Search Result

Pathways Recommended:	TGF-beta/Smad
Targets Recommended:	TGF-beta/Smad β-catenin TGF-β Receptor Beta-secretase Dopamine β-hydroxylase CRM1 PD-1/PD-L1 Mps1 PAI-1 PDK-1 IRE1 Wee1 URAT1 Ack1 sFRP-1 MALT1 PGC-1α IGF-1R MCHR1 (GPR24) Keap1-Nrf2 Adrenergic Receptor Amyloid-β E1/E2/E3 Enzyme c-Fms IFNAR GPR40 EGFR IRAK EAAT2 Adenosine Receptor P-glycoprotein FXR PTEN Oct3/4 PIKfyve

Results for "ActiveIL-1 beta Inhibitors" in MCE Product Catalog:

By Targets:	Ack1 (2) Adenosine Receptor (13) Adrenergic Receptor (169) Amyloid-β (73) Beta-secretase (20) c-Fms (23) CRM1 (2) Dopamine β-hydroxylase (6) E1/E2/E3 Enzyme (58) EAAT2 (3) EGFR (144) FXR (5) GPR40 (3) IFNAR (7) IGF-1R (21) IRAK (18) IRE1 (16) Keap1-Nrf2 (25) MALT1 (5) Mps1 (10) P-glycoprotein (40) PAI-1 (8) PD-1/PD-L1 (13) PDK-1 (6) PGC-1α (1) PIKfyve (5) PTEN (5) sFRP-1 (1) TGF-beta/Smad (18) TGF-β Receptor (40) URAT1 (4) Wee1 (5) β-catenin (31) 15-PGDH (1) 5 alpha Reductase (7) 5-HT Receptor (59) Acetyl-CoA Carboxylase (10) AChE (88) Acyltransferase (38) ADC Cytotoxin (47) ADC Linker (8) Adenosine Deaminase (7) Adenosine Kinase (2) Adenylate Cyclase (10) Adiponectin Receptor (1) Akt (66) Aldehyde Dehydrogenase (ALDH) (11) Aldose Reductase (17) ALK (29) Aminoacyl-tRNA Synthetase (10) Aminopeptidase (11) AMPK (33) Androgen Receptor (16) Angiotensin Receptor (13) Angiotensin-converting Enzyme (ACE) (48) Antibiotic (317) Antifolate (21) APC (4) Apoptosis (917) Arenavirus (4) Arginase (7) Aromatase (11) Arp2/3 Complex (9) Aryl Hydrocarbon Receptor (12) ATGL (1) ATM/ATR (18) ATP Citrate Lyase (8) ATP Synthase (9) Aurora Kinase (42) Autophagy (682) Bacterial (525) Bcl-2 Family (55) Bcr-Abl (44) BCRP (13) BMX Kinase (3) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (43) c-Kit (49) c-Met/HGFR (51) c-Myc (12) Calcium Channel (78) CaMK (22) Cannabinoid Receptor (15) Carbonic Anhydrase (19) Carboxypeptidase (4) Casein Kinase (35) Caspase (39) CaSR (1) Cathepsin (33) CCR (23) CD73 (8) CDK (155) CETP (6) CFTR (6) CGRP Receptor (7) Checkpoint Kinase (Chk) (23) Chloride Channel (11) Cholecystokinin Receptor (6) CMV (19) Complement System (15) COMT (12) COX (180) CRAC Channel (10) CRFR (8) CRISPR/Cas9 (7) CXCR (26) Cyclic GMP-AMP Synthase (4) Cytochrome P450 (97) DAPK (1) Deubiquitinase (37) Dihydroorotate Dehydrogenase (14) Dipeptidyl Peptidase (36) Discoidin Domain Receptor (10) DNA Alkylator/Crosslinker (11) DNA Methyltransferase (22) DNA-PK (20) DNA/RNA Synthesis (151) Dopamine Receptor (39) Dopamine Transporter (15) Drug Metabolite (62) Drug-Linker Conjugates for ADC (33) Dynamin (6) DYRK (17) E3 Ligase Ligand-Linker Conjugate (2) Elastase (17) Endogenous Metabolite (268) Endothelin Receptor (15) Enolase (2) Enterovirus (16) Ephrin Receptor (6) Epigenetic Reader Domain (119) Epoxide Hydrolase (13) ERK (56) Estrogen Receptor/ERR (59) Eukaryotic Initiation Factor (eIF) (19) FAAH (20) FABP (3) Factor Xa (11) FAK (24) Farnesyl Transferase (20) Fatty Acid Synthase (FASN) (25) Ferroptosis (68) FGFR (63) Filovirus (4) FKBP (7) FLAP (8) FLT3 (65) Fungal (125) G-quadruplex (4) GABA Receptor (45) Galectin (3) Gap Junction Protein (6) GHSR (3) Gli (3) Glucagon Receptor (8) Glucocorticoid Receptor (9) Glucokinase (1) Glucosidase (31) GLUT (11) Glutaminase (9) Glutathione Peroxidase (10) GlyT (8) GPCR19 (2) GPR119 (2) GPR120 (1) GPR55 (1) GSK-3 (47) GSNOR (1) Guanylate Cyclase (5) Gutathione S-transferase (8) Haspin Kinase (3) HBV (30) HCN Channel (2) HCV (97) HCV Protease (17) HDAC (99) Hedgehog (12) Hexokinase (4) HIF/HIF Prolyl-Hydroxylase (40) Hippo (MST) (3) Histamine Receptor (34) Histone Acetyltransferase (36) Histone Demethylase (41) Histone Methyltransferase (96) HIV (200) HIV Integrase (20) HIV Protease (25) HMG-CoA Reductase (HMGCR) (37) HSP (48) HSV (45) IAP (10) iGluR (23) IKK (32) Imidazoline Receptor (4) Indoleamine 2,3-Dioxygenase (IDO) (33) Influenza Virus (99) Insulin Receptor (14) Integrin (59) Interleukin Related (59) Isocitrate Dehydrogenase (IDH) (15) Itk (5) JAK (85) JNK (32) Kinesin (18) KLF (4) Lactate Dehydrogenase (11) Leukotriene Receptor (19) Ligand for E3 Ligase (8) Ligand for Target Protein for PROTAC (20) LIM Kinase (LIMK) (5) Lipoxygenase (40) LPL Receptor (12) LRRK2 (15) LXR (11) mAChR (33) MAGL (16) MAP3K (14) MAP4K (8) MAPKAPK2 (MK2) (4) MDM-2/p53 (46) MEK (35) Melanocortin Receptor (4) Melatonin Receptor (2) MELK (3) mGluR (8) MicroRNA (10) Microtubule/Tubulin (94) Mineralocorticoid Receptor (2) Mitochondrial Metabolism (41) Mitophagy (54) Mixed Lineage Kinase (4) MMP (61) MNK (5) Monoamine Oxidase (64) Monoamine Transporter (11) Monocarboxylate Transporter (7) mTOR (68) MyD88 (4) Myosin (13) Na+/Ca2+ Exchanger (10) Na+/HCO3- Cotransporter (1) Na+/K+ ATPase (21) nAChR (45) NADPH Oxidase (10) Nampt (13) NEDD8-activating Enzyme (6) Neprilysin (14) Neurokinin Receptor (3) Neuropeptide Y Receptor (7) Neurotensin Receptor (2) NF-κB (147) NKCC (6) NO Synthase (44) NOD-like Receptor (NLR) (18) Notch (22) Nucleoside Antimetabolite/Analog (47) Opioid Receptor (17) Orexin Receptor (OX Receptor) (2) Oxytocin Receptor (1) P2X Receptor (10) P2Y Receptor (12) p38 MAPK (63) p97 (7) PAK (12) Parasite (160) PARP (54) PDGFR (73) PDHK (9) PERK (4) PGE synthase (12) Phosphatase (107) Phosphodiesterase (PDE) (148) Phospholipase (48) PI3K (130) PI4K (12) Pim (18) PKA (31) PKC (77) PKD (4) Polo-like Kinase (PLK) (22) Porcupine (8) Potassium Channel (90) PPAR (32) Procollagen C Proteinase (1) Progesterone Receptor (3) Prostaglandin Receptor (32) PROTAC (16) PROTAC Linker (15) Protease-Activated Receptor (PAR) (10) Proteasome (44) Protein Arginine Deiminase (7) Proton Pump (38) Pyk2 (4) Pyroptosis (2) Pyruvate Kinase (2) RAD51 (6) Raf (47) RAR/RXR (22) Ras (64) Reactive Oxygen Species (77) Renin (4) RET (24) Reverse Transcriptase (51) RGS Protein (3) Ribosomal S6 Kinase (RSK) (21) RIP kinase (29) ROCK (39) ROR (9) ROS (8) RSV (16) Salt-inducible Kinase (SIK) (7) SARS-CoV (71) Ser/Thr Protease (19) Serotonin Transporter (39) SGK (7) SGLT (19) Sigma Receptor (6) Sirtuin (29) Smo (11) SNIPER (8) Sodium Channel (81) Somatostatin Receptor (3) SPHK (9) Src (63) SRPK (3) STAT (66) Stearoyl-CoA Desaturase (SCD) (10) STING (6) Survivin (3) Syk (24) TAM Receptor (20) Telomerase (8) Thrombin (22) Thymidylate Synthase (9) Thyroid Hormone Receptor (8) TNF Receptor (46) Toll-like Receptor (TLR) (29) TOPK (6) Topoisomerase (98) Trk Receptor (21) TRP Channel (40) Tryptophan Hydroxylase (9) TSH Receptor (2) Tyrosinase (37) ULK (6) Urotensin Receptor (1) VD/VDR (6) VDAC (2) VEGFR (127) Virus Protease (36) Wnt (47) Xanthine Oxidase (12) YAP (9) γ-secretase (27)
By Research Areas:	Cancer (4323) Cardiovascular Disease (719) Endocrinology (345) Infection (1234) Inflammation/Immunology (1534) Metabolic Disease (836) Neurological Disease (1124)

By Targets:

Ack1 (2)

Adenosine Receptor (13)

Adrenergic Receptor (169)

Amyloid-β (73)

Beta-secretase (20)

c-Fms (23)

CRM1 (2)

Dopamine β-hydroxylase (6)

E1/E2/E3 Enzyme (58)

EAAT2 (3)

EGFR (144)

FXR (5)

GPR40 (3)

IFNAR (7)

IGF-1R (21)

IRAK (18)

IRE1 (16)

Keap1-Nrf2 (25)

MALT1 (5)

Mps1 (10)

P-glycoprotein (40)

PAI-1 (8)

PD-1/PD-L1 (13)

PDK-1 (6)

PGC-1α (1)

PIKfyve (5)

PTEN (5)

sFRP-1 (1)

TGF-beta/Smad (18)

TGF-β Receptor (40)

URAT1 (4)

Wee1 (5)

β-catenin (31)

15-PGDH (1)

5 alpha Reductase (7)

5-HT Receptor (59)

Acetyl-CoA Carboxylase (10)

AChE (88)

Acyltransferase (38)

ADC Cytotoxin (47)

ADC Linker (8)

Adenosine Deaminase (7)

Adenosine Kinase (2)

Adenylate Cyclase (10)

Adiponectin Receptor (1)

Akt (66)

Aldehyde Dehydrogenase (ALDH) (11)

Aldose Reductase (17)

ALK (29)

Aminoacyl-tRNA Synthetase (10)

Aminopeptidase (11)

AMPK (33)

Androgen Receptor (16)

Angiotensin Receptor (13)

Angiotensin-converting Enzyme (ACE) (48)

Antibiotic (317)

Antifolate (21)

APC (4)

Apoptosis (917)

Arenavirus (4)

Arginase (7)

Aromatase (11)

Arp2/3 Complex (9)

Aryl Hydrocarbon Receptor (12)

ATGL (1)

ATM/ATR (18)

ATP Citrate Lyase (8)

ATP Synthase (9)

Aurora Kinase (42)

Autophagy (682)

Bacterial (525)

Bcl-2 Family (55)

Bcr-Abl (44)

BCRP (13)

BMX Kinase (3)

Bombesin Receptor (1)

Bradykinin Receptor (1)

Btk (43)

c-Kit (49)

c-Met/HGFR (51)

c-Myc (12)

Calcium Channel (78)

CaMK (22)

Cannabinoid Receptor (15)

Carbonic Anhydrase (19)

Carboxypeptidase (4)

Casein Kinase (35)

Caspase (39)

CaSR (1)

Cathepsin (33)

CCR (23)

CD73 (8)

CDK (155)

CETP (6)

CFTR (6)

CGRP Receptor (7)

Checkpoint Kinase (Chk) (23)

Chloride Channel (11)

Cholecystokinin Receptor (6)

CMV (19)

Complement System (15)

COMT (12)

COX (180)

CRAC Channel (10)

CRFR (8)

CRISPR/Cas9 (7)

CXCR (26)

Cyclic GMP-AMP Synthase (4)

Cytochrome P450 (97)

DAPK (1)

Deubiquitinase (37)

Dihydroorotate Dehydrogenase (14)

Dipeptidyl Peptidase (36)

Discoidin Domain Receptor (10)

DNA Alkylator/Crosslinker (11)

DNA Methyltransferase (22)

DNA-PK (20)

DNA/RNA Synthesis (151)

Dopamine Receptor (39)

Dopamine Transporter (15)

Drug Metabolite (62)

Drug-Linker Conjugates for ADC (33)

Dynamin (6)

DYRK (17)

E3 Ligase Ligand-Linker Conjugate (2)

Elastase (17)

Endogenous Metabolite (268)

Endothelin Receptor (15)

Enolase (2)

Enterovirus (16)

Ephrin Receptor (6)

Epigenetic Reader Domain (119)

Epoxide Hydrolase (13)

ERK (56)

Estrogen Receptor/ERR (59)

Eukaryotic Initiation Factor (eIF) (19)

FAAH (20)

FABP (3)

Factor Xa (11)

FAK (24)

Farnesyl Transferase (20)

Fatty Acid Synthase (FASN) (25)

Ferroptosis (68)

FGFR (63)

Filovirus (4)

FKBP (7)

FLAP (8)

FLT3 (65)

Fungal (125)

G-quadruplex (4)

GABA Receptor (45)

Galectin (3)

Gap Junction Protein (6)

GHSR (3)

Gli (3)

Glucagon Receptor (8)

Glucocorticoid Receptor (9)

Glucokinase (1)

Glucosidase (31)

GLUT (11)

Glutaminase (9)

Glutathione Peroxidase (10)

GlyT (8)

GPCR19 (2)

GPR119 (2)

GPR120 (1)

GPR55 (1)

GSK-3 (47)

GSNOR (1)

Guanylate Cyclase (5)

Gutathione S-transferase (8)

Haspin Kinase (3)

HBV (30)

HCN Channel (2)

HCV (97)

HCV Protease (17)

HDAC (99)

Hedgehog (12)

Hexokinase (4)

HIF/HIF Prolyl-Hydroxylase (40)

Hippo (MST) (3)

Histamine Receptor (34)

Histone Acetyltransferase (36)

Histone Demethylase (41)

Histone Methyltransferase (96)

HIV (200)

HIV Integrase (20)

HIV Protease (25)

HMG-CoA Reductase (HMGCR) (37)

HSP (48)

HSV (45)

IAP (10)

iGluR (23)

IKK (32)

Imidazoline Receptor (4)

Indoleamine 2,3-Dioxygenase (IDO) (33)

Influenza Virus (99)

Insulin Receptor (14)

Integrin (59)

Interleukin Related (59)

Isocitrate Dehydrogenase (IDH) (15)

Itk (5)

JAK (85)

JNK (32)

Kinesin (18)

KLF (4)

Lactate Dehydrogenase (11)

Leukotriene Receptor (19)

Ligand for E3 Ligase (8)

Ligand for Target Protein for PROTAC (20)

LIM Kinase (LIMK) (5)

Lipoxygenase (40)

LPL Receptor (12)

LRRK2 (15)

LXR (11)

mAChR (33)

MAGL (16)

MAP3K (14)

MAP4K (8)

MAPKAPK2 (MK2) (4)

MDM-2/p53 (46)

MEK (35)

Melanocortin Receptor (4)

Melatonin Receptor (2)

MELK (3)

mGluR (8)

MicroRNA (10)

Microtubule/Tubulin (94)

Mineralocorticoid Receptor (2)

Mitochondrial Metabolism (41)

Mitophagy (54)

Mixed Lineage Kinase (4)

MMP (61)

MNK (5)

Monoamine Oxidase (64)

Monoamine Transporter (11)

Monocarboxylate Transporter (7)

mTOR (68)

MyD88 (4)

Myosin (13)

Na+/Ca2+ Exchanger (10)

Na+/HCO3- Cotransporter (1)

Na+/K+ ATPase (21)

nAChR (45)

NADPH Oxidase (10)

Nampt (13)

NEDD8-activating Enzyme (6)

Neprilysin (14)

Neurokinin Receptor (3)

Neuropeptide Y Receptor (7)

Neurotensin Receptor (2)

NF-κB (147)

NKCC (6)

NO Synthase (44)

NOD-like Receptor (NLR) (18)

Notch (22)

Nucleoside Antimetabolite/Analog (47)

Opioid Receptor (17)

Orexin Receptor (OX Receptor) (2)

Oxytocin Receptor (1)

P2X Receptor (10)

P2Y Receptor (12)

p38 MAPK (63)

p97 (7)

PAK (12)

Parasite (160)

PARP (54)

PDGFR (73)

PDHK (9)

PERK (4)

PGE synthase (12)

Phosphatase (107)

Phosphodiesterase (PDE) (148)

Phospholipase (48)

PI3K (130)

PI4K (12)

Pim (18)

PKA (31)

PKC (77)

PKD (4)

Polo-like Kinase (PLK) (22)

Porcupine (8)

Potassium Channel (90)

PPAR (32)

Procollagen C Proteinase (1)

Progesterone Receptor (3)

Prostaglandin Receptor (32)

PROTAC (16)

PROTAC Linker (15)

Protease-Activated Receptor (PAR) (10)

Proteasome (44)

Protein Arginine Deiminase (7)

Proton Pump (38)

Pyk2 (4)

Pyroptosis (2)

Pyruvate Kinase (2)

RAD51 (6)

Raf (47)

RAR/RXR (22)

Ras (64)

Reactive Oxygen Species (77)

Renin (4)

RET (24)

Reverse Transcriptase (51)

RGS Protein (3)

Ribosomal S6 Kinase (RSK) (21)

RIP kinase (29)

ROCK (39)

ROR (9)

ROS (8)

RSV (16)

Salt-inducible Kinase (SIK) (7)

SARS-CoV (71)

Ser/Thr Protease (19)

Serotonin Transporter (39)

SGK (7)

SGLT (19)

Sigma Receptor (6)

Sirtuin (29)

Smo (11)

SNIPER (8)

Sodium Channel (81)

Somatostatin Receptor (3)

SPHK (9)

Src (63)

SRPK (3)

STAT (66)

Stearoyl-CoA Desaturase (SCD) (10)

STING (6)

Survivin (3)

Syk (24)

TAM Receptor (20)

Telomerase (8)

Thrombin (22)

Thymidylate Synthase (9)

Thyroid Hormone Receptor (8)

TNF Receptor (46)

Toll-like Receptor (TLR) (29)

TOPK (6)

Topoisomerase (98)

Trk Receptor (21)

TRP Channel (40)

Tryptophan Hydroxylase (9)

TSH Receptor (2)

Tyrosinase (37)

ULK (6)

Urotensin Receptor (1)

VD/VDR (6)

VDAC (2)

VEGFR (127)

Virus Protease (36)

Wnt (47)

Xanthine Oxidase (12)

YAP (9)

γ-secretase (27)

By Research Areas:

Cancer (4323)

Cardiovascular Disease (719)

Endocrinology (345)

Infection (1234)

Inflammation/Immunology (1534)

Metabolic Disease (836)

Neurological Disease (1124)

8614

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

382

Peptides

MCE Kits

Inhibitory Antibodies

1606

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

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-16702

Pifithrin-β
PFT β
MDM-2/p53 Cancer

Pifithrin-β (PFT β) is a potent p53 inhibitor with an IC₅₀ of 23 μM.
HY-16702A

Pifithrin-β hydrobromide
PFT β hydrobromide
MDM-2/p53 Ferroptosis Cancer

Pifithrin-β hydrobromide (PFT β hydrobromide) is a potent p53 inhibitor with an IC₅₀ of 23 μM.

*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.

Pifithrin-β PFT β	MDM-2/p53	Cancer
Pifithrin-β (PFT β) is a potent p53 inhibitor with an IC₅₀ of 23 μM.

Pifithrin-β hydrobromide PFT β hydrobromide	MDM-2/p53 Ferroptosis	Cancer
Pifithrin-β hydrobromide (PFT β hydrobromide) is a potent p53 inhibitor with an IC₅₀ of 23 μM.

HY-N0550

β-Pinene (-)-β-Pinene	Bacterial	Infection
β-Pinene ((-)-β-Pinene), a major component of turpentine, inhibit infectious bronchitis virus (IBV) with an IC₅₀ of 1.32 mM. β-Pinene presents antimicrobial activity.

HY-125586

β-Amanitin	DNA/RNA Synthesis ADC Cytotoxin	Cancer
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).

HY-N2337

11beta-Hydroxyprogesterone 11β-Hydroxyprogesterone	Endogenous Metabolite	Cardiovascular Disease
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED₅₀ of 10 nM.

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-B1837A

β-Cyfluthrin beta-Cyfluthrin	Calcium Channel	Infection
β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca²⁺ ATPase involved in calcium transport.

HY-107324

β-Elemene (-)-β-Elemene; Levo-β-elemene	Apoptosis	Cancer
β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.

HY-135386

5β-Dutasteride	Drug Metabolite	Inflammation/Immunology
5β-Dutasteride is the S configuration of Dutasteride. 5β-Dutasteride is a potent inhibitor of both 5 alpha-reductase isozymes.

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-Y1750

β-Aminopropionitrile	Monoamine Oxidase	Cancer
β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes.

HY-N5112A

β,β-Dimethylacrylalkannin
Others Others

β,β-Dimethylacrylalkannin is a napthoquinone isolated from Arnebia nobilis Reichb.f, increases collagen and involucrin content in skin cells.
HY-P1286

PKC β pseudosubstrate
PKC Neurological Disease

PKC β pseudosubstrate is a selective cell-permeable inhibitor of PKC.

β,β-Dimethylacrylalkannin	Others	Others
β,β-Dimethylacrylalkannin is a napthoquinone isolated from Arnebia nobilis Reichb.f, increases collagen and involucrin content in skin cells.

PKC β pseudosubstrate	PKC	Neurological Disease
PKC β pseudosubstrate is a selective cell-permeable inhibitor of *PKC*.

HY-N2454

β-Elemonic acid	Apoptosis Reactive Oxygen Species COX	Cancer Inflammation/Immunology
β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects.

HY-133680

β-Tocopherol	Tyrosinase	Metabolic Disease
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.

HY-N2513

β-Boswellic acid	Lipoxygenase DNA/RNA Synthesis	Cancer
β-Boswellic acid is isolated from the gum resin of Boswellia serrate. β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.

HY-126144

GSK-3β inhibitor 1	GSK-3	Metabolic Disease
GSK-3β inhibitor 1 (compound 3a) is a glycogen synthase kinase 3β (GSK-3β) inhibitor and demonstrates high antidiabetic efficacy, with an IC₅₀ of 4.9 nM.

HY-135670A

β-glycosidase-IN-1
Others Metabolic Disease

β-glycosidase-IN-1 (Compound 33) is a piperidine derivative and a β-glycosidase inhibitor. β-glycosidase-IN-1 has hypoglycemic activity.

*β-glycosidase-IN-1*	Others	Metabolic Disease
β-glycosidase-IN-1 (Compound 33) is a piperidine derivative and a *β-glycosidase* inhibitor. β-glycosidase-IN-1 has hypoglycemic activity.

HY-124957

β-NETA	AChE Apoptosis	Cancer
β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC₅₀=76 μM) and cholinesterase (ChE; IC₅₀=40 µM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; *IC₅₀=1 mM).*

HY-N1940

β-Anhydroicaritin	Interleukin Related TNF Receptor MMP	Inflammation/Immunology
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca²⁺, and markedly decreases iNOS protein expression.

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
HY-N7606

(Rac)-β-Chamigrenic acid
Others Others

(Rac)-β-Chamigrenic acid is a racemate of β-Chamigrenic acid. β-Chamigrenic acid is an sesquiterpenoid isolated from S.chinensis

Ehp inhibitor 2	Ephrin Receptor	Cancer
Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

(Rac)-β-Chamigrenic acid	Others	Others
(Rac)-β-Chamigrenic acid is a racemate of β-Chamigrenic acid. β-Chamigrenic acid is an sesquiterpenoid isolated from S.chinensis

HY-N2920

β-Amyrenonol 11-Oxo-β-amyrin	Cytochrome P450	Cancer Inflammation/Immunology
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.

HY-107373

β-Chloro-L-alanine L-β-Chloroalanine	Bacterial	Infection
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.

HY-136234

9-cis-β-Carotene	Others	Others
9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus.

HY-P1084

β-Pompilidotoxin β-PMTX	Sodium Channel	Neurological Disease
β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-108059

β-Cryptoxanthin (3R)-β-Cryptoxanthin	Endogenous Metabolite	Neurological Disease
β-Cryptoxanthin ((3R)-β-Cryptoxanthin), isolated from Satsuma mandarin orange, is an oxygenated carotenoid and a potent antioxidant. β-Cryptoxanthin has an anti-stress effect.

HY-P1286A

PKC β pseudosubstrate TFA
PKC Neurological Disease

PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of PKC.

PKC β pseudosubstrate TFA	PKC	Neurological Disease
PKC β pseudosubstrate TFA is a selective cell-permeable inhibitor of *PKC*.

HY-114464

*11-Beta-hydroxyandrostenedione* 4-Androsten-11β-ol-3,17-dione	Endogenous Metabolite	Endocrinology
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.

HY-U00272

Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- Androst-4-ene-3β,17β-diol, dipropionate	Androgen Receptor	Metabolic Disease Neurological Disease
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- is the dipropanoate of 4-Androstenediol, a metabolite of testosterone.

HY-N2922

β-Amyrin	Others	Neurological Disease
β-Amyrin, an ingredient of the surface wax of tomato fruit and dandelion coffee, blocks amyloid β (Aβ)-induced long-term potentiation (LTP) impairment. β-amyrin is a promising candidate of treatment for AD.

HY-N5112B

β,β-Dimethylacrylshikonin	Others	Cancer
β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity.

HY-136464

β-catenin-IN-2	β-catenin	Cancer
β-catenin-IN-2 is a potent *β-catenin* inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.

HY-N0941

beta-Mangostin β-Mangostin	Others	Others
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).

HY-N2056

*11-Keto-beta-boswellic acid* 11-Keto-β-boswellic acid	Lipoxygenase Leukotriene Receptor NF-κB	Cancer
11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.

HY-12452

DPN Diarylpropionitrile	Estrogen Receptor/ERR	Neurological Disease
DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC₅₀ of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.

HY-W010231

β-Cyclocitral	Others	Others
β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent.

HY-113351

11β-Hydroxyandrosterone
Endogenous Metabolite Endocrinology

11β-Hydroxyandrosterone is a 11-oxygenated androgen metabolite of 11β-hydroxyandrostenedione.

11β-Hydroxyandrosterone	Endogenous Metabolite	Endocrinology
11β-Hydroxyandrosterone is a 11-oxygenated androgen metabolite of 11β-hydroxyandrostenedione.

HY-114392

Gly-β-MCA	FXR Autophagy	Metabolic Disease
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.

HY-F0004

β-Nicotinamide mononucleotide β-NM; NMN	Endogenous Metabolite	Cancer Neurological Disease
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD(+) intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.

HY-135594

4'-Raloxifene-β-D-glucopyranoside	Estrogen Receptor/ERR	Metabolic Disease
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.

HY-135595

6-Raloxifene-β-D-glucopyranoside	Estrogen Receptor/ERR Drug Metabolite	Metabolic Disease
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.

HY-16673

PSN632408	GPR119	Metabolic Disease
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC₅₀=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.

HY-108693

β-Tocotrienol
Others Inflammation/Immunology

β-Tocotrienol is one form of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol.

β-Tocotrienol	Others	Inflammation/Immunology
β-Tocotrienol is one form of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol.

HY-P1084A

β-Pompilidotoxin TFA β-PMTX TFA	Sodium Channel	Neurological Disease
β-Pompilidotoxin TFA (β-PMTX TFA), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

HY-P1522

β-Amyloid (29-40)
Amyloid beta-protein(29-40)
Amyloid-β Neurological Disease

β-Amyloid (29-40) is a fragment of Amyloid-β peptide.

β-Amyloid (29-40) Amyloid beta-protein(29-40)	Amyloid-β	Neurological Disease
β-Amyloid (29-40) is a fragment of Amyloid-β peptide.

HY-P1051

β-amyloid (12-28) Amyloid β-Protein (12-28)	Amyloid-β	Neurological Disease
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.

HY-N7682

β-Tomatine
Others Others

β-Tomatine is a breakdown product of α-tomatine and a less fungitoxic compound. β-Tomatine can suppress plant defense responses.
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-P1521

β-Amyloid 15-21
beta-Amyloid (15-21)
Amyloid-β Neurological Disease

β-amyloid (15-21) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.

HY-B0141

Estradiol β-Estradiol; E2; 17β-Estradiol; 17β-Oestradiol	Estrogen Receptor/ERR Endogenous Metabolite	Endocrinology Cancer
Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway.

HY-P0128

β-Amyloid (25-35) Amyloid beta-peptide (25-35); Aβ25-35; β-Amyloid peptide (25-35)	Amyloid-β	Neurological Disease
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.

HY-N6018

Beta-Eudesmol	TRP Channel	Metabolic Disease
Beta-Eudesmol is a natural oxygenated sesquiterpene, activates *hTRPA1, with an EC₅₀* of 32.5 μM. Beta-Eudesmol increases appetite through TRPA1.

HY-N6741

β-Zearalenol	Others	Infection Endocrinology
β-Zearalenol is a non-steroidal estrogenic mycotoxin synthesized by Fusarium species. β-Zearalenol potentially influences transcription and effects gene expression on translational level.

HY-136552

β-Bisabolene	Others	Cancer
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer.

HY-P1046

β-Amyloid 1-15 Amyloid β-Protein (1-15)	Amyloid-β	Neurological Disease
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.

HY-P0179

β-Casomorphin, bovine β-Casomorphin-7 (bovine); Bovine β-casomorphin-7	Opioid Receptor	Metabolic Disease Neurological Disease
β-Casomorphin, bovine (β-Casomorphin-7 (bovine) ) is a opioid peptide with an IC₅₀ of 14 μM in an Opioid receptors binding assay.

HY-50900

gamma-Secretase Modulators Amyloid-β production inhibitor; γ-Secretase Modulators	Amyloid-β	Neurological Disease
gamma-Secretase Modulators (Amyloid-β production inhibitor) is a Amyloid-β production inhibitor.

HY-N1484

7beta-Hydroxylathyrol
Others Others

7beta-Hydroxylathyrol is a natural product.
HY-P1772

β-Amyloid (1-17)
Amyloid-β Neurological Disease

β-Amyloid (1-17) is a peptide of β-Amyloid, stabilizes the fibres and plays a role in Aβ fibre formation.

HY-N5053

*Periplogenin 3-[O-β-glucopyranosyl-(1→4)-β-sarmentopyranoside]*	Others	Others
Periplogenin 3-[O-β-glucopyranosyl-(1→4)-β-sarmentopyranoside] is a cardenolide isolated from the root barks of Periploca sepium.

HY-113418

Beta-Cortol
Endogenous Metabolite Endocrinology

Beta-Cortol is an androgen metabolite present in adults.

HY-107201

β-Cyclodextrin	Influenza Virus	Infection
β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus *H1N1* activities.

HY-P1481A

β-Casomorphin, human TFA Human β-casomorphin 7 TFA	Opioid Receptor	Metabolic Disease Neurological Disease
β-Casomorphin, human TFA (Human β-casomorphin 7 TFA) is an opioid peptide, acts as an agonist of opioid receptor.

HY-P1468

β-Amyloid (1-28) Amyloid β-Protein (1-28)	Amyloid-β	Neurological Disease
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.

HY-P1466

β-Amyloid 1-16 Amyloid β-Protein (1-16)	Amyloid-β	Neurological Disease
β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.

HY-N4201

β-Hydroxyisovalerylshikonin	EGFR Src	Cancer
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC₅₀s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.

HY-125849

Chrysin 7-O-beta-gentiobioside
Chrysin 7-O-β-gentiobioside
Others Cancer

Chrysin 7-O-beta-gentiobioside (Chrysin 7-O-β-gentiobioside) is the glycosylation product of Chrysin.

HY-P1474

β-Amyloid (22-35) Amyloid β-Protein (22-35)	Amyloid-β	Neurological Disease
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).

HY-N1968

*Quercetin-3-O-β-D-glucose-7-O-β-D-gentiobiosiden* Quercetin-3-O-beta-D-glucose-7-O-beta-D-gentiobioside	Others	Others
Quercetin-3-O-β-D-glucose-7-O-β-D-gentiobiosiden is a flavonoid from Quercetin.

HY-128976

10β,17β-dihydroxyestra-1,4-dien-3-one DHED	Estrogen Receptor/ERR	Metabolic Disease
10β,17β-dihydroxyestra-1,4-dien-3-one (DHED) is a brain-targeting bioprecursor prodrug of the main human estrogen, 17β-estradiol, alleviates hot flushes in rat models of thermoregulatory dysfunction of the brain.

HY-N2274

23-Hydroxylongispinogenin 12-Oleanene-3β,16β,23,28-tetrol; 3β,16β-12-Oleanene-3, 16,23,28-tetrol	Others	Cancer
23-Hydroxylongispinogenin (12-Oleanene-3β,16β,23,28-tetrol) is extracted from Lysimachia heterogenea Klatt. Lysimachia heterogenea Klatt is a perennial herb, which is used as a folk medicine in subduing swelling and detoxicating in China. The effective fraction LH-1 of L. heterogene has antitumor activity.

HY-12780S

*6-beta-Naloxol D5 hydrochloride* 6β-Naloxol D5 hydrochloride	Opioid Receptor	Neurological Disease
6-beta-Naloxol D5 hydrochloride is the deuterium labeled 6-beta-Naloxol, which is an opioid antagonist closely related to naloxone.

HY-22306

β-D-Glucose pentaacetate
Penta-O-acetyl-β-D-glucopyranose
Others Others

β-D-Glucose Pentaacetate (Penta-O-acetyl-β-D-glucopyranose) is used in biochemical reaction.
HY-P1880

β-Amyloid (12-20)
Amyloid-β Neurological Disease

β-Amyloid (12-20) is a peptide fragment of β-Amyloid.
HY-P1879

β-Amyloid (18-28)
Amyloid-β Neurological Disease

β-Amyloid (18-28) is a peptide fragment of β-Amyloid.

HY-113478

3β-Ursodeoxycholic acid Isoursodeoxycholic acid	Others	Metabolic Disease
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA.

HY-N6652

1-beta-D-Arabinofuranosyluracil Uracil 1-β-D-arabinofuranoside	Others	Cancer Inflammation/Immunology Cardiovascular Disease
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells.

HY-136344

Simvastatin Acyl-β-D-glucuronide	Drug Metabolite	Others
Simvastatin Acyl-β-D-glucuronide is a metabolite of Simvastatin. Simvastatin is a competitive inhibitor of HMG-CoA reductase with a K_i of 0.2 nM.

HY-P1051A

β-amyloid (12-28) (TFA) Amyloid β-Protein (12-28) (TFA)	Amyloid-β	Neurological Disease
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.

HY-N1501

Beta-asarone	Others	Inflammation/Immunology Neurological Disease
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.

HY-N6740

Beta-Zearalanol	Apoptosis	Metabolic Disease
Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.

HY-N7683

Prunetin 5-O-β-D-glucopyranoside	Glucosidase	Metabolic Disease
Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC₅₀ of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.

HY-P1787

β-Amyloid (4-10)	Amyloid-β	Neurological Disease
β-Amyloid (4-10) is an epitope for the polyclonal anti-Aβ(1-42) antibody, reduces amyloid deposition in a transgenic Alzheimer disease mouse model.

HY-N2182

Episyringaresinol 4'-O-β-D-glncopyranoside	Others	Inflammation/Immunology
Episyringaresinol 4'-O-β-D-glncopyranoside (compound 22), isolated from Alhagi sparsifolia Shap, is a natural potential neuroinflammatory inhibitor.

HY-P1895

β-Amyloid (33-40)
Amyloid-β Neurological Disease

β-Amyloid (33-40) is a peptide consisting of amino acid of 33 to 40 of beta amyloid protein.
HY-P1903

β-Amyloid (35-42)
Amyloid-β Neurological Disease

β-Amyloid (35-42) is a peptide consisting of amino acid of 35 to 42 of beta amyloid protein.

HY-125773

β-cyano-L-Alanine beta-cyano-l-alanine	Others	Neurological Disease
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.

HY-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.
HY-P1510

β-amyloid 1-11
Amyloid-β Neurological Disease

β-amyloid (1-11) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.
HY-P1517

β-Amyloid (31-35)
Amyloid-β Neurological Disease

β-Amyloid (31-35) is the shortest sequence of native Amyloid-β peptide that retains neurotoxic activity.
HY-N0520

Calycosin-7-O-β-D-glucoside
Reactive Oxygen Species Others

Calycosin-7-O-β-D-glucoside, a melanin biosynthesis inhibitor, is isolated from the methanol extract of astragalus.

HY-N0411

β-Carotene Provitamin A; beta-Carotene	Endogenous Metabolite	Metabolic Disease
β-Carotene (Provitamin A) is an organic compound and classified as a terpenoid. It is a precursor (inactive form) of vitamin A.

HY-P1850

β-Amyloid (1-20)
Amyloid-β Neurological Disease

β-Amyloid (1-20) consists of amino acids 1 to 20 of beta amyloid protein.

HY-B1449

Uridine β-Uridine	Endogenous Metabolite	Others
Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond.

HY-N0087

Gambogic Acid beta-Guttiferrin	Bcl-2 Family Autophagy	Cancer
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, *Bfl-1* and *Mcl-1* with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

HY-N2188

Beta-Acetoxyisovalerylshikonin
Others Inflammation/Immunology

Beta-Acetoxyisovalerylshikonin is a naphthoquinone derivative isolated from Arnebia euchroma.
HY-131108

β-Aspartylaspartic acid
Others Others

β-Aspartylaspartic acid is a natural compound found in Asparagus (Asparagus officinalis) Shoots.

HY-P1362

β-Amyloid (42-1), human Amyloid β Peptide (42-1)(human)	Amyloid-β	Neurological Disease
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). Amyloid β Peptide (1-42) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.

HY-N1415

β-Caryophyllene (-)-(E)-Caryophyllene; (−)-β-caryophyllene; (−)-trans-Caryophyllene	Cannabinoid Receptor Endogenous Metabolite	Cancer Infection Neurological Disease
β-Caryophyllene is a CB2 receptor agonist.

HY-N7635

Oleanolic acid 28-O-β-D-glucopyranoside β-D-Glucopyranosyl oleanolate	Others	Others
Oleanolic acid 28-O-β-D-glucopyranoside (β-D-Glucopyranosyl oleanolate) is a saponin isolated from the roots of Achyranthes bidentata Blume.

HY-P0179A

β-Casomorphin, bovine TFA β-Casomorphin-7 (bovine) (TFA); Bovine β-casomorphin-7 TFA	Opioid Receptor	Metabolic Disease Neurological Disease
β-Casomorphin, bovine TFA (β-Casomorphin-7 (bovine) TFA) is a opioid peptide with an IC₅₀ of 14 μM in an Opioid receptors binding assay.

HY-P1474A

β-Amyloid (22-35) (TFA) Amyloid β-Protein (22-35) (TFA)	Amyloid-β	Neurological Disease
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).

HY-N7489

β-Hederin	Parasite	Infection Inflammation/Immunology
β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC₅₀ values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively.

HY-N4034

Hopane-3β,22-diol
Others Others

Hopane-3β,22-diol (compound 74) is a hopane isolated from A. mariesii.

HY-N0181A

Lumisterol 9β,10α-Ergosterol	Endogenous Metabolite	Metabolic Disease
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.

HY-N0338

*(-)-Syringaresnol-4-O-β-D-apiofuranosyl-(1→2)-β-D-glucopyranoside*	Others	Others
(-)-Syringaresnol-4-O-β-D-apiofuranosyl-(1→2)-β-D-glucopyranoside is isolated from the bark of Albizzia myriophylla.

HY-N6824

Hydroxy-β-sanshool
Others Others

Hydroxy-β-sanshool is an alkylamide exists in Zanthoxylum bungeanum oil and Zanthoxylum schinifolium oil.

HY-N7401

Entadamide-A-β-D-glucopyranoside	Others	Others
Entadamide-A-β-D-glucopyranoside is one of the major components in the seeds of Entada phaseoloides. Entadamide-A-β-D-glucopyranoside has anti-complement activitie.

HY-100740C

*(1α,1'S,4β)-Lanabecestat* (1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814	Beta-secretase	Neurological Disease
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a **Beta site APP Cleaving Enzymel (BACE1)** inhibitor extracted from patent WO2012087237A1, compound 20a, has IC₅₀s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPP_p release assay), respectively.

HY-P1854

β-Amyloid (1-9)	Amyloid-β	Neurological Disease
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism ^[1].

HY-N0180

18β-Glycyrrhetinic acid	Endogenous Metabolite	Cancer Inflammation/Immunology
18β-Glycyrrhetinic acid is the major bioactive component of Glycyrrhizae Radix and possesses anti-ulcerative, anti-inflammatory and antiproliferative properties.

HY-P1502

β-Endorphin, human	Opioid Receptor	Neurological Disease
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.

HY-141379

N-Bromoacetyl-β-alanine	PROTAC Linker ADC Linker	Cancer
N-Bromoacetyl-β-alanine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. N-Bromoacetyl-β-alanine is also a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-P1053

Amyloid β-Protein 10-20
Amyloid-β Neurological Disease

Amyloid β-Protein (10-20) is a fragment of Amyloid-β peptide, maybe used in the research of neurological disease.

HY-136537A

N-β-alanyldopamine hydrochloride NBAD hydrochloride	Endogenous Metabolite	Neurological Disease
N-β-alanyldopamine hydrochloride (NBAD hydrochloride) is the major dopamine derivative in haemolymph.

HY-N6851

Glycyrrhetic acid 3-O-β-D-glucuronide	Others	Inflammation/Immunology
Glycyrrhetic acid 3-O-β-D-glucuronide, isolated from glycyrrhiza, is an important derivative of glycyrrhizin (GL) with an anti -allergic activity. Glycyrrhetic acid 3-O-β-D-glucuronide (GAMG) shows that β‐glucuronidases (β‐GUS) are key GAMG-producing enzymes, displaying a high potential to convert GL directly into GAMG.Glycyrrhetic acid 3-O-β-D-glucuronide is valuable as a sweetener.

HY-N2168

Pinoresinol 4-O-β-D-glucopyranoside (+)-Pinoresinol 4-O-β-D-glucopyranoside	Others	Cardiovascular Disease
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.

HY-N0171B

Beta-Sitosterol (purity>75%) β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)	Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-P2294

pm26TGF-β1 peptide	TGF-β Receptor	Inflammation/Immunology
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.

HY-107670

Dihydro-β-erythroidine hydrobromide DHβE hydrobromide	nAChR	Neurological Disease
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC₅₀s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.

HY-13555

β-Lapachone ARQ-501; NSC-26326	Topoisomerase Autophagy Apoptosis	Cancer
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

HY-N0171

Beta-Sitosterol (purity>80%) β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)	Endogenous Metabolite Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-130269

β-Naphthoflavone-CH2-OH β-NF-CH2-OH	Ligand for E3 Ligase	Cancer
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins ^[1].

HY-128737

Methyl β-D-Galactopyranoside
Endogenous Metabolite Metabolic Disease

Methyl β-D-Galactopyranoside is an endogenous metabolite.

HY-N3517

Oxyresveratrol 3'-O-β-D-glucopyranoside	Tyrosinase	Metabolic Disease
Oxyresveratrol 3'-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC₅₀ of 1.64 μM.

HY-N3516

Oxyresveratrol 2-O-β-D-glucopyranoside	Tyrosinase	Metabolic Disease
Oxyresveratrol 2-O-β-D-glucopyranoside is a phenolic compound isolated from Morus nigra root and is an effective tyrosinase inhibitor with an IC₅₀ of 29.75 μM.

HY-W015084

β-Ionone
Apoptosis Cancer

β-Ionone, isolated from plant oils, is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
HY-116284

Methyl β-D-glucopyranoside
Methyl β-D-glucoside
Others Others

Methyl β-D-glucopyranoside is used to synthesize natural glycophenolics via enzymatic caffeoylation.

HY-112044

*β-catenin/CBP-IN-1*	Wnt β-catenin Epigenetic Reader Domain	Cancer Inflammation/Immunology
β-catenin/CBP-IN-1 is a potent and selective *CBP/β-catenin* antagonist, extracted from the patent WO2014092154A1. β-catenin/CBP-IN-1 has the potential for the study of liver fibrosis induced by hepatitis virus.

HY-P1567

β-Amyloid (10-35), amide	Amyloid-β	Neurological Disease
β-Amyloid (10-35), amide is composed of 26 aa (10-35 residues of the Aβ peptide) and is the primary component of the amyloid plaques of Alzheimer’s disease.

HY-N2075

3-Acetyl-beta-boswellic acid
Others Inflammation/Immunology

3-Acetyl-beta-boswellic acid is a boswellic acid isolated from Boswellia serrata gum resin.

HY-W012875

3-Nitropropanoic acid β-Nitropropionic acid; Bovinocidin	Bacterial Apoptosis	Infection Metabolic Disease
3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM.

HY-N4099

*Luteolin-3-O-beta-D-glucuronide*	Others	Infection Inflammation/Immunology
Luteolin-3-O-beta-D-glucuronide is a luteolin glucosiduronic acid consisting of luteolin having a beta-D-glucosiduronic acid residue attached at the 3'-position.

HY-N2100

*6'-O-beta-D-Glucosylgentiopicroside*	Others	Metabolic Disease
6'-O-beta-D-Glucosylgentiopicroside is a secoiridoid isolated from the roots of G. straminea. 6'-O-beta-D-Glucosylgentiopicroside strongly suppresses N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation.

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-N0406

*2"-O-beta-L-galactopyranosylorientin*	Others	Metabolic Disease
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).

HY-101953

β-Apo-13-carotenone
D'Orenone
Others Others

β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
HY-P2283

Amyloid β-Peptide (1-37) (human)
Amyloid-β

Amyloid β-Peptide (1-37) (human) is an amyloid β-protein fragment cleaved from amyloid precursor protein (APP).
HY-B0708

β-Estradiol 17-acetate
1,3,5(10)-Estratriene-3,17β-diol 17-acetate
Estrogen Receptor/ERR Endocrinology

β-Estradiol 17-acetate is a metabolite of estradiol.

HY-N5111

Aloe-emodin-3-(hydroxymethyl)-O-β-D-glucopyranoside Aloe-emodin 3-O-β-D-glucoside	Others	Others
Aloe-emodin-3-(hydroxymethyl)-O-β-D-glucopyranoside (Aloe-emodin 3-O-β-D-glucoside) is a natural antraquinone.

HY-129993

*Gemfibrozil 1-O-β-glucuronide*	PPAR Cytochrome P450 Drug Metabolite	Metabolic Disease Cardiovascular Disease
Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC₅₀ of 4.07 μM.

HY-N2212

Arctigenin 4'-O-β-gentiobioside
Others Inflammation/Immunology Metabolic Disease

Arctigenin 4'-O-β-gentiobioside is a natural compound isolated from Arctigenin.

HY-P1548

β-CGRP, human Human β-CGRP; CGRP-II (Human)	CGRP Receptor	Inflammation/Immunology Cardiovascular Disease
β-CGRP, human (Human β-CGRP) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC₅₀s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.

HY-P2294A

pm26TGF-β1 peptide TFA	TGF-β Receptor	Inflammation/Immunology
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.

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-N6904

Crocetin β-Crocetin	Others	Inflammation/Immunology Neurological Disease
Crocetin (β-Crocetin), isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity.

HY-N2394

*Emodin-1-O-β-D-glucopyranoside*	Others	Inflammation/Immunology
Emodin-1-O-β-D-glucopyranoside, isolated from medicinal plant Polygonum cuspidatum Sieb. & Zucc, is a potent and noncompetitive bacterial neuraminidase (BNA) inhibitor with an IC₅₀ of 0.85 μM.

HY-N0192

Arbutin β-Arbutin	Tyrosinase	Cancer
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with K_i^app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.

HY-P2290

Beta-defensin 1, pig	Bacterial	Infection Inflammation/Immunology
Beta-defensin 1, pig is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig is active against bacteria such as *Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis* and Candida albicans.

HY-N7598

*Chrysophanol-1-O-β-gentiobioside*	Monoamine Oxidase	Neurological Disease
Chrysophanol-1-O-β-gentiobioside, an anthraquinone glycoside isolated from Cassia obtusifolia seeds. Chrysophanol-1-O-β-gentiobioside shows selective inhibition of hMAO-A isozyme activity (IC₅₀=96.15 μM).

HY-100084

Methyl-3β-hydroxycholenate
ROR Inflammation/Immunology

Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.

HY-N3523

*3-O-Beta-D-Glucopyranosylplatycodigenin*	Others	Cancer
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC₅₀ of 13.36 μM.

HY-P0265

β-Amyloid (1-40)
Amyloid-β Neurological Disease

β-Amyloid (1-40) is a primary protein in plaques found in the brains of patients with Alzheimer's disease.

HY-113949A

Methyl 2,3-O-Isopropylidene-β-L-ribofuranoside	Others	Others
Methyl 2,3-O-Isopropylidene-β-L-ribofuranoside is an enantiomer of Methyl 2,3-O-Isopropylidene-β-D-ribofuranoside. Methyl 2,3-O-Isopropylidene-β-L-ribofuranoside is a derivative of L-ribose.

HY-P1378

*Amyloid β-Peptide(1-43)(human)*	Amyloid-β
Amyloid β-Peptide(1-43) human, the Human β-amyloid peptide, is minor component of neuritic plaques found in brains of patients with Alzheimer's disease.

HY-N6677

β-Apo-8'-carotenal Apocarotenal	Cytochrome P450	Cancer
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of *CYPlA1* and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.

HY-100260

beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
HIV Infection

beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.

HY-P1548B

β-CGRP, human acetate Human β-CGRP acetate; CGRP-II (Human) (acetate)	CGRP Receptor	Inflammation/Immunology Cardiovascular Disease
β-CGRP, human acetate (Human β-CGRP acetate) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC₅₀s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.

HY-N2142

*3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B*	Others	Cancer
3-O-beta-Allopyranosyl-(1->4)-beta-oleandropyranosyl-11-O-isobutyryl-12-O-acetyltenacigenin B is a chemical constituent of the plant Poria cocos ^[1].

HY-P1363

β-Amyloid (1-42), human TFA Amyloid β-Peptide (1-42) (human) TFA	Amyloid-β	Neurological Disease
β-Amyloid (1-42), human TFA (Amyloid β-Peptide (1-42) (human) TFA) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.

HY-N7176

Kaempferol 3-O-β-D-glucuronide Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide	Interleukin Related	Inflammation/Immunology
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.

HY-N5091

Physcion 8-O-β-D-glucopyranoside	Others	Cancer Inflammation/Immunology
Physcion 8-O-β-D-glucopyranosideis an anthraquinone compound isolated from Rumex japonicus Houtt. Physcion 8-O-β-D-glucopyranoside exerts anti-inflammatory and anti-cancer properties, can be for common malignancy cancer research.

HY-N0171A

Beta-Sitosterol (purity>98%) β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)	Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Beta-Sitosterol (purity>98%) is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.

HY-N7422

Kauran-16,17-diol ent-Kauran-16β,17-diol	Apoptosis	Cancer Inflammation/Immunology
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC₅₀ of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.

HY-N6986

*Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside* Liquiritigenin-7-apiosylglucoside	Others	Cancer
Liquiritigenin-7-O-β-D-glucopyranosyl-(1→2)-β-D-apiofuranoside (Liquiritigenin-7-apiosylglucoside) is a flavonoid isolated from the roots of Glycyrrhiza, has weaker cytotoxicity against several tumor cells and normal cells.

HY-P1866

β-Endorphin, equine	Opioid Receptor	Neurological Disease
β-Endorphin, equine is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.

HY-W015546

β-N-methylamino-L-alanine hydrochloride BMAA hydrochloride	Others	Neurological Disease
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.

HY-N2468

Xylobiose
1,4-β-D-Xylobiose; 1,4-D-Xylobiose
Others Others

Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is a disaccharide of xylose monomers with a β-1, 4 bond between monomers.

HY-P2290A

Beta-defensin 1, pig TFA	Bacterial	Infection Inflammation/Immunology
Beta-defensin 1, pig TFA is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig TFA is active against bacteria such as *Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis* and Candida albicans.

HY-43470

3α,12β-Dihydroxycholanoic acid
Endogenous Metabolite Metabolic Disease

3α,12β-Dihydroxycholanoic acid is a bile acid that can be isolated from urine specimens of healthy humans.

HY-11012

TDZD-8 GSK-3β Inhibitor I; NP 01139	GSK-3	Cancer
TDZD-8 is an inhibitor of *GSK-3β, with an IC₅₀* of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC₅₀s of >100 μM.

HY-P1378A

*Amyloid β-Peptide(1-43)(human) TFA*	Amyloid-β
Amyloid β-Peptide(1-43) human TFA, the Human β-amyloid peptide, is minor component of neuritic plaques found in brains of patients with Alzheimer's disease.

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-N6938

Pseudolaric acid B β-D-glucoside
Others Infection

Pseudolaric acid B β-D-glucoside is a diterpenoid isolated from Pseudolarix kaempferi.

HY-N6885

Puerarin-4'-O-β-D-glucopyranoside	Others	Cancer
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells.

HY-N2451

Aloe-emodin-8-O-β-D-glucopyranoside	Phosphatase	Endocrinology Metabolic Disease
Aloe-emodin-8-O-β-D-glucopyranoside, a compound isolated from Saussrurea lappa, is a moderate inhibitor of human protein tyrosine phosphatase 1B (hPTP1B) with an IC₅₀ of 26.6 μM.

HY-N6911

Licorice-saponin H2
(18β,20α)-Glycyrrhizic acid
Others Metabolic Disease

Licorice-saponin H2 ((18β,20α)-Glycyrrhizic acid) is a saponin from Glycyrrhiza uralensis Fischer.

HY-50730

Asparagusic acid	Parasite	Infection
Asparagusic acid a sulfur-containing flavor component produced by Asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.

HY-N6879

DiosMetin 7-O-β-D-Glucuronide
Others Metabolic Disease

DiosMetin 7-O-β-D-Glucuronide is an antioxidant constituent in the fruits of Luffa cylindrical.
HY-N6260

4-O-beta-Glucopyranosyl-cis-coumaric acid
Others Others

4-O-beta-Glucopyranosyl-cis-coumaric acid is a natural compound isolated formn Nelumbo nucifera Gaertn.

HY-101953S

β-Apo-13-carotenone D3 D'Orenone D3	Others	Cancer
β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.

HY-P2313

Human β-defensin-2 HβD-2	Antibiotic Bacterial	Infection
Human β-defensin-2 (HβD-2) is a small cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by a number of epithelial cells.Human β-defensin-2 has antimicrobial activity against gram-negative bacteria and Candida, but not gram-positive Staphylococcus aureus. Human β-defensin-2 can be used for the study of colitis.

HY-113320

Etiocholanolone 5β-Androsterone	GABA Receptor	Neurological Disease
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABA_A receptor than its enantiomer form.

HY-P1548A

β-CGRP, human TFA Human β-CGRP TFA; CGRP-II (Human) (TFA)	CGRP Receptor	Inflammation/Immunology Cardiovascular Disease
β-CGRP, human TFA (Human β-CGRP TFA) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC₅₀s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.

HY-N6006

1,3,6-Tri-O-galloyl-beta-D-glucose 1,3,6-Tri-O-galloyl-β-D-glucose	Others	Others
1,3,6-Tri-O-galloyl-beta-D-glucose (1,3,6-Tri-O-galloyl-β-D-glucose) is a phenolic compound in Black Walnut Kernels.

HY-135103

Tauro-β-muricholic acid sodium T-βMCA sodium	FXR	Cancer
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC₅₀ of 40 μM.

HY-W010452

3-Hydroxybutyric acid sodium β-Hydroxybutyric acid sodium	Endogenous Metabolite	Metabolic Disease
3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids.

HY-113378

3-Hydroxybutyric acid β-Hydroxybutyric acid	Endogenous Metabolite	Metabolic Disease
3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids.

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-112023

Lumisterol 3 (>90%) 9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A	Endogenous Metabolite	Others
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.

HY-P0265A

β-Amyloid (1-40) (TFA)
Amyloid-β Neurological Disease

β-Amyloid (1-40) TFA is a primary protein in plaques found in the brains of patients with Alzheimer's disease.

HY-N4088

Pseudolaric acid A-O-β-D-glucopyranoside	Others	Infection Endocrinology
Pseudolaric acid A-O-β-D-glucopyranoside, isolated from Cortex Pseudolaricis, demonstrates antifungal and antifertility activities.

HY-P1868

α2β1 Integrin Ligand Peptide	Integrin	Infection
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

HY-B0406

Bethanechol Carbamyl-β-methylcholine	mAChR	Neurological Disease
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.

HY-B0406A

Bethanechol chloride Carbamyl-β-methylcholine chloride	mAChR	Neurological Disease
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.

HY-P1388

β-Amyloid (1-42), rat Amyloid β-peptide (1-42) (rat)	Amyloid-β	Neurological Disease
β-Amyloid (1-42), rat is a 42-aa peptide, shows cytotoxic effect on acute hippocampal slices, and used in the research of Alzheimer's disease.

HY-125801

3-Oxo-5β-cholanoic acid Dehydrolithocholic acid; 3-oxoLCA	ROR	Inflammation/Immunology
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (K_d=1.13 μM).

HY-N2107

Physion 8-O-β-D-glucoside	Others	Neurological Disease Cardiovascular Disease
Physion 8-O-β-D-glucoside, a bioactive component of Fallopia multiflora, can be used for the research of dizziness.

HY-136329

β-D-glucuronide-pNP-carbonate
ADC Linker Cancer

β-D-glucuronide-pNP-carbonate is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-128974

N-Dodecyl-β-D-maltoside Lauryl Maltoside	Others	Others
N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.

HY-N0230

β-Alanine 2-Carboxyethylamine; 3-Aminopropanoic acid	Endogenous Metabolite	Metabolic Disease
β-Alanine is a non-essential amino acid that is shown to be metabolized into carnosine, which functions as an intracellular buffer.

HY-111642

3'-Azido-3'-deoxy-beta-L-uridine
Nucleoside Antimetabolite/Analog Others

3'-Azido-3'-deoxy-beta-L-uridine (Compound 25) is a nucleoside derivative.
HY-141131

Propargyl-PEG2-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG2-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141132

Propargyl-PEG4-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG4-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-140012

Azido-PEG4-beta-D-glucose
PROTAC Linker Cancer

Azido-PEG4-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-P2291

Beta-defensin 103 isoform X1, pig	Bacterial	Inflammation/Immunology
Beta-defensin 103 isoform X1, pig is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens.

HY-N7715

Ferulic acid acyl-β-D-glucoside Ferulic acid glucoside	Drug Metabolite	Others
Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060). Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC₅₀s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.

HY-P1866A

β-Endorphin, equine TFA	Opioid Receptor	Neurological Disease
β-Endorphin, equine (TFA) is an endogenous opioid peptide, which binds at high affinity to both μ/δ opioid receptors. Analgesic properties.

HY-19773

*beta-lactamase-IN-1*	Bacterial	Cancer
beta-lactamase-IN-1 targets Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.

HY-A0058

Retinyl glucoside Retinyl β-D-glucoside	Others	Metabolic Disease
Retinyl-β-D-glucoside is a naturally occurring and biologically active metabolites of vitamin A, which are found in fish and mammals.

HY-B1192

Estradiol benzoate β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate	Estrogen Receptor/ERR	Endocrinology Cancer
Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.

HY-N2601

Bayogenin 3-O-β-D-glucopyranoside	Others	Inflammation/Immunology
Bayogenin 3-O-β-D-glucopyranoside, a triterpenoid saponin isolated from Polygala japonica, possesses anti-inflammatory activities.

HY-N0892

AKBA Acetyl-11-keto-β-boswellic acid	HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Endogenous Metabolite	Cancer
AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.

HY-P2312

Human β-defensin-3 HβD-3	Antibiotic Bacterial	Infection
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC₉₀ values of 6-25 μg/ml.

HY-77591A

Cysteamine β-Mercaptoethylamine; 2-Aminoethanethiol; 2-Mercaptoethylamine	Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite	Cancer Metabolic Disease
Cysteamine (β-Mercaptoethylamine) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.

HY-103687

Abiraterone metabolite 1 3β-OH-5α-Abi	Drug Metabolite	Cancer
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.

HY-10512

AR-A014418
AR 0133418; GSK 3β inhibitor VIII; AR 014418
GSK-3 Metabolic Disease Cancer

AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor with an IC₅₀ of 104 nM。

HY-N0713

Diosmetin-7-O-β-D-glucopyranoside	Others	Others
Diosmetin-7-O-β-D-glucopyranoside is a natural product isolated from the flowers of Chrysanthemum morifolium, with antioxidant activity.

HY-P2315

Human β-defensin-1 HβD-1	Antibiotic Bacterial	Infection
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.

HY-P1868A

α2β1 Integrin Ligand Peptide TFA	Integrin	Others
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.

HY-108652

α,β-Methylene ATP trisodium
Others Inflammation/Immunology

α,β-Methylene ATP trisodium, a phosphonic analog of ATP, is a P2X3 and P2X7 receptor ligand.

HY-P1504

β-Melanocyte Stimulating Hormone (MSH), human beta-MSH (1-22) (human)	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

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-P2291A

Beta-defensin 103 isoform X1, pig TFA	Bacterial	Inflammation/Immunology
Beta-defensin 103 isoform X1, pig TFA is an antimicrobial peptide found in different living organisms, involved in the first line of defense in their innate immune response against pathogens.

HY-P1388A

β-Amyloid (1-42), rat TFA Amyloid β-peptide (1-42) (rat) TFA	Amyloid-β	Neurological Disease
β-Amyloid (1-42), rat TFA is a 42-aa peptide, shows cytotoxic effect on acute hippocampal slices, and used in the research of Alzheimer's disease.

HY-N4180

*Pennogenin 3-O-beta-chacotrioside*	Autophagy	Cancer
Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.

HY-B1209

Etofylline 7-(β-Hydroxyethyl)theophylline	Others	Cardiovascular Disease
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.

HY-109564

5α-Pregnane-3β,6α-diol-20-one	Others	Cancer
5α-Pregnane-3β,6α-diol-20-one is a mitogenic metabolite of progesterone, and it can be produced in starved androgen-responsive prostate cancer cells.

HY-77591

Cysteamine hydrochloride β-Mercaptoethylamine Hydrochloride; 2-Aminoethanethiol Hydrochloride; 2-Mercaptoethylamine Hydrochloride; Thioethanolamine Hydrochloride	Autophagy Reactive Oxygen Species Apoptosis Endogenous Metabolite	Metabolic Disease Cancer
Cysteamine hydrochloride (β-Mercaptoethylamine Hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.

HY-N7604

Isorubrofusarin-6-O-β-gentiobioside Isorubrofusarin gentiobioside	Others	Others
Isorubrofusarin-6-O-β-gentiobioside (Isorubrofusarin gentiobioside) is a naphthopyrone glycoside isolated from Cassia obtusifolia Linn seeds.

HY-N0627

Kaempferol-7-O-β-D-glucopyranoside	Others	Inflammation/Immunology
Kaempferol-7-O-β-D-glucopyranoside is a flavonoid isolated from Malus pumila Mill. flowers, has antioxidative, anti-inflammatory and procoagulant activitives.

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-B0672

Estradiol valerianate β-Estradiol 17-valerate	Estrogen Receptor/ERR	Endocrinology Cancer
Estradiol valerianate (β-estradiol 17-valerate) is a synthetic estrogen widely used in combination with other steroid hormones in hormone replacement therapy drugs.

HY-B0151

Pregnenolone 3β-Hydroxy-5-pregnen-20-one	Cannabinoid Receptor Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication.

HY-113013

Hydroxypyruvic acid β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid	Endogenous Metabolite	Metabolic Disease
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.

HY-N2094

*Genipin 1-β-D-gentiobioside* Genipin 1-gentiobioside; Genipin 1-β-gentiobioside; Genipin gentiobioside	Others	Inflammation/Immunology
Genipin 1-β-D-gentiobioside (Genipin 1-gentiobioside) is one of the most abundant and bioactive iridoid glycosides in Gardenia jasminoides Ellis, which possesses hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.

HY-135588

Raloxifene 6,4'-Bis-β-D-glucuronide	Others	Metabolic Disease
Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis.

HY-136614

H-Val-βNA
L-Valine β-naphthylamide
Others Others

H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.

HY-A0083

Methacholine chloride Acetyl-β-methylcholine chloride	mAChR	Others
Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.

HY-W007648

Methyl 3-aminopropanoate hydrochloride β-Alanine methyl ester hydrochloride	Others	Others
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand.

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-P1504A

β-Melanocyte Stimulating Hormone (MSH), human TFA beta-MSH (1-22) (human) TFA	Melanocortin Receptor	Metabolic Disease Neurological Disease Endocrinology
β-Melanocyte Stimulating Hormone (MSH), human TFA, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

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-135955

Levothyroxine acyl glucuronide Thyroxine acyl-β-D-glucuronide	Endogenous Metabolite	Metabolic Disease
Levothyroxine acyl glucuronide (Thyroxine Acyl-β-D-glucuronide), an endogenous metabolite, is the acyl glucuronide formation of thyroxine (T4).

HY-111974

β-D-Glucopyranosyl abscisate ABA-GE; (S)-cis,trans-Abscisic acid glucosyl ester	Others	Endocrinology
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis.

HY-N7024

Quercetin 3-O-(6''-galloyl)-β-D-galactopyranoside
Others Metabolic Disease

Quercetin 3-O-(6''-galloyl)-β-D-galactopyranoside is from the fresh leaves of Psidium Guajava L..

HY-N2190

*Hederagenin 28-O-beta-D-glucopyranosyl ester*	Others	Inflammation/Immunology Cardiovascular Disease
Hederagenin 28-O-beta-D-glucopyranosyl ester, a triterpenoid saponin isolated from Ilex cornuta, exhibits protective effects against H₂O₂-induced myocardial cell injury.

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-N7035

*Wogonin 7-O-beta-D-glucuronide methyl ester* Wogonoside methyl ester	Others	Metabolic Disease
Wogonin 7-O-beta-D-glucuronide methyl ester is a natural compound isolated from Huanglian Jiedutang.

HY-P2558

GSK3 Substrate, α, β subunit
GSK-3 Others

GSK3 Substrate, α, β subunit is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used to measure GSK-3 activity.
HY-141133

Propargyl-PEG4-tetra-Ac-beta-D-glucose
PROTAC Linker Cancer

Propargyl-PEG4-tetra-Ac-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-N4179

Aurantio-obtusin β-D-glucoside Glucoaurantio-obtusin	Others	Metabolic Disease
Aurantio-obtusin β-D-glucoside (Glucoaurantio-obtusin), isolated from Cassiae Semen (seeds of Cassia tora), is a glucoside of aurantio-obtusin.

HY-141135

Propargyl-PEG4-tetra-Ac-beta-D-galactose
PROTAC Linker Cancer

Propargyl-PEG4-tetra-Ac-beta-D-galactose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
HY-141127

Azido-PEG4-tetra-Ac-beta-D-glucose
PROTAC Linker Cancer

Azido-PEG4-tetra-Ac-beta-D-glucose is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-125033

EIDD-1931 β-D-N4-hydroxycytidine; NHC	SARS-CoV Enterovirus HCV Topoisomerase	Infection
EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV).

HY-N3811

ent-11β-Hydroxyatis-16-ene-3,14-dione	RSV	Infection
ent-11β-Hydroxyatis-16-ene-3,14-dione (compound 11) is a diterpenoid from the fresh roots of Euphorbia jolkinii. ent-11β-Hydroxyatis-16-ene-3,14-dione has anti-RSV activity.

HY-B0770

Artemotil β-Arteether; (+)-Arteether; Arteether	Parasite	Infection Cancer
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant *Plasmodium falciparum* malaria with an IC₅₀ of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.

HY-113949

Methyl 2,3-O-Isopropylidene-β-D-ribofuranoside	Others	Others
Methyl 2,3-O-Isopropylidene-β-D-ribofuranoside, obtained from D-ribose, is an intermediate for the synthesis of riboside-containing arsenic compound.

HY-N5039

1,2-O-Dilinoleoyl-3-O-Beta-D-Galactopyranosylracglycerol
Others Others

1,2-O-Dilinoleoyl-3-O-Beta-D-Galactopyranosylracglycerol is isolated from the flower of Magnolia denudate.

HY-N7681

Taxifolin 7-O-β-D-glucoside Taxifolin 7-O-glucoside	Others	Others
Taxifolin 7-O-β-D-glucoside (Taxifolin 7-O-glucoside) is one of the main metabolites at the seed germination stage in Scutellaria baicalensis. Taxifolin 7-O-β-D-glucoside, a flavonoid, mainly exists in the episperm and participates in defending against pathogens and UV-damage.

HY-115365

(3β,20E)-24-Norchola-5,20(22)-diene-3,23-diol
Others Others

(3β,20E)-24-Norchola-5,20(22)-diene-3,23-diol is a steroid-based allylic alcohol.

HY-N7003

28-Demethyl-β-amyrone 28-Norolean-12-en-3-one	Bacterial	Infection
28-Demethyl-β-amyrone (28-Norolean-12-en-3-one) is one of the main triterpenes from Pistacia lentiscus var. Chia. 28-Demethyl-β-amyrone is an antitoxin and can effectively for the toxic effects of Staphylococcal enterotoxins (SEs).

HY-114760

Vanillic acid glucoside Vanillic acid 4-β-D-glucoside	Others	Others
Vanillic acid glucoside (Vanillic acid 4-β-D-glucoside), a hydrolyzable tannin, is isolated from the fruits of C. annuum as well as the leaves of various additional plants. Vanillic acid glucoside can be phytotoxic against different species.

HY-133407

β-Estradiol-6-one 6-(O-carboxymethyloxime)	PROTAC Linker	Cancer
β-Estradiol-6-one 6-(O-carboxymethyloxime) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-111638

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine
Nucleoside Antimetabolite/Analog Infection

1-(2'-O-4-C-Methylene-beta-D-ribofuranosyl)thymine is a bicyclic nucleoside.

HY-131086

Me-triacetyl-β-D-glucopyranuronate-Ph-ald-NO2	ADC Linker	Cancer Inflammation/Immunology
Me-triacetyl-β-D-glucopyranuronate-Ph-ald-NO2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-N4008

Iriflophenone 3-C-glucoside Iriflophenone 3-C-β-D-glucopyranoside	Others	Metabolic Disease
Iriflophenone 3-C-β-D-glucopyranoside, isolated from Cyclopia genistoides, has antioxidant activity.

HY-136318

β-D-tetraacetylgalactopyranoside-PEG1-N3	ADC Linker	Cancer
β-D-tetraacetylgalactopyranoside-PEG1-N3 is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-N6082

Rhein 8-Glucoside Rhein 8-O-β-D-Glucopyranoside	Others	Metabolic Disease
Rhein 8-Glucoside (Rhein 8-O-β-D-Glucopyranoside) is an anthraquinone glycoside that has been found in rhubarb. Purgative activity.

HY-130929

β-Estradiol-6-CMO-PEG3-biotin
ADC Linker Cancer

β-Estradiol-6-CMO-PEG3-biotin is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-B1739

Pregnenolone monosulfate 3β-Hydroxy-5-pregnen-20-one monosulfate	Cannabinoid Receptor Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication.

HY-110189

Pregnenolone monosulfate sodium salt 3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt	Cannabinoid Receptor Endogenous Metabolite Autophagy	Neurological Disease
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.

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-N7628

Cassiaside C Toralactone 9-O-β-D-gentiobioside	Others	Metabolic Disease
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitory activity on advanced glycation end products (AGE) formation in vitro.

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-N5128

Apigenin6-C-α-L-arabinopyranosyl-8-C-β-D-xylopyranoside
Others Others

Apigenin6-C-α-L-arabinopyranosyl-8-C-β-D-xylopyranoside is a natural flavanone compound.

HY-N3893

Farrerol 7-O-β-D-glucopyranoside Farrerol 7-O-glucoside	Others	Others
Farrerol 7-O-β-D-glucopyranoside (Farrerol 7-O-glucoside) is a flavonoid compound isolated from the leaves of Rhododendron dauricum L.

HY-P9911

Vedolizumab Anti-Human lymphocyte α4β7 integrin, Humanized Antibody	Integrin	Inflammation/Immunology
Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.

HY-131087

Me-triacetyl-β-D-glucopyranuronate-Ph-CH2OH-Fmoc	ADC Linker	Cancer
Me-triacetyl-β-D-glucopyranuronate-Ph-CH2OH-Fmoc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

HY-107829

3-Aminopropionitrile fumarate (2:1) Di-β-aminopropionitrile fumarate; β-Aminopropionitrile fumarate; β-Ammoniumpropionitrile hemifumarate	Others	Others
3-Aminopropionitrile fumarate (2:1) is a lathyrogen which inhibits crosslinking of collagen.

HY-131096

L-Proline 4-methoxy-β-naphthylamide hydrochloride H-Pro-4MβNA hydrochloride	Others	Cancer
L-Proline 4-methoxy-β-naphthylamide hydrochloride (H-Pro-4MβNA hydrochloride) can be used for Fap-activated anti-tumor compounds preparaction.

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-N6958

2-O-β-D-Glucopyranosyl-L-ascorbic acid AA-2βG	Others	Cancer Metabolic Disease
2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG), isolated from Lycium Fruit, is a stable vitamin C analog with anti-tumor activity.

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 ^[1].

HY-113013A

Hydroxypyruvic acid lithium hydrate β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate	Endogenous Metabolite	Metabolic Disease
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.

HY-N5084

Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside	Others	Others
Pinocembrin 7-O-[3''-O-galloyl-4'',6''-hexahydroxydiphenoyl]-β-D-glucoside is a flavanone compound.

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-W018512

7-Ketolithocholic acid 3α-Hydroxy-7-oxo-5β-cholanic acid	Endogenous Metabolite	Metabolic Disease
7-Ketolithocholic acid (3α-Hydroxy-7-oxo-5β-cholanic acid), a bile acid, can be absorbed and suppresses endogenous bile acid production and biliary cholesterol secretion.

HY-10590

TWS119
GSK-3 Autophagy Neurological Disease Cancer

TWS119 is a specific inhibitor of GSK-3β, with an IC₅₀ of 30 nM, and activates the wnt/β-catenin pathway.

HY-N2174

*Ophiogenin 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside*	Others	Cardiovascular Disease
Ophiogenin 3-O-α-L-rhamnopyranosyl-(1→2)-β-D-glucopyranoside, a terpenoid glycoside from Ophiopogon japonicus roots, has good pharmacological effects on the cardiovascular system.

HY-107819

5α-Cholestan-3β-ol Dihydrocholesterol; 5α-Cholestanol; NSC 18188	Endogenous Metabolite	Others
5α-Cholestan-3β-ol is a derivitized steroid compound, which is isolated from the testes of White Carneau pigeons.

HY-17631A

Edonerpic maleate
T-817 maleate; T-817MA
Amyloid-β Neurological Disease

Edonerpic maleate is a novel neurotrophic agent which can inhibit amyloid-β peptides (Aβ).

HY-13335

PKCβ inhibitor 1	PKC Apoptosis	Cancer
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC₅₀s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).

HY-N8441

Neriifolin 17β-Neriifolin	Na+/K+ ATPase Apoptosis	Cancer Inflammation/Immunology
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na⁺, K⁺-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells^[2.

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-U00424

Chol-5-en-24-al-3β-ol Vitamin D3 derivative	VD/VDR	Metabolic Disease
Chol-5-en-24-al-3β-ol is a steroid compound (Vitamin D3 derivative) extracted from patent US 4354972 A, Compound IX.

HY-B0381B

Levobetaxolol hydrochloride (S)-betaxolol hydrochloride; AL-1577A	Adrenergic Receptor	Neurological Disease Endocrinology
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker) that can lower the pressure in the eye.

HY-117432

JC-171	NOD-like Receptor (NLR)	Inflammation/Immunology
JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC₅₀ of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages.

HY-19383

Ertiprotafib PTP 112	Phosphatase IKK PPAR	Metabolic Disease
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC₅₀ of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC₅₀ of ~1 μM for PPARα/PPARβ.

HY-14879A

Avibactam sodium NXL-104	Bacterial Antibiotic	Infection
Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam *β-lactamase* inhibitor which inhibits β-lactamase *TEM-1* and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively.

HY-14879B

Avibactam sodium hydrate NXL-104 hydrate	Bacterial Antibiotic	Infection
Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam *β-lactamase* inhibitor which inhibits β-lactamase *TEM-1* and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively.

HY-N4128

4''-methyloxy-Daidzin Daidzein 7-O-Β-D-glucoside 4''-O-methylate	Others	Inflammation/Immunology
4''-methyloxy-Daidzin (Daidzein 7-O-Β-D-glucoside 4''-O-methylate), an isoflavone methyl-glycoside, is isolated from Cordyceps militaris grown on germinated soybeans. Isoflavones possess immunomodulating and antiallergic activities.

HY-12292

IM-12
GSK-3 Cancer

IM-12 is an inhibitor of GSK-3β, with an IC₅₀ of 53 nM, and also enhances Wnt signalling.
HY-19050

BRL-42715
Bacterial Infection

BRL-42715 is a potent inhibitor of a broad range of bacterial beta-lactamases (β-lactamase) ^[1].

HY-B1127

Betamipron N-Benzoyl-β-alanine	Bacterial Antibiotic	Others
Betamipron is a chemical compound which is used together with Panipenem to inhibit Panipenem uptake into the renal tubule and prevent nephrotoxicity.

HY-14879

Avibactam free acid NXL-104 free acid	Bacterial Antibiotic	Infection
Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam *β-lactamase* inhibitor which inhibits β-lactamase *TEM-1* and CTX-M-15 with IC₅₀s of 8 nM and 5 nM, respectively.

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-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-14872

Tideglusib NP031112	GSK-3	Neurological Disease
Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC₅₀s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.

HY-N2481

Oroxylin A-7-O-glucuronide Oroxyloside; Oroxylin A-7-O-β-D-glucuronide	Others	Neurological Disease
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity.

HY-U00426

BF738735
PI4K Reverse Transcriptase Infection

BF738735 is a phosphatidylinositol 4-kinase III beta (PI4KIIIβ) inhibitor with an IC₅₀ of 5.7 nM.
HY-18644

CWHM-12
Integrin Cancer

CWHM-12 is a potent inhibitor of αV integrins with IC₅₀s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.

HY-18173

AZD8329	Others	Metabolic Disease
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.

HY-19676

Pralnacasan VX-740; HMR 3480	Caspase	Inflammation/Immunology
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a K_i of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, *IL-1β* , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.

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-129453

BOP sodium	Integrin	Inflammation/Immunology
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with K_d values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.

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-B1275A

Cephalothin
Cephalotin
Bacterial Antibiotic Infection

Cephalotin (Cephalotin) is a beta-lactam antibiotic, inhibits class C β-lactamase AmpC, with an K_i of 0.32 µM.

HY-17462

Adrenosterone (+)-Adrenosterone	Androgen Receptor Endogenous Metabolite	Endocrinology
Adrenosterone ((+)-Adrenosterone) is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone also is a selective and competitive inhibitor of hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1).

HY-B1418

Tazobactam CL-298741; YTR-830H	Bacterial Antibiotic	Infection
Tazobactam is a beta Lactamase Inhibitor with antibacterial activity Target: Antibacterial Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.

HY-59090

1-Azakenpaullone 1-Akp	GSK-3	Metabolic Disease
1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC₅₀ value of 18 nM.

HY-128483

Fusaric acid
Dopamine β-hydroxylase Infection

Fusaric acid is a potent dopamine β-hydroxylase inhibitor.

HY-10403

PH-797804	p38 MAPK Autophagy	Inflammation/Immunology Cancer
PH-797804 is a ATP-competitive, selective *p38α/p38β* inhibitor (IC₅₀=26 nM and K_i=5.8 nM for p38α; K_i=40 nM for p38β) and does not inhibit JNK2.

HY-16143

Cilengitide TFA EMD 121974 TFA	Integrin Autophagy	Cancer
Cilengitide is a potent and selective integrin inhibitor for α_vβ₃ and α_vβ₅ receptor, with IC₅₀ values of 4 nM and 79 nM, respectively.

HY-B0320A

Cromolyn sodium Disodium Cromoglycate; FPL-670	Calcium Channel GSK-3	Inflammation/Immunology
Cromolyn sodium (Disodium Cromoglycate; FPL-670) is an antiallergic drug. Cromolyn sodium is a *GSK-3β* inhibitor with an IC₅₀ of 2.0 µM.

HY-18748

BQR-695
NVP-BQR695
PI4K Parasite Infection

BQR-695 is a PI4KIIIβ inhibitor with IC₅₀s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
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-18055

BVT-14225
Others Metabolic Disease

BVT-14225 is a selective 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC₅₀ of 52 nM.
HY-18053

AZD 4017
Others Metabolic Disease

AZD 4017 is a potent, selective 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) inhibitor, with an IC₅₀ of 7 nM.

HY-12743A

K-7174 dihydrochloride	Others	Inflammation/Immunology
K-7174 dihydrochloride is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.

HY-12743

K-7174	Others	Inflammation/Immunology
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.

HY-112502

MethADP
Adenosine 5'-(α,β-methylene)diphosphate
CD73 Cancer

MethADP is a specific CD73 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-N0373

Licochalcone B	Amyloid-β	Neurological Disease
Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC₅₀=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.

HY-113960

ERRα antagonist-1	Estrogen Receptor/ERR	Cancer
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC₅₀ values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.

HY-100608

BMS453 BMS-189453	RAR/RXR	Cancer
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.

HY-19306

SB-267268	Integrin	Cancer
SB-267268 is a selective and nonpeptidic *alpha(v)beta3 (αvβ3)* and *alpha(v)beta5 (αvβ5)* integrins antagonist, with K_is of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC₅₀s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.

HY-19964

Potassium clavulanate cellulose Potassium clavulanate:cellulose (1:1)	Bacterial Antibiotic	Infection
Potassium clavulanate cellulose is a mixture of potassium clavulanate and cellulose, is a beta-lactamase inhibitor.

HY-101091

Importazole
Apoptosis Cancer

Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.
HY-50948

Bay 65-1942 hydrochloride
IKK Inflammation/Immunology

Bay 65-1942 hydrochloride is an ATP-competitive and selective IKKβ inhibitor.
HY-112045

PRI-724
Wnt Cancer

PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
HY-105661

IMD-0560
IKK Cancer

IMD-0560 is a novel IκB kinase β inhibitor.
HY-16777

Entasobulin
Microtubule/Tubulin Cancer

Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.

HY-N1280

Semilicoisoflavone B	Amyloid-β	Neurological Disease
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.

HY-B0445

NAD+ β-DPN; β-NAD; β-Nicotinamide Adenine Dinucleotide	Endogenous Metabolite	Metabolic Disease
NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.

HY-16752

Relebactam MK-7655	Bacterial	Infection
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.

HY-15483

DY131 GSK 9089	Estrogen Receptor/ERR Smo	Cancer Endocrinology
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ. DY131 also inhibits Smo signaling.

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-10985

Marizomib Salinosporamide A; NPI-0052	Proteasome	Cancer
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC₅₀=3.5, 28, and 430 nM, respectively).

HY-15721

FH535
PPAR Wnt β-catenin Cancer

FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
HY-103705

iCRT3
Wnt Apoptosis Cancer

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.
HY-19930

Vaborbactam
RPX7009
Bacterial Infection

Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase 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-119706

Barbadin	Others	Others
Barbadin is a novel and selective *β-arrestin/β2-adaptin* interaction inhibitor, has IC₅₀ values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.

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-120697

MSAB	Wnt β-catenin	Cancer
MSAB is a potent and selective inhibitor of *Wnt/β-catenin* signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.

HY-14126

BIO-1211	Integrin	Inflammation/Immunology
BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC₅₀ values of 4 nM and 2 μM for α4β1 and α4β7, respectively.

HY-103394

TC HSD 21	Others	Cancer
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC₅₀ of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.

HY-N6640

2-O-Acetyl-20-hydroxyecdysone 20-Hydroxyeedysone 2-acetate	Others	Neurological Disease
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β₄₂ (Aβ₄₂)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils.

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-15438

SB 415286	GSK-3 Apoptosis	Metabolic Disease
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC₅₀ of 77.5 nM, and a K_i of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and *GSK-3β*.

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-P1481

β-Casomorphin, human
Human β-casomorphin 7
Opioid Receptor Metabolic Disease

is an opioid peptide, acts as an agonist of opioid receptor.
HY-100944

Conduritol B epoxide
Glucosidase Neurological Disease

Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.
HY-107368

Sulcotrione
Reactive Oxygen Species Others

Sulcotrione is a β-triketone herbicide which can inhibit hydroxyphenylpyruvate dioxygenase (HPPD).
HY-A0256A

Clavulanate potassium
Bacterial Antibiotic Infection

Clavulanate potassium is a potent β-lactamase inhibitor and acts as an antibiotic.
HY-12704

ITD-1
TGF-β Receptor Cardiovascular Disease

ITD-1 is the first selective TGFβ receptor inhibitor with an IC₅₀ of 460 nM.
HY-15374

Frentizole
Amyloid-β Inflammation/Immunology

Frentizole, an FDA-approved immunosuppressive drug, is a novel inhibitor of the Aβ-ABAD interaction.

HY-B0203A

Nebivolol hydrochloride R 065824 hydrochloride	Adrenergic Receptor Apoptosis	Cardiovascular Disease Endocrinology
Nebivolol hydrochloride selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.

HY-B0203

Nebivolol
R 065824
Adrenergic Receptor Cardiovascular Disease Endocrinology

Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.

HY-103374

Phenserine (-)-Eseroline phenylcarbamate; (-)-Phenserine	AChE Amyloid-β	Neurological Disease
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.

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-100445A

αvβ1 integrin-IN-1 TFA	Integrin	Cancer Cardiovascular Disease
αvβ1 integrin-IN-1 TFA (Compound C8) is a potent and selective αvβ1 integrin inhibitor with an IC₅₀ of 0.63 nM. Antifibrotic effects.

HY-N0074

Byakangelicol	COX	Inflammation/Immunology
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.

HY-N4186

Glabrolide
Beta-secretase Neurological Disease

Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].

HY-101444A

PAβN dihydrochloride MC-207,110 dihydrochloride; Phe-Arg-β-naphthylamide dihydrochloride	Bacterial	Infection
PAβN dihydrochloride (MC-207110 dihydrochloride) is an efflux pump inhibitor.

HY-13671

LW6 HIF-1α inhibitor; LW8	HIF/HIF Prolyl-Hydroxylase Apoptosis	Cancer
LW6 (HIF-1α inhibitor) is a novel *HIF-1* inhibitor with an IC₅₀ of 4.4 μM. LW6 decreases *HIF-1α* protein expression without affecting HIF-1β expression.

HY-100207

CP21R7
CP21
GSK-3 Cancer

CP21R7 is potent GSK-3β inhibitor, with an IC₅₀ of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC₅₀ of 1900 nM.

HY-N1064

Xanthoplanine	nAChR	Neurological Disease
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC₅₀ ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC₅₀ values of 9 μM (alpha7) and 5 μM (alpha4beta2).

HY-N0249

Saikosaponin C	Amyloid-β	Neurological Disease
Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.

HY-100563

Cyclo(RGDyK) trifluoroacetate
Integrin Cancer

Cyclo(RGDyK) trifluoroacetate is a potent and selective α_Vβ₃ integrin inhibitor with an IC₅₀ of 20 nM.
HY-100563A

Cyclo(RGDyK)
Integrin Cancer

Cyclo(RGDyK) is a potent and selective α_Vβ₃ integrin inhibitor with an IC₅₀ of 20 nM.
HY-B0788A

LY2409881 trihydrochloride
IKK Apoptosis Cancer

LY2409881 trihydrochloride is a selective IκB kinase β (IKK2) inhibitor with an IC₅₀ of 30 nM.
HY-A0256B

Clavulanate lithium
Bacterial Antibiotic Infection

Clavulanate lithium is a potent β-lactamase inhibitor and acts as an antibiotic.

HY-19918A

Anatabine dicitrate	NF-κB Amyloid-β nAChR	Inflammation/Immunology Neurological Disease
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.

HY-13027

DAPT GSI-IX	γ-secretase Amyloid-β Autophagy Notch Apoptosis	Cancer Inflammation/Immunology Neurological Disease
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC₅₀s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ₄₂, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.

HY-N2566

Euscaphic acid	DNA/RNA Synthesis PI3K Apoptosis	Cancer
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC₅₀ values of 61 and 108 μM. Euscaphic acid induces apoptosis.

HY-N0270

Ononin
Ononoside; Formononetin 7-O-β-D-glucopyranoside
Others Others

Ononin is an isoflavonoid, is an additional growth inhibitor in soils associated with the weed, Pluchea lanceolata.

HY-112108

Chitosan oligosaccharide COS	AMPK	Cancer Metabolic Disease
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.

HY-N0042

Ginsenoside Rc Panaxoside Rc	GABA Receptor TNF Receptor Interleukin Related	Cancer Inflammation/Immunology Neurological Disease
Ginsenoside Rc, one of major Ginsenosides from Panax ginseng, enhances GABA receptor_A (GABA_A)-mediated ion channel currents (I_GABA). Ginsenoside Rc inhibits the expression of TNF-α and *IL-1β*.

HY-B1154

Penbutolol sulfate (-)-Terbuclomine	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Penbutolol sulfate is able to bind to both beta-1 adrenergic receptors and beta-2 adrenergic receptors (the two subtypes), thus making it a non-selective β blocker.

HY-101090

KYA1797K
Wnt β-catenin Cancer

KYA1797K is a potent and selective Wnt/β-catenin inhibitor with an IC₅₀ of 0.75 µM.
HY-16294

LY2090314
GSK-3 Cancer

LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC₅₀ values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.

HY-107790

5-Methoxyflavone	DNA/RNA Synthesis	Neurological Disease
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABA_A receptors.

HY-P1420

TAT-cyclo-CLLFVY	HIF/HIF Prolyl-Hydroxylase	Cancer
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of *HIF-1* heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts *HIF-1α/HIF-1β* protein-protein interaction with an IC₅₀ of 1.3 μM.

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-101930

BMS-816336	Others	Metabolic Disease
BMS-816336 is a novel, potent and orally bioavailable inhibitor against *human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme* with an IC₅₀ of 3.0 nM.

HY-15761

AZD2858	GSK-3	Neurological Disease
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC₅₀s of 0.9 and 5 nM for GSK-3α and *GSK-3β*, respectively, used in the research of fracture healing.

HY-111931

Indirubin-3'-monoxime-5-sulphonic acid	CDK GSK-3	Cancer
Indirubin-3'-monoxime-5-sulphonic acid is a potent and selective inhibitor of *CDK1, CDK5, and GSK-3β* with IC₅₀s of 5 nM, 7 nM, and 80 nM, respectively.

HY-14428

ICG-001	β-catenin Apoptosis	Cancer
ICG-001 is an inhibitor of *β-catenin/TCF* mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC₅₀ of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.

HY-129492

GNF4877	DYRK GSK-3	Metabolic Disease
GNF4877 is a potent *DYRK1A* and *GSK3β* inhibitor with IC₅₀s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC₅₀ of 0.66 μM for mouse β (R7T1) cells).

HY-N0722

Neochlorogenic acid trans-5-O-Caffeoylquinic acid	NF-κB Interleukin Related TNF Receptor COX	Inflammation/Immunology Cancer
Neochlorogenic acid is a natural polyphenolic compound found in dried fruits and other plants. Neochlorogenic acid inhibits the production of TNF-α and *IL-1β. Neochlorogenic acid suppresses iNOS and COX-2* protein expression. Neochlorogenic acid also inhibits phosphorylated NF-κB p65 and p38 MAPK activation.

HY-16659

EHT 1864	Ras	Neurological Disease Cancer
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The K_d values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.

HY-B1434

7-Aminocephalosporanic acid 7-ACA	Bacterial Antibiotic	Infection
7-Aminocephalosporanic acid is the core chemical structure for the synthesis of cephalosporin antibiotics, is a potent β-lactamase inhibitor.

HY-16321

Micafungin sodium
FK 463 sodium
Fungal Antibiotic Infection

Micafungin sodium (FK 463 sodium) is an antifungal agent which inhibits 1, 3-beta-D-glucan synthesis.
HY-103095

AAI101
Bacterial Infection

AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
HY-13019

BI605906
IKK Others

BI605906 is a novel IKKβ inhibitor with an IC₅₀ value of 380 nM when assayed at 0.1 mM ATP.
HY-10344

AZD 6482
KIN-193
PI3K Autophagy Cancer

AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC₅₀ of 0.69 nM.
HY-100337

WWL70
MAGL Neurological Disease

WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC₅₀ of 70 nM.
HY-14281

Trilostane
Win 24540
Others Endocrinology Cancer

Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
HY-12014

SU11274
PKI-SU11274
c-Met/HGFR Autophagy Apoptosis Cancer

SU11274 is a selective Met inhibitor with IC₅₀ of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
HY-76691

D-Ribonolactone
Endogenous Metabolite Bacterial Infection

D-Ribonolactone is sugar lactone and an inhibitor of β-galactosidase of Escherichia coli with a K_i of 26 mM.

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-B0240

Disulfiram Tetraethylthiuram disulfide; TETD	Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis	Metabolic Disease Cancer
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells^[1-4].

HY-W010041

Scyllo-Inositol	Amyloid-β Endogenous Metabolite	Neurological Disease
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of *amyloid-β* peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.

HY-103241

Ro 90-7501	Amyloid-β ATM/ATR Phosphatase Apoptosis	Cancer Neurological Disease
Ro 90-7501 is an *amyloid β₄₂* (Aβ₄₂) fibril assembly** inhibitor that reduces Aβ₄₂-induced cytotoxicity (EC₅₀ of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.

HY-126114

Lupeol acetate	Others	Inflammation/Immunology
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.

HY-124257

(R)-Citronellol D-Citronellol; (R)-(+)-β-Citronellol	Endogenous Metabolite	Inflammation/Immunology
(R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products.

HY-101853

STAT5-IN-1
STAT Cancer

STAT5-IN-1 is a STAT5 inhibitor with an IC₅₀ of 47 μM for STAT5β isoform.
HY-U00206

D2343
Adrenergic Receptor Endocrinology

D2343 is a β2-adrenoceptor agonist and also is an α1- adrenoceptor inhibitor.

HY-B0974

Methicillin sodium salt Meticillin sodium	Bacterial Antibiotic	Infection
Methicillin sodium salt (Meticillin sodium) is a β-lactam antibiotic which acts by inhibiting penicillin-binding proteins that are involved in the synthesis of peptidoglycan.

HY-B0703

Eslicarbazepine acetate BIA 2-093	Beta-secretase Sodium Channel	Neurological Disease
Eslicarbazepine acetate (BIA 2-093), an antiepileptic drug, is a dual a dual Inhibitor of *β-Secretase* and voltage-gated sodium channel.

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-100607A

Landiolol hydrochloride ONO1101 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting *beta*-blocker (β1/β2 selectivity = 255:1, a half-life of 4 min)， acts as an adrenoceptor antagonist.

HY-137315

TML-6	Amyloid-β NF-κB mTOR Keap1-Nrf2	Neurological Disease
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.

HY-10016

E 2012	γ-secretase	Neurological Disease
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.

HY-B0379A

Adiphenine hydrochloride	nAChR	Neurological Disease
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC₅₀s of 1.9, 1.8, 3.7, and 6.3 µM for α1, *α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has narcotic and anticonvulsant effects.*

HY-10873

N-Desethyl Sunitinib SU-12662	Others	Cancer
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with K_i values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.

HY-N7115

Sultamicillin	Bacterial Antibiotic	Infection
Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant.

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-14823

Sobetirome GC-1; QRX-431	Thyroid Hormone Receptor	Metabolic Disease Endocrinology
Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC₅₀ of 0.16 μM.

HY-13951

ICI 118,551 hydrochloride ICI 118551 hydrochloride	Adrenergic Receptor	Neurological Disease Endocrinology
ICI 118,551 (hydrochloride) is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

HY-13605

Cytarabine Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C	DNA/RNA Synthesis Nucleoside Antimetabolite/Analog HSV Autophagy Endogenous Metabolite Apoptosis	Cancer Infection
Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC₅₀ of 16 nM. Cytarabine has antiviral effects against HSV.

HY-13605A

Cytarabine hydrochloride Cytosine β-D-arabinofuranoside hydrochloride; Cytosine Arabinoside hydrochloride; Ara-C hydrochloride	DNA/RNA Synthesis Nucleoside Antimetabolite/Analog HSV Autophagy	Cancer Infection
Cytarabine hydrochloride, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC₅₀ of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.

HY-17006

Caspofungin Acetate MK-0991 Acetate; L-743872 Acetate	Fungal Antibiotic	Infection
Caspofungin Acetate (MK-0991 Acetate) is an antifungal drug, and noncompetitively inhibits 1,3-β-d glucan synthase activity.

HY-B0555A

Nafcillin sodium monohydrate	Bacterial Antibiotic	Infection
Nafcillin sodium monohydrate, an antibiotic, is a reversible inhibitor of *β-lactamase. Nafcillin sodium monohydrate can be used for the research of staphylococcal infections.*

HY-12662

PE859
Microtubule/Tubulin Neurological Disease

PE859 is a potent inhibitor of both tau and Aβ aggregation with IC₅₀ values of 0.66 and 1.2 μM, respectively.
HY-12075

LY2109761
TGF-β Receptor Autophagy Cancer

LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with K_is of 38 nM and 300 nM, respectively.
HY-P1613A

Cyclo(Arg-Gly-Asp-D-Phe-Val) TFA
Integrin Cancer

Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
HY-13226

Galunisertib
LY2157299
TGF-β Receptor Cancer

Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC₅₀ of 56 nM.

HY-N0283

Diacerein Diacerhein; Diacetylrhein	Interleukin Related	Inflammation/Immunology
Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a slow-acting medicine of the class anthraquinone used to treat joint diseases.

HY-15509A

Semapimod tetrahydrochloride CNI-1493; CPSI-2364 tetrahydrochloride	TNF Receptor Interleukin Related p38 MAPK	Inflammation/Immunology
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, *IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits* TLR4 signaling (IC₅₀≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.

HY-N0604

Ginsenoside Rh1 Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1	PPAR TNF Receptor Interleukin Related Endogenous Metabolite	Inflammation/Immunology
Ginsenoside Rh1 (Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1) is isolated from the root of Panax Ginseng. Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, IL-6, and *IL-1β*.

HY-111055

BIP-135	GSK-3	Neurological Disease
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC₅₀s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.

HY-14176

Compound E	γ-secretase	Cancer
Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC₅₀s of 0.24, 0.37, 0.32 nM, respectively.

HY-B0927

Hydrastine
(-)-β-Hydrastine; (1R,9S)-β-Hydrastine
Others Others

Hydrastine is a natural alkaloid which is present in Hydrastis canadensis and other plants of the ranunculaceae family.
HY-N0410

Daucosterol
Eleutheroside A; β-Sitosterol β-D-glucoside
Others Cancer

Daucosterol is a natural sterolin.

HY-A0009

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

HY-103442

CGP52411 DAPH	EGFR Amyloid-β	Cancer Neurological Disease
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC₅₀ of 0.3 μM. CGP52411 blocks the toxic influx of Ca²⁺ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.

HY-15770

TR-14035	Integrin	Inflammation/Immunology
TR-14035 is a dual α₄β₇/α_{4_β1} integrin antagonist, with IC₅₀ s of 7 nM and 87 nM for α₄β₇ and α_{4_β1}, respectively. TR-14035 can be used for the research of inflammation and autoimmune disease.

HY-B2230

Hinokitiol β-Thujaplicin	Keap1-Nrf2 DNA Methyltransferase Virus Protease	Cancer Infection
Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases *DNMT1* and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.

HY-N2147

Phorbol
4β-Phorbol
Others Cancer

Phorbol is a highly toxic diterpene, whose esters have important biological properties.

HY-112799

DK419	Wnt β-catenin	Cancer
DK419 is a potent and orally active *Wnt/β-catenin* signaling inhibitor, with an IC₅₀ of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.

HY-10336

Brivanib (alaninate) BMS-582664	VEGFR Autophagy	Cancer
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.

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-101130

PNU-74654
Wnt β-catenin Apoptosis Cancer

PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC₅₀ of 129.8 μM in NCI-H295 cell.
HY-12050

CP-673451
PDGFR Cancer

CP-673451 is a potent and selective inhibitor of PDGFR with IC₅₀s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
HY-12043

SB 525334
TGF-β Receptor Cancer

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC₅₀ of 14.3 nM.
HY-17579

Micafungin
FK463
Fungal Antibiotic Infection

Micafungin (Mycamine; FK463) is an echinocandin antifungal drug which can inhibit 1,3-beta-D-glucan synthase.

HY-108628

SU16f	PDGFR	Cancer
SU16f is a potent and selective PDGFRβ inhibitor with IC₅₀s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.

HY-16910

WIKI4	PARP β-catenin	Cancer
WIKI4 is a potent tankyrase inhibitor with an IC₅₀ of 26 nM for TNKS2. WIKI4 potently inhibits *Wnt/β-catenin* signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on *Wnt/β-catenin* signaling by inhibiting the enzymatic activity of *TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC₅₀* value of 0.02 μM.

HY-114454

INH14	IKK	Cancer Inflammation/Immunology
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC₅₀s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.

HY-N0702

Tenuifolin	Beta-secretase AChE	Neurological Disease
Tenuifolin is a triterpene isolated from Polygala tenuifolia Willd, has neuroprotective effects. Tenuifolin reduces Aβ secretion by inhibiting *β-secretase. Tenuifolin improves learning and memory in aged mice by decreasing AChE* activity and has the potential for Alzheimer’s disease (AD) treatment.

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-50845

Avagacestat BMS-708163	γ-secretase Notch	Cancer
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC₅₀s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC₅₀ of 0.84 nM and shows weak inhibition of CYP2C19, with IC₅₀ of 20 μM.

HY-113914

9-ING-41	GSK-3 Apoptosis	Cancer
9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity.

HY-B1367

Carbenoxolone disodium	Gap Junction Protein	Infection Inflammation/Immunology
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human *11β-HSD* and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.

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-11102

RO4929097 RG-4733	γ-secretase Notch	Neurological Disease Cancer
RO4929097 (RG-4733) is a γ secretase inhibitor with IC₅₀ of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC₅₀ of 14 nM and 5 nM, respectively.

HY-18988

ETC-159
ETC-1922159
Porcupine Wnt Cancer

ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC₅₀ of 2.9 nM.

HY-P0299A

LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)	TGF-β Receptor	Cancer
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive *TGF-β1* antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of *TSP-1* to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of *TSP-1*-mediated *TGF-β1* activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.

HY-U00183

Epanolol Visacor; ICI141292	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Epanolol (Visacor; ICI141292) is a potent *β-adrenoceptor* partial agonist with a greater affinity for β1- than β2-adrenoceptors.

HY-B0452

Ritodrine hydrochloride
DU21220 hydrochloride
Adrenergic Receptor Endocrinology

Ritodrine hydrochloride (DU21220 hydrochloride) is a β-2 adrenergic receptor agonist.
HY-19468

ERB-196
WAY-202196
Estrogen Receptor/ERR Inflammation/Immunology Neurological Disease

ERB-196 is a nonsteroidal selective estrogen receptor-β (ERβ) agonist.

HY-15102

MK-0429 L-000845704	Integrin	Inflammation/Immunology Cancer
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC₅₀ values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.

HY-13076

CHIR-98014	GSK-3	Metabolic Disease
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC₅₀s of 0.65 and 0.58 nM for GSK-3α and *GSK-3β*, respectively; it shows less potent activities against cdc2 and erk2.

HY-P0023

Cyclo(-RGDfK)	Integrin	Cancer
Cyclo(-RGDfK) is a potent and selective inhibitor of the α_vβ₃ integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

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-112619

TES-991
Others Metabolic Disease

TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC₅₀ of 3 nM.
HY-15837

SAR-260301
PI3K Cancer

SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC₅₀ of 23 nM.

HY-N7111

Sultamicillin tosylate	Bacterial	Infection
Sultamicillin (tosylate) is a potent and orally active *beta-lactamase* inhibitor, an antibiotic with antibacterial activity. Sultamicillin (tosylate) is the tosylate salt of the double ester of sulbactam plus ampicillin.

HY-100198

PI4KIIIbeta-IN-10
PI4K Infection

PI4KIIIbeta-IN-10 is a potent PI4KIIIβ inhibitor with an IC₅₀ of 3.6 nM.
HY-B0942

Benzethonium chloride
nAChR Neurological Disease

Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.

HY-10256A

SB 203580 hydrochloride RWJ 64809 hydrochloride	p38 MAPK Autophagy Mitophagy	Inflammation/Immunology Cancer
SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and *SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits* LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.

HY-112220

VIT-2763	Others	Metabolic Disease
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.

HY-10230

Midostaurin PKC412; CGP 41251	PKC	Cancer
Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, *Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ* and *VEGFR1/2* with IC₅₀s ranging from 22-500 nM.

HY-124607B

BRD3731	GSK-3	Neurological Disease
BRD3731 is a selective *GSK3β* inhibitor, with IC₅₀s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 can be used for the research of a mood disorder, post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorder.

HY-125263

OP-1074	Estrogen Receptor/ERR	Cancer
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC₅₀ of 1.6 and 3.2 nM, respectively.

HY-P0023A

Cyclo(-RGDfK) TFA	Integrin	Cancer
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the α_vβ₃ integrin, with an IC₅₀ of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.

HY-111267

Aftin-4
Amyloid-β Neurological Disease

Aftin-4 is an Amyloid-β₄₂ (Aβ₄₂) inducer.

HY-B0158

Cytidine Cytosine β-D-riboside; Cytosine-1-β-D-ribofuranoside	Nucleoside Antimetabolite/Analog Endogenous Metabolite	Neurological Disease
Cytidine is a pyrimidine nucleoside and acts as a component of RNA. Cytidine is a precursor of uridine. Cytidine controls neuronal-glial glutamate cycling, affecting cerebral phospholipid metabolism, catecholamine synthesis, and mitochondrial function.

HY-109103

Tegatrabetan BC2059	β-catenin	Cancer
Tegatrabetan (BC2059) is a *β-Catenin* antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).

HY-75385

Zaurategrast ethyl ester CDP323; UCB1184197	Integrin	Inflammation/Immunology
Zaurategrast ethyl ester (CDP323), the ethyl ester prodrug of CT7758, is a *α4β1/α4β7* integrin antagonist used for the treatment of inflammatory and autoimmune disorders.

HY-14602

Tramiprosate Homotaurine; 3-Amino-1-propanesulfonic acid	Amyloid-β	Cancer
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent deposition target: Aβ In vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors.

HY-B0573

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

HY-B0573B

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

HY-131447

KY19382 A3051	GSK-3	Metabolic Disease
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and *GSK3β, with IC₅₀s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.*

HY-103200

SR59230A hydrochloride	Adrenergic Receptor	Metabolic Disease Cardiovascular Disease
SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

HY-100672

SR59230A	Adrenergic Receptor	Metabolic Disease Cardiovascular Disease
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC₅₀s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.

HY-18959

CWP232228	β-catenin Wnt	Cancer
CWP232228, a highly potent selective *Wnt/β-catenin* signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).

HY-137472

SAR502250	GSK-3	Neurological Disease
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC₅₀ of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).

HY-101085

SKL2001	Wnt β-catenin	Cancer
SKL2001 is an agonist of the *Wnt/β-catenin* pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.

HY-16276

Osilodrostat LCI699	Mineralocorticoid Receptor	Inflammation/Immunology Cancer
Osilodrostat (LCI699) is a potent inhibitor of human *11β-hydroxylase* and aldosterone synthase with IC₅₀ values of 2.5 and 0.7 nM, respectively.

HY-13535A

ATN-161 trifluoroacetate salt ATN-161 TFA salt	Integrin	Cancer
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.

HY-101271

WAY-200070
Estrogen Receptor/ERR Neurological Disease

WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC₅₀ of 2.3 nM.

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-112182

UM-164
DAS-DFGO-II
Src p38 MAPK Autophagy Cancer

UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a K_d of 2.7 nM. UM-164 also potently inhibits p38α and p38β.

HY-111507

PDGFRα kinase inhibitor 1	PDGFR	Cancer
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC₅₀s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.

HY-75385A

Zaurategrast ethyl ester sulfate CDP323 sulfate; UCB1184197 sulfate	Integrin	Inflammation/Immunology
Zaurategrast ethyl ester sulfate (CDP323 sulfate), the ethyl ester prodrug of CT7758, is a *α4β1/α4β7* integrin antagonist used for the treatment of inflammatory and autoimmune disorders.

HY-15147

XAV-939	β-catenin PARP	Cancer
XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC₅₀s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (K_ds of 99 and 93 nM, respectively).

HY-129113

α-Chaconine	COX	Inflammation/Immunology
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, *IL-1β, IL-6, and TNF-α* at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.

HY-13713

LY377604	Adrenergic Receptor	Metabolic Disease Endocrinology
LY377604 is a *human β₃-adrenergic* receptor agonist with an EC₅₀ of 2.4 nM and also a β₁- and β₂-adrenergic receptor** antagonist.

HY-P2285

AC 253	Amyloid-β
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.

HY-112613

UCB9608	PI4K	Inflammation/Immunology
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC₅₀ of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.

HY-N0633

Muscone	Interleukin Related TNF Receptor NF-κB NOD-like Receptor (NLR)	Inflammation/Immunology Cardiovascular Disease
Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.

HY-19717

DCVC S-[(1E)-1,2-dichloroethenyl]--L-cysteine	TNF Receptor	Inflammation/Immunology
DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.

HY-10256

SB 203580 RWJ 64809	p38 MAPK Autophagy Mitophagy	Inflammation/Immunology Cancer
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and *SAPK2b/p38β2, respectively. SB 203580 inhibits* LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.

HY-14300A

Vilanterol trifenatate GW642444 trifenatate	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Vilanterol trifenatate (GW642444 trifenatate) is a long-acting *β₂-adrenoceptor* (β₂-AR) agonist with inherent 24-hour activity. The pEC₅₀s for β₂-AR, β₁-AR and β₃-AR are 10.37, 6.98 and 7.36, respectively.

HY-100007

Vonoprazan TAK-438 free base	Proton Pump	Endocrinology
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker, with antisecretory activity. Vonoprazan inhibits H⁺,K⁺-ATPase activity in porcine gastric microsomes with an IC₅₀ of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.

HY-A0295

(R)-Propranolol hydrochloride	Adrenergic Receptor	Endocrinology Neurological Disease Cardiovascular Disease
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β₁AR and β₂AR with K_i values of 1.8 nM and 0.8 nM, respectively.

HY-N2022

Castanospermine	Glucosidase	Cancer
Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).

HY-16665

iCRT 14
Wnt Cancer

iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC₅₀ of 40.3 nM against Wnt responsive STF16 luciferase.

HY-12325

GSK2194069	Others	Cancer
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.

HY-100506

GLPG0187
Integrin Cancer

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM.
HY-108313

T-00127_HEV1
PI4K Infection

T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC₅₀ of 60 nM.
HY-B1643

Ethyl Vanillate
Fungal Infection

Ethyl Vanillate is a fungicidal agent. Ethyl Vanillate inhibits 17β-HSD2 with an IC₅₀ 1.3 µM.
HY-16265

JI-101
Ephrin Receptor PDGFR VEGFR Cardiovascular Disease Cancer

JI-101 is an orally available multi-kinase inhibitor of VEGFR2，PDGFRβ and EphB4 with potent anti-cancer activity.
HY-N2215

Aloeresin D
Beta-secretase Neurological Disease

Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC₅₀ of 39 μM.
HY-10407

SU 5402
VEGFR FGFR PDGFR Cancer

SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC₅₀ of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.

HY-14503

MDR-1339 DWK-1339	Amyloid-β	Neurological Disease
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.

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-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-W009009

L-838417	GABA Receptor	Neurological Disease
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABA_A receptor and an antagonist at the α1, with binding K_i values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.

HY-14300

Vilanterol GW642444	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Vilanterol (GW642444) is a long-acting *β₂-adrenoceptor* (β₂-AR) agonist with 24 h activity. The pEC₅₀s for β₂-AR,β₁-AR and β₃-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.

HY-N6712

Thiolutin Acetopyrrothin	Bacterial Antibiotic	Infection Metabolic Disease
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.

HY-110266

GN44028	HIF/HIF Prolyl-Hydroxylase	Cancer
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC₅₀ of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.

HY-14951

Firategrast SB 683699	Integrin	Neurological Disease
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.

HY-13438

AZD3839 free base	Beta-secretase	Cancer
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.

HY-13862

AZD1080	GSK-3	Neurological Disease
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and *GSK3β* with pK_i (IC₅₀) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.

HY-100538A

DTP3 TFA	DNA/RNA Synthesis JNK	Cancer
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.

HY-111930

5-Iodo-indirubin-3'-monoxime	GSK-3 CDK	Cancer
5-Iodo-indirubin-3'-monoxime is a potent *GSK-3β, CDK5/P25* and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC₅₀s of 9, 20 and 25 nM, respectively.

HY-13289A

Nepicastat hydrochloride SYN-117 hydrochloride; RS-25560-197 hydrochloride	Dopamine β-hydroxylase	Cardiovascular Disease
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of *dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC₅₀=8.5 nM) and human (IC₅₀=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).*

HY-101930B

(R)-BMS-816336	Others	Metabolic Disease
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and *cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme* with IC₅₀s of 14.5 nM, 50.3 nM and 16 nM, respectively ^[1].

HY-W050031

(S)-3-Hydroxybutanoic acid (S)-β-Hydroxybutanoic acid; L-(+)-3-Hydroxybutyric acid; L-β-Hydroxybutyric acid	Endogenous Metabolite	Others
(S)-3-Hydroxybutanoic acid is a normal human metabolite, that has been found elevated in geriatric patients remitting from depression. In humans, 3-Hydroxybutyric acid is synthesized in the liver from acetyl-CoA, and can be used as an energy source by the brain when blood glucose is low.

HY-10431

SB-431542
TGF-β Receptor Cancer

SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC₅₀ value of 94 nM.

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-10114

TGX-221
PI3K Cancer

TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.

HY-50883

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

HY-111365

TES-1025
Others Metabolic Disease

TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC₅₀ of 13 nM.

HY-W009168

Tazobactam sodium	Bacterial Antibiotic	Infection
Tazobactam sodium is an antibiotic of the beta-lactamase inhibitor class. Ceftolozane combines with Tazobactam, extends the activity of ceftolozane against many ESBL-producing Enterobacteriaceae and some Bacteroides spp..

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-N7697B

Chitobiose dihydrochloride
Others Others

Chitobiose dihydrochloride, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units.

HY-10456

TAK-715	p38 MAPK Casein Kinase	Inflammation/Immunology
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC₅₀s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.

HY-135674

SR-318	p38 MAPK TNF Receptor	Cancer Inflammation/Immunology
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC₅₀s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC₅₀ of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.

HY-19807

Indirubin-3'-monoxime Indirubin-3'-oxime	GSK-3 Lipoxygenase	Cancer
Indirubin-3'-monoxime is a potent *GSK-3β* inhibitor, and weakly inhibits 5-Lipoxygenase, with IC₅₀s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC₅₀s of 100 and 180 nM.

HY-10580

GSK 3 Inhibitor IX 6-Bromoindirubin-3'-oxime; BIO; MLS 2052	GSK-3 CDK Apoptosis	Cancer
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of *GSK-3α/β* and *CDK1-cyclinB* complex with IC₅₀s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

HY-14302

Salmeterol GR33343X	Adrenergic Receptor	Endocrinology Inflammation/Immunology
Salmeterol (GR33343X) is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-17453

Salmeterol xinafoate GR 33343X xinafoate	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Salmeterol (GR 33343X) xinafoate is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-N0540

Cynaroside Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside	Influenza Virus DNA/RNA Synthesis	Cancer Infection
Cynaroside (Luteolin 7-glucoside) is a flavone, a flavonoid-like chemical compound. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 32 nM.

HY-N4326

14,15 β-Dihydroxyklaineanone
Others Cancer

14,15 D-dihydroxyklaineanone, a quassinoid isolated from the root of Eurycoma longifolia, possesses anti-cancer activity.

HY-W010201

Citronellol (±)-Citronellol; (±)-β-Citronellol	Reactive Oxygen Species	Cancer
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium capitatum. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation.

HY-111760

NRX-252262	β-catenin	Cancer
NRX-252262 is a potent enhancer of the interaction between *β-Catenin, and its cognate E3 ligase, SCF^β-TrCP, induces mutant β-catenin degradation, with an EC₅₀* of 3.8 nM.

HY-136449

Bromchlorbuterol hydrochloride	Adrenergic Receptor	Inflammation/Immunology
Bromchlorbuterol hydrochloride is an active β-adrenergic agonist (β-agonist) and can be used for the research of pulmonary disease and asthma.

HY-14652

Tamibarotene
Am 80
RAR/RXR Autophagy Apoptosis Cancer

Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
HY-107437

CD2665
RAR/RXR Metabolic Disease

CD2665 is a selective RAR-beta/gamma antagonist, with K_i values of 110 nM, 306 nM for RARγ and RARβ, respectively.
HY-131166

Curdlan
Others Others

Curdlan is a polysaccharide produced by bacteria and a homopolymer of glucose with β-1,3-glucosidic linkage.

HY-130609A

Aβ42-IN-1 free base	γ-secretase	Neurological Disease
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC₅₀ value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.

HY-130252

YQ128	NOD-like Receptor (NLR) Interleukin Related	Inflammation/Immunology
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC₅₀ of 0.30 µM. YQ128 significantly and selectively suppresses the production of *IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.*

HY-13289

Nepicastat SYN117; RS-25560-197	Dopamine β-hydroxylase	Cardiovascular Disease
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of *dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC₅₀=8.5 nM) and human (IC₅₀=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).*

HY-18754

FR 167653 free base	p38 MAPK Autophagy	Endocrinology
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.

HY-111424

BDP9066	Ras	Cancer
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC₅₀ of 64 nM for MRCKβ in SCC12 cells, K_i values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.

HY-107531

A 1070722	GSK-3	Cancer
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a K_i of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.

HY-14649

Retinoic acid Vitamin A acid; all-trans-Retinoic acid; ATRA	RAR/RXR PPAR Endogenous Metabolite Autophagy	Cancer
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with K_d of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

HY-B0573A

(S)-(-)-Propranolol hydrochloride	Adrenergic Receptor	Inflammation/Immunology Cardiovascular Disease
(S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log K_d values of -8.16, -9.08, and -6.93 for β₁, β₂, and β₃, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

HY-117388

THI0019	Integrin	Inflammation/Immunology
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC₅₀ range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.

HY-120215

KT203
MAGL Metabolic Disease

KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC₅₀ of 0.31 nM in Neuro2A cells.
HY-120177

KT182
MAGL Others

KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC₅₀ of 0.24 nM in Neuro2A cells.
HY-10501

SU14813
PDGFR VEGFR c-Kit Cancer

SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
HY-10501A

SU14813 maleate
PDGFR VEGFR c-Kit Cancer

SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC₅₀s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
HY-14975

R1487 Hydrochloride
p38 MAPK Autophagy Cancer

R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with K_d values of 0.2 nM and 29 nM for p38α and p38β, respectively.

HY-B0573S

Propranolol D7 hydrochloride	Adrenergic Receptor	Endocrinology Neurological Disease Cardiovascular Disease
Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with K_i values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [³H]-DHA binding to rat brain membrane preparation with an IC₅₀ of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.

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-15614A

SC144 hydrochloride	Interleukin Related Apoptosis	Cancer
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.

HY-10230S

Midostaurin-D5 PKC412-D5; CGP 41251-D5	Others	Cancer
Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, *Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ* and *VEGFR1/2* with IC₅₀s ranging from 22-500 nM.

HY-15614

SC144	Interleukin Related Apoptosis	Cancer
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.

HY-119940

MC180295 (rel)-MC180295	CDK	Cancer
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC₅₀ of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.

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-13904

Flumatinib HHGV678	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.

HY-13013

(E)-SIS3	TGF-beta/Smad	Inflammation/Immunology
(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC₅₀ of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.

HY-13905

Flumatinib mesylate HHGV678 mesylate	Bcr-Abl c-Kit PDGFR	Cancer
Flumatinib mesylate (HHGV678 mesylate) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC₅₀s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.

HY-N6630

6-Methylflavone
GABA Receptor Neurological Disease

6-Methylflavone is an activator of α₁β₂γ_2L and α₁β₂ GABA_A receptors.

HY-A0275

Amezinium methylsulfate Amezinium metilsulfate; Lu-1631	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake.

HY-12216

Resmetirom MGL-3196; VIA-3196	Thyroid Hormone Receptor	Cardiovascular Disease Endocrinology
Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC₅₀ value of 0.21 μM.

HY-135119

Salmeterol-D3	Adrenergic Receptor	Endocrinology Inflammation/Immunology
Salmeterol-D3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC₅₀s of 9.6, 6.1, and 5.9, respectively.

HY-136207

TC-2559 difumarate	nAChR	Neurological Disease
TC-2559 idifumarate is a CNS-selective, orally active *α4β2* subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC₅₀=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC₅₀s in the range of 10-30 µM. Antinociceptive effect.

HY-10215

Luminespib VER-52296; AUY922; NVP-AUY922	HSP Autophagy Apoptosis	Cancer
Luminespib (VER-52296) is a potent HSP90 inhibitor with IC₅₀s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.

HY-N2523

Gigantol	Wnt	Cancer
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the *Wnt/β-catenin* pathway.

HY-N7368

Hibifolin	Adenosine Deaminase	Cancer Inflammation/Immunology Neurological Disease
Hibifolin, a flavonol glycoside, is a potential inhibitor of adenosine deaminase (ADA), with a K_i of 49.92 μM. Hibifolin protects neurons against beta-amyloid-induced neurotoxicity.

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-B1189

Meglutol Dicrotalic acid; 3-Hydroxy-3-methylglutaric acid	HMG-CoA Reductase (HMGCR) Autophagy Endogenous Metabolite	Cardiovascular Disease
Meglutol is an antilipemic agent which lowers cholesterol, triglycerides, serum beta-lipoproteins and phospholipids, and inhibits the activity of hydroxymethylglutarryl CoA reductases, which is the rate limiting enzyme in the biosynthesis of cholesterol.

HY-14316A

Tebanicline dihydrochloride Ebanicline dihydrochloride; ABT-594 dihydrochloride	nAChR	Neurological Disease
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a K_i of 37 pM.

HY-13005

Fagomine D-Fagomine	Others	Metabolic Disease
Fagomine is a mild glycosidase inhibitor. The K_i of the iminosugar Fagomine is 4.8 μM, 39 μM, and 70 μM for Amyloglucosidase (A.niger), β-Glucosidase (bovine), and Isomaltase (yeast), respectively.

HY-13689

Go 6983
Gö 6983; Goe 6983
PKC Cancer

Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC₅₀ of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
HY-78349

A 77-01
TGF-β Receptor Cancer

A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC₅₀ of 25 nM.
HY-12437

BDP5290
ROCK Cancer

BDP5290 is a potent inhibitor of both ROCK and MRCK with IC₅₀s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

HY-100760

Toxoflavin Xanthothricin; Toxoflavine; PKF-118-310	β-catenin	Cancer
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.

HY-10401

VX-702
p38 MAPK Autophagy Inflammation/Immunology

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.

HY-N0582

Qingyangshengenin B	Others	Neurological Disease
Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.

HY-N7652

Terminolic acid	Bacterial	Infection Inflammation/Immunology
Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity.

HY-10974

MK-0752	γ-secretase	Neurological Disease Cancer
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC₅₀ of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.

HY-18754A

FR 167653 FR 167653 sulfate	p38 MAPK Autophagy	Endocrinology
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.

HY-111911

Xanthocillin X permethyl ether
Others Neurological Disease

Xanthocillin X permethyl ether is a natural compound isolated from fungal extracts, with Aβ-42 lowering activity.
HY-103456

PHTPP
Estrogen Receptor/ERR Cancer

PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.

HY-N0001

(-)-Epicatechin (-)-Epicatechol; Epicatechin; epi-Catechin	COX Ferroptosis Endogenous Metabolite	Cancer Inflammation/Immunology
(-)-Epicatechin inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

HY-100935S

Cimaterol-D7	Adrenergic Receptor
Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC₅₀s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.

HY-N1431A

Tabersonine hydrochloride	Others	Inflammation/Immunology Neurological Disease
Tabersonine hydrochloride is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and is a potential therapeutic candidate for the treatment of ALI/ARDS.

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-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-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-16988A

SR9011 hydrochloride
Autophagy Cancer

SR9011 hydrochloride is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-A0070

Liothyronine sodium Triiodothyronine sodium; 3,3',5-Triiodo-L-thyronine sodium; T3 sodium	Thyroid Hormone Receptor	Cancer Endocrinology
Liothyronine sodium is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

HY-16989

SR9009
Autophagy Cancer

SR9009 is a REV-ERBα/β agonist with IC₅₀s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
HY-108013

Armillarisin A
Interleukin Related Inflammation/Immunology

Armillarisin A has the potential for the ulcerative colitis (UC) study. Armillarisin A increases IL-4 and lower IL-1β.
HY-16988

SR9011
Autophagy Cancer

SR9011 is a REV-ERBα/β agonist with IC₅₀s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.

HY-A0070A

Liothyronine Triiodothyronine; 3,3',5-Triiodo-L-thyronine; T3	Thyroid Hormone Receptor Endogenous Metabolite	Cancer Endocrinology
Liothyronine is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

HY-N1431

Tabersonine	Others	Inflammation/Immunology Neurological Disease
Tabersonine is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and acts as a potential therapeutic candidate for the treatment of ALI/ARDS.

HY-B0849

Azoxystrobin	Fungal Reactive Oxygen Species Apoptosis	Infection
Azoxystrobin is a broad-spectrum β-methoxyacrylate fungicide. Azoxystrobin inhibits mitochondrial respiration by binding to the Qo site of the cytochrome bc1 complex and inhibiting electron transfer. Azoxystrobin induces the production of reactive oxygen species (ROS) and induces cell apoptosis.

HY-135670

Glycosidase-IN-1	Others	Metabolic Disease
Glycosidase-IN-1 (Compound 9) is a glycosidase inhibitor synthesized from D-mannose. Glycosidase-IN-1 be used to synthesize some immunosuppressive agents and β-glucosidase inhibitors. Glycosidase-IN-1 has hypoglycemic activity.

HY-13815

KY02111	Wnt	Cardiovascular Disease
KY02111 is a canonical WNT signaling (β-catenin) inhibitor which promotes differentiation of hPSCs to cardiomyocytes. KY02111 can be used for the research of human cardiomyocyte regeneration.

HY-B1100

Estradiol (cypionate)	Estrogen Receptor/ERR	Endocrinology Cancer
Estradiol cypionate is a 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor IC50 value: Target: estrogen receptor Estradiol cypionate is a synthetic ester, is a estrogen.

HY-16786

AI-10-49
Others Cancer

AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.
HY-13469

Debio 0932
CUDC-305
HSP Cancer

Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC₅₀s of 100 and 103 nM for HSP90α and HSP90β, respectively.

HY-119109

Laminaran	Others	Cancer
Laminaran is a neutral water-soluble *β-1-3-glucan* and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.

HY-12302

Kenpaullone 9-Bromopaullone; NSC-664704	CDK GSK-3	Cancer
Kenpaullone is a potent inhibitor of CDK1/cyclin B and *GSK-3β, with IC₅₀s of 0.4 μM and 23 nM, and also inhibits* CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC₅₀s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.

HY-N0665

Specnuezhenide (8E)-Nuezhenide	NF-κB Wnt	Inflammation/Immunology
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and *wnt/β-catenin* signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).

HY-103238

RSVA405	AMPK STAT Autophagy	Metabolic Disease Inflammation/Immunology Neurological Disease
RSVA405 is a potent, orally active activator of AMPK, with an EC₅₀ of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.

HY-12383

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

HY-18054

BVT 2733	Others	Inflammation/Immunology
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC₅₀=96 nM) over the human enzyme (IC₅₀=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.

HY-50673

Dactolisib BEZ235; NVP-BEZ235	PI3K mTOR Autophagy	Cancer
Dactolisib (BEZ235) is a dual pan-class I PI3K and mTOR kinase inhibitor with IC₅₀s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for *p110α/p110γ/p110δ/p110β* and mTOR, respectively. Dactolisib (BEZ235) inhibits both *mTORC1* and mTORC2.

HY-13205

Belnacasan VX-765	Caspase	Inflammation/Immunology
Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with K_is of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC₅₀ of ~0.7 μM.

HY-B0436

Salbutamol hemisulfate Albuterol hemisulfate; AH-3365 hemisulfate	Adrenergic Receptor Autophagy	Inflammation/Immunology Endocrinology Cancer
Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting β2 adrenergic receptor agonist Target: β2 Adrenergic Receptor Salbutamol Hemisulfate (Albuterol hemisulfate) is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD.

HY-N0377

Liquiritigenin 4',7-Dihydroxyflavanone	Estrogen Receptor/ERR	Cancer Inflammation/Immunology Neurological Disease
Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC₅₀ of 36.5 nM for activation of the ERE tk-Luc.

HY-B1459

Dicloxacillin sodium	Bacterial Antibiotic	Infection
Dicloxacillin sodium is a narrow-spectrum β-lactam antibiotic of the penicillin family. Dicloxacillin sodium is active against β-lactamase-producing organisms such as Staphylococcus aureus.

HY-13520

Nocodazole Oncodazole; R17934	Microtubule/Tubulin Bcr-Abl CRISPR/Cas9 Autophagy Apoptosis	Cancer
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.

HY-B1035

Levobunolol hydrochloride
l-Bunolol hydrochloride
Others Others

Levobunolol hydrochloride is a non-selective beta blocker.
HY-B1392

Esmolol hydrochloride
Adrenergic Receptor Autophagy Mitophagy Cardiovascular Disease Endocrinology

Esmolol hydrochloride is a beta adrenergic receptor blocker.
HY-101658

Pargolol hydrochloride
Ko 1400 hydrochloride
Adrenergic Receptor Neurological Disease Endocrinology

Pargolol hydrochloride is a β adrenergic receptor antagonist.
HY-101817

Spirendolol
Li 32-468; S 32-468; Substance 32468
Adrenergic Receptor Neurological Disease Endocrinology

Spirendolol is a β adrenergic receptor antagonist.

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-112157

PF-06751979	Beta-secretase	Neurological Disease
PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC₅₀ of 7.3 nM in BACE1 binding assay.

HY-10402

Losmapimod GSK-AHAB; GW856553X; SB856553	p38 MAPK Autophagy	Inflammation/Immunology Cancer
Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pK_is of 8.1 and 7.6 for p38α and p38β, respectively.

HY-N2121

Neoisoliquiritigenin	Apoptosis	Cancer
Neoisoliquiritigenin, isolated from Spatholobus suberectus, inhibits cell proliferation and induces cell apoptosis in breast cancer by directly binding to GRP78 to regulate the β-catenin pathway.

HY-14838A

Etamicastat hydrochloride BIA 5-453 hydrochloride	Dopamine β-hydroxylase	Cardiovascular Disease
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible *dopamine-β-hydroxylase* (DBH) inhibitor with an IC₅₀ value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.

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-B0979

Lobeline hydrochloride α-Lobeline hydrochloride; L-Lobeline hydrochloride	nAChR	Neurological Disease
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.

HY-112331

SJ000291942	TGF-β Receptor	Cancer
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.

HY-14537

Latrepirdine dihydrochloride Dimebolin dihydrochloride	Amyloid-β Histamine Receptor Adrenergic Receptor 5-HT Receptor Autophagy	Neurological Disease Endocrinology
Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and *amyloid-β* (Aβ) secretion.

HY-N3514

Kuwanon E
Others Cancer

Kuwanon E is a flavonoid isolated from Morus alba, cytotoxic to human monocytic leukemic cell lines, and reduces the level of IL-1β.

HY-103207

Amibegron hydrochloride SR 58611A	Adrenergic Receptor	Neurological Disease Endocrinology
Amibegron hydrochloride is a selective *β3-adrenoceptor* agonist, with an EC₅₀ of 3.5 nM for *β-adrenoceptor* in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.

HY-129630

Tetrahydrocortisol	Endogenous Metabolite	Metabolic Disease
Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity.

HY-16708A

ZLN024 hydrochloride	AMPK	Metabolic Disease
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC₅₀s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.

HY-14933

Prinaberel ERB-041	Estrogen Receptor/ERR Wnt Apoptosis	Cancer
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC₅₀s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the *WNT/β-catenin* signaling pathway. Prinaberel induces ovarian cancer *apoptosis*.

HY-109052

Atabecestat JNJ-54861911	Beta-secretase	Neurological Disease
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.

HY-P0178A

LXW7 TFA	Integrin	Inflammation/Immunology
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC₅₀ of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.

HY-10472

LY2811376	Beta-secretase	Neurological Disease
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC₅₀ of 239 nM-249 nM, that acts to decrease Aβ secretion with EC₅₀ of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.

HY-122537A

Arotinolol	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to *5HT_1B*-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.

HY-10328

Neflamapimod VX-745	p38 MAPK Autophagy	Inflammation/Immunology
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC₅₀ for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.

HY-134130

Integrin modulator 1	Integrin	Inflammation/Immunology
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC₅₀ of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC₅₀ of 12.9 nM.

HY-17497A

Acebutolol hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Acebutolol hydrochloride is a β1 adrenergic receptor (β1AR) antagonist. Acebutolol hydrochloride is used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.

HY-102028

KY1220
Wnt β-catenin Cancer

KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC₅₀ of 2.1 μM in HEK293 reporter cells.

HY-14399

Itanapraced CHF5074; CSP-1103	γ-secretase	Neurological Disease
Itanapraced (CHF5074) is a novel γ-secretase modulator, reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM, respectively.

HY-121251

BI-167107	Adrenergic Receptor	Cancer Neurological Disease Endocrinology
BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant K_d of 84 pM.

HY-B0334

Sulbactam CP45899	Bacterial Antibiotic	Infection
Sulbactam (CP45899) is a competitive, irreversible *beta-lactamase* inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.

HY-13514

TG 100713
PI3K Cancer

TG 100713 is an inhibitor of PI3K, with IC₅₀s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.

HY-N0602

Ginsenoside Rg2 Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2	NF-κB Amyloid-β	Neurological Disease Cardiovascular Disease Cancer
Ginsenoside Rg2 is one of the major active components of ginseng. Ginsenoside Rg2 acts as a NF-κB inhibitor. Ginsenoside Rg2 also reduces Aβ_1-42 accumulation.

HY-13493

AC710
PDGFR c-Kit FLT3 Cancer

AC710 is a potent PDGFR inhibitor with K_ds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
HY-17044

Duvelisib
IPI-145; INK1197
PI3K Cancer

Duvelisib is a selectivite p100δ inhibitor with IC₅₀ of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
HY-15190

NVP-HSP990
HSP-990
HSP Apoptosis Cancer

NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC₅₀ values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.

HY-14175

Begacestat GSI-953	γ-secretase	Neurological Disease
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC₅₀Aβ₄₀=15 nM) for the treatment of Alzheimer's disease.

HY-11035

WAY-262611	β-catenin	Cancer
WAY-262611 is a wingless *β-Catenin* agonist that increases bone formation rate with an EC₅₀ of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a *Dkk1* inhibitor.

HY-12113

Oprozomib ONX 0912; PR-047	Proteasome Autophagy	Cancer
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.

HY-N1949

Homoplantaginin	TNF Receptor NF-κB	Inflammation/Immunology
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

HY-B0334A

Sulbactam sodium CP45899 sodium	Bacterial Antibiotic	Infection
Sulbactam (CP45899) sodium is a competitive, irreversible *beta-lactamase* inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.

HY-18179

AZD2932
PDGFR VEGFR FLT3 c-Kit Cancer

AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC₅₀s of 8, 4, 7 and 9 nM in cell assay, respectively.
HY-101752

(±)-Befunolol
Adrenergic Receptor Cardiovascular Disease Endocrinology

(±)-Befunolol is a β-adrenoceptor blocking agent.
HY-U00016

Teoprolol
Adrenergic Receptor Endocrinology

Teoprolol is a β-adrenergic receptor blocker.
HY-100141

Ancarolol
Adrenergic Receptor Cardiovascular Disease Endocrinology

Ancarolol is a beta-adrenergic blocking agent.

HY-10320

Doramapimod BIRB 796	p38 MAPK Raf Autophagy	Inflammation/Immunology Cancer
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC₅₀ for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (K_d=0.1 nM). Doramapimod also inhibits B-Raf with an IC₅₀ of 83 nM.

HY-N0012

Glycitin Glycitein 7-O-β-glucoside	Influenza Virus Bacterial	Cancer Infection
Glycitin is a natural isoflavone isolated from legumes; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.Glycitin is antibacterial, antiviral and estrogenic.

HY-N0203

Atractylenolide III ICodonolactone; 8β-Hydroxyasterolide	Apoptosis	Cancer
Atractylenolide III is a major component of Atractylodes rhizome can induce apoptosis of the lung carcinoma cells.

HY-N0176

Dihydroartemisinin
Dihydroqinghaosu; β-Dihydroartemisinin; Artenimol
Parasite NF-κB Autophagy Apoptosis Cancer Infection

Dihydroartemisinin is a potent anti-malaria agent.

HY-N0610A

Cinnamic acid 3-Phenylacrylic acid; β-Phenylacrylic acid	Endogenous Metabolite	Cancer
Cinnamic acid has potential use in cancer intervention, with IC₅₀s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.

HY-15174

Dactolisib Tosylate BEZ235 Tosylate; NVP-BEZ 235 Tosylate	PI3K mTOR Autophagy	Cancer
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC₅₀ values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits *mTORC1* and mTORC2.

HY-108470

Ro5-3335	Others	Cancer
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.

HY-12046

PIK-93	PI4K PI3K Virus Protease	Cancer
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC₅₀ of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC₅₀ of 16 nM and 39 nM, respectively.

HY-B0976

Fenoterol Th-1165; Phenoterol	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Fenoterol (Th-1165) is a β2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.

HY-B1486

Oxprenolol hydrochloride Ba 39089	Adrenergic Receptor	Cardiovascular Disease
Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable *β-adrenergic* receptor (β-AR) antagonist with a K_i of 7.10 nM in a radioligand binding assay using rat heart muscle.

HY-B0976A

Fenoterol hydrobromide Fenoterol bromide; Th-1165a; Phenoterol hydrobromide	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Fenoterol hydrobromide (Fenoterol bromide) is a β2 adrenergic agonist designed to open up the airways to the lungs, is classed as sympathomimetic β2 agonist and asthma medication.

HY-18295

Erteberel LY500307	Estrogen Receptor/ERR	Neurological Disease
Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with K_i and EC₅₀ of 1.54 nM and 3.61 nM, respectively. Anti-tumor activities.

HY-10232

THIP Gaboxadol	GABA Receptor	Neurological Disease
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.

HY-117482

BPN-15606	γ-secretase	Neurological Disease
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC₅₀ values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.

HY-15356

BIO-acetoxime BIA	GSK-3 Apoptosis HSV	Infection Inflammation/Immunology Neurological Disease
BIO-acetoxime (BIA) is a potent and selective GSK-3 inhibitor, with IC₅₀s of both 10 nM for GSK-3α/β. BIO-acetoxime has anticonvulsant and anti-infection activity.

HY-10342

Enzastaurin LY317615	PKC Autophagy Apoptosis	Cancer
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC₅₀ of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.

HY-15897

LDN-212854	TGF-β Receptor	Cancer
LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.

HY-103021

LY3200882	TGF-β Receptor	Cancer Inflammation/Immunology
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC₅₀ of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.

HY-N0158

Oxymatrine	TGF-beta/Smad Influenza Virus	Cancer Infection Inflammation/Immunology
Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and *TGF-β/Smad* pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.

HY-105272A

Loreclezole hydrochloride R 72063 hydrochloride	GABA Receptor	Neurological Disease
Loreclezole hydrochloride, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

HY-B1270

Isoxsuprine hydrochloride	Adrenergic Receptor iGluR	Neurological Disease Endocrinology
Isoxsuprine hydrochloride is a beta-adrenergic receptor agonist with K_is of 13.65 μΜ and 3.48 μΜ for myometrial and placcntal beta-adrenergic receptor, respectively. Isoxsuprine hydrochloride is also a NMDA receptor antagonist.

HY-105272

Loreclezole R 72063	GABA Receptor	Neurological Disease
Loreclezole, an antiepileptic compound, is a selective GABA_A receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.

HY-111413A

c(phg-isoDGR-(NMe)k) TFA
Integrin Cancer

c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC₅₀ of 2.9 nM.

HY-N7204

4-Hydroxyderricin	Monoamine Oxidase Dopamine β-hydroxylase	Neurological Disease
4-Hydroxyderricin, the major active ingredients of Angelica keiskei Koidzumi, is a potent selective MAO-B (Monoamine oxidase inhibitors) inhibitor with an IC₅₀ of 3.43 μM. 4-Hydroxyderricin also mildly inhibits DBH (dopamine β-hydroxylase) activity. 4-Hydroxyderricin has antidepressant activity.

HY-W015445

SD-169	p38 MAPK	Metabolic Disease
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC₅₀ of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC₅₀ of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.

HY-U00205

Dopexamine hydrochloride
FPL60278AR
Adrenergic Receptor Cardiovascular Disease Endocrinology

Dopexamine hydrochloride is a β2 adrenergic receptor agonist.
HY-113404

DL-Dopa
Endogenous Metabolite Others

DL-Dopa is a beta-hydroxylated derivative of phenylalanine.
HY-B1286

Piperacillin sodium
Sodium piperacillin
Bacterial Antibiotic Infection

Piperacillin sodium is a broad-spectrum β-lactam antibiotic.
HY-B1463

Penicillin G sodium salt
Benzylpenicillin sodium salt
Bacterial Antibiotic Infection

Penicillin G sodium salt is a typical β-lactam antibiotic.
HY-U00066

Cicloprolol hydrochloride
Adrenergic Receptor Cardiovascular Disease Endocrinology

Cicloprolol is a partial β 1-adrenoceptor agonist .
HY-101691

Ecastolol
Adrenergic Receptor Cardiovascular Disease Endocrinology

Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.

HY-100634

4-Hydroxypropranolol hydrochloride (±)-4-hydroxy Propranolol hydrochloride	Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA₂ values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.

HY-107589A

BIO5192 hydrate	Integrin	Inflammation/Immunology
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (K_d<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC₅₀=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

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-N0815

Resibufogenin Bufogenin; Recibufogenin	Others	Cancer
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.

HY-116446

Pironetin	Microtubule/Tubulin	Cancer
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.

HY-10517

Orantinib SU6668; TSU-68	PDGFR FGFR VEGFR Apoptosis	Cancer
Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with K_is of 2.1 μM, 8 nM and 1.2 μM for *Flt-1, PDGFRβ* and *FGFR1*, respectively.

HY-10065

Axitinib AG-013736	VEGFR PDGFR	Cancer
Axitinib is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 0.1, 0.2, 0.1-0.3, 1.6 nM for *VEGFR1, VEGFR2, VEGFR3* and PDGFRβ, respectively.

HY-P0318

Hemorphin-7	Opioid Receptor Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Hemorphin-7 is a hemorphin peptide, an endogenous opioid peptide derived from the β-chain of hemoglobin. Hemorphin peptides exhibits antinociceptive and antihypertensive activities, activating opioid receptors and inhibiting angiotensin-converting enzyme (ACE).

HY-N0250

Saikosaponin D	STAT NF-κB Estrogen Receptor/ERR Bacterial	Cancer Infection Inflammation/Immunology
Saikosaponin D is a triterpene saponin isolated from Bupleurum, with anti-inflammatory, anti-bacterial, anti-tumor, and anti-allergic activities; Saikosaponin D inhibits selectin, STAT3 and NF-kB and activates estrogen receptor-β.

HY-17406

Tolcapone Ro 40-7592	COMT Amyloid-β	Neurological Disease
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.

HY-B0422

Nateglinide A4166; Senaglinide	Potassium Channel Dipeptidyl Peptidase	Metabolic Disease
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K⁺ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.

HY-15244

Alpelisib BYL-719	PI3K	Cancer
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC₅₀s of 5/250/290/1200 nM, respectively. Antineoplastic activity.

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-16268

Kartogenin KGN	TGF-beta/Smad	Inflammation/Immunology
Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC₅₀ of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).

HY-112769

EX229	AMPK	Metabolic Disease
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with K_ds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.

HY-N0044

Ginsenoside Re Ginsenoside B2; Panaxoside Re; Sanchinoside Re	Amyloid-β NF-κB JNK Endogenous Metabolite	Inflammation/Immunology Neurological Disease Cancer
Ginsenoside Re (Ginsenoside B2) is an extract from Panax notoginseng. Ginsenoside Re decreases the *β-amyloid* protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.

HY-B0977

Dicloxacillin Sodium hydrate Dicloxacillin sodium salt monohydrate	Bacterial Antibiotic	Infection
Dicloxacillin Sodium hydrate (Dicloxacillin sodium salt monohydrate) is a narrow-spectrum β-Lactam antibiotic of the penicillin class, is used to treat infections caused by susceptible Gram-positive bacteria, active against beta-lactamase-producing organisms such as Staphylococcus aureus.

HY-15473

MLN120B ML120B	IKK	Cancer
MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC₅₀ of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.

HY-12903

Macozinone PBTZ169	Bacterial	Infection
Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent *DprE1* (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect.

HY-16316

Metipranolol hydrochloride
Adrenergic Receptor Cardiovascular Disease Endocrinology

Metipranolol hydrochloride is a non-selective β adrenergic receptor blocking agent.
HY-101585

Imoxiterol
RP 58802B
Adrenergic Receptor Neurological Disease Endocrinology

Imoxiterol (RP 58802B) is a β-adrenergic agonist.

HY-10408

Ki20227	c-Fms VEGFR c-Kit PDGFR	Inflammation/Immunology
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC₅₀s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.

HY-N0619

Mulberroside A	TNF Receptor Interleukin Related Tyrosinase	Inflammation/Immunology
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, *IL-1β, and IL-6* and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM.

HY-13598

Valecobulin CKD-516	Microtubule/Tubulin	Cancer
Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.

HY-N2998

Ganoderenic acid A	Others	Metabolic Disease
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of *β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury.*

HY-50698

BI 2536	Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis	Cancer
BI 2536 is a dual *PLK1* and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.

HY-19369

L-685458 L-685,458	γ-secretase Apoptosis	Neurological Disease Cancer
L-685458 is a potent inhibitor of Amyloid β-Protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested.

HY-13223

Crenolanib CP-868596	FLT3 PDGFR Autophagy	Cancer
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with K_ds of 0.74 nM and 2.1 nM/3.2 nM, respectively.

HY-N0020

Echinacoside	Wnt Reactive Oxygen Species	Neurological Disease
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.

HY-P1060

LPYFD-NH2	Amyloid-β	Neurological Disease
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.

HY-B1276A

Metaproterenol Orciprenaline	Adrenergic Receptor	Inflammation/Immunology Cardiovascular Disease Endocrinology
Metaproterenol (Orciprenaline) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC₅₀ of 68 nM. Metaproterenol also has anti-inflammatory activity.

HY-100370

MRK-016	GABA Receptor	Cancer
MRK-016 is a selective, orally bioavailable inverse agonist of GABA_A α5 receptor, with an EC₅₀ of 3 nM for GABA_A α5, and K_is of 0.83, 0.85, 0.77 and 1.4 nM for human GABA_A α1β3γ2, GABA_A α2β3γ2, GABA_A α3β3γ2, and GABA_A α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.

HY-12762

QS11	Others	Cancer
QS11 is an inhibitor of *ARFGAP1* (ADP-ribosylation factor GTPase-activating protein 1), with an EC₅₀ of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.

HY-15597

Salinomycin Procoxacin	Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic	Cancer
Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of *Wnt/β-catenin* signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.

HY-111383

LX2343	Beta-secretase PI3K Amyloid-β Autophagy	Neurological Disease
LX2343 is a *BACE1* enzyme inhibitor with an IC₅₀ value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC₅₀ of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.

HY-12009

Pazopanib Hydrochloride GW786034 (Hydrochloride)	PDGFR VEGFR FGFR c-Kit c-Fms Autophagy	Cancer
Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of *VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms* with an IC₅₀ of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

HY-B1238

Pronethalol (±)-Pronethalo	Adrenergic Receptor	Neurological Disease Cardiovascular Disease
Pronethalol ((±)-Pronethalo) is a non-selective *β-adrenergic* antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).

HY-10337

Brivanib BMS-540215	VEGFR Autophagy	Cancer
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC₅₀ of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.

HY-50094

Pictilisib GDC-0941	PI3K Autophagy Apoptosis	Cancer
Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

HY-B1238A

Pronethalol hydrochloride (±)-Pronethalo hydrochloride	Adrenergic Receptor	Neurological Disease Cardiovascular Disease
Pronethalol ((±)-Pronethalo) is a non-selective *β-adrenergic* antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs).

HY-12036

GSK1059615
PI3K mTOR Apoptosis Cancer

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC₅₀ of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

HY-N0439

Asiaticoside	TGF-beta/Smad Reactive Oxygen Species Apoptosis Endogenous Metabolite	Inflammation/Immunology Neurological Disease Cardiovascular Disease Cancer
Asiaticoside, a trisaccaride triterpene from Centella asiatica, suppresses *TGF-β/Smad* signaling through inducing Smad7 and inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties.

HY-19744

T6167923	MyD88	Inflammation/Immunology
T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an ₅₀ of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.

HY-111386

E-7386
Epigenetic Reader Domain Cancer

E-7386 is an orally active CBP/beta-catenin modulator.
HY-33353

GSK-4716
Estrogen Receptor/ERR Cancer

GSK-4716 is a selective ERRβ/γ agonist.
HY-B0925

Oxacillin sodium salt
Bacterial Antibiotic Infection

Oxacillin sodium salt is a narrow-spectrum β-lactam antibiotic of the penicillin class.
HY-B0467

Amoxicillin sodium
Amoxycillin sodium
Bacterial Antibiotic Infection

Amoxicillin sodium (Amoxycillin sodium) is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.
HY-U00293

ZK-90055 hydrochloride
Adrenergic Receptor Inflammation/Immunology Endocrinology

ZK-90055 hydrochloride is a β2 adrenergic receptor agonist.

HY-131145

Brombuterol hydrochloride Bromobuterol hydrochloride	Adrenergic Receptor	Inflammation/Immunology
Brombuterol hydrochloride (Bromobuterol hydrochloride) is a β-adrenergic receptor agonist.

HY-101604

Atrimustine
Bestrabucil; KM2210
Others Cancer

Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.
HY-U00019

Pamatolol
Adrenergic Receptor Cardiovascular Disease Endocrinology

Pamatolol is a cardioselective beta-adrenoceptor antagonist without sympathomimetic activity.

HY-136866

Aβ42-IN-2	γ-secretase	Neurological Disease
Aβ42-IN-2 is a γ-secretase modulators extracted from patent WO2016070107, compound example 36. Aβ42-IN-2 has an IC₅₀ of 6.5 nM for Αβ₄₂. Aβ42-IN-2 can be used for the research of a disorder associated with aberrant A3 peptide levels, including Alzheimer's disease.

HY-B0449

Methacycline hydrochloride	Bacterial Antibiotic	Infection
Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.

HY-P1060A

LPYFD-NH2 TFA	Amyloid-β	Neurological Disease
LPYFD-NH2 TFA, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 TFA can be used for the research of Alzheimer’s disease.

HY-130778

N,N'-Diacetylchitobiose	Others	Others
N,N'-Diacetylchitobiose is a dimer of β(1,4) linked N-acetyl-D glucosamine. N,N'-Diacetylchitobiose is the hydrolysate of chitin and can be used as alternative carbon source by E. coli.

HY-B1264

Celiprolol hydrochloride	Adrenergic Receptor	Cardiovascular Disease
Celiprolol hydrochloride is a potent, selective and orally active antagonist of *β1-andrenoceptor* with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.

HY-B0982

Pindolol LB-46	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).

HY-U00278

Deloxolone (3β,20β)-3-(3-Carboxy-1-oxopropoxy)olean-9(11)-en-29-oic acid	Others	Inflammation/Immunology
Deloxolone has the potential for inflammatory, ischemic and proliferative diseases treatment.

HY-135391S

Ezetimibe phenoxy glucuronide-D4 Ezetimibe glucuronide-D4; Ezetimibe β-D-glucuronide-D4	Others	Metabolic Disease
Ezetimibe phenoxy glucuronide-D4 (Ezetimibe glucuronide-D4) is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.

HY-N6964

*Quercetin 3-O-β-D-(6''-p-coumaroyl)glucopyranosyl(1→2)-α-L-rhamnopyranoside* Quercetin-3-O-[2-O-(6-O-p-hydroxyl-E-coumaroyl)-D-glucosyl]-(1→2)-L-rhamnoside	Others	Metabolic Disease
Quercetin 3-O-β-D-(6''-p-coumaroyl)glucopyranosyl(1→2)-α-L-rhamnopyranoside (Quercetin-3-O-[2-O-(6-O-p-hydroxyl-E-coumaroyl)-D-glucosyl]-(1→2)-L-rhamnoside) is one of the major antioxidants of Ginkgo biloba leaves.

HY-15506

TAK-593	PDGFR VEGFR	Cancer
TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC₅₀s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

HY-16759

Verubecestat MK-8931	Beta-secretase	Neurological Disease
Verubecestat (MK-8931) is an orally active, high-affinity *BACE1* and BACE2 inhibitor with K_i values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.

HY-12033

2-Methoxyestradiol 2-ME2; NSC-659853	Apoptosis Microtubule/Tubulin Autophagy Endogenous Metabolite	Cancer
2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules.

HY-13049

Cediranib maleate AZD-2171 maleate	VEGFR Autophagy PDGFR	Cancer
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

HY-N2319

Dihydroergocristine mesylate DHEC mesylate	Amyloid-β	Neurological Disease
Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease *amyloid-β* peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (K_d) of 25.7 nM and 9.8 μM, respectively.

HY-N0197

Baicalin Baicalein 7-O-β-D-glucuronide	NF-κB Autophagy HIV	Inflammation/Immunology Cancer
Baicalin is a flavonoid glycoside isolated from Scutellaria baicalensis. Baicalin reduces the expression of NF-κB.

HY-B0172

Lithocholic acid 3α-Hydroxy-5β-cholanic acid	Autophagy Endogenous Metabolite Apoptosis	Metabolic Disease
Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity.

HY-N0419

Quercimeritrin
Quercetin-7-O-β-D-glucopyranoside
Others Metabolic Disease

Quercimeritrin, isolated from the leaves of Ixeridium dentatum, exhibits significant amylase activity.

HY-P1106

K41498	CRFR	Cardiovascular Disease
K41498 is a potent and highly selective CRF2 receptor antagonist with K_i values of 0.66 nM, 0.62 nM and 425 nM for human CRF_2α, CRF_2β and CRF₁ receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF_2α- and hCRF_2β-expressing cells. K41498 can be used for hypotension study.

HY-114263

NXT629	PPAR	Cancer
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC₅₀ of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC₅₀s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.

HY-13521

SB-505124	TGF-β Receptor	Cancer
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC₅₀s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

HY-108847

Etanercept	TNF Receptor	Inflammation/Immunology
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.

HY-16018

Ilorasertib ABT-348	Aurora Kinase VEGFR PDGFR RET	Cancer
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC₅₀s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib also suppresses RET tyrosine kinase, PDGFRβ and *Flt1* with IC₅₀s of 7 nM, 3 nM and 32 nM, respectively.

HY-107411

Bromoenol lactone (6E)-Bromoenol lactone	Phospholipase	Inflammation/Immunology
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A₂ (iPLA₂β) with an IC₅₀ value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca²⁺ influx.

HY-B1276

Metaproterenol hemisulfate Orciprenaline hemisulfate	Adrenergic Receptor	Inflammation/Immunology Cardiovascular Disease Endocrinology
Metaproterenol hemisulfate (Orciprenaline hemisulfate) is a direct-acting sympathomimetic and a β2-adrenergic receptor (β2AR) agonist with an IC₅₀ of 68 nM. Metaproterenol hemisulfate also has anti-inflammatory activity.

HY-117516

SR10067	Others	Neurological Disease
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC₅₀ values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.

HY-10912

Fexaramine	FXR Autophagy	Others
Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.

HY-107688A

UB-165 fumarate	nAChR	Neurological Disease
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a K_i value of 0.27 nM for nicotine binding in rat brain.

HY-117937

BC-1215	Ligand for E3 Ligase	Inflammation/Immunology
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC₅₀=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF^Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.

HY-14299

Indacaterol
Adrenergic Receptor Neurological Disease Endocrinology

Indacaterol(Onbrez; Arcapta) is an ultra-long-acting β-adrenoceptor agonist.

HY-100583

(-)-(S)-Equol	Estrogen Receptor/ERR Endogenous Metabolite	Cancer Metabolic Disease Neurological Disease
(-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a K_i of 0.73 nM.

HY-14299A

Indacaterol maleate
QAB149
Adrenergic Receptor Endocrinology

Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
HY-19737A

DG172 dihydrochloride
PPAR Cancer

DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC₅₀ of 27 nM.
HY-100699

Clenproperol
Adrenergic Receptor Endocrinology

Clenproperol is a β2-adrenergic agonist.
HY-13588

Cefsulodin sodium
Bacterial Antibiotic Infection

Cefsulodin sodium salt hydrate is a third generation β lactam antibiotic and member of the cephems subgroub of antibiotics.

HY-B0076

(±)-Bisoprolol hemifumarate Bisoprolol hemifumarate salt	Adrenergic Receptor	Inflammation/Immunology Endocrinology
(±)-Bisoprolol (hemifumarate) is a selective type β1 adrenergic receptor blocker.

HY-17503B

Metoprolol Tartrate
Adrenergic Receptor Cardiovascular Disease Endocrinology

Metoprolol is a cardioselective β1-adrenergic blocking agent.

HY-U00386

Bometolol Hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Bometolol Hydrochloride is a *beta-adrenergic* blocking agent, used for the research of cardiovascular disease.

HY-101973

XL041
BMS-852927
LXR Cardiovascular Disease

XL041 (BMS-852927) is an LXRβ-selective agonist.

HY-10205

Cediranib AZD2171	VEGFR Autophagy PDGFR	Cancer
Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC₅₀s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

HY-10208

Pazopanib GW786034	VEGFR c-Kit PDGFR Autophagy FGFR	Cancer
Pazopanib (GW786034) is a novel multi-target inhibitor of *VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms* with IC₅₀s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.

HY-N6679A

10,11-Dehydrocurvularin	HSP TGF-beta/Smad	Cancer Infection
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.

HY-20180

Pictilisib dimethanesulfonate GDC-0941 dimethanesulfonate; GDC-0941 2 MeSO3H salt	PI3K Autophagy Apoptosis	Cancer
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC₅₀ of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

HY-16782

Pexmetinib ARRY-614	p38 MAPK Autophagy	Cancer
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

HY-P1269

α-Conotoxin AuIB	nAChR	Neurological Disease
α-Conotoxin AuIB, a potent and selective *α3β4* nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC₅₀ of 0.75 μM.

HY-110160

Pozanicline dihydrochloride ABT-089 dihydrochloride	nAChR	Neurological Disease
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a K_i of 16.7 nM for binding to [³H]cytisine sites. Pozanicline is an *α4β2*-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a K_i of 17 nM while binding to α7 nAChR is insignificant.

HY-107436

LE135	RAR/RXR TRP Channel	Cancer Neurological Disease
LE135 is a potent RAR antagonist that binds selectively to RARα (K_i of 1.4 μM) and RARβ (K_i of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent *TRPV1* and TRPA1 receptors activator with EC₅₀s of 2.5 μM and 20 μM, respectively.

HY-18676

OSU-T315	Integrin Autophagy Apoptosis	Cancer
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC₅₀ of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and *autophagy*.

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-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-101355B

CGP 20712 A CGP 20712 mesylate	Adrenergic Receptor	Cardiovascular Disease
CGP 20712 A (CGP 20712 mesylate) is a highly selective *β1-adrenoceptor* antagonist with an IC₅₀ of 0.7 nM. CGP 20712 A exhibits ~10,000-fold selectivity over β2-adrenoceptors.

HY-12560A

PNU-282987	nAChR	Neurological Disease
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).

HY-P1269A

α-Conotoxin AuIB TFA	nAChR	Neurological Disease
α-Conotoxin AuIB TFA, a potent and selective *α3β4* nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC₅₀ of 0.75 μM.

HY-19798

PI4KIIIbeta-IN-9	PI4K PI3K	Cancer
PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC₅₀ of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC₅₀s of 152 nM and 1046 nM, respectively.

HY-B0006A

Carvedilol phosphate hemihydrate BM 14190 phosphate hemihydrate	Adrenergic Receptor Autophagy	Cancer Inflammation/Immunology Cardiovascular Disease
Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective *β/α-1* blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC₅₀ of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.

HY-10330

Toceranib SU11654; PHA 291639E	PDGFR VEGFR c-Kit	Cancer
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with K_is of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.

HY-112700

SHIP2-IN-1	Phosphatase	Neurological Disease
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC₅₀ of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.

HY-B0422S

Nateglinide D5 A4166 D5; Senaglinide D5	Potassium Channel Dipeptidyl Peptidase	Metabolic Disease
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K⁺ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.

HY-10330A

Toceranib phosphate SU11654 phosphate; PHA 291639E phosphate	PDGFR VEGFR c-Kit	Cancer
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with K_is of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .

HY-13598A

Valecobulin hydrochloride CKD-516 hydrochloride	Microtubule/Tubulin	Cancer
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.

HY-50937

ST 2825	MyD88	Inflammation/Immunology
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.

HY-108966

Kushenol C	Beta-secretase	Inflammation/Immunology
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC₅₀ of 5.45 µM.

HY-101457

JZP-430	MAGL	Metabolic Disease
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC₅₀ of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).

HY-B0467B

Amoxicillin trihydrate
Amoxycillin trihydrate
Bacterial Antibiotic Infection

Amoxicillin trihydrate (Amoxycillin trihydrate) is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.

HY-17495A

Carteolol hydrochloride OPC-1085 hydrochloride	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Carteolol hydrochloride (OPC-1085 hydrochloride) is a non-selective beta blocker used to treat glaucoma.

HY-101804

(E)-Alprenoxime
CDDD-1815
Others Cardiovascular Disease

(E)-Alprenoxime is the isomer of the Alprenoxime. Alprenoxime is a site-activated ocular β-blocker.
HY-101721

Ko-3290
Adrenergic Receptor Cardiovascular Disease Endocrinology

Ko-3290 is an antagonist of β-adrenoceptor, with cardioselectivity and antilipolytic effects in animals.
HY-U00283

Falintolol, (Z)-
Adrenergic Receptor Endocrinology

Falintolol, (Z)-, a new β-adrenergic antagonist, is characterized by the presence of an oxime function.
HY-136435

Mapenterol hydrochloride
Adrenergic Receptor Endocrinology

Mapenterol hydrochloride is a type of β2-adrenoceptor agonist.
HY-10004

Faropenem daloxate
Faropenem medoxil
Bacterial Antibiotic Infection

Faropenem daloxate is the first oral penem in a new class of beta-lactam antibiotics.
HY-113201

Tetradecanoylcarnitine
Endogenous Metabolite Metabolic Disease

Tetradecanoylcarnitine is a human carnitine involved in β-oxidation of long-chain fatty acids.

HY-17498

Atenolol (RS)-Atenolol	Adrenergic Receptor	Neurological Disease Endocrinology
Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a K_i of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.

HY-103040

Zuranolone	GABA Receptor	Neurological Disease
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABA_A receptor, with EC₅₀s of 296 and 163 nM for *α₁β₂γ₂* and α₄β₃δ GABA_A receptors, respectively.

HY-N0506

Rosarin	Others	Neurological Disease
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .

HY-P1106A

K41498 TFA	CFTR	Cardiovascular Disease
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with K_i values of 0.66 nM, 0.62 nM and 425 nM for human CRF_2α, CRF_2β and CRF₁ receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF_2α- and hCRF_2β-expressing cells. K41498 TFA can be used for hypotension study.

HY-100634S

4-Hydroxypropranolol D7 hydrochloride (±)-4-hydroxy Propranolol D7 hydrochloride	Adrenergic Receptor	Neurological Disease
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA₂ values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.

HY-N0060B

(E)-Ferulic acid (E)-Coniferic acid	β-catenin Bcl-2 Family Ferroptosis Endogenous Metabolite	Cancer
(E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of *β-catenin* and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.

HY-N0619A

cis-Mulberroside A Mulberroside D	TNF Receptor Interleukin Related Tyrosinase	Inflammation/Immunology
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, *IL-1β, and IL-6* and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC₅₀ of 53.6 μM.

HY-N0651

Spinosin	Others	Neurological Disease
Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ_1-42 production and aggregation via activating Nrf2/HO-1 pathway.

HY-124607

(R)-BRD3731	GSK-3	Neurological Disease
(R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC₅₀s of 1.05 and 6.7 μM for *GSK3β* and GSK3α, respectively.

HY-N3413

Kushenol X	Others	Metabolic Disease
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent *β-glucuronidase* and human carboxylesterase 2 (hCE2) inhibitor with IC₅₀s of 2.07 μM and 3.05 μM, respectively.

HY-N2625A

Harmalol hydrochloride	Others	Others
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.

HY-107661

Arundic Acid ONO-2506; (R)-2-Propyloctanoic acid	Others	Neurological Disease
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.

HY-13894

Tyrphostin AG1296 AG1296	PDGFR c-Kit FLT3 Apoptosis	Cancer Inflammation/Immunology Cardiovascular Disease
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC₅₀ of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and *β-receptors* as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC₅₀ in the micromolar range.

HY-14773

Mirabegron
YM178
Adrenergic Receptor Neurological Disease Endocrinology

Mirabegron is a selective β₃-adrenoceptor agonist with EC₅₀ of 22.4 nM.
HY-Y0932

Isophorone
Others Others

Isophorone, an α,β-unsaturated cyclic ketone, is used as a precursor to polymers.

HY-B1108

Labetalol hydrochloride AH-5158 hydrochloride; Sch-15719W	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Labetalol hydrochloride is a mixed alpha/beta adrenergic antagonist that is used to treat high blood pressure.

HY-101489

GZD856	PDGFR Bcr-Abl Apoptosis	Cancer
GZD856 is a potent and orally bioavailable PDGFRα/β inhibitor with IC₅₀s of 68.6 and 136.6 nM, respectively.GZD856 is also a Bcr-Abl^T315I inhibitor with IC₅₀s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant. Antitumor activity.

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-77251

TAK1/MAP4K2 inhibitor 1	MAP4K MAP3K	Cancer
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC₅₀s of 41.1 nM and 18.2 nM, respectively.

HY-B0006

Carvedilol BM 14190	Adrenergic Receptor Autophagy	Cancer Inflammation/Immunology Cardiovascular Disease
Carvedilol (BM 14190) is a non-selective *β/α-1* blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC₅₀ of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.

HY-17406S

Tolcapone D7 Ro 40-7592 D7	COMT Amyloid-β	Neurological Disease
Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.

HY-108264

TCS 21311 NIBR3049	JAK PKC GSK-3	Cancer
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC₅₀ of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and *GSK3β* with IC₅₀s of 13, 68, and 3 nM, respectively.

HY-128773A

MRL-494 hydrochloride	Bacterial	Infection
MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for *Staphylococcus aureus* COL) and Gram-negative (MIC of 25 μM for *E. coli* JCM158) *bacterias*.

HY-P1119

WRW4	Others	Neurological Disease
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC₅₀ of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.

HY-16361A

Omigapil maleate CGP3466B maleate	Apoptosis	Metabolic Disease Neurological Disease
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ_1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD).

HY-129029

Bisoprolol	Adrenergic Receptor	Cardiovascular Disease
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.

HY-16579

Etifoxine hydrochloride HOE 36-801 hydrochloride	GABA Receptor	Neurological Disease
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA_A receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.

HY-P0295

Gly-Arg-Gly-Asp-Ser	Integrin	Others
Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC₅₀ of ∼5 and ∼6.5 μM

HY-100689

Propyl pyrazole triol PPT	Estrogen Receptor/ERR	Cancer
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).

HY-16579A

Etifoxine HOE 36-801	GABA Receptor	Neurological Disease
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABA_A receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.

HY-113402A

Gamma-glutamylcysteine TFA γ-glutamylcysteine TFA	Interleukin Related TNF Receptor	Inflammation/Immunology
Gamma-glutamylcysteine (TFA) ((γ-glutamylcysteine (TFA)), an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine (TFA) also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and *IL-1β) and attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.*

HY-70063

Buparlisib BKM120; NVP-BKM120	PI3K Apoptosis	Cancer
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC₅₀s of 52, 166, 116 and 262 nM for p110α, *p110β, p110δ* and p110γ, respectively.

HY-10432A

A 83-01 sodium salt	TGF-β Receptor ALK	Cancer
A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC₅₀s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.

HY-13308

Regorafenib Hydrochloride BAY 73-4506 hydrochloride	VEGFR Autophagy PDGFR Raf RET	Cancer
Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for *VEGFR1/2/3, PDGFRβ, Kit, RET* and *Raf-1* with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-N0366

Sennoside B	PDGFR	Cancer
Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.

HY-10331A

Regorafenib monohydrate BAY 73-4506 monohydrate	VEGFR Autophagy PDGFR Raf RET	Cancer
Regorafenib monohydrate (BAY 73-4506 monohydrate) is a multi-target inhibitor for *VEGFR1/2/3, PDGFRβ, Kit, RET* and *Raf-1* with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-N2491

Deoxyelephantopin	NF-κB	Cancer
Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and *β-catenin* signaling.

HY-103254

ML221	Others	Neurological Disease
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC₈₀ of 10 nM in both assays.

HY-117541

Glycyl-glutamine Glycyl-L-glutamine	Others	Neurological Disease
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of *β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems.* Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).

HY-B0381A

Betaxolol hydrochloride SL75212	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.

HY-14533

K 01-162
K162
Amyloid-β Neurological Disease

K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM.
HY-19334

L755507
Adrenergic Receptor CRISPR/Cas9 Cancer Endocrinology

L755507 is a potent, selective agonist of β₃-AR with an IC₅₀ of 35 nM.
HY-N2146

Combretastatin A4
CRC 87-09
Microtubule/Tubulin Cancer

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM.

HY-B0381

Betaxolol	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Betaxolol is a selective beta1 adrenergic receptor blocker that can be used for the research of hypertension and glaucoma.

HY-10182B

CHIR-99021 trihydrochloride CT99021 trihydrochloride	GSK-3 Wnt β-catenin Autophagy	Cancer
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective *GSK-3α/β* inhibitor with IC₅₀s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent *Wnt/β-catenin* signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces *autophagy*.

HY-108359

Alsterpaullone 9-Nitropaullone; NSC 705701	CDK GSK-3	Cancer
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC₅₀s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to *GSK-3alpha/GSK-3beta* with IC₅₀s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders.

HY-10182

CHIR-99021 CT99021	GSK-3 Wnt β-catenin Autophagy	Cancer
CHIR-99021 (CT99021) is a potent and selective *GSK-3α/β* inhibitor with IC₅₀s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent *Wnt/β-catenin* signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces *autophagy*.

HY-N7676

Marein	AMPK HDAC	Metabolic Disease Neurological Disease Cardiovascular Disease
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC₅₀ of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.

HY-111932

Indirubin-5-sulfonate	CDK GSK-3	Cancer
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC₅₀ values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against *GSK-3β*.

HY-19624

NVP-ACC789 ACC-789; ZK202650	VEGFR PDGFR	Cancer
NVP-ACC789 is an inhibitor of human *VEGFR-1, VEGFR-2* (mouse VEGFR-2), VEGFR-3 and *PDGFR-β* with IC₅₀s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.

HY-10204

OSI-930	c-Fms c-Kit VEGFR Apoptosis	Cancer
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.

HY-10331

Regorafenib BAY 73-4506	VEGFR Autophagy PDGFR Raf RET	Cancer
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for *VEGFR1/2/3, PDGFRβ, Kit, RET* and *Raf-1*, respectively.

HY-15177

PF-04691502	PI3K mTOR Autophagy	Cancer
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

HY-N4195

Resveratroloside trans-Resveratrol 4'-O-β-D-glucopyranoside	Glucosidase	Metabolic Disease Cardiovascular Disease
Resveratroloside is a competitive inhibitior of α-glucosidase with an IC₅₀ of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect.

HY-I0352

Epiandrosterone 3β-Androsterone; trans-Androsterone; iso-Androsterone	Androgen Receptor Endogenous Metabolite	Endocrinology
Epiandrosterone is a steroid hormone with weak androgenic activity.

HY-B1076

Medrysone
HMS; 6α-Methyl-11β-hydroxyprogesterone
Others Inflammation/Immunology

Medrysone is a corticosteroid, in ophthalmology for the treatment of eye inflammations.
HY-N1459

Campesterol
(24R)-5-Ergosten-3β-ol
Endogenous Metabolite Cancer

Campesterol is a plant sterol with cholesterol lowering and anticarcinogenic effects.

HY-N0343

Helicid Helicide; Helicidum; 4-Formylphenyl-β-D-allopyranoside	Others	Neurological Disease
Helicid (Helicide) is a major constituent of Helicia nilgirica Bedd. Helicid has been used to treat psychoneurosis for its sedative-hypnotic and analgesic properties.

HY-B1172

Lactulose
4-O-β-D-Galactopyranosyl-D-fructose
Others Others

Lactulose is a non-absortable sugar used in the treatment of constipation and hepatic encephalopathy.

HY-N4285

Negletein 5,6-Dihydroxy-7-methoxyflavone	TNF Receptor Interleukin Related	Inflammation/Immunology Neurological Disease
Negletein is a neuroprotectant enhances the action of nerve growth factor and induces neurite outgrowth in PC12 cells. Negletein shows promising anti-inflammatory activity via inhibition of TNF-α and *IL-1β* with IC₅₀ values of 16.4 and 10.8 μM, respectively.

HY-14190

Valategrast R-411 free base	Integrin	Inflammation/Immunology
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and *α4β7* dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.

HY-N4327

Eurycomalactone	NF-κB	Infection Inflammation/Immunology
Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC₅₀ of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.

HY-16018A

Ilorasertib hydrochloride ABT-348 hydrochloride	Aurora Kinase PDGFR RET VEGFR	Cancer
Ilorasertib (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC₅₀s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and *Flt1* with IC₅₀s of 7 nM, 3 nM and 32 nM, respectively.

HY-B0116

Stavudine d4T	Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis	Infection
Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against *HIV-1* and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.

HY-B0116A

Stavudine sodium d4T sodium	Reverse Transcriptase HIV Nucleoside Antimetabolite/Analog NOD-like Receptor (NLR) Autophagy Apoptosis	Infection
Stavudine (d4T) sodium is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine sodium has activity against *HIV-1* and HIV-2. Stavudine sodium also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine sodium reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine sodium induces apoptosis.

HY-19805

STO-609	CaMK AMPK Autophagy	Metabolic Disease
STO-609 is a selective and cell-permeable inhibitor of the Ca²⁺/calmodulin-dependent protein kinase kinase (CaM-KK), with K_i values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC₅₀ ~0.02 g/ml.

HY-118567

Bis(maltolato)oxovanadium(IV) BMOV	Phosphatase	Metabolic Disease
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, *PTP1B, HPTPβ* and SHP2 with IC₅₀s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.

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-B1803A

Tracazolate hydrochloride ICI 136753 hydrochloride	GABA Receptor	Neurological Disease
Tracazolate (ICI 136753) hydrochloride is a potent GABA_A receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC₅₀=13.2 μM), α1β3γ2 (EC₅₀=1.5 μM). Tracazolate hydrochloride has the potency (EC₅₀) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.

HY-112813

TUG-1375	Others	Metabolic Disease
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pK_i of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.

HY-N0569

Madecassic acid	NO Synthase COX TNF Receptor Interleukin Related	Inflammation/Immunology
Madecassic acid is isolated from Centella asiatica (Umbelliferae). Madecassic acid has anti-inflammatory properties caused by iNOS, COX-2, TNF-alpha, *IL-1beta, and IL-6* inhibition via the downregulation of NF-κB activation in RAW 264.7 macrophage cells.

HY-P0295A

Gly-Arg-Gly-Asp-Ser (TFA)	Integrin	Inflammation/Immunology
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC₅₀ of ∼5 and ∼6.5 μM.

HY-10012

AZD-5438	CDK	Cancer
AZD-5438 is a potent *CDK1, CDK2, and CDK9* inhibitor, with IC₅₀s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 ^[1].

HY-10343

Sotrastaurin AEB071	PKC	Inflammation/Immunology Cancer
Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.

HY-B1517A

Alprenolol hydrochloride (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochloride	5-HT Receptor	Cancer
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.

HY-U00356

Tertatolol (±)-Tertatolol; Racemic Tertatolol; dl-Tertatolol	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease Endocrinology
Tertatolol is a potent antagonist of *beta-adrenoceptor* and 5-HT receptor, with unique renal vasodilatatory effects.

HY-B0525A

Carbenicillin disodium Sodium carbenicillin	Bacterial Antibiotic	Infection
Carbenicillin disodium is a beta-lactam penicillin derivative that interference with final stage of bacterial cell wall synthesis.

HY-131105S

Cimbuterol-D9
Adrenergic Receptor Cardiovascular Disease

Cimbuterol-D9 is the deuterium labeled Cimbuterol. Cimbuterol is aβ-adrenergic agonist.
HY-19919

BMS-779788
EXEL04286652; XL-652; BMS-788
LXR Metabolic Disease

BMS-779788 is a LXR partial agonist with IC₅₀ values of 68 nM for LXRα and 14 nM for LXRβ.
HY-N2183

Baimaside
Quercetin 3-O-sophoroside
Others Others

Quercetin 3-beta-sophoroside is isolated from the flowers of A. venetum, is an scavengers of superoxide anions.
HY-B1517

Alprenolol
(RS)-Alprenolol; dl-Alprenolol
5-HT Receptor Cancer

Alprenolol is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
HY-100347A

SRI-011381 hydrochloride
TGF-beta/Smad Neurological Disease

SRI-011381 hydrochloride is an oral bioavailabile TGF-beta signaling agonist, exhibits neuroprotective effect.
HY-108414

(R)-Equol
(+)-Equol
Estrogen Receptor/ERR Cancer

(R)-Equol is an agonist of both ERα and ERβ with K_is of 27.4 and 15.4 nM, respectively.
HY-N1499

Nystose
Others Metabolic Disease

Nystose is a tetrasaccharide with two fructose molecules linked via beta (1→2) bonds to the fructosyl moiety of sucrose.

HY-B0522

Ampicillin D-(-)-α-Aminobenzylpenicillin	Bacterial Antibiotic	Infection
Ampicillin is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.

HY-101822

Naminterol	Adrenergic Receptor	Inflammation/Immunology Endocrinology
Naminterol is a phenethanolamine derivative, is a β₂ adrenoceptor agonist with bronchodilatory properties. Naminterol is used for treatment of asthma.

HY-12767

Carvedilol metabolite 4-Hydroxyphenyl Carvedilol 4-Hydroxyphenyl Carvedilol; 4-Hydroxycarvedilol	Drug Metabolite	Cancer Cardiovascular Disease Inflammation/Immunology
4-Hydroxyphenyl Carvedilol is a metabolite of Carvedilol, which is a nonselective beta blocker/alpha-1 blocker.

HY-12377

GSK0660
PPAR Metabolic Disease

GSK0660 is a potent antagonist of PPARβ and PPARδ, with IC₅₀s of 155 nM for both isoforms.

HY-131103

Phenylethanolamine A	Adrenergic Receptor	Metabolic Disease Inflammation/Immunology
Phenylethanolamine A acts as a *β-adrenergic* agonist. Phenylethanolamine A is a byproduct during the Ractopamine synthesis process.

HY-100564

2',3'-cGAMP 2'-3'-cyclic GMP-AMP	Endogenous Metabolite STING IFNAR	Metabolic Disease
2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm.

HY-100564A

2',3'-cGAMP sodium 2'-3'-cyclic GMP-AMP sodium	Endogenous Metabolite STING IFNAR	Metabolic Disease
2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a high affinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm.

HY-135235

Cysteine thiol probe	Others	Others
Cysteine Thiol Probe is a thiol-based probe designed to label electrophilic natural products. Cysteine Thiol Probe possesses each of the characteristics of an ideal pharmacophore probe, and has a chromophore. Cysteine Thiol Probe is capable of engaging enone-, β-lactam-, and β-lactone-based electrophilic metabolites.

HY-B0593

Ceftazidime GR20263	Bacterial Antibiotic	Infection
Ceftazidime (GR20263) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases.

HY-114170

ML604440	Proteasome	Inflammation/Immunology
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.

HY-12330

AZD8186
PI3K Cancer

AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC₅₀=4 nM) and PI3Kδ (IC50₅₀=12 nM) with selectivity over PI3Kα (IC₅₀=35 nM) and PI3Kγ (IC₅₀=675 nM).

HY-13241

Ralimetinib dimesylate LY2228820 dimesylate	p38 MAPK Autophagy Apoptosis	Cancer Inflammation/Immunology
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

HY-N6736

K-252c	PKC Bacterial Apoptosis	Cancer Infection
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC₅₀ of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.

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-15245

GSK2636771	PI3K	Cancer
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a K_i of 0.89 nM and an IC₅₀ of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

HY-101569

LXS196	PKC	Cancer
LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC₅₀ values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research.

HY-I0678

Regorafénib N-oxyde (M2)	Drug Metabolite	Cancer
Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-121765

Dacisteine N,S-Diacetyl-L-cysteine	Endogenous Metabolite	Metabolic Disease
Dacisteine (N,S-Diacetyl-L-cysteine) is a cysteine derivative and displays a less New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitor with an IC₅₀ value of 1000 μM. Dacisteine can be used for the treatment of cardiovascular and cerebrovascular diseases caused by platelet aggregation.

HY-100500

Lenampicillin hydrochloride KBT 1585 hydrochloride	Bacterial	Cancer
Lenampicillin hydrochloride (KBT 1585 hydrochloride) is an orally active prodrug of Ampicillin and is an effective beta-lactam antibacterial agent that inhibits bacterial penicillin-binding proteins (transpeptidase). Lenampicillin hydrochloride has improved absorption and decreased side effects compares to Ampicillin and is applied in the investigation of the suppurative skin and soft tissue infection ^[1] .

HY-113953

Z-Asp-CH2-DCB	Caspase	Inflammation/Immunology
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.

HY-16232

GLUFOSFAMIDE D 19575; Glucosylifosfamide mustard	Others	Cancer
Glufosfamide is a novel alkylating agent in which the active metabolite of isophosphoramide mustard is glycosidically linked to *β-D-glucose*.

HY-105252A

BF 227
Amyloid-β Neurological Disease

BF 227 is a candidate for an amyloid imaging probe for PET, with a K_i of 4.3 nM for Aβ1-42 fibrils.

HY-17457

Levalbuterol tartrate Levosalbutamol tartrate	Adrenergic Receptor	Neurological Disease Endocrinology
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.

HY-18292

ARN2966
Amyloid-β Neurological Disease

ARN2966 is a potent post-transcriptional modulator of APP expression; reduces expression of APP with resultant lower production of Aβ.
HY-14927

Lificiguat
YC-1
Guanylate Cyclase Cancer

Lificiguat binds to the β subunit of soluble guanylyl cyclase(sGC) with K_d of 0.6-1.1 μM in the presence of CO.
HY-108688

GSK2033
LXR Metabolic Disease

GSK2033 is a LXR antagonist with pIC₅₀s of 7 and 7.4 for LXRα or LXRβ, respectively.
HY-P0315

Crosstide
Akt Others

Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.

HY-B0468

Isoprenaline hydrochloride Isoproterenol hydrochloride	Adrenergic Receptor Endogenous Metabolite	Cardiovascular Disease Endocrinology
Isoprenaline hydrochloride is a non-selective beta-adrenergic receptor agonist with potent peripheral vasodilator, bronchodilator, and cardiac stimulating activities.

HY-14565

Pozanicline ABT-089	nAChR	Neurological Disease
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (K_i=16 nM) and shows high selectivity for α6β2* and *α4α5β2* nAChR subtypes, the binding affinity (K_i, rat) for Pozanicline to [³H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.

HY-107684

3-Bromocytisine 3-Br-cytisine	nAChR	Neurological Disease
3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC₅₀s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC₅₀s are 8 and 50 nM, respectively.

HY-12270

T-5224	MMP	Others
T-5224 is a transcription factor c-Fos/activator protein (AP)-1 inhibitor with anti-inflammatory effects, which specifically inhibits the DNA binding activity of c-Fos/c-Jun without affecting other transcription factors. T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription.

HY-133987

AP-1/NF-κB activation inhibitor 1	NF-κB	Inflammation/Immunology
AP-1/NF-κB activation inhibitor 1 is a potent *AP-1* and NF-κB mediated transcriptional activation inhibitor (IC₅₀=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.

HY-124745

KY-05009	MAP4K Wnt Apoptosis	Cancer
KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a K_i of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.

HY-78263

MNS NSC 170724; 5-(2-Nitrovinyl)benzodioxole	Src Syk	Cancer
MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC₅₀ values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS inhibits Src, Syk, and FAK with IC₅₀ of 27.3, 2.8, and 97.6 μM, respectively.

HY-12980

Batefenterol GSK961081; TD-5959	Adrenergic Receptor mAChR	Inflammation/Immunology Endocrinology
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and *β₂-adrenoceptor* agonist; displays high affinity for hM2, hM3 muscarinic and hβ₂-adrenoceptor with K_i values of 1.4, 1.3 and 3.7 nM, respectively.

HY-N6927

Isoforskolin Coleonol B	TNF Receptor Interleukin Related	Inflammation/Immunology
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, *IL-1β, IL-6* and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.

HY-N7363

Isolongifolene (-)-Isolongifolene	Others	Cancer Inflammation/Immunology Neurological Disease
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of P13K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties.

HY-10942

VER-82576 NVP-BEP800	HSP	Cancer
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC₅₀ of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC₅₀s of 4.1 and 5.5 μM, respectively.

HY-10277

Odiparcil SB-424323	Thrombin	Cardiovascular Disease
Odiparcil (SB-424323) is an orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) ^[1].

HY-131081

γ-Amanitin	DNA/RNA Synthesis ADC Cytotoxin	Cancer
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin (HY-19610) and β-Amanitin (HY-125586).

HY-12235

PI-3065	PI3K	Inflammation/Immunology Cancer
PI-3065 is a potent inhibitor of PI3K p110δ, with IC₅₀ and K_i values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC₅₀s of 910, 600, >10000 nM.

HY-10185

TG 100572 Hydrochloride	Src VEGFR FGFR PDGFR	Inflammation/Immunology
TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

HY-124634

PZ-2891	Others	Neurological Disease
PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC₅₀s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.

HY-106004

Zamicastat BIA 5-1058	Dopamine β-hydroxylase P-glycoprotein BCRP	Cancer Cardiovascular Disease
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC₅₀ values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.

HY-18285

Longdaysin	Casein Kinase ERK CDK	Cancer
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits *CK1α, CK1δ, CDK7, and ERK2* with IC₅₀s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.

HY-B0368

Captopril SQ 14225	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Captopril (SQ 14225), antihypertensive agent, is a thiol-containing competitive, orally active angiotensin-converting enzyme (ACE) inhibitor (IC₅₀=0.025 μM) and has been widely used for research of hypertension and congestive heart failure. Captopril is also a New Delhi metallo-β-lactamase-1 *(NDM-1)* inhibitor with an IC₅₀ of 7.9 μM.

HY-N0603

20(S)-Ginsenoside Rg3 20(S)-Propanaxadiol; S-ginsenoside Rg3	Sodium Channel Potassium Channel NF-κB COX Amyloid-β Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
20(S)-Ginsenoside Rg3 is the main component of Red ginseng. Ginsenoside Rg3 inhibits Na⁺ and *hKv1.4* channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

HY-17503

Metoprolol	Adrenergic Receptor	Cardiovascular Disease Endocrinology
Metoprolol (Toprol) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.

HY-108869

Fodipir DPDP	Others	Inflammation/Immunology
Fodipir is an active metabolite of mangafodipir, involved in mangafodipir-mediated cytoprotection against 7β-hydroxycholesterol-induced cell death.

HY-A0269

Mecillinam
Amdinocillin; FL 1060
Bacterial Infection

Mecillinam (Amdinocillin), the β-lactam antibiotic, has a broad spectrum of activity against gram-negative organisms.

HY-100434

PD-161570	FGFR PDGFR EGFR Src TGF-β Receptor	Cancer Cardiovascular Disease
PD-161570 is a potent and ATP-competitive *human FGF-1 receptor* inhibitor with an IC₅₀ of 39.9 nM and a K_i of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC₅₀ values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC₅₀s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.

HY-18085

Quercetin	PI3K Autophagy Mitophagy Reactive Oxygen Species Apoptosis	Cancer
Quercetin, a natural flavonoid, is a stimulator of recombinant *SIRT1* and also a PI3K inhibitor with IC₅₀ of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

HY-50847

ZSTK474	PI3K Autophagy	Cancer
ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC₅₀s of16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.

HY-B0252

Hydrochlorothiazide HCTZ	TGF-beta/Smad Potassium Channel	Metabolic Disease Cardiovascular Disease
Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming *TGF-β/Smad* signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.

HY-130613

MAC-545496	Bacterial	Infection
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (K_d ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).

HY-B0593A

Ceftazidime pentahydrate GR20263 pentahydrate	Bacterial Antibiotic	Infection
Ceftazidime pentahydrate (GR20263 pentahydrate) is a third generation cephalosporin administered intravenously or intramuscularly. Ceftazidime pentahydrate has a broad spectrum of in vitro activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is particularly active against Enterobacteriaceae (including beta-lactamase-positive strains) and is resistant to hydrolysis by most beta-lactamases.

HY-120051

Afizagabar S44819; Egis-13529	GABA Receptor	Neurological Disease
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC₅₀ of 585 nM for α5β2γ2 and a K_i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy.

HY-10426

XCT790	Estrogen Receptor/ERR Autophagy	Cancer
XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

HY-B1794A

Thiethylperazine dimaleate	Dopamine Receptor Histamine Receptor Bacterial	Infection Neurological Disease
Thiethylperazine dimaleate is a phenothiazine derivate, and an orally active dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a slective *ABCC1*activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.

HY-N0175

Cytisinicline Cytisine; Sophorine; Baptitoxine	nAChR	Metabolic Disease
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.

HY-14650

DHEA Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone	Androgen Receptor Endogenous Metabolite	Endocrinology Cancer
DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.

HY-15507

VGX-1027 GIT 27	Interleukin Related TNF Receptor	Metabolic Disease Inflammation/Immunology
VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events.

HY-19975

RN-1734	TRP Channel	Neurological Disease
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC₅₀s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.

HY-10182A

CHIR-99021 monohydrochloride CT99021 monohydrochloride	GSK-3 Wnt β-catenin Autophagy	Cancer
CHIR-99021 monohydrochloride (CT99021 monohydrochloride) is a potent and selective *GSK-3α/β* inhibitor with IC₅₀s of 10 nM and 6.7 nM. CHIR-99021 monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 monohydrochloride is also a potent *Wnt/β-catenin* signaling pathway activator. CHIR-99021 monohydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 monohydrochloride induces *autophagy*.

HY-N0015

Astragalin Astragaline; 3-Glucosylkaempferol; Kaempferol 3-β-D-glucopyranoside	Apoptosis	Inflammation/Immunology Cancer
Astragalin (kaempferol-3-O-glucoside) is a flavonoid with anti-inflammatory activity and newly found in persimmon leaves and green tea seeds.

HY-N0595

Genistin Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside	Estrogen Receptor/ERR Apoptosis	Cancer Metabolic Disease
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.

HY-B0277

Vidarabine
Ara-A; Adenine Arabinoside; 9-β-D-Arabinofuranosyladenine
HSV Nucleoside Antimetabolite/Analog