Search Result

Targets Recommended:	γ-secretase Beta-secretase GABA Receptor

Results for "565789 1mg γ secretase Inhibitors" in MCE Product Catalog:

By Targets:	Beta-secretase (19) GABA Receptor (42) γ-secretase (30) 15-PGDH (1) 5 alpha Reductase (7) 5-HT Receptor (44) Acetyl-CoA Carboxylase (9) AChE (84) Ack1 (1) Acyltransferase (37) ADC Cytotoxin (49) ADC Linker (2) Adenosine Deaminase (7) Adenosine Kinase (2) Adenosine Receptor (10) Adenylate Cyclase (10) Adrenergic Receptor (38) Akt (66) Aldehyde Dehydrogenase (ALDH) (11) Aldose Reductase (16) ALK (29) Aminoacyl-tRNA Synthetase (10) Aminopeptidase (10) AMPK (30) Amyloid-β (24) Androgen Receptor (11) Angiotensin Receptor (13) Angiotensin-converting Enzyme (ACE) (47) Antibiotic (260) Antifolate (21) APC (3) Apoptosis (854) Arenavirus (4) Arginase (7) Aromatase (11) Arp2/3 Complex (9) Aryl Hydrocarbon Receptor (11) ATGL (1) ATM/ATR (19) ATP Citrate Lyase (8) ATP Synthase (9) Aurora Kinase (39) Autophagy (663) Bacterial (449) Bcl-2 Family (54) Bcr-Abl (43) BCRP (11) BMX Kinase (3) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (40) c-Fms (21) c-Kit (49) c-Met/HGFR (50) c-Myc (12) Calcium Channel (69) CaMK (22) Cannabinoid Receptor (14) Carbonic Anhydrase (17) Carboxypeptidase (4) Casein Kinase (35) Caspase (37) CaSR (1) Cathepsin (31) CCR (21) CD73 (7) CDK (150) CETP (6) CFTR (6) CGRP Receptor (3) Checkpoint Kinase (Chk) (22) Chloride Channel (10) Cholecystokinin Receptor (6) CMV (18) Complement System (14) COMT (12) COX (172) CRAC Channel (10) CRFR (3) CRISPR/Cas9 (5) CRM1 (2) CXCR (23) Cytochrome P450 (86) DAPK (1) Deubiquitinase (37) Dihydroorotate Dehydrogenase (10) Dipeptidyl Peptidase (35) Discoidin Domain Receptor (9) DNA Alkylator/Crosslinker (9) DNA Methyltransferase (21) DNA-PK (20) DNA/RNA Synthesis (139) Dopamine Receptor (30) Dopamine Transporter (15) Dopamine β-hydroxylase (6) Drug Metabolite (61) Drug-Linker Conjugates for ADC (30) Dynamin (6) DYRK (17) E1/E2/E3 Enzyme (51) E3 Ligase Ligand-Linker Conjugate (2) EAAT2 (3) EGFR (139) Elastase (16) Endogenous Metabolite (209) Endothelin Receptor (13) Enolase (1) Enterovirus (12) Ephrin Receptor (5) Epigenetic Reader Domain (106) Epoxide Hydrolase (12) ERK (54) Estrogen Receptor/ERR (38) Eukaryotic Initiation Factor (eIF) (19) FAAH (19) FABP (3) Factor Xa (10) FAK (21) Farnesyl Transferase (20) Fatty Acid Synthase (FASN) (23) Ferroptosis (71) FGFR (59) Filovirus (4) FKBP (7) FLAP (7) FLT3 (57) Fungal (117) FXR (4) G-quadruplex (4) Galectin (3) Gap Junction Protein (6) GHSR (3) Gli (3) Glucagon Receptor (1) Glucocorticoid Receptor (5) Glucosidase (27) GLUT (9) Glutaminase (8) Glutathione Peroxidase (10) GlyT (8) GPCR19 (2) GPR120 (1) GPR40 (1) GPR55 (1) GSK-3 (43) GSNOR (1) Guanylate Cyclase (4) Gutathione S-transferase (9) Haspin Kinase (3) HBV (28) HCN Channel (2) HCV (84) HCV Protease (15) HDAC (99) Hedgehog (12) Hexokinase (4) HIF/HIF Prolyl-Hydroxylase (38) Hippo (MST) (3) Histamine Receptor (33) Histone Acetyltransferase (35) Histone Demethylase (39) Histone Methyltransferase (93) HIV (191) HIV Integrase (18) HIV Protease (25) HMG-CoA Reductase (HMGCR) (37) HSP (46) HSV (39) IAP (9) IFNAR (5) IGF-1R (21) iGluR (21) IKK (32) Imidazoline Receptor (3) Indoleamine 2,3-Dioxygenase (IDO) (30) Influenza Virus (93) Insulin Receptor (12) Integrin (36) Interleukin Related (49) IRAK (15) IRE1 (16) Isocitrate Dehydrogenase (IDH) (15) Itk (5) JAK (78) JNK (31) Keap1-Nrf2 (21) Kinesin (17) KLF (4) Lactate Dehydrogenase (11) Leukotriene Receptor (19) Ligand for E3 Ligase (7) Ligand for Target Protein for PROTAC (19) LIM Kinase (LIMK) (5) Lipoxygenase (39) LPL Receptor (11) LRRK2 (15) LXR (3) mAChR (26) MAGL (16) MALT1 (4) MAP3K (13) MAP4K (8) MAPKAPK2 (MK2) (4) MDM-2/p53 (42) MEK (35) Melanocortin Receptor (6) Melatonin Receptor (2) MELK (3) mGluR (6) MicroRNA (7) Microtubule/Tubulin (86) Mineralocorticoid Receptor (2) Mitochondrial Metabolism (37) Mitophagy (53) Mixed Lineage Kinase (4) MMP (59) MNK (5) Monoamine Oxidase (62) Monoamine Transporter (11) Monocarboxylate Transporter (7) Mps1 (10) mTOR (69) MyD88 (4) Myosin (13) Na+/Ca2+ Exchanger (10) Na+/HCO3- Cotransporter (1) Na+/K+ ATPase (16) nAChR (13) NADPH Oxidase (11) Nampt (11) NEDD8-activating Enzyme (6) Neprilysin (14) Neurokinin Receptor (3) Neuropeptide Y Receptor (6) Neurotensin Receptor (1) NF-κB (145) NKCC (6) NO Synthase (42) NOD-like Receptor (NLR) (15) Notch (21) Nucleoside Antimetabolite/Analog (37) Opioid Receptor (9) Orexin Receptor (OX Receptor) (2) Oxytocin Receptor (1) P-glycoprotein (39) P2X Receptor (11) P2Y Receptor (12) p38 MAPK (59) p97 (7) PAI-1 (8) PAK (12) Parasite (139) PARP (51) PD-1/PD-L1 (13) PDGFR (72) PDHK (9) PDK-1 (6) PERK (4) PGC-1α (2) PGE synthase (12) Phosphatase (100) Phosphodiesterase (PDE) (141) Phospholipase (43) PI3K (124) PI4K (12) PIKfyve (5) Pim (18) PKA (30) PKC (73) PKD (4) Polo-like Kinase (PLK) (22) Porcupine (7) Potassium Channel (83) PPAR (70) Procollagen C Proteinase (1) Progesterone Receptor (2) Prostaglandin Receptor (31) PROTAC (16) PROTAC Linker (5) Protease-Activated Receptor (PAR) (9) Proteasome (43) Protein Arginine Deiminase (4) Proton Pump (36) PTEN (5) Pyk2 (4) Pyruvate Kinase (2) RAD51 (6) Raf (44) RAR/RXR (23) Ras (61) Reactive Oxygen Species (70) Renin (3) RET (19) Reverse Transcriptase (49) RGS Protein (3) Ribosomal S6 Kinase (RSK) (21) RIP kinase (28) ROCK (38) ROR (15) ROS (8) RSV (14) Salt-inducible Kinase (SIK) (6) SARS-CoV (61) Ser/Thr Protease (18) Serotonin Transporter (41) sFRP-1 (1) SGK (7) SGLT (18) Sigma Receptor (6) Sirtuin (30) Smo (10) SNIPER (8) Sodium Channel (69) Somatostatin Receptor (3) SPHK (9) Src (62) SRPK (3) STAT (63) Stearoyl-CoA Desaturase (SCD) (10) STING (3) Survivin (3) Syk (23) TAM Receptor (20) Telomerase (8) TGF-beta/Smad (12) TGF-β Receptor (34) Thrombin (21) Thymidylate Synthase (7) TNF Receptor (37) Toll-like Receptor (TLR) (28) TOPK (6) Topoisomerase (90) Trk Receptor (19) TRP Channel (37) Tryptophan Hydroxylase (8) TSH Receptor (1) Tyrosinase (35) ULK (4) URAT1 (4) Urotensin Receptor (1) VD/VDR (4) VDAC (2) VEGFR (122) Virus Protease (32) Wee1 (4) Wnt (33) Xanthine Oxidase (11) YAP (9) β-catenin (16)
By Research Areas:	Cancer (4036) Cardiovascular Disease (604) Endocrinology (210) Infection (1067) Inflammation/Immunology (1366) Metabolic Disease (712) Neurological Disease (931)

By Targets:

Beta-secretase (19)

GABA Receptor (42)

γ-secretase (30)

15-PGDH (1)

5 alpha Reductase (7)

5-HT Receptor (44)

Acetyl-CoA Carboxylase (9)

AChE (84)

Ack1 (1)

Acyltransferase (37)

ADC Cytotoxin (49)

ADC Linker (2)

Adenosine Deaminase (7)

Adenosine Kinase (2)

Adenosine Receptor (10)

Adenylate Cyclase (10)

Adrenergic Receptor (38)

Akt (66)

Aldehyde Dehydrogenase (ALDH) (11)

Aldose Reductase (16)

ALK (29)

Aminoacyl-tRNA Synthetase (10)

Aminopeptidase (10)

AMPK (30)

Amyloid-β (24)

Androgen Receptor (11)

Angiotensin Receptor (13)

Angiotensin-converting Enzyme (ACE) (47)

Antibiotic (260)

Antifolate (21)

APC (3)

Apoptosis (854)

Arenavirus (4)

Arginase (7)

Aromatase (11)

Arp2/3 Complex (9)

Aryl Hydrocarbon Receptor (11)

ATGL (1)

ATM/ATR (19)

ATP Citrate Lyase (8)

ATP Synthase (9)

Aurora Kinase (39)

Autophagy (663)

Bacterial (449)

Bcl-2 Family (54)

Bcr-Abl (43)

BCRP (11)

BMX Kinase (3)

Bombesin Receptor (1)

Bradykinin Receptor (1)

Btk (40)

c-Fms (21)

c-Kit (49)

c-Met/HGFR (50)

c-Myc (12)

Calcium Channel (69)

CaMK (22)

Cannabinoid Receptor (14)

Carbonic Anhydrase (17)

Carboxypeptidase (4)

Casein Kinase (35)

Caspase (37)

CaSR (1)

Cathepsin (31)

CCR (21)

CD73 (7)

CDK (150)

CETP (6)

CFTR (6)

CGRP Receptor (3)

Checkpoint Kinase (Chk) (22)

Chloride Channel (10)

Cholecystokinin Receptor (6)

CMV (18)

Complement System (14)

COMT (12)

COX (172)

CRAC Channel (10)

CRFR (3)

CRISPR/Cas9 (5)

CRM1 (2)

CXCR (23)

Cytochrome P450 (86)

DAPK (1)

Deubiquitinase (37)

Dihydroorotate Dehydrogenase (10)

Dipeptidyl Peptidase (35)

Discoidin Domain Receptor (9)

DNA Alkylator/Crosslinker (9)

DNA Methyltransferase (21)

DNA-PK (20)

DNA/RNA Synthesis (139)

Dopamine Receptor (30)

Dopamine Transporter (15)

Dopamine β-hydroxylase (6)

Drug Metabolite (61)

Drug-Linker Conjugates for ADC (30)

Dynamin (6)

DYRK (17)

E1/E2/E3 Enzyme (51)

E3 Ligase Ligand-Linker Conjugate (2)

EAAT2 (3)

EGFR (139)

Elastase (16)

Endogenous Metabolite (209)

Endothelin Receptor (13)

Enolase (1)

Enterovirus (12)

Ephrin Receptor (5)

Epigenetic Reader Domain (106)

Epoxide Hydrolase (12)

ERK (54)

Estrogen Receptor/ERR (38)

Eukaryotic Initiation Factor (eIF) (19)

FAAH (19)

FABP (3)

Factor Xa (10)

FAK (21)

Farnesyl Transferase (20)

Fatty Acid Synthase (FASN) (23)

Ferroptosis (71)

FGFR (59)

Filovirus (4)

FKBP (7)

FLAP (7)

FLT3 (57)

Fungal (117)

FXR (4)

G-quadruplex (4)

Galectin (3)

Gap Junction Protein (6)

GHSR (3)

Gli (3)

Glucagon Receptor (1)

Glucocorticoid Receptor (5)

Glucosidase (27)

GLUT (9)

Glutaminase (8)

Glutathione Peroxidase (10)

GlyT (8)

GPCR19 (2)

GPR120 (1)

GPR40 (1)

GPR55 (1)

GSK-3 (43)

GSNOR (1)

Guanylate Cyclase (4)

Gutathione S-transferase (9)

Haspin Kinase (3)

HBV (28)

HCN Channel (2)

HCV (84)

HCV Protease (15)

HDAC (99)

Hedgehog (12)

Hexokinase (4)

HIF/HIF Prolyl-Hydroxylase (38)

Hippo (MST) (3)

Histamine Receptor (33)

Histone Acetyltransferase (35)

Histone Demethylase (39)

Histone Methyltransferase (93)

HIV (191)

HIV Integrase (18)

HIV Protease (25)

HMG-CoA Reductase (HMGCR) (37)

HSP (46)

HSV (39)

IAP (9)

IFNAR (5)

IGF-1R (21)

iGluR (21)

IKK (32)

Imidazoline Receptor (3)

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

Influenza Virus (93)

Insulin Receptor (12)

Integrin (36)

Interleukin Related (49)

IRAK (15)

IRE1 (16)

Isocitrate Dehydrogenase (IDH) (15)

Itk (5)

JAK (78)

JNK (31)

Keap1-Nrf2 (21)

Kinesin (17)

KLF (4)

Lactate Dehydrogenase (11)

Leukotriene Receptor (19)

Ligand for E3 Ligase (7)

Ligand for Target Protein for PROTAC (19)

LIM Kinase (LIMK) (5)

Lipoxygenase (39)

LPL Receptor (11)

LRRK2 (15)

LXR (3)

mAChR (26)

MAGL (16)

MALT1 (4)

MAP3K (13)

MAP4K (8)

MAPKAPK2 (MK2) (4)

MDM-2/p53 (42)

MEK (35)

Melanocortin Receptor (6)

Melatonin Receptor (2)

MELK (3)

mGluR (6)

MicroRNA (7)

Microtubule/Tubulin (86)

Mineralocorticoid Receptor (2)

Mitochondrial Metabolism (37)

Mitophagy (53)

Mixed Lineage Kinase (4)

MMP (59)

MNK (5)

Monoamine Oxidase (62)

Monoamine Transporter (11)

Monocarboxylate Transporter (7)

Mps1 (10)

mTOR (69)

MyD88 (4)

Myosin (13)

Na+/Ca2+ Exchanger (10)

Na+/HCO3- Cotransporter (1)

Na+/K+ ATPase (16)

nAChR (13)

NADPH Oxidase (11)

Nampt (11)

NEDD8-activating Enzyme (6)

Neprilysin (14)

Neurokinin Receptor (3)

Neuropeptide Y Receptor (6)

Neurotensin Receptor (1)

NF-κB (145)

NKCC (6)

NO Synthase (42)

NOD-like Receptor (NLR) (15)

Notch (21)

Nucleoside Antimetabolite/Analog (37)

Opioid Receptor (9)

Orexin Receptor (OX Receptor) (2)

Oxytocin Receptor (1)

P-glycoprotein (39)

P2X Receptor (11)

P2Y Receptor (12)

p38 MAPK (59)

p97 (7)

PAI-1 (8)

PAK (12)

Parasite (139)

PARP (51)

PD-1/PD-L1 (13)

PDGFR (72)

PDHK (9)

PDK-1 (6)

PERK (4)

PGC-1α (2)

PGE synthase (12)

Phosphatase (100)

Phosphodiesterase (PDE) (141)

Phospholipase (43)

PI3K (124)

PI4K (12)

PIKfyve (5)

Pim (18)

PKA (30)

PKC (73)

PKD (4)

Polo-like Kinase (PLK) (22)

Porcupine (7)

Potassium Channel (83)

PPAR (70)

Procollagen C Proteinase (1)

Progesterone Receptor (2)

Prostaglandin Receptor (31)

PROTAC (16)

PROTAC Linker (5)

Protease-Activated Receptor (PAR) (9)

Proteasome (43)

Protein Arginine Deiminase (4)

Proton Pump (36)

PTEN (5)

Pyk2 (4)

Pyruvate Kinase (2)

RAD51 (6)

Raf (44)

RAR/RXR (23)

Ras (61)

Reactive Oxygen Species (70)

Renin (3)

RET (19)

Reverse Transcriptase (49)

RGS Protein (3)

Ribosomal S6 Kinase (RSK) (21)

RIP kinase (28)

ROCK (38)

ROR (15)

ROS (8)

RSV (14)

Salt-inducible Kinase (SIK) (6)

SARS-CoV (61)

Ser/Thr Protease (18)

Serotonin Transporter (41)

sFRP-1 (1)

SGK (7)

SGLT (18)

Sigma Receptor (6)

Sirtuin (30)

Smo (10)

SNIPER (8)

Sodium Channel (69)

Somatostatin Receptor (3)

SPHK (9)

Src (62)

SRPK (3)

STAT (63)

Stearoyl-CoA Desaturase (SCD) (10)

STING (3)

Survivin (3)

Syk (23)

TAM Receptor (20)

Telomerase (8)

TGF-beta/Smad (12)

TGF-β Receptor (34)

Thrombin (21)

Thymidylate Synthase (7)

TNF Receptor (37)

Toll-like Receptor (TLR) (28)

TOPK (6)

Topoisomerase (90)

Trk Receptor (19)

TRP Channel (37)

Tryptophan Hydroxylase (8)

TSH Receptor (1)

Tyrosinase (35)

ULK (4)

URAT1 (4)

Urotensin Receptor (1)

VD/VDR (4)

VDAC (2)

VEGFR (122)

Virus Protease (32)

Wee1 (4)

Wnt (33)

Xanthine Oxidase (11)

YAP (9)

β-catenin (16)

By Research Areas:

Cancer (4036)

Cardiovascular Disease (604)

Endocrinology (210)

Infection (1067)

Inflammation/Immunology (1366)

Metabolic Disease (712)

Neurological Disease (931)

7651

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

268

Peptides

MCE Kits

Inhibitory Antibodies

1365

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-50889

gamma-secretase modulator 3
γ-secretase Neurological Disease

gamma-secretase modulator 3 is a gamma-secretase modulator.
HY-10043

gamma-secretase modulator 1
γ-secretase Neurological Disease

γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

gamma-secretase modulator 3	γ-secretase	Neurological Disease
gamma-secretase modulator 3 is a gamma-secretase modulator.

gamma-secretase modulator 1	γ-secretase	Neurological Disease
γ-secretase inhibitior-1 is a gamma-secretase modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

HY-10043A

gamma-secretase modulator 1 hydrochloride	γ-secretase	Neurological Disease
gamma-secretase inhibitior-1 is a *gamma-secretase* modulator, γ-secretase inhibitior-1 is useful for Alzheimer's disease.

HY-50754

gamma-secretase modulator 2
γ-secretase Neurological Disease

gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.

gamma-secretase modulator 2	γ-secretase	Neurological Disease
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease.

HY-12465

Z-Ile-Leu-aldehyde Z-IL-CHO; GSI-XII; γ-secretase inhibitor XII	Notch γ-secretase Apoptosis	Cancer
Z-Ile-Leu-aldehyde (Z-IL-CHO) is a potent and competitive peptide aldehyde inhibitor of *γ-secretase* and *notch*.

HY-B1786

Sulindac sulfide cis-Sulindac sulfide	γ-secretase	Neurological Disease
Sulindac sulfide is a noncompetitive *γ-secretase* inhibitor, with an IC₅₀ of 20.2 μM for γ₄₂-secretase activity.

HY-N7148

γ-Tocopherol D-γ-Tocopherol; (+)-γ-Tocopherol	COX	Cancer Inflammation/Immunology
γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.

HY-108714

NGP555
γ-secretase Neurological Disease

NGP555 is a γ-secretase modulator.

NGP555	γ-secretase	Neurological Disease
NGP555 is a *γ-secretase* modulator.

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-14174

MRK-560
γ-secretase Neurological Disease

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

MRK-560	γ-secretase	Neurological Disease
MRK-560 is a potent, orally bioavailable and brain-penetrant *γ-secretase* inhibitor.

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-50752A

LY-411575 isomer 1
γ-secretase Neurological Disease

LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

LY-411575 isomer 1	γ-secretase	Neurological Disease
LY-411575 isomer 1 is an isomer of LY411575, which is a potent γ-secretase inhibitor.

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-B2194

γ-Oryzanol	DNA Methyltransferase	Metabolic Disease Cancer
γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of *DNMT1* (IC₅₀=3.2 μM), DNMT3a (IC₅₀=22.3 μM).

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.

*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-101399

γ-Glu-Phe γ-Glutamylphenylalanine	Endogenous Metabolite	Others
γ-Glu-Phe (γ-Glutamylphenylalanine) is synthesized by Bacillus amyloliquefaciens (GBA) and Aspergillus oryzae (GAO). γ-Glu-Phe or the post-enzymatic reaction mixture enhances the umami intensity of commercial soy sauce and model chicken broth.

HY-W015892

γ-Hexalactone
Others Others

γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage and acts a substrate of paraoxonase 1 (PON1).
HY-10974

MK-0752
γ-secretase Neurological Disease Cancer

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.

γ-Hexalactone	Others	Others
γ-Hexalactone is a gamma-lactone found in ripe fruits. γ-Hexalactone induces DNA damage and acts a substrate of paraoxonase 1 (PON1).

MK-0752	γ-secretase	Neurological Disease Cancer
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM.

HY-N1957

Gamma-Mangostin γ-Mangostin	5-HT Receptor	Metabolic Disease
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptors antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 µM) ^[1].

HY-136211

Cystathionine-γ-lyase-IN-1	Others	Metabolic Disease Inflammation/Immunology
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC₅₀ of 6.3 μM.

HY-112103

6-(γ,γ-Dimethylallylamino)purine
N6-(2-lsopentenyl)adenine
Others Others

6-(γ,γ-Dimethylallylamino)purine is a plant growth substance.

*6-(γ,γ-Dimethylallylamino)purine* N6-(2-lsopentenyl)adenine	Others	Others
6-(γ,γ-Dimethylallylamino)purine is a plant growth substance.

HY-N7014

Hydroxyl-γ-isosanshool	Others	Neurological Disease
Hydroxyl-γ-isosanshool is one of the major alkylamides in Z. bungeanum and Z. schinifolium oils. Hydroxyl-γ-isosanshoo induces a numbing sensation.

HY-N7105

Gamma-decalactone	Others	Others
Gamma-decalactone, γ-decalactone is used as an essential food additive with a ruity peach flavor. Ricinoleic acid (12-hydroxy-octadec-9-enoic acid) is used as the substrate in most production processes of γ-decalactone.

HY-15670

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

HY-W040040

γ-Cyclodextrin
Endogenous Metabolite Metabolic Disease

γ-Cyclodextrin is an endogenous metabolite.
HY-100785

gamma-DGG
γDGG; γ-D-Glutamylglycine
iGluR Neurological Disease

gamma-DGG is a competitive AMPA receptor blocker.

γ-Cyclodextrin	Endogenous Metabolite	Metabolic Disease
γ-Cyclodextrin is an endogenous metabolite.

gamma-DGG γDGG; γ-D-Glutamylglycine	iGluR	Neurological Disease
gamma-DGG is a competitive AMPA receptor blocker.

HY-13526

YO-01027 Dibenzazepine; DBZ	Notch γ-secretase	Cancer
YO-01027 (Dibenzazepine;DBZ) is a potent *γ-secretase* inhibitor with IC₅₀ values of 2.92 and 2.64 nM for Notch and APPL cleavage, respectively.

HY-50882

ELN318463	γ-secretase	Neurological Disease
ELN318463 is an amyloid precursor protein (APP) selective *γ-secretase* inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC₅₀s of 12 nM and 656 nM for PS1 and PS2, respectively. ELN318463 is 51-fold more selective for PS1.

HY-108694

γ-Tocotrienol
Others Metabolic Disease Inflammation/Immunology

γ-Tocotrienol is an active form of vitamin E.

γ-Tocotrienol	Others	Metabolic Disease Inflammation/Immunology
γ-Tocotrienol is an active form of vitamin E.

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-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-N3918

γ-Fagarine	HCV	Infection
γ-Fagarine is a furoquinoline alkaloid naturally occurring in Rutae Herba. γ-Fagarine has strong anti-HCV activities with IC₅₀ of 20.4 μg/mL and is also a sister chromatid exchanges (SCEs) inducer.

HY-12449

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

HY-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-N6823

Hydroxy-γ-sanshool
Others Others

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

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

HY-N7140

Gamma-Linolenic acid	Endogenous Metabolite	Metabolic Disease
Gamma-linolenic acid is an omega-6 (n-6), 18 carbon (18C-) polyunsaturated fatty acid (PUFA) extracted from human milk and several botanical seed oils. Gamma-linolenic acid supplements could restore needed PUFAs and mitigate the disease.

HY-112171

γ-L-Glutamyl-L-alanine
Endogenous Metabolite Others

γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

γ-L-Glutamyl-L-alanine	Endogenous Metabolite	Others
γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.

HY-50752

LY-411575	γ-secretase Notch Apoptosis	Neurological Disease
LY-411575 is a potent *γ-secretase* inhibitor with IC₅₀ of 0.078 nM/0.082 nM (membrane/cell-based), and also inhibits Notch S3 cleavage with IC₅₀ of 0.39 nM.

HY-B0530

Azacyclonol
γ-pipradol
Others Neurological Disease

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

Azacyclonol γ-pipradol	Others	Neurological Disease
Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

HY-P1214

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

HY-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-118870

γ-Globulins from human blood	Endogenous Metabolite	Inflammation/Immunology
γ-Globulins from human blood are a class of proteins in the blood. γ-Globulin is a protein fraction of blood serum containing many antibodies that protect against bacterial and viral infectious diseases. γ-Globulins from human blood is used for common variable immunodeficiency

HY-U00110

MG 1
Adrenergic Receptor Cardiovascular Disease Endocrinology

MG 1 is an α1 adrenergic receptor antagonist.

MG 1	Adrenergic Receptor	Cardiovascular Disease Endocrinology
MG 1 is an α1 adrenergic receptor antagonist.

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-133994

Octakis-(6-bromo-6-deoxy)-γ-cyclodextrin	Others	Others
Octakis-(6-bromo-6-deoxy)-γ-cyclodextrin is a perbrominated γ-cyclodextrin at the primary side. Octakis-(6-bromo-6-deoxy)-γ-cyclodextrin is also a commonly used intermediate in the modification of cyclodextrin.

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-B0033

Vigabatrin hydrochloride γ-Vinyl-GABA hydrochloride	GABA Receptor	Neurological Disease
Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.

HY-15399

Vigabatrin γ-Vinyl-GABA	GABA Receptor	Neurological Disease
Vigabatrin (γ-Vinyl-GABA), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.

HY-P1214A

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

HY-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-18236

MDL-28170 Calpain Inhibitor III	Proteasome	Inflammation/Immunology Neurological Disease
MDL-28170 (Calpain Inhibitor III) is a potent, selective and membrane-permeable cysteine protease inhibitor of calpain that rapidly penetrates the blood-brain barrier following systemic administration. MDL-28170 also block γ-secretase.

HY-P1217

[D-Trp8]-γ-MSH	Melanocortin Receptor	Inflammation/Immunology
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC₅₀s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis.

HY-113089

*Epsilon-(gamma-glutamyl)-lysine* H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys	Others	Metabolic Disease
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.

HY-15185

Nirogacestat PF-3084014; PF-03084014	γ-secretase Apoptosis	Cancer
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective *γ-secretase* inhibitor with an IC₅₀ of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers.

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-111826

γ-Glutamyl-S-1-propenyl cysteine
Others Others

γ-Glutamyl-S-1-propenyl cysteine is a compound isolated from garlic.
HY-U00264

2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol
Others Metabolic Disease

2-γ-Linolenoyl-1,3-dilinoleoyl-sn-glycerol is a triglyceride.

HY-P1217A

[D-Trp8]-γ-MSH TFA	Melanocortin Receptor	Inflammation/Immunology
[D-Trp8]-γ-MSH TFA is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC₅₀s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH TFA could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis.

HY-N0067

γ-Aminobutyric acid 4-Aminobutyric acid	GABA Receptor Endogenous Metabolite	Neurological Disease
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain, binding to the ionotropic GABA receptors (GABA_A receptors) and metabotropic receptors (GABA_B receptors).

HY-N0089

Schisandrin B γ-Schisandrin; Wuweizisu B	Autophagy Reactive Oxygen Species	Neurological Disease Cancer
Schisandrin B (γ-Schisandrin) is a dibenzocyclooctadiene derivative isolated from Fructus Schisandrae, has been shown to produce antioxidant effect on rodent liver and heart.

HY-A0143

Dihomo-γ-linolenic acid all-cis-8,11,14-Eicosatrienoic acid	Endogenous Metabolite	Cancer Inflammation/Immunology Cardiovascular Disease
Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system.

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-Y1620

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

HY-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-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-D0187

L-Glutathione reduced GSH; γ-L-Glutamyl-L-cysteinyl-glycine	Endogenous Metabolite Reactive Oxygen Species Ferroptosis	Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.

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-111360

SPL-707	γ-secretase	Inflammation/Immunology
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC₅₀ of 77 nM for hSPPL2a. SPL-707 inhibits *γ-secretase* (IC₅₀=6.1 μM) and SPP (IC₅₀=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.

HY-N4186

Glabrolide
Beta-secretase Neurological Disease

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

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-121879

SHP836
Phosphatase Cancer

SHP836 is a SHP2 allosteric inhibitor, with an IC₅₀ of 12 μM for the full length SHP2.
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-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-111919

3-Nitrocoumarin
Phospholipase Others

3-Nitrocoumarin (3-NC) is a potent and selective Phospholipase C-γ (PLC-γ) inhibitor.

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-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-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-108707

LY3130481	iGluR	Neurological Disease
LY3130481 is an AMPA receptor antagonist that is dependent upon transmembrane AMPA receptor regulatory protein (TARP) γ-8, selective inhibits AMPA/TARP γ-8 with an IC₅₀ of 65 nM.

HY-19609

Calicheamicin Calicheamicin γ1	DNA Alkylator/Crosslinker ADC Cytotoxin Bacterial Apoptosis Antibiotic	Cancer Infection
Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor.

HY-15121

L-Theanine L-Glutamic Acid γ-ethyl amide; Nγ-Ethyl-L-glutamine	Apoptosis	Neurological Disease
L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake.

HY-14600

Rosiglitazone maleate BRL 49653C	PPAR TRP Channel Autophagy Ferroptosis	Cancer Metabolic Disease Inflammation/Immunology
Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

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-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-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-17386

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

HY-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-120210

XY018	ROR	Cancer Inflammation/Immunology
XY018 is a potent *ROR-γ*-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC₅₀, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).

HY-101423

NIH-12848
Others Cardiovascular Disease

NIH-12848 is a putative phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ) inhibitor with an IC₅₀ of 1 μM.
HY-19770

GSK2981278
ROR Inflammation/Immunology

GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.

HY-15655

GW1929	PPAR	Metabolic Disease Neurological Disease
GW1929 is a potent *PPAR-γ* agonist, with a pK_i of 8.84 for human *PPAR-γ, and pEC₅₀s of 8.56 and 8.27 for human PPAR-γ* and murine *PPAR-γ*, respectively.

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-14799

Palovarotene
R 667; Ro 3300074
RAR/RXR Autophagy Others

Palovarotene is a nuclear retinoic acid receptor γ (RAR-γ) agonist.
HY-100532

CD437
AHPN
RAR/RXR Autophagy Cancer

CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.

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-100779

Rimacalib SMP 114	CaMK Autophagy	Metabolic Disease
Rimacalib (SMP 114) is a Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC₅₀s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.

HY-16787

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

HY-18728

STF-31
GLUT Autophagy Cancer

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1μM^[1][2].
HY-107765

LY2955303
RAR/RXR Autophagy Inflammation/Immunology

LY2955303 is a potent and selective retinoic acid receptor gamma (RARγ) antagonist with a K_i of 1.09 nM.

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-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-16086

Balaglitazone
DRF 2593; NN 2344
PPAR Metabolic Disease

Balaglitazone is a selective partial PPARγ agonist with an EC₅₀ of 1.351 μM for human PPARγ.
HY-13530

CAY10505
PI3K Apoptosis Cancer

CAY10505 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30 nM in neurons.

HY-N0495

Aloenin Aloenin A	Beta-secretase	Neurological Disease
Aloenin (Aloenin A) is a class of anthraquinones isolated from Aloe arborescens. Aloenin has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).

HY-13956

Pioglitazone U 72107	PPAR Ferroptosis	Metabolic Disease Cancer
Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

HY-13532

AS-252424
PI3K Cancer

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 30±10 nM.
HY-50935

Troglitazone
CS-045
PPAR Autophagy Apoptosis Ferroptosis Cancer

Troglitazone is a PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.

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-N3026

Soyasaponin Ab	Others	Metabolic Disease
Soyasaponin Ab is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).

HY-N3027

Soyasaponin Aa	Others	Metabolic Disease
Soyasaponin Aa is a soyasaponin that exerts an anti-obesity effect in 3T3-L1 adipocytes through downregulation of peroxisome proliferator-activated receptor γ (PPARγ).

HY-111751

JNJ-61432059	iGluR	Neurological Disease
JNJ-61432059 is an oral active and selective negative modulator of AMPAR associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC₅₀ of 9.7 for GluA1/γ-8. Exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.

HY-19791

N-Acetyl-Calicheamicin
N-Acetyl-Calicheamicin γ; N-Acetyl-γ-calicheamicin
Bacterial Cancer

N-Acetyl-Calicheamicin is a potent enediyne antitumor antibiotic.

HY-108022

MSDC-0602	Mitochondrial Metabolism	Metabolic Disease
MSDC-0602, a PPARγ-sparing thiazolidinedione (TZD), interacts with the mitochondrial pyruvate carrier (MPC) and inhibits its activity and has the potential for type 2 diabetes study with reducing risk of PPARγ-mediated side effects.

HY-14422

SR1078	ROR	Cancer
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.

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-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-10109

AS-605240
PI3K Autophagy Cancer

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC₅₀ of 8 nM, and a K_i of 7.8 nM.

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-14601

Pioglitazone hydrochloride U 72107A; AD 4833	PPAR Ferroptosis	Cancer Metabolic Disease
Pioglitazone hydrochloride is a potent and selective PPARγ agonist with EC₅₀s of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

HY-14792

Inolitazone Efatutazone; CS-7017; RS5444	PPAR	Cancer
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

HY-Y0078

Cinnamyl Alcohol
PPAR Metabolic Disease

Cinnamyl Alcohol is an active component from chestnut flower, inhibits increased PPARγ expression, with anti-obesity activity.

HY-14792B

Inolitazone dihydrochloride Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride	PPAR	Cancer
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

HY-14817

Indeglitazar
PPM 204
PPAR Metabolic Disease

Indeglitazar (PPM 204) is an orally available PPAR pan-agonist for all three PPARα, PPARδ and PPARγ.
HY-15725

CDDO-Im
RTA-403; TP-235; CDDO-Imidazolide
Keap1-Nrf2 PPAR Ferroptosis Cancer

CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with K_is of 232 and 344 nM for PPARα and PPARγ.
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-13956S

Pioglitazone D4 U 72107 D4	PPAR Ferroptosis	Cancer Metabolic Disease
Pioglitazone D4 (U 72107 D4) is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.

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-117727

Leriglitazone Hydroxypioglitazone	PPAR	Metabolic Disease
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone. Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy. Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with K_i of 1.2 μM，induces transcriptional efficacy of the PPARγ (LBD) with EC₅₀ of 680 nM.

HY-15180

Buparlisib Hydrochloride BKM120 Hydrochloride; NVP-BKM120 Hydrochloride	PI3K Apoptosis	Cancer
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC₅₀ of 52 nM/166 nM/116 nM/262 nM for *p110α/p110β/p110δ/p110γ*, respectively.

HY-114411

ERRγ Inverse Agonist 1	Estrogen Receptor/ERR	Cancer
ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC₅₀ of 40 nM.

HY-15294

CZC24832
PI3K Inflammation/Immunology Cancer

CZC24832 is a highly selective and potent PI3Kγ inhibitor (IC₅₀=27 nM) with apparent dissociation constants (K_d^app) of 19 nM.
HY-112897

IITZ-01
Autophagy PI3K Apoptosis Cancer

IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC₅₀ of 2.62 μM for PI3Kγ.
HY-13202

T0070907
PPAR RAD51 Cancer

T0070907 is a potent PPARγ antagonist with a K_i of 1 nM.
HY-A0173

Progabide
SL 76002
GABA Receptor Neurological Disease

Progabide is a gamma-aminobutyric acid receptor (GABA) agonist.

HY-B0287

Clofibrate	PPAR	Metabolic Disease
Clofibrate is an agonist of PPAR, with EC₅₀s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.

HY-112443

AZD3458	PI3K	Cancer Metabolic Disease Inflammation/Immunology
AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC₅₀s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.

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-113270A

(3-Carboxypropyl)trimethylammonium chloride γ-Butyrobetaine hydrochloride	Endogenous Metabolite	Metabolic Disease Cardiovascular Disease
(3-Carboxypropyl)trimethylammonium chloride is angiopathic substance produced as an intermediary metabolite by gut microbiota that feed on carnitine in dietary red meat.

HY-17645

Tenalisib
RP6530
PI3K Cancer

Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC₅₀ values of 25 and 33 nM, respectively.
HY-16122A

CAL-130
PI3K Cancer

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.
HY-16122B

CAL-130 Hydrochloride
PI3K Cancer

CAL-130 is a PI3Kδ and PI3Kγ inhibitor with IC₅₀s of 1.3 and 6.1 nM, respectively.

HY-15027

5-Aminosalicylic Acid Mesalamine; 5-ASA; Mesalazine	PPAR PAK NF-κB Endogenous Metabolite	Inflammation/Immunology Cancer
5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

HY-U00036

Naveglitazar racemate LY519818 racemate	PPAR	Metabolic Disease
Naveglitazar racemate (LY519818 racemate) is the racemate of Naveglitazar. Naveglitazar is a nonthiozolidinedione peroxisome proliferator-activated receptor (PPAR) α-γ dual, γ-dominant agonist that has shown glucose-lowering potential in animal models.

HY-12030

PIK-90
PI3K DNA-PK Cancer

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC₅₀s of 11, 18 and 13 nM, respectively.

HY-13531

AS-604850	PI3K	Cancer
AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC₅₀ value of 0.25 μM and a K_i value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively.

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-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-33353

GSK-4716
Estrogen Receptor/ERR Cancer

GSK-4716 is a selective ERRβ/γ agonist.
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-D0889

Glycylglycine
Endogenous Metabolite Metabolic Disease

Glycylglycine is the simplest of all peptides and could function as a gamma-glutamyl acceptor.

HY-15682

TTNPB Ro 13-7410; Arotinoid acid; AGN191183	RAR/RXR Autophagy Apoptosis	Cancer
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC₅₀s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.

HY-N2025

Oroxin A	PARP Glucosidase	Metabolic Disease
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.

HY-101676

RG-12525 NID 525	Leukotriene Receptor PPAR Cytochrome P450	Metabolic Disease
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC₅₀s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC₅₀ of appr 60 nM and a potent inhibitor of CYP3A4, with a K_i value of 0.5 µM.

HY-N0548

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

HY-17002

Suplatast (Tosilate) IPD 1151T	Interleukin Related	Inflammation/Immunology
Suplatast Tosilate (IPD 1151T) is a Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production.

HY-12776

GSK805
ROR Inflammation/Immunology

GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC₅₀ of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
HY-10111

TG100-115
PI3K Cardiovascular Disease Cancer

TG100-115 is a selective PI3Kγ/PI3Kδ inhibitor with IC₅₀s of 83 and 235 nM, respectively.
HY-B0007

Baclofen
GABA Receptor Neurological Disease

Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.
HY-101411

4-Acetamidobutanoic acid
N-acetyl GABA
GABA Receptor Endogenous Metabolite Others

4-Acetamidobutanoic acid (N-acetyl GABA) is a γ-aminobutyric acid (GABA) derivative.

HY-17444

Tesaglitazar	PPAR	Cancer Metabolic Disease
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC₅₀s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats.

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-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-100716

IPI549
PI3K Cancer

IPI549 is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 16 nM. IPI549 shows >100-fold selectivity over other lipid and protein kinases.

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-B0079

Sugammadex sodium
Org25969
Others Neurological Disease

Sugammadex sodium is a synthetic γ-cyclodextrin derivative, and acts as a new reversal agent for neuromuscular block.

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-16995

Pirinixic acid Wy-14643	PPAR	Metabolic Disease Inflammation/Immunology
Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC₅₀s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

HY-128671

6-Thioinosine 6TI; 6-Mercaptopurine riboside	Nucleoside Antimetabolite/Analog	Metabolic Disease
6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.

HY-100277

Mifobate SR-202	PPAR	Metabolic Disease
Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC₅₀=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects.

HY-B0637

Bezafibrate BM15075	PPAR	Metabolic Disease Cardiovascular Disease
Bezafibrate is an agonist of PPAR, with EC₅₀s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.

HY-124108

Eicosatetraynoic acid ETYA	COX PPAR	Others
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID₅₀=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.

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-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-16998

SR2211
ROR Inflammation/Immunology

SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a K_i of 105 nM and an IC₅₀ of ~320 nM.

HY-B1803A

Tracazolate hydrochloride ICI 136753 hydrochloride	GABA Receptor	Neurological Disease
Tracazolate hydrochloride (ICI 136753 hydrochloride) is a potent GABA_A receptor modulator. Tracazolate hydrochloride potentiates α1β1γ2s (EC₅₀=13.2 μM) and α1β3γ2 (EC₅₀=1.5 μM) in a concentration-dependent manner. Tracazolate hydrochloride has the potency (EC₅₀) is determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.

HY-W016586

Acivicin AT-125; U-42126	Parasite	Cancer Infection
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.

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-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-W015878

5-Aminovaleric acid	Endogenous Metabolite	Metabolic Disease Neurological Disease
5-Aminovaleric acid is believed to act as a methylene homologue of gamma-aminobutyric acid (GABA) and functions as a weak GABA agonist.

HY-14644A

Apilimod mesylate STA 5326 mesylate	Interleukin Related PIKfyve	Inflammation/Immunology
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

HY-14644

Apilimod STA 5326	Interleukin Related PIKfyve	Inflammation/Immunology
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC₅₀s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

HY-14743B

Golotimod hydrochloride SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride	Bacterial STAT	Infection Inflammation/Immunology
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).

HY-14743

Golotimod SCV 07; Gamma-D-glutamyl-L-tryptophan	Bacterial STAT	Infection Inflammation/Immunology
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).

HY-104037

Cintirorgon LYC-55716	ROR	Cancer
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.

HY-12307

(-)-Indolactam V Indolactam V	PKC	Cancer
(-)-Indolactam V is a PKC activator, with K_is of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and K_ds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

HY-12034

WYE-354	mTOR Autophagy Apoptosis	Cancer
WYE-354 is an ATP-competitive mTOR inhibitor with an IC₅₀ of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC₅₀s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both *mTORC1* and mTORC2.

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-101491

SR-18292	PGC-1α Autophagy	Metabolic Disease
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.

HY-100348

EPI-001	Androgen Receptor PPAR Apoptosis	Cancer
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC₅₀ of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo.

HY-N0625A

Alpinetin
PPAR Inflammation/Immunology Cancer

Alpinetin is a flavonoid isolated from Alpinia katsumadai Hayata, activates activates PPAR-γ, with potent anti-inflammatory activity.
HY-101649

Imiglitazar
TAK-559
PPAR Cardiovascular Disease

Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC₅₀ values of 67 and 31 nM.

HY-B0585

Piracetam UCB-6215	iGluR	Neurological Disease
Piracetam (UCB-6215) is a cyclic derivative of the neurotransmitter gamma-aminobutyric acid (GABA), used in treatment of a wide range of cognitive disorders.

HY-B1715

Oxiracetam ISF2522	GABA Receptor	Neurological Disease
Oxiracetam is a cyclic derivative of γ-aminobutyric acid (GABA) which has been commonly used as nootropic drug to treat cognitive impairments.

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-14831

Arhalofenate MBX 102; JNJ 39659100	PPAR	Metabolic Disease
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor *(PPAR)-γ*, used for the treatment of type 2 diabetes.

HY-19775

GNE-6468
ROR Inflammation/Immunology

GNE-6468 is a potent and selective RORγ(RORc) agonists with an EC₅₀ value of 13 nM for HEK-293 cell.

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-131265

Mesalamine impurity P	PPAR PAK NF-κB	Cancer Inflammation/Immunology
Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

HY-101146

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

HY-N6630

6-Methylflavone
GABA Receptor Neurological Disease

6-Methylflavone is an activator of α₁β₂γ_2L and α₁β₂ GABA_A receptors.
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-103683

PF-06409577
AMPK Metabolic Disease

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC₅₀ of 7 nM.
HY-128604

XY101
ROR Cancer

XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC₅₀ of 30 nM and a K_d of 380 nM.

HY-100256

Trifarotene CD5789	RAR/RXR Autophagy	Inflammation/Immunology
Trifarotene (CD5789) is a retinoic acid receptor (RAR) agonist with K_d^app of 2, 15 and 500 nM for RARγ, RARβ and RARα, respectively.

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-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-16974

Afoxolaner	GABA Receptor Chloride Channel	Infection
Afoxolaner is an orally active isoxazoline insecticide/acaricide against Ixodes scapularis in dogs. Afoxolaner acts on the insect γ-aminobutyric acid receptor (GABA) and glutamate receptors, inhibiting GABA & glutamate-regulated uptake of chloride ions, resulting in excess neuronal stimulation and death of the arthropod.

HY-B0760

Fenofibric acid FNF acid	PPAR COX	Metabolic Disease
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

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-B1026

Adelmidrol	NF-κB COX PPAR	Inflammation/Immunology
Adelmidrol exerts important anti-inflammatory effects that are partly dependent on PPARγ. Adelmidrol reduces NF-κB translocation, and COX-2 expression.

HY-N2209

Angeloylgomisin H	PPAR	Metabolic Disease
Angeloylgomisin H, as a major lignin extract of Schisandra rubriflora, has the potential to improve insulin-stimulated glucose uptake by activating *PPAR-γ*.

HY-U00340

PPAR agonist 1
PPAR Metabolic Disease

PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.

HY-111226A

(E/Z)-GSK5182	Estrogen Receptor/ERR Reactive Oxygen Species	Cancer Cardiovascular Disease
(E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC₅₀ of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma.

HY-D0254

Gallein Pyrogallol phthalein	Others	Cancer
Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.

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-15271A

WYE-687 dihydrochloride	mTOR PI3K	Cancer
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC₅₀ of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of *mTORC1* and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC₅₀s of 81 nM and 3.11 μM, respectively.

HY-14728

Aleglitazar
R1439; RO0728804
PPAR Metabolic Disease

Aleglitazar(R1439; RO-0728804) is a new dual PPAR-α/γ agonist with IC50 of 2.8 nM/4.6 nM.

HY-114336

Enocyanin	Phosphatase	Inflammation/Immunology
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity.

HY-N0479

Licarin B (-)-Licarin B	PPAR GLUT	Metabolic Disease
Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.

HY-N4194

Glabrone	PPAR	Metabolic Disease
Glabrone is an isoflavone isolated from Glycyrrhiza glabra roots. Glabrone exhibits anti-influenza activity and significant PPAR-γ ligand-binding activity.

HY-B0837

Emamectin Benzoate MK-244	GABA Receptor	Infection
Emamectin Benzoate (MK-244) works as a chloride channel activator by binding gamma aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods.

HY-N7078

Spiculisporic acid	Others	Others
Spiculisporic acid is a γ-butenolide isolated from the cultue of Aspergillus sp. Spiculisporic acid is a microbial biosurfactant and has anti-oxidative stress actions.

HY-16684

AGN 195183
RAR/RXR Autophagy Cancer

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.
HY-17538

ZLN005
PGC-1α Autophagy Metabolic Disease

ZLN005 is a potent activator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).

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-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-111745

Tyk2-IN-5	JAK	Inflammation/Immunology
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a K_i of 0.086 nM for Tyk2 JH2 and an IC₅₀ of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.

HY-16578

GW9662
PPAR Cancer

GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

HY-N0704

Agrimol B	Sirtuin PPAR	Metabolic Disease
Agrimol B is a polyphenol derived from Agrimonia pilosa Ledeb, suppresses adipogenesis via inducing *SIRT1* translocation and expression, and reducing PPARγ expression.

HY-N6775

Sonolisib PX-866	PI3K	Cancer
Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC₅₀=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.

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-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-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-133615

8(14)-Abietenic acid	Others	Others
8(14)-Abietenic acid is an abietane diterpenoid. Abietenic acid is racemic of 8(14)-Abietenic acid. Abietenic acid acts as a PPARα/γ dual activator.

HY-U00450

4-O-Methyl honokiol	PPAR NF-κB	Cancer Inflammation/Immunology
4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.

HY-N7624

Methyl oleanonate	PPAR	Cancer
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.

HY-U00449

AGN 193109	RAR/RXR Autophagy	Cancer
AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with K_ds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively.

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-W011391

GPNA hydrochloride	Apoptosis	Cancer
GPNA hydrochloride is a well known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride is a specific glutamine (Gln) transporter ASCT2 inhibitor. GPNA hydrochloride also inhibit Na⁺-dependent carriers, such as SNAT family (SNAT1/2/4/5), and the Na⁺-independent leucine transporters LAT1/2. GPNA reversibly induces apoptosis in A549 cells.

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-20019

L-165041	PPAR	Metabolic Disease
L-165041 is a cell permeable PPARδ agonist, with K_is of 6 nM and appr 730 nM for PPARδ and PPARγ, respectively, and induces adipocyte differentiation in NIH-PPARδ cells.

HY-120384

AZD-0284	ROR	Inflammation/Immunology
AZD-0284 is a selective inverse agonist of the nuclear receptor RORγ. AZD-0284 has the potential for plaque psoriasis vulgaris and respiratory tract disorders treatment.

HY-13861

GW7647
PPAR Cardiovascular Disease

GW7647 is a potent PPARα agonist, with EC₅₀s of 6 nM, 1.1 μM, and 6.2 μM for human PPARα, PPARγ and PPARδ, respectively.

HY-Y0313

p-Hydroxybenzaldehyde	Endogenous Metabolite GABA Receptor	Neurological Disease
p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABA_A receptor of the α₁β₂γ₂S subtype at high concentrations.

HY-109068

Parsaclisib INCB050465	PI3K	Cancer
Parsaclisib (INCB050465) is a potent and selective PI3Kδ inhibitor, with an IC₅₀ of 1 nM at 1 mM ATP, and shows appr 20,000-fold selectivity for PI3Kα, PI3Kβ, PI3Kγ and 57 other kinases.

HY-19962

Paxalisib GDC-0084	PI3K mTOR	Cancer
Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with K_is of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.

HY-N0146

Quercetin dihydrate	PI3K Apoptosis	Inflammation/Immunology Cancer
Quercetin dihydrate, a natural flavonoid, is a stimulator of recombinant *SIRT1* and a PI3K inhibitor with IC₅₀s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

HY-16526

Pilaralisib XL-147; SAR245408	PI3K	Cancer
Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC₅₀s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

HY-122181B

OTS186935 hydrochloride	Histone Methyltransferase	Cancer
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC₅₀ of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.

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-107390A

AX-024 hydrochloride	TNF Receptor Interleukin Related IFNAR	Inflammation/Immunology
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC₅₀ ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, *IFN-γ, IL-10* and IL-17A.

HY-107390

AX-024	TNF Receptor Interleukin Related IFNAR	Inflammation/Immunology
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC₅₀ ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, *IFN-γ, IL-10* and IL-17A.

HY-N2096

Kavain	GABA Receptor	Neurological Disease
Kavain is a class of kavalactone isolated from Piper methysticum, which has anxiolytic and sedative properties in animals and humans. Kavain positively modulated γ-Aminobutyric acid type A (GABAA) receptor.

HY-128400

4'-Methoxychalcone	PARP	Metabolic Disease Cancer
4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity.

HY-10678

BMS-687453	PPAR	Cardiovascular Disease
BMS-687453 is a potent and selective PPARα agonist, with an EC₅₀ and IC₅₀ of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

HY-N0163

Magnolol	RAR/RXR PPAR Autophagy Bacterial	Cancer Inflammation/Immunology Neurological Disease Cardiovascular Disease
Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC₅₀ values of 10.4 µM and 17.7 µM, respectively.

HY-104049

Lanifibranor IVA337	PPAR	Metabolic Disease Cancer
Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC₅₀s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.

HY-15483

DY131 GSK 9089	Estrogen Receptor/ERR	Cancer
DY131(GSK 9089) is a novel selective agonist of ERRβ and ERRγ; displays minimal activity at ERRα, ERα and ERβ at concentrations up to 30 μM.

HY-N6642

Ankaflavin	PPAR	Cancer Inflammation/Immunology
Ankaflavin, isolated from Monascus-Fermented red rice, is a PPARγ agonist with anti-inlfammatory activity. Ankaflavin exhibits selective cytotoxic effect and induces cell death on cancer cells.

HY-19937A

Saroglitazar Magnesium	PPAR	Metabolic Disease
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC₅₀ values of 0.65 pM and 3 nM in HepG2 cells, respectively.

HY-10681

Gedatolisib PKI-587; PF-05212384	PI3K mTOR	Cancer
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC₅₀s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. PKI-587 is equally effective in both complexes of mTOR, *mTORC1* and mTORC2.

HY-133897

(Rac)-Indoximod 1-Methyl-DL-tryptophan; (Rac)-NLG-8189	Indoleamine 2,3-Dioxygenase (IDO)	Cancer Inflammation/Immunology
(Rac)-Indoximod (1-Methyl-DL-tryptophan) is an indoleamine 2,3-dioxygenase (IDO) inhibitor. Co-treatment with IFN-γ and (Rac)-Indoximod markedly reduces the activity of human cardiac myofibroblasts (hCMs) expressing α-SMA and induces apoptosis through up-regulating the IRF-1, Fas, and FasL genes.

HY-15505

RWJ-67657 JNJ 3026582	p38 MAPK	Cancer Inflammation/Immunology Cardiovascular Disease
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC₅₀s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.

HY-13898

Taselisib GDC-0032; RG-7604	PI3K	Cancer
Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

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-104070

LG-100064	RAR/RXR Autophagy	Cancer
LG-100064 is a retinoid-X-receptor (RXR) agonist, with EC₅₀s of 330 nM, 200 nM, and 260 nM for RXRα, RXRβ and RXRγ; LG-100064 can be used in the research of cancer.

HY-12868

Bimiralisib PQR309	PI3K mTOR	Cancer
Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC₅₀s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an *mTORC1* and mTORC2 inhibitor.

HY-129624A

Bisindolylmaleimide VIII acetate Ro 31-7549 acetate; Bis VIII acetate	PKC Apoptosis	Cancer Inflammation/Immunology
Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC₅₀ of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate has IC₅₀s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively. Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.

HY-13281

PIK-75 hydrochloride	DNA-PK PI3K Apoptosis	Cancer
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 hydrochloride induces apoptosis.

HY-N0292

Oleuropein	PPAR Apoptosis Aromatase	Cancer Inflammation/Immunology Cardiovascular Disease
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.

HY-130354

Dibutyryl-cGMP sodium Bt2cGMP sodium	Potassium Channel	Cardiovascular Disease
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [³H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K⁺ channels.

HY-10811

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

HY-128932

Cefminox sodium MT-141	Bacterial PPAR Prostaglandin Receptor Antibiotic	Infection Cardiovascular Disease Endocrinology
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.

HY-18085S

Quercetin D5	PI3K Autophagy Mitophagy Apoptosis	Cancer
Quercetin D5 is a deuterium labeled Quercetin. 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-16681

AGN 194310 VTP-194310	RAR/RXR Autophagy	Cancer
AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with K_d values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively.

HY-108034

GET73	Others	Neurological Disease
GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.

HY-15340

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

HY-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-13334

BGT226 maleate NVP-BGT226 maleate	PI3K mTOR Autophagy Apoptosis	Cancer
BGT226 maleate (NVP-BGT226 maleate) is a PI3K (with IC₅₀s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

HY-10405

Pamapimod Ro4402257; R1503	p38 MAPK Autophagy	Inflammation/Immunology
Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC₅₀s of 14 nM and 480 nM and K_is of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.

HY-111508

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

HY-19522A

Seladelpar sodium salt MBX-8025 sodium salt; RWJ-800025 sodium salt	PPAR	Metabolic Disease
Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC₅₀ of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

HY-N0301

Thiocolchicoside	GABA Receptor	Inflammation/Immunology Neurological Disease
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GAB_AA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.

HY-10683

PKI-402	PI3K mTOR	Cancer
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC₅₀=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).

HY-16903

PKC-IN-1	PKC	Inflammation/Immunology
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with K_is of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC₅₀s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

HY-128872

EHP-101 VCE-004.8	PPAR Cannabinoid Receptor HIF/HIF Prolyl-Hydroxylase	Metabolic Disease Inflammation/Immunology
EHP-101 (VCE-004.8) is an orally active, specific PPARγ and CB₂ receptor dual agonist. EHP-101 inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. EHP-101, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

HY-N7687

Caulophyllogenin	PPAR	Metabolic Disease Inflammation/Immunology
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC₅₀ of 12.6 μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation.

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-P1847A

IKKγ NBD Inhibitory Peptide TFA	NF-κB	Inflammation/Immunology
IKKγ NBD Inhibitory Peptide TFA is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.

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-10115

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

HY-10115A

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

HY-13928

GW0742 GW610742	PPAR	Metabolic Disease Inflammation/Immunology Cardiovascular Disease Cancer
GW0742 is a potent PPARβ and PPARδ agonist, with an IC₅₀ of 1 nM for human PPARδ in binding assay, and EC₅₀s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

HY-15900

Voxtalisib XL765; SAR245409	PI3K mTOR	Cancer
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC₅₀s=39, 113, 9 and 43 nM for p110α, p110β, *p110γ* and p110δ, respectively), also inhibits DNA-PK (IC₅₀=150 nM) and mTOR (IC₅₀=157 nM). Voxtalisib (XL765) inhibits *mTORC1* and mTORC2 with IC₅₀s of 160 and 910 nM, respectively.

HY-108642

AMG-548	p38 MAPK Casein Kinase	Inflammation/Immunology
AMG-548, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

HY-120327

KY-226	Phosphatase	Metabolic Disease Neurological Disease
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC₅₀ of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.

HY-10195B

Ruboxistaurin hydrochloride LY 333531 hydrochloride	PKC	Metabolic Disease
Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is a selective and ATP-competitive PKCβ inhibitor with IC₅₀s of 4.7 nM and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin hydrochlorid shows less potent inhibition on PKCη (IC₅₀, 52 nM), PKCα (IC₅₀, 360 nM), PKCγ (IC₅₀, 300 nM), PKCδ (IC₅₀, 250 nM), and has no effect on PKCζ (IC₅₀, >100 μM).

HY-16585

VS-5584 SB2343	PI3K mTOR	Cancer
VS-5584 is a pan-PI3K/mTOR kinase inhibitor with IC₅₀s of 16 nM, 68 nM, 42 nM, 25 nM, and 37 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively. VS-5584 simultaneously blocks mTORC2 as well as *mTORC1*.

HY-114495

Caerulomycin A Cerulomycin; Caerulomycin	Fungal Antibiotic	Infection Inflammation/Immunology
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.

HY-108523

LG100754 UVI 2112	RAR/RXR	Metabolic Disease
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.

HY-129636A

GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM.

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-13866

Ro 31-8220 mesylate Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate	PKC	Neurological Disease Cardiovascular Disease Cancer
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

HY-108601A

Ro 32-0432 hydrochloride	PKC	Inflammation/Immunology Neurological Disease
Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC₅₀ values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.

HY-13866A

Ro 31-8220 Bisindolylmaleimide IX	PKC	Neurological Disease Cardiovascular Disease
Ro 31-8220 is a potent PKC inhibitor, with IC₅₀s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC₅₀s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

HY-13440

AMG 511	PI3K	Cancer
AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with K_is of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model.

HY-10297

Omipalisib GSK2126458; GSK458	PI3K mTOR Autophagy	Cancer
Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with K_is of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity.

HY-108642B

AMG-548 dihydrochloride	p38 MAPK Casein Kinase	Inflammation/Immunology
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (K_i=0.5 nM), shows slightly selective over p38β (K_i=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC₅₀=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.

HY-N0600

Ginsenoside F3	Interleukin Related IFNAR	Inflammation/Immunology
Ginsenoside F3, a component of PPTGs (an minor saponin in the leaves of Panax ginseng), has immunoenhancing activity by regulating production and gene expression of type 1 cytokines (IL-2, IFN-gamma) and type 2 cytokines (IL-4 and IL-10).

HY-10626

T0901317	LXR FXR ROR Apoptosis	Cancer Metabolic Disease Cardiovascular Disease
T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

HY-11068

SB 239063	p38 MAPK Autophagy	Inflammation/Immunology
SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC₅₀ of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.

HY-18980

Rottlerin Mallotoxin; NSC 56346; NSC 94525	PKC Autophagy Apoptosis	Infection Cancer
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC₅₀ values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.

HY-N0393

Glabridin	PPAR Reactive Oxygen Species Bacterial	Cancer Infection Inflammation/Immunology
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC₅₀ of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.

HY-B0719

Ingenol Mebutate Ingenol 3-angelate; PEP005	PKC	Cancer Inflammation/Immunology
Ingenol Mebutate is an active ingredient in Euphorbia peplus, acts as a potent PKC modulator, with K_is of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively, and has antiinflammatory and antitumor activity.

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-12513

Samotolisib LY3023414	PI3K DNA-PK mTOR Autophagy	Cancer
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and *mTORC1/2* with IC₅₀s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits *mTORC1/2 at low nanomolar concentrations.*

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-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-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-14913

Apricitabine SPD754; AVX754	Nucleoside Antimetabolite/Analog HIV DNA/RNA Synthesis	Infection
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (K_i=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with K_i value of 300 μM, 12 μM, and 112.25 μM, respectively. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection^[2].

HY-136065A

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

HY-136065

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

HY-N6776

Penitrem A	Potassium Channel	Cancer Neurological Disease
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.

HY-Y0839

Levulinic acid 4-Oxovaleric acid; Laevulinic acid; Levulic acid; NSC 3716; β-Acetylpropionic acid; γ-Ketovaleric acid	Endogenous Metabolite	Others
Levulinic acid is a precursor for the synthesis of biofuels, such as ethyl levulinate.

HY-113456

Leukotriene D4	Drug Metabolite
Leukotriene D4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) produced by the metabolism of LTC4 by γ-glutamyl transpeptidase. Leukotriene D4 is the first cysteinyl-leukotriene metabolite of LTC4. Leukotriene D4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute hypersensitivity.

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-100369A

DMCM hydrochloride	GABA Receptor	Neurological Disease
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with K_is of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.

HY-129636

(E)-GABAB receptor antagonist 1	GABA Receptor	Neurological Disease
(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist 1. GABAB receptor antagonist 1 (compound 14) is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors. (E)-GABAB receptor antagonist 1 decreases GABA-induced IP3 (inositol trisphosphate) production with IC₅₀ of 37.9 μM.

HY-W012123

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

HY-13246

Apitolisib GDC-0980; GNE 390; RG 7422	PI3K mTOR Apoptosis	Cancer
Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC₅₀s of 5 nM/27 nM/7 nM/14 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ, and with a K_i of 17 nM for mTOR.

HY-15346

Copanlisib BAY 80-6946	PI3K	Cancer
Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC₅₀s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity.

HY-15346A

Copanlisib dihydrochloride BAY 80-6946 dihydrochloride	PI3K	Cancer
Copanlisib dihydrochloride (BAY 80-6946 dihydrochloride) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC₅₀s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib dihydrochloride has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib dihydrochloride has superior antitumor activity.

HY-12783

SCH 50911 hydrochloride	GABA Receptor	Neurological Disease
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM.

HY-13717

AGN194204 IRX4204; NRX194204; VTP 194204	RAR/RXR Apoptosis	Cancer Inflammation/Immunology
AGN194204 (IRX4204) is an orally active and selective RXR agonist with K_d values 0.4 nM, 3.6 nM and 3.8 nM and EC₅₀s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.

HY-12783A

SCH 50911	GABA Receptor	Neurological Disease
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC₅₀ of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated ³H overflow with an IC₅₀ of 3 μM.

HY-B2163

Astaxanthin	PPAR Reactive Oxygen Species	Cancer Cardiovascular Disease
Astaxanthin, a red dietary carotenoid isolated from Haematococcus pluvialis, is a modulator of PPARγ and a potent antioxidant with antiproliferative, neuroprotective and anti-inflammatory activity. Astaxanthin has potential in the study of various diseases, such as cancers and Parkinson’s disease, cardiovascular disease. Due to its bright red colour, Astaxanthin could be used as a food colorant in animal feeds.

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-41982

D-Glucuronic acid lactone D-Glucurono-6,3-lactone; D-Glucurono-γ-lactone; D-Glucuronolactone; Dicurone; Glucoxy; Glucurolactone; Glucurone	Endogenous Metabolite	Metabolic Disease
D-Glucuronic acid lactone is an endogenous metabolite.

HY-N0222

Avicularin	Others	Cancer Inflammation/Immunology
Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.

HY-N2453

Convallatoxin	PPAR NF-κB P-glycoprotein	Cancer Inflammation/Immunology
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.

HY-N0407

Picroside I 6'-Cinnamoylcatalpol	STAT	Inflammation/Immunology
Picroside I is the major ingredient of Picrorhiza kurroa. Picrorhiza kurroa is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.

HY-11052A

Trap-101 hydrochloride	Opioid Receptor	Neurological Disease
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHO_hNOP membranes with pK_i values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.

HY-P2141A

TRV-120027 TFA	Angiotensin Receptor	Cardiovascular Disease
TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.

HY-10233

Gaboxadol hydrochloride Lu 02-030 hydrochloride; THIP hydrochloride	GABA Receptor	Neurological Disease
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP hydrochloride) is a potent agonist of the GABA_A receptor and an antagonist of GABA_C receptors (IC₅₀=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED₅₀ value of 143 µM, a full agonist efficacy at α5 subunit (ED₅₀=28-129 µM) and a superagonist efficacy at α4β3δ (ED₅₀=6 µM). Gaboxadol hydrochloride is a non-opioid analgesic and has hypnotic activities.

HY-108568

15-Deoxy-Δ-12,14-prostaglandin J2 15d-PGJ2; 15-Deoxy-Δ12,14-PGJ2	PPAR Endogenous Metabolite	Cancer Inflammation/Immunology Neurological Disease
15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC₅₀ of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC₅₀ of 7 μM.

HY-32015

Cot inhibitor-1
MAP3K Cancer

Cot inhibitor-1 is a COT/Tpl2 inhibitor.

HY-136121

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

HY-112812

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

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

HY-B0552A

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

HY-112911

Endothelial lipase inhibitor-1
Others Cardiovascular Disease

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

Dibucaine
Cinchocaine
Sodium Channel Neurological Disease

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

HY-18353

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

HY-112722

Neurotoxin Inhibitor
Others Neurological Disease

Neurotoxin Inhibitor is a neurotoxin inhibitor.
HY-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-D0843

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

HY-13278A

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

HY-111412

DAAO inhibitor-1
Others Neurological Disease

DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC₅₀ of 0.12 μM.
HY-70005

CPA inhibitor
Carboxypeptidase inhibitor
Carboxypeptidase Metabolic Disease

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

Cysteine Protease inhibitor hydrochloride
Cathepsin Others

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

Cysteine Protease inhibitor
Cathepsin Others

Cysteine Protease inhibitor is an inhibitor of cysteine protease.

HY-21141

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

HY-112914

mTOR inhibitor-1
mTOR Autophagy Cancer

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

HY-128703

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

HY-110101

ARN272
Others Neurological Disease

ARN272 is an anandamide transport inhibitor.
HY-12202

MEK inhibitor
MEK Cancer

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

Allylthiourea
Thiosinamine; N-Allylthiourea
Reactive Oxygen Species Metabolic Disease

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

Tyrosine kinase inhibitor
c-Met/HGFR Cancer

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

Gabexate mesylate
FOY
Factor Xa Proteasome Inflammation/Immunology

Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
HY-128722

HIV-1 inhibitor-3
HIV Infection

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

HY-136660

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

HY-P0017

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

HY-112843

CNT2 inhibitor-1
Others Others

CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC₅₀ of 640 nM for hCNT2.
HY-15182

Collagen proline hydroxylase inhibitor-1
Others Cancer

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

Tyrphostin AG 112
EGFR Cancer

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

ALK inhibitor 2
ALK Cancer

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

Itopride hydrochloride
HSR803
AChE Neurological Disease

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

ALK inhibitor 1
ALK Cancer

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

HY-136279

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

HY-101297

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

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

HY-100732

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

HY-136920

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

HY-13973A

GSK-3 inhibitor 1
GSK-3 Metabolic Disease

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

HY-104051

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

HY-111347A

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

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

Homo Sildenafil
Phosphodiesterase (PDE) Endocrinology

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

CG347B
HDAC Cancer

CG347B is a selective HDAC6 inhibitor.
HY-15444

D159687
Phosphodiesterase (PDE) Neurological Disease

D159687 is a selective PDE4D inhibitor.
HY-119937

ROCK inhibitor-2
ROCK Inflammation/Immunology Cardiovascular Disease

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

HY-15253

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

HY-13662

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

HY-13662A

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

HY-112390A

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

HY-114317

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

HY-15002

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

HY-135826

Necroptosis-IN-1
RIP kinase Cancer

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

EOAI3402143
Deubiquitinase Cancer

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

HY-N2033

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

HY-100463

TPI-1
Phosphatase Inflammation/Immunology Cancer

TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC₅₀ of 40 nM.
HY-B0884

Minaprine
Monoamine Oxidase Neurological Disease

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

MAT2A inhibitor 2
Others Cancer

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

HY-B0884A

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

HY-15167

Glyoxalase I inhibitor
Others Cancer

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

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

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

Propaquizafop
Acetyl-CoA Carboxylase Others

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

PDE4 inhibitor intermediate 1
Others Others

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

IRAK inhibitor 2
IRAK Inflammation/Immunology

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

HY-B0218

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

HY-106067A

Dazoxiben
Prostaglandin Receptor Inflammation/Immunology

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

HY-112607

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

HY-124798

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

HY-32018

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

HY-N6717

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

HY-17542

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

HY-15760

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

HY-N1504

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

HY-15604

AZD1208
Pim Autophagy Apoptosis Cancer

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

Doxycycline
MMP Bacterial Parasite Antibiotic Infection

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

Collagen proline hydroxylase inhibitor
Others Cancer

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

HY-U00387

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

HY-107986

GNE-6776
Deubiquitinase Cancer

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

AKT Kinase Inhibitor
Akt Cancer

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

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

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

Doxycycline hydrochloride
MMP Bacterial Antibiotic Infection

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

NBTGR
Others Cardiovascular Disease

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

Nav1.7 inhibitor
Sodium Channel Neurological Disease

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

Elacridar hydrochloride
GF120918A
P-glycoprotein Cancer

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

Ganoderal A
Others Metabolic Disease

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

Dantrolene sodium
F 440
Calcium Channel Metabolic Disease

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

TNP-470
AGM-1470
Aminopeptidase Cancer Cardiovascular Disease

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

Linderene acetate
Others Inflammation/Immunology

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

Lipid peroxidation inhibitor 1
Others Neurological Disease

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

IWP L6
Porcn Inhibitor III
Porcupine Cancer

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

Lck Inhibitor
Src Inflammation/Immunology

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

HY-13718

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

HY-112269

Glutaminyl Cyclase Inhibitor 1
Amyloid-β Neurological Disease

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

Dapagliflozin impurity
Others Others

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

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

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

HY-10217

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

HY-P1029

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

HY-13662B

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

HY-104032

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

HY-10172

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

HY-136270

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

HY-103310

MRS1845	Calcium Channel CRAC Channel	Cardiovascular Disease
MRS1845 is a selective store-operated calcium (SOC) channel inhibitor with an IC₅₀ of 1.7 μM. MRS1845 is an *ORAI1* inhibitor.

HY-B0083

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

HY-101474A

Zanubrutinib
BGB-3111
Btk Cancer

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

HY-16569

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

HY-N7592

Arjunetin
Others Others

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

HY-12186

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

HY-W008923

Doxycycline monohydrate
MMP Bacterial Parasite Antibiotic Infection

Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
HY-12238

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

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

KNK437
Heat Shock Protein Inhibitor I
HSP Cancer

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

tert-Buthyl Pitavastatin
Drug Metabolite Cardiovascular Disease

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

Voclosporin
ISAtx-247
Phosphatase Inflammation/Immunology

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

HY-122856

AZ12601011	TGF-β Receptor	Cancer
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC₅₀ of 18 nM and a K_d of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, *TGFBR1, and ALK7. AZ12601011 inhibits* mammary tumor growth ^[1].

HY-100933

MY-5445
Phosphodiesterase (PDE) Cardiovascular Disease

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

HY-A0276

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

HY-N0518

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

HY-16657

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

HY-19931

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

HY-119808

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

HY-128729

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

HY-P1260

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

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

ML241 hydrochloride
p97 Cancer

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

Anastrozole
ZD1033
Aromatase Cancer

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

Nor-Acetildenafil
Others Others

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

Delamanid
OPC-67683
Bacterial Antibiotic Cancer

Delamanid, a newer mycobacterial cell wall synthesis inhibitor, inhibits the synthesisi of mucolic acids.
HY-W013478

PTP inhibitor 1
Phosphatase Cancer

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

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

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

RG13022
Tyrphostin RG13022
EGFR Cancer

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

Nitrofen
Others Cancer

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

Picfeltarraegenin X
AChE Neurological Disease

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

ML240
p97 Cancer

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

Aristeromycin
Bacterial Cancer Infection

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

BGG463
K03859
CDK Others

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

Isoginkgetin
MMP Cancer

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

Polyoxin D
Polyoxorim
Fungal Antibiotic Infection

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

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

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

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

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

Toloxatone
MD 69276
Monoamine Oxidase Neurological Disease

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

HY-17396

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

HY-14440

MP7
PDK1 inhibitor
PDK-1 Cancer

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

DGAT-1 inhibitor 2
Acyltransferase Metabolic Disease

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

HY-U00145

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

HY-116770

PFM01
Others Cancer

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

HY-13417A

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

HY-113951

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

HY-124718

p32 Inhibitor M36
M36
PKC Cancer

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

HY-13417

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

HY-P2478

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

HY-P2477

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

HY-10917

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

HY-B0113A

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

HY-10255A

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

HY-111429

YAP/TAZ inhibitor-1
YAP Cancer

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

HY-120859

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

HY-118355

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

HY-N0565B

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

HY-15699A

SAR7334 hydrochloride
TRP Channel Neurological Disease

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

Chlorobenzuron
Others Others

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

Ganoderic acid A
Apoptosis Autophagy Endogenous Metabolite Cancer

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

Glyoxalase I inhibitor free base
Others Cancer

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

SIRT5 inhibitor 1
Sirtuin Others

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

Daclatasvir Impurity C
Others Others

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

Mutant IDH1 inhibitor
Isocitrate Dehydrogenase (IDH) Cancer

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

SAR7334
TRP Channel Neurological Disease

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

Phenthoate
AChE Neurological Disease

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

HY-B1596

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

HY-P1260A

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

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

LCL521 dihydrochloride
Phospholipase Cancer

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

LCL521
Phospholipase Cancer

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

HY-I0637

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

HY-16187

EL-102
HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer

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

Daclatasvir Impurity B
Others Others

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

HY-D0886

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

HY-18965

TAS-301
PKC Cardiovascular Disease

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

AZ191
DYRK Cancer

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

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

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

HIV-1 integrase inhibitor 8
HIV Integrase Infection

HIV-1 integrase inhibitor 8 is a HIV-1 integrase inhibitor, compound 8.
HY-N7511

O-Nornuciferine
Potassium Channel Metabolic Disease

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

Arjungenin
Others Metabolic Disease

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

Fluazifop-P-butyl
Acetyl-CoA Carboxylase Metabolic Disease

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

Stattic
STAT Apoptosis Cancer Inflammation/Immunology

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

GSK2256098
FAK Apoptosis Cancer

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

FK 3311
COX-2 Inhibitor V
COX Inflammation/Immunology

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

CGP60474
VEGFR PKC Cancer

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

4μ8C
IRE1 Inhibitor III
IRE1 Metabolic Disease

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

ON-013100
CDK Cancer

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

ZL006
iGluR Neurological Disease

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

LRRK2 inhibitor 1
LRRK2 Neurological Disease

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

HY-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-100932

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

HY-B0113

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

HY-50706A

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

HY-105917

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

HY-10326

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

HY-P0118

Disitertide P144	TGF-beta/Smad PI3K	Cancer
Disitertide (P144) is a peptidic TGFβ1 inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor.

HY-13228

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

HY-10227

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

HY-10255

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

HY-17367

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

HY-22166

Glycolic acid oxidase inhibitor 1
Others Metabolic Disease

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

4-Hydroxy-3,3-dimethylcyclohexanone
Others Others

4-Hydroxy-3,3-dimethylcyclohexanone is a key intermediate for the synthesis of hAChE inhibitor.
HY-112451

cFMS Receptor Inhibitor II
c-Fms Inflammation/Immunology

cFMS Receptor Inhibitor II is a CSF1R kinase inhibitor. CSF-1 is a cytokine.
HY-15217

CHR-6494
Haspin Kinase Cancer

CHR-6494 is a potent inhibitor of haspin, inhibiting histone H3T3 phosphorylation, with an IC₅₀ of 2 nM.
HY-13902

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

Berzosertib (VE-822) is an ATR inhibitor with a K_i value of less than 0.2 nM. It also inhibits ATM with a K_i of 34 nM.
HY-15859

Atglistatin
ATGL Metabolic Disease

Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC₅₀ of 0.7 μM in vitro.

HY-77521

Dabigatran ethyl ester hydrochloride	Thrombin	Cardiovascular Disease
Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC₅₀ value of 0.8 μM and a thrombin inhibitor.

HY-13502

Mitoxantrone
mitozantrone
Topoisomerase PKC Cancer

Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM.

HY-107994

Aminooxyacetic acid hemihydrochloride Carboxymethoxylamine Hemihydrochloride	GABA Receptor	Cancer
Aminooxyacetic acid hemihydrochloride is a malate-aspartate shuttle (MAS) inhibitor which also inhibits the GABA degradating enzyme GABA-T.

HY-N2567

(±)-Decursinol
Bacterial Cancer

(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC₅₀ of 102 μM.
HY-13278

IRAK inhibitor 4
IRAK Inflammation/Immunology

IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4(IRAK4) inhibitor.

HY-112860

Asp-AMS	Aminoacyl-tRNA Synthetase Mitochondrial Metabolism	Metabolic Disease
Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.

HY-12000

AG-490
Tyrphostin AG 490
EGFR STAT Autophagy Cancer

AG-490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

HY-A0116S

Trandolaprilate D5 Trandolaprilat D5; RU 44403 D5	Angiotensin-converting Enzyme (ACE)	Cardiovascular Disease
Trandolaprilate D5 is a deuterium labeled Trandolaprilate (Trandolaprilat). Trandolaprilate is an angiotensin-converting enzyme (ACE) inhibitor.

HY-13060

ACHP Hydrochloride
IKK-2 Inhibitor VIII
IKK Inflammation/Immunology

ACHP Hydrochloride (IKK-2 Inhibitor VIII) is a highly potent and selective IKK-β inhibitor with an IC₅₀ of 8.5 nM.
HY-101474

(±)-Zanubrutinib
(±)-BGB-3111
Btk Cancer

(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
HY-19731

SID 3712249
MiR-544 Inhibitor 1
MicroRNA Apoptosis Cancer

SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544).

HY-B0392

(S)-(+)-Rolipram (+)-Rolipram; (S)-Rolipram	Phosphodiesterase (PDE) Apoptosis	Inflammation/Immunology Cancer
(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R enantiomer.

HY-101462

RAD51 Inhibitor B02
B02
RAD51 Apoptosis Cancer

RAD51 Inhibitor B02 (B02) is an inhibitor of human RAD51 with an IC₅₀ of 27.4 μM.

HY-B0902A

Rufloxacin hydrochloride MF-934 hydrochloride	Bacterial	Infection
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.

HY-101963

AD80
Raf Src Ribosomal S6 Kinase (RSK) RET Cancer

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
HY-70073

Zaurategrast
CT7758
Integrin Inflammation/Immunology

Zaurategrast (CT7758) is a potent and oral-effective α₄-integrin inhibitor.
HY-15775

Arginase inhibitor 1
Arginase Cancer

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC₅₀s of 223 and 509 nM, respectively.

HY-13502A

Mitoxantrone dihydrochloride mitozantrone dihydrochloride	Topoisomerase PKC	Cancer
Mitoxantrone dihydrochloride is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM.

HY-70003

Carboxypeptidase G2 (CPG2) Inhibitor
CPG2 Inhibitor
Carboxypeptidase Cancer

Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
HY-112720

AGL-2263
Insulin Receptor Metabolic Disease Endocrinology

AGL-2263 is an insulin receptor and insulin-like growth factor (IGF) receptor inhibitor.
HY-111784

CBP-IN-1
Epigenetic Reader Domain Cancer

CBP-IN-1 is a potent p300/CBP bromodomain inhibitor.

HY-12031A

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

HY-U00453

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

HY-112910

Grp94 Inhibitor-1
HSP Cancer Infection

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

HY-15339

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

HY-13984

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

HY-P0118A

Disitertide TFA P144 TFA	TGF-beta/Smad PI3K	Cancer
Disitertide (P144) TFA is a peptidic TGFβ1 inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor.

HY-10439

HPGDS inhibitor 1	PGE synthase	Inflammation/Immunology
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC₅₀s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.

HY-100816

Rbin-1 Ribozinoindole-1	Phosphatase	Metabolic Disease
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI₅₀ of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).

HY-120675

SSTC3	Casein Kinase Wnt	Cancer
SSTC3 is a casein kinase 1α (CK1α) activator (K_d = 32 nM) that inhibits WNT signaling (EC₅₀ = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.

HY-100556

Tie2 kinase inhibitor 1	Others	Cancer
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC₅₀ of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.

HY-112715

ATP synthase inhibitor 1	ATP Synthase	Cardiovascular Disease
ATP synthase inhibitor 1 is a potent inhibitor of *c subunit of the F₁/F_O-ATP* synthase** complex, inhibits mitochondrial permeability transition pore (mPTP) opening, does not affect ATP levels.

HY-14165

Veliflapon BAY X 1005; DG-031	FLAP Leukotriene Receptor	Inflammation/Immunology Cardiovascular Disease
Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

HY-128918

SIS17	HDAC	Others
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC₅₀ value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.

HY-P1111

Lyn peptide inhibitor	Src Interleukin Related	Inflammation/Immunology
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

HY-100932A

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

HY-135318

NBDHEX	Glutathione Peroxidase Apoptosis Autophagy	Cancer
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the *GSTP1-1* and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.

HY-121172

1,4-DPCA	HIF/HIF Prolyl-Hydroxylase	Cancer
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC₅₀ of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits *factor inhibiting* HIF (FIH) with an IC₅₀** of 60 μM.

HY-12364

C75
Fatty Acid Synthase (FASN) Cancer

C75 is a synthetic fatty-acid synthase (FASN) inhibitor; inhibits prostate cancer cells PC3 with an IC₅₀ of 35 μM.
HY-P0081

Bax inhibitor peptide V5
BIP-V5; BAX Inhibiting Peptide V5
Bcl-2 Family Cancer

Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
HY-133110

Afatinib N-Oxide
Others Others

Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
HY-15798

UNC2881
TAM Receptor Cardiovascular Disease

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.
HY-114418

MMP3 inhibitor 1
MMP Cancer

MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC₅₀ of 1 nM.
HY-N5038

Mauritianin
Topoisomerase Cancer

Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.

HY-13606

Dacinostat NVP-LAQ824; LAQ824	HDAC Autophagy	Cancer
Dacinostat is a potent HDAC inhibitor, with an IC₅₀ of 32 nM; Dacinostat also inhibits *HDAC1* with an IC₅₀ of 9 nM, and used in cancer research.

HY-13256

Desmethyl Erlotinib hydrochloride OSI-420; CP-373420 hydrochloride	Drug Metabolite	Cancer
Desmethyl Erlotinib hydrochloride (OSI-420) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.

HY-P1452A

RNAIII-inhibiting peptide(TFA)	Bacterial	Infection
RNAIII-inhibiting peptide(TFA) is a potent inhibitor of Staphylococcus aureus, effective in the diseases such as cellulitis, keratitis, septic arthritis, osteomylitis and mastitis.

HY-Y0882

Hydroxyamine hydrochloride	Monoamine Oxidase	Cardiovascular Disease
Hydroxyamine hydrochloride is a selective monoamine oxidase (MAO) inhibitor used for inhibiting of platelet aggregation. Hydroxyamine hydrochloride is an intermediate of organic synthesis.

HY-16420

R112
Syk Inflammation/Immunology

R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
HY-15588

L189
DNA/RNA Synthesis Cancer

L189 is a novel human DNA ligase inhibitor, inhibits hLigI/III/IV with IC50 of 5/9/5 μM.
HY-B0830

Isoprocarb
AChE Neurological Disease

Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
HY-N1502

Carboxyatractyloside
Gummiferin
Others Cancer

Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.

HY-12054A

Hesperadin hydrochloride	Aurora Kinase Autophagy Influenza Virus Parasite	Cancer
Hesperadin hydrochloride is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin hydrochloride inhibits Aurora B with an IC₅₀ of 250 nM.

HY-114423

p38α inhibitor 1
p38 MAPK Autophagy Inflammation/Immunology

p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.

HY-10809

Bitopertin RG1678; RO4917838	GlyT	Neurological Disease
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human *GlyT1* with a concentration exhibiting IC50 of 25 nM.

HY-131268

O-Desisobutyl-O-n-propyl Febuxostat
Xanthine Oxidase Metabolic Disease

O-Desisobutyl-O-n-propyl Febuxostat, extracted from the patent CN 103467412, is an xanthine oxidase inhibitor.
HY-N6619A

Lycoramine
AChE Neurological Disease

Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
HY-104028

BAY 73-6691
(R)-BAY 73-6691
Phosphodiesterase (PDE) Neurological Disease

BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
HY-12814

TH588
DNA/RNA Synthesis Cancer

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC₅₀= 5 nM).

HY-12054

Hesperadin	Aurora Kinase Autophagy Influenza Virus Parasite	Cancer
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC₅₀ of 250 nM.

HY-12420

JNJ-47117096 hydrochloride MELK-T1 hydrochloride	MELK FLT3	Cancer
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC₅₀ of 23 nM, also effectively inhibits Flt3, with an IC₅₀ of 18 nM.

HY-16982

Cercosporamide (-)-Cercosporamide	Fungal MNK	Cancer Infection
Cercosporamide is a highly potent, ATP-competitive *Pkc1* kinase inhibitor, with an IC₅₀ of <50 nM and a K_i of <7 nM. Cercosporamide is a unique Mnk inhibitor.

HY-136347

3α-Hydroxy pravastatin sodium	HMG-CoA Reductase (HMGCR) Drug Metabolite	Cardiovascular Disease
3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor.

HY-13280

IRAK inhibitor 6
IRAK Inflammation/Immunology

IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4) with IC₅₀ of 160 nM.
HY-103002

SU5408
VEGFR2 Kinase Inhibitor I
VEGFR Cardiovascular Disease

SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC₅₀ of 70 nM.

HY-B0497B

Niclosamide monohydrate BAY2353 monohydrate	STAT Bacterial Antibiotic	Infection
Niclosamide monohydrate is an inhibitor of STAT3 with IC₅₀ of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.

HY-131446

Chk1-IN-5	Checkpoint Kinase (Chk)	Cancer
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.

HY-50202

Etomoxir (R)-(+)-Etomoxir	Apoptosis	Cancer Metabolic Disease
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

HY-19727A

FOY 251	Ser/Thr Protease SARS-CoV	Metabolic Disease
FOY 251 is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.FOY 251 inhibit SARS-CoV-2 infection in cells assay.

HY-50202A

Etomoxir sodium salt (R)-(+)-Etomoxir sodium salt	Apoptosis	Metabolic Disease Cancer
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.

HY-124416

ML604086	CCR	Inflammation/Immunology Endocrinology
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca²⁺ concentrations.

HY-103490

Takinib	MAP3K Apoptosis	Cancer
Takinib is a potent and selective *TAK1* inhibitor with an IC₅₀ of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.

HY-17367A

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

HY-122866

ZT-12-037-01	Ras	Cancer
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC₅₀ of 24 nM.

HY-100899

Heparastatin
Others Metabolic Disease

Heparastatin is a heparanase inhibitor.
HY-101705

Tibenelast sodium
LY 186655
Phosphodiesterase (PDE) Inflammation/Immunology

Tibenelast sodium is a phosphodiesterase inhibitor.
HY-14807

Tosedostat
CHR-2797
Aminopeptidase Cancer

Tosedostat is an aminopeptidase inhibitor.

HY-15766A

GNE-617 hydrochloride	Nampt	Cancer
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

HY-15233

Letermovir AIC246	CMV	Infection
Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

HY-12399

MKC9989
IRE1 Cancer

MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC₅₀ of 0.23 to 44 μM.

HY-101053

Src Inhibitor 1 Src Kinase Inhibitor 1; Src-l1	Src	Cancer
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC₅₀ values of 44 nM for Src and 88nM for Lck.

HY-10247

BRAF inhibitor
Raf Cancer

BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.

HY-N2522

Carboxyatractyloside dipotassium Gummiferin dipotassium	Others	Others
Carboxyatractyloside dipotassium is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.

HY-109565

ASTX660
IAP Cancer

ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
HY-108820

HIV-1 integrase inhibitor 4
HIV Integrase HIV Infection

HIV-1 integrase inhibitor 4 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 3.7 nM.
HY-108817

HIV-1 integrase inhibitor 3
HIV Integrase HIV Infection

HIV-1 integrase inhibitor 3 is a HIV-1 integrase strand transfer (INST) inhibitor with an IC₅₀ of 2.7 nM.

HY-10978

Crisaborole AN-2728; PF-06930164	Phosphodiesterase (PDE)	Inflammation/Immunology
Crisaborole (AN-2728) is a potent inhibitor of PDE4 and cytokine release; inhibit PDE4 with an IC₅₀ of 0.49 μM.

HY-13452

CID-1067700
ML282
Ras Inflammation/Immunology

CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a K_i of 13 nM.
HY-119459

Fluopyram
Fungal Infection

Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC₅₀ of 3.35 µg/mL.
HY-135383A

(3S,5R)-Pitavastatin calcium
Others Metabolic Disease

(3S,5R)-Pitavastatin cacium is the enantiomer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

HY-17469

Gimeracil Gimestat	Others	Cancer
Gimeracil(Gimestat) is an inhibitor of dihydropyrimidine dehydrogenase (DPYD), which degrades pyrimidine including 5-fluorouracil in the blood; inhibits homologous recombination.

HY-A0122

Plicamycin Mithramycin A	DNA/RNA Synthesis Bacterial Antibiotic	Cancer Infection
Plicamycin is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.

HY-17381

Idarubicin hydrochloride 4-Demethoxydaunorubicin hydrochloride	Topoisomerase Bacterial Fungal Autophagy	Cancer Infection
Idarubicin hydrochloride is an anthracycline antileukemic drug. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.

HY-N6031

Dendrophenol
NF-κB Cancer

Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.

HY-Y0172

Butylated hydroxytoluene	Ferroptosis	Cancer
Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products. Butylated hydroxytoluene is a Ferroptosis inhibitor.

HY-108941

Salicyl-AMS
Bacterial Infection

Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.

HY-15282

E-64 Proteinase inhibitor E 64	Cathepsin Autophagy Bacterial	Inflammation/Immunology Cancer
E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

HY-B0806

Proguanil	Parasite Antifolate	Infection
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.

HY-N2597

Prunetin	Aldehyde Dehydrogenase (ALDH)	Inflammation/Immunology
Prunetin, an O-methylated isoflavone, possesses anti-inflammatory activity. Prunetin is a potent human aldehyde dehydrogenases inhibitor.

HY-B0806A

Proguanil hydrochloride	Parasite Antifolate	Infection
Proguanil hydrochloride, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil hydrochloride is a dihydrofolate reductase (DHFR) inhibitor.

HY-13420

Zebularine NSC309132; 4-Deoxyuridine	DNA Methyltransferase Autophagy	Cancer
Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a K_i of 0.95 μM.

HY-100736

ML348
GNF-Pf-1127
Phospholipase Cancer

ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC₅₀ of 210 nM, and barely inhibits LYPLA2.
HY-15202

Binimetinib
MEK162; ARRY-162; ARRY-438162
MEK Autophagy Cancer

Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC₅₀ of 12 nM.
HY-18988

ETC-159
ETC-1922159
Wnt Cancer

ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC₅₀ of 2.9 nM.
HY-12726

Liproxstatin-1
Ferroptosis Cancer

Liproxstatin-1 is a potent ferroptosis inhibitor and inhibits ferroptotic cell death (IC₅₀=22 nM).

HY-N1724

Concanamycin A Antibiotic X 4357B; Concanamycin; X 4357B	Proton Pump Bacterial Antibiotic	Cancer Infection
Concanamycin A (Antibiotic X 4357B) is a macrolide antibiotic and a specific vacuolar type H⁺-ATPase (V-ATPase) inhibitor.

HY-15766

GNE-617	Nampt	Metabolic Disease Cancer
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC₅₀ of 5 nM and exhibits efficacy in xenograft models of cancer.

HY-111489B

LMPTP INHIBITOR 1 dihydrochloride	Phosphatase	Metabolic Disease
LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC₅₀ of 0.8 μM LMPTP-A.

HY-126253

BI-4916
Others Cancer

BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD⁺-competitive PHGDH inhibitor.
HY-136485

FEN1-IN-4
Others Cancer

FEN1-IN-4 (Compound 2) is a human flap endonuclease-1 (hFEN1) inhibitor.
HY-B1863

Iprobenfos
Fungal Infection

Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.

HY-B0882

Edrophonium chloride	AChE	Neurological Disease
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.

HY-100227

E 64c	Cathepsin SARS-CoV	Metabolic Disease
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.

HY-66004

4-Acetamidophenyl acetate	Others	Inflammation/Immunology
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC₅₀=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

HY-115502

BCI (E)-BCI	Phosphatase	Cancer Inflammation/Immunology
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and *DUSP1* with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.

HY-P1045

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

HY-124653

HSP27 inhibitor J2 J2	HSP	Cancer
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.

HY-P1045A

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

HY-P1111A

Lyn peptide inhibitor TFA	Src Interleukin Related	Inflammation/Immunology
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.

HY-135899

SIRT7 inhibitor 97491	Sirtuin Apoptosis	Cancer
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC₅₀ of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

HY-B2145

Ilaprazole sodium IY-81149 sodium	Proton Pump TOPK	Cancer Inflammation/Immunology
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H⁺/K⁺-ATPase in a dose-dependent manner with an IC₅₀ of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

HY-107412

Proteasome inhibitor IX PS-IX; AM114	Proteasome	Cancer
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC₅₀ value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53^+/+ cells growth inhibitory activity with an IC₅₀ value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.

HY-130795

GSK-3β inhibitor 2	GSK-3	Neurological Disease
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC₅₀ of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.

HY-N7674A

Angoline hydrochloride	STAT	Cancer
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

HY-13624A

Epirubicin hydrochloride 4'-Epidoxorubicin hydrochloride	Topoisomerase Apoptosis	Cancer
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting *Topoisomerase. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3)* inhibitor and inhibits regulatory T cell activity.

HY-P1290

PKA Inhibitor Fragment (6-22) amide PKI-(6-22)-amide	PKA	Neurological Disease
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a K_i of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.

HY-N7674

Angoline	STAT	Cancer
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC₅₀ of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.

HY-109019

Vorolanib CM082; X-82	VEGFR PDGFR	Cancer Cardiovascular Disease
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).

HY-100734

Histone Acetyltransferase Inhibitor II	Histone Acetyltransferase	Cancer
Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC₅₀ of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

HY-123772

CDK5 inhibitor 20-223	CDK	Cancer
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC₅₀s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.

HY-13624

Epirubicin 4'-Epidoxorubicin	Topoisomerase Apoptosis	Cancer
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting *Topoisomerase. Epirubicin is a Forkhead box protein p3 (Foxp3)* inhibitor and inhibits regulatory T cell activity.

HY-N6619

Lycoramine hydrobromide	AChE	Neurological Disease
Lycoramine hydrobromide, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine hydrobromide is a potent acetylcholinesterase (AChE) inhibitor.

HY-109877

Ro 22-3581
4'-(Imidazol-1-yl) acetophenone
Others Cardiovascular Disease

Ro 22-3581 (4'-(Imidazol-1-yl) acetophenone) is a selective thromboxane (Tx) synthetase inhibitor.

HY-100299

RPR107393 free base	Farnesyl Transferase	Metabolic Disease
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC₅₀ of 0.8 nM.

HY-P2470

Human PD-L1 inhibitor II
PD-1/PD-L1 Cancer

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.
HY-B0106

Levetiracetam
UCB L059
mAChR Neurological Disease

Levetiracetam (UCB L059) is a selective M2 muscarinic acetylcholine receptors (mAChR) inhibitor. Antiepileptic agent.
HY-50710

KU-0063794
mTOR Cancer

KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC₅₀s of 10 nM.
HY-137239

1,4-DPCA ethyl ester
HIF/HIF Prolyl-Hydroxylase Cancer

1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
HY-100303A

FR194738
Others Metabolic Disease

FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC₅₀ of 9.8 nM.

HY-50946

Imatinib Mesylate STI571 Mesylate; CGP-57148B Mesylate	c-Kit Bcr-Abl PDGFR Autophagy	Cancer
Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC₅₀=100 nM) tyrosine kinases.

HY-15886

Mdivi-1 Mitochondrial division inhibitor 1	Dynamin Mitophagy Autophagy Apoptosis	Cancer
Mdivi-1 is a selective dynamin-related protein 1 (Drp1) inhibitor. Mdivi-1 is a mitochondrial division/mitophagy inhibitor.

HY-112131

MAT2A inhibitor 1
Others Cancer

MAT2A inhibitor 1 is a methionine adenosyltransferase 2A (MATA2) inhibitor with an IC₅₀ less than l00 nM.
HY-19326

SU1498
AG 1498; Tyrphostin SU 1498
VEGFR Cancer Inflammation/Immunology

SU1498 (AG 1498) is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC₅₀ of value of 700 nM.
HY-12971

Nampt-IN-1
LSN3154567
Nampt Cancer

Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC₅₀ of 3.1 nM.
HY-101479

Iclaprim
AR-100
Bacterial Infection

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

HY-108900A

Leu-AMS R enantiomer	Aminoacyl-tRNA Synthetase	Others
Leu-AMS R enantiomer is the R enatiomer of Leu-AMS. Leu-AMS is a potent inhibitor of leucyl-tRNA synthetase (LRS) and inhibits the growth of bacteria.

HY-N5118

Chimonanthine (-)-Chimonanthine	Tyrosinase	Cancer
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.

HY-U00049

Mioflazine	Others	Neurological Disease Cardiovascular Disease
Mioflazine is an orally active nucleoside transport inhibitor, has the potential for sleep disorders treatment. Mioflazine inhibits nucleoside uptake.

HY-16904

RI-2
RAD51 Cancer

RI-2 is a reversible RAD51 inhibitor, with an IC₅₀ of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
HY-130760

HIV-1 integrase inhibitor 7
HIV Integrase Infection

HIV-1 integrase inhibitor 7 is a potent HIV-1 integrase inhibitor, with an IC₅₀ of 33.3 nM.
HY-103036

BET bromodomain inhibitor
Epigenetic Reader Domain Cancer

BET bromodomain inhibitor is a potent BET inhibitor extracted from patent WO/2015/153871A2, compound example 11.
HY-111410

ATX inhibitor 1
Phosphodiesterase (PDE) Cancer

ATX inhibitor 1 is a potent ATX (IC₅₀=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
HY-13229

BOC-D-FMK
Caspase Cancer

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC₅₀ of 39 µM.
HY-10862

FAAH inhibitor 1
Benzothiazole analog 3
FAAH Autophagy Cancer

FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ of 18±8 nM.

HY-13256A

Desmethyl Erlotinib OSI-420 free base; CP-373420	Drug Metabolite	Cancer
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.

HY-15735

c-Met inhibitor 1	c-Met/HGFR	Cancer
c-Met inhibitor 1 is an inhibitor of the c-Met receptor signaling pathway useful for the treatment of cancer including gastric, glioblastoma, and pancreatic cancer.

HY-10997S

Ibrutinib D5
PCI-32765 D5
Btk Cancer

Ibrutinib D5 (PCI-32765 D5) is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor.
HY-15586

L67
DNA Ligase Inhibitor
DNA/RNA Synthesis Cancer

L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.
HY-B0008

Sulindac
MK-231
COX Autophagy Inflammation/Immunology Cancer

Sulindac (MK-231) is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.

HY-115502A

BCI hydrochloride (E)-BCI hydrochloride	Phosphatase	Cancer Inflammation/Immunology
BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI hydrochloride specifically inhibits DUSP6 and *DUSP1* with EC₅₀s of 13.3 and 8.0 μM in cells, respectively. BCI hydrochloride does not inhibit DUSP5.

HY-12031

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

HY-136538

LQZ-7I	Survivin	Cancer
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.

HY-19727

FOY 251 free base	Ser/Thr Protease SARS-CoV	Metabolic Disease
FOY 251 free base is an anti-proteolytic active metabolite camostate (HY-13512), acts as a proteinase inhibitor.FOY 25 free base inhibit SARS-CoV-2 infection in cells assay.

HY-N2006

Ganoderic acid B	HIV Protease	Infection
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against **HIV-1 protease**.

HY-P1376

G-Protein antagonist peptide	mAChR Adrenergic Receptor
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

HY-114169

WRG-28	Discoidin Domain Receptor	Cancer
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor with an IC₅₀ of 230 nM. WRG-28 uniquely inhibits receptor-ligand interactions via allosteric modulation of the receptor. WRG-28 inhibits tumor invasion and migration, as well as tumor-supporting roles of the stroma, and inhibits metastatic breast tumor cell colonization in the lungs by targeting DDR2.

HY-16592

Brefeldin A BFA; Cyanein; Decumbin	Autophagy CRISPR/Cas9 Mitophagy HSV Antibiotic	Cancer Infection
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits *HSV-1* and has anti-cancer activity.

HY-101664

Ilaprazole IY-81149	Proton Pump TOPK	Cancer Inflammation/Immunology
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H⁺/K⁺-ATPase in a dose-dependent manner with an IC₅₀ of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.

HY-112373

Aurora Kinase Inhibitor 3	Aurora Kinase	Others
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC₅₀ of 42 nM, and weakly inhibits EGFR with an IC₅₀>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures.

HY-135396

(1S,2S)-Bortezomib	Proteasome	Cancer
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (K_i of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.

HY-N0149

Salicin
D-(−)-Salicin; Salicoside
COX Cancer Inflammation/Immunology

Salicin is a natural COX inhibitor.
HY-100263

Metofenazate
Methophenazine
CaMK Autophagy Neurological Disease

Metofenazate is a selective calmodulin inhibitor.
HY-N0342

Scopoletin
Gelseminic acid; Chrysatropic acid
AChE Apoptosis Inflammation/Immunology

Scopoletin is an inhibitor of acetylcholinesterase (AChE).
HY-101244

ZINC00881524
ROCK Cancer

ZINC00881524 is a ROCK inhibitor.
HY-100384

NKL 22
HDAC Cancer

NKL 22 is a HDAC inhibitor.
HY-112870A

AST2818 mesylate
EGFR Cancer

AST2818 mesylate is an EGFR inhibitor.
HY-P0290A

GRGDSP TFA
Integrin Cancer

GRGDSP (TFA) is an integrin inhibitor.

HY-135391

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

HY-50909

Perifosine KRX-0401; NSC 639966; D21266	Akt Autophagy Apoptosis	Cancer
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC₅₀s of 0.6-8.9 μM.

HY-101766

Btk inhibitor 2
BGB-3111 analog
Btk Inflammation/Immunology

Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
HY-16510A

UNC926 hydrochloride
Epigenetic Reader Domain Cancer

UNC926 hydrochloride is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM.

HY-N0143

Phlorizin Floridzin; NSC 2833	SGLT Na+/K+ ATPase	Metabolic Disease
Phlorizin is a non-selective SGLT inhibitor with K_is of 300 and 39 nM for *hSGLT1* and hSGLT2, respectively. Phlorizin is also a Na⁺/K⁺-ATPase inhibitor.

HY-U00096

Ansofaxine hydrochloride LY03005; LPM570065	5-HT Receptor Dopamine Receptor	Inflammation/Immunology Neurological Disease
Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC₅₀ values of 723, 491 and 763 nM, respectively.

HY-B1243

Propoxycaine hydrochloride	Sodium Channel	Neurological Disease
Propoxycaine hydrochloride inhibits voltage-gated sodium channels, and thereby inhibits the ionic flux required for the initiation and conduction of impulses. Propoxycaine hydrochloride application can lead to a loss of sensation.

HY-32351

Calcifediol 25-hydroxy Vitamin D3	VD/VDR Endogenous Metabolite	Metabolic Disease
Calcifediol (25-hydroxy Vitamin D3), a major circulating metabolite of vitamin D3, is a potent VDR inhibitor.

HY-13012

RepSox
E-616452; SJN 2511
TGF-β Receptor Cancer

RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC₅₀ of 4 nM.

HY-N7089

Benzoyleneurea	Bacterial	Infection
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.

HY-18931A

NSC305787 hydrochloride	Others	Cancer
NSC305787 hydrochloride is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

HY-15247

Vistusertib AZD2014	mTOR Autophagy Apoptosis	Cancer
Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC₅₀ of 2.81 nM. AZD2014 inhibits both *mTORC1* and mTORC2 complexes.

HY-16510

UNC926
Epigenetic Reader Domain Cancer

UNC926 is a methyl-lysine (Kme) reader domain inhibitor that inhibits L3MBTL1 with an IC₅₀ of 3.9 μM.
HY-12357

Bempedoic acid
ETC-1002; ESP-55016
ATP Citrate Lyase AMPK Metabolic Disease

Bempedoic acid (ETC-1002) is an ATP-citrate lyase (ACL) inhibitor. Bempedoic acid (ETC-1002) activates AMPK.
HY-101464

ML329
Others Others

ML329 is a micropthalmia-associated transcription factor (MITF) inhibitor, which inhibits TRPM-1 promoter activity with an IC₅₀ of 1.2 μM.

HY-12682

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

HY-102007A

Gamitrinib TPP hexafluorophosphate	HSP	Cancer
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.

HY-100541

INH6
Apoptosis Cancer

INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC₅₀ of 2.4 μM.

HY-32351A

Calcifediol monohydrate 25-hydroxy Vitamin D3 monohydrate	VD/VDR Endogenous Metabolite	Metabolic Disease
Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate), a major circulating metabolite of vitamin D3, is a potent VDR inhibitor.

HY-100735

C 87
TNF Receptor Inflammation/Immunology

C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC₅₀ of 8.73 μM.

HY-13067

Tripterin Celastrol	Proteasome Autophagy Mitophagy Apoptosis	Inflammation/Immunology Cancer
Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM.

HY-15679

PI4KIII beta inhibitor 3
PI4K Cancer

PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC₅₀ of 5.7 nM.
HY-19352

T56-LIMKi
T5601640
LIM Kinase (LIMK) Cancer

T56-LIMKi is a selective inhibitor of LIMK2; inhibits the growth of Panc-1 cells with an IC₅₀ of 35.2 μM.
HY-107433

U18666A
HCV Infection Neurological Disease

U18666A, an intra-cellular cholesterol transport inhibitor, inhibits replication of Ebola virus, dengue virus, and human hepatitis C virus.

HY-126134

HPGDS inhibitor 2	PGE synthase	Inflammation/Immunology
HPGDS inhibitor 2 is a highly potent and selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with an IC₅₀ of 9.9 nM.

HY-18931

NSC305787
Others Cancer

NSC305787 is an inhibitor of ezrin with a K_d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC₅₀ of 8.3 μM, has antitumor activity.

HY-15223

MI-3 Menin-MLL inhibitor 3	Epigenetic Reader Domain Apoptosis	Cancer
MI-3 (Menin-MLL inhibitor 3) is a potent and high affinity menin-MLL inhibitor with an IC₅₀ of 648 nM and a K_d of 201 nM.

HY-15457

Triciribine API-2; NSC 154020; TCN	DNA/RNA Synthesis Akt HIV	Cancer
Triciribine is a DNA synthesis inhibitor, also inhibits Akt and *HIV-1/2* with IC₅₀ of 130 nM, and 0.02-0.46 μM, respectively.

HY-100792

URB602
Others Cancer

URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC₅₀ of 28±4 μM through a noncompetitive mechanism.

HY-112164

IACS-8968 IDO/TDO Inhibitor	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
IACS-8968 (IDO/TDO Inhibitor) is a dual IDO and TDO inhibitor, with pIC₅₀s of 6.43 for IDO and <5 for TDO, respectively.

HY-N7452

Coumermycin A1
JAK Bacterial Metabolic Disease

Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.

HY-P1290A

PKA Inhibitor Fragment (6-22) amide TFA PKI-(6-22)-amide TFA	PKA	Neurological Disease
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a K_i of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.

HY-B0166

L-Ascorbic acid L-Ascorbate; Vitamin C	Calcium Channel Reactive Oxygen Species Apoptosis	Metabolic Disease
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-P0222

PKI(5-24)	PKA	Others
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a K_i of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.

HY-114996

ADAMTS-5 Inhibitor	Others	Inflammation/Immunology
ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC₅₀ of 1.1 µM. ADAMTS-5 Inhibitor shows >40-fold functional selectivity over ADAMTS-4 (aggrecanase-1).

HY-103032

Multi-kinase inhibitor 1	PDGFR c-Kit Bcr-Abl	Cancer
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and *Bcr-abl*.

HY-Y0445A

Sodium dichloroacetate	PDHK Reactive Oxygen Species NKCC Apoptosis	Cancer
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.

HY-66005

Acetaminophen Paracetamol; 4-Acetamidophenol; 4'-Hydroxyacetanilide	COX Histone Acetyltransferase Endogenous Metabolite	Inflammation/Immunology
Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

HY-13512

Camostat mesylate Camostat mesilate; FOY305; FOY-S980	Ser/Thr Protease SARS-CoV	Infection Inflammation/Immunology
Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.

HY-122632

Ciliobrevin D	Hedgehog	Cancer
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro.

HY-16594

Lactacystin	Proteasome	Neurological Disease
Lactacystin, an antibiotic Streptomyces spp. metabolite, is a potent and selective proteasome inhibitor with an IC₅₀ of 4.8 μM for 20S proteasome. Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces neurite outgrowth.

HY-B0166A

L-Ascorbic acid sodium salt Sodium L-ascorbate; Vitamin C sodium salt	Calcium Channel Reactive Oxygen Species Apoptosis	Cancer
L-Ascorbic acid sodium salt (Sodium L-ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt inhibits selectively Ca_v3.2 channels with an IC₅₀ of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.

HY-13803C

Tazemetostat hydrobromide EPZ-6438 hydrobromide; E-7438 hydrobromide	Histone Methyltransferase	Cancer
Tazemetostat hydrobromide (EPZ-6438 hydrobromide) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat hydrobromide inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits Rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat hydrobromide also inhibits EZH1 with an IC₅₀ of 392 nM.

HY-19763

BEBT-908 PI3Kα inhibitor 1	PI3K	Cancer
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an *IC₅₀*<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC₅₀≤1 μM) .

HY-N0822

Shikonin C.I. 75535; Isoarnebin 4	Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV	Cancer
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis.

HY-18979

Lactimidomycin	Influenza Virus	Cancer Infection
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC₅₀ value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities.

HY-23460A

4-Ethynyl-L-phenylalanine hydrochloride	Tryptophan Hydroxylase	Neurological Disease
4-Ethynyl-L-phenylalanine hydrochloride is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine hydrochloride is a competitive inhibitor with regard to the substrate tryptophan, with a K_i of 32.6 μM. 4-Ethynyl-L-phenylalanine hydrochloride selectively and reversibly inhibits the biosynthesis of serotonin.

HY-103194

KH7	Others	Others
KH7 is a soluble adenylyl cyclase (sAC)-specific inhibitor, with IC₅₀s of 3-10 μM toward both recombinant purified human sAC_t protein and heterologously expressed sACt in cellular assays. KH7 is also a cAMP inhibitor.

HY-23460

4-Ethynyl-L-phenylalanine	Tryptophan Hydroxylase	Neurological Disease
4-Ethynyl-L-phenylalanine is a selective, reversible, potent and competitive inhibitor of tryptophan hydroxylase (TPH). 4-Ethynyl-L-phenylalanine is a competitive inhibitor with regard to the substrate tryptophan, with a K_i of 32.6 μM. 4-Ethynyl-L-phenylalanine selectively and reversibly inhibits the biosynthesis of serotonin.

HY-P1376A

G-Protein antagonist peptide TFA	mAChR Adrenergic Receptor
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.

HY-133114

Ezetimibe ketone EZM-K	Keap1-Nrf2 Autophagy	Cancer Cardiovascular Disease
Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.

HY-W006230

Anthraflavic acid	Others	Cancer
Anthraflavic acid, a flavonoid, is a potent IQ mutagenicity inhibitor by virtue of its ability to inhibit both its microsomal and cytosolic activation pathways. Anthraflavic acid is a potent and specific cytochrome P-448 inhibitor activity an enzyme system closely associated with the activation of many chemical carcinogens.

HY-118532

Tyrphostin AG30 AG30	EGFR	Cancer
Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.

HY-N0112

Dihydromyricetin Ampelopsin; Ampeloptin	mTOR Influenza Virus DNA/RNA Synthesis Autophagy	Cancer Infection
Dihydromyricetin is a potent inhibitor with an IC₅₀ of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 22 nM.

HY-11001

PHA-793887	CDK Apoptosis	Cancer
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC₅₀s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC₅₀ of 79 nM.

HY-100222

CZ415
mTOR Cancer

CZ415 is a potent and highly selective mTOR inhibitor with a pIC₅₀ of 8.07. CZ415 inhibits mTORC1 and mTORC2 protein complex.

HY-119692

Curvulin	Microtubule/Tubulin	Others
Curvulin, isolated from Curvularia lunata, is a phytotoxin. Curvularin is reported to inhibit microtubule assembly and has also been shown to inhibit iNOS expression.

HY-12056

BIX02189
MEK ERK Cancer

BIX02189 is a potent and selective MEK5 inhibitor with an IC₅₀ of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC₅₀ of 59 nM.

HY-12957

NITD008 7-Deaza-2'-C-acetylene-adenosine	DNA/RNA Synthesis Influenza Virus	Infection
NITD008 is a potent and selective flaviviruse inhibitor which can inhibit Dengue Virus Type 2 (DENV-2) with an EC₅₀ of 0.64 μM.

HY-10367A

Canertinib dihydrochloride CI-1033 dihydrochloride; PD-183805 dihydrochloride	EGFR	Cancer
Canertinib dihydrochloride (CI-1033 dihydrochloride) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM.

HY-135383

(3S,5S)-Pitavastatin calcium
Others Metabolic Disease

(3S,5S)-Pitavastatin cacium is the 3-epimer of Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.
HY-12204

PFK-015
Autophagy Cancer

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.

HY-100750

Norverapamil hydrochloride (±)-Norverapamil hydrochloride; D591 hydrochloride	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-13577A

Oclacitinib maleate PF-03394197 maleate	JAK	Inflammation/Immunology
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting *JAK1* (IC₅₀=10 nM).

HY-N3002

α-Arbutin 4-Hydroxyphenyl α-D-glucopyranoside	Tyrosinase	Metabolic Disease
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.

HY-111357

Antifungal agent 2	Fungal	Infection
Antifungal agent 2 is a broad-spectrum fungal inhibitor which inhibits growth of pertinent species of Candida, Cryptococcus, and Aspergillus at a concentration as low as 0.5 μg/mL.

HY-13966

2-Deoxy-D-glucose 2-Deoxy-D-arabino-hexose; D-Arabino-2-deoxyhexose	Hexokinase HSV Apoptosis	Cancer
2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on *hexokinase*.

HY-12589

ZM39923 hydrochloride	JAK	Cancer Neurological Disease
ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC₅₀ of 7.1; ZM39923 hydrochloride also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.

HY-126482

Telomerase-IN-2	Telomerase	Cancer
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC₅₀ of 0.89 µM. Anti-cancer activity.

HY-15162A

D8-MMAE D8-Monomethyl auristatin E	Microtubule/Tubulin ADC Cytotoxin	Cancer
D8-MMAE (D8-Monomethyl auristatin E) is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

HY-15417

ML-7 hydrochloride
Myosin YAP Cancer

ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC₅₀=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.
HY-12622

HSP70-IN-1
HSP Cancer

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC₅₀ of 2.3 μM.

HY-112861A

Gln-AMS TFA	Aminoacyl-tRNA Synthetase	Infection
Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor. Gln-AMS inhibits glutaminyl-tRNA synthetase (GlnRS) with a K_i of 1.32 µM.

HY-12444

Y15 FAK Inhibitor 14	FAK	Cancer
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.

HY-100852

ER-000444793	Mitochondrial Metabolism	Cancer
ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC₅₀ of 2.8 μM.

HY-12289A

Defactinib hydrochloride VS-6063 hydrochloride; PF 04554878 hydrochloride	FAK	Cancer
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

HY-W018931

DDR Inhibitor	Discoidin Domain Receptor	Cancer
DDR Inhibitor is a potent discoidin domain receptor (DDR) inhibitor, with an IC₅₀ of 3.3 nM for DDR2, and shows 53% inhibition on DDR1 at 1.5 nM.

HY-12589A

ZM39923
JAK Cancer Neurological Disease

ZM39923 is a JAK3 inhibitor, with a pIC₅₀ of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC₅₀ of 10 nM.
HY-115666

COH34 analog 1
Others Cancer

COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
HY-13806

XL388
mTOR Autophagy Cancer

XL388 is a highly potent and ATP-competitive mTOR inhibitor with an IC₅₀ of 9.9 nM. XL388 simultaneously inhibits both mTORC1 and mTORC2.

HY-12744

Genz-123346 free base	Others	Metabolic Disease Cancer
Genz-123346 (free base) is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1; inhibits GM1 with IC₅₀ value of 14 nM.

HY-10129

Veliparib
ABT-888
PARP Autophagy Cancer

Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with K_is of 5.2 and 2.9 nM, respectively.
HY-11108

R406 free base
Syk Apoptosis Inflammation/Immunology Cancer

R406 free base is a potent Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3.

HY-111651

Gboxin	ATP Synthase Mitochondrial Metabolism	Cancer
Gboxin is an oxidative phosphorylation (OXPHOS) inhibitor that targets glioblastoma. Gboxin inhibits the activity of F₀F₁ ATP synthase. Antitumour activity.

HY-N5015

Rosmanol	Others	Inflammation/Immunology Cancer
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.

HY-133246

Monodes(N-carboxymethyl)valine Daclatasvir Daclatasvir Impurity A	HCV	Infection
Monodes(N-carboxymethyl)valine Daclatasvir (Daclatasvir Impurity A) is the main degradation product of Daclatasvir. Daclatasvir is a potent HCV NS5A protein inhibitor.

HY-10366

BI-78D3
JNK Metabolic Disease Cancer

BI-78D3 functions as a substrate competitive inhibitor of JNK, inhibit the JNK kinase activity (IC₅₀=280 nM).
HY-112445

SGC3027
Histone Methyltransferase Cancer

SGC3027 is a histone methyltransferase inhibitor. SGC3027 is the first potent, selective and cell active chemical probe for PRMT7.

HY-12479A

Epetraborole hydrochloride GSK2251052 hydrochloride	Bacterial	Infection
Epetraborole hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding "to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase".

HY-19832

SC66	Akt Apoptosis	Cancer
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.

HY-136110

2-Keto-D-galactose D-Galactosone	DNA/RNA Synthesis	Cancer
2-Keto-D-galactose (D-Galactosone) inhibits DNA synthesis, and inhibits proliferation of in vitro grown Ehrlich ascites tumor cells.

HY-115584

Lufenuron	Parasite	Infection
Lufenuron is a lipophilic benzoylurea insecticide and a chitin synthesis inhibitor that can used for flea and fish lice control. Lufenuron inhibits moulting of arthropods.

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-100303

FR194738 free base	Others	Metabolic Disease
FR194738 free base is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC₅₀ of 9.8 nM.

HY-135328

Norverapamil (±)-Norverapamil; D591	Calcium Channel P-glycoprotein Drug Metabolite	Cardiovascular Disease
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

HY-B1479C

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

HY-112136

TAO Kinase inhibitor 1	Others	Cancer
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC₅₀s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.

HY-100374

Val-Cit-PAB-MMAE	Drug-Linker Conjugates for ADC	Cancer
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE (HY-15162). MMAE a potent mitotic* inhibitor* by inhibiting tubulin polymerization.

HY-P0222A

PKI(5-24) TFA	PKA	Others
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a K_i of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor.

HY-B1479

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

HY-50846

SCH772984	ERK	Cancer
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC₅₀s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-naïve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.

HY-15480

NSC 42834 JAK2 Inhibitor V; Z3	JAK	Cancer
NSC 42834 (JAK2 Inhibitor V), a novel specific inhibitor of Jak2, inhibits Jak2-V617F and Jak2-WT autophosphorylation in a dose-dependent manner but was not cytotoxic to cells at concentrations that inhibited kinase activity.

HY-B1479B

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

HY-100126

Tubercidin 7-Deazaadenosine	Bacterial DNA/RNA Synthesis Influenza Virus Antibiotic	Infection
Tubercidin (7-Deazaadenosine) is an antibiotic obtained from Streptomyces tubercidicus. Tubercidin inhibits the growth of Streptococcus faecalis (8043) with an IC₅₀ of 0.02 μM. Tubercidin inhibits polymerases by incorporating DNA or RNA, thereby inhibiting DNA replication, RNA and protein synthesis. Tubercidin is a weak inhibitor of adenosine phosphorylase, and interferes with the phosphorylation of adenosine and AMP. Tubercidin has antiviral activity.

HY-B0968A

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

HY-15463

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

HY-110100

CPYPP	Others	Inflammation/Immunology
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2^DHR-2 for Rac1 in a dose-dependent manner with an IC₅₀ of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9.

HY-112701

CCR6 inhibitor 1	CCR	Cancer Inflammation/Immunology Endocrinology
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC₅₀s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC₅₀, > 30000 nM), and CCR7 (IC₅₀, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer.

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-B0879A

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

HY-B0879

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

HY-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-12062

PD318088
MEK Cancer

PD318088 is an allosteric MEK inhibitor.
HY-14645

(-)-DHMEQ
Dehydroxymethylepoxyquinomicin
NF-κB Cancer

(–)-DHMEQ is a potent NF-κB inhibitor.
HY-112504

INCB054329
Epigenetic Reader Domain Cancer

INCB054329 is a potent BET inhibitor.
HY-B1480

Ethoxzolamide
Redupresin; L-643786; PNU-4191
Carbonic Anhydrase Bacterial Infection Inflammation/Immunology

Ethoxzolamide is a carbonic anhydrase inhibitor with K_i of 1 nM.
HY-17479A

Amfenac Sodium Hydrate
COX Inflammation/Immunology

Amfenac Sodium Hydrate is a COX-2 inhibitor.
HY-19819

NSC117079
Others Inflammation/Immunology

NSC117079 is a novel PHLPP inhibitor.
HY-A0063A

Tipiracil
Thymidylate Synthase Nucleoside Antimetabolite/Analog Cancer

Tipiracil is a thymidine phosphorylase (TPase) inhibitor.
HY-U00208

Prinoxodan
RGW2938
Phosphodiesterase (PDE) Cardiovascular Disease

Prinoxodan (RGW2938) is a phosphodiesterase inhibitor.
HY-19649

Candoxatril
UK 79300
Neprilysin Metabolic Disease

Candoxatril is a neutral endopeptidase (NEP) inhibitor.
HY-100143

Pentiapine
CGS 10746
Dopamine Receptor Neurological Disease

Pentiapine is a novel dopamine release inhibitor.
HY-B0715

Pentoxifylline
BL-191; PTX; Oxpentifylline
Phosphodiesterase (PDE) Autophagy HIV Cardiovascular Disease Cancer

Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor.
HY-112502B

MethADP sodium salt
CD73 Cancer

MethADP (sodium salt) is a specific CD73 inhibitor.
HY-N0274

Caffeic acid phenethyl ester
NF-κB Apoptosis Cancer Inflammation/Immunology

Caffeic acid phenethyl ester is a NF-κB inhibitor.
HY-112502

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

MethADP is a specific CD73 inhibitor.
HY-15759A

Napsagatran hydrate
Ro 46-6240 hydrate; Ro 46-6240/010 hydrate
Thrombin Cardiovascular Disease

Napsagatran hydrate is a novel and specific thrombin inhibitor.
HY-17620

Sacubitrilat
LBQ-657
Neprilysin Neurological Disease

Sacubitrilat is an active neprilysin (NEP) inhibitor.
HY-U00065

Tritoqualine
Inhibostamin; Hypostamine
Others Inflammation/Immunology

Tritoqualine is used as a histidine decarboxylase inhibitor.
HY-112504A

INCB054329 Racemate
Epigenetic Reader Domain Cancer

INCB054329 Racemate is a BET protein inhibitor.

HY-15769A

WHI-P180 hydrochloride Janex 3 hydrochloride	RET VEGFR EGFR	Cancer
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC₅₀s of 5 nM, 66 nM and 4 μM, respectively.

HY-19762

GSK1940029 SCD inhibitor 1	Stearoyl-CoA Desaturase (SCD)	Cancer
GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor extracted from patent WO/2009060053 A1, compound example 16.

HY-16511

Upamostat WX-671	Ser/Thr Protease PAI-1	Cancer
Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.

HY-14754

Salirasib S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS	Ras Autophagy	Cancer
Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.

HY-101873

Atorvastatin lactone	HMG-CoA Reductase (HMGCR)	Metabolic Disease Inflammation/Immunology
Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.

HY-70035

Otamixaban FXV673	Factor Xa	Cardiovascular Disease
Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.

HY-107643

Reversan
CBLC4H10
P-glycoprotein Cancer

Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
HY-100737

ML349
Phospholipase Cancer

ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a K_i of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC₅₀ of 144 nM.

HY-50714

Quiflapon sodium MK-591 sodium	FLAP Apoptosis	Inflammation/Immunology
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.

HY-103334

MAFP Methyl Arachidonyl Fluorophosphonate	Phospholipase	Metabolic Disease Neurological Disease Cardiovascular Disease
MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.

HY-18729A

L-NAME hydrochloride NG-Nitroarginine methyl ester hydrochloride	NO Synthase	Cancer
L-NAME hydrochloride inhibits NOS with an IC₅₀ of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC₅₀ value of 1.4 μM.

HY-B0069

Fludarabine F-ara-A; NSC 118218	Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis	Cancer
Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of *STAT1*. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A.

HY-16214

FX-11 LDHA Inhibitor FX11	Lactate Dehydrogenase	Cancer
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC₅₀ of 23.3 μM for HeLa cell，a K_i value of 8 μM.

HY-12055

BIX02188
MEK ERK Cancer

BIX02188 is a potent MEK5-selective inhibitor with an IC₅₀ of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC₅₀ of 810 nM.
HY-100891

CD80-IN-3
Others Inflammation/Immunology

CD80-IN-3, a potent CD80 inhibitor, inhibits CD80/CD28 interaction with an EC₅₀ of 630 nM and a K_d of 125 nM.
HY-15248

GDC-0349
mTOR Autophagy Cancer

GDC-0349 is a potent and selective ATP-competitive mTOR inhibitor with a K_i of 3.8 nM. GDC-0349 inhibits of both mTORC1 and mTORC2 complexes.

HY-13327

Evacetrapib LY2484595	CETP	Cardiovascular Disease
Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC₅₀ 5.5 nM) and CETP activity in human plasma (IC₅₀ 36 nM) in vitro.

HY-19331

WZB117
GLUT Cancer

WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.

HY-N3266

Methyl rosmarinate	Tyrosinase	Cancer
Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC₅₀ of 0.28 mM for mushroom tyrosinase, and also inhibits *a-glucosidase*.

HY-100965

Diphenyleneiodonium chloride DPI	TRP Channel NADPH Oxidase Reactive Oxygen Species	Inflammation/Immunology Neurological Disease
Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a *TRPA1* activator with an EC₅₀ of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.

HY-33900

Dihydrofuran-3(2H)-one 3-Oxotetrahydrofuran	Others	Others
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.

HY-15769

WHI-P180
Janex 3
VEGFR EGFR Cancer

WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC₅₀s of 5 nM, 66 nM and 4 μM, respectively.

HY-100562

Flopropione	5-HT Receptor COMT	Neurological Disease
Flopropione is a 5-HT receptor antagonist and also a catechol-o-methyltransferase (COMT) inhibitor. Flopropione also as an antispasmodic agent.

HY-15338

TG003
CDK Cancer

TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC₅₀ values of 20 and 15 nM, respectively.
HY-111621

DC661
Autophagy Apoptosis Cancer

DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
HY-12964

SGI-7079
TAM Receptor Cancer

SGI-7079 is an Axl inhibitor, significantly inhibits the proliferation of SUM149 or KPL-4 cells with an IC50 of 0.43 or 0.16 μM, respectively.
HY-10165

PSI-6130
R 1656
HCV Infection

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC₅₀ of 0.6 μM.

HY-P1044

Spinorphin LVV-hemorphin-4	Others	Neurological Disease
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.

HY-135570

DHODH-IN-2	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus	Infection
DHODH-IN-2 (compound 21d) is a human dihydroorotate dehydrogenase (HsDHODH) inhibitor, inhibits measles virus replication with a pMIC₅₀ value of 8.6.

HY-101587

PGS-IN-1 KME-4	PGE synthase Lipoxygenase	Inflammation/Immunology
PGS-IN-1 is a potent inhibitor of prostaglandin synthetase (PGS) with an IC₅₀ of 0.28 μM; also inhibits 5-lipoxygenase with an IC₅₀ of 1.05 μM.

HY-101872

GSK-872
RIP kinase Inflammation/Immunology

GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC₅₀ of 1.8 nM, and inhibits kinase activity with an IC₅₀ of 1.3 nM.

HY-10005

Flavopiridol HMR-1275; Alvocidib; L86-8275	CDK Autophagy HIV	Cancer
Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC₅₀s of 30, 170, 100 nM, respectively.

HY-111381

BI-3812
Bcl-2 Family Cancer

BI-3812 is potent and efficacious BCL6 inhibitor, inhibiting the BTB domain of BCL6, with an IC₅₀ of ≤3 nM; BI-3812 has antitumor activity.

HY-12041

SP600125	JNK Autophagy Apoptosis Ferroptosis	Cancer
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC₅₀s of 40, 40 and 90 nM for *JNK1, JNK2* and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 inhibits autophagy and activates *apoptosis*.

HY-N2360

Hinokiflavone	E1/E2/E3 Enzyme	Cancer
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.

HY-122727

STL127705	DNA-PK	Cancer
STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC₅₀ of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC₅₀, 2.5 μM).

HY-113957

MPI_5a	HDAC	Cancer
MPI_5a is a potent and selective HDAC6 inhibitor (IC₅₀=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC₅₀ value of 210 nM.

HY-N2150

Psammaplin A	HDAC DNA Methyltransferase DNA/RNA Synthesis Bacterial	Cancer Infection
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective *DAC1* inhibitor with an IC₅₀ of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.

HY-18707

K-Ras(G12C) inhibitor 12	Ras Apoptosis	Cancer
K-Ras(G12C) inhibitor 12 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0.32 μM.

HY-101938

Sinefungin Adenosyl-Ornithine; A-9145; Antibiotic 32232RP	Histone Methyltransferase Fungal Antibiotic	Infection Inflammation/Immunology
Sinefungin is a potent inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin, a SET7/9 inhibitor, ameliorates renal fibrosis by inhibiting H3K4 methylation.

HY-N2553

4-Deoxypyridoxine 5'-phosphate	LPL Receptor	Metabolic Disease
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a K_i of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (K_i of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.

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-124756

SBI-425	Phosphatase	Cardiovascular Disease
SBI-425 is a potent, selective and oral bioavailable tissue-nonspecific alkaline phosphatase (TNAP) inhibitor. Long-term administration of SBI-425 effectively reaches and inhibits TNAP in the vasculature, improving cardiovascular parameters and survival at a dose that does not cause a detectable change in bone.

HY-12842

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

HY-B0789

SU6656	Src FAK Akt	Cancer
SU6656 is a Src family kinases inhibitor with IC₅₀s of 280, 20, 130, 170 nM for Src, Yes, Lyn, and Fyn, respectively. SU6656 inhibits FAK phosphorylation at Y576/577, Y925, Y861 sites. SU6656 also inhibits p-AKT.

HY-106697

Statil Ponalrestat	Aldose Reductase	Metabolic Disease
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (K_i=7.7 nM) over ALR1 (K_i=60 μM). Statil inhibits the conversion of glucose to sorbitol.

HY-108486

Herbimycin A	Bacterial Antibiotic
Herbimycin A, an ansamycin ^antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60^v-src and p210^BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.

HY-12810

EHop-016
Ras Cancer

EHop-016 is a novel potent and selective inhibitor of Rac GTPase; inhibits Rac1 activity in MDA-MB-435 cells with an IC50 of 1.1 uM.

HY-100111

GLX351322	NADPH Oxidase	Metabolic Disease
GLX351322 is an inhibitor of NADPH oxidase 4 (Nox4), and inhibits hydrogen peroxide production from NOX4-overexpressing cells with an IC₅₀ of 5 μM.

HY-12871C

Atuveciclib S-Enantiomer BAY-1143572 S-Enantiomer	CDK	Cancer
Atuveciclib S-Enantiomer (BAY-1143572 S-Enantiomer) is a potent and selective CDK9 inhibitor, which inhibits *CDK9/CycT1* with an IC₅₀ of 16 nM.

HY-B0856

Validamycin A	Fungal Tyrosinase	Infection
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A is a reversible tyrosinase inhibitor, with a K_i of 5.893 mM.

HY-W011044

CID 5951923
KLF Cancer

CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC₅₀ of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.

HY-19363

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

HY-13991

CCG-1423	Ras	Cancer
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.

HY-50866

NVP-AEW541
AEW541
IGF-1R Insulin Receptor Autophagy Cancer Endocrinology

NVP-AEW541 is a potent inhibitor of IGF-1R with IC₅₀ of 0.15 μM, also inhibits InsR, with IC₅₀ of 0.14 μM.
HY-124861

Malic enzyme inhibitor ME1
ME1
Others Cancer Metabolic Disease

Malic enzyme inhibitor ME1 (ME1; compound 1) is a potent inhibitor of Malic enzyme (ME1) with an IC₅₀ of 0.15 μM.
HY-16667

HLM006474
Others Cancer

HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC₅₀ of 29.8 µM in A375 cells.

HY-19696A

Tauroursodeoxycholate Sodium Sodium tauroursodeoxycholate; Tauroursodeoxycholic acid sodium salt	ERK Caspase	Cancer
Tauroursodeoxycholate Sodium is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

HY-15881

TCS JNK 5a
JNK Inhibitor IX
JNK Apoptosis Cancer

TCS JNK 5a is a potent JNK3 inhibitor with a pIC₅₀ of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC₅₀ of 6.5.
HY-13227

SD-208
TGF-β Receptor Cancer

SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC₅₀ of 48 nM, and > 100-fold selectivity over TGF-βRII.
HY-15125

(R)-(+)-Bay-K-8644
Calcium Channel Cardiovascular Disease

(R)-(+)-Bay-K-8644 is a calcium channel inhibitor. (R)-(+)-Bay-K-8644 inhibits Ba²⁺ currents (I_Ba) (IC₅₀=975 nM).

HY-14682

GSK319347A	IKK	Inflammation/Immunology
GSK319347A is a dual inhibitor of *TBK1* and IKKε with IC₅₀s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC₅₀ of 790 nM.

HY-13648

Incyclinide CMT-3; COL-3	MMP	Cancer
Incyclinide (CMT-3, COL-3) is a matrix metalloproteinase (MMP) inhibitor, thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis.

HY-15192

GSK 650394	SGK Influenza Virus	Cancer Infection
GSK 650394 is a novel SGK inhibitor with IC₅₀ of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively. GSK 650394 also inhibits influenza virus replication.

HY-15719

NU 7026
LY293646
DNA-PK Apoptosis Cancer

NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC₅₀ of 0.23 μM, also inhibits PI3K with IC₅₀ of 13 μM.

HY-12993

RSV604 (S)-1-(2-Fluorophenyl)-3-(2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)urea	RSV	Infection
RSV604 is a novel inhibitor of respiratory syncytial virus replication(EC50=0.86 uM); a putative RSV nucleoprotein(N) inhibitor in phase 2 clinical trials.

HY-B0869A

Bispyribac sodium	Others	Others
Bispyribac sodium is a selective, systemic and post emergent herbicide used to eradicate grasses and broad leaf weeds. Bispyribac sodium is also an acetolactate synthase (ALS or known as AHAS) inhibitor.

HY-13915

NSC348884	Apoptosis	Cancer
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.

HY-112522

HS79	Fatty Acid Synthase (FASN)	Cancer
HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC₅₀ of 1.57 μM.

HY-16663

ITX3	Others	Others
ITX3 is a specific and nontoxic inhibitor of the TrioN (N-terminal GEF domain of the multidomain Trio protein) with IC50 of 76 uM; inhibits TrioN-stimulated RhoG exchange in vitro.

HY-100223

Calpeptin	Cathepsin Proteasome Apoptosis	Inflammation/Immunology
Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

HY-13803

Tazemetostat EPZ-6438; E-7438	Histone Methyltransferase	Cancer
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC₅₀ of 392 nM.

HY-W009783

1-Deoxymannojirimycin hydrochloride	HIV Influenza Virus	Infection
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC₅₀ of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits *HIV‐1* strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.

HY-101920

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

HY-N1127

Tricin	CMV	Cancer Infection
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.

HY-W011094

Win 18446	Aldehyde Dehydrogenase (ALDH)	Endocrinology
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC₅₀ of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.

HY-N2532

Diphyllin	HIV Proton Pump Influenza Virus	Cancer Infection Inflammation/Immunology
Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent *HIV-1* inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H⁺-ATPase (V-ATPase) inhibitor with an IC₅₀ value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC₅₀ of 50 μM and has anticancer and anti-inflammatory activities.

HY-115510

SPR inhibitor 3 SPRi3	Others	Inflammation/Immunology
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC₅₀=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC₅₀=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.

HY-12276

MALT1 inhibitor MI-2	MALT1	Cancer
MALT1 inhibitor MI-2 is a *MALT1* inhibitor (IC₅₀=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.

HY-14521

Lometrexol DDATHF	Antifolate Apoptosis	Cancer
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

HY-131275

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

HY-14521B

Lometrexol hydrate DDATHF hydrate	Antifolate Apoptosis	Cancer
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.

HY-N6701

Dihydrocytochalasin B	Arp2/3 Complex	Cancer
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca²⁺increase in the mucosal scrapings.

HY-12688A

Succinyl phosphonate trisodium salt	Endogenous Metabolite Reactive Oxygen Species	Cancer Metabolic Disease Neurological Disease
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.

HY-12961A

Bretylium tosylate
Others Neurological Disease

Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
HY-19236

PNU-103017
HIV Protease HIV Infection

PNU-103017 is an HIV protease inhibitor.
HY-101835

Decoyinine
Angustmycin A
Others Cancer

Decoyinine is a selective inhibitor of GMP synthetase (GMPS).
HY-B1839

Fluazinam
Fungal Infection

Fluazinam is a broad spectrum pyridinamine fungal inhibitor.
HY-B0207A

Pyridostigmine bromide
AChE Neurological Disease

Pyridostigmine bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
HY-15681

Senexin A
CDK Cancer

Senexin A is a CDK8 inhibitor with an IC₅₀ of 280 nM.
HY-112670

Exo1
Others Others

Exo1 is a chemical inhibitor of the exocytic pathway.
HY-19123

Z-321
Others Neurological Disease

Z-321 is a prolylendopeptidase (PEP) inhibitor.
HY-103710

IBR2
RAD51 Cancer

IBR2 is a specific RAD51 inhibitor.
HY-U00222

S3337
Proton Pump Inflammation/Immunology

S3337 is an H⁺, K⁺-ATPase inhibitor.
HY-12703

KSI-3716
c-Myc Autophagy Cancer

KSI-3716 is a c-Myc inhibitor.
HY-B1542A

Benactyzine hydrochloride
AChE Neurological Disease

Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a K_i of 0.010 mM.
HY-103706

ROC-325
Autophagy Apoptosis Cancer

ROC-325 is a novel inhibitor of autophagy.
HY-112097

E260
Others Cancer

E260 is a Fer/FerT kinase inhibitor.
HY-19979

RCM-1
Others Cancer

RCM-1 is a FOXM1 inhibitor.
HY-U00176

Org30958
Aromatase Metabolic Disease

Org30958 is a potent aromatase inhibitor in vivo.
HY-13603

Crolibulin
EPC2407
Microtubule/Tubulin Cancer

Crolibulin is a small molecule tubulin polymerization inhibitor.
HY-N0221

Daurisoline
(R,R)-Daurisoline
Autophagy Potassium Channel Cancer

Daurisoline is a hERG inhibitor and also an autophagy blocker.
HY-U00175

Pamicogrel
KBT3022
COX Cardiovascular Disease

Pamicogrel (KBT3022) is a cyclooxygenase (COX) inhibitor.
HY-10827

Kelatorphan
Opioid Receptor Neurological Disease

Kelatorphan is a full inhibitor of enkephalin degrading enzymes.
HY-13061

Daun02
Topoisomerase ADC Cytotoxin Cancer

Daun02 is a prodrug of the topoisomerase inhibitor Daunorubicin.
HY-15723A

NSC 23766 trihydrochloride
Ras Apoptosis Cancer

NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.
HY-66009

Epalrestat
ONO2235
Aldose Reductase Metabolic Disease

Epalrestat is an aldose reductase inhibitor for the treatment of diabetic neuropathy.
HY-B0597

Fondaparinux sodium
Fondaparin sodium; SR-90107A
Factor Xa Cardiovascular Disease

Fondaparinux sodium is an antithrombin-dependent factor Xa inhibitor.
HY-101644A

Saterinone hydrochloride
BDF 8634 hydrochloride
Phosphodiesterase (PDE) Cardiovascular Disease

Saterinone hydrochloride is a phosphodiesterase III (PDE III) inhibitor.
HY-101647

Intoplicine
Topoisomerase Cancer

Intoplicine is a DNA topoisomerase I and II inhibitor.

HY-50671

Zosuquidar trihydrochloride RS 33295-198 trihydrochloride; LY-335979 trihydrochloride	P-glycoprotein	Cancer
Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a K_i value of 59 nM.

HY-12804

VAS2870
NADPH Oxidase Cardiovascular Disease

VAS2870 is a NADPH oxidase (NOX) inhibitor.
HY-104074

Pocapavir
SCH-48973; V-073
Enterovirus Infection

Pocapavir is an investigational enterovirus (EV) capsid inhibitor.
HY-107362

CH7057288
Trk Receptor Cancer

CH7057288 is a potent and selective TRK inhibitor.
HY-101862

CB-7921220
Adenylate Cyclase Neurological Disease Cardiovascular Disease

CB-7921220 is an adenylate cyclase inhibitor.
HY-113057

3-Hydroxycapric acid
Endogenous Metabolite Cancer

3-Hydroxycapric acid is an inhibitor for mitotic progression.
HY-12527

Pyridoclax
MR-29072
Bcl-2 Family Cancer

Pyridoclax is a potential Mcl-1 inhibitor.
HY-18643

TZ9
E1/E2/E3 Enzyme Cancer

TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.

HY-18696

AMG-337	c-Met/HGFR	Cancer
AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor. AMG 337 inhibits MET kinase activity with an IC50 of < 5nM in enzymatic assays.

HY-B1490

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

HY-P2502

Hepatitis Virus C NS3 Protease Inhibitor 2	HCV Protease HCV	Infection
Hepatitis Virus C NS3 Protease Inhibitor 2 is a product-based peptide inhibitor of hepatitis C virus (HCV) NS3 protease, with a K_i of 41 nM.

HY-10006

Flavopiridol Hydrochloride Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride	CDK Autophagy HIV	Cancer
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC₅₀s of 30, 170, 100 nM, respectively.

HY-N0102

Isoliquiritigenin GU17; ISL; Isoliquiritigen	Aldose Reductase Influenza Virus Autophagy Apoptosis	Cancer Infection Inflammation/Immunology
Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza glabra, which inhibits aldose reductase with an IC₅₀ of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC₅₀ of 24.7 μM.

HY-14427

4E1RCat
Eukaryotic Initiation Factor (eIF) Autophagy Cancer

4E1RCat is an inhibitor of cap-dependent translation, and inhibits eIF4E:eIF4GI interaction, with an IC₅₀ an of ∼4 μM.
HY-13865

P 22077
Deubiquitinase Cancer

P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC₅₀ of 8.01 μM. It also inhibits USP47 with an EC₅₀ of 8.74 μM.
HY-16712

LDN-214117
TGF-β Receptor Cancer

LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).

HY-15716

Kobe0065	Ras Apoptosis	Cancer
Kobe0065 is a novel and effective inhibitor of Ras-Raf interaction, competitively inhibiting the binding of H-Ras·GTP to c-Raf-1 RBD with a K_i value of 46±13 μM.

HY-U00422

K-756
PARP Cancer

K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC₅₀s of 31 and 36 nM, respectively.

HY-100742

GNE-140 racemate	Lactate Dehydrogenase	Cancer
GNE-140 racemate is a racemate mixture of (R)-GNE-140 and (S)-GNE-140. GNE-140 racemate is a potent lactate dehydrogenase A (LDHA) inhibitor.

HY-114166

2-D08
E1/E2/E3 Enzyme TAM Receptor Cancer

2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC₅₀ of 0.49 nM.

HY-109031

Dotinurad	URAT1	Metabolic Disease
Dotinurad is a potent and selective urate reabsorption inhibitor. Dotinurad inhibits urate transporter 1 (URAT1) with an IC₅₀ value of 37.2 nM. Dotinurad acts as a uricosuric agent.

HY-101840

EIPA L593754; MH 12-43	TRP Channel Sodium Channel	Cancer Inflammation/Immunology
EIPA (L593754) is a TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA also inhibits Na⁺/H⁺-exchanger (NHE) and *macropinocytosis*.

HY-15004

AUZ 454
K03861
CDK Cancer

AUZ 454 (K03861) is a type II CDK2 inhibitor with K_d of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.

HY-12067

R406	Syk Apoptosis	Cancer
R406 is a competitive Syk inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value.

HY-N6738

Bafilomycin B1	Bacterial Fungal Antibiotic	Infection
Bafilomycin B1 is a macrolide antibiotic isolated from Streptomyces sp, inhibits Gram-positive bacteria and fungi, and acts as an inhibitor of K⁺-dependent ATPase of E. coli.

HY-128726

ITK inhibitor 2	Itk	Inflammation/Immunology
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC₅₀ of 2 nM.

HY-19712

LJH685	Ribosomal S6 Kinase (RSK) Apoptosis	Cancer
LJH685 is a potent, specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC₅₀s of 6, 5, 4 nM, respectively.

HY-102087

JPM-OEt	Cathepsin	Cancer
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.

HY-50908

Ridaforolimus MK-8669; Deforolimus; AP23573	mTOR Autophagy	Cancer
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC₅₀ of 0.2 nM in HT-1080 cells.

HY-101840A

EIPA hydrochloride L593754 hydrochloride; MH 12-43 hydrochloride	TRP Channel Sodium Channel	Cancer Inflammation/Immunology
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC₅₀ of 10.5 μM. EIPA hydrochloride also inhibits Na⁺/H⁺-exchanger (NHE) and *macropinocytosis*.

HY-15839

UNC 669
Epigenetic Reader Domain Cancer

UNC 669 is a potent L3MBTL1 (IC₅₀=4.2 uM) and L3MBTL3 (3.1 uM) inhibitor.

HY-10074

TPCA-1	IKK STAT Apoptosis	Inflammation/Immunology Cancer
TPCA-1 is a potent and selective inhibitor of IKK-2 with IC₅₀ of 17.9 nM. TPCA-1 is an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation.

HY-13020

GSK1838705A	ALK IGF-1R Insulin Receptor	Cancer Endocrinology
GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC₅₀s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC₅₀ of 0.5 nM.

HY-112433

NIK SMI1	NF-κB	Inflammation/Immunology
NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC₅₀ of 0.23±0.17 nM.

HY-129700

MCL-1/BCL-2-IN-2
Bcl-2 Family Cancer

MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
HY-124944

APS6-45
Ras Cancer

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

HY-18964

MG-101 Calpain inhibitor I; Ac-LLnL-CHO; ALLN	Proteasome	Cancer
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with K_is of 190, 220, 150 and 500 pM, respectively.

HY-B1320

Meclofenamate sodium Meclofenamic acid sodium	Gap Junction Protein	Inflammation/Immunology
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.

HY-N5011

5,7-Dimethoxyflavone	Cytochrome P450	Cancer Inflammation/Immunology
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.

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-111549

Bragsin1	Others	Cancer
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC₅₀ of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.

HY-17401

Ranolazine dihydrochloride CVT 303 dihydrochloride; RS 43285	Calcium Channel Sodium Channel Autophagy	Cardiovascular Disease Cancer
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.

HY-13982

JSH-23	NF-κB	Cancer Metabolic Disease Inflammation/Immunology
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC₅₀ of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.

HY-W009156

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

HY-13599

Cladribine 2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA	Adenosine Deaminase Apoptosis	Cardiovascular Disease Cancer
Cladribine (2CdA), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity and can be used for the research of several hematologic malignancies and multiple sclerosis.

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-11006

KU-57788 NU7441	DNA-PK CRISPR/Cas9	Cancer
KU-57788 (NU7441) is a highly potent and selective DNA-PK inhibitor with an IC₅₀ of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC₅₀s of 5.0 and 1.7 μM, respectively.

HY-129769

CMLD012073	Eukaryotic Initiation Factor (eIF)	Cancer
CMLD012073 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012073 inhibits the growth of NIH/3T3 cells with an IC₅₀ of 10 nM. CMLD012073 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A).

HY-136199

SIRT1-IN-1	Sirtuin CMV	Infection
SIRT1-IN-1 is a selective *SIRT1* inhibitor with an IC₅₀ of 0.205 μM. SIRT1-IN-1 inhibits SIRT2 with an IC₅₀ of 11.5 μM. SIRT1-IN-1, a indole, is a cytomegalovirus (CMV) inhibitors and has antiviral activity.

HY-108900

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

HY-N2036

Mosloflavone	Enterovirus Bacterial	Infection
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.

HY-108341A

PF-06424439 methanesulfonate	Acyltransferase	Metabolic Disease
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC₅₀ of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

HY-15982

APY0201	PIKfyve Interleukin Related	Inflammation/Immunology
APY0201 is a potent PIKfyve inhibitor, which inhibits the conversion of PtdIns3P to PtdIns(3,5)P₂ in the presence of in the presence of [³³P]ATP with an IC₅₀ of 5.2 nM. APY0201 also inhibits IL-12/IL-23 production.

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-117889

PARP14 inhibitor H10	PARP Apoptosis	Cancer
PARP14 inhibitor H10, compound H 10, is a selective inhibitor against PARP14 (IC₅₀=490 nM), over other PARPs (≈24 fold over PARP1). PARP14 inhibitor H10 induces caspase-3/7-mediated cell *apoptosis*.

HY-110150

UNC3230	Others	Cancer Inflammation/Immunology
UNC3230 is a potent, selective and ATP-competitive *PIP5K1C* inhibitor with an IC₅₀ of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.

HY-U00444

DDR1-IN-2	Discoidin Domain Receptor	Inflammation/Immunology
DDR1-IN-2 is a potent inhibitor of discoidin domain receptor 1 (DDR1), with an IC₅₀ of 13.1 nM, and also less potently inhibits DDR2, with an IC₅₀ of 203 nM.

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-17393

Carboplatin NSC 241240	DNA Alkylator/Crosslinker Autophagy DNA/RNA Synthesis	Cancer
Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of CDDP and a potent anti-cancer agent.

HY-N4315

Pomiferin NSC 5113	HDAC mTOR	Cancer
Pomiferin (NSC 5113), a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC₅₀ of 1.05 μM, and also potently inhibits mTOR (IC₅₀, 6.2 µM).

HY-13728A

(R)-Plevitrexed (R)-ZD 9331; (R)-BGC9331	Others	Cancer
(R)-Plevitrexed ((R)-ZD 9331; (R)-BGC9331) is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent thymidylate synthase (TS) inhibitor.

HY-100578

AGK2
Sirtuin Apoptosis Cancer

AGK2 is a selective SIRT2 inhibitor with IC₅₀ of 3.5 μM. AGK2 can also inhibit SIRT1 and SIRT3 with IC₅₀ of 30 and 91 μM, respectively.

HY-108318

RK-24466 KIN 001-51	Src	Inflammation/Immunology Cardiovascular Disease
RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC₅₀s of less than 1 and 2 nM, respectively.

HY-16736A

Centanafadine hydrochloride EB-1020 hydrochloride	Adrenergic Receptor Dopamine Transporter Serotonin Transporter	Neurological Disease Endocrinology
Centanafadine (hydrochloride) is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC₅₀s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.

HY-16134A

Celgosivir hydrochloride MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride	Glucosidase HCV HIV	Infection
Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC₅₀ of 1.27 μM in in vitro assay.

HY-107366

SGN-2FF
Others Cancer

SGN-2FF is a potent and orally active inhibitor of fucosylation, directly inhibits fucosyltransferase activity. SGN-2FF possesses antitumor activity.

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-113950

Dichlorophenyl-ABA	Others	Neurological Disease
Dichlorophenyl-ABA is an inhibitor of transthyretin (TTR) amyloid fibril formation, inhibiting aggregate formation in more than 80% in TTR L55P-expressing cells.

HY-16956

CC-223	mTOR Apoptosis	Cancer
CC-223 is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC₅₀ value for mTOR kinase of 16 nM. CC-223 inhibits both *mTORC1* and mTORC2.

HY-14908

Vidofludimus 4sc-101; SC12267	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Interleukin Related	Inflammation/Immunology
Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.

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-12558

LY3009120
DP-4978
Raf Autophagy Cancer

LY3009120 is a pan RAF inhibitor which inhibits BRAF^V600E, BRAF^WT and CRAF^WT with IC₅₀s of 5.8, 9.1 and 15 nM, respectively.
HY-12990

Spautin-1
Autophagy Apoptosis Cancer

Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC₅₀s of 0.6-0.7 μM.

HY-100625

BVT948	Phosphatase Cytochrome P450 Histone Methyltransferase	Cancer
BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).

HY-15614A

SC144 hydrochloride	Interleukin Related	Cancer
SC144 hydrochloride is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.

HY-15871

GGTI298 Trifluoroacetate	Ras Apoptosis	Cancer
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit *Rap1A* with IC₅₀ of 3 μM; little effect on Ha-Ras with IC₅₀ of >20 μM.

HY-103028A

GSK963	RIP kinase	Others
GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC₅₀ of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.

HY-10241

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

HY-P1291

PKI 14-22 amide,myristoylated	PKA	Cancer
PKI 14-22 amide,myristoylated is a potent cAMP-dependent PKA inhibitor. PKI 14-22 amide,myristoylated reduces the IgG-mediated phagocytic response and also inhibits neutrophil adhesion.

HY-100437

HA15
HSP Autophagy Apoptosis Cancer

HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.

HY-10367

Canertinib CI-1033; PD-183805	EGFR	Cancer
Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC₅₀s of 7.4 and 9 nM.

HY-N2403

Dihydrolycorine
Othe