer
Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (GMP) is a Bucladesine sodium (HY-B0764) produced by using GMP guidelines. Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks