Search Result

Targets Recommended:	Oct3/4 PI4K MAP4K GSK-3 PI3K FLT3 Arp2/3 Complex Na+/HCO3- Cotransporter MAP3K Ligand for E3 Ligase Indoleamine 2,3-Dioxygenase (IDO) E3 Ligase Ligand-Linker Conjugate Progesterone Receptor FXR E1/E2/E3 Enzyme Serotonin Transporter PIKfyve TAM Receptor Dopamine Transporter ATM/ATR

Results for "Ang (3-4) Inhibitors" in MCE Product Catalog:

By Targets:	Arp2/3 Complex (9) ATM/ATR (19) Dopamine Transporter (15) E1/E2/E3 Enzyme (51) E3 Ligase Ligand-Linker Conjugate (2) FLT3 (59) FXR (4) GSK-3 (43) Indoleamine 2,3-Dioxygenase (IDO) (30) Ligand for E3 Ligase (8) MAP3K (13) MAP4K (8) Na+/HCO3- Cotransporter (1) Oct3/4 (2) PI3K (125) PI4K (12) PIKfyve (5) Progesterone Receptor (3) Serotonin Transporter (41) TAM Receptor (20) 15-PGDH (1) 5 alpha Reductase (7) 5-HT Receptor (49) Acetyl-CoA Carboxylase (9) AChE (85) Ack1 (1) Acyltransferase (37) ADC Cytotoxin (49) ADC Linker (3) Adenosine Deaminase (7) Adenosine Kinase (2) Adenosine Receptor (11) Adenylate Cyclase (10) Adrenergic Receptor (40) Akt (66) Aldehyde Dehydrogenase (ALDH) (11) Aldose Reductase (16) ALK (29) Aminoacyl-tRNA Synthetase (10) Aminopeptidase (10) AMPK (27) Amyloid-β (24) Androgen Receptor (11) Angiotensin Receptor (21) Angiotensin-converting Enzyme (ACE) (47) Antibiotic (268) Antifolate (22) APC (3) Apoptosis (865) Arenavirus (4) Arginase (7) Aromatase (11) Aryl Hydrocarbon Receptor (12) ATGL (1) ATP Citrate Lyase (8) ATP Synthase (9) Aurora Kinase (40) Autophagy (655) Bacterial (464) Bcl-2 Family (54) Bcr-Abl (43) BCRP (11) Beta-secretase (18) BMX Kinase (3) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (40) c-Fms (22) c-Kit (49) c-Met/HGFR (50) c-Myc (12) Calcium Channel (74) CaMK (22) Cannabinoid Receptor (14) Carbonic Anhydrase (17) Carboxypeptidase (4) Casein Kinase (35) Caspase (37) CaSR (1) Cathepsin (31) CCR (21) CD73 (7) CDK (151) CETP (6) CFTR (6) CGRP Receptor (3) Checkpoint Kinase (Chk) (22) Chloride Channel (12) Cholecystokinin Receptor (6) CMV (18) Complement System (15) COMT (12) COX (173) CRAC Channel (10) CRFR (3) CRISPR/Cas9 (5) CRM1 (2) CXCR (23) Cytochrome P450 (88) DAPK (1) Deubiquitinase (37) Dihydroorotate Dehydrogenase (11) Dipeptidyl Peptidase (35) Discoidin Domain Receptor (9) DNA Alkylator/Crosslinker (10) DNA Methyltransferase (21) DNA-PK (20) DNA/RNA Synthesis (142) Dopamine Receptor (36) Dopamine β-hydroxylase (6) Drug Metabolite (61) Drug-Linker Conjugates for ADC (30) Dynamin (6) DYRK (17) EAAT2 (3) EGFR (139) Elastase (16) Endogenous Metabolite (220) Endothelin Receptor (15) Enolase (1) Enterovirus (13) Ephrin Receptor (5) Epigenetic Reader Domain (110) Epoxide Hydrolase (12) ERK (54) Estrogen Receptor/ERR (33) Eukaryotic Initiation Factor (eIF) (19) FAAH (19) FABP (3) Factor Xa (10) FAK (21) Farnesyl Transferase (20) Fatty Acid Synthase (FASN) (23) Ferroptosis (65) FGFR (60) Filovirus (4) FKBP (7) FLAP (7) Fungal (120) G-quadruplex (4) GABA Receptor (23) Galectin (3) Gap Junction Protein (6) GHSR (3) Gli (3) Glucagon Receptor (3) Glucocorticoid Receptor (9) Glucosidase (27) GLUT (9) Glutaminase (9) Glutathione Peroxidase (10) GlyT (8) GPCR19 (2) GPR120 (1) GPR40 (2) GPR55 (1) GSNOR (1) Guanylate Cyclase (4) Gutathione S-transferase (9) Haspin Kinase (3) HBV (28) HCN Channel (2) HCV (83) HCV Protease (15) HDAC (99) Hedgehog (12) Hexokinase (4) HIF/HIF Prolyl-Hydroxylase (40) Hippo (MST) (3) Histamine Receptor (34) Histone Acetyltransferase (35) Histone Demethylase (39) Histone Methyltransferase (93) HIV (194) HIV Integrase (18) HIV Protease (25) HMG-CoA Reductase (HMGCR) (37) HSP (47) HSV (39) IAP (9) IFNAR (4) IGF-1R (21) iGluR (20) IKK (32) Imidazoline Receptor (4) Influenza Virus (100) Insulin Receptor (12) Integrin (36) Interleukin Related (50) IRAK (16) IRE1 (16) Isocitrate Dehydrogenase (IDH) (15) Itk (5) JAK (78) JNK (31) Keap1-Nrf2 (22) Kinesin (17) KLF (4) Lactate Dehydrogenase (11) Leukotriene Receptor (21) Ligand for Target Protein for PROTAC (19) LIM Kinase (LIMK) (5) Lipoxygenase (39) LPL Receptor (11) LRRK2 (15) LXR (3) mAChR (32) MAGL (16) MALT1 (4) MAPKAPK2 (MK2) (4) MCHR1 (GPR24) (3) MDM-2/p53 (44) MEK (35) Melanocortin Receptor (5) Melatonin Receptor (3) MELK (3) mGluR (11) MicroRNA (7) Microtubule/Tubulin (87) Mineralocorticoid Receptor (2) Mitochondrial Metabolism (39) Mitophagy (53) Mixed Lineage Kinase (4) MMP (59) MNK (5) Monoamine Oxidase (62) Monoamine Transporter (11) Monocarboxylate Transporter (7) Mps1 (10) mTOR (70) MyD88 (4) Myosin (13) Na+/Ca2+ Exchanger (10) Na+/K+ ATPase (16) nAChR (15) NADPH Oxidase (11) Nampt (11) NEDD8-activating Enzyme (6) Neprilysin (14) Neurokinin Receptor (3) Neuropeptide Y Receptor (10) Neurotensin Receptor (2) NF-κB (141) NKCC (6) NO Synthase (43) NOD-like Receptor (NLR) (15) Notch (22) Nucleoside Antimetabolite/Analog (37) Opioid Receptor (9) Orexin Receptor (OX Receptor) (2) Oxytocin Receptor (1) P-glycoprotein (39) P2X Receptor (13) P2Y Receptor (12) p38 MAPK (60) p97 (7) PAI-1 (8) PAK (12) Parasite (145) PARP (50) PD-1/PD-L1 (13) PDGFR (72) PDHK (9) PDK-1 (6) PERK (4) PGC-1α (1) PGE synthase (12) Phosphatase (99) Phosphodiesterase (PDE) (143) Phospholipase (43) Pim (18) PKA (33) PKC (72) PKD (4) Polo-like Kinase (PLK) (22) Porcupine (8) Potassium Channel (87) PPAR (27) Procollagen C Proteinase (1) Prostaglandin Receptor (31) PROTAC (19) PROTAC Linker (16) Protease-Activated Receptor (PAR) (9) Proteasome (43) Protein Arginine Deiminase (4) Proton Pump (36) PTEN (5) Pyk2 (4) Pyruvate Kinase (2) RAD51 (5) Raf (44) RAR/RXR (11) Ras (61) Reactive Oxygen Species (71) Renin (3) RET (20) Reverse Transcriptase (49) RGS Protein (3) Ribosomal S6 Kinase (RSK) (21) RIP kinase (28) ROCK (38) ROR (9) ROS (8) RSV (14) Salt-inducible Kinase (SIK) (6) SARS-CoV (62) Ser/Thr Protease (19) sFRP-1 (1) SGK (7) SGLT (18) Sigma Receptor (6) Sirtuin (29) Smo (10) SNIPER (8) Sodium Channel (73) Somatostatin Receptor (8) SPHK (9) Src (63) SRPK (3) STAT (62) Stearoyl-CoA Desaturase (SCD) (10) STING (6) Survivin (3) Syk (23) Telomerase (8) TGF-beta/Smad (12) TGF-β Receptor (35) Thrombin (21) Thymidylate Synthase (7) Thyroid Hormone Receptor (5) TNF Receptor (37) Toll-like Receptor (TLR) (28) TOPK (6) Topoisomerase (91) Trk Receptor (19) TRP Channel (37) Tryptophan Hydroxylase (8) TSH Receptor (1) Tyrosinase (36) ULK (4) URAT1 (4) Urotensin Receptor (1) Vasopressin Receptor (2) VD/VDR (5) VDAC (2) VEGFR (123) Virus Protease (33) Wee1 (4) Wnt (36) Xanthine Oxidase (11) YAP (9) β-catenin (16) γ-secretase (21)
By Research Areas:	Cancer (4068) Cardiovascular Disease (620) Endocrinology (230) Infection (1097) Inflammation/Immunology (1378) Metabolic Disease (709) Neurological Disease (947)

By Targets:

Arp2/3 Complex (9)

ATM/ATR (19)

Dopamine Transporter (15)

E1/E2/E3 Enzyme (51)

E3 Ligase Ligand-Linker Conjugate (2)

FLT3 (59)

FXR (4)

GSK-3 (43)

Indoleamine 2,3-Dioxygenase (IDO) (30)

Ligand for E3 Ligase (8)

MAP3K (13)

MAP4K (8)

Na+/HCO3- Cotransporter (1)

Oct3/4 (2)

PI3K (125)

PI4K (12)

PIKfyve (5)

Progesterone Receptor (3)

Serotonin Transporter (41)

TAM Receptor (20)

15-PGDH (1)

5 alpha Reductase (7)

5-HT Receptor (49)

Acetyl-CoA Carboxylase (9)

AChE (85)

Ack1 (1)

Acyltransferase (37)

ADC Cytotoxin (49)

ADC Linker (3)

Adenosine Deaminase (7)

Adenosine Kinase (2)

Adenosine Receptor (11)

Adenylate Cyclase (10)

Adrenergic Receptor (40)

Akt (66)

Aldehyde Dehydrogenase (ALDH) (11)

Aldose Reductase (16)

ALK (29)

Aminoacyl-tRNA Synthetase (10)

Aminopeptidase (10)

AMPK (27)

Amyloid-β (24)

Androgen Receptor (11)

Angiotensin Receptor (21)

Angiotensin-converting Enzyme (ACE) (47)

Antibiotic (268)

Antifolate (22)

APC (3)

Apoptosis (865)

Arenavirus (4)

Arginase (7)

Aromatase (11)

Aryl Hydrocarbon Receptor (12)

ATGL (1)

ATP Citrate Lyase (8)

ATP Synthase (9)

Aurora Kinase (40)

Autophagy (655)

Bacterial (464)

Bcl-2 Family (54)

Bcr-Abl (43)

BCRP (11)

Beta-secretase (18)

BMX Kinase (3)

Bombesin Receptor (1)

Bradykinin Receptor (1)

Btk (40)

c-Fms (22)

c-Kit (49)

c-Met/HGFR (50)

c-Myc (12)

Calcium Channel (74)

CaMK (22)

Cannabinoid Receptor (14)

Carbonic Anhydrase (17)

Carboxypeptidase (4)

Casein Kinase (35)

Caspase (37)

CaSR (1)

Cathepsin (31)

CCR (21)

CD73 (7)

CDK (151)

CETP (6)

CFTR (6)

CGRP Receptor (3)

Checkpoint Kinase (Chk) (22)

Chloride Channel (12)

Cholecystokinin Receptor (6)

CMV (18)

Complement System (15)

COMT (12)

COX (173)

CRAC Channel (10)

CRFR (3)

CRISPR/Cas9 (5)

CRM1 (2)

CXCR (23)

Cytochrome P450 (88)

DAPK (1)

Deubiquitinase (37)

Dihydroorotate Dehydrogenase (11)

Dipeptidyl Peptidase (35)

Discoidin Domain Receptor (9)

DNA Alkylator/Crosslinker (10)

DNA Methyltransferase (21)

DNA-PK (20)

DNA/RNA Synthesis (142)

Dopamine Receptor (36)

Dopamine β-hydroxylase (6)

Drug Metabolite (61)

Drug-Linker Conjugates for ADC (30)

Dynamin (6)

DYRK (17)

EAAT2 (3)

EGFR (139)

Elastase (16)

Endogenous Metabolite (220)

Endothelin Receptor (15)

Enolase (1)

Enterovirus (13)

Ephrin Receptor (5)

Epigenetic Reader Domain (110)

Epoxide Hydrolase (12)

ERK (54)

Estrogen Receptor/ERR (33)

Eukaryotic Initiation Factor (eIF) (19)

FAAH (19)

FABP (3)

Factor Xa (10)

FAK (21)

Farnesyl Transferase (20)

Fatty Acid Synthase (FASN) (23)

Ferroptosis (65)

FGFR (60)

Filovirus (4)

FKBP (7)

FLAP (7)

Fungal (120)

G-quadruplex (4)

GABA Receptor (23)

Galectin (3)

Gap Junction Protein (6)

GHSR (3)

Gli (3)

Glucagon Receptor (3)

Glucocorticoid Receptor (9)

Glucosidase (27)

GLUT (9)

Glutaminase (9)

Glutathione Peroxidase (10)

GlyT (8)

GPCR19 (2)

GPR120 (1)

GPR40 (2)

GPR55 (1)

GSNOR (1)

Guanylate Cyclase (4)

Gutathione S-transferase (9)

Haspin Kinase (3)

HBV (28)

HCN Channel (2)

HCV (83)

HCV Protease (15)

HDAC (99)

Hedgehog (12)

Hexokinase (4)

HIF/HIF Prolyl-Hydroxylase (40)

Hippo (MST) (3)

Histamine Receptor (34)

Histone Acetyltransferase (35)

Histone Demethylase (39)

Histone Methyltransferase (93)

HIV (194)

HIV Integrase (18)

HIV Protease (25)

HMG-CoA Reductase (HMGCR) (37)

HSP (47)

HSV (39)

IAP (9)

IFNAR (4)

IGF-1R (21)

iGluR (20)

IKK (32)

Imidazoline Receptor (4)

Influenza Virus (100)

Insulin Receptor (12)

Integrin (36)

Interleukin Related (50)

IRAK (16)

IRE1 (16)

Isocitrate Dehydrogenase (IDH) (15)

Itk (5)

JAK (78)

JNK (31)

Keap1-Nrf2 (22)

Kinesin (17)

KLF (4)

Lactate Dehydrogenase (11)

Leukotriene Receptor (21)

Ligand for Target Protein for PROTAC (19)

LIM Kinase (LIMK) (5)

Lipoxygenase (39)

LPL Receptor (11)

LRRK2 (15)

LXR (3)

mAChR (32)

MAGL (16)

MALT1 (4)

MAPKAPK2 (MK2) (4)

MCHR1 (GPR24) (3)

MDM-2/p53 (44)

MEK (35)

Melanocortin Receptor (5)

Melatonin Receptor (3)

MELK (3)

mGluR (11)

MicroRNA (7)

Microtubule/Tubulin (87)

Mineralocorticoid Receptor (2)

Mitochondrial Metabolism (39)

Mitophagy (53)

Mixed Lineage Kinase (4)

MMP (59)

MNK (5)

Monoamine Oxidase (62)

Monoamine Transporter (11)

Monocarboxylate Transporter (7)

Mps1 (10)

mTOR (70)

MyD88 (4)

Myosin (13)

Na+/Ca2+ Exchanger (10)

Na+/K+ ATPase (16)

nAChR (15)

NADPH Oxidase (11)

Nampt (11)

NEDD8-activating Enzyme (6)

Neprilysin (14)

Neurokinin Receptor (3)

Neuropeptide Y Receptor (10)

Neurotensin Receptor (2)

NF-κB (141)

NKCC (6)

NO Synthase (43)

NOD-like Receptor (NLR) (15)

Notch (22)

Nucleoside Antimetabolite/Analog (37)

Opioid Receptor (9)

Orexin Receptor (OX Receptor) (2)

Oxytocin Receptor (1)

P-glycoprotein (39)

P2X Receptor (13)

P2Y Receptor (12)

p38 MAPK (60)

p97 (7)

PAI-1 (8)

PAK (12)

Parasite (145)

PARP (50)

PD-1/PD-L1 (13)

PDGFR (72)

PDHK (9)

PDK-1 (6)

PERK (4)

PGC-1α (1)

PGE synthase (12)

Phosphatase (99)

Phosphodiesterase (PDE) (143)

Phospholipase (43)

Pim (18)

PKA (33)

PKC (72)

PKD (4)

Polo-like Kinase (PLK) (22)

Porcupine (8)

Potassium Channel (87)

PPAR (27)

Procollagen C Proteinase (1)

Prostaglandin Receptor (31)

PROTAC (19)

PROTAC Linker (16)

Protease-Activated Receptor (PAR) (9)

Proteasome (43)

Protein Arginine Deiminase (4)

Proton Pump (36)

PTEN (5)

Pyk2 (4)

Pyruvate Kinase (2)

RAD51 (5)

Raf (44)

RAR/RXR (11)

Ras (61)

Reactive Oxygen Species (71)

Renin (3)

RET (20)

Reverse Transcriptase (49)

RGS Protein (3)

Ribosomal S6 Kinase (RSK) (21)

RIP kinase (28)

ROCK (38)

ROR (9)

ROS (8)

RSV (14)

Salt-inducible Kinase (SIK) (6)

SARS-CoV (62)

Ser/Thr Protease (19)

sFRP-1 (1)

SGK (7)

SGLT (18)

Sigma Receptor (6)

Sirtuin (29)

Smo (10)

SNIPER (8)

Sodium Channel (73)

Somatostatin Receptor (8)

SPHK (9)

Src (63)

SRPK (3)

STAT (62)

Stearoyl-CoA Desaturase (SCD) (10)

STING (6)

Survivin (3)

Syk (23)

Telomerase (8)

TGF-beta/Smad (12)

TGF-β Receptor (35)

Thrombin (21)

Thymidylate Synthase (7)

Thyroid Hormone Receptor (5)

TNF Receptor (37)

Toll-like Receptor (TLR) (28)

TOPK (6)

Topoisomerase (91)

Trk Receptor (19)

TRP Channel (37)

Tryptophan Hydroxylase (8)

TSH Receptor (1)

Tyrosinase (36)

ULK (4)

URAT1 (4)

Urotensin Receptor (1)

Vasopressin Receptor (2)

VD/VDR (5)

VDAC (2)

VEGFR (123)

Virus Protease (33)

Wee1 (4)

Wnt (36)

Xanthine Oxidase (11)

YAP (9)

β-catenin (16)

γ-secretase (21)

By Research Areas:

Cancer (4068)

Cardiovascular Disease (620)

Endocrinology (230)

Infection (1097)

Inflammation/Immunology (1378)

Metabolic Disease (709)

Neurological Disease (947)

7744

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

292

Peptides

MCE Kits

Inhibitory Antibodies

1386

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-N1775

3',4'-Dihydroxyacetophenone 3,4-DHAP	Tyrosinase	Cancer
3',4'-Dihydroxyacetophenone (3,4-DHAP), isolated from Picea Schrenkiana Needles exhibits a strong suppressive action against tyrosinase activity, with an IC₅₀ of 10 μM. 3',4'-Dihydroxyacetophenone (3,4-DHAP) is a vasoactive agent and antioxidant.

HY-111802

3,4'-Dihydroxyflavone
3,4'-DHF
Influenza Virus Infection

3,4'-Dihydroxyflavone (3,4'-DHF) is an oral active flavonoid with antiviral activity against Influenza A virus.

3,4'-Dihydroxyflavone 3,4'-DHF	Influenza Virus	Infection
3,4'-Dihydroxyflavone (3,4'-DHF) is an oral active flavonoid with antiviral activity against Influenza A virus.

HY-117570

KSC-34	Others	Neurological Disease
KSC-34 is a potent and site-selective inhibitor of PDIA1 (containing two active-site domains a and a′). KSC-34 displays a 30-fold selectivity for a domain over a′ domain and time-dependent inhibition of PDIA1 reductase activity. KSC-34 displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.

HY-101667

LTURM34	DNA-PK	Cancer
LTURM34 is a specific DNA-PK inhibitor (IC₅₀=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.

HY-N1780

3,4-Dimethoxyphenol	Tyrosinase	Endocrinology Metabolic Disease
3,4-Dimethoxyphenol is a plant-derived phenylpropanoid compound and can use as a whitening agent in cosmetics. 3,4-Dimethoxyphenol has *tyrosinase*-inhibiting activity. 3,4-Dimethoxyphenol has potent antioxidant effect isolated from the bacterial fermentation broth.

HY-12794

Vps34-PIK-III
PI3K Autophagy Neurological Disease

Vps34-PIK-III is a potent and selective inhibitor of VPS34 with an IC₅₀ of 18 nM.
HY-12795

Vps34-IN-1
PI3K Autophagy Cancer

Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC₅₀ of 4 nM. Vps34-IN-1 modulates autophagy.
HY-Y0935

3,4-Dimethoxyphenethylamine
Endogenous Metabolite Metabolic Disease

3,4-Dimethoxyphenethylamine is an endogenous metabolite.
HY-113474

3,4-Dihydroxymandelic acid
Endogenous Metabolite Metabolic Disease

3,4-Dihydroxymandelic acid is a metabolite of norepinephrine.

Vps34-PIK-III	PI3K Autophagy	Neurological Disease
Vps34-PIK-III is a potent and selective inhibitor of *VPS34* with an IC₅₀ of 18 nM.

Vps34-IN-1	PI3K Autophagy	Cancer
Vps34-IN-1 is an inhibitor of *Vps34* extracted from patent WO2012085815A1, compound example 16a, with an IC₅₀ of 4 nM. Vps34-IN-1 modulates autophagy.

3,4-Dimethoxyphenethylamine	Endogenous Metabolite	Metabolic Disease
3,4-Dimethoxyphenethylamine is an endogenous metabolite.

3,4-Dihydroxymandelic acid	Endogenous Metabolite	Metabolic Disease
3,4-Dihydroxymandelic acid is a metabolite of norepinephrine.

HY-12473

Vps34-IN-2	PI3K	Cancer
Vps34-IN-2 is a novel, potent and selective inhibitor of *Vps34* with IC₅₀s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.

HY-13519

TRAM-34
Potassium Channel Neurological Disease

TRAM-34 is a highly selective blocker of intermediate-conductance calcium-activated K⁺ channel (IKCa1) (K_d=20 nM).
HY-W001080

3,4-Dihydroxybenzeneacetic acid
Endogenous Metabolite Others

3,4-Dihydroxybenzeneacetic acid is the main neuronal metabolite of dopamine.
HY-Y0771

3,4-Dimethoxyphenylacetic acid
Endogenous Metabolite Others

3,4-Dimethoxyphenylacetic acid is a building block in the chemical synthesis.
HY-13688

PJ34 hydrochloride
PARP Cancer

PJ34 hydrochloride is an inhibitor of PARP1/2 with IC₅₀ of 110 nM and 86 nM, respectively.
HY-13688A

PJ34
PARP Cancer

PJ34 is a potent specific inhibitor of PARPl/2 with IC₅₀ of 110 nM and 86 nM, respectively.

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

3,4-Dihydroxybenzeneacetic acid	Endogenous Metabolite	Others
3,4-Dihydroxybenzeneacetic acid is the main neuronal metabolite of dopamine.

3,4-Dimethoxyphenylacetic acid	Endogenous Metabolite	Others
3,4-Dimethoxyphenylacetic acid is a building block in the chemical synthesis.

PJ34 hydrochloride	PARP	Cancer
PJ34 hydrochloride is an inhibitor of PARP1/2 with IC₅₀ of 110 nM and 86 nM, respectively.

PJ34	PARP	Cancer
PJ34 is a potent specific inhibitor of PARPl/2 with IC₅₀ of 110 nM and 86 nM, respectively.

HY-N0057

3,4-Dicaffeoylquinic acid 3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B	Glucosidase Influenza Virus Apoptosis Endogenous Metabolite	Cancer Infection
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.

HY-W017434

3,4-Dimethylbenzoic acid
Others Others

3,4-Dimethylbenzoic acid acts as a product of dimethylbenzoate metabolism by Rhodococcus rhodochrous N75.

3,4-Dimethylbenzoic acid	Others	Others
3,4-Dimethylbenzoic acid acts as a product of dimethylbenzoate metabolism by Rhodococcus rhodochrous N75.

HY-128760

COH34	Others	Cancer
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC₅₀ of 0.37 nM. COH34 binds to the catalytic domain of PARG (K_d=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.

HY-P2426

(D-Trp12,Tyr34)-pTH (7-34) amide (bovine)	Thyroid Hormone Receptor	Metabolic Disease
(D-Trp12,Tyr34)-pTH (7-34) amide (bovine) is a potent and competitive antagonist of parathyroid hormone (PTH), with a K_i of 69 nM in bovine renal cortical membrane. (D-Trp12,Tyr34)-pTH (7-34) amide (bovine) can be used for growth and development regulation.

HY-106934

Peldesine BCX 34	Nucleoside Antimetabolite/Analog HIV	Cancer Infection Inflammation/Immunology
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC₅₀s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC₅₀ of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection treatment.

HY-109714

3,4-Benzocoumarin	Others	Inflammation/Immunology
3,4-Benzocoumarin is a kind of the expanded structure of coumarin derivatives.Coumarin is a chemical compound in the benzopyrone chemical class that can be found in many natural species. Coumarins possess variety of biological activities and unique photophysical properties. 3,4-Benzocoumarin, a AOH‐like compound , has the sensibility of the antibody with an IC₅₀ of 919.2 ng/mL.

HY-133611

3,4-Dichlorocatechol
Others Infection

3,4-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71.
HY-115666

COH34 analog 1
Others Cancer

COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
HY-14946

Amifampridine
3,4-Diaminopyridine
Others Others

Amifampridine (3,4-Diaminopyridine) is a drug, predominantly in the treatment of a number of rare muscle diseases.

3,4-Dichlorocatechol	Others	Infection
3,4-Dichlorocatechol is a substrate of the broad-spectrum chlorocatechol 1,2-dioxygenase of pseudomonas chlororaphis RW71.

COH34 analog 1	Others	Cancer
COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.

Amifampridine 3,4-Diaminopyridine	Others	Others
Amifampridine (3,4-Diaminopyridine) is a drug, predominantly in the treatment of a number of rare muscle diseases.

HY-136593

*(S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid* (S)-3-(4-Hydroxyphenyl)lactic acid	Others	Others
(S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid (compound 1) is a metabolite isolated from the culture medium of Leuconostoc mesenteroides. (S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid has high DPPH radical-scavenging activities and antioxidative activities.

HY-P1322

[D-Trp34]-Neuropeptide Y	Neuropeptide Y Receptor	Neurological Disease
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y₅ receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y₁, Y₂, Y₄, and y₆ receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats.

HY-117771

DO34	Others	Metabolic Disease
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC₅₀ of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC₅₀ for DAGLβ.

HY-111583

RXFP3/4 agonist 1	Others	Metabolic Disease
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC₅₀s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.

HY-P1223

Exendin-3/4 (59-86)
Glucagon Receptor Metabolic Disease

Exendin-3/4 (59-86) is a Exendin-4 peptide derivative.
HY-117771A

DO34 analog
Others Metabolic Disease

DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.

*Exendin-3/4* (59-86)**	Glucagon Receptor	Metabolic Disease
Exendin-3/4 (59-86) is a Exendin-4 peptide derivative.

DO34 analog	Others	Metabolic Disease
DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.

HY-113304

*(S)-3,4-Dihydroxybutyric acid*	Endogenous Metabolite	Metabolic Disease
(S)-3,4-Dihydroxybutyric acid is a normal human urinary metabolite that is excreted in increased concentration in patients with succinic semialdehyde dehydrogenase (SSADH) deficiency.

HY-111804

3',4'-Dihydroxyflavonol DiOHF	NO Synthase	Metabolic Disease Cardiovascular Disease
3',4'-Dihydroxyflavonol (DiOHF) is an effective antioxidant, which reduces superoxide and improves nitric oxide (NO) function in diabetic rat mesenteric arteries.

HY-107575

TLR4-IN-C34	Toll-like Receptor (TLR)	Inflammation/Immunology
TLR4-IN-C34 is an orally active TLR4 inhibitor and reduces systemic inflammation in models of endotoxemia and necrotizing enterocolitis.

HY-135910

3,4-Dehydro Cilostazol OPC-13015	Drug Metabolite	Cancer Cardiovascular Disease
3,4-Dehydro Cilostazol (OPC-13015) is an active metabolite of Cilostazol (CLZ; HY-17464). 3,4-Dehydro Cilostazol is used for pharmacokinetic study.

HY-N1778

3,4-Dimethoxycinnamic acid O-Methylferulic acid	Reactive Oxygen Species Virus Protease	Cancer Infection
3,4-Dimethoxycinnamic acid (O-Methylferulic acid) is a monomer extracted and purified from Securidaca inappendiculata Hassk. 3,4-Dimethoxycinnamic acid exerts anti-apoptotic effects on L-02 cells via the ROS-mediated signaling pathway. Anti-apoptotic effects.

HY-N7641

3',4',7-Trimethoxyquercetin Quercetin 3′,4′,7-trimethyl ether	Others	Others
3',4',7-Trimethoxyquercetin (Quercetin 3′,4′,7-trimethyl ether) is a polymethoxylated flavone isolated from the plant of genus Taraxacum, has antioxidant activity.

HY-N7557

*(E)-2'-Hydroxy-3,4-dimethoxychalcone*	Others	Cancer
(E)-2'-Hydroxy-3,4-dimethoxychalcone (compound 7) is a Chalcone derivative with orally active. (E)-2'-Hydroxy-3,4-dimethoxychalcone has anti-tumour activities.

HY-P1322A

[D-Trp34]-Neuropeptide Y TFA	Neuropeptide Y Receptor	Neurological Disease
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y₅ receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y₁, Y₂, Y₄, and y₆ receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats.

HY-111818

TH34
HDAC Cancer

TH34, an HDAC6/8/10 inhibitor with IC₅₀s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.
HY-P1225

{Val1}-Exendin-3/4
Glucagon Receptor Metabolic Disease

{Val1}-Exendin-3/4 is the first N-terminal 1-28 residues of Exendin-4 peptide.

TH34	HDAC	Cancer
TH34, an HDAC6/8/10 inhibitor with IC₅₀s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.

{Val1}-Exendin-3/4	Glucagon Receptor	Metabolic Disease
{Val1}-Exendin-3/4 is the first N-terminal 1-28 residues of Exendin-4 peptide.

HY-P1252

Parathyroid Hormone (1-34), bovine	Thyroid Hormone Receptor	Metabolic Disease
Parathyroid Hormone (1-34), bovine is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.

HY-W016993

2,3,4-Trihydroxybenzoic acid
Others Others

2,3,4-Trihydroxybenzoic acid is an internal standard in separation of phenolic acids by HPLC.

*2,3,4-Trihydroxybenzoic acid*	Others	Others
2,3,4-Trihydroxybenzoic acid is an internal standard in separation of phenolic acids by HPLC.

HY-P1323

[Leu31,Pro34]-Neuropeptide Y(human,rat)	Neuropeptide Y Receptor	Neurological Disease Cardiovascular Disease
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y₁ receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao inhibits Y₄, Y₅. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake.

HY-W010130

*7-Hydroxy-3,4-dihydro-2(1H)-quinolinone* 3,4-Dihydro-7-hydroxy-2(1H)-quinolinone	Monoamine Oxidase	Neurological Disease
7-Hydroxy-3,4-dihydro-2(1H)-quinolinone (3,4-Dihydro-7-hydroxy-2(1H)-quinolinone) is a weak MAO-A inhibitor, with an IC₅₀ of 183 μM, and has no effect on MAO-B.

HY-135976

P2X3 antagonist 34	P2X Receptor	Inflammation/Immunology Neurological Disease
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC₅₀s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.

HY-P0059

Teriparatide
Human parathyroid hormone-(1-34); hPTH (1-34)
Others Cancer

Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC₅₀ of 2 nM in HEK293 cells.

Teriparatide Human parathyroid hormone-(1-34); hPTH (1-34)	Others	Cancer
Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC₅₀ of 2 nM in HEK293 cells.

HY-P1252A

Parathyroid Hormone (1-34), bovine TFA	Thyroid Hormone Receptor	Metabolic Disease
Parathyroid Hormone (1-34), bovine TFA is a potent parathyroid hormone (PTH) receptor agonist. Parathyroid Hormone (1-34), bovine increases calcium and inorganic phosphate levels in vivo. Parathyroid Hormone (1-34), bovine can be used for th reseach of osteoporosis.

HY-N2044

*Methyl 3,4,5-trimethoxybenzoate*	Others	Others
Methyl 3,4,5-trimethoxybenzoate can be synthesized from Gallic acid. Methyl 3,4,5-trimethoxybenzoate is mainly used in the production of Trimethoprim (TMP), Sulfa synergistic intermediates, and many other agents.

HY-133598

3,4,5-Trichlorocatechol
Others Cancer

3,4,5-Trichlorocatechol is a catechol derivative of pentachlorophenol and induces oxidative DNA lesions.

HY-N7427

*2-(2',3',4'-Trihydroxybutyl)quinoxaline*	Endogenous Metabolite	Metabolic Disease
2-(2',3',4'-Trihydroxybutyl)quinoxaline is a food metabolite. 2-(2',3',4'-Trihydroxybutyl)quinoxaline can be formed from homoglucans.

HY-107858

Veratryl alcohol 3,4-Dimethoxybenzyl alcohol	Others	Others
Veratryl alcohol (3,4-Dimethoxybenzenemethanol), a secondary metabolite of some lignin degrading fungi, is commonly used nonphenolic substrate for assaying ligninolytic activity.

HY-N0871

Ingenol-3,4,5,20-diacetonide
Ingenol 3,4:5,20-bisacetonide
Others Others

Ingenol-3,4,5,20-diacetonide is a natural compound.

HY-N3023

3,4-Dihydroxybenzylamine hydrobromide NSC 263475 hydrobromide	DNA/RNA Synthesis	Cancer
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.

HY-133606

3,4,5-Trichlorosyringol
Others Others

3,4,5-Trichlorosyringol is a chlorophenolic compound synthetised by chlorination of syringol in carbon disulphide (CS₂).
HY-133601

3,4,5-Trichloroguaiacol
Others Others

3,4,5-Trichloroguaiacol is a phenolic compound occurring in effluents from bleached kraft pulp mills.

HY-P1323A

[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA	Neuropeptide Y Receptor	Neurological Disease Cardiovascular Disease
[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y₁ receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao inhibits Y₄, Y₅. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake.

HY-W012123

3,4,5-Trimethoxycinnamic acid	GABA Receptor Endogenous Metabolite	Neurological Disease
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.

HY-Y1620

*3-(3,4-Dimethoxyphenyl)propanoic acid*	Others	Cardiovascular Disease
3-(3,4-Dimethoxyphenyl)propanoic acid is an orally active short-chain fatty acids (SCFAs). 3-(3,4-Dimethoxyphenyl)propanoic acid stimulates γ globin gene expression, erythropoiesis in vivo and is used for the β hemoglobinopathies and other anemias.

HY-W016289

Antiarol
3,4,5-Trimethoxyphenol
Others Others

Antiarol (3,4,5-Trimethoxyphenol) is a natural compound isolated from Salmaliamalabaricum.

HY-111388A

SEL120-34A monohydrochloride	CDK	Cancer
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC₅₀s of 4.4 nM and 10.4 nM, respectively, with a K_d of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC₅₀=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.

HY-141007

3,4-Dibromo-Mal-PEG8-Boc
PROTAC Linker Cancer

3,4-Dibromo-Mal-PEG8-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141004

3,4-Dibromo-Mal-PEG2-amine
PROTAC Linker Cancer

3,4-Dibromo-Mal-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141006

3,4-Dibromo-Mal-PEG4-Boc
PROTAC Linker Cancer

3,4-Dibromo-Mal-PEG4-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-N7012

*7,3',4'-Tri-O-methylluteolin* 5-Hydroxy-3',4',7-trimethoxyflavone	TNF Receptor Interleukin Related COX	Cancer Metabolic Disease Inflammation/Immunology
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level.

HY-W022390

*3-(3,4,5-Trimethoxyphenyl)propanoic acid*	Endogenous Metabolite	Others
3-(3,4,5-Trimethoxyphenyl)propanoic acid is found in herbs and spices. 3-(3,4,5-Trimethoxyphenyl)propanoic acid is a constituent of Piper longum (long pepper) and Piper retrofractum (Javanese long pepper).

HY-125907

Dox-Ph-PEG1-Cl
PROTAC Linker 34
PROTAC Linker Cancer

Dox-Ph-PEG1-Cl (PROTAC Linker 34) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

HY-N2007

Veratric acid 3,4-Dimethoxybenzoic acid	COX Reactive Oxygen Species	Inflammation/Immunology Cardiovascular Disease
Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.

HY-125828

1-(3,4-Dimethoxycinnamoyl)piperidine
Others Infection

1-(3,4-Dimethoxycinnamoyl)piperidine, a synthesized piperidine analog, possesses antimicrobial and antioxidant activity.

HY-N7030

*5,7,3',4'-Tetramethoxyflavone*	Others	Infection
5,7,3',4'-Tetramethoxyflavone, one of the major polymethoxyflavones (PMFs) isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.

HY-133610

3,4,6-Trichlorocatechol	Others	Others
3,4,6-trichlorocatechol (TCC) is the metabolite produced by industrial pollutant through post-mitochondrial liver fraction from Aroclor-1254 induced rats.

HY-141005

3,4-Dibromo-Mal-PEG2-N-Boc
PROTAC Linker Cancer

3,4-Dibromo-Mal-PEG2-N-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-P2279

Parathyroid hormone (1-34) (rat)	Thyroid Hormone Receptor	Endocrinology Metabolic Disease
Parathyroid hormone (1-34) (rat) is a parathyroid hormone (PTH) receptor agonist, increasing serum PTH levels and bone mass in rats.

HY-Z0548

*Methyl 3,4-dihydroxybenzoate* Protocatechuic acid methyl ester; Methyl protocatechuate	Keap1-Nrf2 Apoptosis	Cancer Inflammation/Immunology
Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect.

HY-111388B

SEL120-34A HCl	CDK	Cancer
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC₅₀s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.

HY-N7690

*3,5,7,3′,4′-Pentamethoxyflavone*	Others	Metabolic Disease
3,5,7,3′,4′-Pentamethoxyflavone is a polymethoxyflavonoid isolated from Kaempferia parviflora. 3,5,7,3′,4′-Pentamethoxyflavone can induce adipogenesis on 3T3-L1 preadipocytes by regulating transcription factors at an early stage of differentiation.

HY-133604

3,4,5-Trichloroveratrole	Others	Others
3,4,5-Trichloroveratrole is one of the biodegradation products of bacterial O-methylation of Tri- and Tetra chloroguaiacols. The Tri- and Tetra chloroguaiacols are formed during bleaching of wood pulp in the paper manufacturing industry.

HY-Y0084

3,4,5-Trimethoxybenzoic acid Eudesmic acid; Trimethylgallic Acid	Others	Others
3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis.

HY-P1586

HIV-1 Rev 34-50 HIV-1 rev Protein (34-50)	HIV	Infection
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.

HY-N7428

*1-(2-Quinoxalinyl)-1,2,3,4-butanetetrol*	Others	Others
1-(2-Quinoxalinyl)-1,2,3,4-butanetetrol is an endogenous metabolite. The imprinted polymer P-1 shows affinity for 1-(2-Quinoxalinyl)-1,2,3,4-butanetetrol.

HY-W008437

*(S)-2-Amino-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid dihydrate*	Endogenous Metabolite	Metabolic Disease
(S)-2-Amino-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid dihydrate is an endogenous metabolite.

HY-N1753

3-(4-Hydroxyphenyl)-1-propanol
Dihydro-p-coumaryl alcohol; 3-(p-Hydroxyphenyl)propyl alcohol
Others Others

3-(4-Hydroxyphenyl)-1-propanol is used in the synthesis of (-)-centrolobine.

HY-100511

Benzophenonetetracarboxylic acid 3,3',4,4'-Benzophenonetetracarboxylic acid	Others	Others
Benzophenonetetracarboxylic acid (3,3',4,4'-Benzophenonetetracarboxylic acid) is particularly useful in the preparation of high performance polyimides and also useful as curing agents for epoxy resins.

HY-N2038

*3,5,6,7,8,3',4'-Heptemthoxyflavone*	Others	Cancer Neurological Disease
3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.

HY-N2009

3-O-Methylgallic acid 3,4-Dihydroxy-5-methoxybenzoic acid	Apoptosis	Cancer
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC₅₀ value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects.

HY-N4311

2,3,4,5-Tetracaffeoyl-D-Glucaric acid
Others Inflammation/Immunology

2,3,4,5-Tetracaffeoyl-D-Glucaric acid is a caffeoyl-D-glucaric acid derivative isolated from the Genus Gnaphalium.

HY-N7029

3',4',5',5,7-Pentamethoxyflavone	Others	Cancer
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway.

HY-N6829

Retusin Quercetin-3,3',4',7-tetramethylether	Others	Infection Inflammation/Immunology
Retusin (Quercetin-3,3',4',7-tetramethylether), a natural compound isolated from the leaves of Talinum triangulare, possesses antiviral and anti-inflammatory activities.

HY-135652

Hexyl gallate Hexyl 3,4,5-trihydroxybenzoate	Bacterial Parasite	Infection
Hexyl gallates (Hexyl 3,4,5-trihydroxybenzoate) shows antibacterial activity and inhibits the production of rhamnolipid and pyocyanin by inhibiting RhlR. Hexyl gallate, a alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum, with IC₅₀ of 0.11 mM.

HY-P2510

Parathyroid Hormone (1-34), human, biotinylated	Thyroid Hormone Receptor	Metabolic Disease
Parathyroid Hormone (1-34), human, biotinylated is a probe for the parathyroid hormone receptor, can be used for analyzing the interaction between parathyroid hormone and parathyroid hormone receptors in living cells and for purifying hormone-receptor complexes with affinity columns.

HY-12403

Angiotensin (1-7) Ang-(1-7)	Angiotensin Receptor Angiotensin-converting Enzyme (ACE)	Inflammation/Immunology Cardiovascular Disease Endocrinology
Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). Angiotensin 1-7 inhibits purified canine ACE activity (IC₅₀=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .

HY-N5030

8-Hydroxy-3,5,6,7,3',4'-hexamethoxyflavone
Others Others

8-Hydroxy-3,5,6,7,3',4'-hexamethoxyflavone is a polymethoxyflavone (PMF) isolated from pericarpium citri reticulatae.

HY-P1324

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide	Neuropeptide Y Receptor	Neurological Disease
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y₅ receptor agonist with an IC₅₀ of 0.24 nM for binding to the hY₅ receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.

HY-P1324A

[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA	Neuropeptide Y Receptor	Neurological Disease
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y₅ receptor agonist with an IC₅₀ of 0.24 nM for binding to the hY₅ receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.

HY-141137

*2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide*	PROTAC Linker	Cancer
2,3,4,6-Tetra-o-acetyl-alpha-galactosylpyranosyl bromide is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-135591

*Methyl Raloxifene 4'-(2,3,4-Tri-O-acetyl-β-D-glycopyranuronate)*	Others	Others
Methyl Raloxifene 4'-(2,3,4-Tri-O-acetyl-β-D-glycopyranuronate) is an analogue of Raloxifene 4'-glucuronide.

HY-N2207

*rel-(8R,8'R)-Dimethyl-(7S,7'R)-bis(3,4-methylenedioxyphenyl)tetrahydro-furan*	Others	Others
rel-(8R,8'R)-Dimethyl-(7S,7'R)-bis(3,4-methylenedioxyphenyl)tetrahydro-furan is a chemical constituent of the fruit of Myristica fragrans.

HY-13987

*(R)-1,2,3,4-Tetrahydro-3-isoquinolinecarboxylic acid* D-phenylalanine analogue	Others	Others
(R)-1,2,3,4-Tetrahydro-3-isoquinolinecarboxylic acid is a constrained Phe analogue which can fold into a beta-bend and a helical structure, and to adopt a preferred side-chain disposition in the peptide.

HY-141139

*1-(Isopropylthio)-2,3,4,6-tetra-o-Ac-beta-D-glucosylpyranose*	PROTAC Linker	Cancer
1-(Isopropylthio)-2,3,4,6-tetra-o-Ac-beta-D-glucosylpyranose is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-W014410

(2R,3S,4R,5S)-2,3,4,5-Tetrahydroxyhexanedioic acid
Endogenous Metabolite Metabolic Disease

(2R,3S,4R,5S)-2,3,4,5-Tetrahydroxyhexanedioic acid is an endogenous metabolite.
HY-W040240

(3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one
Endogenous Metabolite Metabolic Disease

(3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.

HY-N0652

2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside 2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside	Others	Others
2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonum species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.

HY-W021425

*(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride*	Endogenous Metabolite	Metabolic Disease
(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride is an endogenous metabolite.

HY-42680

(3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one
Tagatose, D- (8CI)
Endogenous Metabolite Metabolic Disease

(3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.

HY-N0252

Catharanthine (+)-3,4-Didehydrocoronaridine	Calcium Channel	Cancer Cardiovascular Disease
Catharanthine is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-70061

TCS7010
Aurora Kinase Apoptosis Cancer

TCS7010 is a potent and highly selective Aurora A inhibitor with with an IC₅₀ of 3.4 nM.

HY-12594

Paritaprevir ABT-450; Veruprevir	HCV Protease HCV	Infection
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC₅₀s of 1 and 0.21 nM against HCV 1a and 1b, respectively.

HY-U00439

Protein kinase inhibitors 1
DYRK Cancer

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.

HY-N0523

Gallic acid 3,4,5-Trihydroxybenzoic acid	COX Reactive Oxygen Species Apoptosis Ferroptosis Endogenous Metabolite	Cancer Metabolic Disease
Gallic acid is an antioxidant which can inhibit both COX-2.

HY-19677

Cipemastat
Ro 32-3555
MMP Cancer

Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with K_is of 3.0, 4.4 and 3.4 nM, respectively.

HY-66012

Proparacaine Hydrochloride Proxymetacaine Hydrochloride	Sodium Channel Bacterial	Neurological Disease
Proparacaine Hydrochloride is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.

HY-N0294

Protocatechuic acid
3,4-Dihydroxybenzoic acid
Others Neurological Disease

Protocatechuic acid is a phenolic compound which exhibits neuroprotective effect.
HY-17634

Glecaprevir
ABT-493
HCV HCV Protease Infection

Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC₅₀ values ranging from 3.5 to 11.3 nM.
HY-B2136

Tannic acid
Potassium Channel Cancer Inflammation/Immunology

Tannic acid is a novel hERG channel blocker with IC₅₀ of 3.4 μM.
HY-15485

Zardaverine
Phosphodiesterase (PDE) Inflammation/Immunology

Zardaverine is a newly developed dual-selective PDE3/4 inhibitor with IC50 values of 0.5 uM and 0.8 uM respectively.

HY-W050145

*(1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol*	Endogenous Metabolite	Metabolic Disease
(1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol is an endogenous metabolite.

HY-18771

O4I1
Oct3/4 Others

O4I1 is as a potent Oct3/4 inducer.

HY-101920

Autophinib	Autophagy	Cancer Neurological Disease
Autophinib is a potent, selective autophagy inhibitor with IC₅₀s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC₅₀ of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting *VPS34*.

HY-10452

Ixazomib citrate MLN9708	Proteasome Autophagy	Cancer
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC₅₀ of 3.4 nM and a K_i of 0.93 nM.

HY-12481A

SAR405 R enantiomer
Others Cancer

SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor.

HY-10241

Simeprevir TMC435	HCV HCV Protease	Infection
Simeprevir (TMC435) is an oral and potent *HCV NS3/4A* protease** inhibitor with a K_i of 0.36 nM, and inhibits HCV replication with an EC₅₀ of 7.8 nM.

HY-N0252A

Catharanthine Tartrate (+)-3,4-Didehydrocoronaridine Tartrate	Calcium Channel	Cancer Cardiovascular Disease
Catharanthine Tartrate is an alkaloid isolated from Madagascar periwinkle, inhibits voltage-operated L-type Ca²⁺ channel, with anti-cancer and blood pressure-lowering activity.

HY-12873

RBC8
Ras Cancer

RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
HY-18563

4-Phenoxybenzylamine
HCV Infection

4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC₅₀ of about 500 μM against FL NS3/4a.

HY-10453

Ixazomib MLN2238	Proteasome Autophagy	Cancer
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC₅₀ of 3.4 nM (K_i of 0.93 nM).

HY-124772

BI-2545	Phosphodiesterase (PDE)	Inflammation/Immunology
BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC₅₀s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively.

HY-N2406

Dihydrocaffeic acid 3,4-Dihydroxy-benzenepropanoic acid	p38 MAPK Endogenous Metabolite	Inflammation/Immunology
Dihydrocaffeic acid is a phenolic acid found in Gynura bicolor, reduces phosphorylation of MAPK p38 and prevent UVB-induced skin damage. Antioxidant potential and anti-inflammatory activity.

HY-B1805

Triclocarban
3,4,4′-Trichlorocarbanilide
Bacterial Infection

Triclocarban is an antimicrobial agent used in personal cleaning products.

HY-W015346

Desaminotyrosine 3-(4-Hydroxyphenyl)propionic acid	Influenza Virus Endogenous Metabolite	Infection
Desaminotyrosine is a microbially associated metabolite protecting from influenza through augmentation of type I interferon signaling.

HY-19340

TMS
(E)-2,3',4,5'-tetramethoxystilbene
Cytochrome P450 Cancer

TMS is a selective inhibitor of CYP1B1 activity.
HY-18772

O4I2
Oct3/4 Others

O4I2 is a potent Oct3/4 inducer in various human cell lines including human fibroblasts.
HY-112376

MZP-54
PROTAC Epigenetic Reader Domain Cancer

MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a K_d of 4 nM for Brd4^BD2.
HY-112377

MZP-55
Epigenetic Reader Domain PROTAC Cancer

MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a K_d of 8 nM for Brd4^BD2.
HY-19863

F-15599
NLX-101
5-HT Receptor Neurological Disease

F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with K_i of 3.4 nM.

HY-50874

BCX 1470	Complement System	Inflammation/Immunology
BCX 1470 inhibits the esterolytic activity of factor D (IC₅₀=96 nM) and C1s (IC₅₀=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.

HY-16558

Butein 2’,3,4,4’-tetrahydroxy Chalcone	EGFR Autophagy Apoptosis Phosphodiesterase (PDE)	Cancer
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC₅₀ of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC₅₀s of 16 and 65 μM for EGFR and p60^c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).

HY-W008923

Doxycycline monohydrate
MMP Bacterial Parasite Antibiotic Infection

Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-141003

3,4-Dibromo-Mal-PEG8-acid
PROTAC Linker Cancer

3,4-Dibromo-Mal-PEG8-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-A0296

Chlormethiazole hydrochloride Clomethiazole hydrochloride	Others	Neurological Disease
Clomethiazole hydrochloride is a sedative and anticonvulsant. Clomethiazole hydrochloride is neuroprotective and prevents the degeneration of serotonergic nerve terminals induced by 3,4-methylenedioxymethamphetamine (MDMA).

HY-50875

BCX 1470 methanesulfonate	Complement System	Inflammation/Immunology
BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D (IC₅₀=96 nM) and C1s (IC₅₀=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.

HY-15260A

XL413 hydrochloride	CDK	Cancer
XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC₅₀ of 3.4 nM, and also shows potent effect with IC₅₀s of 215, 42 nM on CK2, PIM1, respectively, and an EC₅₀ of 118 nM on pMCM.

HY-107377

Benzo[a]pyrene
3,4-Benzopyrene
Others Cancer

Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies.

HY-N0304

L-DOPA Levodopa; 3,4-Dihydroxyphenylalanine	Dopamine Receptor Endogenous Metabolite	Neurological Disease
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.

HY-10238

Danoprevir ITMN-191; R7227; RO5190591; RG7227	HCV Protease HCV	Infection
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC₅₀ of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC₅₀ higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC₅₀s=0.2-0.4 nM) as well as 2b and 3a (IC₅₀s=1.6, 3.5 nM).

HY-13902

Berzosertib
VE-822; VX-970
ATM/ATR Cancer

Berzosertib (VE-822) is an ATR inhibitor with a K_i value of less than 0.2 nM. It also inhibits ATM with a K_i of 34 nM.

HY-P0216

A 779	Angiotensin Receptor	Cardiovascular Disease Endocrinology
A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.

HY-111400

SR-4370
HDAC Cancer

SR-4370 is an inhibitor of HDAC, with IC₅₀s of 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively.

HY-10235

Telaprevir VX-950	HCV Protease HCV	Infection
Telaprevir is a highly selective, reversible, and potent peptidomimetic inhibitor of the *HCV NS3-4A* protease, the steady-state inhibitory constant (K_i**) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide.

HY-N1272

Secaubryenol	Endogenous Metabolite	Others
Secaubryenol is a class of 3,4-secocycloartane triterpenes isolated from Coussarea macrophylla. Secaubryenol does not display any cytotoxic effect at a dose of 10 µg/mL.

HY-115661

Bisdionin C	Bacterial	Infection
Bisdionin C is a potent GH18 chitinases inhibitor, with an IC₅₀ of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC₅₀s of 8.3 and 3.4 μM, respectively.

HY-15778A

AVE 0991 sodium salt	Angiotensin Receptor	Cardiovascular Disease Endocrinology
AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [¹²⁵I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC₅₀ of 21 nM.

HY-101428

NS-638	Calcium Channel	Neurological Disease
NS-638 is a small nonpeptide molecule with Ca²⁺-channel blocking properties. K⁺-stimulated intracellular Ca²⁺-elevation is blocked with an IC₅₀ value of 3.4 μM.

HY-15472

PRX-08066	5-HT Receptor	Cardiovascular Disease
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

HY-13270

ABT-751 E7010	Microtubule/Tubulin Autophagy	Cancer
ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.

HY-100352

BI-9564	Epigenetic Reader Domain	Cancer
BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family.

HY-W008566

Norharmane Norharman; β-Carboline	Monoamine Oxidase Endogenous Metabolite	Neurological Disease
Norharmane (Norharman), isolated from coffee, is a potent and selective monoamine oxidase A (MAO-A) inhibitor with a K_i of 3.34 μM.

HY-B0233

Isradipine
PN 200-110
Calcium Channel Autophagy Cardiovascular Disease

Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.

HY-10126

Barasertib-HQPA AZD2811; INH-34; AZD1152-HQPA	Aurora Kinase	Cancer
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC₅₀ of 0.37 nM in a cell-free assay, and shows 3700-fold selectivity for Aurora B over Aurora A.

HY-15895

Aprocitentan ACT-132577	Endothelin Receptor	Cardiovascular Disease Endocrinology
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC₅₀s of 3.4 nM and 987 nM, and pA₂ valus of 6.7 and 5.5, respectively.

HY-N1584

Halofuginone RU-19110	DNA/RNA Synthesis TGF-beta/Smad Parasite	Inflammation/Immunology Cancer
Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity.

HY-U00171

SQ28603 SQ28,603; Squibb 28603	Neprilysin	Metabolic Disease
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).

HY-13461A

PHA-767491 hydrochloride
CAY-10572 hydrochloride
CDK Apoptosis Cancer

PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC₅₀s of 10 nM and 34 nM, respectively.
HY-13783

BIBF0775
TGF-β Receptor Cancer

BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC₅₀ of 34 nM.

HY-15670

BMS-906024	γ-secretase Notch	Cancer
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC₅₀s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.

HY-N1584A

Halofuginone hydrobromide RU-19110 hydrobromide	DNA/RNA Synthesis TGF-beta/Smad Parasite	Inflammation/Immunology Cancer
Halofuginone hydrobromide (RU-19110 hydrobromide) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity.

HY-111663

VL285
Ligand for E3 Ligase Cancer

VL285 is a potent VHL ligand with an IC₅₀ of 0.34 μM.

HY-10969

Obatoclax Mesylate GX15-070 Mesylate	Bcl-2 Family Autophagy Parasite	Cancer Infection
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

HY-15298C

Grazoprevir sodium salt MK-5172 (sodium salt)	HCV HCV Protease	Infection
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-15298

Grazoprevir MK-5172	HCV Protease HCV	Infection
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-10969A

Obatoclax GX15-070	Bcl-2 Family Autophagy Parasite	Cancer Infection
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.

HY-15298A

Grazoprevir potassium salt MK-5172 (potassium salt)	HCV HCV Protease	Infection
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with K_is of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.

HY-N2129

N-Nornuciferine	Cytochrome P450	Metabolic Disease Cardiovascular Disease
N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC₅₀ and K_i of 3.76 and 2.34 μM, respectively.

HY-15743

Birabresib
OTX-015; MK-8628
Epigenetic Reader Domain Cancer

Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.
HY-112065

PF-06869206
Sodium Channel Metabolic Disease

PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC₅₀ of 380 nM.

HY-109121

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

HY-W003445

4-Bromo-3-hydroxybenzoic acid	Endogenous Metabolite	Neurological Disease
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC₅₀s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC₅₀s of 1 mM for both enzymes.

HY-19363

GW4869	Phospholipase	Inflammation/Immunology Cardiovascular Disease
GW4869 is a noncompetitive neutral sphingomyelinase (N-SMase) inhibitor with an IC₅₀ of 1 μM. GW4869 is an inhibitor of exosome biogenesis/release.

HY-10259

PD 123319 (S)-(+)-PD 123319	Angiotensin Receptor	Cardiovascular Disease Endocrinology
PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM.

HY-10259A

PD 123319 ditrifluoroacetate	Angiotensin Receptor	Cardiovascular Disease Endocrinology
PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC₅₀ of 34 nM.

HY-N7112

Leucomycin
Kitasamycin
Bacterial Antibiotic Infection

Leucomycin (kitasamycin) is a macrolide antibiotic produced by Streptomyces kitasatoensis.

HY-15225

Telomestatin	Telomerase ADC Cytotoxin	Cancer
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research.

HY-A0077

Perphenazine	5-HT Receptor Adrenergic Receptor Dopamine Receptor Histamine Receptor	Neurological Disease Endocrinology
Perphenazine is a typical antipsychotic drug, inhibits 5-HT_2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with K_i values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

HY-10811

GNE-493	PI3K mTOR	Cancer
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC₅₀s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.

HY-N0570

Hydroxytyrosol DOPET; 3,4-Dihydroxyphenethyl alcohol; 3-Hydroxytyrosol	Endogenous Metabolite	Cancer Infection Inflammation/Immunology
Hydroxytyrosol (DOPET) is a phenolic compound drawn from the olive tree and its leaves with anti-oxidant, anti-atherogenic, anti-thrombotic, antimicrobial, anti-inflammatory and anti-tumour effects.

HY-121526

S-Nitroso-N-acetyl-DL-penicillamine SNAP	NO Synthase	Cardiovascular Disease
S-Nitroso-N-acetyl-DL-penicillamine (SNAP) is a nitric oxide donor and acts as a stable inhibitor of platelet aggregation.

HY-22385

Salsolidine 6,7-Dimethoxy-1-methyl-1,2,3,4-tetrahydroisoquinoline	Monoamine Oxidase	Neurological Disease
Salsolidine is a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A inhibitor.

HY-B1490

Imipramine hydrochloride	Serotonin Transporter	Neurological Disease
Imipramine hydrochloride inhibits serotonin transporter with an IC₅₀ value of 32 nM in vitro. Imipramine hydrochloride is reported to prevent the translocation of aSMase, inhibiting MV and exosomes secretion.

HY-14894

Ipragliflozin
ASP1941
SGLT Metabolic Disease

Ipragliflozin (ASP1941) is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6.
HY-15602

Ledipasvir
GS-5885
HCV Infection

Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC₅₀s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
HY-108261

Tomeglovir
BAY 38-4766
CMV Infection

Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC₅₀s of 0.34 μM and 0.039 μM for HCMV and MCMV.

HY-15591A

TMC647055 Choline salt	HCV	Infection
TMC647055 choline salt is a cell-permeating, selective HCV NS5B inhibitor, eliciting a mean IC50 of 34 nM, as assessed in the RdRp primer-dependent transcription assay.

HY-13433

Thapsigargin	Calcium Channel Apoptosis	Cancer
Thapsigargin is an inhibitor of microsomal Ca²⁺-ATPase. Thapsigargin is a well characterized Endoplasmic Reticulum (ER) stress inducing agent.

HY-P0227

SHU 9119	Melanocortin Receptor	Metabolic Disease
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC₅₀ values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.

HY-15895S

Aprocitentan D4 ACT-132577 D4	Endothelin Receptor	Endocrinology Cardiovascular Disease
Aprocitentan D4 (ACT-132577 D4) is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC₅₀s of 3.4 nM and 987 nM, and pA₂ valus of 6.7 and 5.5, respectively.

HY-N2359

Chelerythrine	PKC Bcl-2 Family Apoptosis Autophagy	Cancer Metabolic Disease Inflammation/Immunology
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca²⁺/phospholopid-dependent PKC antagonist, with an IC₅₀ of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC₅₀ of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and *autophagy*.

HY-19834

Fenebrutinib GDC-0853	Btk	Cancer
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with K_is of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.

HY-12887

Piclamilast RP 73401; RPR 73401	Phosphodiesterase (PDE)	Cancer Inflammation/Immunology
Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC₅₀ values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.

HY-100517

TP-472
Epigenetic Reader Domain Cancer

TP-472 is a selective BRD7/9 inhibitor, with K_Ds of 0.34 μM and 33 nM for BRD7 and BRD9, respectively.

HY-12449

Crenigacestat LY3039478	Notch γ-secretase	Cancer
Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC₅₀ of 1 nM in most of the tumor cell lines tested.

HY-15602B

Ledipasvir D-tartrate GS-5885 D-tartrate	HCV	Infection
Ledipasvir D-tartrate is an inhibitor of the hepatitis C virus NS5A, with EC₅₀ values of 34 pM against GT1a and 4 pM against GT1b replicon.

HY-101191

Ecteinascidin 770 Ecteinascidine 770; Et-770	Apoptosis	Cancer
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC₅₀ of 4.83 nM.

HY-W002587

4-Hydroxy-3-methylbenzoic acid
Endogenous Metabolite Others

4-Hydroxy-3-methylbenzoic acid is a normal organic acid identified in urine specimens from a healthy population.

HY-107623

TC-MCH 7c	MCHR1 (GPR24)	Metabolic Disease
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH₁R antagonist with an IC₅₀ of 5.6 nM for hMCH₁R. TC-MCH 7c has K_is of 3.4 nM and 3.0 nM of human and mouse MCH₁R, respectively.

HY-12031A

U0126	MEK Autophagy Mitophagy Influenza Virus	Cancer
U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

HY-101860

GIBH-130	Interleukin Related	Neurological Disease
GIBH-130 is an effective inhibitor of neuroinflammation. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia (IC₅₀=3.4 nM).

HY-103225

S-8510 phosphate SB-737552 phosphate	GABA Receptor	Neurological Disease
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with K_is of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.

HY-125880

SBI-553
Neurotensin Receptor Endocrinology Neurological Disease

SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC₅₀ of 0.34 μM.
HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-B0879A

Suramin sodium salt Suramin hexasodium salt	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis	Cancer Infection Cardiovascular Disease
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

HY-B0879

Suramin	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase Parasite Apoptosis	Cancer Infection Cardiovascular Disease
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC₅₀=297 nM), SirT2 (IC₅₀=1.15 μM), and SirT5 (IC₅₀=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC₅₀=5 μM). Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

HY-111508

PI3K/mTOR Inhibitor-2	PI3K mTOR	Cancer
PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC₅₀s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.

HY-107795

Benorilate Salipran	Prostaglandin Receptor	Inflammation/Immunology Endocrinology
Benorylate (Salipran) is the esterification product of paracetamol and acetylsalicylic acid. Benorylate has anti-inflammatory, analgesic and antipyretic properties. Benorylate could also inhibit prostaglandin (PG) synthesis.

HY-N0872

Isosteviol (-)-Isosteviol; iso-Steviol	Reactive Oxygen Species Topoisomerase	Cardiovascular Disease Cancer
Isosteviol ((-)-Isosteviol) is a derivative of Stevioside through acid catalyzed hydrolysis of Stevioside. Isosteviol inhibits DNA polymerase and DNA topoisomerase and has antibacterial, anticancer and anti-tuberculosis effects.

HY-11004

AZ 628
Raf Apoptosis Cancer

AZ 628 is a pan-Raf kinase inhibitor with IC₅₀s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
HY-135317

CA-4948
IRAK FLT3 Cancer Inflammation/Immunology

CA-4948 is a potent IRAK4/FLT3 inhibtor with anti-tumor activity.

HY-W013706

Inosine-5'-triphosphate trisodium salt	Endogenous Metabolite	Metabolic Disease
Inosine-5'-triphosphate trisodium salt is a nucleoside triphosphate and functions as an substrate for ATPases and GTPases.

HY-U00122

Antiulcer Agent 1	Others	Inflammation/Immunology
Antiulcer Agent 1 is a 2-(3,4-dimethoxyphenyl)ethylamine derivative for oral administration at an exploratory stage of new drug development.

HY-12341

ML355	Lipoxygenase	Inflammation/Immunology
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC₅₀ of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.

HY-13515

Sirtinol
Sirtuin Autophagy Apoptosis Cancer

Sirtinol is a sirtuin (SIRT) inhibitor, with IC₅₀s of 48 μM, 57.7 μM and 131 μM for ySir2, hSIRT2 and hSIRT2, respectively.
HY-12012

SB 216763
GSK-3 Autophagy Neurological Disease Cancer

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC₅₀s of 34.3 nM for both GSK-3α and GSK-3β.

HY-15301

CC0651	E1/E2/E3 Enzyme	Cancer
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC₅₀=1.72 μM) inhibits the ubiquitination of p27^Kip1, as confirmed by dose-response analysis.

HY-18708

Erdafitinib JNJ-42756493	FGFR Apoptosis	Cancer
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC₅₀s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

HY-126750

GNF362	Phosphatase	Inflammation/Immunology
GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC₅₀ of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC₅₀ values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca²⁺-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].

HY-N6782

Oligomycin	ATP Synthase Fungal Antibiotic	Cancer Infection
Oligomycin, an antifungal antibiotic, is an inhibitor of H⁺-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.

HY-13016

Cabozantinib XL184; BMS-907351	VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis	Cancer
Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

HY-120088A

PF-06446846 hydrochloride	Ser/Thr Protease	Cardiovascular Disease
PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34.

HY-101957

AG 1295	PDGFR	Cardiovascular Disease
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.

HY-B0975

Penicillin V Potassium Phenoxymethylpenicillin potassium salt	Bacterial Antibiotic	Infection
Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus, and can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.

HY-N2575

Hypocrellin A	PKC	Cancer Infection
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).

HY-130122

MG-277	PROTAC Apoptosis	Cancer
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC₅₀ of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC₅₀s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.

HY-N3945

Glaucine O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396	Phosphodiesterase (PDE) Calcium Channel Adrenergic Receptor Dopamine Receptor Influenza Virus	Infection Inflammation/Immunology
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with K_is of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca²⁺ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.

HY-N0834

Pulsatilla saponin D
SB365; Hederacolchiside A
Apoptosis Cancer

Pulsatilla saponin D (SB365), isolated from the root of Pulsatilla koreana Nakai, is an anti-tumor agent.
HY-10935

LY450108
iGluR Neurological Disease

LY450108 is a potent AMPA receptor potentiator. LY450108 has the potential for depression and Parkinson's disease research.
HY-126525

4-N3Pfp-NHS ester
ADC Linker Cancer

4-N3Pfp-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-13685

Miltefosine HePC; Hexadecyl phosphocholine	Akt HIV	Infection Cancer
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).

HY-103443

HKI-357	EGFR	Cancer
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC₅₀s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.

HY-10460

PF-431396	Pyk2 FAK	Cancer
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC₅₀ values of 2 nM and 11 nM, respectively.

HY-136610

Chlorpyrifos-oxon	AChE	Neurological Disease
Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.

HY-13564A

Batimastat sodium salt BB-94 sodium salt	MMP	Cancer
Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC₅₀ of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

HY-B0190A

Nafamostat mesylate FUT-175	Ser/Thr Protease Apoptosis SARS-CoV	Cardiovascular Disease Cancer
Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..

HY-B0190

Nafamostat	Ser/Thr Protease Apoptosis SARS-CoV	Cardiovascular Disease
Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.

HY-13564

Batimastat
BB94
MMP Cancer

Batimastat is a potent broad spectrum MMP inhibitor with IC₅₀ of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.

HY-B0190B

Nafamostat hydrochloride	Ser/Thr Protease Apoptosis SARS-CoV	Cardiovascular Disease
Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..

HY-B1813A

(±)-Vesamicol hydrochloride (±)-AH5183 hydrochloride	Sigma Receptor	Neurological Disease
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a K_i of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with K_is of 26 nM and 34 nM, respectively.

HY-12031

U0126-EtOH	MEK Autophagy Mitophagy Influenza Virus	Cancer
U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

HY-127039

Antipain	Ser/Thr Protease DNA/RNA Synthesis	Cancer Metabolic Disease
Antipain is a protease inhibitor isolated from Actinomycetes. Antipain inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain restricts uterine DNA synthesis and function in mice.

HY-127034

Antipain dihydrochloride	Ser/Thr Protease DNA/RNA Synthesis	Cancer Metabolic Disease
Antipain dihydrochloride is a protease inhibitor isolated from Actinomycetes. Antipain dihydrochloride inhibits N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced transformation and increases chromosomal aberrations. Antipain dihydrochloride restricts uterine DNA synthesis and function in mice.

HY-136559

6-Azathymine	Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial Influenza Virus	Infection
6-Azathymine, a 6-nitrogen analog of thymine, is a potent D-3-aminoisobutyrate-pyruvate aminotransferase inhibitor. 6-Azathymine inhibits the biosynthesis of DNA, and has antibacterial and antiviral activities.

HY-P1236

Atrial Natriuretic Peptide (ANP) (1-28), rat Atrial natriuretic factor (1-28) (rat)	Endothelin Receptor	Cardiovascular Disease Endocrinology
Atrial Natriuretic Peptide (ANP) (1-28), rat is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.

HY-Y0892

4-Hydroxybenzyl alcohol	Apoptosis Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
4-Hydroxybenzyl alcohol is a phenolic compound widely distributed in various kinds of plants. Anti-inflammatory, anti-oxidant, anti-nociceptive activity. Neuroprotective effect. Inhibitor of tumor angiogenesis and growth.

HY-10162

Olaparib AZD2281; KU0059436	PARP Autophagy Mitophagy	Cancer
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.

HY-136195

TL13-110
ALK Cancer

TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC₅₀ of 0.34 nM. TL13-110 does not degrade ALK in cells.

HY-P1204

[Ala17]-MCH	MCHR1 (GPR24)	Metabolic Disease
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR₁ (K_i=0.16 nM) over MCHR₂ (K_i=34 nM). [Eu³⁺ chelate-labeled [Ala17]-MCH shows high affnity for MCHR₁ (K_d=0.37 nM) while has little demonstrable binding affnity for MCHR₂.

HY-12429

Beclabuvir BMS-791325	HCV	Infection
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC₅₀ of < 28 nM.

HY-13570A

Betamethasone hydrochloride	Glucocorticoid Receptor Apoptosis	Inflammation/Immunology Endocrinology
Betamethasone hydrochloride is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone hydrochloride accelerates fetal lung maturation and induces gene expression and apoptosis.

HY-13570

Betamethasone	Glucocorticoid Receptor Apoptosis	Inflammation/Immunology Endocrinology Cancer
Betamethasone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activities. Betamethasone accelerates fetal lung maturation and induces gene expression and apoptosis.

HY-P1236A

Atrial Natriuretic Peptide (ANP) (1-28), rat TFA Atrial natriuretic factor (1-28) (rat) TFA	Endothelin Receptor	Cardiovascular Disease Endocrinology
Atrial Natriuretic Peptide (ANP) (1-28), rat (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.

HY-12445

CDKI-73	CDK Apoptosis	Cancer
CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).

HY-B0348

Liranaftate Piritetrate; M-732	Fungal	Infection
Liranaftate (Piritetrate) is a squalene epoxidase inhibitor with anti-fungicidal activities. Liranaftate can be used for the research of dermatophytes. Liranaftate also suppresses fungal element-promoted production of IL-8 and experimental inflammation.

HY-15602A

Ledipasvir (acetone) GS-5885 acetone	HCV	Infection
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC₅₀ values of 34 pM against GT1a and 4 pM against GT1b replicon.

HY-13524A

AG-1478 hydrochloride Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride	EGFR HCV Influenza Virus	Cancer Infection Metabolic Disease Cardiovascular Disease
AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

HY-15141

Staurosporine Antibiotic AM-2282; STS; AM-2282	PKC PKA Apoptosis Bacterial Fungal Antibiotic	Cancer Infection
Staurosporine is a potent and non-selective inhibitor of protein kinases with IC₅₀s of 6 nM, 15 nM, 2 nM, and 3 nM for PKC, PKA, c-Fgr, and Phosphorylase kinase respectively. Staurosporine is an apoptosis inducer.

HY-P1204A

[Ala17]-MCH TFA	MCHR1 (GPR24)	Metabolic Disease
[Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR₁ (K_i=0.16 nM) over MCHR₂ (K_i=34 nM). [Eu³⁺ chelate-labeled [Ala17]-MCH shows high affnity for MCHR₁ (K_d=0.37 nM) while has little demonstrable binding affnity for MCHR₂.

HY-B1479C

Emetine hydrochloride	Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic	Infection
Emetine hydrochloride, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine hydrochloride inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine hydrochloride potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.

HY-B1479

Emetine	Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic	Infection
Emetine, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.

HY-B1479B

Emetine dihydrochloride hydrate	Parasite DNA/RNA Synthesis Autophagy Bacterial Antibiotic	Infection Cancer
Emetine dihydrochloride hydrate, derived from the ipecac root, is a potent anti-protozoal and emetic agent. Emetine dihydrochloride hydrate inhibits viral polymerases and inhibits Zika and Ebola virus infections. Emetine dihydrochloride hydrate potently inhibits autophagy and has anti-malarial, anti-bacterial and anti-amoebic effect.

HY-125658

Biotinyl tyramide	Others	Others
Biotinyl tyramide is a biotin derivative used for tyramide signal amplification (TSA), as a reagent to amplify both immunohistochemical signals and in situ hybridization protocols.

HY-106244A

DOTATATE acetate	Others	Cancer
DOTATATE acetate, a DOTA-conjugated peptide, and can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).

HY-N0344

Farrerol	Others	Cancer Inflammation/Immunology Neurological Disease
Farrerol is a bioactive constituent of Rhododendron, with broad activities such as anti-oxidative, anti-inflammatory, anti-tumor, neuroprotective and hepatoprotective effects.

HY-41076

Ca2+ channel agonist 1	Calcium Channel CDK	Neurological Disease
Ca²⁺ channel agonist 1 is an agonist of N-type Ca²⁺ channel and an inhibitor of Cdk2, with EC₅₀s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.

HY-15666

GZD824 HQP1351	Bcr-Abl	Cancer
GZD824 (HQP1351) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC₅₀=0.34 nM). GZD824 has antitumor activity.

HY-B1370A

(S)-Hydroxychloroquine (S)-HCQ	Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy	Infection
(S)-Hydroxychloroquine ((S)-HCQ) is the enantiomer of Hydroxychloroquine. Hydroxychloroquine, a synthetic antimalarial drug, inhibits Toll-like receptor 7/9 (TLR7/9) signaling, and shows efficiently inhibits SARS-CoV-2 infection in vitro.

HY-12044

Cabozantinib S-malate XL184 S-malate; BMS-907351 S-malate	VEGFR Apoptosis	Cancer
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

HY-B0640

Epinastine WAL801	Histamine Receptor	Inflammation/Immunology Endocrinology
Epinastine (WAL801) is an antihistamine and mast cell stabilizer. Epinastine is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine also inhibits IL-8 release and has an antiallergic action.

HY-100443A

PX20606 trans racemate PX-102 trans racemate	FXR Autophagy	Metabolic Disease
PX20606 trans racemate (PX-102 trans racemate) is a FXR agonist with EC₅₀s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.

HY-B2068

Iron sucrose Iron saccharate	Reactive Oxygen Species	Metabolic Disease
Iron sucrose (Iron saccharate) is a intravenous iron preparation and a pro-oxidant agent. Iron sucrose has the potential for iron deficiency anemia treatment.

HY-10003

Alfacalcidol 1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3	VD/VDR	Metabolic Disease
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.

HY-106369

HMR 1556	Potassium Channel	Cardiovascular Disease
HMR 1556, a chromanol derivative, is a potent I_Ks blocker with IC₅₀s of 10.5 nM and 34 nM in canine and guinea pig left ventricular myocytes, respectively.

HY-101019

Ossirene AS101	Interleukin Related Caspase	Cancer Inflammation/Immunology
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.

HY-12842

UC-112	IAP	Cancer
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).

HY-B1370B

(R)-Hydroxychloroquine (R)-HCQ	Parasite Toll-like Receptor (TLR) SARS-CoV Autophagy	Infection
(R)-Hydroxychloroquine is the enantiomer of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.

HY-B1617A

Zuclomiphene citrate	Estrogen Receptor/ERR	Endocrinology Metabolic Disease
Zuclomiphene citrate is a cis isomer of Clomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.

HY-101047

D-erythro-Sphingosine Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine	PKC Phosphatase Endogenous Metabolite	Cancer
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC₅₀ of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.

HY-100228A

SKF89976A hydrochloride d,l-SKF89976A hydrochloride	GABA Receptor	Neurological Disease
SKF89976A hydrochloride is a selective GABA transporter (GAT-1) inhibitor with IC₅₀s of 0.28 μM, 137.34 μM and 202.8 μM for GAT-1, GAT-2 and GAT-3 in CHO cells, respectively.

HY-W030545

(4-Oxo-4H-quinazolin-3-yl)-acetic acid
PROTAC Linker Cancer

(4-Oxo-4H-quinazolin-3-yl)-acetic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.

HY-N0809

Sesamolin	p38 MAPK JNK Caspase	Metabolic Disease Neurological Disease
Sesaminol, isolated from Justicia orbiculata, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression.

HY-17443

Sivelestat EI546; LY544349; ONO5046	Elastase SARS-CoV	Cancer
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

HY-17443A

Sivelestat sodium ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium	Elastase SARS-CoV	Cancer
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

HY-117832

Pyripyropene A	Acyltransferase	Infection Inflammation/Immunology Cardiovascular Disease
Pyripyropene A is a potent and selective sterol O-acyltransferase 2 (SOAT2)/acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2) inhibitor, with an IC₅₀ of 0.07 µM. Pyripyropene A attenuates hypercholesterolemia and atherosclerosis in vivo.

HY-15666A

GZD824 dimesylate HQP1351 dimesylate	Bcr-Abl	Cancer
GZD824 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC₅₀=0.34 nM). GZD824 dimesylate has antitumor activity.

HY-101146

SF2523	PI3K Epigenetic Reader Domain DNA-PK	Cancer
SF2523 is a highly selective and potent inhibitor of PI3K with IC₅₀s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

HY-W009156

Hydroxycitric acid tripotassium hydrate Potassium citrate monohydrate	ATP Citrate Lyase HIF/HIF Prolyl-Hydroxylase	Cancer Metabolic Disease Inflammation/Immunology
Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) is the major active ingredient of Garcinia cambogia and a derivative of citric acid. Hydroxycitric acid tripotassium hydrate competitively inhibits ATP citrate lyase with weight loss benefits. Hydroxycitric acid tripotassium hydrate effective inhibits stones formation and also inhibits HIF, and has antioxidation, anti-inflammation and anti-tumor effects.

HY-108900

Leu-AMS	Aminoacyl-tRNA Synthetase Bacterial	Cancer Infection
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC₅₀ of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.

HY-P0118

Disitertide P144	TGF-beta/Smad PI3K Apoptosis	Cancer
Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.

HY-128855

Talsaclidine	mAChR	Neurological Disease
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.

HY-N0150

Monensin sodium salt Monensin A sodium salt	Bacterial Sodium Channel Antibiotic	Infection Cancer
Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Monensin sodium salt is an ionophore that mediates Na⁺/H⁺ exchange. Monensin sodium salt causes a marked enlargement of the MVBs and regulates exosome secretion.

HY-12512

cGAMP Cyclic GMP-AMP; 3',3'-cGAMP	STING	Inflammation/Immunology
cGAMP (Cyclic GMP-AMP; 3',3'-cGAMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.

HY-B1617AS

Zuclomiphene D4 citrate	Estrogen Receptor/ERR	Endocrinology Metabolic Disease
Zuclomiphene D4 citrate is a deuterium labeled Zuclomiphene citrate. Zuclomiphene citrate has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer. Zuclomiphene citrate is also an orally active hypocholesterolemic agent.

HY-N0907

Ginsenoside Rg6	NF-κB Apoptosis	Cancer Inflammation/Immunology
Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC₅₀ of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.

HY-114334

Glutaminase-IN-1 CB839 derivative	Glutaminase	Cancer
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC₅₀ of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.

HY-10446

Pralatrexate	Antifolate Apoptosis	Cancer
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a K_i of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.

HY-15416

NS309	Potassium Channel	Neurological Disease Cardiovascular Disease
NS309 is a potent and selective opener of the small or intermediate conductance Ca²⁺-activated K⁺ (SK or IK, respectively) channels, but displays no activity at BK channels.

HY-N7699E

D-Heptamannuronic acid	Others	Neurological Disease
D-Heptamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Heptamannuronic acid can be used for the research of pain and vascular dementia.

HY-N7699C

D-Pentamannuronic acid	Others	Neurological Disease
D-Pentamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Pentamannuronic acid can be used for the research of pain and vascular dementia.

HY-15744

LY255283
Leukotriene Receptor Cancer Inflammation/Immunology

LY255283 is a LTB₄ receptor (BLT2) antagonist, with an IC₅₀ of ~100 nM for [³H]LTB₄ binding to guinea pig lung membranes.

HY-N7699F

D-Octamannuronic acid	Others	Neurological Disease
D-Octamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Octamannuronic acid can be used for the research of pain and vascular dementia.

HY-N7699G

D-Nonamannuronic acid	Others	Neurological Disease
D-Nonamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Nonamannuronic acid can be used for the research of pain and vascular dementia.

HY-N7699B

D-Tetramannuronic acid	Others	Neurological Disease
D-Tetramannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Tetramannuronic acid can be used for the research of pain and vascular dementia.

HY-N7699D

D-Hexamannuronic acid	Others	Neurological Disease
D-Hexamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Hexamannuronic acid can be used for the research of pain and vascular dementia.

HY-107416

RHC 80267 U-57908	Acyltransferase mAChR COX Phospholipase	Metabolic Disease Neurological Disease
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC₅₀ of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC₅₀ of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).

HY-N4149

Quercetagetin 6-Hydroxyquercetin	Pim	Cancer Inflammation/Immunology
Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC₅₀, 0.34 μM). Anti-inflammatory and anticancer properties.

HY-14590

Kaempferol Kempferol; Robigenin	Estrogen Receptor/ERR Autophagy Mitophagy Apoptosis HIV Parasite Endogenous Metabolite	Cancer
Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.

HY-B0764

Bucladesine sodium Dibutyryl cAMP sodium salt; DBcAMP sodium salt	PKA Phosphodiesterase (PDE)	Inflammation/Immunology
Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.

HY-17443B

Sivelestat sodium tetrahydrate EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate	Elastase SARS-CoV	Cancer
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

HY-10529

Betulinic acid Lupatic acid; Betulic acid	Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite	Cancer Infection Inflammation/Immunology
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.

HY-122898

Ru360	Calcium Channel Mitochondrial Metabolism	Cardiovascular Disease
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca²⁺ uptake into mitochondria with an IC₅₀ of 0.184 nM. Ru360 binds to mitochondria with high affinity (K_d of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects.

HY-N2450

Sulforaphene	Apoptosis EGFR ERK NF-κB	Cancer
Sulforaphene, isolated from radish seeds, exhibits an ED₅₀ against velvetleaf seedlings approximately 2 x 10^-4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.

HY-P0118A

Disitertide TFA P144 TFA	TGF-beta/Smad PI3K Apoptosis	Cancer
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.

HY-16952A

Bepridil hydrochloride hydrate (±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate	Calcium Channel	Cardiovascular Disease
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca⁺ channel antagonist and Na⁺, K⁺ channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na⁺/Ca2⁺ exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.

HY-N2071

Cedrol (+)-Cedrol; α-Cedrol	Cytochrome P450 Fungal	Infection Inflammation/Immunology Cancer
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with K_i of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.

HY-15724A

Vercirnon sodium GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium	CCR	Inflammation/Immunology Endocrinology
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca²⁺ mobilization and chemotaxis on Molt-4 cells with IC₅₀ values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC₅₀s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC₅₀ values of 2.8 and 2.6 nM, respectively.

HY-15724

Vercirnon GSK-1605786; CCX282-B; Traficet-EN	CCR	Inflammation/Immunology Endocrinology
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca²⁺ mobilization and chemotaxis on Molt-4 cells with IC₅₀ values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC₅₀s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC₅₀ values of 2.8 and 2.6 nM, respectively.

HY-141274

4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenol	PROTAC Linker	Cancer
4-(6-Methyl-1,2,4,5-tetrazin-3-yl)phenol is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-14144

Aclidinium Bromide LAS 34273; LAS-W 330	mAChR	Inflammation/Immunology
Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research.

HY-101731

CP-96021 hydrochloride	Leukotriene Receptor	Inflammation/Immunology
CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with K_i values of 34 nM and 37 nM, respectively.

HY-12151

NS 1738 NSC 213859	nAChR	Neurological Disease
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC₅₀=3.4 μM in oocyte experiments).

HY-126145

S1PR1 modulator 1	LPL Receptor	Inflammation/Immunology
S1PR1 modulator 1 is a selective S1PR1 inhibitor, with a pIC₅₀ of 7.6, with >40- and >80-fold selectivity, over the other S1PR isoforms S1PR2/3/4.

HY-A0088

Cefotaxime sodium salt Cefotaxim sodium salt; HR-756 sodium salt	Bacterial Antibiotic	Infection
Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria.

HY-N0819

Raddeanin A	Apoptosis	Cancer
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.

HY-A0088A

Cefotaxime Cefotaxim; HR-756	Bacterial Antibiotic	Infection Inflammation/Immunology
Cefotaxime, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria.

HY-14171S

Bexarotene D4 LGD1069 D4	RAR/RXR Autophagy	Cancer
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.

HY-N7062

JNJ-1661010 Takeda-25	FAAH	Neurological Disease
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC₅₀s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.

HY-15340

LG100268 LG268	RAR/RXR Autophagy	Metabolic Disease
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC₅₀ values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the K_i values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.

HY-133887

Methotrexate α-tert-butyl ester	Antifolate DNA/RNA Synthesis	Cancer
Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent.

HY-126562

Piperlonguminine	Bacterial Fungal	Cancer Infection Inflammation/Immunology Neurological Disease Cardiovascular Disease
Piperlonguminine is an alkaloid amide isolated from the Piper species. Piperlonguminine shows various biological properties, including anti-inflammatory, antitumor, neuroprotective, anti-platelet, anti-melanogenic, antifungal and antibacterial activities.

HY-B0743A

Pipecuronium bromide	nAChR	Neurological Disease
Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM.

HY-17363S

Dimethyl fumarate D6 DMF D6	Keap1-Nrf2	Inflammation/Immunology
Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.

HY-B1866

Linuron	Androgen Receptor	Endocrinology
Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a K_i of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.

HY-10046

Plerixafor AMD 3100; JM3100; SID791	CXCR HIV Virus Protease	Cancer Infection Endocrinology Inflammation/Immunology
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-140347

APN-C3-NH-Boc tert-Butyl 3-(4-(2-cyanoethynyl)phenylcarbamoyl)propylcarbamate	PROTAC Linker	Cancer
APN-C3-NH-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-112729

HC-056456 3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide	Others	Others
HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na⁺]_i rise is slowed by HC-056456 (IC₅₀~3 µM).

HY-W016622

Watermelon ketone 7-Methyl-2H-1,5-benzodioxepin-3(4H)-one	Others	Others
Watermelon ketone is fragrance chemical compound with special odorant which has been widely used in the fragrance industry, extracted from patent CN 103058984 A.

HY-13755

Sulforaphane	HDAC Keap1-Nrf2 Apoptosis	Cancer Inflammation/Immunology
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.

HY-119757

Tyrphostin AG1433 SU1433; AG1433	PDGFR VEGFR	Cancer
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC₅₀s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.

HY-P1189

Echistatin	Integrin	Metabolic Disease Inflammation/Immunology
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of α_IIbβ₃, α_vβ₃ and *α₅β₁*.

HY-12481

SAR405	PI3K Autophagy	Cancer
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform *Vps34* inhibitor (IC₅₀=1.2 nM; K_d=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.

HY-N0814

Phytic acid Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)	Xanthine Oxidase Endogenous Metabolite	Inflammation/Immunology Neurological Disease
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.

HY-107613

R 59-022 DKGI-I; Diacylglycerol kinase inhibitor I	PKC 5-HT Receptor	Inflammation/Immunology
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC₅₀=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.

HY-19373

RWJ-445167 3DP-10017	Thrombin Factor Xa	Cardiovascular Disease
RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with K_i of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.

HY-103354

Proglumide sodium	Cholecystokinin Receptor	Cancer Endocrinology Neurological Disease
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.

HY-101768

PRN1371	FGFR c-Fms	Cancer
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC₅₀s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.

HY-B1322A

Amodiaquine Amodiaquin	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-10014

R547	CDK GSK-3 Apoptosis	Cancer
R547 is a potent, selective and oral orally bioavailable ATP-competitive CDK inhibitor, with K_is of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.

HY-107856

5-Fluorouridine	Others	Cancer
5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC₅₀ of 2 nM.

HY-N2435

[8]-Shogaol	COX Apoptosis	Cancer
[8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC₅₀=5 μM) and inhibits COX-2 (IC₅₀=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.

HY-B1330

Proglumide	Cholecystokinin Receptor	Cancer Endocrinology Neurological Disease
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.

HY-136265

BC-LI-0186	Aminoacyl-tRNA Synthetase	Cancer
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC₅₀=46.11 nM). BC-LI-0186 competively binds to the RagD interacting site of LRS (K_d=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.

HY-U00439A

*Protein kinase inhibitors* 1 hydrochloride** (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride	DYRK	Cancer
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC₅₀s of 136 and 74 nM for HIPK1 and HIPK2, and a K_d of 9.5 nM for HIPK2.

HY-17507

Pantoprazole BY1023; SKF96022	Proton Pump Autophagy Apoptosis	Cancer Inflammation/Immunology
Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H⁺/K⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).

HY-N0814A

Phytic acid dodecasodium salt hydrate Inositol hexaphosphate dodecasodium salt hydrate; myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate	Xanthine Oxidase Endogenous Metabolite	Inflammation/Immunology Neurological Disease
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.

HY-P1189A

Echistatin TFA	Integrin	Metabolic Disease Inflammation/Immunology
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of α_IIbβ₃, α_vβ₃ and *α₅β₁*.

HY-17507B

Pantoprazole sodium hydrate BY1023 sodium hydrate; SKF96022 sodium hydrate	Proton Pump Autophagy Apoptosis	Cancer Inflammation/Immunology
Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H⁺/K⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).

HY-17507A

Pantoprazole sodium BY1023 sodium; SKF96022 sodium	Proton Pump Autophagy Apoptosis	Cancer Inflammation/Immunology
Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H⁺/K⁺-ATPase inhibitor with an IC₅₀ of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).

HY-15785

TAS-116	HSP	Cancer
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (K_is of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.

HY-135731

4-Methylamino antipyrine	COX Drug Metabolite	Inflammation/Immunology
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.

HY-17589

Chloroquine phosphate	Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic	Cancer Infection Inflammation/Immunology
Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

HY-17589B

Chloroquine dihydrochloride	Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic	Cancer Infection Inflammation/Immunology
Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

HY-N5077

Sinapine	AChE P-glycoprotein	Cancer Inflammation/Immunology Neurological Disease
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

HY-B1836

Mildronate Meldonium; MET-88; Quaterin	Others	Metabolic Disease Cardiovascular Disease
Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC₅₀ values of 34-62 μM for human recombinant BBOX and an EC₅₀ of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.

HY-135731A

4-Methylamino antipyrine hydrochloride	COX Drug Metabolite	Inflammation/Immunology
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.

HY-12278

K02288	TGF-β Receptor	Others
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC₅₀s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC₅₀s of of 5-34 nM.

HY-50904

Nintedanib BIBF 1120	PDGFR VEGFR FGFR	Cancer
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC₅₀s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-17589A

Chloroquine	Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV Antibiotic	Cancer Infection Inflammation/Immunology
Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

HY-107457

AZD-8529	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-B0968A

Trimetazidine	Autophagy	Cardiovascular Disease
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC₅₀ of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

HY-15463

Imatinib STI571; CGP-57148B	Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy	Cancer
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

HY-B0968

Trimetazidine dihydrochloride	Autophagy	Cardiovascular Disease
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC₅₀ of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.

HY-N4308

Hexamethylquercetagetin Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone	Others	Cancer
Hexamethylquercetagetin is a polymethoxylated flavone in peels of citrus cultivars.

HY-N0527

Pentagalloylglucose Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose	Influenza Virus	Infection
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.

HY-N6840

Xylotetraose	Others	Others
Xylotetraose is a hydrolysis product of Xylan. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose. Xylotetraose can be used for enzyme biochemical analysis.

HY-N6779

Patulin Terinin	Bacterial Apoptosis Antibiotic	Infection
Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin (Terinin) induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.

HY-15128

9-cis-Retinoic acid ALRT1057	RAR/RXR Apoptosis	Cancer Inflammation/Immunology Neurological Disease
9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities.

HY-P1076

CALP2	Calcium Channel Phosphodiesterase (PDE)	Inflammation/Immunology
CALP2 is a calmodulin (CaM) antagonist ( (K_d of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca²⁺-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca²⁺ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.

HY-B1322

Amodiaquine dihydrochloride dihydrate Amodiaquin dihydrochloride dihydrate	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-11106

Nintedanib esylate BIBF 1120 esylate	PDGFR VEGFR FGFR	Cancer
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC₅₀s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.

HY-103354A

Proglumide hemicalcium	Cholecystokinin Receptor	Cancer Endocrinology Neurological Disease
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.

HY-N5077B

Sinapine hydroxide	AChE P-glycoprotein	Cancer Inflammation/Immunology Neurological Disease
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

HY-10987A

ENMD-2076	Aurora Kinase FLT3 VEGFR FGFR PDGFR Src Apoptosis	Cancer
ENMD-2076 is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, *Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα*, respectively.

HY-B1322B

Amodiaquine dihydrochloride Amodiaquin dihydrochloride	Parasite Histone Methyltransferase	Infection Inflammation/Immunology Neurological Disease
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a K_i of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

HY-18641

Ki16198	LPL Receptor	Cancer
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA₁ and LPA₃-induced inositol phosphate production with K_i values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo.

HY-B1836A

Mildronate dihydrate Meldonium dihydrate; MET-88 dihydrate; Quaterin dihydrate	Others	Metabolic Disease Cardiovascular Disease
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC₅₀ values of 34-62 μM for human recombinant BBOX and an EC₅₀ of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.

HY-N0450

Sinapine thiocyanate	P-glycoprotein AChE	Cancer
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.

HY-15486

Salubrinal	Phosphatase HSV Autophagy Apoptosis	Cancer Infection Inflammation/Immunology
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.

HY-B1640

Ethacrynic acid	Gutathione S-transferase NF-κB Calcium Channel	Cancer Inflammation/Immunology
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.

HY-116767

BLT-1	HCV	Metabolic Disease Inflammation/Immunology
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor. BLT-1 has pro-inflammatory functions through neutrophil recruitment.

HY-79135

Pasireotide ditrifluoroacetate SOM230 ditrifluoroacetate; Pasireotide TFA salt	Somatostatin Receptor	Endocrinology Cancer
Pasireotide (ditrifluoroacetate) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively).

HY-103642

D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt Inositol 1,4,5-trisphosphate hexapotassium salt; Ins(1,4,5)-P3 hexapotassium salt	Others	Metabolic Disease
D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt is the hexapotassium salt of D-myo-Inositol 1,4,5-trisphosphate (1,4,5-IP3), which is a second messenger that stimulates the discharge of calcium from the endoplasmic reticulum.

HY-107457A

AZD-8529 mesylate	mGluR	Neurological Disease
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-W012037

8-Hydroxyquinoline hemisulfate 8-Quinolinol hemisulfate	Bacterial Antibiotic	Infection
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.

HY-N6687

Calcimycin A-23187; Antibiotic A-23187	Bacterial Fungal Apoptosis Autophagy Antibiotic	Cancer Infection
Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca²⁺-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.

HY-B0537A

Pentamidine dihydrochloride MP-601205 dihydrochloride	Parasite Fungal Phosphatase Bacterial Antibiotic	Cancer Infection
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite *Leishmania infantum* with an IC₅₀ of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

HY-B0537

Pentamidine MP-601205	Parasite Fungal Phosphatase Bacterial Antibiotic	Cancer Infection
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite *Leishmania infantum* with an IC₅₀ of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

HY-100530D

Rp-cAMPS sodium salt	PKA	Neurological Disease
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (K_is of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.

HY-15794

Nemorubicin Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243	Others	Cancer
Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.

HY-100530A

Rp-cAMPS	PKA	Neurological Disease
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (K_is of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.

HY-W001187

Tempo	DNA/RNA Synthesis Reactive Oxygen Species Mitochondrial Metabolism	Cancer
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects.

HY-N0587

Demethylzeylasteral	Apoptosis	Cancer Inflammation/Immunology
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.

HY-10510

BI-D1870	Ribosomal S6 Kinase (RSK) Autophagy	Cancer
BI-D1870 is an ATP-competitive, cell permeable inhibitor of RSK isoforms, with IC₅₀s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.

HY-100360

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

HY-10583

Y-27632 dihydrochloride	ROCK Apoptosis	Cancer
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with K_is of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.

HY-10987

ENMD-2076 Tartrate	Aurora Kinase FLT3 VEGFR FGFR Src PDGFR Apoptosis	Cancer
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, *Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα*, respectively.

HY-15652

Freselestat ONO-6818; ONO-PO-736	Elastase	Inflammation/Immunology
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a K_i of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.

HY-131275

Imatinib Impurity E	Others	Others
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.

HY-P1214

γ1-MSH	Melanocortin Receptor	Cardiovascular Disease
γ1-MSH is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH displays ~40-fold selectivity over MC4 (K_i=1318 nM).

HY-79136

Pasireotide L-aspartate salt SOM230 L-aspartate	Somatostatin Receptor	Cancer Endocrinology
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).

HY-P1076A

CALP2 TFA	Calcium Channel Phosphodiesterase (PDE)	Inflammation/Immunology
CALP2 TFA is a calmodulin (CaM) antagonist (K_d of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca²⁺-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca²⁺ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.

HY-13821

Epoxomicin BU-4061T	Proteasome Apoptosis	Cancer Inflammation/Immunology
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.

HY-106634

Mitoguazone Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG	HIV Apoptosis	Cancer Infection
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.

HY-115292

Simvastatin hydroxy acid sodium Tenivastatin sodium; Simvastatin Impurity A sodium	HMG-CoA Reductase (HMGCR)	Cancer
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a K_i value of 0.12 nM.

HY-13948

Angiotensin II human Angiotensin II; Ang II; DRVYIHPF	Angiotensin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT₁ receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.

HY-13948A

Angiotensin II human acetate Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate	Angiotensin Receptor Apoptosis	Cancer Endocrinology Cardiovascular Disease
Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT₁ receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis.

HY-108538

Ethacrynic acid D5	Gutathione S-transferase NF-κB Calcium Channel	Inflammation/Immunology
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.

HY-100530

Rp-cAMPS triethylammonium salt	PKA	Neurological Disease
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (K_is of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.

HY-13676

Megestrol acetate	Progesterone Receptor Autophagy HIV	Endocrinology Cancer
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.

HY-135147

ONC206	Dopamine Receptor	Cancer Neurological Disease
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors *(DRD2/3/4)* at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.

HY-15414S

Vortioxetine D8 Lu AA 21004 D8	5-HT Receptor Serotonin Transporter	Neurological Disease
Vortioxetine D8 is a deuterium labeled Vortioxetine. Vortioxetine is an inhibitor of 5-HT_1A, 5-HT_1B, 5-HT_3A, 5-HT₇ receptor and SERT, with K_i values of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

HY-128862

EGFR-IN-7	EGFR	Cancer
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC₅₀s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.

HY-13716

Noscapine (S,R)-Noscapine	Opioid Receptor Apoptosis	Cancer Inflammation/Immunology Neurological Disease
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.

HY-17589AS

Chloroquine D5	Parasite Autophagy SARS-CoV Toll-like Receptor (TLR) HIV	Cancer Infection Inflammation/Immunology
Chloroquine D5 is deuterium labeled Chloroquine. Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC₅₀=1.13 μM).

HY-126047B

(R)-(+)-Anatabine	NF-κB Amyloid-β nAChR	Inflammation/Immunology Neurological Disease
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

HY-13716A

Noscapine hydrochloride (S,R)-Noscapine hydrochloride	Opioid Receptor Apoptosis	Cancer Inflammation/Immunology Neurological Disease
Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.

HY-10322

Falnidamol BIBX 1382	EGFR	Cancer
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC₅₀ of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC₅₀=3.4 μM) and a range of other related tyrosine kinases (IC₅₀>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.

HY-111415

EGFR-IN-5
EGFR Cancer

EGFR-IN-5 is a EGFR inhibitor with IC₅₀s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR^L858R, EGFR^L858R/T790M, and EGFR^{L858R/T790M/C797S}, respectively.

HY-B0537B

Pentamidine isethionate MP-601205 isethionate	Parasite Fungal Phosphatase Bacterial Antibiotic	Infection Cancer
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite *Leishmania infantum* with an IC₅₀ of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.

HY-100999

(R)-(-)-α-Methylhistamine dihydrobromide	Histamine Receptor	Neurological Disease
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective H3 histamine receptor agonist with a K_d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can cross the blood-brain barrier, and can enhance memory retention, attenuates memory impairment in rats.

HY-P1214A

γ1-MSH TFA	Melanocortin Receptor	Cardiovascular Disease
γ1-MSH TFA is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH TFA displays ~40-fold selectivity over MC4 (K_i=1318 nM).

HY-W020182

α-Terpinene Terpilene	Fungal Parasite	Infection
α-Terpinene (Terpilene) is a monoterpene found in the essential oils of a large variety of foods and aromatic plants such as Mentha piperita. α-Terpinene is active against *Trypanosoma evansi* and has the potential for trypanosomosis treatment. α-Terpinene has antioxidant and antifungal properties.

HY-128463

N-tert-Butyl-α-phenylnitrone	COX Reactive Oxygen Species	Metabolic Disease Inflammation/Immunology Neurological Disease
N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier.

HY-N0095

(S)-10-Hydroxycamptothecin 10-HCPT; 10-Hydroxycamptothecin	Topoisomerase Apoptosis	Cancer
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.

HY-17386

Rosiglitazone BRL 49653	PPAR TRP Channel Autophagy Ferroptosis	Cancer Metabolic Disease Inflammation/Immunology Neurological Disease
Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a K_d of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC₅₀=~30 μM) and an inhibitor of *TRPM3*.

HY-15652A

Freselestat quarterhydrate ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate	Elastase	Inflammation/Immunology
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a K_i of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.

HY-13317S

Oseltamivir D3	Influenza Virus	Infection
Oseltamivir D3 is a deuterium labeled Oseltamivir. Oseltamivir is an influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC₅₀s of 0.67, 0.9, 1.34 and 13 nM, respectively. Anti-influenza A and B agent.

HY-10514

BX795	PDK-1 IKK Autophagy	Cancer
BX795 is a potent and selective inhibitor of PDK1, with an IC₅₀ of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC₅₀ of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates *autophagy*.

HY-N0498

Nitidine chloride	Parasite Apoptosis STAT Topoisomerase ERK FAK p38 MAPK NF-κB	Cancer Inflammation/Immunology
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.

HY-108485

Damnacanthal	Src Apoptosis Fungal	Cancer Infection Inflammation/Immunology
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56^lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 ^lck autophosphorylation and phosphorylation of exogenous substrates with IC₅₀s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.

HY-N6687B

Calcimycin hemimagnesium A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium	Bacterial Fungal Apoptosis Autophagy	Cancer Infection
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca²⁺-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces *apoptosis*.

HY-N6687A

Calcimycin hemicalcium salt A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt	Bacterial Fungal Apoptosis Autophagy Antibiotic	Cancer Infection
Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca²⁺-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces *apoptosis*.

HY-135813

LtaS-IN-1	Bacterial	Infection
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.

HY-113038

D-α-Hydroxyglutaric acid (R)-2-Hydroxypentanedioic acid	Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
D-α-Hydroxyglutaric acid ((R)-2-Hydroxypentanedioic acid) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a K_i of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.

HY-P1932

Cortistatin-14	Somatostatin Receptor	Inflammation/Immunology Neurological Disease Endocrinology
Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.

HY-76772

Cevimeline hydrochloride hemihydrate SNI-2011; AF102B hydrochloride hemihydrate	mAChR	Neurological Disease
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).

HY-70020B

Cevimeline hydrochloride AF102B hydrochloride	mAChR	Neurological Disease
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).

HY-100867A

TAK-659 hydrochloride	Syk FLT3	Cancer
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC₅₀ of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

HY-N7665

Prosaikogenin G	Others	Metabolic Disease
Prosaikogenin G, isolated from the roots of Buleurum bicaule Helm (Apiaceae), exhibits significant inhibitory effects on rat mesangial cell proliferation induced by Ang II. Prosaikogenin G has protective action on the kidney. Prosaikogenin G is a derivative of Saikosaponin d in the gastrointestinal tract.

HY-101918

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

HY-113498

Sphingomyelin	Endogenous Metabolite	Metabolic Disease Inflammation/Immunology Neurological Disease
Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.

HY-P1932A

Cortistatin-14 TFA	Somatostatin Receptor	Inflammation/Immunology Neurological Disease Endocrinology
Cortistatin-14 (TFA), a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 (TFA) shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties.

HY-14539S

Clozapine D8 HF 1854 D8	Dopamine Receptor mAChR	Neurological Disease
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a K_i of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

HY-70020

Cevimeline AF102B	mAChR	Neurological Disease
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).

HY-100490B

Rilmenidine phosphate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells ^[1].

HY-12972

Mavelertinib PF-06747775	EGFR	Cancer
Mavelertinib is a selective, orally available and irreversible *EGFR tyrosine kinase inhibitor* (EGFR TKI), with IC₅₀*s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).*

HY-N7647

Methyl brevifolincarboxylate Brevifolincarboxylic acid methyl ester	Influenza Virus	Infection
Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC₅₀s of 27.16 μM and 33.41 μM. Anti-oxidant activity.

HY-10115

PI-103	PI3K mTOR DNA-PK Autophagy Apoptosis	Cancer
PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces *autophagy*.

HY-12170

Prinomastat AG3340; KB-R9896	MMP	Cancer
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC₅₀s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with K_is of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.

HY-12170A

Prinomastat hydrochloride AG3340 hydrochloride; KB-R9896 hydrochloride	MMP	Cancer
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC₅₀s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with K_is of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.

HY-107024

Osteogenic Growth Peptide (10-14) OGP(10-14); Historphin	Src	Others
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.

HY-10115A

PI-103 Hydrochloride	PI3K mTOR DNA-PK Autophagy Apoptosis	Cancer
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces *autophagy*.

HY-113952

Actinonin (-)-Actinonin	Aminopeptidase Bacterial MMP Apoptosis Antibiotic	Cancer Infection
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a K_i of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with K_i values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.

HY-16787

ICA-121431	Sodium Channel	Cardiovascular Disease
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Na_v) blocker, shows equipotent selectivity for human Na_v1.1 and Na_v1.3 subtypes with IC₅₀ values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Na_v1.2 (IC₅₀=240 nM) and 1,000 fold selectivity against Na_v1.4, Na_v1.6, and the TTX-resistant human Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 µM).

HY-18728

STF-31
GLUT Autophagy Cancer

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].

HY-102022

α-Galactosylceramide α-GalCer; KRN7000	Others	Cancer Inflammation/Immunology
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).

HY-136429

Ethylhydrocupreine Optochin	Bacterial Parasite	Infection
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against *S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC₅₀* of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.

HY-136429A

Ethylhydrocupreine hydrochloride Optochin hydrochloride	Bacterial Parasite	Infection
Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against *S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC₅₀* of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.

HY-108768

Pasireotide pamoate SOM230 pamoate	Somatostatin Receptor	Cancer
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

HY-135795

1-Cyclohexyl-3-dodecyl urea CDU; N-Cyclohexyl-N-dodecyl urea; NCND	Epoxide Hydrolase	Metabolic Disease Cardiovascular Disease
1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.

HY-124662

IHVR-19029	Glucosidase	Infection
IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC₅₀ of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.

HY-101180

C2 Ceramide Ceramide 2	Phosphatase Mitochondrial Metabolism Apoptosis	Endocrinology Metabolic Disease
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.

HY-100490

Rilmenidine	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy	Cardiovascular Disease
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.

HY-125957

A-3 hydrochloride	PKA Casein Kinase CaMK PKC	Others
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (K_i=4.3 µM), casein kinase II (K_i=5.1 µM) and myosin light chain kinase (MLCK) (K_i=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with K_i values of 47 µM and 80 µM, respectively.

HY-W011109

CKI-7	Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK)	Cancer
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.

HY-100542

D-α-Hydroxyglutaric acid disodium Disodium (R)-2-hydroxyglutarate	Reactive Oxygen Species ATP Synthase mTOR Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a K_i of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling.

HY-12554

Terlipressin	Vasopressin Receptor	Endocrinology Inflammation/Immunology Cardiovascular Disease
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

HY-101299A

Dihydrexidine DAR-0100	Dopamine Receptor	Neurological Disease
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC₅₀ of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.

HY-12554A

Terlipressin acetate	Vasopressin Receptor	Endocrinology Inflammation/Immunology Cardiovascular Disease
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.

HY-13591

Piclidenoson IB-MECA; CF-101	Adenosine Receptor Apoptosis	Cancer
Piclidenoson (IB-MECA;CF-101) is a first-in-class, orally bioavailable and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.

HY-135416

Streptolysin O	Endogenous Metabolite	Infection
Streptolysin O, a group A streptococcal toxin, is a well-characterized oxygen-labile prototype of a cholesterol-binding bacterial exotoxin. Streptolysin O causes both lysis of cells and cardiotoxicity. Streptolysin O is widely used for the controlled permeabilization of cell membranes. Streptolysin O exists in two forms, a reduced active state and an oxidized reversibly inactive state.

HY-101299B

Dihydrexidine hydrochloride DAR-0100 hydrochloride	Dopamine Receptor	Neurological Disease
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC₅₀ of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.

HY-100490A

Rilmenidine hemifumarate	Imidazoline Receptor Adrenergic Receptor Apoptosis Autophagy
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na⁺/H⁺ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells ^[1].

HY-19357

E3330 APX-3330	DNA/RNA Synthesis	Cancer
E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.

HY-13285

Ki16425 Debio 0719	LPL Receptor	Neurological Disease Cancer
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with K_is of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.

HY-19618

BRD3308	HDAC HIV	Infection Metabolic Disease
BRD3308 is a highly selective HDAC3 inhibitor with an IC₅₀ of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC₅₀ of 1.26 μM) or HDAC2 (IC₅₀ of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.

HY-100972

ARV-771	PROTAC Epigenetic Reader Domain	Cancer
ARV-771 is a potent BET degrader based on PROTAC technology with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

HY-W014502

D-Kynurenine	Aryl Hydrocarbon Receptor Endogenous Metabolite	Cancer
D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).

HY-34758

N-Nitroso-N-methylurea NMU; MNU; NMH	DNA Alkylator/Crosslinker	Cancer
N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane.

HY-15583

Auristatin F	Microtubule/Tubulin ADC Cytotoxin	Cancer
Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).

HY-128067

5-(N,N-Hexamethylene)-amiloride Hexamethylene amiloride; HMA	Sodium Channel HIV Apoptosis	Cancer Infection
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na⁺/H⁺ exchanger inhibitor, which decreases the intracellular pH (pH_i) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC₅₀s of 3.91 μM and 1.34 μM, respectively.

HY-123823

Nitroaspirin NCX 4016	COX Apoptosis	Cancer
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.

HY-16561

Resveratrol trans-Resveratrol; SRT501	IKK Autophagy Mitophagy Sirtuin Apoptosis Bacterial Fungal Antibiotic Keap1-Nrf2	Cancer Infection Inflammation/Immunology
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model.

HY-13453

BAY 11-7082 BAY 11-7821	IKK Deubiquitinase Autophagy Apoptosis	Cancer Inflammation/Immunology
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC₅₀=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

HY-122470

Stampidine	Reverse Transcriptase HIV	Infection
Stampidine is a *nucleoside reverse transcriptase inhibitor* (NRTI)** with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV_IIIB (B-envelope subtype) and primary clinical isolates with IC₅₀s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC₅₀s of 8.7 nM and 11.2 nM, respectively.

HY-B1716

L-5-Hydroxytryptophan L-5-HTP; Oxitriptan	Endogenous Metabolite	Metabolic Disease Neurological Disease
L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia.

HY-100574A

Cl-amidine hydrochloride	Protein Arginine Deiminase Apoptosis MicroRNA	Cancer Inflammation/Immunology
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC₅₀ values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

HY-103444

ARP-100	MMP	Cancer
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC₅₀=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).

HY-15477A

YS-49 monohydrate	Akt PI3K Angiotensin Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits *angiotensin II (Ang* II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors**.

HY-15477

YS-49	Akt PI3K Angiotensin Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits *angiotensin II (Ang* II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors**.

HY-133028

CKI-7 free base	Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK)	Cancer
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC₅₀ of 6 μM and a K_i of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.

HY-15504A

RGB-286638 free base	CDK GSK-3 MEK JAK	Cancer
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC₅₀s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC₅₀s of 3, 5, 50, and 54 nM.

HY-15504

RGB-286638	CDK GSK-3 MEK JAK	Cancer
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC₅₀s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC₅₀s of 3, 5, 50, and 54 nM.

HY-N0155

Nobiletin	ROR Reactive Oxygen Species Apoptosis Autophagy	Cancer Inflammation/Immunology Neurological Disease
Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced *apoptosis*.

HY-108676

NF023 hexasodium	P2X Receptor	Neurological Disease
NF023 hexasodium is a selective and competitive P2X₁ receptor antagonist, with IC₅₀ values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X₁, P2X₃, P2X₂, and P2X₄-mediated responses respectively.

HY-W011500

TCEP hydrochloride Tris(2-carboxyethyl)phosphine hydrochloride	Others	Others
TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry.

HY-136065A

bpV(phen) hydrate	PTEN Phosphatase Parasite Apoptosis	Cancer Infection Metabolic Disease Inflammation/Immunology
bpV(phen) hydrate is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC₅₀s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) hydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) hydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) hydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

HY-136065

bpV(phen)	PTEN Phosphatase Parasite Apoptosis	Cancer Infection Metabolic Disease Inflammation/Immunology
bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC₅₀s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

HY-14994

SCH79797 dihydrochloride	Protease-Activated Receptor (PAR) Apoptosis	Cardiovascular Disease
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC₅₀ of 70 nM and a K_i of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC₅₀ of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.

HY-11007

GNF-2
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-N0548

α-Angelica lactone	Gutathione S-transferase	Cancer
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.

HY-100609

4-P-PDOT	Melatonin Receptor	Neurological Disease
4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

HY-P1077

CALP1	Calcium Channel mGluR Phosphodiesterase (PDE)	Inflammation/Immunology
CALP1 is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.

HY-12882A

Ifenprodil tartrate	iGluR Potassium Channel	Neurological Disease
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.

HY-128718

Carbodine	Influenza Virus	Infection
Carbodine (Carbocyclic cytidine) is a broad-spectrum antiviral agent active against DNA viruses, (+)RNA viruses, (-)RNA viruses, paramyxo, rhabdo and (+/-)RNA viruses, targets CTP synthetase that converts UTP to CTP. Carbodine (Carbocyclic cytidine) possesses significant antiviral activity against influenza virus types A0/PR-8/34 and A2/Aichi/2/68 in vitro.

HY-P1077A

CALP1 TFA	Calcium Channel mGluR Phosphodiesterase (PDE)	Inflammation/Immunology
CALP1 TFA is a calmodulin (CaM) agonist (K_d of 88 µM) with binding to the CaM EF-hand/Ca²⁺-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC₅₀ of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.

HY-101202

SNC80 NIH 10815	Opioid Receptor	Neurological Disease
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a K_i of 1.78 nM and an IC₅₀ of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC₅₀ of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.

HY-B0639

Amifostine WR2721	MDM-2/p53 HIF/HIF Prolyl-Hydroxylase	Cancer
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action.

HY-105231

Bryostatin 1	PKC HIV	Cancer Infection Inflammation/Immunology Neurological Disease
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with K_is of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.

HY-N0215

L-Phenylalanine (S)-2-Amino-3-phenylpropionic acid	Calcium Channel iGluR Endogenous Metabolite	Metabolic Disease
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca⁺ channels antagonist with a K_i of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (K_B of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.

HY-N0638

Dendrobine	Influenza Virus	Infection
Dendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC₅₀s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively.

HY-P1416A

Foxy-5 TFA	Wnt	Cancer
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.

HY-B0639A

Amifostine trihydrate WR2721 trihydrate	MDM-2/p53 HIF/HIF Prolyl-Hydroxylase	Cancer
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action.

HY-15310

Ivermectin MK-933	Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy	Infection Cancer
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-108511A

PB28	Sigma Receptor Apoptosis SARS-CoV	Cancer Infection
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 is also a σ1 antagonist with a K_i of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.

HY-P1064

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

HY-108556A

RWJ-56110 dihydrochloride	Protease-Activated Receptor (PAR) Apoptosis	Cardiovascular Disease
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC₅₀=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC₅₀=0.16 μM) and thrombin (IC₅₀=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

HY-13106

Olodanrigan EMA401; PD-126055	Angiotensin Receptor	Neurological Disease Endocrinology
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.

HY-15589

GW9508	GPR40 Potassium Channel	Metabolic Disease Inflammation/Immunology Cardiovascular Disease
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC₅₀s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.

HY-12765

Losartan Carboxylic Acid E-3174; EXP-3174	Angiotensin Receptor	Cardiovascular Disease
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The K_i values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.

HY-P1064A

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

HY-N0515

Ophiopogonin D	PPAR NF-κB Calcium Channel	Inflammation/Immunology Cardiovascular Disease
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C₂₉ steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca²⁺ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.

HY-12326A

c-di-AMP sodium Cyclic diadenylate sodium; Cyclic-di-AMP sodium	STING Bacterial Endogenous Metabolite	Inflammation/Immunology
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.

HY-122815

Fusicoccin Fusicoccin A	Apoptosis	Cancer
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H⁺-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.

HY-B1371A

Spiperone hydrochloride Spiroperidol hydrochloride	Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel	Inflammation/Immunology Neurological Disease
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.

HY-15746

Dobutamine hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion.

HY-108357

6-Diazo-5-oxo-L-nor-Leucine L-6-Diazo-5-oxonorleucine; DON	Glutaminase Bacterial Influenza Virus Antibiotic	Cancer Infection Neurological Disease
L-6-Diazo-5-oxonorleucine (L-6-Diazo-5-oxonorleucine) is a glutaminases antagonist with a K_i of 6 μM. L-6-Diazo-5-oxonorleucine exhibits analgesic, antibacterial, antiviral and anticancer properties. L-6-Diazo-5-oxonorleucine displays genetic toxicity in vitro. L-6-Diazo-5-oxonorleucine decreases the self-renewal potential and metastatic ability of tumor cell.

HY-12326

c-di-AMP Cyclic diadenylate; Cyclic-di-AMP	STING Bacterial	Inflammation/Immunology
c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.

HY-106178

PMX-53 3D53	Complement System	Cancer Inflammation/Immunology Cardiovascular Disease
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC₅₀ of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

HY-P1454A

Fz7-21 TFA Ac-LPSDDLEFWCHVMY-NH2 TFA	Wnt	Cancer
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC₅₀ values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC₅₀=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC₅₀=50 nM).

HY-137471

RBPJ Inhibitor-1 RIN1	Notch	Cancer
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.

HY-32015

Cot inhibitor-1
MAP3K Cancer

Cot inhibitor-1 is a COT/Tpl2 inhibitor.

HY-136121

Tubulin inhibitor 6	Microtubule/Tubulin	Cancer
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC₅₀ of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC₅₀ of 840 nM.

HY-112812

SCD1 inhibitor-1
Stearoyl-CoA Desaturase (SCD) Cancer Metabolic Disease

SCD1 inhibitor-1 is a potent and liver-selective stearoyl-CoA desaturase-1 (SCD1) inhibitor.

HY-B0552A

Dibucaine hydrochloride Cinchocaine hydrochloride	Sodium Channel	Neurological Disease
Dibucaine hydrochloride (Cinchocaine hydrochloride) is a sodium channel inhibitor. Dibucaine hydrochloride is a potent SChE inhibitor.

HY-112911

Endothelial lipase inhibitor-1
Others Cardiovascular Disease

Endothelial lipase inhibitor-1 is a potent endothelial lipase inhibitor with an IC₅₀ of 49 nM.
HY-B0552

Dibucaine
Cinchocaine
Sodium Channel Neurological Disease

Dibucaine (Cinchocaine) is a sodium channel inhibitor. Dibucaine is a potent SChE inhibitor.

HY-18353

mTOR inhibitor-3	mTOR	Cancer
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a K_i of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.

HY-112722

Neurotoxin Inhibitor
Others Neurological Disease

Neurotoxin Inhibitor is a neurotoxin inhibitor.

HY-D0843

N-Ethylmaleimide NEM	Cathepsin Deubiquitinase	Others
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.

HY-101275

EMT inhibitor-1
Hippo (MST) TGF-beta/Smad Wnt Cancer

EMT inhibitor-1 is an inhibitor of of Hippo, TGF-β, and Wnt signaling pathways with antitumor activities.

HY-13278A

IRAK inhibitor 4 trans	IRAK	Inflammation/Immunology
IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor.

HY-111412

DAAO inhibitor-1
Others Neurological Disease

DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC₅₀ of 0.12 μM.

HY-21141

Cysteine protease inhibitor-2	Cathepsin	Cancer
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI₅₀ values of 6.5 μM and 4.4 μM, respectively.

HY-70005

CPA inhibitor
Carboxypeptidase inhibitor
Carboxypeptidase Metabolic Disease

CPA inhibitor is a potent inhibitor for carboxypeptidase A (CPA).
HY-17541A

Cysteine Protease inhibitor hydrochloride
Cathepsin Others

Cysteine Protease inhibitor hydrochloride is an inhibitor of cysteine protease.
HY-17541

Cysteine Protease inhibitor
Cathepsin Others

Cysteine Protease inhibitor is an inhibitor of cysteine protease.
HY-112914

mTOR inhibitor-1
mTOR Autophagy Cancer

mTOR inhibitor-1 is a novel mTOR pathway inhibitor which can suppress cells proliferation and inducing autophagy.

HY-128703

Bromodomain inhibitor-8	Epigenetic Reader Domain	Inflammation/Immunology
Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases.

HY-136660

mTOR inhibitor-7	mTOR	Neurological Disease
mTOR inhibitor-7 is an orally available, and brain-penetrant mTOR inhibitor extracted from patent WO2017198346A1, compound example 44, has an IC₅₀ of 5 nM for mTOR. mTOR inhibitor-7 can be used for the research of neurological disorder.

HY-128722

HIV-1 inhibitor-3
HIV Infection

HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
HY-110101

ARN272
Others Neurological Disease

ARN272 is an anandamide transport inhibitor.
HY-12202

MEK inhibitor
MEK Cancer

MEK inhibitor is a potent MEK inhibitor with antitumor potency.
HY-B0543

Allylthiourea
Thiosinamine; N-Allylthiourea
Reactive Oxygen Species Metabolic Disease

Allylthiourea is a metabolic inhibitor that selective inhibits ammonia oxidation.
HY-10421

Tyrosine kinase inhibitor
c-Met/HGFR Cancer

Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.
HY-B0385

Gabexate mesylate
FOY
Factor Xa Proteasome Inflammation/Immunology

Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .

HY-P0017

Aprotinin	Influenza Virus	Cardiovascular Disease Cancer
Aprotinin is a *bovine pancreatic trypsin inhibitor* (BPTI)** inhibitor which inhibits trypsin and chymotrypsin with K_is of 0.06 pM and 9 nM, respectively.

HY-112843

CNT2 inhibitor-1
Others Others

CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC₅₀ of 640 nM for hCNT2.

HY-136279

TrxR inhibitor D9	Apoptosis	Cancer
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC₅₀ of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.

HY-101297

Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
Caspase Cancer

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.

HY-100732

Cambinol	Sirtuin Apoptosis Phospholipase	Cancer
Cambinol is a SIRT1 and SIRT2 inhibitor with IC₅₀ values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-15182

Collagen proline hydroxylase inhibitor-1
Others Cancer

Collagen proline hydroxylase inhibitor-1 is an antifibroproliferative agents.
HY-112474

Tyrphostin AG 112
EGFR Cancer

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor.
HY-15358

ALK inhibitor 2
ALK Cancer

ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
HY-B0732

Itopride hydrochloride
HSR803
AChE Neurological Disease

Itopride hydrochloride is an AChE inhibitor (acetylcholinesterase) and D2DR inhibitor.
HY-15357

ALK inhibitor 1
ALK Cancer

ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.

HY-136920

CBP/P300 bromodomain inhibitor-3	Epigenetic Reader Domain	Cancer
CBP/P300 bromodomain inhibitor-3 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/P300 bromodomain inhibitor-3 inhibits CBP (IC₅₀=0.01-0.1 µΜ) and BRD4 (IC₅₀=1-1000 µΜ) activity.

HY-13662

Lansoprazole AG-1749	Proton Pump Bacterial Phospholipase	Inflammation/Immunology Cancer
Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-13662A

Lansoprazole sodium AG-1749 sodium	Proton Pump Phospholipase Bacterial	Inflammation/Immunology
Lansoprazole sodium (AG 1749 sodium) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole sodium (AG 1749 sodium) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-119937

ROCK inhibitor-2
ROCK Inflammation/Immunology Cardiovascular Disease

ROCK inhibitor-2 is a selective dual ROCK1 and ROCK2 inhibitor with IC₅₀s of 17 nM and 2 nM, respectively.

HY-15253

Tiplaxtinin PAI-039; Tiplasinin	PAI-1 Apoptosis	Metabolic Disease Cancer
Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC₅₀ of 2.7 μM.

HY-13973A

GSK-3 inhibitor 1
GSK-3 Metabolic Disease

GSK-3 inhibitor 1 is an inhibitor of GSK-3.

HY-104051

Monacolin J Antibiotic MB 530A; Lovastatin diol lactone	HMG-CoA Reductase (HMGCR) Autophagy	Metabolic Disease
Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.

HY-111347A

BB-Cl-Amidine hydrochloride
Protein Arginine Deiminase Inflammation/Immunology

BB-Cl-Amidine hydrochloride is a peptidylarginine deminase (PAD) inhibitor.
HY-131100

Homo Sildenafil
Phosphodiesterase (PDE) Endocrinology

Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor.
HY-135890

CG347B
HDAC Cancer

CG347B is a selective HDAC6 inhibitor.
HY-15444

D159687
Phosphodiesterase (PDE) Neurological Disease

D159687 is a selective PDE4D inhibitor.

HY-112390A

Syk Inhibitor II	Syk 5-HT Receptor	Inflammation/Immunology
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC₅₀ of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC₅₀ of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.

HY-122723

GOT1 inhibitor-1	Others	Cancer
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with IC₅₀ of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).

HY-114317

MARK4 inhibitor 1	Apoptosis	Cancer
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC₅₀ of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.

HY-15002

AST 487 NVP-AST 487	RET FLT3 VEGFR c-Kit Bcr-Abl	Cancer
AST 487 is a RET kinase inhibitor with IC₅₀ of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC₅₀ of 520 nM.

HY-135826

Necroptosis-IN-1
RIP kinase Cancer

Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
HY-111408

EOAI3402143
Deubiquitinase Cancer

EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.

HY-N2033

Chebulinic acid	DNA/RNA Synthesis TGF-beta/Smad Proton Pump	Infection
Chebulinic acid is a potent natural inhibitor of M. tuberculosis DNA gyrase, also can inhibit SMAD-3 phosphorylation, inhibit H+ K+-ATPase activity.

HY-100463

TPI-1
Phosphatase Inflammation/Immunology Cancer

TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC₅₀ of 40 nM.

HY-112607

Tubulin inhibitor 1	Microtubule/Tubulin Apoptosis	Cancer
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.

HY-B0884

Minaprine
Monoamine Oxidase Neurological Disease

Minaprine is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.
HY-112569

MAT2A inhibitor 2
Others Cancer

MAT2A inhibitor 2 is a methionine adenosyltransferase 2A (MAT2A) inhibitor.

HY-B0884A

Minaprine dihydrochloride	Monoamine Oxidase	Neurological Disease
Minaprine dihydrochloride is a reversible inhibitor of MAO-A; weakly inhibit acetylcholinesterase; an antidepressant for treatment of depression.

HY-15167

Glyoxalase I inhibitor
Others Cancer

Glyoxalase I inhibitor is a potent Glyoxalase I inhibitor, candidate for anticancer agents.
HY-50856A

Ruxolitinib (S enantiomer)
S-Ruxolitinib; S-INCB18424
JAK Cancer

Ruxolitinib S enantiomer is the S-enantiomer of Ruxolitinib. Ruxolitinib S enantiomer is a JAK inhibitor
HY-117262

Propaquizafop
Acetyl-CoA Carboxylase Others

Propaquizafop is a phenoxyisopropionic acid herbicide and an acetyl-coA carboxylase inhibitor.
HY-U00410

PDE4 inhibitor intermediate 1
Others Others

PDE4 inhibitor intermediate 1 is an intermediate for PDE4 inhibitor synthesis.
HY-13276

IRAK inhibitor 2
IRAK Inflammation/Immunology

IRAK inhibitor 2 is interleukin-1 receptor associated kinase inhibitor .

HY-B0218

Orlistat Tetrahydrolipstatin; Ro-18-0647	Fatty Acid Synthase (FASN) Apoptosis	Metabolic Disease Cancer
Orlistat is a lipase inhibitor for obesity management that acts by inhibiting the absorption of dietary fats.

HY-106067A

Dazoxiben
Prostaglandin Receptor Inflammation/Immunology

Dazoxiben is a potent and orally active thromboxane (TX) synthase inhibitor.

HY-124798

Rheb inhibitor NR1	mTOR	Cancer Inflammation/Immunology Neurological Disease
Rheb inhibitor NR1 is a Rheb inhibitor with an IC₅₀ of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 also is a selective mTORC1 inhibitor. NR1 inhibits the phosphorylation of ^T389pS6K1 and increases the phosphorylation of ^S473pAKT in a dose-dependent manner.

HY-32018

Cot inhibitor-2	MAP3K	Cancer
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC₅₀ of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC₅₀ of 0.3 μM.

HY-N6717

Tentoxin	Others	Infection
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.

HY-17542

PLpro inhibitor	SARS-CoV	Infection
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC₅₀ of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC₅₀ of 5.0 µM and an EC₅₀ of 21.0 µM.

HY-15760

Necrostatin-1 Nec-1	RIP kinase Autophagy Indoleamine 2,3-Dioxygenase (IDO) Ferroptosis	Cancer
Necrostatin-1 (Nec-1) is a potent necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor.

HY-N1504

Loureirin B	PAI-1 Potassium Channel ERK JNK	Metabolic Disease
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC₅₀ of 26.10 μM; Loureirin B also inhibits K_ATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.

HY-13662B

(R)-Lansoprazole Dexlansoprazole	Proton Pump	Inflammation/Immunology
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-10217

Thrombin Inhibitor 2	Thrombin	Cardiovascular Disease
Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.

HY-P1029

MLCK inhibitor peptide 18	Myosin CaMK Autophagy	Others
MLCK inhibitor peptide 18 is a myosin light chain kinase (MLCK) inhibitor with an IC₅₀ of 50 nM, and inhibits CaM kinase II only at 4000-fold higher concentrations.

HY-15604

AZD1208
Pim Autophagy Apoptosis Cancer

AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
HY-N0565

Doxycycline
MMP Bacterial Parasite Antibiotic Infection

Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-15183

Collagen proline hydroxylase inhibitor
Others Cancer

Collagen proline hydroxylase inhibitor is a collagen proline hydroxylase inhibitor; useful for antifibroproliferative agents.

HY-U00387

CCK-A receptor inhibitor 1	Cholecystokinin Receptor	Metabolic Disease Endocrinology
CCK-A receptor inhibitor 1 is a cholecystokinin A (CCK-A) receptor inhibitor with a binging IC₅₀ of 340 nM.

HY-107986

GNE-6776
Deubiquitinase Cancer

GNE-6776 is a selective and orally bioavailable USP7 inhibitor.
HY-10249A

AKT Kinase Inhibitor
Akt Cancer

AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity.
HY-100962

(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
EGFR Cancer

(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
HY-N0565A

Doxycycline hydrochloride
MMP Bacterial Antibiotic Infection

Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-108322

NBTGR
Others Cardiovascular Disease

NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a K_i of 70 nM.
HY-13985

Nav1.7 inhibitor
Sodium Channel Neurological Disease

Nav1.7 inhibitor is a potent Nav1.7 inhibitor.
HY-50880

Elacridar hydrochloride
GF120918A
P-glycoprotein Cancer

Elacridar hydrochloride (GF120918A) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
HY-N2221

Ganoderal A
Others Metabolic Disease

Ganoderal A, an oxygenated sterol from G. lucidum, is a cholesterol synthesis inhibitor.
HY-14657

Dantrolene sodium
F 440
Calcium Channel Metabolic Disease

Dantrolene sodium is a inhibitor of calcium channel proteins, inhibiting the release of Ca2+ from the sarcoplasm.
HY-101932

TNP-470
AGM-1470
Aminopeptidase Cancer Cardiovascular Disease

TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
HY-N6902

Linderene acetate
Others Inflammation/Immunology

Linderene acetate, isolated from the root of Lindera strychnifolia, is a prolyl endopeptidase inhibitor.
HY-U00319

Lipid peroxidation inhibitor 1
Others Neurological Disease

Lipid peroxidation inhibitor 1 is a lipid peroxidation inhibitor with an IC₅₀ of 0.07 μM.
HY-15825

IWP L6
Porcn Inhibitor III
Porcupine Cancer

IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC₅₀ of 0.5 nM.
HY-12072

Lck Inhibitor
Src Inflammation/Immunology

Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.

HY-13718

Oglufanide H-Glu-Trp-OH; L-Glutamyl-L-tryptophan	VEGFR HCV Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis.

HY-112269

Glutaminyl Cyclase Inhibitor 1
Amyloid-β Neurological Disease

Glutaminyl Cyclase Inhibitor 1 is a glutaminyl cyclase inhibitor with an IC₅₀ of 0.5 μM.
HY-128723

Dapagliflozin impurity
Others Others

Dapagliflozin impurity is an enantiomer of Dapagliflozin which is a sodium-glucose transporter 2 inhibitor.
HY-50879

Elacridar
GF120918; GW0918; GG918; GW120918
P-glycoprotein BCRP Cancer

Elacridar (GF120918) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.

HY-104032

Ac-CoA Synthase Inhibitor1	RSV	Infection Metabolic Disease
Ac-CoA Synthase Inhibitor1 is a potent, reversible acetate-dependent acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC₅₀ of 0.6 µM. Ac-CoA Synthase Inhibitor1 inhibits the respiratory syncytial virus (RSV).

HY-10172

IMD-0354 IKK2 Inhibitor V	IKK	Cancer
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC₅₀ of 1.2 uM.

HY-136270

ATR inhibitor 2	ATM/ATR	Cancer
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a K_i of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC₅₀ of 8 nM. Antitumor activity.

HY-103310

MRS1845
Calcium Channel CRAC Channel Cardiovascular Disease

MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC₅₀ of 1.7 μM. MRS1845 is an ORAI1 inhibitor.

HY-122856

AZ12601011	TGF-β Receptor	Cancer
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC₅₀ of 18 nM and a K_d of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .

HY-B0083

Leflunomide HWA486; RS-34821; SU101	Others	Cancer
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.

HY-101474A

Zanubrutinib
BGB-3111
Btk Cancer

Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.

HY-16569

Colchicine	Microtubule/Tubulin Autophagy	Cancer
Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC₅₀ of 3 nM.

HY-N7592

Arjunetin
Others Others

Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.

HY-12186

3-Deazaneplanocin A hydrochloride DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride	Histone Methyltransferase	Cancer
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor.

HY-12238

IWR-1
endo-IWR 1; IWR-1-endo
Wnt Cancer

IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
HY-100110

KNK437
Heat Shock Protein Inhibitor I
HSP Cancer

KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
HY-135384

tert-Buthyl Pitavastatin
Drug Metabolite Cardiovascular Disease

tert-Buthyl Pitavastatin is the metabolite of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
HY-106638

Voclosporin
ISAtx-247
Phosphatase Inflammation/Immunology

Voclosporin (ISAtx-247) is a calcineurin (PP2B) (CN) inhibitor.
HY-100933

MY-5445
Phosphodiesterase (PDE) Cardiovascular Disease

MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor. MY-5445 selectively inhibits cGMP PDE with a K_i of 1.3 μM.

HY-A0276

Gentamicin sulfate	Bacterial Antibiotic	Infection
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC₅₀ of 0.57 mM.

HY-N0518

Toddalolactone	PAI-1	Cardiovascular Disease
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant *human plasminogen activator inhibitor-1 (PAI-1)*, with an IC₅₀ value of 37.31 μM.

HY-16657

TAPI-1	MMP	Cancer Inflammation/Immunology
TAPI-1 is a TACE (ADAM17) inhibitor and blocks the shedding of several cell surface proteins. TAPI-1 is also a metalloproteinase (MMP) inhibitor.

HY-19931

COH29 RNR Inhibitor COH29	DNA/RNA Synthesis	Cancer
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC₅₀s of 16 μM.

HY-119808

Terrein	Melanocortin Receptor Apoptosis Antibiotic	Cancer
Terrein is a melanogenesis inhibitor. Terrein induces apoptosis in breast cancer cell lines . Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa.

HY-128729

DNA2 inhibitor C5	Others	Cancer
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC₅₀ of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.

HY-P2478

Human PD-L1 inhibitor V	PD-1/PD-L1	Inflammation/Immunology
Human PD-L1 inhibitor V, a polypeptide, is a competitive human PD-1 protein inhibitor with a K_d value of 3.32 μM. Human PD-L1 inhibitor V inhibit the interaction of hPD-1/hPD-L1.

HY-P2477

Human PD-L1 inhibitor IV	PD-1/PD-L1	Inflammation/Immunology
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a K_d value of 1.38 μM. Human PD-L1 inhibitor IV inhibits the interaction of hPD-1/hPD-L1.

HY-10917

GW2580	c-Fms	Inflammation/Immunology Cancer
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.

HY-13417A

AICAR phosphate Acadesine phosphate; AICA Riboside phosphate	AMPK Autophagy YAP Mitophagy	Cancer
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.

HY-113951

Prolyl Endopeptidase Inhibitor 1 Boc-Pro-prolinal; (Boc)-Prolyl-prolinal; BPP	Dipeptidyl Peptidase	Neurological Disease
Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a K_i value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.

HY-124718

p32 Inhibitor M36
M36
PKC Cancer

p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.

HY-13417

AICAR Acadesine; AICA Riboside	AMPK Autophagy YAP Mitophagy	Cancer
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.

HY-P1260

FSLLRY-NH2
Protease-Activated Receptor (PAR) Neurological Disease

FSLLRY-NH2 is a protease-activated receptor 2 (PAR2) inhibitor.
HY-19797A

ML241 hydrochloride
p97 Cancer

ML241 hydrochloride is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM.
HY-14274

Anastrozole
ZD1033
Aromatase Cancer

Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC₅₀ of 15 nM.
HY-131101

Nor-Acetildenafil
Others Others

Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
HY-10846

Delamanid
OPC-67683
Bacterial Antibiotic Cancer

Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids.
HY-18930

NU6300
CDK Cancer

NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
HY-W013478

PTP inhibitor 1
Phosphatase Cancer

PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.
HY-15700

PluriSIn 1
NSC 14613
Stearoyl-CoA Desaturase (SCD) Apoptosis Cancer

PluriSIn 1 (NSC 14613) is an inhibitor of stearoyl-coA desaturase (SCD), and is a pluripotent cell-specific inhibitor.
HY-101429

RG13022
Tyrphostin RG13022
EGFR Cancer

RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC₅₀ of 4 μM.
HY-B1877

Nitrofen
Others Cancer

Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
HY-N2219

Picfeltarraegenin X
AChE Neurological Disease

Picfeltarraenin X, a triterpenoid isolated from Picria fel-terrae Lour, is an AChE inhibitor.
HY-19795

ML240
p97 Cancer

ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM.
HY-112639

Aristeromycin
Bacterial Cancer Infection

Aristeromycin, an adenosine analog, is an antibiotic and a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
HY-100600

BGG463
K03859
CDK Others

BGG463 (K03859) is an orally active type II CDK2 inhibitor.
HY-N2117

Isoginkgetin
MMP Cancer

Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
HY-136461

Polyoxin D
Polyoxorim
Fungal Antibiotic Infection

Polyoxin D (Polyoxorim), a polyoxin antibiotic fungicide, is a potent chitin synthetase inhibitor.
HY-P2564

Human PD-L1 inhibitor III
PD-1/PD-L1 Cancer Inflammation/Immunology

Human PD-L1 inhibitor III is a human PD-L1 inhibitor.
HY-15222

Menin-MLL inhibitor MI-2
Epigenetic Reader Domain Apoptosis Cancer

Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC₅₀ of 446±28 nM.
HY-14196

Toloxatone
MD 69276
Monoamine Oxidase Neurological Disease

Toloxatone (MD 69276) is a reversible monoamine oxidase A (MAO_A) inhibitor. Antidepressant.

HY-17396

Butenafine Hydrochloride KP363 Hydrochloride	Fungal Antibiotic	Infection
Butenafine Hydrochloride (KP363 Hydrochloride) is a synthetic benzylamine antifungal, works by inhibiting the synthesis of sterols by inhibiting squalene epoxidase.

HY-14440

MP7
PDK1 inhibitor
PDK-1 Cancer

MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
HY-50670

DGAT-1 inhibitor 2
Acyltransferase Metabolic Disease

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.

HY-U00145

Digeranyl bisphosphonate DGBP	Ras	Inflammation/Immunology
Digeranyl bisphosphonate (DGBP) is a potent geranylgeranylpyrophosphate (GGPP) synthase inhibitor, which inhibits geranylgeranylation of Rac1.

HY-116770

PFM01
Others Cancer

PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor.

HY-B0113A

Omeprazole sodium H 16868 sodium	Proton Pump Autophagy Bacterial Phospholipase	Cancer Infection Metabolic Disease
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a K_i of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-10255A

Sunitinib SU 11248	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-111429

YAP/TAZ inhibitor-1
YAP Cancer

YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC₅₀ of <0.100 μΜ in firefly luciferase assay.

HY-120859

Zidebactam WCK-5107	Bacterial	Infection
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC₅₀ of 0.26 μg/mL.

HY-118355

ALLM Calpain inhibitor II	Proteasome Cathepsin	Neurological Disease
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).

HY-N0565B

Doxycycline (hyclate) Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031	MMP Bacterial Antibiotic	Infection
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.

HY-15699A

SAR7334 hydrochloride
TRP Channel Neurological Disease

SAR7334 hydrochloride is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC₅₀ of 7.9 nM.
HY-B2063

Chlorobenzuron
Others Others

Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
HY-N1447

Ganoderic acid A
Apoptosis Autophagy Endogenous Metabolite Cancer

Ganoderic acid A can inhibit of the JAK-STAT3 signaling pathway, also inhibit proliferation, viability, ROS.
HY-15167A

Glyoxalase I inhibitor free base
Others Cancer

Glyoxalase I inhibitor (free base) is a potent Glyoxalase I (GLO1) inhibitor, candidate for anticancer agents.
HY-112634

SIRT5 inhibitor 1
Sirtuin Others

SIRT5 inhibitor 1 is a potent Human Sirtuin 5 deacylase inhibitor, with an IC₅₀ of 0.11 μM.
HY-133248

Daclatasvir Impurity C
Others Others

Daclatasvir Impurity C is the impurity of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.
HY-13972

Mutant IDH1 inhibitor
Isocitrate Dehydrogenase (IDH) Cancer

Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC₅₀ of < 72 nM.
HY-15699

SAR7334
TRP Channel Neurological Disease

SAR7334 is a potent and specific TRPC6 inhibitor, inhibiting TRPC6 currents with IC₅₀ of 7.9 nM.
HY-118165

Phenthoate
AChE Neurological Disease

Phenthoate is an organophosphorus pesticide having low toxicity in animals. Phenthoate is also a AChE inhibitor.

HY-B1596

Ceftizoxime	Bacterial Antibiotic	Infection
Ceftizoxime is a bacterial inhibitor which acts by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan.

HY-P1260A

FSLLRY-NH2 TFA
Protease-Activated Receptor (PAR) Neurological Disease

FSLLRY-NH2 TFA is a protease-activated receptor 2 (PAR2) inhibitor.
HY-103593A

LCL521 dihydrochloride
Phospholipase Cancer

LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
HY-103593

LCL521
Phospholipase Cancer

LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).

HY-I0637

Isovanillin 3-Hydroxy-4-methoxybenzaldehyde	Others	Metabolic Disease Neurological Disease
Isovanillin is an aldehyde oxidase inhibitor. Antispasmodic activities. Antidiarrheal activities.

HY-16187

EL-102
HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer

EL102 is a inhibitor of HIF1α , Which can inhibit tubulin polymerisation and decreased microtubule stability.
HY-133247

Daclatasvir Impurity B
Others Others

Daclatasvir Impurity B is the impurity of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.

HY-D0886

β-Glycerol phosphate disodium salt pentahydrate β-Glycerophosphate disodium salt pentahydrate	Phosphatase	Cancer Neurological Disease
β-Glycerol phosphate disodium salt pentahydrate (β-Glycerophosphate disodium salt pentahydrate) is a phosphatase inhibitor.

HY-18965

TAS-301
PKC Cardiovascular Disease

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, and inhibits PKC activation induced by PDGF.
HY-12277

AZ191
DYRK Cancer

AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC₅₀ of 17 nM.
HY-107451

PROTAC BET-binding moiety 1
Ligand for Target Protein for PROTAC Cancer

PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.
HY-107485

HIV-1 integrase inhibitor 8
HIV Integrase Infection

HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.
HY-14174

MRK-560
γ-secretase Neurological Disease

MRK-560 is a potent, orally bioavailable and brain-penetrant γ-secretase inhibitor.
HY-N7511

O-Nornuciferine
Potassium Channel Metabolic Disease

O-Nornuciferine, an aporphine-type alkaloid from lotus leaf, is a potent hERG channel inhibitor.
HY-N4294

Arjungenin
Others Metabolic Disease

Arjungenin, a triterpene isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
HY-B2007

Fluazifop-P-butyl
Acetyl-CoA Carboxylase Metabolic Disease

Fluazifop-P-butyl, a graminicide from arylophenoxypropionate group, is a acetyl-CoA carboxylase (ACCase) inhibitor.
HY-13818

Stattic
STAT Apoptosis Cancer Inflammation/Immunology

Stattic is a potent STAT3 inhibitor. Stattic inhibits STAT3 phosphorylation (at Y705 and S727).
HY-100498

GSK2256098
FAK Apoptosis Cancer

GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
HY-14445

FK 3311
COX-2 Inhibitor V
COX Inflammation/Immunology

FK 3311 (COX-2 Inhibitor V) is a selective inhibitor of COX-2 with antiinflammatory agent.
HY-11009

CGP60474
VEGFR PKC Cancer

CGP60474 is a potent VEGFR-2 inhibitor, with an IC₅₀ of 84 nM, and also an ATP-competitive PKC inhibitor.
HY-19707

4μ8C
IRE1 Inhibitor III
IRE1 Metabolic Disease

4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
HY-112822

ON-013100
CDK Cancer

ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
HY-100456

ZL006
iGluR Neurological Disease

ZL006 is a potent inhibitor of nNOS/PSD-95 interaction, and inhibits NMDA receptor-mediated NO synthesis.
HY-111493

LRRK2 inhibitor 1
LRRK2 Neurological Disease

LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC₅₀ of 6.8 nM.

HY-100932

ML-9	Myosin	Cancer
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.

HY-B0113

Omeprazole H 16868	Proton Pump Autophagy Bacterial Phospholipase	Cancer Infection Metabolic Disease
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a K_i of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

HY-50706A

Selumetinib sulfate AZD6244 sulfate; ARRY-142886 sulfate	MEK Apoptosis	Cancer
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2* inhibitor,* with an IC₅₀ of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

HY-105917

Endovion NS3728	Chloride Channel	Others
Endovion (NS3728) is a pharmacological *anion channel inhibitor* (like chloride channel) and the specific VRAC/VSOAC** blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.

HY-10326

GW788388	TGF-β Receptor	Cancer
GW788388 is a potent and selective inhibitor of ALK5 with IC₅₀ of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.

HY-13228

YM-201636	PIKfyve PI3K Autophagy Influenza Virus	Cancer Infection
YM-201636 is a potent and selective PIKfyve inhibitor with an IC₅₀ of 33 nM. YM-201636 also inhibits p110α with an IC₅₀ of 3.3 μM. YM-201636 inhibits retroviral replication.

HY-10227

Bortezomib PS-341; LDP-341; NSC 681239	Proteasome NF-κB Apoptosis Autophagy	Cancer
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.

HY-10255

Sunitinib Malate SU 11248 Malate	PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.

HY-17367

Atazanavir BMS-232632	HIV HIV Protease Cytochrome P450 P-glycoprotein	Infection Cancer
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).

HY-U00453

Soluble epoxide hydrolase inhibitor	Epoxide Hydrolase	Metabolic Disease Cardiovascular Disease
Soluble epoxide hydrolase inhibitor is an inhibitor of soluble epoxide hydrolase, and inhibits human soluble epoxide hydrolase (h-sEH) with pIC₅₀ of 8.4, extracted from patent WO 2010096722 A1, example 57.

HY-112910

Grp94 Inhibitor-1
HSP Cancer Infection

Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC₅₀ value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.

HY-15339

CVT-313 Cdk2 Inhibitor III	CDK	Cancer
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC₅₀ of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.

HY-13984

Mutant EGFR inhibitor	EGFR	Cancer
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR^L858R, EGFR^{Exon 19 deletion} and EGFR^T790M.

HY-22166

Glycolic acid oxidase inhibitor 1
Others Metabolic Disease

Glycolic acid oxidase inhibitor 1 is a glycolate oxidase inhibitor, extracted from patent EP0021228A1, in Table IV.
HY-W047428

4-Hydroxy-3,3-dimethylcyclohexanone
Others Others

4-Hydroxy-3,3-dimethylcyclohexanone is a key intermediate for the synthesis of hAChE inhibitor.
HY-112451

cFMS Receptor Inhibitor II
c-Fms Inflammation/Immunology

cFMS Receptor Inhibitor II is a CSF1R kinase inhibitor. CSF-1 is a cytokine.
HY-15217

CHR-6494
Haspin Kinase Cancer

CHR-6494 is a potent inhibitor of haspin, inhibiting histone H3T3 phosphorylation, with an IC₅₀ of 2 nM.
HY-15859

Atglistatin
ATGL Metabolic Disease

Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC₅₀ of 0.7 μM in vitro.

HY-77521

Dabigatran ethyl ester hydrochloride	Thrombin	Cardiovascular Disease
Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC₅₀ value of 0.8 μM and a thrombin inhibitor.

HY-13502

Mitoxantrone
mitozantrone
Topoisomerase PKC Cancer

Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM.

HY-107994

Aminooxyacetic acid hemihydrochloride Carboxymethoxylamine Hemihydrochloride	GABA Receptor	Cancer
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.

HY-N2567

(±)-Decursinol
Bacterial Cancer

(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC₅₀ of 102 μM.
HY-13278

IRAK inhibitor 4
IRAK Inflammation/Immunology

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.

HY-112860

Asp-AMS	Aminoacyl-tRNA Synthetase Mitochondrial Metabolism	Metabolic Disease
Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.

HY-12000

AG-490
Tyrphostin AG 490
EGFR STAT Autophagy Cancer

AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

HY-A0116S

Trandolaprilate D5 Trandolaprilat D5; RU 44403 D5	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Trandolaprilate D5 is a deuterium labeled Trandolaprilate (Trandolaprilat). Trandolaprilate is an angiotensin-converting enzyme (ACE) inhibitor.

HY-13060

ACHP Hydrochloride
IKK-2 Inhibitor VIII
IKK Inflammation/Immunology

ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC₅₀ of 8.5 nM.
HY-101474

(±)-Zanubrutinib
(±)-BGB-3111
Btk Cancer

(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
HY-19731

SID 3712249
MiR-544 Inhibitor 1
MicroRNA Apoptosis Cancer

SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544).

HY-B0392

(S)-(+)-Rolipram (+)-Rolipram; (S)-Rolipram	Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology Cancer
(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R enantiomer.

HY-101462

RAD51 Inhibitor B02
B02
RAD51 Apoptosis Cancer

RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC₅₀ of 27.4 μM.

HY-B0902A

Rufloxacin hydrochloride MF-934 hydrochloride	Bacterial	Infection
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.

HY-101963

AD80
Raf Src Ribosomal S6 Kinase (RSK) RET Cancer

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
HY-70073

Zaurategrast
CT7758
Integrin Inflammation/Immunology

Zaurategrast (CT7758) is a potent and oral-effective α₄-integrin inhibitor.
HY-15775

Arginase inhibitor 1
Arginase Cancer

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC₅₀s of 223 and 509 nM, respectively.

HY-13502A

Mitoxantrone dihydrochloride mitozantrone dihydrochloride	Topoisomerase PKC	Cancer
Mitoxantrone dihydrochloride is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM.

HY-70003

Carboxypeptidase G2 (CPG2) Inhibitor
CPG2 Inhibitor
Carboxypeptidase Cancer

Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
HY-112720

AGL-2263
Insulin Receptor Metabolic Disease Endocrinology

AGL-2263 is an insulin receptor and insulin-like growth factor (IGF) receptor inhibitor.
HY-111784

CBP-IN-1
Epigenetic Reader Domain Cancer

CBP-IN-1 is a potent p300/CBP bromodomain inhibitor.

HY-10439

HPGDS inhibitor 1	PGE synthase	Inflammation/Immunology
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC₅₀s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.

HY-100816

Rbin-1 Ribozinoindole-1	Phosphatase	Metabolic Disease
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI₅₀ of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).

HY-120675

SSTC3	Casein Kinase Wnt	Cancer
SSTC3 is a casein kinase 1α (CK1α) activator (K_d = 32 nM) that inhibits WNT signaling (EC₅₀ = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.

HY-100556

Tie2 kinase inhibitor 1	Others	Cancer
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC₅₀ of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.

HY-112715

ATP synthase inhibitor 1	ATP Synthase	Cardiovascular Disease
ATP synthase inhibitor 1 is a potent inhibitor of c subunit of the F₁/F_O-ATP synthase complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.

HY-14165

Veliflapon BAY X 1005; DG-031	FLAP Leukotriene Receptor	Inflammation/Immunology Cardiovascular Disease
Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

HY-128918

SIS17	HDAC	Others
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC₅₀ value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.

HY-P1111

Lyn peptide inhibitor	Src Interleukin Related	Inflammation/Immunology
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

HY-100932A

ML-9 Free Base	Myosin	Cancer
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.

HY-135318

NBDHEX	Glutathione Peroxidase Apoptosis Autophagy	Cancer
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.

HY-121172

1,4-DPCA	HIF/HIF Prolyl-Hydroxylase	Cancer
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC₅₀ of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits *factor inhibiting* HIF (FIH) with an IC₅₀** of 60 μM.

HY-12364

C75
Fatty Acid Synthase (FASN) Cancer

C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC₅₀ of 35 μM.
HY-P0081

Bax inhibitor peptide V5
BIP-V5; BAX Inhibiting Peptide V5
Bcl-2 Family Cancer

Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
HY-133110

Afatinib N-Oxide
Others Others

Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
HY-15798

UNC2881
TAM Receptor Cardiovascular Disease

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.
HY-114418

MMP3 inhibitor 1
MMP Cancer

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC₅₀ of 1 nM.
HY-N5038

Mauritianin
Topoisomerase Cancer

Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.

HY-13606

Dacinostat NVP-LAQ824; LAQ824	HDAC Autophagy	Cancer
Dacinostat is a potent HDAC inhibitor, with an IC₅₀ of 32 nM; Dacinostat also inhibits HDAC1 with an IC₅₀ of 9 nM, and used in cancer research.

HY-13256

Desmethyl Erlotinib hydrochloride OSI-420; CP-373420 hydrochloride	Drug Metabolite	Cancer
Desmethyl Erlotinib hydrochloride (OSI-420) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.

HY-P1452A

RNAIII-inhibiting peptide(TFA)	Bacterial	Infection
RNAIII-inhibiting peptide(TFA) is a potent inhibitor of Staphylococcus aureus, effective in the diseases such as cellulitis, keratitis, septic arthritis, osteomylitis and mastitis.

HY-Y0882

Hydroxyamine hydrochloride	Monoamine Oxidase	Cardiovascular Disease
Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis.

HY-16420

R112
Syk Inflammation/Immunology

R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
HY-111919

3-Nitrocoumarin
Phospholipase Others

3-Nitrocoumarin (3-NC) is a potent and selective Phospholipase C-γ (PLC-γ) inhibitor.
HY-15588

L189
DNA/RNA Synthesis Cancer

L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV with IC50 of 5/9/5 μM.
HY-B0830

Isoprocarb
AChE Neurological Disease

Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
HY-N1502

Carboxyatractyloside
Gummiferin
Others Cancer

Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.

HY-12054A

Hesperadin hydrochloride	Aurora Kinase Autophagy Influenza Virus Parasite	Cancer
Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC₅₀ of 250 nM.

HY-114423

p38α inhibitor 1
p38 MAPK Autophagy Inflammation/Immunology

p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.

HY-10809

Bitopertin RG1678; RO4917838	GlyT	Neurological Disease
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.

HY-19609

Calicheamicin Calicheamicin γ1	DNA Alkylator/Crosslinker ADC Cytotoxin Bacterial Apoptosis Antibiotic	Cancer Infection
Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.

HY-131268

O-Desisobutyl-O-n-propyl Febuxostat
Xanthine Oxidase Metabolic Disease

O-Desisobutyl-O-n-propyl Febuxostat, extracted from the patent CN 103467412, is an xanthine oxidase inhibitor.
HY-N6619A

Lycoramine
AChE Neurological Disease

Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
HY-104028

BAY 73-6691
(R)-BAY 73-6691
Phosphodiesterase (PDE) Neurological Disease

BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
HY-12814

TH588
DNA/RNA Synthesis Cancer

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC₅₀= 5 nM).

HY-12054

Hesperadin	Aurora Kinase Autophagy Influenza Virus Parasite	Cancer
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM.

HY-12420

JNJ-47117096 hydrochloride MELK-T1 hydrochloride	MELK FLT3	Cancer
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC₅₀ of 23 nM, also effectively inhibits Flt3, with an IC₅₀ of 18 nM.

HY-16982

Cercosporamide (-)-Cercosporamide	Fungal MNK	Cancer Infection
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC₅₀ of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

HY-136347

3α-Hydroxy pravastatin sodium	HMG-CoA Reductase (HMGCR) Drug Metabolite	Cardiovascular Disease
3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor.

HY-13280

IRAK inhibitor 6
IRAK Inflammation/Immunology

IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC₅₀ of 160 nM.
HY-N4186

Glabrolide
Beta-secretase Neurological Disease

Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].
HY-103002

SU5408
VEGFR2 Kinase Inhibitor I
VEGFR Cardiovascular Disease

SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC₅₀ of 70 nM.

HY-B0497B

Niclosamide monohydrate BAY2353 monohydrate	STAT Bacterial Antibiotic	Infection
Niclosamide monohydrate is an inhibitor of STAT3 with IC₅₀ of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.

HY-131446

Chk1-IN-5	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.

HY-50202

Etomoxir (R)-(+)-Etomoxir	Apoptosis	Cancer Metabolic Disease
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

HY-19727A

FOY 251	Ser/Thr Protease SARS-CoV	Metabolic Disease
FOY 251 is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.FOY 251 inhibit SARS-CoV-2 infection in cells assay.

HY-50202A

Etomoxir sodium salt (R)-(+)-Etomoxir sodium salt	Apoptosis	Metabolic Disease Cancer
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

HY-124416

ML604086	CCR	Inflammation/Immunology Endocrinology
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca²⁺ concentrations.

HY-103490

Takinib	MAP3K Apoptosis	Cancer
Takinib is a potent and selective TAK1 inhibitor with an IC₅₀ of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.

HY-17367A

Atazanavir sulfate BMS-232632 sulfate	HIV HIV Protease Cytochrome P450 P-glycoprotein	Cancer Infection
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).

HY-122866

ZT-12-037-01	Ras	Cancer
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC₅₀ of 24 nM.

HY-100227

E 64c	Cathepsin SARS-CoV	Metabolic Disease
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.

HY-66004

4-Acetamidophenyl acetate	Others	Inflammation/Immunology
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC₅₀=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

HY-115502

BCI (E)-BCI	Phosphatase	Cancer Inflammation/Immunology
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.

HY-15766A

GNE-617 hydrochloride	Nampt	Cancer
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

HY-15233

Letermovir
AIC246
CMV Infection

Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
HY-12399

MKC9989
IRE1 Cancer

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC₅₀ of 0.23 to 44 μM.

HY-101053

Src Inhibitor 1 Src Kinase Inhibitor 1; Src-l1	Src	Cancer
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC₅₀ values of 44 nM for Src and 88nM for Lck.

HY-10247

BRAF inhibitor
Raf Cancer

BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.

HY-N2522

Carboxyatractyloside dipotassium Gummiferin dipotassium	Others	Others
Carboxyatractyloside dipotassium is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.

HY-109565

ASTX660
IAP Cancer

ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
HY-108820

HIV-1 integrase inhibitor 4
HIV Integrase HIV Infection

HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 3.7 nM.
HY-108817

HIV-1 integrase inhibitor 3
HIV Integrase HIV Infection

HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 2.7 nM.

HY-10978

Crisaborole AN-2728; PF-06930164	Phosphodiesterase (PDE)	Inflammation/Immunology
Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC₅₀ of 0.49 μM.

HY-13452

CID-1067700
ML282
Ras Inflammation/Immunology

CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a K_i of 13 nM.
HY-119459

Fluopyram
Fungal Infection

Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC₅₀ of 3.35 µg/mL.
HY-135383A

(3S,5R)-Pitavastatin calcium
Others Metabolic Disease

(3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

HY-17469

Gimeracil Gimestat	Others	Cancer
Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.

HY-A0122

Plicamycin Mithramycin A	DNA/RNA Synthesis Bacterial Antibiotic	Cancer Infection
Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.

HY-17381

Idarubicin hydrochloride 4-Demethoxydaunorubicin hydrochloride	Topoisomerase Bacterial Fungal Autophagy	Cancer Infection
Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.

HY-N6031

Dendrophenol
NF-κB Cancer

Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.

HY-Y0172

Butylated hydroxytoluene	Ferroptosis	Cancer
Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products. Butylated hydroxytoluene is a Ferroptosis inhibitor.

HY-108941

Salicyl-AMS
Bacterial Infection

Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.

HY-15282

E-64 Proteinase inhibitor E 64	Cathepsin Autophagy Bacterial	Inflammation/Immunology Cancer
E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

HY-B0806

Proguanil	Parasite Antifolate	Infection
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.

HY-N2597

Prunetin	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
Prunetin, an O-methylated isoflavone, possesses anti-inflammatory activity. Prunetin is a potent human aldehyde dehydrogenases inhibitor.

HY-B0806A

Proguanil hydrochloride	Parasite Antifolate	Infection
Proguanil hydrochloride, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.

HY-13420

Zebularine NSC309132; 4-Deoxyuridine	DNA Methyltransferase Autophagy	Cancer
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a K_i of 0.95 μM.

HY-100736

ML348
GNF-Pf-1127
Phospholipase Cancer

ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC₅₀ of 210 nM, and barely inhibits LYPLA2.
HY-15202

Binimetinib
MEK162; ARRY-162; ARRY-438162
MEK Autophagy Cancer

Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.
HY-12726

Liproxstatin-1
Ferroptosis Cancer

Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC₅₀=22 nM).

HY-N1724

Concanamycin A Antibiotic X 4357B; Concanamycin; X 4357B	Proton Pump Bacterial Antibiotic	Cancer Infection
Concanamycin A (Antibiotic X 4357B) is a macrolide antibiotic and a specific vacuolar type H⁺-ATPase (V-ATPase) inhibitor.

HY-15766

GNE-617	Nampt	Metabolic Disease Cancer
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

HY-111489B

LMPTP INHIBITOR 1 dihydrochloride	Phosphatase	Metabolic Disease
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A.

HY-126253

BI-4916
Others Cancer

BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD⁺-competitive PHGDH inhibitor.
HY-136485

FEN1-IN-4
Others Cancer

FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.
HY-B1863

Iprobenfos
Fungal Infection

Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.

HY-B0882

Edrophonium chloride	AChE	Neurological Disease
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.

HY-100899

Heparastatin
Others Metabolic Disease

Heparastatin is a heparanase inhibitor.
HY-101705

Tibenelast sodium
LY 186655
Phosphodiesterase (PDE) Inflammation/Immunology

Tibenelast sodium is a phosphodiesterase inhibitor.
HY-14807

Tosedostat
CHR-2797
Aminopeptidase Cancer

Tosedostat is an aminopeptidase inhibitor.

HY-P1045

187-1, N-WASP inhibitor	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-124653

HSP27 inhibitor J2 J2	HSP	Cancer
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.

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.

HY-P1111A

Lyn peptide inhibitor TFA	Src Interleukin Related	Inflammation/Immunology
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.

HY-135899

SIRT7 inhibitor 97491	Sirtuin Apoptosis	Cancer
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC₅₀ of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

HY-B2145

Ilaprazole sodium IY-81149 sodium	Proton Pump TOPK	Cancer Inflammation/Immunology
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H⁺/K⁺-ATPase in a dose-dependent manner with an IC₅₀ of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

HY-107412

Proteasome inhibitor IX PS-IX; AM114	Proteasome	Cancer
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.

HY-130795

GSK-3β inhibitor 2	GSK-3	Neurological Disease
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC₅₀ of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.

HY-N7674A

Angoline hydrochloride	STAT	Cancer
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

HY-13624A

Epirubicin hydrochloride 4'-Epidoxorubicin hydrochloride	Topoisomerase Apoptosis	Cancer
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.

HY-P1290

PKA Inhibitor Fragment (6-22) amide PKI-(6-22)-amide	PKA	Neurological Disease
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a K_i of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.

HY-10009

Semagacestat LY450139	γ-secretase Amyloid-β Notch	Neurological Disease
Semagacestat is a γ-secretase inhibitor, inhibits β-amyloid (Aβ42), Aβ38 and Aβ40 with IC₅₀ of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC₅₀ of 14.1 nM.

HY-N7674

Angoline	STAT	Cancer
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

HY-109019

Vorolanib CM082; X-82	VEGFR PDGFR	Cancer Cardiovascular Disease
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).

HY-100734

Histone Acetyltransferase Inhibitor II	Histone Acetyltransferase	Cancer
Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC₅₀ of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

HY-123772

CDK5 inhibitor 20-223	CDK	Cancer
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC₅₀s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.

HY-13624

Epirubicin 4'-Epidoxorubicin	Topoisomerase Apoptosis	Cancer
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.

HY-N6619

Lycoramine hydrobromide	AChE	Neurological Disease
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase (AChE) inhibitor.

HY-109877

Ro 22-3581
4'-(Imidazol-1-yl) acetophenone
Others Cardiovascular Disease

Ro 22-3581 (4'-(Imidazol-1-yl) acetophenone) is a selective thromboxane (Tx) synthetase inhibitor.

HY-100299

RPR107393 free base	Farnesyl Transferase	Metabolic Disease
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC₅₀ of 0.8 nM.

HY-P2470

Human PD-L1 inhibitor II
PD-1/PD-L1 Cancer

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.
HY-B0106

Levetiracetam
UCB L059
mAChR Neurological Disease

Levetiracetam (UCB L059) is a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. Antiepileptic agent.
HY-50710

KU-0063794
mTOR Cancer

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.
HY-137239

1,4-DPCA ethyl ester
HIF/HIF Prolyl-Hydroxylase Cancer

1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
HY-100303A

FR194738
Others Metabolic Disease

FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC₅₀ of 9.8 nM.

HY-50946

Imatinib Mesylate STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

HY-15886

Mdivi-1 Mitochondrial division inhibitor 1	Dynamin Mitophagy Autophagy Apoptosis	Cancer
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. Mdivi-1 is a mitochondrial division/mitophagy inhibitor.

HY-112131

MAT2A inhibitor 1
Others Cancer

MAT2A inhibitor 1 is a methionine adenosyltransferase 2A (MATA2) inhibitor with an IC₅₀ less than l00 nM.
HY-19326

SU1498
AG 1498; Tyrphostin SU 1498
VEGFR Cancer Inflammation/Immunology

SU1498 (AG 1498) is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC₅₀ of value of 700 nM.
HY-12971

Nampt-IN-1
LSN3154567
Nampt Cancer

Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC₅₀ of 3.1 nM.
HY-101479

Iclaprim
AR-100
Bacterial Infection

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-108900A

Leu-AMS R enantiomer	Aminoacyl-tRNA Synthetase	Others
Leu-AMS R enantiomer is the R enatiomer of Leu-AMS. Leu-AMS is a potent inhibitor of leucyl-tRNA synthetase (LRS) and inhibits the growth of bacteria.

HY-N5118

Chimonanthine (-)-Chimonanthine	Tyrosinase	Cancer
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.

HY-U00049

Mioflazine	Others	Neurological Disease Cardiovascular Disease
Mioflazine is an orally active nucleoside transport inhibitor, has the potential for sleep disorders treatment. Mioflazine inhibits nucleoside uptake.

HY-16904

RI-2
RAD51 Cancer

RI-2 is a reversible RAD51 inhibitor, with an IC₅₀ of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
HY-130760

HIV-1 integrase inhibitor 7
HIV Integrase Infection

HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC₅₀ of 33.3 nM.
HY-103036

BET bromodomain inhibitor
Epigenetic Reader Domain Cancer

BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
HY-111410

ATX inhibitor 1
Phosphodiesterase (PDE) Cancer

ATX inhibitor 1 is a potent ATX (IC₅₀=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
HY-13229

BOC-D-FMK
Caspase Cancer

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC₅₀ of 39 µM.
HY-10862

FAAH inhibitor 1
Benzothiazole analog 3
FAAH Autophagy Cancer

FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ of 18±8 nM.

HY-13256A

Desmethyl Erlotinib OSI-420 free base; CP-373420	Drug Metabolite	Cancer
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.

HY-15735

c-Met inhibitor 1	c-Met/HGFR	Cancer
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.

HY-10997S

Ibrutinib D5
PCI-32765 D5
Btk Cancer

Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
HY-15586

L67
DNA Ligase Inhibitor
DNA/RNA Synthesis Cancer

L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
HY-B0008

Sulindac
MK-231
COX Autophagy Inflammation/Immunology Cancer

Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.

HY-115502A

BCI hydrochloride (E)-BCI hydrochloride	Phosphatase	Cancer Inflammation/Immunology
BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and DUSP1 with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.

HY-136538

LQZ-7I	Survivin	Cancer
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.

HY-19727

FOY 251 free base	Ser/Thr Protease SARS-CoV	Metabolic Disease
FOY 251 free base is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.FOY 25 free base inhibit SARS-CoV-2 infection in cells assay.

HY-N2006

Ganoderic acid B	HIV Protease	Infection
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.

HY-P1376

G-Protein antagonist peptide	mAChR Adrenergic Receptor
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

HY-114169

WRG-28	Discoidin Domain Receptor	Cancer
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC₅₀ of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.

HY-16592

Brefeldin A BFA; Cyanein; Decumbin	Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic	Cancer Infection
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.

HY-101664

Ilaprazole IY-81149	Proton Pump TOPK	Cancer Inflammation/Immunology
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H⁺/K⁺-ATPase in a dose-dependent manner with an IC₅₀ of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

HY-112373

Aurora Kinase Inhibitor 3	Aurora Kinase	Others
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC₅₀ of 42 nM, and weakly inhibits EGFR with an IC₅₀>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures.

HY-135396

(1S,2S)-Bortezomib	Proteasome	Cancer
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.

HY-13803C

Tazemetostat hydrobromide EPZ-6438 hydrobromide; E-7438 hydrobromide	Histone Methyltransferase	Cancer
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC₅₀ of 392 nM.

HY-P1290A

PKA Inhibitor Fragment (6-22) amide TFA PKI-(6-22)-amide TFA	PKA	Neurological Disease
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a K_i of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.

HY-B0166

L-Ascorbic acid L-Ascorbate; Vitamin C	Calcium Channel Reactive Oxygen Species Apoptosis	Metabolic Disease
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-P0222

PKI(5-24)	PKA	Others
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a K_i of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.

HY-114996

ADAMTS-5 Inhibitor	Others	Inflammation/Immunology
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC₅₀ of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).

HY-103032

Multi-kinase inhibitor 1	PDGFR c-Kit Bcr-Abl	Cancer
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.

HY-Y0445A

Sodium dichloroacetate	PDHK Reactive Oxygen Species NKCC Apoptosis	Cancer
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.

HY-66005

Acetaminophen Paracetamol; 4-Acetamidophenol; 4'-Hydroxyacetanilide	COX Histone Acetyltransferase Endogenous Metabolite	Inflammation/Immunology
Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

HY-13512

Camostat mesylate Camostat mesilate; FOY305; FOY-S980	Ser/Thr Protease SARS-CoV	Infection Inflammation/Immunology
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.

HY-122632

Ciliobrevin D	Hedgehog	Cancer
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

HY-16594

Lactacystin	Proteasome	Neurological Disease
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC₅₀ of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.

HY-B0166A

L-Ascorbic acid sodium salt Sodium L-ascorbate; Vitamin C sodium salt	Calcium Channel Reactive Oxygen Species Apoptosis	Cancer
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-135391

Ezetimibe phenoxy glucuronide Ezetimibe glucuronide; Ezetimibe β-D-glucuronide	Drug Metabolite	Metabolic Disease
Ezetimibe phenoxy glucuronide (Ezetimibe glucuronide) is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.

HY-50909

Perifosine KRX-0401; NSC 639966; D21266	Akt Autophagy Apoptosis	Cancer
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC₅₀s of 0.6-8.9 μM.

HY-101766

Btk inhibitor 2
BGB-3111 analog
Btk Inflammation/Immunology

Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
HY-16510A

UNC926 hydrochloride
Epigenetic Reader Domain Cancer

UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM.

HY-N0143

Phlorizin Floridzin; NSC 2833	SGLT Na+/K+ ATPase	Metabolic Disease
Phlorizin is a non-selective SGLT inhibitor with K_is of 300 and 39 nM for hSGLT1 and hSGLT2, respectively. Phlorizin is also a Na⁺/K⁺-ATPase inhibitor.

HY-U00096

Ansofaxine hydrochloride LY03005; LPM570065	5-HT Receptor Dopamine Receptor	Inflammation/Immunology Neurological Disease
Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC₅₀ values of 723, 491 and 763 nM, respectively.

HY-B1243

Propoxycaine hydrochloride	Sodium Channel	Neurological Disease
Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation.

HY-32351

Calcifediol 25-hydroxy Vitamin D3	VD/VDR Endogenous Metabolite	Metabolic Disease
Calcifediol (25-hydroxy Vitamin D3), a major circulating metabolite of vitamin D3, is a potent VDR inhibitor.

HY-13012

RepSox
E-616452; SJN 2511
TGF-β Receptor Cancer

RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC₅₀ of 4 nM.

HY-N7089

Benzoyleneurea	Bacterial	Infection
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.

HY-18931A

NSC305787 hydrochloride	Others	Cancer
NSC305787 hydrochloride is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

HY-15247

Vistusertib
AZD2014
mTOR Autophagy Apoptosis Cancer

Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
HY-16510

UNC926
Epigenetic Reader Domain Cancer

UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM.
HY-12357

Bempedoic acid
ETC-1002; ESP-55016
ATP Citrate Lyase AMPK Metabolic Disease

Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.
HY-101464

ML329
Others Others

ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC₅₀ of 1.2 μM.

HY-12682

Glutaminase C-IN-1 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-102007A

Gamitrinib TPP hexafluorophosphate	HSP	Cancer
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.

HY-100541

INH6
Apoptosis Cancer

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC₅₀ of 2.4 μM.

HY-32351A

Calcifediol monohydrate 25-hydroxy Vitamin D3 monohydrate	VD/VDR Endogenous Metabolite	Metabolic Disease
Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), a major circulating metabolite of vitamin D3, is a potent VDR inhibitor.

HY-100735

C 87
TNF Receptor Inflammation/Immunology

C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC₅₀ of 8.73 μM.

HY-13067

Tripterin Celastrol	Proteasome Autophagy Mitophagy Apoptosis	Inflammation/Immunology Cancer
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

HY-15679

PI4KIII beta inhibitor 3
PI4K Cancer

PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC₅₀ of 5.7 nM.
HY-19352

T56-LIMKi
T5601640
LIM Kinase (LIMK) Cancer

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC₅₀ of 35.2 μM.
HY-107433

U18666A
HCV Infection Neurological Disease

U18666A, an intra-cellular cholesterol transport inhibitor, inhibits replication of Ebola virus, dengue virus, and human hepatitis C virus.

HY-126134

HPGDS inhibitor 2	PGE synthase	Inflammation/Immunology
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC₅₀ of 9.9 nM.

HY-18931

NSC305787
Others Cancer

NSC305787 is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

HY-15223

MI-3 Menin-MLL inhibitor 3	Epigenetic Reader Domain Apoptosis	Cancer
MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC₅₀ of 648 nM and a K_d of 201 nM.

HY-15457

Triciribine API-2; NSC 154020; TCN	DNA/RNA Synthesis Akt HIV	Cancer
Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC₅₀ of 130 nM, and 0.02-0.46 μM, respectively.

HY-100792

URB602
Others Cancer

URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC₅₀ of 28±4 μM through a noncompetitive mechanism.

HY-112164

IACS-8968 IDO/TDO Inhibitor	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
IACS-8968 (IDO/TDO Inhibitor) is a dual IDO and TDO inhibitor, with pIC₅₀s of 6.43 for IDO and <5 for TDO, respectively.

HY-N7452

Coumermycin A1
JAK Bacterial Metabolic Disease

Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.
HY-N0149

Salicin
D-(−)-Salicin; Salicoside
COX Cancer Inflammation/Immunology

Salicin is a natural COX inhibitor.
HY-100263

Metofenazate
Methophenazine
CaMK Autophagy Neurological Disease

Metofenazate is a selective calmodulin inhibitor.
HY-N0342

Scopoletin
Gelseminic acid; Chrysatropic acid
AChE Apoptosis Inflammation/Immunology

Scopoletin is an inhibitor of acetylcholinesterase (AChE).
HY-101244

ZINC00881524
ROCK Cancer

ZINC00881524 is a ROCK inhibitor.
HY-100384

NKL 22
HDAC Cancer

NKL 22 is a HDAC inhibitor.
HY-112870A

AST2818 mesylate
EGFR Cancer

AST2818 mesylate is an EGFR inhibitor.
HY-P0290A

GRGDSP TFA
Integrin Cancer

GRGDSP (TFA) is an integrin inhibitor.

HY-19763

BEBT-908 PI3Kα inhibitor 1	PI3K	Cancer
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC₅₀<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC₅₀≤1 μM) .

HY-N0822

Shikonin C.I. 75535; Isoarnebin 4	Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV	Cancer
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.

HY-18979

Lactimidomycin	Influenza Virus	Cancer Infection
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC₅₀ value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.

HY-23460A

4-Ethynyl-L-phenylalanine hydrochloride	Tryptophan Hydroxylase	Neurological Disease
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a K_i of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin.

HY-103194

KH7	Others	Others
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC₅₀s of 3-10 μM toward both recombinant purified human sAC_t protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.

HY-23460

4-Ethynyl-L-phenylalanine	Tryptophan Hydroxylase	Neurological Disease
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a K_i of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin.

HY-P1376A

G-Protein antagonist peptide TFA	mAChR Adrenergic Receptor
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

HY-133114

Ezetimibe ketone EZM-K	Keap1-Nrf2 Autophagy	Cancer Cardiovascular Disease
Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.

HY-W006230

Anthraflavic acid	Others	Cancer
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.

HY-118532

Tyrphostin AG30 AG30	EGFR	Cancer
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

HY-N0112

Dihydromyricetin Ampelopsin; Ampeloptin	mTOR Influenza Virus DNA/RNA Synthesis Autophagy	Cancer Infection
Dihydromyricetin is a potent inhibitor with an IC₅₀ of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 22 nM.

HY-11001

PHA-793887	CDK Apoptosis	Cancer
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC₅₀s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC₅₀ of 79 nM.

HY-100222

CZ415
mTOR Cancer

CZ415 is a potent and highly selective mTOR inhibitor with a pIC₅₀ of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

HY-119692

Curvulin	Microtubule/Tubulin	Others
Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.

HY-12056

BIX02189
MEK ERK Cancer

BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC₅₀ of 59 nM.

HY-12957

NITD008 7-Deaza-2'-C-acetylene-adenosine	DNA/RNA Synthesis Influenza Virus	Infection
NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC₅₀ of 0.64 μM.

HY-10367A

Canertinib dihydrochloride CI-1033 dihydrochloride; PD-183805 dihydrochloride	EGFR	Cancer
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM.

HY-135383

(3S,5S)-Pitavastatin calcium
Others Metabolic Disease

(3S,5S)-Pitavastatin cacium is the 3-epimer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
HY-12204

PFK-015
Autophagy Cancer

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.

HY-100750

Norverapamil hydrochloride (±)-Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-13577A

Oclacitinib maleate PF-03394197 maleate	JAK	Inflammation/Immunology
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC₅₀=10 nM).

HY-N3002

α-Arbutin 4-Hydroxyphenyl α-D-glucopyranoside	Tyrosinase	Metabolic Disease
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.

HY-111357

Antifungal agent 2	Fungal	Infection
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.

HY-13966

2-Deoxy-D-glucose 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose	Hexokinase HSV Apoptosis	Cancer
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase.

HY-12589

ZM39923 hydrochloride	JAK	Cancer Neurological Disease
ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC₅₀ of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.

HY-126482

Telomerase-IN-2	Telomerase	Cancer
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC₅₀ of 0.89 µM. Anti-cancer activity.

HY-15162A

D8-MMAE D8-Monomethyl auristatin E	Microtubule/Tubulin ADC Cytotoxin	Cancer
D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

HY-15417

ML-7 hydrochloride
Myosin YAP Cancer

ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC₅₀=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
HY-12622

HSP70-IN-1
HSP Cancer

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC₅₀ of 2.3 μM.

HY-112861A

Gln-AMS TFA	Aminoacyl-tRNA Synthetase	Infection
Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor. Gln-AMS inhibits glutaminyl-tRNA synthetase (GlnRS) with a K_i of 1.32 µM.