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Results for "

Allosteric inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Acetyl-CoA Carboxylase (3) ADC Linker (1) ADC Payload (1) Adenosine Receptor (4) Adenylate Cyclase (1) Adrenergic Receptor (1) Akt (24) Amino acid Transporter (2) Aminoacyl-tRNA Synthetase (1) Aminopeptidase (1) Amyloid-β (3) Anaplastic lymphoma kinase (ALK) (1) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (9) AP-1 (1) Apoptosis (48) Arp2/3 Complex (2) Atg4 (1) ATP Citrate Lyase (3) ATP Synthase (3) Aurora Kinase (2) Autophagy (16) Bacterial (18) Bcl-2 Family (4) Bcr-Abl (10) Biochemical Assay Reagents (1) Bombesin Receptor (2) c-Kit (2) c-Met/HGFR (1) Calcium Channel (2) Cannabinoid Receptor (3) Carbamoyl Phosphate Synthetase (CPS) (2) Carbonic Anhydrase (3) Carboxypeptidase (1) Casein Kinase (3) Caspase (10) CaSR (2) CCR (3) CDK (5) Cholinesterase (ChE) (6) ClpP (1) Complement System (1) Connective Peptide (1) COX (7) CXCR (9) Cyclic GMP-AMP Synthase (2) Cytochrome P450 (12) Dengue Virus (2) Deubiquitinase (3) Discoidin Domain Receptor (1) DNA Alkylator/Crosslinker (1) DNA Methyltransferase (2) DNA/RNA Synthesis (22) Dopamine Receptor (7) Dopamine Transporter (4) Drug Intermediate (4) Drug Isomer (2) Drug Metabolite (1) Dynamin (3) DYRK (1) E1/E2/E3 Enzyme (4) EGFR (25) Endogenous Metabolite (10) Enterovirus (1) Environmental Pollutants (4) Epigenetic Reader Domain (2) ERK (18) Estrogen Receptor/ERR (3) Eukaryotic Initiation Factor (eIF) (1) Factor Xa (1) Factor XI (1) FAK (1) FBPase (3) Ferroptosis (1) FGFR (3) Filovirus (1) FKBP (7) Flavivirus (1) FLT3 (1) Fructose-1,6-bisphosphate aldolase (1) Fungal (8) G protein-coupled Bile Acid Receptor 1 (1) GABA Receptor (18) Galectin (1) GLP Receptor (2) Glucosylceramide Synthase (GCS) (1) Glutaminase (8) Glutathione Peroxidase (3) Glutathione S-transferase (1) Glycosidase (1) GlyT (1) GnRH Receptor (1) Guanylate Cyclase (1) HCN Channel (1) HCV (5) HDAC (1) Heme Oxygenase (HO) (1) Hemoglobin (1) HIF/HIF Prolyl-Hydroxylase (2) Histamine Receptor (5) Histone Methyltransferase (10) HIV (12) HIV Integrase (7) HSP (5) HSV (1) IFNAR (8) IGF-1R (1) iGluR (7) IKK (5) Influenza Virus (2) Insecticide (2) Integrin (4) Interleukin Related (12) IRE1 (5) Isocitrate Dehydrogenase (IDH) (5) Isotope-Labeled Compounds (15) JAK (8) JNK (2) Kinesin (12) Ligands for Target Protein for PROTAC (1) LIM Kinase (LIMK) (2) Lipoxygenase (2) mAChR (10) MALT1 (7) MAP4K (1) MAPKAPK2 (MK2) (1) MDM-2/p53 (2) MEK (11) Melanocortin Receptor (6) Methionine Adenosyltransferase (MAT) (3) mGluR (20) MicroRNA (1) Microtubule/Tubulin (2) Mitochondrial Metabolism (3) Mitophagy (1) Mitosis (2) Molecular Glues (1) Monoamine Transporter (1) mTOR (11) MyD88 (1) Myosin (3) Na+/K+ ATPase (4) nAChR (6) Necroptosis (1) NEKs (1) NF-κB (3) NO Synthase (3) NOD-like Receptor (NLR) (2) NTPDase (6) Nucleoside Antimetabolite/Analog (4) Opioid Receptor (2) Organoid (1) Ornithine decarboxylase (ODC) (1) P2X Receptor (3) p38 MAPK (7) p62 (1) p97 (6) PAK (3) PANK (1) Parasite (8) PARP (4) PD-1/PD-L1 (1) PDGFR (1) PDHK (3) PDI (3) Penicillin-binding protein (PBP) (2) PERK (1) Phosphatase (24) Phosphodiesterase (PDE) (3) Phosphoglycerate Dehydrogenase (PHGDH) (3) Phospholipase (2) PI3K (7) PI5P4K (1) PKA (1) PKC (2) Potassium Channel (5) PPAR (1) Prostaglandin Receptor (1) PROTACs (4) Protease Activated Receptor (PAR) (3) Proteasome (2) Protein Arginine Deiminase (2) Pyroptosis (1) Pyruvate Kinase (2) Raf (3) Ras (14) Reactive Oxygen Species (ROS) (8) Reference Standards (40) Reverse Transcriptase (3) RGS Protein (1) RIP kinase (1) ROR (1) RSV (1) RUNX (2) SARS-CoV (8) Ser/Thr Protease (1) Serotonin Transporter (2) SHP1 (1) SHP2 (32) Smo (1) Sodium Channel (3) SOS1 (2) STAT (5) STING (1) TGF-beta/Smad (1) TGF-β Receptor (2) TNF Receptor (2) Toll-like Receptor (TLR) (1) Topoisomerase (1) Trk Receptor (5) TRP Channel (2) TSH Receptor (2) VEGFR (1) Virus Protease (6) WDR5 (2) WNK Kinase (1) Wnt (4) YAP (2) β-catenin (4) β-glucuronidase (1)
By Research Areas:	Cancer (327) Cardiovascular Disease (32) Endocrinology (12) Infection (62) Inflammation/Immunology (82) Metabolic Disease (40) Neurological Disease (93)
Click Chemistry:	Azide (1) Alkynes (2)

555

Inhibitors & Agonists

Screening Libraries

Fluorescent Dyes

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12683

BPTES 60+ Cited Publications	Glutaminase	Cancer
BPTES is an allosteric and selective glutaminase inhibitor with an IC₅₀ of 0.16 μM.

HY-101068

TOFA 10+ Cited Publications RMI14514; MDL14514	Acetyl-CoA Carboxylase	Cancer
TOFA (RMI14514;MDL14514) is an allosteric inhibitor of acetyl-CoA carboxylase-α (ACCA ).

HY-15251

Reparixin 60+ Cited Publications Repertaxin; DF 1681Y	CXCR	Inflammation/Immunology Endocrinology Cancer
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC₅₀s of 1 and 100 nM, respectively.

HY-138630

AG-270 5+ Cited Publications	Methionine Adenosyltransferase (MAT)	Cancer
AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC₅₀ of 14 nM .

HY-12682

Glutaminase C-IN-1 10+ Cited Publications Compound 968	Glutaminase	Cancer
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts .

HY-A0005

Clofarabine 10+ Cited Publications	Nucleoside Antimetabolite/Analog Autophagy Apoptosis	Metabolic Disease Cancer
Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC₅₀=65 nM) by binding to the allosteric site on the regulatory subunit .

HY-104010

Asciminib 10+ Cited Publications ABL001	Bcr-Abl	Cancer
Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM .

HY-158102

Rinzimetostat 1 Publications Verification ORIC-944	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer.

HY-15713

NMS-873 15+ Cited Publications	p97	Cancer
NMS-873 is a potent, selective allosteric VCP/p97 inhibitor with an IC₅₀ value of 30 nM.

HY-Y1683

DL-Menthol Racementhol	Environmental Pollutants GABA Receptor	Infection Neurological Disease
DL-Menthol (Racementhol) is an orally active, GABA_aR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABA_AR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .

HY-100386

Ticlopidine 3 Publications Verification PCR 5332	NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively.

HY-103269

BAI1 10+ Cited Publications	Bcl-2 Family Apoptosis	Cancer
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death .

HY-116009

RMC-4550 10+ Cited Publications	SHP2 Phosphatase	Cancer
RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC₅₀ of 0.583 nM.

HY-13449

TAK-733 5+ Cited Publications	MEK	Cancer
TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC₅₀ of 3.2 nM.

HY-100519

NVS-PAK1-1 5 Publications Verification	PAK	Cancer
NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC₅₀ of 5 nM .

HY-142618

TNF-α-IN-6	TNF Receptor	Inflammation/Immunology
TNF-α-IN-6 (compound 12) is an orally effective allosteric inhibitor of TNFα (K_D = 6.8 nM). TNF-α-IN-6 has anti-inflammatory effects .

HY-12042

Pimasertib 5+ Cited Publications AS703026; MSC1936369B	MEK	Cancer
Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .

HY-104010A

Asciminib hydrochloride 10+ Cited Publications ABL001 hydrochloride	Bcr-Abl	Cancer
Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC₅₀ of 0.25 nM .

HY-148510

HKB99	Phosphatase Apoptosis Akt ERK Reactive Oxygen Species (ROS)	Cancer
HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 induces apoptosis. HKB99 inhibits the formation of invasive pseudopodia and inhibits migration. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC) .

HY-17537

APY29 10+ Cited Publications	IRE1	Cancer
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC₅₀ of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .

HY-112094

WNK-IN-11 4 Publications Verification	Ser/Thr Protease WNK Kinase	Others
WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor, with an IC₅₀ of 4 nM for WNK1.

HY-15252

Reparixin L-lysine salt 60+ Cited Publications Repertaxin L-lysine salt	CXCR	Inflammation/Immunology Endocrinology Cancer
Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.

HY-11007

GNF-2 3 Publications Verification	Bcr-Abl SARS-CoV	Cancer
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

HY-100524

LRE1 2 Publications Verification	Adenylate Cyclase	Cancer
LRE1 is a specific and allosteric inhibitor of soluble adenylyl cyclase.

HY-15857

CW-069 1 Publications Verification	Kinesin	Cancer
CW-069 is an allosteric inhibitor of microtubule motor protein HSET with an IC₅₀ of 75 μM.

HY-156659

NC1	Phosphatase ERK	Inflammation/Immunology
NC1 is a selective non-competitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a K_i value 4.3 μM. NC1 allosterically regulates LYP/PTPN22 activity by restricting WPD loop movement. NC1 inhibits LYP activity in lymphoid T cells and enhances T-cell receptor signaling. NC1 can be used for the research of autoimmune diseases .

HY-124805

MAL3-101	HSP	Cancer
MAL3-101 is a potent HSP70 allosteric inhibitor. MAL3-101 inhibits HSP70 ATPase activity by blocking Hsp40 co-chaperone interaction. MAL3-101 can be used for researching muscle invasive bladder cancer (MIBC) .

HY-115466

MLT-748 5 Publications Verification	MALT1	Inflammation/Immunology
MLT-748 is a potent, selective and allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC₅₀ of 5 nM .

HY-15599

SSR128129E 1 Publications Verification SSR	FGFR	Cancer
SSR128129E is an orally available and allosteric FGFR inhibitor with an IC₅₀ of 1.9 μM for FGFR1.

HY-143899

FBA-IN-1	Fructose-1,6-bisphosphate aldolase Fungal	Infection
FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC₈₀ of 1 μg/mL .

HY-100386R

Ticlopidine (Standard) PCR 5332 (Standard)	Reference Standards NTPDase Cytochrome P450	Cardiovascular Disease
Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-18296

AKT-IN-1 5 Publications Verification	Akt	Cancer
AKT-IN-1 is an allosteric AKT inhibitor with an IC₅₀ of 1.042 μM.

HY-114397

SHP394 1 Publications Verification	SHP2 Phosphatase	Cancer
SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC₅₀ of 23 nM .

HY-121879

SHP836 1 Publications Verification	SHP2 Phosphatase	Cancer
SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2 .

HY-145159

SHP2 protein degrader-1	SHP2 PROTACs Phosphatase Apoptosis	Cancer
SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for researching SHP2 related diseases .

HY-161431

RTx-152	DNA/RNA Synthesis	Cancer
RTx-152 traps Polθ on DNA and is an allosteric Polθ-pol inhibitor (IC₅₀: 6.2 nM). RTx-152 selectively kills HR-deficient cancer cells, and suppresses PARP inhibitor resistance in multiple genetic backgrounds, including homologous recombination (HR)-proficient cells. RTx-152 selectively kills BRCA2-null cells .

HY-158102A

Rinzimetostat TFA 1 Publications Verification ORIC-944 TFA	Histone Methyltransferase	Cancer
Rinzimetostat (ORIC-944) TFA is the TFA salt form of ORIC (HY-158102). Rinzimetostat TFA is a selective, orally active, allosteric inhibitor targeting the EED subunit of polycomb repressive complex 2 (PRC2). Rinzimetostat TFA is synergistic with androgen receptor pathway inhibitors (ARPIs) for the study of metastatic prostate cancer .

HY-174802

XL-3158	Cyclic GMP-AMP Synthase IKK IFNAR	Neurological Disease Inflammation/Immunology Cancer
XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC₅₀: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS). XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases.

HY-156466

QL-1200186	STAT Interleukin Related IFNAR	Inflammation/Immunology
QL-1200186 is a selective, orally active, allosteric inhibitor targeting the tyrosine kinase TYK2 pseudokinase domain JH2 (IC₅₀=0.06 nM, TYK2 JH2), with 164-fold selectivity over TYK1 JH2 (IC₅₀=9.85 nM，TYK1 JH2). QL-1200186 first stabilizes the TYK2 JH2 conformation, inhibits the activity of the JH1 catalytic domain, and blocks the IFNα, IL-12/IL-23-mediated JAK-STAT signaling pathway. QL-1200186 can inhibit the production of Th1/Th17 cell-related cytokines (such as IFNγ, IL-23), reduce immune cell activation, and has no significant effect on JAK1/2/3 kinase activity. QL-1200186 can significantly improve skin inflammation in the Imiquimod (HY-B0180)-induced psoriasis mouse model and reduce the Psoriasis Area and Severity Index (PASI) score. QL-1200186 can be used in the study of autoimmune diseases such as psoriasis and systemic lupus erythematosus (SLE) .

HY-110031

BAI1 hydrochloride 10+ Cited Publications	Apoptosis Bcl-2 Family	Cancer
BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases .

HY-12446

K-Ras(G12C) inhibitor 9	Ras	Cancer
K-Ras (G12C) inhibitor 9 is an allosteric inhibitor of the K-Ras (G12C) .

HY-126300

SGC6870 1 Publications Verification	Histone Methyltransferase	Cancer
SGC6870, a chemical probe, is a potent, selective and cytoactive allosteric inhibitor of PRMT6 with IC₅₀ of 77 nM .

HY-161288

UKTT15	PARP	Cancer
UKTT15 (compound 6) is an allosteric inhibitor of PARP1 .

HY-172911

SHP2-IN-37	SHP2	Cancer
SHP2-IN-37 (compound C5) is a potent and selective SHP2 allosteric inhibitor with an IC₅₀ of 0.023 μM. SHP2-IN-37 exhibits antiproliferative effect on KYSE-520 and MV-411 cells with IC₅₀s of 6.97 and 0.67 μM, respectively

HY-124587

MLT-747	MALT1	Inflammation/Immunology
MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC₅₀ of 14 nM .

HY-179428

JAK2-IN-17	JAK	Cancer
JAK2-IN-17 (compound 20) is a potent JAK2 allosteric inhibitor. JAK2-IN-17 inhibits full-length JAK2 and JAK2 V617F with IC₅₀s of 160 and 130 nM, respectively. JAK2-IN-17 covalently modifies Lys677 in the pseudokinase domain .

HY-161363

ERK2 allosteric-IN-1	ERK	Metabolic Disease Cancer
ERK2 allosteric-IN-1 (compound 1) is a selective and allosteric ERK2 inhibitor with the IC₅₀ of 11 μM .

HY-158369

CK2-IN-10	Casein Kinase	Cancer
CK2-IN-10 (31), an allosteric CK2 inhibitor, can be used in the research of cancer .

HY-121094

Androgen receptor allosteric antagonist 1	Estrogen Receptor/ERR	Cancer
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the K_i of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .

HY-147653

*Integrase-LEDGF/p75 allosteric* inhibitor 1**	HIV Integrase	Infection
Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC₅₀ of 3.9 nM against HIV-1 recombinant molecular clone NL432 .

Cat. No.	Product Name

HY-L943

MCE‑18 Novelty drug‑like Library

37030 compounds

MCE-18 stands for Medicinal Chemistry Evolution 2018, which was first published in Journal of Medicinal Chemistry in 2019 for assessing molecular novelty and three-dimensional complexity. Developed based on Clarivate global pharmaceutical patent database, this descriptor was constructed via big-data analysis covering 28,161 patented lead compounds, 1,370 approved drugs and nearly 30,000 preclinical-to-phase III drug candidates from 23 top pharmaceutical companies worldwide between 1950 and 2018, followed by structural clustering and removal of redundant outdated scaffolds for data denoising. Its scoring system integrates five core structural features including aromatic ring (AR), aliphatic heterocycle (NAR), chiral center (CHIRAL), spiro atom (SPIRO), cyclic and acyclic sp³ carbon ratio together with a quadratic topological correction factor. Breaking the limitations of the single Fsp³ parameter, MCE-18 effectively distinguishes conventional flat aromatic scaffolds from modern 3D-enriched novel chemotypes, overcoming typical drawbacks of traditional compound libraries such as scaffold redundancy, low screening hit rates and poor compatibility with allosteric and PPI-related difficult targets.

This library contains over 37,000 structurally diverse compounds with favorable overall drug-likeness, suitable for high-throughput screening against canonical targets including kinases, GPCRs and proteases as well as challenging allosteric and PPI targets. Compounds comply with the developmental trend of modern novel drug discovery, supporting routine primary screening as well as early hit identification of allosteric modulators and PPI inhibitors, serving as an efficient screening resource for early-stage innovative drug discovery.

Cat. No.	Product Name	Type

HY-10219G

Rapamycin

Sirolimus; AY-22989; NSC 226080

Fluorescent Dyes

Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-10219GL

Rapamycin (GMP Like)

Sirolimus (GMP Like); AY-22989 (GMP Like); NSC 226080 (GMP Like)

Fluorescent Dyes

Rapamycin (Sirolimus) GMP Like is Rapamycin (HY-10219) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-141520G

ART558

Fluorescent Dyes

ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

Cat. No.	Product Name	Type

HY-10219G

Rapamycin

Sirolimus; AY-22989; NSC 226080

Biochemical Assay Reagents

HY-10219GL

Rapamycin (GMP Like)

Sirolimus (GMP Like); AY-22989 (GMP Like); NSC 226080 (GMP Like)

Biochemical Assay Reagents

HY-141520G

ART558

Biochemical Assay Reagents

Cat. No.	Product Name	Target	Research Area

HY-W096171

D-Dopa 3-Hydroxy-D-tyrosine	Carboxypeptidase	Infection Neurological Disease
D-Dopa (3-Hydroxy-D-tyrosine) is a potent, orally active, non-competitive and allosteric inhibitor of glutamate carboxypeptidase II (GCPII) with an IC₅₀ of 200 nM. D-Dopa elevates brain dopamine and produce turning behavior in rats. D-Dopa inhibit severe fever with thrombocytopenia syndrome (SFTS) virus infection. D-Dopa can be used for neurological disease and virus infection research .

HY-107663A

MIF-1 TFA Pro-Leu-Gly-NH2 TFA; Melanostatin TFA	Dopamine Receptor	Neurological Disease
MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-P5542

Vicatertide SB-01; Peniel 2000	Factor Xa TGF-beta/Smad	Inflammation/Immunology
Vicatertide (SB-01, Peniel 2000) is a polypeptide with both competitive inhibitory activity against TGF-β1 and selective inhibitory activity against human factor XIa (hFXIa, with a K_a of 80 nM for hFXIa). Vicatertide binds allosterically to the two binding sites of dimeric hFXI/hFXIa, while directly binding to activated TGF-β1, selectively blocking the Smad1/5/8 pathway and maintaining low-level activation of the Smad2 pathway to enhance the synthesis of type Ⅱ collagen and aggrecan. Vicatertide inhibits thrombus formation in arteriovenous thrombosis models, and also reduces thrombus weight and thrombus incidence in mouse lung cancer models. Vicatertide can be used for research on degenerative disc disease and thrombosis-related diseases .

HY-P10948A

CS-VIP 8 hydrochloride	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 hydrochloride is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 hydrochloride induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 hydrochloride is promising for research of hematological diseases such as leukemia .

HY-P1259A

PR-39 TFA	Proteasome Bacterial	Inflammation/Immunology
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P1073

ProTx-I	Calcium Channel Potassium Channel Sodium Channel TRP Channel	Neurological Disease Cancer
ProTx-I is a toxin derived from Thrixopelma pruriens and a peptide inhibitor targeting TTX-resistant sodium channels. ProTx-I interacts with voltage sensors of multiple domains such as NaV1.7, reduces neuronal excitability through allosteric modulation of channel gating and alteration of voltage dependence. The IC₅₀ values of ProTx-I against human NaV1.7, NaV1.2, NaV1.6, and NaV1.5 are 95 nM, 104 nM, 21 nM, and 358 nM, respectively; ProTx-I also potently inhibits Ba ²⁺ currents of hCav3.1, while its inhibitory potency against hCav3.2 is approximately 160-fold lower. ProTx-I is applicable to the research of chronic pain .

HY-P10436

Braftide	Raf	Cancer
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF ^G469A with IC₅₀ of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC₅₀ is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .

HY-107663

MIF-1 Pro-Leu-Gly-NH2; Melanostatin	Dopamine Receptor	Neurological Disease
MIF-1 (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 inhibits melanin formation. MIF-1 blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB) .

HY-P4160

PDC31 THG113.31; ILGHXDYK	Prostaglandin Receptor	Endocrinology
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca ²⁺-dependent large-conductance K ⁺-channel in human myometrial cells .

HY-P1402

[Glu27]-PKC (19-36)	PKC	Others
[Glu27]-PKC (19-36) is an inactive control for protein kinase C (PKC) (19-36). PKC (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C, it may be responsible for maintaining the enzyme in the inactive form in the absence of allosteric activators such as phospholipids .

HY-P1259

PR-39	Proteasome Bacterial	Inflammation/Immunology
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .

HY-P10948

CS-VIP 8	WDR5 Histone Methyltransferase	Cardiovascular Disease
CS-VIP 8 is a selective allosteric WDR5 protein inhibitor (K_i= 0.008 μM). CS-VIP 8 induces conformational changes in the MLL1 complex, leading to the dissociation of MLL1 from the complex, inhibiting MLL1 histone methyltransferase activity and regulating HOX gene expression. CS-VIP 8 is promising for research of hematological diseases such as leukemia .

HY-P11553

ECL1i	CCR	Inflammation/Immunology
ECL1i is an allosteric, selective CCR2 inhibitor. ECL1i specifically inhibits CCL2-/CCR2-mediated chemotaxis. ECL1i interferes with CCR2-positive cell recruitment and attenuates disease progression in experimental autoimmune encephalomyelitis .

HY-P11553A

ECL1i TFA	CCR	Infection Inflammation/Immunology
ECL1i TFA is an allosteric, selective CCR2 inhibitor. ECL1i TFA specifically inhibits CCL2-/CCR2-mediated chemotaxis. ECL1i TFA interferes with CCR2-positive cell recruitment and attenuates disease progression in experimental autoimmune encephalomyelitis .

HY-P1045

187-1, N-WASP inhibitor 1 Publications Verification	Arp2/3 Complex	Others
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .

HY-P10010

DB21, Galectin-1 Antagonist	Galectin	Cancer
DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models .

HY-P1045A

187-1, N-WASP inhibitor TFA	Arp2/3 Complex	Others
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC₅₀ of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-10219

Rapamycin Maximum Cited Publications 1338 Publications Verification Sirolimus; AY-22989; NSC 226080	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Classification of Application Fields Antibiotics Anti-aging Disease Research Disease Research Fields Source Classification Cancer	mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial
Rapamycin (Sirolimus; AY 22989) is a potent and specific blood-brain barrier-transmissible mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-15310

Ivermectin 45+ Cited Publications MK-933; CD-5024; K-237	Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Antiviral Anti-parasitic Disease Research Disease Research Fields Source Classification Cancer	Environmental Pollutants Antibiotic Mitophagy Bacterial Parasite Autophagy Flavivirus HSV HIV SARS-CoV Dengue Virus
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X₄ and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import . Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19 .

HY-112942A

CMP-Sialic acid sodium salt 4 Publications Verification CMP-Neu5Ac sodium salt	Natural Products Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
CMP-Sialic acid (CMP-Neu5Ac) sodium salt is an allosteric inhibitor of UDP-GlcNAc 2-epimerase. CMP-Sialic acid sodium salt provides a substrate for Golgi sialyltransferases. CMP-Sialic acid sodium salt is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates .

HY-Y1683

DL-Menthol Racementhol	Structural Classification Natural Products Classification of Application Fields Leguminosae Labiatae Other Diseases Erythrina poeppigiana Plants Glycyrrhiza uralensis Fisch. Disease Research Fields Source Classification	Environmental Pollutants GABA Receptor
DL-Menthol (Racementhol) is an orally active, GABA_aR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABA_AR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .

HY-N0240

Herbacetin 5 Publications Verification	Flavonols Structural Classification Flavonoids Linum usitatissimum Linn. Classification of Application Fields Linaceae Phenols Polyphenols Plants Disease Research Fields Source Classification Cancer	Ornithine decarboxylase (ODC)
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

HY-A0009

Galanthamine hydrobromide 10+ Cited Publications Galantamine hydrobromide	Alkaloids Other Alkaloids Plants Amaryllidaceae	Cholinesterase (ChE) nAChR
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-12545

Brevetoxin-3 1 Publications Verification PbTx-3	Natural Products other families Classification of Application Fields Plants Inflammation/Immunology Disease Research Fields Source Classification	Sodium Channel
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na ⁺ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain) . Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na ⁺ channels, inhibits the inactivation of Na ⁺ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation .

HY-112942

CMP-Sialic acid CMP-Neu5Ac	Natural Products Human Gut Microbiota Metabolites Classification of Application Fields Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
CMP-Sialic acid (CMP-Neu5Ac) is an allosteric inhibitor of UDP-GlcNAc 2-epimerase. CMP-Sialic acid provides a substrate for Golgi sialyltransferases. CMP-Sialic acid is an important sugar nucleotide for biosynthesis of sialic acid and its conjugates .

HY-10219R

Rapamycin (Standard) Sirolimus (Standard); AY-22989 (Standard); NSC 226080 (Standard)	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Antibiotics Disease Research Endogenous metabolite Source Classification	Reference Standards mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial
Rapamycin (Standard) is the analytical standard of Rapamycin (HY-10219). This product is intended for research and analytical applications. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-156193

PF-07208254	Cardiovascular Disease Classification of Application Fields Ketones, Aldehydes, Acids Endogenous metabolite Disease Research Fields Source Classification	PDHK
PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase (BDK) (IC₅₀=110 nM, K_i=54 nM, K_D=84 nM). PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids (BCAAs) and branched-chain keto acids (BCKAs) by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells (IC₅₀=540 nM) and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases (e.g., heart failure, type 2 diabetes) .

HY-113604

Pentabromopseudilin	Natural Products Marine natural products Marine microorganism Source Classification	TGF-β Receptor
Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer .

HY-A0009R

Galanthamine hydrobromide (Standard) Galantamine hydrobromide (Standard)	Structural Classification Alkaloids Other Alkaloids Plants Amaryllidaceae Source Classification	nAChR Cholinesterase (ChE) Reference Standards
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α₃β₄, α₄β₂, α₆β₄ nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-N3755R

Dihydroresveratrol (Standard)	Structural Classification Human Gut Microbiota Metabolites Phenols Polyphenols Plants Endogenous metabolite Dioscorea bulbifera Linn. Dioscoreaceae Source Classification	Reference Standards Estrogen Receptor/ERR
Clofarabine (Standard) is the analytical standard of Clofarabine. This product is intended for research and analytical applications. Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit .

HY-N0240R

Herbacetin (Standard)	Flavonols Structural Classification Flavonoids Linum usitatissimum Linn. Linaceae Phenols Polyphenols Plants Source Classification	Reference Standards Others
Herbacetin (Standard) is the analytical standard of Herbacetin. This product is intended for research and analytical applications. Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .

HY-W097625R

6-Methoxyflavone (Standard)	Structural Classification Flavonoids Flavones Thymelaeaceae Plants Pimelea simplex F.Muell. Source Classification	Toll-like Receptor (TLR) MyD88 p38 MAPK NF-κB Heme Oxygenase (HO) Reference Standards PERK
6-Methoxyflavone (Standard) is the analytical standard of 6-Methoxyflavone (HY-W097625). This product is intended for research and analytical applications. 6-Methoxyflavone is an orally active methoxyflavone. 6-Methoxyflavone suppresses neuroinflammation in microglia through the inhibition of TLR4/MyD88/p38 MAPK/NF-κB dependent pathways and the activation of HO-1/NQO-1 signaling. 6-Methoxyflavone induces S-phase arrest through the CCNA2/CDK2/p21CIP1 signaling pathway and activates the PERK/EIF2a/ATF4/CHOP pathway in HeLa cells. 6-Methoxyflavone acts as a Flumazenil (HY-B0009)-insensitive positive allosteric modulator at human recombinant α1β2γ2L and α2β2γ2L GABAα receptors. 6-Methoxyflavone inhibits NFAT Translocation into the nucleus and suppresses T cell activation. 6-Methoxyflavone partially restores chronic ethanol-induced behavioral deficits in mice. 6-Methoxyflavone antagonizes chronic constriction injury and diabetes associated neuropathic nociception expression. 6-Methoxyflavone can be used for the study of cancer, inflammation and neurological diseases .

Cat. No.	Product Name	Chemical Structure

HY-117287

Deucravacitinib

30+ Cited Publications

Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC₅₀ of 0.2 nM and a K_i of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation . Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus .

HY-10219S

Rapamycin-d3 1 Publications Verification
Rapamycin-d₃ is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant .

HY-153701S

Envudeucitinibum

Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases .

HY-10219S1

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

HY-139289S

ART899
ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone .

HY-10046S

Plerixafor-d4
Plerixafor-d₄ is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM .

HY-114169S

WRG-28-d5
WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC₅₀ of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic

HY-W725476

Bifenazate-d5
Bifenazate-d₅ is the deuterium labeled Bifenazate (HY-119687). Bifenazate is a carbazate acaricide that control 100% of mites at a concentration of 25 ppm . Bifenazate is a positive allosteric modulator of GABA receptor . Bifenazate is the inhibitor for the mitochondrial electron transport chain complex III .

HY-10250S1

Triciribine phosphate-d3

Triciribine phosphate-d3 (TCN-P-d3) is a deuterated compound of Triciribine phosphate (TCN-P). TCN-P inhibits adenosine monophosphate (AMP)-activated protein kinase through an allosteric mechanism, affecting the first key step in de novo purine biosynthesis. Triciribine phosphate also inhibits inosine monophosphate dehydrogenase, which is the first key step in guanosine nucleotide synthesis. Triciribine phosphate does not affect ligase activity .

HY-W765245

Rapamycin-13C,d3-1
Rapamycin- ¹³C,d₃-1 (Sirolimus- ¹³C,d₃-1) is the deuterium labeled and ¹³C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-B0520AS1

Benztropine-d3 mesylate

Benztropine-d₃ (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-100386S

Ticlopidine-d4

Ticlopidine-d₄ is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-B0520AS

Benztropine-13C,d3 mesylate

Benztropine- ¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .

HY-B0153AS

Ticlopidine-d4 hydrochloride

Ticlopidine-d₄ hydrochloride is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-W707554

Ticlopidine hydrochloride-d6

Ticlopidine hydrochloride-d₆ is the deuterium labeled Ticlopidine hydrochloride (HY-B0153A). Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-A0009S

Galanthamine-d3 hydrobromide

Galanthamine-d₃ (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC₅₀ of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .

HY-B1456AS

Fenoprofen-13C6 sodium hydrate

Fenoprofen- ¹³C₆ (LILLY-53858- ¹³C₆) sodium hydrate is the ¹³C labeled Fenoprofen (HY-B1456A).Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis .

HY-166530S

Ticlopidine-d6 hydrochloride

Ticlopidine-d₆ hydrochloride is the deuterium labeled Ticlopidine hydrochloride. Ticlopidine (PCR 5332) hydrochloride, an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC₅₀ of 81.7 μM. Ticlopidine hydrochloride blocks several NTPDase isoenzymes with IC₅₀s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively . Ticlopidine hydrochloride is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine hydrochloride inhibits CYP2C9 and CYP3A4 with IC₅₀s of 26.0 and 32.3 μM, respectively .

HY-166594S

Deucravacitinib-13C,d3

Deucravacitinib- ¹³C,d₃ is the ¹³C- and deuterium labeled Deucravacitinib. 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 .

Cat. No.	Product Name		Classification

HY-16062

ARQ 621		Alkynes
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity . ARQ 621 is a kinesin inhibitor . ARQ 621 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-151829

Fmoc-L-Asn(EDA-N3)-OH		Azide
Fmoc-L-Asn(EDA-N3)-OH is a click chemistry reagent containing an azide group. This building block is reported in literature for the modification of Amanitin via Click Chemistry. Alpha-Amanitin is the deadliest member of the amatoxin peptide family produced by the death-cap mushroom A. phalloides. It is an orally available, rigid, bicyclic octapeptide and one of the most lethal known natural products (LD50 = 50-100 μg/kg) acting as highly selective allosteric inhibitor of the RNA polymerase II . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.

HY-168152

SARS-CoV-2 3CLpro-IN-26		Alkynes
SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC₅₀ of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10219G

Rapamycin Sirolimus; AY-22989; NSC 226080	mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Bacterial	Infection Cancer
Rapamycin (Sirolimus) (GMP) is Rapamycin (HY-10219) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC₅₀ of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1 . Rapamycin is an autophagy activator, an immunosuppressant .

HY-141520G

ART558	DNA/RNA Synthesis	Cancer
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC₅₀=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .

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