Search Result

Targets Recommended:	NEDD8-activating Enzyme GSK-3 PI3K FLT3 Oct3/4 Arp2/3 Complex Na+/HCO3- Cotransporter MAP3K Ligand for E3 Ligase Indoleamine 2,3-Dioxygenase (IDO) E3 Ligase Ligand-Linker Conjugate Progesterone Receptor E1/E2/E3 Enzyme PIKfyve TAM Receptor Dopamine Transporter ATM/ATR

Results for "Ang (3-8)/ Inhibitors" in MCE Product Catalog:

By Targets:	Arp2/3 Complex (9) ATM/ATR (21) Dopamine Transporter (17) E1/E2/E3 Enzyme (69) E3 Ligase Ligand-Linker Conjugate (4) FLT3 (79) GSK-3 (48) Indoleamine 2,3-Dioxygenase (IDO) (38) Ligand for E3 Ligase (11) MAP3K (16) Na+/HCO3- Cotransporter (1) NEDD8-activating Enzyme (6) PI3K (167) PIKfyve (5) Progesterone Receptor (2) TAM Receptor (24) 15-PGDH (1) 5 alpha Reductase (7) 5-HT Receptor (62) Acetyl-CoA Carboxylase (11) AChE (96) Ack1 (3) Acyltransferase (49) ADC Cytotoxin (52) ADC Linker (4) Adenosine Deaminase (8) Adenosine Kinase (2) Adenosine Receptor (12) Adenylate Cyclase (10) Adrenergic Receptor (46) Akt (72) Aldehyde Dehydrogenase (ALDH) (13) Aldose Reductase (17) ALK (44) Aminoacyl-tRNA Synthetase (10) Aminopeptidase (12) AMPK (33) Amyloid-β (35) Androgen Receptor (16) Angiotensin Receptor (23) Angiotensin-converting Enzyme (ACE) (50) Antibiotic (280) Antifolate (21) APC (4) Apoptosis (1068) Arenavirus (6) Arginase (9) Aromatase (11) Aryl Hydrocarbon Receptor (14) ATGL (1) ATP Citrate Lyase (8) ATP Synthase (9) Aurora Kinase (48) Autophagy (701) Bacterial (516) Bcl-2 Family (74) Bcr-Abl (59) BCRP (15) Beta-secretase (28) BMX Kinase (4) Bombesin Receptor (1) Bradykinin Receptor (1) Btk (55) c-Fms (29) c-Kit (55) c-Met/HGFR (62) c-Myc (14) Calcium Channel (80) CaMK (23) Cannabinoid Receptor (17) Carbonic Anhydrase (20) Carboxypeptidase (4) Casein Kinase (38) Caspase (47) CaSR (1) Cathepsin (39) CCR (26) CD73 (8) CDK (187) CETP (9) CFTR (6) CGRP Receptor (3) Checkpoint Kinase (Chk) (30) Chloride Channel (12) Cholecystokinin Receptor (6) CMV (19) Complement System (22) COMT (12) COX (180) CRAC Channel (11) CRFR (4) CRISPR/Cas9 (7) CRM1 (4) CXCR (31) Cyclic GMP-AMP Synthase (4) Cytochrome P450 (112) DAPK (3) Deubiquitinase (41) Dihydroorotate Dehydrogenase (27) Dipeptidyl Peptidase (45) Discoidin Domain Receptor (16) DNA Alkylator/Crosslinker (12) DNA Methyltransferase (25) DNA-PK (20) DNA/RNA Synthesis (188) Dopamine Receptor (38) Dopamine β-hydroxylase (7) Drug Metabolite (64) Drug-Linker Conjugates for ADC (63) Dynamin (6) DYRK (21) EAAT2 (4) EGFR (163) Elastase (18) Endogenous Metabolite (215) Endothelin Receptor (15) Enolase (3) Enterovirus (15) Ephrin Receptor (7) Epigenetic Reader Domain (147) Epoxide Hydrolase (14) ERK (59) Estrogen Receptor/ERR (37) Eukaryotic Initiation Factor (eIF) (20) FAAH (23) FABP (5) Factor Xa (20) FAK (27) Farnesyl Transferase (24) Fatty Acid Synthase (FASN) (28) Ferroptosis (72) FGFR (73) Filovirus (5) FKBP (7) FLAP (10) Fungal (140) FXR (3) G-quadruplex (5) GABA Receptor (24) Galectin (3) Gap Junction Protein (7) GHSR (4) Gli (3) Glucagon Receptor (5) Glucocorticoid Receptor (11) Glucosidase (28) GLUT (10) Glutaminase (10) Glutathione Peroxidase (10) GlyT (12) GPCR19 (2) GPR120 (1) GPR40 (4) GPR55 (1) GSNOR (1) Guanylate Cyclase (5) Gutathione S-transferase (11) Haspin Kinase (4) HBV (33) HCN Channel (2) HCV (111) HCV Protease (23) HDAC (117) Hedgehog (13) Hexokinase (4) HIF/HIF Prolyl-Hydroxylase (47) Hippo (MST) (3) Histamine Receptor (36) Histone Acetyltransferase (39) Histone Demethylase (56) Histone Methyltransferase (124) HIV (216) HIV Integrase (21) HIV Protease (26) HMG-CoA Reductase (HMGCR) (39) HSP (62) HSV (45) IAP (11) IFNAR (5) IGF-1R (23) iGluR (25) IKK (44) Imidazoline Receptor (5) Influenza Virus (109) Insulin Receptor (17) Integrin (43) Interleukin Related (55) IRAK (20) IRE1 (21) Isocitrate Dehydrogenase (IDH) (20) Itk (6) JAK (115) JNK (37) Keap1-Nrf2 (24) Kinesin (21) KLF (4) Lactate Dehydrogenase (11) Leukotriene Receptor (19) Ligand for Target Protein for PROTAC (27) LIM Kinase (LIMK) (7) Lipoxygenase (41) LPL Receptor (14) LRRK2 (18) LXR (3) mAChR (31) MAGL (19) MALT1 (6) MAP4K (13) MAPKAPK2 (MK2) (5) MCHR1 (GPR24) (2) MDM-2/p53 (55) MEK (45) Melanocortin Receptor (2) Melatonin Receptor (2) MELK (4) mGluR (9) MicroRNA (13) Microtubule/Tubulin (101) Mineralocorticoid Receptor (2) Mitochondrial Metabolism (45) Mitophagy (56) Mixed Lineage Kinase (6) MMP (68) MNK (5) Monoamine Oxidase (71) Monoamine Transporter (13) Monocarboxylate Transporter (8) Mps1 (12) mTOR (79) MyD88 (4) Myosin (14) Na+/Ca2+ Exchanger (11) Na+/K+ ATPase (19) nAChR (16) NADPH Oxidase (11) NAMPT (17) Neprilysin (15) Neurokinin Receptor (4) Neuropeptide Y Receptor (6) Neurotensin Receptor (4) NF-κB (148) NKCC (6) NO Synthase (50) NOD-like Receptor (NLR) (19) Notch (24) Nucleoside Antimetabolite/Analog (44) Opioid Receptor (10) Orexin Receptor (OX Receptor) (2) P-glycoprotein (44) P2X Receptor (11) P2Y Receptor (14) p38 MAPK (80) p97 (8) PAI-1 (11) PAK (15) Parasite (176) PARP (65) PD-1/PD-L1 (27) PDGFR (86) PDHK (10) PDK-1 (8) PERK (8) PGC-1α (1) PGE synthase (15) Phosphatase (122) Phosphodiesterase (PDE) (177) Phospholipase (54) PI4K (13) Pim (25) PKA (30) PKC (81) PKD (4) Polo-like Kinase (PLK) (29) Porcupine (8) Potassium Channel (93) PPAR (30) Procollagen C Proteinase (1) Prostaglandin Receptor (35) PROTAC (25) PROTAC Linker (7) Protease-Activated Receptor (PAR) (14) Proteasome (51) Protein Arginine Deiminase (11) Proton Pump (45) PTEN (5) Pyk2 (6) Pyroptosis (4) Pyruvate Kinase (3) RAD51 (10) Raf (54) RAR/RXR (10) Ras (89) Reactive Oxygen Species (72) Renin (7) RET (28) Reverse Transcriptase (53) RGS Protein (3) Ribosomal S6 Kinase (RSK) (26) RIP kinase (36) ROCK (45) ROR (10) ROS (12) RSV (17) Salt-inducible Kinase (SIK) (7) SARS-CoV (83) Ser/Thr Protease (24) Serotonin Transporter (42) sFRP-1 (1) SGK (8) SGLT (27) Sigma Receptor (6) Sirtuin (33) Smo (11) SNIPER (12) Sodium Channel (99) Somatostatin Receptor (3) SPHK (14) Src (78) SRPK (3) STAT (73) Stearoyl-CoA Desaturase (SCD) (12) STING (3) Survivin (3) Syk (32) Target Protein Ligand-Linker Conjugate (1) Telomerase (9) TGF-beta/Smad (14) TGF-β Receptor (43) Thrombin (26) Thymidylate Synthase (9) TNF Receptor (44) Toll-like Receptor (TLR) (32) TOPK (8) Topoisomerase (102) Trk Receptor (27) TRP Channel (43) Tryptophan Hydroxylase (11) TSH Receptor (2) Tyrosinase (36) ULK (8) URAT1 (5) Urotensin Receptor (1) Vasopressin Receptor (3) VD/VDR (6) VDAC (3) VEGFR (145) Virus Protease (36) Wee1 (5) Wnt (44) Xanthine Oxidase (14) YAP (11) β-catenin (22) γ-secretase (27)
By Research Areas:	Cancer (4878) Cardiovascular Disease (715) Endocrinology (251) Infection (1324) Inflammation/Immunology (1677) Metabolic Disease (853) Neurological Disease (1100)

By Targets:

Arp2/3 Complex (9)

ATM/ATR (21)

Dopamine Transporter (17)

E1/E2/E3 Enzyme (69)

E3 Ligase Ligand-Linker Conjugate (4)

FLT3 (79)

GSK-3 (48)

Indoleamine 2,3-Dioxygenase (IDO) (38)

Ligand for E3 Ligase (11)

MAP3K (16)

Na+/HCO3- Cotransporter (1)

NEDD8-activating Enzyme (6)

PI3K (167)

PIKfyve (5)

Progesterone Receptor (2)

TAM Receptor (24)

15-PGDH (1)

5 alpha Reductase (7)

5-HT Receptor (62)

Acetyl-CoA Carboxylase (11)

AChE (96)

Ack1 (3)

Acyltransferase (49)

ADC Cytotoxin (52)

ADC Linker (4)

Adenosine Deaminase (8)

Adenosine Kinase (2)

Adenosine Receptor (12)

Adenylate Cyclase (10)

Adrenergic Receptor (46)

Akt (72)

Aldehyde Dehydrogenase (ALDH) (13)

Aldose Reductase (17)

ALK (44)

Aminoacyl-tRNA Synthetase (10)

Aminopeptidase (12)

AMPK (33)

Amyloid-β (35)

Androgen Receptor (16)

Angiotensin Receptor (23)

Angiotensin-converting Enzyme (ACE) (50)

Antibiotic (280)

Antifolate (21)

APC (4)

Apoptosis (1068)

Arenavirus (6)

Arginase (9)

Aromatase (11)

Aryl Hydrocarbon Receptor (14)

ATGL (1)

ATP Citrate Lyase (8)

ATP Synthase (9)

Aurora Kinase (48)

Autophagy (701)

Bacterial (516)

Bcl-2 Family (74)

Bcr-Abl (59)

BCRP (15)

Beta-secretase (28)

BMX Kinase (4)

Bombesin Receptor (1)

Bradykinin Receptor (1)

Btk (55)

c-Fms (29)

c-Kit (55)

c-Met/HGFR (62)

c-Myc (14)

Calcium Channel (80)

CaMK (23)

Cannabinoid Receptor (17)

Carbonic Anhydrase (20)

Carboxypeptidase (4)

Casein Kinase (38)

Caspase (47)

CaSR (1)

Cathepsin (39)

CCR (26)

CD73 (8)

CDK (187)

CETP (9)

CFTR (6)

CGRP Receptor (3)

Checkpoint Kinase (Chk) (30)

Chloride Channel (12)

Cholecystokinin Receptor (6)

CMV (19)

Complement System (22)

COMT (12)

COX (180)

CRAC Channel (11)

CRFR (4)

CRISPR/Cas9 (7)

CRM1 (4)

CXCR (31)

Cyclic GMP-AMP Synthase (4)

Cytochrome P450 (112)

DAPK (3)

Deubiquitinase (41)

Dihydroorotate Dehydrogenase (27)

Dipeptidyl Peptidase (45)

Discoidin Domain Receptor (16)

DNA Alkylator/Crosslinker (12)

DNA Methyltransferase (25)

DNA-PK (20)

DNA/RNA Synthesis (188)

Dopamine Receptor (38)

Dopamine β-hydroxylase (7)

Drug Metabolite (64)

Drug-Linker Conjugates for ADC (63)

Dynamin (6)

DYRK (21)

EAAT2 (4)

EGFR (163)

Elastase (18)

Endogenous Metabolite (215)

Endothelin Receptor (15)

Enolase (3)

Enterovirus (15)

Ephrin Receptor (7)

Epigenetic Reader Domain (147)

Epoxide Hydrolase (14)

ERK (59)

Estrogen Receptor/ERR (37)

Eukaryotic Initiation Factor (eIF) (20)

FAAH (23)

FABP (5)

Factor Xa (20)

FAK (27)

Farnesyl Transferase (24)

Fatty Acid Synthase (FASN) (28)

Ferroptosis (72)

FGFR (73)

Filovirus (5)

FKBP (7)

FLAP (10)

Fungal (140)

FXR (3)

G-quadruplex (5)

GABA Receptor (24)

Galectin (3)

Gap Junction Protein (7)

GHSR (4)

Gli (3)

Glucagon Receptor (5)

Glucocorticoid Receptor (11)

Glucosidase (28)

GLUT (10)

Glutaminase (10)

Glutathione Peroxidase (10)

GlyT (12)

GPCR19 (2)

GPR120 (1)

GPR40 (4)

GPR55 (1)

GSNOR (1)

Guanylate Cyclase (5)

Gutathione S-transferase (11)

Haspin Kinase (4)

HBV (33)

HCN Channel (2)

HCV (111)

HCV Protease (23)

HDAC (117)

Hedgehog (13)

Hexokinase (4)

HIF/HIF Prolyl-Hydroxylase (47)

Hippo (MST) (3)

Histamine Receptor (36)

Histone Acetyltransferase (39)

Histone Demethylase (56)

Histone Methyltransferase (124)

HIV (216)

HIV Integrase (21)

HIV Protease (26)

HMG-CoA Reductase (HMGCR) (39)

HSP (62)

HSV (45)

IAP (11)

IFNAR (5)

IGF-1R (23)

iGluR (25)

IKK (44)

Imidazoline Receptor (5)

Influenza Virus (109)

Insulin Receptor (17)

Integrin (43)

Interleukin Related (55)

IRAK (20)

IRE1 (21)

Isocitrate Dehydrogenase (IDH) (20)

Itk (6)

JAK (115)

JNK (37)

Keap1-Nrf2 (24)

Kinesin (21)

KLF (4)

Lactate Dehydrogenase (11)

Leukotriene Receptor (19)

Ligand for Target Protein for PROTAC (27)

LIM Kinase (LIMK) (7)

Lipoxygenase (41)

LPL Receptor (14)

LRRK2 (18)

LXR (3)

mAChR (31)

MAGL (19)

MALT1 (6)

MAP4K (13)

MAPKAPK2 (MK2) (5)

MCHR1 (GPR24) (2)

MDM-2/p53 (55)

MEK (45)

Melanocortin Receptor (2)

Melatonin Receptor (2)

MELK (4)

mGluR (9)

MicroRNA (13)

Microtubule/Tubulin (101)

Mineralocorticoid Receptor (2)

Mitochondrial Metabolism (45)

Mitophagy (56)

Mixed Lineage Kinase (6)

MMP (68)

MNK (5)

Monoamine Oxidase (71)

Monoamine Transporter (13)

Monocarboxylate Transporter (8)

Mps1 (12)

mTOR (79)

MyD88 (4)

Myosin (14)

Na+/Ca2+ Exchanger (11)

Na+/K+ ATPase (19)

nAChR (16)

NADPH Oxidase (11)

NAMPT (17)

Neprilysin (15)

Neurokinin Receptor (4)

Neuropeptide Y Receptor (6)

Neurotensin Receptor (4)

NF-κB (148)

NKCC (6)

NO Synthase (50)

NOD-like Receptor (NLR) (19)

Notch (24)

Nucleoside Antimetabolite/Analog (44)

Opioid Receptor (10)

Orexin Receptor (OX Receptor) (2)

P-glycoprotein (44)

P2X Receptor (11)

P2Y Receptor (14)

p38 MAPK (80)

p97 (8)

PAI-1 (11)

PAK (15)

Parasite (176)

PARP (65)

PD-1/PD-L1 (27)

PDGFR (86)

PDHK (10)

PDK-1 (8)

PERK (8)

PGC-1α (1)

PGE synthase (15)

Phosphatase (122)

Phosphodiesterase (PDE) (177)

Phospholipase (54)

PI4K (13)

Pim (25)

PKA (30)

PKC (81)

PKD (4)

Polo-like Kinase (PLK) (29)

Porcupine (8)

Potassium Channel (93)

PPAR (30)

Procollagen C Proteinase (1)

Prostaglandin Receptor (35)

PROTAC (25)

PROTAC Linker (7)

Protease-Activated Receptor (PAR) (14)

Proteasome (51)

Protein Arginine Deiminase (11)

Proton Pump (45)

PTEN (5)

Pyk2 (6)

Pyroptosis (4)

Pyruvate Kinase (3)

RAD51 (10)

Raf (54)

RAR/RXR (10)

Ras (89)

Reactive Oxygen Species (72)

Renin (7)

RET (28)

Reverse Transcriptase (53)

RGS Protein (3)

Ribosomal S6 Kinase (RSK) (26)

RIP kinase (36)

ROCK (45)

ROR (10)

ROS (12)

RSV (17)

Salt-inducible Kinase (SIK) (7)

SARS-CoV (83)

Ser/Thr Protease (24)

Serotonin Transporter (42)

sFRP-1 (1)

SGK (8)

SGLT (27)

Sigma Receptor (6)

Sirtuin (33)

Smo (11)

SNIPER (12)

Sodium Channel (99)

Somatostatin Receptor (3)

SPHK (14)

Src (78)

SRPK (3)

STAT (73)

Stearoyl-CoA Desaturase (SCD) (12)

STING (3)

Survivin (3)

Syk (32)

Target Protein Ligand-Linker Conjugate (1)

Telomerase (9)

TGF-beta/Smad (14)

TGF-β Receptor (43)

Thrombin (26)

Thymidylate Synthase (9)

TNF Receptor (44)

Toll-like Receptor (TLR) (32)

TOPK (8)

Topoisomerase (102)

Trk Receptor (27)

TRP Channel (43)

Tryptophan Hydroxylase (11)

TSH Receptor (2)

Tyrosinase (36)

ULK (8)

URAT1 (5)

Urotensin Receptor (1)

Vasopressin Receptor (3)

VD/VDR (6)

VDAC (3)

VEGFR (145)

Virus Protease (36)

Wee1 (5)

Wnt (44)

Xanthine Oxidase (14)

YAP (11)

β-catenin (22)

γ-secretase (27)

By Research Areas:

Cancer (4878)

Cardiovascular Disease (715)

Endocrinology (251)

Infection (1324)

Inflammation/Immunology (1677)

Metabolic Disease (853)

Neurological Disease (1100)

9237

Inhibitors & Agonists

Screening Libraries

Dye Reagents

Biochemical Assay Reagents

338

Peptides

MCE Kits

Inhibitory Antibodies

1398

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-P1515

Angiotensin II (3-8), human
Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin II (3-8), human is a less effective agonist at the angiotensin AT₁ receptor.
HY-P1515A

Angiotensin II (3-8), human TFA
Angiotensin Receptor Cardiovascular Disease Endocrinology

Angiotensin II (3-8), human (TFA) is a less effective agonist at the angiotensin AT₁ receptor.

*Angiotensin II (3-8), human*	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Angiotensin II (3-8), human is a less effective agonist at the angiotensin AT₁ receptor.

*Angiotensin II (3-8), human TFA*	Angiotensin Receptor	Cardiovascular Disease Endocrinology
Angiotensin II (3-8), human (TFA) is a less effective agonist at the angiotensin AT₁ receptor.

HY-136170

MC-SN38	Drug-Linker Conjugates for ADC	Cancer
MC-SN38 is a drug-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody drug conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks.

HY-13704

SN-38 NK012	Topoisomerase ADC Cytotoxin Autophagy	Cancer
SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC₅₀s of 0.077 and 1.3 μM, respectively.

HY-15847

HS38	DAPK	Cardiovascular Disease
HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with K_ds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC₅₀ of 200 nM. HS38 can be used for the research of smooth muscle related disorders.

HY-126350

CL2-SN-38	Drug-Linker Conjugates for ADC	Cancer
CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.

HY-U00324

p38 MAPK-IN-2
p38 MAPK Autophagy Cancer

p38 MAPK-IN-2 is an inhibitor of p38 kinase.

p38 MAPK-IN-2	p38 MAPK Autophagy	Cancer
p38 MAPK-IN-2 is an inhibitor of p38 kinase.

HY-131057

Mc-VC-PAB-SN38	Drug-Linker Conjugates for ADC	Cancer
Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs).

HY-12339

NVS-CRF38
CRFR Endocrinology

NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.
HY-123999

CD38 inhibitor 1
Others Metabolic Disease

CD38 inhibitor 1 (compound 78c) is a potent CD38 inhibitor with IC₅₀s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38.
HY-18874

p38-α MAPK-IN-1
p38 MAPK Autophagy Others

p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC₅₀ of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

NVS-CRF38	CRFR	Endocrinology
NVS-CRF38 is a novel corticotropin-releasing factor receptor 1 (CRF1) antagonist with low water solubility.

CD38 inhibitor 1	Others	Metabolic Disease
CD38 inhibitor 1 (compound 78c) is a potent *CD38* inhibitor with IC₅₀s of 7.3 nM and 1.9 nM for hCD38 and mouse CD38.

p38-α MAPK-IN-1	p38 MAPK Autophagy	Others
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC₅₀ of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.

HY-12839

p38 MAPK-IN-1	p38 MAPK Autophagy	Inflammation/Immunology
p38 MAPK-IN-1 (Compound 4) is a novel potent and selective inhibitor of p38 MAPK with IC₅₀ of 68 nM. p38 MAPK-IN-1 shows sustained levels, low clearance and good bioavailability.

HY-128943

MAC glucuronide phenol-linked SN-38	Drug-Linker Conjugates for ADC	Cancer
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) drug linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC₅₀ values of 113 and 67 ng/mL, respectively.

HY-128946

CL2A-SN-38	Drug-Linker Conjugates for ADC	Cancer Inflammation/Immunology
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.

HY-108618

BC11-38	Phosphodiesterase (PDE)	Endocrinology
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC₅₀s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.

HY-114423

p38α inhibitor 1
p38 MAPK Autophagy Inflammation/Immunology

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

p38α inhibitor 1	p38 MAPK Autophagy	Inflammation/Immunology
p38α inhibitor 1 is a *p38α* inhibitor extracted from patent WO 2008076265 A1.

HY-119744

BAY 38-7271	Cannabinoid Receptor	Neurological Disease
BAY 38-7271 is selective and highly potent and cannabinoid CB₁/CB₂ receptor agonist, with K_is of 1.85 nM and 5.96 nM for recombinant human CB₁ receptor and CB₂ receptor, respectively. BAY 38-7271 has strong neuroprotective properties.

HY-128942

MAC glucuronide α-hydroxy lactone-linked SN-38	Drug-Linker Conjugates for ADC	Cancer
MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 drug linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC₅₀ values of 99 and 105 ng/mL, respectively.

HY-131335

p38α inhibitor 2	p38 MAPK	Inflammation/Immunology
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC₅₀ of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC₅₀=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.

HY-112272

Lerociclib
G1T38
CDK Cancer

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

Lerociclib G1T38	CDK	Cancer
Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

HY-112272A

Lerociclib dihydrochloride G1T38 dihydrochloride	CDK	Cancer
Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC₅₀s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

HY-P2538

Big Endothelin-1 (1-38), human	Vasopressin Receptor	Cardiovascular Disease
Big Endothelin-1 (1-38), human is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide.

HY-P1459

Sphistin Synthetic Peptide(12-38,Fitc in N-Terminal-Fluorescently Labeled Peptide)	Bacterial	Infection
Sphistin Synthetic Peptide (12-38, Fitc in N-Terminal-Fluorescently Labeled Peptide) is a truncated fragments of Sphistin Synthetic Peptide that shows potent antimicrobial activity.

HY-12403

Angiotensin (1-7) Ang-(1-7)	Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite	Inflammation/Immunology Cardiovascular Disease Endocrinology
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACE activity (IC₅₀=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .

HY-12403A

Angiotensin (1-7) (acetate) Ang-(1-7) (acetate)	Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Endogenous Metabolite	Endocrinology Inflammation/Immunology Cardiovascular Disease
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACE activity (IC₅₀=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium.

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-108261

Tomeglovir
BAY 38-4766
CMV Infection

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

Tomeglovir BAY 38-4766	CMV	Infection
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC₅₀s of 0.34 μM and 0.039 μM for HCMV and MCMV.

HY-10403

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

HY-14992

Bay 60-7550
BAY 607550
Phosphodiesterase (PDE) Neurological Disease

Bay 60-7550 is a potent and selective PDE2 inhibitor with a K_i of 3.8 nM.
HY-14975

R1487 Hydrochloride
p38 MAPK Autophagy Cancer

R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with K_d values of 0.2 nM and 29 nM for p38α and p38β, respectively.
HY-10401

VX-702
p38 MAPK Autophagy Inflammation/Immunology

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

Bay 60-7550 BAY 607550	Phosphodiesterase (PDE)	Neurological Disease
Bay 60-7550 is a potent and selective PDE2 inhibitor with a K_i of 3.8 nM.

R1487 Hydrochloride	p38 MAPK Autophagy	Cancer
R1487 Hydrochloride is a highly potent and selective *p38α* inhibitor, with K_d values of 0.2 nM and 29 nM for p38α and p38β, respectively.

VX-702	p38 MAPK Autophagy	Inflammation/Immunology
VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.

HY-10256A

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

HY-10256

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

HY-10402

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

HY-10295

SB 202190	p38 MAPK Autophagy Apoptosis Ferroptosis	Cancer Neurological Disease
SB 202190 is a selective p38 MAP kinase inhibitor with IC₅₀s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a K_d of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits.

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-114405

SJFδ
PROTAC p38 MAPK Autophagy Cancer

SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC₅₀ of 46.17 nM, but does not degrade p38α, p38β, or p38γ.

SJFδ	PROTAC p38 MAPK Autophagy	Cancer
SJFδ is a 10-atom linker PROTAC. SJFδ degrades *p38δ* with a DC₅₀ of 46.17 nM, but does not degrade p38α, p38β, or p38γ.

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-135674

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

HY-15288

PI3kδ inhibitor 1
PI3K Cancer

PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 3.8 nM.

PI3kδ inhibitor 1	PI3K	Cancer
PI3kδ inhibitor 1 is a potent and selective PI3Kδ inhibitor with an IC₅₀ of 3.8 nM.

HY-11087

SD 0006 SD-06	p38 MAPK Autophagy	Inflammation/Immunology
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC₅₀ of 110 nM for p38α.

HY-10328

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

HY-U00439

Protein kinase inhibitors 1
DYRK Cancer

Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC₅₀ of 74 nM and K_d of 9.5 nM.
HY-16715

Acumapimod
p38 MAPK Autophagy Inflammation/Immunology

Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC₅₀ of less than 1 μM for p38α.

*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.

Acumapimod	p38 MAPK Autophagy	Inflammation/Immunology
Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC₅₀ of less than 1 μM for p38α.

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-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.

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-16782

Pexmetinib ARRY-614	p38 MAPK Autophagy	Cancer
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

HY-13468

KW-2478
HSP Cancer

KW-2478 is an inhibitor of Hsp90α, with an IC₅₀ of 3.8 nM, and has antitumor activity against various human hematological tumor cells.

HY-108645

AL 8697	p38 MAPK Autophagy	Inflammation/Immunology
AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC₅₀ of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC₅₀=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.

HY-10512

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

AR-A014418 is a potent, selective and ATP-competitive GSK3β inhibitor (IC₅₀=104 nM; K_i=38 nM).
HY-112182

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

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

HY-10211

Tanespimycin 17-AAG; NSC 330507; CP 127374	HSP Autophagy Mitophagy Bacterial Apoptosis Antibiotic	Cancer Infection
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC₅₀ of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.

HY-14877

Anagliptin SK-0403	Dipeptidyl Peptidase	Metabolic Disease
Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC₅₀ of 3.8 nM, and less selective at DPP-8/9 (IC₅₀, 68, 60 nM, respectively).

HY-128947

CL2 Linker	ADC Linker	Cancer
CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in drug substitution (~6), cell binding (K_d ~1.2 nM), cytotoxicity (IC₅₀ ~2.2 nM), and serum stability in vitro (t_1/2 ~20 hours).

HY-10578

PD 169316	p38 MAPK Autophagy Enterovirus	Cancer
PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor, with IC₅₀ of 89 nM. PD169316 selectively inhibits the kinase activity of the phosphorylated p38 without hindering upstream kinases to phosphorylate p38. PD169316 shows antiviral activity against Enterovirus71. PD169316 shows antiviral activity against Enterovirus71.

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-B1197

Amcinonide
CL-34699
Glucocorticoid Receptor Inflammation/Immunology Endocrinology

Amcinonide inhibit NO release from activated microglia with IC50 3.38 nM.

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-103672

AZD7624
p38 MAPK Autophagy Inflammation/Immunology

AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.

HY-115521

Jarin-1	Others	Others
Jarin-1 is a jasmonic acid-amido synthetase (JAR1) inhibitor with an IC₅₀ of 3.8 μM. Jarin-1 specific inhibits bioactive JA (jasmonoyl-isoleucine, JA-Ile) biosynthesis in Arabidopsis and other plants.

HY-10454

Delanzomib CEP-18770	Proteasome NF-κB Apoptosis	Cancer
Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC₅₀ of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.

HY-128594

BACE1-IN-4	Beta-secretase	Neurological Disease
BACE1-IN-4 is a potent and highly selective BACE1 inhibitor, with an IC₅₀ of 3.8 nM and a K_i of 1.9 nM, more selective at BACE1 over BACE2. Anti-Alzheimer’s disease.

HY-12757

YHO-13177	BCRP	Cancer
YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.

HY-128817

cIAP1 Ligand-Linker Conjugates 12 E3 ligase Ligand-Linker Conjugates 38	E3 Ligase Ligand-Linker Conjugate	Cancer
cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs.

HY-15300

Skepinone-L
CBS3830
p38 MAPK Autophagy Inflammation/Immunology

Skepinone-L (CBS3830) is a selective p38 mitogen-activated protein kinase inhibitor.

HY-10456

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

HY-12855A

Lys05 Lys01 trihydrochloride	Autophagy	Cancer
Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC₅₀ values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.

HY-100114

TA-01	Casein Kinase p38 MAPK Autophagy	Cardiovascular Disease
TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC₅₀s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.

HY-N2232

N-Feruloyloctopamine	Akt p38 MAPK	Cancer
N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and *p38 MAPK*.

HY-15747A

Deltarasin hydrochloride
Ras Phosphodiesterase (PDE) Cancer

Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with K_d of 38 nM for binding to purified PDEδ.

HY-114404

SJFα	PROTAC p38 MAPK Autophagy	Cancer
SJFα is a 13-atom linker PROTAC. SJFα degrades *p38α* with a DC₅₀ of 7.16 nM, but is far less effective at degrading p38δ (DC₅₀=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM.

HY-110398

5,6,7-Trimethoxyflavone Baicalein trimethyl ether	p38 MAPK	Inflammation/Immunology Cancer
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.

HY-13983

IDO-IN-7
NLG-919 analogue; GDC-0919 analogue
Indoleamine 2,3-Dioxygenase (IDO) Cancer

IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC₅₀ of 38 nM.
HY-15747

Deltarasin
Ras Phosphodiesterase (PDE) Cancer

Deltarasin is an inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ.
HY-18850

MAPK13-IN-1
p38 MAPK Autophagy Others

MPAK13-IN-1 is a MAPK13 (p38δ) inhibitor, with an IC₅₀ of 620 nM.

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-18862

PF-03715455	p38 MAPK	Inflammation/Immunology
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC₅₀ values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC₅₀=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).

HY-10619B

Niraparib tosylate MK-4827 tosylate	PARP Apoptosis	Cancer
Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC₅₀ of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

HY-120111

MW-150 MW01-18-150SRM	p38 MAPK Autophagy	Inflammation/Immunology Neurological Disease
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K_i of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

HY-106723

AMP-PCP
HSP Cancer

AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a K_d value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90.

HY-13913

NS-398	COX	Inflammation/Immunology Cancer
NS-398 is a non-steroidal an-inflammatory agent with analgesic and antipyretic effects, and selectively inhibits prostaglandin G/H synthase 2/cyclooxygenase 2 (COX-2) activity, with an IC₅₀ of 3.8 μM, and has no effect on COX-1 at 100 μM.

HY-10619

Niraparib MK-4827	PARP Apoptosis	Cancer
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

HY-10619A

Niraparib hydrochloride MK-4827 hydrochloride	PARP Apoptosis	Cancer
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

HY-B0224

Chlorothiazide
Others Cardiovascular Disease

Chlorothiazide is a diuretic and antihypertensive. (IC50=3.8 mM)

HY-106723A

AMP-PCP disodium	HSP	Cancer
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a K_d value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90.

HY-N1969

3,3'-Di-O-methylellagic acid 3,8-Di-O-methylellagic acid	Others	Infection
3,3'-Di-O-methylellagic acid obtained from Euphorbia adenochlora selectively inhibits the formation of acid-fastness in mycobacteria without retardation of their growth. 3,3'-di-O-methylellagic acid as a hepatoprotective compound is apparently due to its antioxidative effect.

HY-119917

Gossypetin	p38 MAPK MEK Bacterial	Cancer Infection
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the *MKK3/6-p38* signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.

HY-N0316

Mollugin	Others	Cancer
Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .

HY-120012

AZD9567	Glucocorticoid Receptor	Inflammation/Immunology Endocrinology
AZD9567 (compound 15) is a potent, oral active, non-steroidal and selective glucocorticoid receptor modulator (SGRM), with an IC₅₀ of 3.8 nM. Exhibits excellent efficacy in the streptococcal cell wall (SCW) reactivation model of joint inflammation.

HY-100429

CAN508	CDK	Cancer
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC₅₀ of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.

HY-12075

LY2109761
TGF-β Receptor Autophagy Cancer

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

HY-10404

Dilmapimod SB-681323; GW 681323	p38 MAPK Autophagy	Inflammation/Immunology Cancer
Dilmapimod (SB-681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.

HY-111760

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

HY-50674

INCB3344	CCR	Inflammation/Immunology Endocrinology
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC₅₀ values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

HY-10406

Talmapimod SCIO-469	p38 MAPK	Cancer
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive *p38α* inhibitor with an IC₅₀ of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

HY-10406A

Talmapimod hydrochloride SCIO-469 hydrochloride	p38 MAPK	Cancer
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive *p38α* inhibitor with an IC₅₀ of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.

HY-120111A

MW-150 hydrochloride MW01-18-150SRM hydrochloride	p38 MAPK Autophagy	Inflammation/Immunology Neurological Disease
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K_i of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

HY-112432

GlyT1 Inhibitor 1
GlyT Neurological Disease

GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC₅₀ of 38 nM for rGlyT1. Antipsychotic activity.
HY-134358

Ara-F-NAD+
Others Neurological Disease

Ara-F-NAD+, an arabino analogue of NAD⁺, is a potent, slow-binding CD38 NADase inhibitor, with a K_i of 169 nM.
HY-12019

SGX-523
c-Met/HGFR Cancer

SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.
HY-10212

BIIB021
CNF2024
HSP Autophagy Cancer

BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a K_i and an EC₅₀ of 1.7 nM and 38 nM, respectively.
HY-19900

ITX5061
p38 MAPK Autophagy HCV Infection

ITX5061 is a type II inhibitor of p38 MAPK and also an antagonist of scavenger receptor B1 (SR-B1).
HY-111463

CDK8-IN-3
CDK Cancer Metabolic Disease Inflammation/Immunology

CDK8-IN-3 is an inhibitor of CDK8 extracted from patent WO2016041618A1, compound example 1.7.

HY-18161

CCT241736	FLT3 Aurora Kinase	Cancer
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A K_d, 7.5 nM, IC₅₀, 38 nM; Aurora-B K_d, 48 nM), FLT3 kinase (K_d, 6.2 nM), and FLT3 mutants including FLT3-ITD (K_d, 38 nM) and FLT3(D835Y) (K_d, 14 nM).

HY-13241

Ralimetinib dimesylate LY2228820 dimesylate	p38 MAPK Autophagy Apoptosis	Cancer Inflammation/Immunology
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

HY-131707

LEO 39652	Phosphodiesterase (PDE)	Inflammation/Immunology
LEO 39652 is a dual-soft PDE4 inhibitor with IC₅₀s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC₅₀ value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .

HY-18754

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

HY-14374

GPP78 CAY10618	NAMPT Autophagy	Cancer Inflammation/Immunology
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC₅₀ of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC₅₀ of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.

HY-15557

AZ20
ATM/ATR Cancer

AZ20 is a potent and selective inhibitor of ATR with an IC₅₀ of 5 nM, and has 8-fold selectivity against mTOR (IC₅₀=38 nM).
HY-18306

SB 242235
p38 MAPK Autophagy Cancer

SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC₅₀ of 1.0　μM in primary human chondrocytes.

HY-117273

AZ304	Raf Autophagy	Cancer
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC₅₀s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC₅₀, 6 nM), CSF1R (IC₅₀, 35 nM). Anti-tumor activity.

HY-120111B

MW-150 dihydrochloride dihydrate MW01-18-150SRM dihydrochloride dihydrate	p38 MAPK Autophagy	Inflammation/Immunology Neurological Disease
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a K_i of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

HY-13241A

Ralimetinib LY2228820	p38 MAPK Autophagy	Cancer Inflammation/Immunology
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC₅₀s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.

HY-18754A

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

HY-101518

APG-115 AA-115	MDM-2/p53 E1/E2/E3 Enzyme Apoptosis	Cancer
APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC₅₀ and K_i values of 3.8 nM and 1 nM, respectively. APG-115 blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.

HY-10971

Alisertib MLN 8237	Aurora Kinase Autophagy Apoptosis	Cancer
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC₅₀=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the *AKT/mTOR/AMPK/p38* pathway in leukemic cells. Antitumor activity.

HY-P0216

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

HY-15778A

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

HY-104065

Pyrotinib
SHR-1258
EGFR Cancer

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC₅₀s of 13 and 38 nM, respectively.
HY-15811

XMD8-87
ACK1-B19
Tyrosinase Cancer

XMD8-87 is a potent TNK2 inhibitor with IC₅₀ values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
HY-103001

HMN-154
Others Cancer

HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC₅₀ values of 0.0026 and 0.003 μg/mL, respectively.

HY-N1517

Ganoderic acid C2	Others	Cancer
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitory activity against the rat lens aldose reductase (RLAR) with an IC₅₀ of 3.8 µM.

HY-100526

XMU-MP-1
Hippo (MST) Cancer

XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC₅₀s of 71.1 and 38.1 nM, respectively.

HY-18271

CaMKII-IN-1	CaMK Autophagy	Inflammation/Immunology
CaMKII-IN-1 is a potent and highly selective CaMKII inhibitor with IC50 of 63 nM; significantly high selectivity against CaMKIV, MLCK, p38a, Akt1, and PKC.

HY-108643

CMPD1
MAPKAPK2 (MK2) Cancer

CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent K_i (K_i^app) of 330 nM.

HY-16736

Centanafadine EB-1020	Adrenergic Receptor Dopamine Transporter Serotonin Transporter	Neurological Disease Endocrinology
Centanafadine 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-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-126296

RIPK1-IN-3
RIP kinase Inflammation/Immunology

RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties.
HY-104065B

Pyrotinib dimaleate
SHR-1258 dimaleate
EGFR Cancer

Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC₅₀s of 13 and 38 nM, respectively.

HY-50674A

INCB3344 R-isomer	Others	Inflammation/Immunology
INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC₅₀ values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

HY-N0168A

(Rac)-Hesperetin	p38 MAPK Apoptosis Autophagy	Cancer Neurological Disease
(Rac)-Hesperetin is the racemate of Hesperetin. Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation.

HY-11034

CVT-12012	Stearoyl-CoA Desaturase (SCD)	Metabolic Disease
CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC₅₀s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

HY-70044

GSK-1070916 GSK-1070916A	Aurora Kinase Apoptosis	Cancer
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with K_is of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.

HY-N0265

Asperosaponin VI	Caspase Apoptosis	Cardiovascular Disease
Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway. Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB.

HY-N2270

Chicanine	p38 MAPK ERK IKK	Inflammation/Immunology
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity.

HY-107523

WAY-213613	EAAT2	Neurological Disease
WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC₅₀ of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC₅₀s are 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.

HY-W018643

Ferulic acid methyl ester Methyl ferulate	p38 MAPK Autophagy	Inflammation/Immunology Neurological Disease Cancer
Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks *p-p38* and p-JNK in primary bone marrow derived-macrophages.

HY-107523A

WAY-213613 hydrochloride	EAAT2	Neurological Disease
WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC₅₀ of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC₅₀s are 5 and 3.8 μM, respectively). WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.

HY-N3032

Xanthatin	Apoptosis VEGFR Lipoxygenase Bacterial	Cancer Infection Inflammation/Immunology
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC₅₀ of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.

HY-19330

DASA-58
Pyruvate Kinase Cancer

DASA-58 is a potent activator of pyruvate kinase M2 (PKM2) with an AC₉₀ of 680 nM, and an AC₅₀ of 38 nM.

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-15965

Uprosertib
GSK2141795
Akt Cancer

Uprosertib (GSK2141795) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

HY-12299

WH-4-023 Dual LCK/SRC inhibitor	Src	Cancer
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC₅₀ of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.

HY-15965A

Uprosertib hydrochloride GSK2141795 (hydrochloride)	Akt	Cancer
Uprosertib hydrochloride (GSK2141795 hydrochloride) is a potent and selective pan-Akt inhibitor with IC₅₀ values of 180/328/38 nM for Akt1/Akt2/Akt3, respectively.

HY-N2666

5α-Hydroxycostic acid	VEGFR	Cancer
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and *Ang2/Tie2* pathways.

HY-12511

SKF-86002	p38 MAPK	Inflammation/Immunology
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.

HY-W007355

Skatole 3-Methylindole; 3-Methyl-1H-indole	Aryl Hydrocarbon Receptor p38 MAPK Endogenous Metabolite Autophagy Bacterial Fungal	Others
Skatole is produced by intestinal bacteria, regulates intestinal epithelial cellular functions through activating aryl hydrocarbon receptors and *p38*.

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-16558

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

HY-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-32718

Pelitinib EKB-569; WAY-EKB 569	EGFR Src	Cancer
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC₅₀ of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC₅₀s of 282, 800, and 1255 nM, respectively.

HY-112614

ATM Inhibitor-1	ATM/ATR	Cancer
ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC₅₀ of 0.7 nM, shows weak activity against mTOR (IC₅₀, 21 μM), DNAPK (IC₅₀, 2.8 μM), PI3Kα (IC₅₀, 3.8 μM), PI3Kβ (IC₅₀, 10.3 μM), PI3Kγ (IC₅₀, 3 μM) and PI3Kδ (IC₅₀, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.

HY-101910

PSB-12062
N-(p-Methylphenylsulfonyl)phenoxazine
P2X Receptor Neurological Disease

PSB-12062 is a potent and selective P2X4 antagonist with an IC₅₀ of 1.38 μM for human P2X4.

HY-14305A

BMS-582949 hydrochloride	p38 MAPK Autophagy	Inflammation/Immunology
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC₅₀ of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.

HY-115453

UBCS039
Sirtuin Autophagy Cancer

UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC₅₀ of 38 μM.

HY-10505

Orteronel TAK-700	Others	Cancer
Orteronel is a highly selective inhibitor of human 17,20-lyase with IC₅₀ of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.

HY-N4202

Dihydrorotenone	Mitochondrial Metabolism Apoptosis	Neurological Disease
Dihydrorotenone, a natural pesticide, is a potent mitochondrial inhibitor. Dihydrorotenone probably induces Parkinsonian syndrome. Dihydrorotenone induces human plasma cell apoptosis by triggering endoplasmic reticulum stress and activating p38 signaling pathway.

HY-120097

R-10015	LIM Kinase (LIMK) Reverse Transcriptase	Infection
R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC₅₀ of 38 nM for human LIMK1.

HY-119257

ABT-100	Farnesyl Transferase Apoptosis	Cancer
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC₅₀s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity.

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 IC₅₀s of 10.9, 12 and 12.1 nM, respectively; also inhibits Notch signaling with IC₅₀ of 14.1 nM.

HY-N2406

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

HY-129997

Luteolinidin chloride	Others	Inflammation/Immunology
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.

HY-16759

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

HY-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-103021

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

HY-10520

CGP 57380	MNK Apoptosis	Cancer
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC₅₀ of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

HY-N0505

Rosiridin	Monoamine Oxidase	Neurological Disease
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC₅₀=5.38).

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-N7377

Butyl isobutyl phthalate	Glucosidase	Metabolic Disease
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC₅₀ value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment.

HY-18991

CCG215022	PKA	Cancer
CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC₅₀s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.

HY-P1125

4-CMTB
Others Others

4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC₅₀=6.38).

HY-N0809

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

HY-135845

TP3011 CH0793011	Topoisomerase	Cancer
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38. TP3011 is against cancer cell lines growth with IC₅₀s at the range sub-nanomolar in vitro.

HY-100115

TA-02	p38 MAPK Autophagy	Cancer Inflammation/Immunology Cardiovascular Disease
TA-02, an analog of SB 203580 (HY-10256), is a p38 MAPK inhibitor with an IC₅₀ of 20 nM. TA-02 especially inhibits TGFBR-2. TA-02 exhibits similar cardiogenic properties as SB 203580 and SB 202190 (HY-10295).

HY-P1424

Lei-Dab7	Potassium Channel
Lei-Dab7 is a high affinity, selective K_Ca2.2 (SK2) channel blocker (K_d=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for K_Ca2.2 over K_Ca2.1, K_Ca2.3, K_Ca3.1, K_v and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.

HY-126325

BY27	Epigenetic Reader Domain	Cancer
BY27 is a potent and selective BET BD2 inhibitor, shows 38, 5, 7, and 21-fold BD1/BD2 selectivity for BRD2, BRD3, BRD4, and BRDT. Anti-cancer activity.

HY-10008

SNS-032 BMS-387032	CDK Apoptosis	Cancer
SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC₅₀s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.

HY-N0722

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

HY-13018

MRT67307	IKK ULK Autophagy	Cancer Inflammation/Immunology
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.

HY-13018A

MRT67307 hydrochloride	IKK ULK Autophagy	Cancer Inflammation/Immunology
MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.

HY-N6826

Asatone	NF-κB	Inflammation/Immunology
Asatone is an active component isolated from Radix et Rhizoma Asari, with anti-inflammatory effect via activation of NF-κB and donwn regulation of p-MAPK (ERK, JNK and p38) pathways.

HY-19624

NVP-ACC789 ACC-789; ZK202650	VEGFR PDGFR	Cancer
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC₅₀s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.

HY-B0846

Dimethomorph	Fungal Androgen Receptor	Infection
Dimethomorph is a morpholine fungicide that inhibits fungal cell wall formation. Dimethomorph inhibits mycelial growth of the oomycete fungi, *P. citrophthora, P. parasitica, P. capsici, and P. infestans* (EC₅₀s=0.1, 0.38, <0.1, and 0.16-0.3 µg/mL, respectively), but is less active against the green algae species C. vulgaris or S. obliquus in vitro (EC₅₀s=47.46 and 44.87 µg/mL, respectively). Dimethomorph inhibits androgen receptor (AR) activity in a reporter assay in MDA-kb2 human breast cancer cells but not in a yeast antiandrogen screen (IC₂₀s=0.263 and 38.5 µM, respectively).

HY-12305

Q-VD-OPh QVD-OPH; Quinoline-Val-Asp-Difluorophenoxymethylketone	Caspase HIV	Cancer Infection
Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC₅₀ of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.

HY-107597

SU3327	JNK	Metabolic Disease Inflammation/Immunology
SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC₅₀ of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC₅₀ of 239 nM. SU3327 shows less active against p38α and Akt kinase.

HY-P2319

OVA-E1 peptide	p38 MAPK JNK	Inflammation/Immunology
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.

HY-N0840

Bruceantin (-)-Bruceantin; NCI165563; NSC165563	Others	Cancer
Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.

HY-N0674A

Dehydrocorydaline chloride 13-Methylpalmatine chloride	Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy	Cancer Infection
Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline chloride shows strong anti-malarial effects (IC₅₀ =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

HY-N0674

Dehydrocorydaline 13-Methylpalmatine	Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy	Cancer Infection
Dehydrocorydaline (13-Methylpalmatine) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline shows strong anti-malarial effects (IC₅₀ =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

HY-P1236

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

HY-14728

Aleglitazar R1439; RO0728804	PPAR	Metabolic Disease
Aleglitazar (R1439) is a potent dual PPARα/γ agonist, with IC₅₀s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

HY-P2319A

OVA-E1 peptide TFA	p38 MAPK JNK	Inflammation/Immunology
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes.

HY-19921

JTK-853	HCV	Infection
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC₅₀s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.

HY-P1236A

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

HY-10542

GW 5074	Raf Apoptosis	Cancer
GW 5074 is a potent and selective c-Raf inhibitor with IC₅₀ of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.

HY-N1353

Rhamnocitrin	Others	Inflammation/Immunology Cardiovascular Disease
Rhamnocitrin is a flavonoid isolated from astragalus complanatus R. Br. (Sha-yuan-zi). Rhamnocitrin is a scavenger of DPPH with an IC₅₀ of 28.38 mM. Rhamnocitrin has anti-oxidant, anti-inflammatory and an-tiatherosclerosis activity.

HY-128591

DIPQUO	Others	Metabolic Disease
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC₅₀ of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.

HY-114379

AS2717638	LPL Receptor	Inflammation/Immunology
AS2717638 is an oral active and selective lysophosphatidic acid receptor 5 (LPA5) antagonist, with an IC₅₀ of 38 nM for hLPA5. AS2717638 also significantly improves PGE₂-, PGF_2α-, and AMPA-induced allodynia.

HY-N4238

Dehydrocorydaline nitrate 13-Methylpalmatine nitrate	Bcl-2 Family Caspase PARP p38 MAPK Parasite Autophagy	Cancer Infection
Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid isolated from traditional Chinese herb Corydalis yanhusuo W.T. Wang. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC₅₀ =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.

HY-16434

DGAT1-IN-3	Acyltransferase	Metabolic Disease
DGAT1-IN-3 is a potent, selective and orally bioavailable inhibitor of DGAT-1, with IC₅₀s of 38 nM for human DGAT-1 and 120 nM for rat DGAT-1. DGAT1-IN-3 could be used to research of obesity, dyslipidemia, and metabolic syndrome.

HY-111820

CK1-IN-1	Casein Kinase	Inflammation/Immunology
CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC₅₀s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

HY-124614

GLP-26	HBV	Infection
GLP-26 is a HBV capsid assembly modulators (CAM), inhibits HBV DNA replication in Hep AD38 system (IC₅₀=3 nM), and reduces cccDNA by >90% at 1 μM. GLP-26 disrupts the encapsidation of pre-genomic RNA, causes nucleocapsid disassembly and reduces cccDNA pools.

HY-14894

Ipragliflozin ASP1941	SGLT	Metabolic Disease
Ipragliflozin (ASP1941) is an orally active and selective SGLT2 inhibitor with IC₅₀s of 7.38 and 1876 nM, 6.73 and 1166 nM, 5.64 and 1380 nM for human SGLT2 and SGLT1, rat SGLT2 and SGLT1, mouse SGLT2 and SGLT1, respectively. Antidiabetic agent.

HY-16071

AT13148	Akt PKA ROCK Ribosomal S6 Kinase (RSK)	Cancer
AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC₅₀s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.

HY-129522

Sulfo-ara-F-NMN CZ-48	Toll-like Receptor (TLR)	Neurological Disease
Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting *CD38* (IC₅₀ around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.

HY-19337

ORM-15341	Androgen Receptor	Endocrinology
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.

HY-107725

BIBO3304 TFA	Neuropeptide Y Receptor	Metabolic Disease
BIBO3304 TFA is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC₅₀=0.38 and 0.72 nM, respectively).

HY-15856

cis-(Z)-Flupentixol dihydrochloride cis-(Z)-Flupenthixol dihydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with K_i values of 0.38 nM and 7 nM for D2 receptor and 5-HT_2A, respectively.

HY-19333

OG-L002	Histone Demethylase Monoamine Oxidase HSV	Infection
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC₅₀ of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC₅₀s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes.

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-121879

SHP836
Phosphatase Cancer

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

HY-135034

UMB68 sodium	Others	Neurological Disease
UMB68 sodium is a selective GHB receptor ligand. UMB68 sodium displaces [³H]NCS-382 with an IC₅₀ of 38 nM in rat cerebrocortical membranes. UMB68 sodium has no significant affinity at GABAB receptors, cannot be metabolized to GABA-active compounds.

HY-112762

LHF-535	Arenavirus	Infection
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC₅₀s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.

HY-124679

DS86760016	Bacterial	Infection
DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC₅₀s of 0.38, 0.62, and 0.16 μM, respectively.

HY-113756A

Latanoprost acid	Prostaglandin Receptor	Inflammation/Immunology
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.

HY-109041

Razuprotafib AKB-9778	Phosphatase	Inflammation/Immunology
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC₅₀of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC₅₀ of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC₅₀=36 pM) and HPTPγ (100 pM).

HY-15314

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

HY-N0108

Physcion Parietin; Rheochrysidin	Bacterial	Cancer Infection Inflammation/Immunology
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC₅₀ and a K_d of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.

HY-119163

L-902688	Prostaglandin Receptor	Inflammation/Immunology Cardiovascular Disease
L-902688 is a potent, selective and orally active EP4 receptor agonist with a K_i of 0.38 nM and an EC₅₀ of 0.6 nM. L-902688 shows >4,000-fold selective for EP4 over other EP and prostanoid receptors.

HY-N2375

L-Quebrachitol	Wnt β-catenin	Metabolic Disease
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.

HY-114933

VU0119498	mAChR	Metabolic Disease
VU0119498 is a pan G_q mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC₅₀s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity.

HY-107427

PF-3644022	MAPKAPK2 (MK2) p38 MAPK	Inflammation/Immunology
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 5.2 nM and a K_i of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC₅₀s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.

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-108632

BYK204165	PARP	Cancer
BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC₅₀ of 7.35 (pK_i=7.05), and murine PARP-2 (mPARP-2) with a pIC₅₀ of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1.

HY-12436

NTRC-824	Neurotensin Receptor	Neurological Disease
NTRC-824 (Compound 5) is a potent, selective and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist with an IC₅₀ of 38 nM and a K_i of 202 nM. NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (K_i >30 μM).

HY-136342

Antitumor agent-23	Others	Cancer
Antitumor agent-23 is a potent anti-cancer agent with GI₅₀s of 38, 48, 5, 27, 80, and 28 nM for lymphoma cell line GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI, respectively. Antitumoral activity.

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-13863

Hydroxy-Dynasore Dyngo-4a	Dynamin	Neurological Disease
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC₅₀ values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC₅₀ of 5.7 μM in vitro.

HY-18766

EW-7195	TGF-β Receptor p38 MAPK	Cancer
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC₅₀ of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.

HY-107426

Verrucarin A Muconomycin A	Apoptosis Reactive Oxygen Species	Cancer
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.

HY-18303

AMG-47a	Src VEGFR p38 MAPK JAK	Inflammation/Immunology
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC₅₀ of 0.2 nM. AMG-47a also inhibits VEGF2, *p38α, Jak3* and MLR and IL-2 with IC₅₀s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.

HY-N7255

Cycloartenol	p38 MAPK Apoptosis	Cancer
Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.

HY-13334

BGT226 maleate NVP-BGT226 maleate	PI3K mTOR Autophagy Apoptosis	Cancer
BGT226 (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-N0646

Silydianin	Phosphatase	Cancer
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC₅₀ of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.

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-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-13334A

BGT226 NVP-BGT226	PI3K mTOR Autophagy	Cancer
BGT226 (NVP-BGT226) 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-N2259

Curcumenol (+)-Curcumenol	Cytochrome P450	Cancer Inflammation/Immunology Neurological Disease
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC₅₀ of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.

HY-N2208

4-Hydroxylonchocarpin	p38 MAPK Autophagy	Cancer Infection Metabolic Disease Inflammation/Immunology
4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities.

HY-N1483

Guanfu base A	Potassium Channel	Cardiovascular Disease
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a K_i of 1.20 μM in human liver microsomes (HLMs) and a K_i of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (K_i of 0.38 μM) and dog (K_i of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.

HY-123824

GNE-0439	Others	Neurological Disease
GNE-0439 is a novel Nav1.7-selective inhibitor with IC₅₀ of 0.34 uM and inhibits Nav1.5 with an IC₅₀ of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC₅₀=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders.

HY-108587

ICA 110381	Potassium Channel	Neurological Disease
ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/Q3 agonist (EC₅₀=0.38 μM) as well as KCNQ1 antagonist (IC₅₀=15 μM).

HY-120789

PF-06648671	γ-secretase	Neurological Disease
PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.

HY-112762A

(E)-LHF-535	Arenavirus	Infection
(E)-LHF-535 is the E-isomer of LHF-535. LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC₅₀s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively.

HY-107417

Hypothemycin	VEGFR MEK FLT3 PDGFR ERK	Cancer
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with K_is of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.

HY-122114

ICA-27243	Potassium Channel	Neurological Disease
ICA-27243 is a selective, potent and orally active KCNQ2/Q3 potassium channel opener with an EC₅₀ of 0.38 μM. ICA-27243 is less effective at activating KCNQ4 and KCNQ3/Q5. ICA-27243 has antiepileptic and anticonvulsant effects.

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-N0619

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

HY-13948

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

HY-13948A

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

HY-16688

RU 24969	5-HT Receptor	Neurological Disease
RU 24969 is a preferential 5-HT_1B agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.

HY-50730

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

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-16688B

RU 24969 hemisuccinate	5-HT Receptor	Neurological Disease
RU 24969 hemisuccinate is a preferential 5-HT_1B agonist, with a K_i of 0.38 nM, but also displays appreciable affinity for the 5-HT_1A receptor (K_i=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion.

HY-100195

SAR-020106	Checkpoint Kinase (Chk)	Cancer
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC₅₀ of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.

HY-18758

IN-1130	TGF-β Receptor	Cancer Inflammation/Immunology
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC₅₀ of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC₅₀=36 nM) and p38α mitogen-activated protein kinase (IC₅₀=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis.

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-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-N7665

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

HY-136390

ML417	Dopamine Receptor	Neurological Disease
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC₅₀ of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.

HY-P1163

D[LEU4,LYS8]-VP	Vasopressin Receptor	Neurological Disease Cardiovascular Disease
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V_1b receptor, with the K_is of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V_1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities.

HY-N0619A

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

HY-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-P1163A

D[LEU4,LYS8]-VP TFA	Vasopressin Receptor	Neurological Disease Cardiovascular Disease
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V_1b receptor, with the K_is of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V_1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities.

HY-N6002

3'-Hydroxypterostilbene	Apoptosis Autophagy	Cancer
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC₅₀s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.

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-135795

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

HY-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-21994

Org-12962 hydrochloride	5-HT Receptor	Neurological Disease
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT_2C receptor agonist and exhibits pEC₅₀ values of 7.01, 6.38 and 6.28 for 5-HT_2C, 5-HT_2A and 5-HT_2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.

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-136065

bpV(phen)	PTEN Phosphatase Parasite Apoptosis	Cancer Infection Metabolic Disease Inflammation/Immunology
bpV(phen), a insulin-mimetic agent, 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-126291

GNE-616	Sodium Channel	Neurological Disease
GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (K_i of 0.79 nM and K_d of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM K_d and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively.

HY-112289

IDH889	Isocitrate Dehydrogenase (IDH)	Cancer
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC₅₀s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1^R132H, IDH1^R132C and IDH1^wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC₅₀ of 0.014 μM.

HY-138563

GSK973	Epigenetic Reader Domain	Cancer
GSK973 is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC₅₀ of 7.8 and a pK_d of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC₅₀=7.4~7.8; pK_d=8.3~8.5).

HY-N0925

Tetrahydroberberine Canadine	Dopamine Receptor	Neurological Disease
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).

HY-122818

bpV(phen) trihydrate	PTEN Phosphatase Parasite Apoptosis	Cancer Infection Metabolic Disease Inflammation/Immunology
bpV(phen) trihydrate, a insulin-mimetic agent, 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) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate 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) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.

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-15477A

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

HY-15477

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

HY-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-108511A

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

HY-13106

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

HY-131345A

(S)-PI3Kα-IN-4	PI3K	Cancer
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC₅₀ of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer.

HY-11007

GNF-2
Bcr-Abl SARS-CoV Cancer

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

HY-12583

A-366	Histone Methyltransferase Epigenetic Reader Domain	Cancer
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC₅₀s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC₅₀=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (K_i=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.

HY-118152

Org-12962	5-HT Receptor	Neurological Disease
Org-12962 is a potent, selective and orally active 5-HT_2C receptor agonist with a pEC₅₀ value of 7.01. Org-12962 also exhibits high effacy for the 5-HT_2A and 5-HT_2B receptor with pEC₅₀s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.

HY-B1101

Pimethixene Pimetixene	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-B1101A

Pimethixene maleate Pimetixene maleate	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-N0515

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

HY-122872

MKK7-COV-9	p38 MAPK	Cancer
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC₅₀ of 4.98 μM.

HY-15295

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

HY-100007

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

HY-120944

BAY-7598	MMP	Inflammation/Immunology
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC₅₀s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.

HY-137471

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

HY-131344

mTOR inhibitor-8	mTOR Autophagy	Cancer
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.

HY-136123

Tubulin inhibitor 8	Microtubule/Tubulin	Cancer
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC₅₀ of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC₅₀ of 14 nM.

HY-136122

Tubulin inhibitor 7	Microtubule/Tubulin	Cancer
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC₅₀ of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC₅₀ of 11 nM.

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-112851

Diacylglycerol acyltransferase inhibitor-1
Acyltransferase Metabolic Disease

Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
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-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-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-112722

Neurotoxin Inhibitor
Others Neurological Disease

Neurotoxin Inhibitor is a neurotoxin inhibitor.

HY-137497

KRAS inhibitor-9	Ras Apoptosis	Cancer
KRAS inhibitor-9, a potent KRAS inhibitor (K_d=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.

HY-D0843

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

HY-101275

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

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

HY-13278A

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

HY-111370

mTOR inhibitor-2	mTOR	Cancer
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC₅₀ of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.

HY-119369

FadD32 Inhibitor-1
Bacterial Infection

FadD32 Inhibitor-1 is a potent FadD32 inhibitor with anti-tubercular activity.
HY-111412

DAAO inhibitor-1
Others Neurological Disease

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

HY-21141

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

HY-17541A

Cysteine Protease inhibitor hydrochloride
Cathepsin Others

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

Cysteine Protease inhibitor
Cathepsin Others

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

mTOR inhibitor-1
mTOR Autophagy Cancer

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

HY-70005

CPA inhibitor Carboxypeptidase inhibitor	Carboxypeptidase	Metabolic Disease
CPA inhibitor (Carboxypeptidase inhibitor; compound 5) is a potent carboxypeptidase A (CPA) inhibitor with a K_i of 0.32 μM.

HY-130260

KRAS inhibitor-4
Ras Cancer

KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents.

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-10442

3-Deazaneplanocin A DZNep; 3-Deazaneplanocin	Histone Methyltransferase	Cancer
3-Deazaneplanocin A (DZNep) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.

HY-138295

KRAS inhibitor-10	Ras	Cancer
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.

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. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.

HY-112807

SGLT inhibitor-1	SGLT	Metabolic Disease
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC₅₀s of 43 nM and 9 nM, respectively.

HY-128722

HIV-1 inhibitor-3
HIV Infection

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

ARN272
Others Neurological Disease

ARN272 is an anandamide transport inhibitor.
HY-12202

MEK inhibitor
MEK Cancer

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

Allylthiourea
Thiosinamine; N-Allylthiourea
Reactive Oxygen Species Metabolic Disease

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

Tyrosine kinase inhibitor
c-Met/HGFR Cancer

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

Gabexate mesylate
FOY
Factor Xa Proteasome Inflammation/Immunology

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

HY-32015

Cot inhibitor-1	MAP3K	Inflammation/Immunology
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC₅₀ of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC₅₀ of 5.7 nM.

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-115514A

BRK inhibitor P21d hydrochloride	Others	Cancer
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC₅₀ of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC₅₀ of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.

HY-128859

EMT inhibitor-2	Cytochrome P450	Metabolic Disease
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC₅₀s of 49.72 and 5.54 μM, respectively.

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-128917

DNA31
DNA/RNA Synthesis Infection

DNA31 is a potent RNA polymerase inhibitor.
HY-15182

Collagen proline hydroxylase inhibitor-1
Others Cancer

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

Tyrphostin AG 112
EGFR Cancer

Tyrphostin AG 112 is an EGFR phosphorylation inhibitor.
HY-119372

TDP1 Inhibitor-1
Phosphodiesterase (PDE) Cancer

TDP1 Inhibitor-1 is a potent Tyrosyl-DNA Phosphodiesterase 1 (TDP1) inhibitor with an IC₅₀ of 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-128617

Legumain inhibitor 1
Others Cancer

Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC₅₀ of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
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-112390A

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

HY-122723

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

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-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-135864

KRAS inhibitor-6
Ras Cancer

KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
HY-135866

KRAS inhibitor-8
Ras Cancer

KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
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-135865

KRAS inhibitor-7
Ras Cancer

KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.

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-118810

BIO-013077-01
TGF-β Receptor Cancer

BIO-013077-01 is a pyrazole TGF-β inhibitor.
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-112906

C-176
STING Inflammation/Immunology

C-176 is a strong and covalent mouse STING inhibitor.
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-104022

CHK1 inhibitor
GDC-0575 analog
Checkpoint Kinase (Chk) Cancer

CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1.
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-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-126328

PKC-theta inhibitor 1	PKC	Inflammation/Immunology
PKC-theta inhibitor 1 is the PKCθ inhibitor with an K_i value of 6 nM, inhibits IL-2 production in vivo with an IC₅₀ of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.

HY-15760

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

HY-N1504

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

HY-13662B

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

HY-131705

BTK inhibitor 17	Btk	Inflammation/Immunology
BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC₅₀ of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research.

HY-10217

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

HY-P1029

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

HY-15604

AZD1208
Pim Autophagy Apoptosis Cancer

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

Doxycycline
MMP Bacterial Parasite Antibiotic Infection

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

Collagen proline hydroxylase inhibitor
Others Cancer

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

HY-U00387

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

HY-107986

GNE-6776
Deubiquitinase Cancer

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

AKT Kinase Inhibitor
Akt Cancer

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

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

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

Doxycycline hydrochloride
MMP Bacterial Antibiotic Infection

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

NBTGR
Others Cardiovascular Disease

NBTGR (p-Nitrobenzylthioguanosine) is a potent inhibitor of nucleoside transport; inhibits adenosine uptake with a K_i of 70 nM.
HY-112270

Glutaminyl Cyclase Inhibitor 2
Amyloid-β Neurological Disease

Glutaminyl Cyclase Inhibitor 2 is a glutaminyl cyclase inhibitor with an IC₅₀ of 1.23 μM.
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-15604A

AZD1208 hydrochloride
Pim Autophagy Apoptosis Cancer

AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
HY-112269

Glutaminyl Cyclase Inhibitor 1
Amyloid-β Neurological Disease

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

Dapagliflozin impurity
Others Others

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

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

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

HY-104032

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

HY-10172

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

HY-136270

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

HY-103310

MRS1845
Calcium Channel CRAC Channel Cardiovascular Disease

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

HY-122856

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

HY-50900

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

HY-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 Apoptosis	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-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-101791

P-gp inhibitor 1
P-glycoprotein Cancer

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.

HY-A0276

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

HY-N0518

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

HY-16657

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

HY-19931

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

HY-119808

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

HY-128729

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

HY-P2478

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

HY-13624A

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

HY-15358

ALK inhibitor 2	ALK FAK	Cancer
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=37 nM) and focal adhesion kinase (FAK; IC₅₀=5 nM).

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-15357

ALK inhibitor 1	ALK FAK	Cancer
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC₅₀=31 nM) and focal adhesion kinase (FAK; IC₅₀=2 nM).

HY-13624

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

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-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-12072

Lck Inhibitor	Src	Inflammation/Immunology
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC₅₀s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.

HY-P1398

Compstatin control peptide
Complement System Inflammation/Immunology

Compstatin control peptide is a complement inhibitor that binds and inhibits cleavage of complement C3.
HY-P1260

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

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

ML241 hydrochloride
p97 Cancer

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

Anastrozole
ZD1033
Aromatase Cancer

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

Nor-Acetildenafil
Others Others

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

Delamanid
OPC-67683
Bacterial Antibiotic Cancer

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

NU6300
CDK Cancer

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

PTP inhibitor 1
Phosphatase Cancer

PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.
HY-10451S

Canagliflozin D4
JNJ 28431754 D4
SGLT Cancer Metabolic Disease

Canagliflozin D4 is a deuterium labeled Canagliflozin. Canagliflozin is a selective SGLT2 inhibitor.
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-112913

SOCE inhibitor 1
CRAC Channel Metabolic Disease Neurological Disease

SOCE inhibitor 1 is a store-operated calcium entry (SOCE) inhibitor with an IC₅₀ of 4.4 μM.
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-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-114309

URAT1 inhibitor 1	URAT1	Inflammation/Immunology
URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC₅₀ of 32 nM. URAT1 inhibitor 1 has potential to treat hyperuricemia associated with gout.

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-120859A

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

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-126331

Glutaminyl Cyclase Inhibitor 4	Amyloid-β	Neurological Disease
Glutaminyl Cyclase Inhibitor 4 (compound 90) is a potent, selective glutaminyl cyclase (QC) inhibitor with an IC₅₀ of 6.1 nM. Glutaminyl Cyclase Inhibitor 4 is a potent anti-Alzheimer’s agent.

HY-12824

RNPA1000	Antibiotic Bacterial	Infection
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC₅₀ of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.

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-N0565B

Doxycycline (hyclate) Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031	Antibiotic MMP Bacterial	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 Infection

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-15842

SF1670
PTEN Phosphatase Autophagy Cancer

SF1670 is a potent and specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor.
HY-103593

LCL521
Phospholipase Cancer

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

HY-I0637

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

HY-16187

EL-102
HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer

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

Daclatasvir Impurity B
Others Others

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

HY-D0886

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

HY-18965

TAS-301
PKC Cardiovascular Disease

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

AZ191
DYRK Cancer

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

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

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

HIV-1 integrase inhibitor 8
HIV Integrase Infection

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

MRK-560
γ-secretase Neurological Disease

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

O-Nornuciferine
Potassium Channel Metabolic Disease

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

Arjungenin
Others Metabolic Disease

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

Fluazifop-P-butyl
Acetyl-CoA Carboxylase Metabolic Disease

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

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-125997

BTK inhibitor 10	Btk	Inflammation/Immunology
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.

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-126288

ERK1/2 inhibitor 2
ERK Cancer

ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.

HY-16062

ARQ 621	Kinesin	Cancer
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.

HY-119935

JAK3 covalent inhibitor-1	JAK	Inflammation/Immunology
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC₅₀ of 11 nM and shows 246-fold selectivity vs other JAKs.

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-N8533

Sodium Camptothecin	DNA/RNA Synthesis	Cancer Infection
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.

HY-13985

Nav1.7 inhibitor	Sodium Channel	Neurological Disease
Nav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain.

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-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-U00377

Cathepsin Inhibitor 2
Cathepsin Cancer Inflammation/Immunology

Cathepsin Inhibitor 2 is a potent Cathepsin S inhibitor extracted from patent WO2009123623A1, has a K_i of <20 nM.
HY-15217

CHR-6494
Haspin Kinase Cancer

CHR-6494 is a potent inhibitor of haspin, inhibiting histone H3T3 phosphorylation, with an IC₅₀ of 2 nM.
HY-15859

Atglistatin
ATGL Metabolic Disease

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

HY-77521

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

HY-13502

Mitoxantrone
mitozantrone
Topoisomerase PKC Cancer

Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM.
HY-119938

Tuberculosis inhibitor 1
Bacterial Infection

Tuberculosis inhibitor 1 is a potent and non-cytotoxic trypanosoma brucei growth inhibitor with an EC₅₀ of 5 nM.

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-70027A

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.

HY-N2567

(±)-Decursinol
Bacterial Cancer

(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC₅₀ of 102 μM.
HY-128962

AZ1508
MC-Lys-MMETA
Drug-Linker Conjugates for ADC Cancer

AZ1508 is a drug-linker conjugates for ADC for the treatment of breast and stomach cancer, and the drug is a tubulin inhibitor.
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-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-124594

CA inhibitor 1
GS-6207 analog
HIV Infection

CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
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-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-115213

SORT-PGRN interaction inhibitor 1	Neurotensin Receptor	Neurological Disease
SORT-PGRN interaction inhibitor 1 is a potent inhibitor of the sortilin-progranulin interaction with an IC₅₀ of 2 μM.

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-W010538

trans-4-Methylcyclohexanamine
Parasite Infection

trans-4-Methylcyclohexanamine is an intermediate and can be used for the development of T. cruzi enzyme inhibitor.
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-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-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-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. Shikonin inhibits AIM2 inflammasome activation.

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-124793A

GAK inhibitor 49 hydrochloride	Others	Infection
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a K_i of 0.54 nM and a cell IC₅₀ of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.

HY-19727A

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

HY-129167

Menin-MLL inhibitor 4	Epigenetic Reader Domain	Cancer
Menin-MLL inhibitor 4 is an inhibitor of Menin- MLL (mixed-lineage leukemia protein) interaction extracted from patent WO2017214367, compound example 1. Menin-MLL inhibitor 4 has antitumor activity.

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-124793

GAK inhibitor 49	Others	Infection
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a K_i of 0.54 nM and a cell IC₅₀ of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.

HY-B0879A

Suramin sodium salt Suramin hexasodium salt	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV 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 is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

HY-B0879

Suramin	Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV 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 is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.

HY-P0081

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

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

Afatinib N-Oxide
Others Others

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

UNC2881
TAM Receptor Cardiovascular Disease

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

MMP3 inhibitor 1
MMP Cancer

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

Mauritianin
Topoisomerase Cancer

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

HY-13606

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

HY-13256

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

HY-P1452A

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

HY-Y0882

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

HY-16420

R112
Syk Inflammation/Immunology

R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
HY-111919

3-Nitrocoumarin
Phospholipase Others

3-Nitrocoumarin (3-NC) is a potent and selective Phospholipase C-γ (PLC-γ) inhibitor.
HY-15588

L189
DNA/RNA Synthesis Cancer

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

Isoprocarb
AChE Neurological Disease

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

Carboxyatractyloside
Gummiferin
Others Cancer

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

HY-12054A

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

HY-16931

SMIFH2
Others Cancer

SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.

HY-10809

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

HY-19609

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

HY-131268

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

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

Lycoramine
AChE Neurological Disease

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

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

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

HY-12814A

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

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-111506

Aurora inhibitor 1
Aurora Kinase Cancer

Aurora inhibitor 1 is a potent Aurora inhibitor with an IC₅₀ of ≤ 4 nM and ≤13 nM for Aurora A and Aurora B kinase, respectively.

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-18928

FAK inhibitor 5
FAK Cancer

FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC₅₀ values in the low micromolar range.
HY-N4186

Glabrolide
Beta-secretase Neurological Disease

Glabrolide, derived from Glycyrrhiza uralensis Fisch., is a β-secretase 1 (BACE-1) inhibitor[1].
HY-103002

SU5408
VEGFR2 Kinase Inhibitor I
VEGFR Cardiovascular Disease

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

HY-B0497B

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

HY-131446

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

HY-50202

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

HY-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-117491

BRD4 Inhibitor-10
Epigenetic Reader Domain Cancer

BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC₅₀ of 8 nM.

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-109574

Raf inhibitor 2	Raf	Cancer
Raf inhibitor 2 is a potent raf kinase (IC₅₀<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.

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-80003

QL47	Btk	Cancer Infection
QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC₅₀ of 7 nM.

HY-133019

ATX inhibitor 5	Phosphodiesterase (PDE)	Inflammation/Immunology
ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC₅₀ of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.

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-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-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-112280

CDK4/6/1 Inhibitor
CDK Cancer

CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.
HY-10247

BRAF inhibitor
Raf Cancer

BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
HY-12726A

Liproxstatin-1 hydrochloride
Ferroptosis Cancer

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

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-10162S

Olaparib D5
AZD2281 D5; KU0059436 D5
PARP Autophagy Mitophagy Cancer

Olaparib D5 (AZD2281 D5) is a deuterium labeled Olaparib. Olaparib is a potent and oral PARP inhibitor.
HY-U00370

Thrombin inhibitor 1
Thrombin Cardiovascular Disease

Thrombin inhibitor 1 is a potent thrombin inhibitor (K_i=0.66 nM, 2xaPTT=0.43 μM).

HY-111489A

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

HY-17421A

Tenatoprazole sodium Tenatoprazole sodium salt	Proton Pump	Cardiovascular Disease
Tenatoprazole sodium (TU-199 sodium) is a proton pump inhibitor; inhibits hog gastric H⁺/K⁺-ATPase with an IC₅₀ of 6.2 μM.

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-128977

CD235
Epigenetic Reader Domain Cancer

CD235 is a structurally similar analogue of CD161. CD161 is a potent and orally bioavailable BET bromodomain inhibitor.
HY-12000

AG490
Tyrphostin AG490; Tyrphostin B42
EGFR STAT JAK Autophagy Cancer

AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

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-111446

EPAC 5376753
Others Cancer Metabolic Disease Cardiovascular Disease

EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC₅₀ of 4 µM in Swiss 3T3 cells.

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-13026S

Idelalisib D5
CAL-101 D5; GS-1101 D5
PI3K Autophagy Cancer

Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ 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-112297

BACE-1 inhibitor 1
Beta-secretase Neurological Disease

BACE-1 inhibitor 1 (Compound 8a) is a potent BACE-1 inhibitor with an IC₅₀ of 56 nM.

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-102007

Gamitrinib TPP
HSP Cancer

Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
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-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-10255AS

Sunitinib D10 SU 11248 D10	VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis	Cancer
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib 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-124726

Aumitin	Autophagy	Cancer Neurological Disease
Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC₅₀s of 0.12 μM and 0.24 μM, respectively.

HY-19727

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

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-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-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. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.

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-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-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-130255

BTK inhibitor 13
Btk Inflammation/Immunology

BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC₅₀ of 1.2 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-70027

p53 and MDM2 proteins-interaction-inhibitor (chiral)	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.

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-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-15231

PSI-352938
PSI-938
HCV Infection

PSI-352938 (PSI-938) is a hepatitis C virus (HCV) nucleotide 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-10268S

Betrixaban D6	Factor Xa	Cardiovascular Disease
Betrixaban D6 is a deuterium labeled Betrixaban. Betrixaban is a highly potent, selective, and orally efficacious factor Xa (fXa) inhibitor.

HY-10450S

Dapagliflozin D5
BMS-512148 D5
SGLT Cancer Metabolic Disease

Dapagliflozin D5 (BMS-512148 D5) is a deuterium labeled Dapagliflozin. Dapagliflozin is a competitive SGLT2 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-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-119934

NaV1.7 inhibitor-1	Sodium Channel	Neurological Disease
NaV1.7 inhibitor-1 is an efficacious voltage-gated sodium channel (NaV) 1.7 inhibitor with an IC₅₀ of 0.6 nM for hNaV1.7, exhibits 80-fold selectivity versus hNaV1.5.

HY-P1376

G-Protein antagonist peptide	mAChR Adrenergic Receptor	Endocrinology
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-103359

Ceranib1	Others	Cancer
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.

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 Apoptosis	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-136149A

Mpro inhibitor N3 hemihydrate	SARS-CoV Virus Protease	Infection
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC₅₀ of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC₅₀ of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.

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-13803A

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

HY-122862

RAS inhibitor Abd-7	Ras	Cancer
RAS inhibitor Abd-7, a potent RAS-binding compound (K_d=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V.

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-133014

RIP2 kinase inhibitor 1	RIP kinase	Inflammation/Immunology
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC₅₀ of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.

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-10261S

Afatinib D6
BIBW 2992 D6
EGFR Autophagy Cancer

Afatinib D6 (BIBW 2992 D6) is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family 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-B1279A

Metamizole sodium	COX	Inflammation/Immunology Neurological Disease
Metamizole sodium is a non-opioid compound with excellent analgesic and antipyretic effects. Metamizole (sodium) is a cyclooxygenase-3 (COX-3) inhibitor.

HY-15233

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

HY-128580

FAK inhibitor 2
FAK Cancer

FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC₅₀  of 0.07 nM, with antitumor and anti-angiogenesis activities.

HY-101053

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

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-112494

KRas G12C inhibitor 4
Ras Cancer

KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

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-112491

KRas G12C inhibitor 1
Ras Cancer

KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

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-N2403

Dihydrolycorine	Others	Neurological Disease
Dihydrolycorine, isolated from Lycoris radiate Herb, is an inhibitor of protein synthesis in eukarytic cells by inhibiting the peptide bone formation step.

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-126142

Top1 inhibitor 1
Topoisomerase ADC Cytotoxin Cancer

Top1 inhibitor 1 (compound 28) is a potent human topoisomerase I (Top1) inhibitor with an IC₅₀ value of 29 nM.
HY-112493

KRas G12C inhibitor 3
Ras Cancer

KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
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-13062

Daunorubicin hydrochloride Daunomycin hydrochloride; RP 13057 hydrochloride; Rubidomycin hydrochloride	Topoisomerase DNA/RNA Synthesis ADC Cytotoxin Bacterial Autophagy Apoptosis Antibiotic	Cancer Infection
Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities. Daunorubicin hydrochloride inhibits DNA and RNA synthesis in sensitive and resistant Ehrlich ascites tumor cells.

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-112128

USP7-IN-3
Deubiquitinase Cancer

USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.

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-112492

KRas G12C inhibitor 2
Ras Cancer

KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.

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-70028

p53 and MDM2 proteins-interaction-inhibitor (racemic)	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
p53 and MDM2 proteins-interaction-inhibitor (racemic) (Compound 2j) is an inhibitor of the interaction between p53 and MDM2 proteins.

HY-111784

CBP/p300-IN-4
Epigenetic Reader Domain Cancer

CBP/p300-IN-4 is a potent p300/CBP bromodomain inhibitor.
HY-131002

DPTIP
Phospholipase Inflammation/Immunology

DPTIP is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC₅₀ of 30 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-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-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-P1376A

G-Protein antagonist peptide TFA	mAChR Adrenergic Receptor	Endocrinology
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-112800

cyt-PTPε Inhibitor-1	Phosphatase	Metabolic Disease
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.

HY-112062

POL1-IN-1	DNA/RNA Synthesis	Cancer
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC₅₀ of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.

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-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-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-112870A

AST2818 mesylate
EGFR Cancer

AST2818 mesylate is an EGFR inhibitor.
HY-P0290A

GRGDSP TFA
Integrin Cancer

GRGDSP (TFA) is an integrin inhibitor.
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-112907

RIP2 Kinase Inhibitor 3	RIP kinase	Inflammation/Immunology
RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC₅₀ of 1 nM .

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-128889

FXIa-IN-1
Factor Xa Cardiovascular Disease

FXIa-IN-1 (compound EP-7041) is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.
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-112712

Cyclophilin inhibitor 1	HCV	Infection
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a K_d of 5 nM, shows effective anti-HCV activity, with an EC₅₀ of 98 nM for HCV 2a.

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-10331S

Regorafenib D3 BAY 73-4506 D3	VEGFR Autophagy PDGFR Raf RET	Cancer
Regorafenib D3 (BAY 73-4506 D3) is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase 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-DG; 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; Deuterated labeled MMAE	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-126292

KRAS G12C inhibitor 13
Ras Cancer

KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.

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-14560C

Reboxetine mesylate FCE20124 mesylate; PNU155950E mesylate	Adrenergic Receptor	Neurological Disease
Reboxetine mesylate (FCE20124 mesylate) is a potent, selective, and specific *noradrenaline reuptake inhibitor* (NARI)** for the research of depression. Reboxetine mesylate inhibits the uptake of norepinephrine, with a K_i of 8 nM.

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-14934

Rosabulin STA 5312	Microtubule/Tubulin	Cancer
Rosabulin (STA 5312) is a potent and orally active microtubule inhibitor that inhibits microtubule assembly. Rosabulin has broad-spectrum anti-tumor activity.

HY-111451

ATR inhibitor 1
ATM/ATR Cancer

ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a K_i value below 1 µΜ.

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-126146

PKC-iota inhibitor 1
PKC Cancer

PKC-iota inhibitor 1 (compound 19) is a protein kinase C-iota (PKC-ι ℩) inhibitor with an IC₅₀ value of 0.34 μM.

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-100886

BAY1082439	PI3K Apoptosis	Cancer
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

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-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 μM.

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-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-N2533

Cyanidin 3-sambubioside chloride Cyanidin-3-O-sambubioside chloride	Influenza Virus Angiotensin-converting Enzyme (ACE)	Cancer Infection Inflammation/Immunology
Cyanidin 3-sambubioside chloride (Cyanidin-3-O-sambubioside chloride), a major anthocyanin, a natural colorant, and is a potent NO inhibitor. Cyanidin 3-sambubioside chloride is a H274Y mutation inhibitor, and inhibits influenza neuraminidase activity with an IC₅₀ of 72 μM. Cyanidin 3-sambubioside chloride inhibits angiotensin-converting enzyme (ACE) activity and has antioxidant, anti-angiogenic and antiviral properties.

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-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-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-119375

Syncytial Virus Inhibitor-1	Bacterial	Infection
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC₅₀s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively.

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-13818

Stattic	STAT Apoptosis	Cancer Inflammation/Immunology
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice.

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-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-114168

KRAS G12C inhibitor 5
Ras Cancer

KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.

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 Apoptosis	Cancer
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC₅₀ of 23.3 μM for HeLa cell and 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-122903B

(+)-TK216
DNA/RNA Synthesis Others

(+)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor.

HY-17469

Gimeracil Gimestat	Others	Cancer
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).

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-112915

Eg5 Inhibitor V, trans-24
Kinesin Cancer

Eg5 Inhibitor V, trans-24 is a potent and specific kinesin Eg5 inhibitor with an IC₅₀ of 0.65 μM, and can be used in the research of cancer.
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-111184

PIK-108
PI3K Cancer

PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.

HY-13229

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

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

hDHODH-IN-3	Dihydroorotate Dehydrogenase DNA/RNA Synthesis Influenza Virus	Infection
hDHODH-IN-3 (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-128661

IDH1 Inhibitor 2	Isocitrate Dehydrogenase (IDH)	Metabolic Disease
IDH1 Inhibitor 2 (compound 13) is a potent IDH1 inhibitor via a direct covalent modification of His315, with an IC₅₀ of 110 nM.

HY-10005

Flavopiridol HMR-1275; Alvocidib; L86-8275	CDK Autophagy HIV Apoptosis	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-12688

Succinyl phosphonate	Endogenous Metabolite Reactive Oxygen Species	Neurological Disease
Succinyl phosphonate 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-116171

(Rac)-Calpain Inhibitor XII	Proteasome	Neurological Disease Cardiovascular Disease
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, K_i=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, K_i=120 nM) and cathepsin B (K_i=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.

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-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 Apoptosis	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-108341

PF-06424439	Acyltransferase	Metabolic Disease
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC₅₀ of 14 nM. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.

HY-108486

Herbimycin A	Bacterial Antibiotic	Infection
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-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-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-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-B1490

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

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-111409

RIP1 kinase inhibitor 1	RIP kinase	Inflammation/Immunology
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pK_i=9.04).

HY-15656S

Ceritinib D7 LDK378 D7	ALK Insulin Receptor IGF-1R	Cancer Endocrinology
Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.

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-13012

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

RepSox (E-616452) is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with an IC₅₀ of 4 nM.
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 Apoptosis	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-14605BS

Rasagiline 13C3 mesylate racemic AGN1135 13C3; TVP1012 13C3 racemic	Monoamine Oxidase	Neurological Disease
Rasagiline 13C3 mesylate racemic is the deuterium labeled Rasagiline mesylate racemic. Rasagiline mesylate racemic is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor.

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-U00327

Prenyl-IN-1	Farnesyl Transferase	Neurological Disease
Prenyl-IN-1 is a protein prenylation inhibitor, especially a geranylgeranyltransferase (GGT) or a farnesyltransferase (FT) inhibitor, exhibiting potent activity against oxidative stress, and particularly in the treatment of Parkinson's Disease.

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-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-112522A

HS80	Fatty Acid Synthase (FASN)	Cancer
HS-80 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-80 is able to inhibit the incorporation of tritiated acetate into lipids with an IC₅₀ of 7.13 μM.

HY-135282

DHODH-IN-1	Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection
DHODH-IN-1 (compound 18d) is a potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC₅₀ of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway.

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-122700

Factor D inhibitor 6	Complement System	Inflammation/Immunology
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC₅₀ of 30 nM and a K_d of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.

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-120548

KBU2046	Others	Cancer
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.

HY-100431

IMR-1	Notch	Cancer
IMR-1 is a novel class of Notch inhibitors targeting the transcriptional activation with an IC₅₀ of 26 μM. IMR-1 prevents the recruitment of Mastermind-like 1 (Maml1) to the Notch Ternary Complex (NTC) on chromatin, inhibits Notch target gene transcription and dramatically inhibits tumor growth.

HY-B0167A

Sodium Salicylate Salicylic acid sodium salt; 2-Hydroxybenzoic acid sodium salt	COX NF-κB Ribosomal S6 Kinase (RSK) Autophagy Apoptosis	Inflammation/Immunology Cancer
Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle.

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-106697

Ponalrestat ICI 128436	Aldose Reductase	Metabolic Disease
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (K_i=7.7 nM) over ALR1 (K_i=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol.

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-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-103710

IBR2	RAD51 Apoptosis	Cancer
IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.

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-114320

BuChE-IN-TM-10 TM-10	AChE	Neurological Disease
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC₅₀ of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease.

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-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-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-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-B0182

Carmofur HCFU	Nucleoside Antimetabolite/Analog SARS-CoV Virus Protease	Cancer
Carmofur (HCFU), a derivative of 5-Fluorouracil, is an antineoplastic agent. Carmofur is an inhibitor of acid ceramidase with an IC₅₀ of 79 nM for the rat enzyme. Carmofur inhibits the SARS-CoV-2 main protease (Mpro). Carmofur Inhibits SARS-CoV-2 in Vero E6 cell with an EC₅₀ of 24.3 μM.

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-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-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-B1099

Hycanthone	DNA/RNA Synthesis Topoisomerase Parasite	Infection
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a K_D of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.

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-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-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-134665

NITD-2
DNA/RNA Synthesis Infection

NITD-2, a dengue virus (DENV) polymerase inhibitor, inhibits the DENV RdRp-mediated RNA elongation. NITD-2 penetrates cell membrane poorly.

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-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-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-136182

YM-244769 dihydrochloride	Na+/Ca2+ Exchanger	Neurological Disease
YM-244769 dihydrochloride is a potent Na⁺/Ca²⁺ exchange (NCX) inhibitor that preferentially inhibits NCX3 (IC₅₀=18 nM). Neuronal and renal protection.

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-112080

BAY-6035	Histone Methyltransferase	Cancer
BAY-6035 is a potent, selective and substrate-competitive inhibitor of SMYD3. BAY-6035 inhibits methylation of MEKK2 peptide with an IC₅₀ of 88 nM.

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-112147

IDO1 and HDAC1 Inhibitor	Indoleamine 2,3-Dioxygenase (IDO) HDAC	Cancer
IDO1 and HDAC1 Inhibitor (Compound 10) is a dual IDO1 and HDAC1 inhibitor with IC₅₀s of 69.0 nM and 66.5 nM, respectively.

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-138203

Z-LE(OMe)TD(OMe)-FMK
Caspase Apoptosis Cancer

Z-LE(OMe)TD(OMe)-FMK is a selective caspase-8 inhibitor. Z-LE(OMe)TD(OMe)-FMK can inhibit cell apoptosis.
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-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.