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Results for "

AR Inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5 alpha Reductase (5) 5-HT Receptor (5) Acetolactate Synthase (ALS) (1) ADC Cytotoxin (1) Adenosine Receptor (20) Adrenergic Receptor (20) Aldose Reductase (16) Androgen Receptor (63) Antibiotic (4) Apoptosis (27) Aryl Hydrocarbon Receptor (2) Aurora Kinase (1) Autophagy (2) AUTOTACs (1) Bacterial (6) c-Myc (3) CaMK (1) Carbonic Anhydrase (1) CD20 (1) CDK (1) Complement System (7) COX (1) Cytochrome P450 (1) DNA Methyltransferase (1) DNA/RNA Synthesis (2) Dopamine Receptor (1) Drug Metabolite (1) EGFR (1) Endogenous Metabolite (5) Epigenetic Reader Domain (4) Epoxide Hydrolase (1) Estrogen Receptor/ERR (4) Free Fatty Acid Receptor (1) Fungal (9) G protein-coupled Bile Acid Receptor 1 (1) G Protein-coupled Receptor Kinase (GRK) (1) Glucocorticoid Receptor (2) GLUT (1) GSK-3 (2) HDAC (2) Histone Acetyltransferase (3) Histone Methyltransferase (1) Influenza Virus (1) Isotope-Labeled Compounds (6) MAP3K (1) MAPKAPK2 (MK2) (1) MDM-2/p53 (1) MicroRNA (4) Mitochondrial Metabolism (2) Mitophagy (1) MNK (1) Molecular Glues (1) Monoamine Oxidase (1) Monocarboxylate Transporter (2) mTOR (1) nAChR (1) NF-κB (1) NO Synthase (3) P2Y Receptor (1) p38 MAPK (2) Parasite (3) PARP (2) PDK-1 (1) Phosphodiesterase (PDE) (3) Photosystem II (1) PKC (1) Polo-like Kinase (PLK) (1) PPAR (2) Progesterone Receptor (2) PROTACs (10) Reactive Oxygen Species (3) Renin (3) ROCK (6) ROS Kinase (1) STAT (2) Thrombin (3) TNF Receptor (1) Topoisomerase (1) Transketolase (1) Trk Receptor (1)
By Research Areas:	Cancer (107) Cardiovascular Disease (20) Endocrinology (21) Infection (16) Inflammation/Immunology (27) Metabolic Disease (22) Neurological Disease (26)
Oligonucleotides:	miRNA antagomirs (2) MicroRNAs (4) miRNA inhibitors (2)

195

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10547

OSU-03012 4 Publications Verification AR-12; PDK1 Inhibitor AR-12	PDK-1 Autophagy	Cancer
OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC₅₀ of 5 μM .

HY-10512

AR-A014418 15+ Cited Publications AR 0133418; GSK 3β Inhibitor VIII; AR 014418	GSK-3	Metabolic Disease Cancer
AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC₅₀=104 nM; K_i=38 nM) .

HY-164373

SC428	Androgen Receptor Apoptosis	Cancer
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .

HY-12798C

AR-13503 AR-13324 M1 metabolite	Drug Metabolite	Others
AR-13503 (AR-13324 M1 metabolite) is a hydrolysis metabolite of AR-13324 mesylate. AR-13324 is a inhibitor of ROCK kinase.

HY-19346

AR-13324 analog mesylate	ROCK	Others
AR-13324 analog mesylate is an analog of AR-13324. AR-13324 is an ROCK and norepinephrine transporter (NET) inhibitor .

HY-120208

MK204	Aldose Reductase	Metabolic Disease
MK204 is an aldose reductase (AR) inhibitor that can be used in diabetes research .

HY-RI01656

hsa-miR-548ar-3p inhibitor	MicroRNA	Cancer
hsa-miR-548ar-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

hsa-miR-548ar-3p inhibitor hsa-miR-548ar-3p inhibitor

HY-RI01657

hsa-miR-548ar-5p inhibitor	MicroRNA	Cancer
hsa-miR-548ar-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

hsa-miR-548ar-5p inhibitor hsa-miR-548ar-5p inhibitor

HY-10512S

AR-A014418-d3 AR 0133418-d₃; GSK 3β Inhibitor VIII-d₃; AR 014418-d₃	Isotope-Labeled Compounds GSK-3	Metabolic Disease Cancer
AR-A014418-d₃ is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].

HY-105122

Zanoterone WIN 49596	Androgen Receptor	Endocrinology Cancer
Zanoterone is an orally active antagonist of the androgen receptor (AR) with a K_i of 2.2 μM. Zanoterone blocks the binding of androgens such as testosterone and dihydrotestosterone (DHT), inhibiting the androgen signaling pathway, thereby reducing androgen-dependent prostate hyperplasia and prostate cancer growth .

HY-125639

(rac)-AR-13503 (rac)-AR-13324 M1 metabolite	PKC ROCK	Cardiovascular Disease
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .

HY-106769B

(3aR,9aR)-Fluparoxan (3AR,9AR)-GR50360	Others	Neurological Disease
(3aR,9aR)-Fluparoxan ((3aR,9aR)-GR50360) is a highly selective and potent α2B adrenaline receptor antagonist with the activity of preventing, improving or inhibiting neurodevelopmental disorders and neurodegenerative diseases. As an α2B receptor antagonist, (3aR,9aR)-Fluparoxan can promote the recovery of neurological function. The mechanism of action of (3aR,9aR)-Fluparoxan makes it have important application potential in neuroscience research .

HY-163510

AR/AR-V7-IN-1	Androgen Receptor	Cancer
AR/AR-V7-IN-1 (Compound 20i) is an *AR/ARV7* inhibitor (IC₅₀ = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC₅₀ values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .

HY-142923

AR antagonist 2	Androgen Receptor	Cancer
AR antagonist 2 (compound 58) is a potent androgen receptor (AR) inhibitor with an IC₅₀ of 0.95 μM. AR antagonist 2 has the potential for cancer research .

HY-158180

A3AR agonist 4	Adenosine Receptor	Inflammation/Immunology
A3AR agonist 4 is an A3 adenosine receptor (A3AR) agonist (K_i: 1.24 nM for hA3AR). A3AR agonist 4 inhibits cAMP production with an EC₅₀ of 0.17 nM. A3AR agonist 4 can be used for research of inflammation and pain .

HY-13265

AR-42 2 Publications Verification HDAC-42; OSU-HDAC42	HDAC Autophagy Apoptosis	Cancer
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC₅₀=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .

HY-164552

ZNU-IMB-Z15	Apoptosis Androgen Receptor	Cancer
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .

HY-111151

AR-9281 APAU	Epoxide Hydrolase	Infection Cardiovascular Disease Metabolic Disease
AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC₅₀ values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes .

HY-N1943

Ailanthone Δ13-DehydrochapARrinone	Androgen Receptor	Inflammation/Immunology Cancer
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC₅₀=69 nM) and constitutively active truncated AR splice variants (AR_1-651 IC₅₀=309 nM).

HY-155543

Anticancer agent 135	Androgen Receptor	Cancer
Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .

HY-148771

MTX-23 PROTAC AR-V7 degrader-2	PROTACs Androgen Receptor Apoptosis	Cancer
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis .

HY-16758

Verosudil AR-12286	ROCK	Neurological Disease
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with K_is of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork .

HY-120018

VPC-13566	Androgen Receptor	Cancer
VPC-13566, a BF3-specific small molecule, is an androgen receptor (AR) inhibitor. VPC-13566 is effective in inhibiting AR transcriptional activity in vitro as well as the growth of AR-dependent PCa cell lines. VPC-13566 can be used as a chemical probe to help identify unknown AR partners.VPC-13566 can be used for the research of cancer.

HY-162585

5-HT1AR agonist 1	5-HT Receptor	Neurological Disease
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including *5-HT1AR* agonist with an EC₅₀ value of 34 nM, SERT reuptake ihibitor (IC₅₀ =12 nM), NET reuptake inhibitor (IC₅₀ =78 nM) and DAT reuptake inhibitor (IC₅₀ =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .

HY-116522

AR420626 3 Publications Verification	Free Fatty Acid Receptor Histone Methyltransferase HDAC mTOR CaMK p38 MAPK Epigenetic Reader Domain GLUT nAChR TNF Receptor	Metabolic Disease Inflammation/Immunology Cancer
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC₅₀=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca ²⁺ signal-mediated glucose uptake and improve diabetes .

HY-12798A

Netarsudil dimesylate AR-13324 dimesylate	ROCK	Others
Netarsudil mesylate (AR-13324 mesylate) is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.

HY-15314

Ranirestat 1 Publications Verification AS-3201	Aldose Reductase	Neurological Disease Metabolic Disease
Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC₅₀s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a K_i of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas .

HY-117669

VPC-14228	Androgen Receptor	Cancer
VPC-14228 is a potent androgen receptor DNA binding domain (AR-DBD) inhibitor that interferes with the interaction of AR with androgen response elements and effectively blocks AR transcriptional activity. VPC-14228 can be used in prostate cancer research .

HY-116501

VPC-14449	Androgen Receptor	Cancer
VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC₅₀ of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer .

HY-12122

AR-C102222	NO Synthase	Neurological Disease
AR-C102222 is a spirocyclic fluoropiperidine quinazoline selective iNOS inhibitor. AR-C102222 can be used for the research of neuropathic pain .

HY-156111

ARD-1676	PROTACs Androgen Receptor	Cancer
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .

HY-110126

AR-C118925XX 1 Publications Verification	P2Y Receptor	Inflammation/Immunology Cancer
AR-C118925XX is a selective P2Y2 receptor antagonist. AR-C118925XX inhibits ATP-induced IL-6 production and phosphorylation of p38. AR-C118925XX also inhibits Bleomycin (HY-108345)-induced dermal fibrosis in mice. AR-C118925XX also inhibits ATP-induced tumor growth .

HY-145709

Ar-V7-IN-1	Androgen Receptor	Cancer
Ar-V7-IN-1 is a potent inhibitor of *Ar-V7*. AR-V7 is a hormone-independent splice variant of the androgen receptor. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer (extracted from patent WO2018114781A1, compound 43) .

HY-119993

AR03 BMH-23	DNA/RNA Synthesis	Cancer
AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC₅₀ of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .

HY-16055

Silatecan AR-67; DB 67	Topoisomerase	Cancer
Silatecan (AR-67; DB 67) is a Camptothecin (HY-16560) analogue with improved stability and lipophilicity. Silatecan is an inhibitor for topoisomerase I, that inhibits the DNA replication and transcription, and exhibits antitumor and radiosensitizing activities

HY-151596

MAO-A/5-HT2AR-IN-1	Monoamine Oxidase 5-HT Receptor	Neurological Disease
MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and *5-HT2AR* dual inhibitor, with IC₅₀ values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent .

HY-121588

IMTPPE	Adrenergic Receptor	Cancer
IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .

HY-N4089

Quercetin 3-gentiobioside	Aldose Reductase	Metabolic Disease
Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs) .

HY-12798B

Netarsudil hydrochloride AR-13324 hydrochloride	ROCK	Neurological Disease
Netarsudil hydrochloride (AR-13324 hydrochloride) is a Rho-associated protein kinas (ROCK) and norepinephrine transporter (NET) inhibitor. Netarsudil hydrochloride has effective in intraocular pressure (IOP) reduction .

HY-147907

*Adenosine receptor inhibitor* 1**	Adenosine Receptor	Neurological Disease Inflammation/Immunology Cancer
Adenosine receptor inhibitor 1 is a potent and selective adenosine receptor (AR) inhibitor with K_i values of >1000, 68.5, >1000, >1000 nM for A₁AR, A_2AAR, A_2BAR, A₃AR, respectively. Adenosine receptor inhibitor 1 shows antinociceptive activity, anti-inflammatory effect and peripheral analgesic effect. Adenosine receptor inhibitor 1 has the potential for the research of cancer or neurodegenerative diseases .

HY-163940

LX1	Aldose Reductase Androgen Receptor	Cancer
LX1 is an anti-prostate cancer compound that targets androgen receptor (AR), AR variants and steroidogenic enzyme AKR1C3. LX1 inhibits the enzymatic activity of AKR1C3, reduces the conversion of androstenedione to testosterone and reduces the expression of AR and *AR-V7* and downregulates their target genes. LX1 overcomes the resistance of tumor cells to Enzalutamide (HY-70002), and the combination with Enzalutamide (HY-70002) further inhibits tumor growth .

HY-163363

β-AR antagonist 2	Adrenergic Receptor	Cancer
β-AR antagonist 2 (compound 43) is an antagonist of *β-AR* (IC₅₀: 0.17 μM). β-AR-IN-1 inhibits the growth of mouse A549 xenograft tumors and shows cardioprotective efficacy against DOX-induced HF in C57 mice .

HY-16079

AZD3514 3 Publications Verification	Androgen Receptor	Cancer
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC₅₀ value of 5.75. AZD3514 can be used for the research of prostate cancer .

HY-123875A

Ralaniten triacetate EPI-506	Androgen Receptor	Cancer
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7 .

HY-132292

ARD-2128	PROTACs Androgen Receptor	Cancer
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer .

HY-161409

SC912	Androgen Receptor Apoptosis	Cancer
SC912 is an *AR-V7* inhibitor (IC₅₀ = 0.36 μM). SC912 possesses safety, potency and selectivity. SC912 binds directly to AR-FL and AR-V7 proteins, inhibites nuclear localization and chromatin binding capabilities. SC912 exerts anticancer activity through inhibition of proliferation, induction of cell cycle arrest and apoptosis .

HY-150025

(4aS,8aR)-NPD-001	DNA Methyltransferase Apoptosis	Cancer
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .

HY-147706

AR524	Others	Cancer
Ar524 has higher inhibitory activity than the known transgenic inhibitor kifunensine. At the same time, ar524 inhibited low concentration (10 μ M) Spheroid formation of human malignant cells.

HY-163379

C5aR1 antagonist 2	Complement System	Inflammation/Immunology
C5aR1 antagonist 2 (Compound 6a) is an orally active C5a receptor 1 (C5aR1) antagonist that shows efficacy in inhibiting the C5a-induced neutrophil count increase. C5aR1 antagonist 2 is potent in the DISCO and migration assays, with IC₅₀ values of 21 and 3 nM, respectively. C5aR1 antagonist 2 can be used for the research of acute and chronic inflammatory diseases .

HY-101479S

Iclaprim-d6	Isotope-Labeled Compounds Bacterial Antibiotic	Infection
Iclaprim-d₆ (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.

Cat. No.	Product Name

HY-L129

Target Protein Ligand Library

37 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 37 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Cat. No.	Product Name	Target	Research Area

HY-P10542

Dodecapeptide AR71	Peptides	Cancer
Dodecapeptide AR71 is an inhibitor of melanoma inhibitory activity (MIA). Dodecapeptide AR71 can reduce cell migration, reduce metastasis formation, and increase immune response. Dodecapeptide AR71 can be used in research on the treatment of malignant melanoma .

HY-P5509

C5aR1 antagonist peptide	Peptides	Others
C5aR1 antagonist peptide is a biological active peptide. (This linear peptide is derived from the C-terminus of the chemokine, complement fragment 5 anaphylatoxin (C5a). This peptide functions to inhibit C5a binding and function at human and rat C5a receptors. C5a is crucial to triggering cellular immune responses and its overexpression is involved in arthritis, Alzheimer’s disease, cystic fibrosis, systemic lupus erythematosus, and other immunoinflammatory diseases.)

Cat. No.	Product Name	Target	Research Area

HY-P99483

Blontuvetmab AT 004; VT 007	CD20 Adenosine Receptor	Cancer
Blontuvetmab (AT 004) is a caninized CD20 monoclonal antibody and is also a potent, selective, highly potent antagonist of A2aR receptor. Blontuvetmab behaves as Nociceptin (HY-P0183)/Orphanin (HY-P0183) FQ receptor (NOP) agonists displaying weak NOP affinity. Blontuvetmab inhibits 5'-N-Ethylcarboxamidoadenosine (NECA)-mediated A2aR activation and significantly reverses the ability of adenosine to suppress CD8 T cell activation, increasing levels of cytokines such as IFN-γ. Blontuvetmab Blontuvetmab can be used for the research of Canine B-cell lymphoma .

HY-P990186

Anti-Mouse MHC Class II (I-Ak, I-Ar, I-Af, I-As,I-Ag7) Antibody (10-3.6.2)	Inhibitory Antibodies	Others
Anti-Mouse MHC Class II (I-Ak, I-Ar, I-Af, I-As,I-Ag7) Antibody (10-3.6.2) is a mouse-derived IgG2c, κ type antibody inhibitor, targeting to mouse MHC Class II.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N1943

Ailanthone Δ13-DehydrochapARrinone	Structural Classification Simaroubaceae Ailanthus altissima (Mill.) Swingle Classification of Application Fields Terpenoids Source classification Diterpenoids Plants Inflammation/Immunology Disease Research Fields	Androgen Receptor
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of both full-length androgen receptor (AR) (IC₅₀=69 nM) and constitutively active truncated AR splice variants (AR_1-651 IC₅₀=309 nM).

HY-N4089

Quercetin 3-gentiobioside	Flavonols Structural Classification Flavonoids other families Classification of Application Fields Source classification Phenols Polyphenols Metabolic Disease Plants Disease Research Fields	Aldose Reductase
Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs) .

HY-N0138

Theobromine 1 Publications Verification 3,7-Dimethylxanthine	Alkaloids Structural Classification Microorganisms Neurological Disease Classification of Application Fields Cocoa beans Other Alkaloids Sterculiaceae Source classification Plants Endogenous metabolite Disease Research Fields	Adenosine Receptor Endogenous Metabolite
Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.

HY-114936

Piericidin A 1 Publications Verification AR-054	Structural Classification Neurological Disease Classification of Application Fields Source classification Anti-parasitic Antibacterial Disease Research Other Antibiotics Infection Microorganisms Antibiotics Anticancer Disease Research Fields	Bacterial ADC Cytotoxin Antibiotic Mitochondrial Metabolism
Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity .

HY-B0573

Propranolol hydrochloride Maximum Cited Publications 23 Publications Verification	Alkaloids Neurological Disease Classification of Application Fields Other Alkaloids Source classification Endogenous metabolite Disease Research Fields Endocrinology	Adrenergic Receptor Bacterial
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-B0573B

Propranolol Maximum Cited Publications 23 Publications Verification	Cardiovascular Disease Alkaloids Neurological Disease Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Adrenergic Receptor Bacterial
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-N7045

Isosilybin B 1 Publications Verification	Structural Classification Classification of Application Fields Source classification Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Flavanonols Flavonoids Glycine soya Phenols Polyphenols Disease Research Fields Cancer	Androgen Receptor Apoptosis
Isosilybin B, a flavonolignan isolated from Silybum marianum, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation .

HY-N4089R

Quercetin 3-gentiobioside (Standard)	Flavonols Structural Classification Flavonoids other families Source classification Phenols Polyphenols Plants	Aldose Reductase
Quercetin 3-gentiobioside (Standard) is the analytical standard of Quercetin 3-gentiobioside. This product is intended for research and analytical applications. Quercetin 3-gentiobioside is isolated from A. iwayomogi, AR and AGE formation inhibitor, demonstrates biological activities against Aldose reductase (AR) and the formation of advanced glycation endproducts (AGEs) .

HY-N0138R

Theobromine (Standard)	Alkaloids Structural Classification Microorganisms Cocoa beans Other Alkaloids Sterculiaceae Source classification Plants Endogenous metabolite	Adenosine Receptor Endogenous Metabolite
Theobromine (Standard) is the analytical standard of Theobromine. This product is intended for research and analytical applications. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.

HY-B0573R

Propranolol hydrochloride (Standard)	Alkaloids Other Alkaloids Source classification Endogenous metabolite	Adrenergic Receptor Bacterial
Propranolol (hydrochloride) (Standard) is the analytical standard of Propranolol (hydrochloride). This product is intended for research and analytical applications. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ ³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .

HY-112052

Aminomalonic acid	Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Endogenous Metabolite
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (K_i= 0.0023 M) and mouse pancreas (K_i= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis .

HY-122917

Danshenol A	Terpenoids Labiatae Samanea saman (Jacq.) Merr. Diterpenoids Plants	Aldose Reductase Reactive Oxygen Species
Danshenol A, an abietane-type diterpenoid, is an aldose reductase (AR) inhibitor with an IC₅₀ of 0.1 μM. Danshenol A can protect endothelial cells from oxidative stress by directly scavenging ROS. Danshenol A has anti-inflammatory and antitumor properties. Danshenol A can be used for atherosclerosis research .

HY-N2037

Higenamine 3 Publications Verification Norcoclaurine; Demethyl-Coclaurine	Alkaloids Structural Classification Classification of Application Fields Ranunculaceae Source classification Phenols Polyphenols Aconitum carmichaeli Debx. Plants Isoquinoline Alkaloids Disease Research Fields Endocrinology	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-N7043

Isosilybin A 2 Publications Verification	Structural Classification Classification of Application Fields Source classification Cyamopsis tetragonoloba (L.) Taub. Plants Compositae Flavanonols Flavonoids Glycine soya Phenols Polyphenols Disease Research Fields Cancer	Apoptosis
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .

HY-N0790

Lupeol 3 Publications Verification Clerodol; Monogynol B; FagARasterol	Triterpenes Structural Classification other families Classification of Application Fields Terpenoids Source classification Plants Disease Research Fields Cancer	Androgen Receptor Apoptosis
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-N3716

Dehydroglyasperin D	Structural Classification Leguminosae Source classification Phenols Polyphenols Plants Glycyrrhiza uralensis Fisch.	Aldose Reductase COX
Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC₅₀: 62.4 μM and 176.2 μM respectively). Dehydroglyasperin D has anti-obesity, antioxidant effects. Dehydroglyasperin D shows anti-inflammatory activity by inhibiting COX-2 expression and the MLK3 signaling pathway. Dehydroglyasperin D also inhibits melanin synthesis. Dehydroglyasperin D is a prenylated flavonoid that can be isolated from Glycyrrhiza uralensi .

HY-N6883

6-Methoxytricin	Flavonoids other families Classification of Application Fields Flavones Source classification Phenols Polyphenols Metabolic Disease Plants Disease Research Fields	Aldose Reductase
6-Methoxytricin (Compound 6) is an flavonoid isolated from Artemisia iwayomogi. 6-Methoxytricin (Compound 6) is an inhibitor on aldose reductase (AR) and advanced glycation endproduct (AGE) formation activities with IC₅₀ values of 30.29 μM and 134.88 μM, respectively. 6-Methoxytricin (Compound 6) has potential as an anti-diabetic complications agent .

HY-139104

Thailanstatin D	Alkaloids Microorganisms Classification of Application Fields Source classification Disease Research Fields Cancer	DNA/RNA Synthesis Apoptosis
Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis .

HY-N2908

Atraric acid Methyl atrARate	Structural Classification Microorganisms Classification of Application Fields Phenols Essence, Fragrance Cosmetic Research Plants Inflammation/Immunology Disease Research Fields Cancer	Androgen Receptor NO Synthase p38 MAPK NF-κB
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .

HY-N7043R

Isosilybin A (Standard)	Flavanonols Structural Classification Flavonoids Glycine soya Source classification Phenols Polyphenols Cyamopsis tetragonoloba (L.) Taub. Plants Compositae	Apoptosis
Isosilybin A (Standard) is the analytical standard of Isosilybin A. This product is intended for research and analytical applications. Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis .

HY-N0236

Corylin 5 Publications Verification	Infection Structural Classification Monophenols Flavonoids Classification of Application Fields Leguminosae Source classification Phenols Psoralea corylifolia L. Plants Disease Research Fields Isoflavones	Antibiotic STAT
Corylin is an orally active flavonoid anti-inflammatory and osteogenic agent that inhibits IL-6-induced STAT3 promoter activity and STAT3 phosphorylation. Corylin also has anticancer, antiatherosclerotic, and ameliorating activity in hyperlipidemia and insulin resistance, inducing adipocyte browning and lipolysis through SIRT1 or β3-AR-dependent pathways .

HY-N0790R

Lupeol (Standard)	Triterpenes Structural Classification other families Terpenoids Source classification Plants	Androgen Receptor Apoptosis
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .

HY-N0236R

Corylin (Standard)	Structural Classification Monophenols Flavonoids Leguminosae Source classification Phenols Psoralea corylifolia L. Plants Isoflavones	Antibiotic STAT
Corylin (Standard) is the analytical standard of Corylin. This product is intended for research and analytical applications. Corylin is an orally active flavonoid anti-inflammatory and osteogenic agent that inhibits IL-6-induced STAT3 promoter activity and STAT3 phosphorylation. Corylin also has anticancer, antiatherosclerotic, and ameliorating activity in hyperlipidemia and insulin resistance, inducing adipocyte browning and lipolysis through SIRT1 or β3-AR-dependent pathways .

Cat. No.	Product Name	Chemical Structure

HY-N0138S

Theobromine-d6
Theobromine-d₆ is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.

HY-N0138S1

Theobromine-d3
Theobromine-d₃ is the deuterium labeled Theobromine. Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 (AR1) signaling.

HY-B0573BS

Propranolol-d7

Propranolol-d₇ is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

HY-B0573S

Propranolol-d7 hydrochloride

Propranolol-d₇ (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

HY-B0573S1

Propranolol-d7 (ring-d7)

Propranolol-d₇ (ring-d₇) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].

HY-10512S

AR-A014418-d3
AR-A014418-d₃ is the deuterium labeled AR-A014418. AR-A014418 is a potent, selective, and ATP-competitive GSK3β inhibitor (IC50=104 nM; Ki=38 nM)[1].

HY-101479S

Iclaprim-d6
Iclaprim-d₆ (AR-100-d6) is the deuterium labeled Iclaprim. Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.

HY-116214S1

Cyprodinil-13C6

Cyprodinil- ¹³C₆ is the ¹³C₆ labeled Cyprodinil. Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC₅₀s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).

HY-116214S

Cyprodinil-d5

Cyprodinil-d₅is the deuterium labeledCyprodinil(HY-116214) . Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC₅₀s=0.44, 4.8, and 0.03 μM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC₅₀=1.91 μM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC₅₀=15.1 μM) .

HY-B0846S

Dimethomorph-d8
Dimethomorph-d₈ is the deuterium labeled Dimethomorph[1]. Dimethomorph is a fungicide belongs to the fungicide group of sterol biosynthesis inhibitor. Dimethomorph can inhibit fungal cell wall formation. Dimethomorph also inhibits androgen receptor (AR) activity in MDA-kb2 cells with an IC20 of 0.263 μM[2][3][4].

HY-13613S

Dutasteride-13C6
Dutasteride- ¹³C₆ is the ¹³C labeled Dutasteride[1]. Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT[2].

HY-13613S2

Dutasteride-13C,15N,d
Dutasteride- ¹³C, ¹⁵N,d is ¹⁵N and deuterated labeled Dutasteride (HY-13613). Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .

Cat. No.	Product Name		Classification

HY-RI01656

hsa-miR-548ar-3p inhibitor		MicroRNAs miRNA inhibitors
hsa-miR-548ar-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

HY-RI01657

hsa-miR-548ar-5p inhibitor		MicroRNAs miRNA inhibitors
hsa-miR-548ar-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

HY-RI01656A

hsa-miR-548ar-3p antagomir		MicroRNAs miRNA antagomirs
hsa-miR-548ar-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

HY-RI01657A

hsa-miR-548ar-5p antagomir		MicroRNAs miRNA antagomirs
hsa-miR-548ar-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

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