Search Result

Targets Recommended:	NEDD8-activating Enzyme CRM1 PD-1/PD-L1 Mps1 PAI-1 PDK-1 IRE1 Wee1 URAT1 Ack1 sFRP-1 MALT1 PGC-1α IGF-1R MCHR1 (GPR24) Keap1-Nrf2 E1/E2/E3 Enzyme c-Fms GPR40 EGFR IRAK EAAT2 Adenosine Receptor P-glycoprotein FXR PTEN Oct3/4 PIKfyve

Results for "Ang (1-8) Inhibitors" in MCE Product Catalog:

By Targets:	Adenosine Receptor (2) c-Fms (1) E1/E2/E3 Enzyme (1) EGFR (6) FXR (1) IGF-1R (1) IRE1 (2) Mps1 (1) PD-1/PD-L1 (2) PDK-1 (1) 5-HT Receptor (3) AChE (2) ADC Cytotoxin (3) Adiponectin Receptor (2) Adrenergic Receptor (6) Akt (5) Aldose Reductase (1) ALK (3) AMPK (2) Amyloid-β (1) Angiotensin Receptor (7) Angiotensin-converting Enzyme (ACE) (1) Antibiotic (7) Apoptosis (24) Aromatase (1) Aurora Kinase (1) Autophagy (31) Bacterial (23) Bcl-2 Family (1) Bcr-Abl (1) Beta-secretase (1) Bombesin Receptor (1) c-Kit (6) c-Met/HGFR (1) c-Myc (1) Calcium Channel (6) CaMK (2) Cannabinoid Receptor (3) Casein Kinase (2) Caspase (3) CCR (5) CDK (6) Complement System (3) COX (6) CRFR (1) CXCR (2) Cytochrome P450 (2) Deubiquitinase (1) Dihydroorotate Dehydrogenase (2) Dipeptidyl Peptidase (2) DNA-PK (1) DNA/RNA Synthesis (7) Dopamine Receptor (7) DYRK (3) E3 Ligase Ligand-Linker Conjugate (1) Endogenous Metabolite (11) Endothelin Receptor (2) Ephrin Receptor (1) Epigenetic Reader Domain (7) Epoxide Hydrolase (2) ERK (2) Estrogen Receptor/ERR (1) Eukaryotic Initiation Factor (eIF) (1) FAAH (3) Factor Xa (1) FAK (1) Fatty Acid Synthase (FASN) (2) FGFR (3) Filovirus (1) FLT3 (1) Fungal (2) GABA Receptor (1) GHSR (1) Glucocorticoid Receptor (1) GLUT (1) GPR55 (1) GSK-3 (2) HDAC (7) HIF/HIF Prolyl-Hydroxylase (1) Histamine Receptor (3) Histone Acetyltransferase (2) Histone Demethylase (1) Histone Methyltransferase (4) HIV (5) HSP (1) HSV (1) iGluR (1) IKK (1) Indoleamine 2,3-Dioxygenase (IDO) (1) Insulin Receptor (1) Integrin (5) Interleukin Related (1) JAK (9) JNK (1) Lactate Dehydrogenase (1) Ligand for E3 Ligase (1) Lipoxygenase (2) LPL Receptor (1) mAChR (4) MAP3K (1) MAP4K (2) MDM-2/p53 (1) Melanocortin Receptor (2) MELK (1) Microtubule/Tubulin (4) Mineralocorticoid Receptor (2) Mitophagy (2) MMP (5) mTOR (3) Myosin (1) Na+/Ca2+ Exchanger (1) nAChR (2) NF-κB (3) NO Synthase (2) Opioid Receptor (4) P2X Receptor (1) p38 MAPK (4) PAK (2) Parasite (7) PARP (1) PDGFR (2) Phosphatase (5) Phosphodiesterase (PDE) (5) PI3K (11) Pim (2) PKA (1) PKC (6) Potassium Channel (8) PPAR (1) PROTAC (3) PROTAC Linker (3) Proteasome (1) Ras (1) Reactive Oxygen Species (3) Reverse Transcriptase (1) Ribosomal S6 Kinase (RSK) (1) RIP kinase (1) ROCK (1) ROR (1) SARS-CoV (2) Sodium Channel (15) SPHK (1) Src (4) STAT (1) Survivin (1) TAM Receptor (1) TGF-beta/Smad (2) TGF-β Receptor (3) Thrombin (1) TNF Receptor (2) Toll-like Receptor (TLR) (3) Topoisomerase (3) TRP Channel (4) Tyrosinase (1) ULK (3) VEGFR (1) Virus Protease (1) Wnt (1) Xanthine Oxidase (1) β-catenin (1) γ-secretase (1)
By Research Areas:	Cancer (171) Cardiovascular Disease (38) Endocrinology (24) Infection (30) Inflammation/Immunology (60) Metabolic Disease (24) Neurological Disease (67)

By Targets:

Adenosine Receptor (2)

c-Fms (1)

E1/E2/E3 Enzyme (1)

EGFR (6)

FXR (1)

IGF-1R (1)

IRE1 (2)

Mps1 (1)

PD-1/PD-L1 (2)

PDK-1 (1)

5-HT Receptor (3)

AChE (2)

ADC Cytotoxin (3)

Adiponectin Receptor (2)

Adrenergic Receptor (6)

Akt (5)

Aldose Reductase (1)

ALK (3)

AMPK (2)

Amyloid-β (1)

Angiotensin Receptor (7)

Angiotensin-converting Enzyme (ACE) (1)

Antibiotic (7)

Apoptosis (24)

Aromatase (1)

Aurora Kinase (1)

Autophagy (31)

Bacterial (23)

Bcl-2 Family (1)

Bcr-Abl (1)

Beta-secretase (1)

Bombesin Receptor (1)

c-Kit (6)

c-Met/HGFR (1)

c-Myc (1)

Calcium Channel (6)

CaMK (2)

Cannabinoid Receptor (3)

Casein Kinase (2)

Caspase (3)

CCR (5)

CDK (6)

Complement System (3)

COX (6)

CRFR (1)

CXCR (2)

Cytochrome P450 (2)

Deubiquitinase (1)

Dihydroorotate Dehydrogenase (2)

Dipeptidyl Peptidase (2)

DNA-PK (1)

DNA/RNA Synthesis (7)

Dopamine Receptor (7)

DYRK (3)

E3 Ligase Ligand-Linker Conjugate (1)

Endogenous Metabolite (11)

Endothelin Receptor (2)

Ephrin Receptor (1)

Epigenetic Reader Domain (7)

Epoxide Hydrolase (2)

ERK (2)

Estrogen Receptor/ERR (1)

Eukaryotic Initiation Factor (eIF) (1)

FAAH (3)

Factor Xa (1)

FAK (1)

Fatty Acid Synthase (FASN) (2)

FGFR (3)

Filovirus (1)

FLT3 (1)

Fungal (2)

GABA Receptor (1)

GHSR (1)

Glucocorticoid Receptor (1)

GLUT (1)

GPR55 (1)

GSK-3 (2)

HDAC (7)

HIF/HIF Prolyl-Hydroxylase (1)

Histamine Receptor (3)

Histone Acetyltransferase (2)

Histone Demethylase (1)

Histone Methyltransferase (4)

HIV (5)

HSP (1)

HSV (1)

iGluR (1)

IKK (1)

Indoleamine 2,3-Dioxygenase (IDO) (1)

Insulin Receptor (1)

Integrin (5)

Interleukin Related (1)

JAK (9)

JNK (1)

Lactate Dehydrogenase (1)

Ligand for E3 Ligase (1)

Lipoxygenase (2)

LPL Receptor (1)

mAChR (4)

MAP3K (1)

MAP4K (2)

MDM-2/p53 (1)

Melanocortin Receptor (2)

MELK (1)

Microtubule/Tubulin (4)

Mineralocorticoid Receptor (2)

Mitophagy (2)

MMP (5)

mTOR (3)

Myosin (1)

Na+/Ca2+ Exchanger (1)

nAChR (2)

NF-κB (3)

NO Synthase (2)

Opioid Receptor (4)

P2X Receptor (1)

p38 MAPK (4)

PAK (2)

Parasite (7)

PARP (1)

PDGFR (2)

Phosphatase (5)

Phosphodiesterase (PDE) (5)

PI3K (11)

Pim (2)

PKA (1)

PKC (6)

Potassium Channel (8)

PPAR (1)

PROTAC (3)

PROTAC Linker (3)

Proteasome (1)

Ras (1)

Reactive Oxygen Species (3)

Reverse Transcriptase (1)

Ribosomal S6 Kinase (RSK) (1)

RIP kinase (1)

ROCK (1)

ROR (1)

SARS-CoV (2)

Sodium Channel (15)

SPHK (1)

Src (4)

STAT (1)

Survivin (1)

TAM Receptor (1)

TGF-beta/Smad (2)

TGF-β Receptor (3)

Thrombin (1)

TNF Receptor (2)

Toll-like Receptor (TLR) (3)

Topoisomerase (3)

TRP Channel (4)

Tyrosinase (1)

ULK (3)

VEGFR (1)

Virus Protease (1)

Wnt (1)

Xanthine Oxidase (1)

β-catenin (1)

γ-secretase (1)

By Research Areas:

Cancer (171)

Cardiovascular Disease (38)

Endocrinology (24)

Infection (30)

Inflammation/Immunology (60)

Metabolic Disease (24)

Neurological Disease (67)

353

Inhibitors & Agonists

Dye Reagents

Biochemical Assay Reagents

Peptides

Natural
Products

Recombinant Proteins

Cat. No.	Product Name	Target	Research Areas

HY-136278

NOC 18	NO Synthase
NOC 18 is a nitric oxide donor and activates an inward current in cultured rat cerebellar granules cells. NOC 18 increases cGMP production in cultured vascular smooth muscle cells. NOC 18 reduces contractility of cardiac muscle preparations in vitro.

HY-113151

18-Oxocortisol	Mineralocorticoid Receptor Endogenous Metabolite	Cardiovascular Disease
18-Oxocortisol is a derivative of cortisol that is produced by aldosterone synthase (CYP11B2). 18-Oxocortisol is a naturally occurring mineralocorticoid agonist. 18-Oxocortisol is a biomarker in adrenal vein sampling.

HY-128972

Purpurin 18
Others Others

Purpurin 18, a derivative of chlorophyll, is an interesting dihydroporphyrin for generating photosensitizers.

Purpurin 18	Others	Others
Purpurin 18, a derivative of chlorophyll, is an interesting dihydroporphyrin for generating photosensitizers.

HY-W013179

18-Hydroxycorticosterone	Endogenous Metabolite	Metabolic Disease
18-Hydroxycorticosterone is a corticosteroid and a derivative of corticosterone, which can lead to serious electrolyte imbalances.

HY-N0716

Berberine Natural Yellow 18	Topoisomerase Autophagy Bacterial Reactive Oxygen Species Endogenous Metabolite Antibiotic	Inflammation/Immunology
Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties.

HY-101844

ML-18
Bombesin Receptor Cancer

ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC₅₀ of 4.8 μM.
HY-102014

RN-18
HIV Infection

RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC₅₀ of 6 μM in nonpermissive H9 cells.
HY-B0803S

Lumefantrine D18
Benflumetol D18
Parasite Infection

Lumefantrine D18 is the deuterium labeled Lumefantrine, which is an antimalarial drug.

ML-18	Bombesin Receptor	Cancer
ML-18 is a non-peptide bombesin receptor subtype-3 (BRS-3) antagonist with an IC₅₀ of 4.8 μM.

RN-18	HIV	Infection
RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC₅₀ of 6 μM in nonpermissive H9 cells.

Lumefantrine D18 Benflumetol D18	Parasite	Infection
Lumefantrine D18 is the deuterium labeled Lumefantrine, which is an antimalarial drug.

HY-111969

BT18	Others	Neurological Disease
BT18 is a molecule mimic with function similar to glial cell line-derived neurotrophic factor (GDNF). BT18 shows an effect on GDNF family receptor GFRα1 and RET receptor tyrosine kinase RetA function.

HY-18672

SMER18
Autophagy Cancer

SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer.

SMER18	Autophagy	Cancer
SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer.

HY-117163

FzM1.8	Wnt β-catenin	Cancer
FzM1.8 derives from FzM1, is an allosteric agonist of FZD4 with pEC₅₀ of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.

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-U00193

Ro18-5362	Others	Metabolic Disease
Ro18-5362 is the less active prodrug of Ro 18-5364. Even at concentrations as high as 0.1 mM Ro 18-5362 fails to affect significantly (H⁺+K⁺)-ATPase activity and associated proton translocation.

HY-129653

E3 ligase Ligand 18	Ligand for E3 Ligase	Cancer
E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.

HY-W018745

Tetraethylene glycol
PROTAC Linker 18
PROTAC Linker Cancer

Tetraethylene glycol (PROTAC Linker 18) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

Tetraethylene glycol PROTAC Linker 18	PROTAC Linker	Cancer
Tetraethylene glycol (PROTAC Linker 18) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

HY-119366

S18-000003	ROR	Inflammation/Immunology
S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC₅₀ of 29 nM. S18-000003 inhibits IL-17 production.

HY-101098

PD-1-IN-18
PD-1/PD-L1 Inflammation/Immunology

PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.

PD-1-IN-18	PD-1/PD-L1	Inflammation/Immunology
PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts as an immunomodulator.

HY-N0180

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

HY-P1039

R18 PHCVPRDLSWLDLEANMCLP	Others	Cancer
R18 is a peptide antagonists of 14-3-3, with a K_D of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.

HY-114368

Kira8
AMG-18
IRE1 Inflammation/Immunology

Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM.
HY-N4324

cis-p-Menthan-1,8-diol
4-p-Menthan-1,8-diol
Others Infection

cis-p-Menthan-1,8-diol is a natural menthane monoterpenoid.
HY-P1879

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

β-Amyloid (18-28) is a peptide fragment of β-Amyloid.
HY-103128

inS3-54A18
STAT Cancer

inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

Kira8 AMG-18	IRE1	Inflammation/Immunology
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM.

*cis-p-Menthan-1,8-diol* 4-p-Menthan-1,8-diol	Others	Infection
cis-p-Menthan-1,8-diol is a natural menthane monoterpenoid.

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

inS3-54A18	STAT	Cancer
inS3-54A18 is a potent STAT3 inhibitor, with anti-cancer properties.

HY-17577

Berberine chloride hydrate Natural Yellow 18 chloride hydrate	Topoisomerase Autophagy Bacterial Reactive Oxygen Species Antibiotic	Cancer
Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.

HY-140324

*Tetraethyl octane-1,8-diylbis(phosphonate)*	PROTAC Linker	Cancer
Tetraethyl octane-1,8-diylbis(phosphonate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

HY-114368A

Kira8 Hydrochloride AMG-18 Hydrochloride	IRE1	Inflammation/Immunology
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC₅₀ of 5.9 nM.

HY-103660

18:0 LYSO-PE
Stearoyl lysophosphatidylethanolamine
Others Neurological Disease

18:0 LYSO-PE is an agent that can induce [Ca²⁺]_i increase.
HY-N6911

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

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

18:0 LYSO-PE Stearoyl lysophosphatidylethanolamine	Others	Neurological Disease
18:0 LYSO-PE is an agent that can induce [Ca²⁺]_i increase.

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

HY-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-18258

Berberine chloride Natural Yellow 18 chloride	Topoisomerase Autophagy Bacterial Reactive Oxygen Species Antibiotic	Cancer
Berberine chloride is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.

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-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-10021

Varenicline Tartrate CP 526555-18	nAChR	Neurological Disease
Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.

HY-15243

Capromorelin Tartrate CP 424391-18	GHSR	Neurological Disease Endocrinology
Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

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-15644

Tyrphostin 23
Tyrphostin A23; RG-50810; AG 18
EGFR Cancer

Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC₅₀ and K_iof 35 and 11 μM, respectively.

Tyrphostin 23 Tyrphostin A23; RG-50810; AG 18	EGFR	Cancer
Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC₅₀ and K_iof 35 and 11 μM, respectively.

HY-B0923

Danthron Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone	AMPK Autophagy Bacterial Virus Protease	Cancer
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.

HY-12403

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

HY-103615

Thalidomide-O-amido-C4-N3 Cereblon Ligand-Linker Conjugates 4; E3 ligase Ligand-Linker Conjugates 18	E3 Ligase Ligand-Linker Conjugate	Others
Thalidomide-O-amido-C4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

HY-101047

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

HY-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-101383

PF-01247324
Sodium Channel Neurological Disease

PF-01247324 is a selective and orally bioavailable Na_v1.8 channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.
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-90009A

Tadalafil
IC-351
Phosphodiesterase (PDE) Apoptosis Cardiovascular Disease

Tadalafil (IC-351) is a PDE5 inhibitor with an IC₅₀ value of 1.8 nM.

PF-01247324	Sodium Channel	Neurological Disease
PF-01247324 is a selective and orally bioavailable *Na_v1.8* channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.

*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.

Tadalafil IC-351	Phosphodiesterase (PDE) Apoptosis	Cardiovascular Disease
Tadalafil (IC-351) is a PDE5 inhibitor with an IC₅₀ value of 1.8 nM.

HY-P0216

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

HY-12660

MPI-0479605
Mps1 Apoptosis Cancer

MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC₅₀ of 1.8 nM.
HY-105283

PF 04531083
Sodium Channel Neurological Disease

PF 04531083 is a selective Na_V1.8 blocker, and used for the research of neuropathic/inflammatory pain.

MPI-0479605	Mps1 Apoptosis	Cancer
MPI-0479605 is a potent and selective ATP-competitive inhibitor of Mps1, with an IC₅₀ of 1.8 nM.

PF 04531083	Sodium Channel	Neurological Disease
PF 04531083 is a selective *Na_V1.8* blocker, and used for the research of neuropathic/inflammatory pain.

HY-123879

BAA473	Others	Inflammation/Immunology
BAA473 is a bile acid analog and is a potent activator of the pyrin inflammasome that induces the secretion of interleukin 18 (IL-18) through activation of the inflammasome in both myeloid and intestinal epithelial cells.

HY-126226

MK-6240 Precursor	Others	Cancer
MK-6240 Precursor (6e) is the synthetic precursor of (18)F]-MK-6240. (18)F]-MK-6240 is a tau positron emission tomography (PET) tracer for neurofibrillary tangles (NFTs), exhibiting high specificity and selectivity for binding to NFTs.

HY-101386

PZM21
Opioid Receptor Neurological Disease

PZM21 is a potent and selective μ opioid receptor agonist with an EC₅₀ of 1.8 nM.

HY-120947

AV-105	Others	Neurological Disease
AV-105 is a Florbetapir (¹⁸F)-radiolabeled slyrylpyridine tosylate precursor extracted from patent WO2010078370A1, example 1.5. AV-105 can synthesize ¹⁸F-radiolabeled compounds, which are used for positron emission tomography (PET) imaging of neurodegenerative diseases of the brain.

HY-15144

Trichostatin A
TSA
HDAC Cancer

Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC₅₀ value of 1.8 nM for HDAC.

HY-N2392

Kukoamine A	Parasite	Infection Cardiovascular Disease
Kukoamine A is a natural occurring spermine derivative, acts as a potent inhibitor of trypanothione reductase (K_i, 1.8 μM), with antihypertensive activity.

HY-122683

sAJM589
c-Myc Cancer

sAJM589 is a Myc inhibitor which potently disrupts the Myc-Max heterodimer with an IC₅₀ of 1.8 μM.

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-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-125079

DSP-2230
Sodium Channel Neurological Disease Cardiovascular Disease

DSP-2230 is a selective Nav1.7/Nav1.8 blocker.

HY-15848

AdipoRon	Adiponectin Receptor	Metabolic Disease
AdipoRon is an orally active adiponectin receptor (AdipoR) agonist, binding to AdipoR1 and AdipoR2 with K_ds of 1.8 and 3.1 μM, respectively.

HY-110164

AdipoRon hydrochloride	Adiponectin Receptor	Metabolic Disease
AdipoRon hydrochloride is an orally active and specific AdipoR agonist, binding to AdipoR1 and AdipoR2, with K_ds of 1.8 and 3.1 μM, respectively.

HY-100230A

ML133 hydrochloride
Potassium Channel Others

ML133 hydrochloride is a selective K_ir2 family channels inhibitor, with an IC₅₀ of 1.8 μM at pH 7.4 and 290 nM at pH 8.5.
HY-13895

WHI-P154
EGFR JAK Apoptosis Cancer

WHI-P154 is a potent EGFR inhibitor, and also modestly blocks JAK3, with IC₅₀s of 4 nM and 1.8 μM, respectively.
HY-114322

VZ185
PROTAC Epigenetic Reader Domain Cancer

VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC₅₀s of 4.5 and 1.8 nM, respectively.

HY-14595

Biochanin A 4-Methylgenistein; Olmelin	FAAH Autophagy	Neurological Disease Cancer
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC₅₀s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.

HY-120588

CCR1 antagonist 8	CCR	Inflammation/Immunology Endocrinology
CCR1 antagonist 8 (compound 19n), a third azaindazole series compound, is a CCR1 antagonist, with an IC₅₀ of 1.8 nM in Ca²⁺ flux assay.

HY-15701

Leukadherin-1
Complement System Integrin Inflammation/Immunology

Leukadherin-1 is a specific agonist of complement receptor 3 (CR3) and the leukocyte surface αMβ2 integrin CD11b/CD18.

HY-111445

CeMMEC1	Epigenetic Reader Domain DNA/RNA Synthesis	Cancer
CeMMEC1 is an inhibitor of BRD4, and also has high affinity for TAF1, with an IC₅₀ of 0.9 μM for TAF1, and a K_d of 1.8 μM for TAF1 (2).

HY-114301

PF-06305591	Sodium Channel	Neurological Disease
PF-06305591 is a potent and highly selective voltage gated sodium channel *NaV1.8* blocker, with an IC₅₀ of 15 nM. An excellent preclinical in vitro ADME and safety profile.

HY-110325

PF-04885614	Sodium Channel	Neurological Disease
PF-04885614 is a potent *NaV1.8* inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment.

HY-100207

CP21R7
CP21
GSK-3 Cancer

CP21R7 is potent GSK-3β inhibitor, with an IC₅₀ of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC₅₀ of 1900 nM.
HY-13330

AZD4547
FGFR Cancer

AZD4547 is a potent inhibitor of the FGFR family with IC₅₀s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

HY-14136

Rimonabant SR141716	Cannabinoid Receptor Bacterial	Infection Metabolic Disease Cancer
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a K_i of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-18644

CWHM-12
Integrin Cancer

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

HY-14137

Rimonabant Hydrochloride SR 141716A Hydrochloride	Cannabinoid Receptor Bacterial	Cancer Infection Metabolic Disease
Rimonabant hHydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an K_i of 1.8 nM. Rimonabant hHydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

HY-10963

Momelotinib Mesylate CYT387 (Mesylate)	JAK Autophagy	Cancer
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.

HY-B0579

Cyclosporin A Cyclosporine; Ciclosporin	Complement System	Inflammation/Immunology Cancer
Cyclosporin A is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of calcineurin with an IC₅₀ of 5 nM. Cyclosporin A also inhibits *CD11a/CD18* adhesion.

HY-11079

A-803467
Sodium Channel Neurological Disease

A 803467 is a selective Nav1.8 sodium channel blocker with an IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.

HY-19981

Derazantinib ARQ-087	FGFR	Cancer
Derazantinib (ARQ-087) is an ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC₅₀s of 4.5, 1.8, and 4.5 nM, respectively.

HY-10863

Anandamide	Cannabinoid Receptor GPR55 Endogenous Metabolite	Inflammation/Immunology
Anandamide is an immune modulator in the central nervous system acts via not only cannabinoid receptors (CB1 and CB2) but also other targets (e.g., *GPR18/GPR55*).

HY-100080

A-887826	Sodium Channel	Neurological Disease
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC₅₀ of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.

HY-133111

3-Hydroxy agomelatine	5-HT Receptor	Neurological Disease
3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT_2C receptor antagonist with an IC₅₀ of 3.2 μM and a K_i of 1.8 μM.

HY-128677

NCC007	Casein Kinase	Neurological Disease
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC₅₀s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.

HY-136405

Melanin probe-2	Others	Others
Melanin probe-2 (compound 5) is a non-radioactive bromopicolinamide precursor. Melanin probe-2 can be used for ¹⁸F-Labeled Picolinamide PET probe synthesis (HY-136404).

HY-100742A

(R)-GNE-140	Lactate Dehydrogenase	Cancer
(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC₅₀s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.

HY-13531

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

HY-122607

DPA-714	Others	Cancer Inflammation/Immunology
DPA-714 is a high affinity translocator protein (TSPO) ligand (K_i=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. [18F]DPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model.

HY-B1516

3'-Fluoro-3'-deoxythymidine Alovudine	Others	Cancer
3'-Fluoro-3'-deoxythymidine (Alovudine) is a marker of DNA synthesis that is less susceptible to inflammatory changes than ¹⁸F-Fluorodeoxyglucose (FDG) and thus is a better biomarker in pancreatic cancer.

HY-B1837

Cyfluthrin	Sodium Channel	Infection
Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav_1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.

HY-12948

AMG319
PI3K Cancer

AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC₅₀ of 18 nM.
HY-131345

PI3Kα-IN-4
PI3K Cancer

PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC₅₀ of 1.8 nM. PI3Kα-IN-4 has antitumor activity.

HY-15177

PF-04691502	PI3K mTOR Autophagy	Cancer
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with K_is of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.

HY-110303

Xanthine amine congener dihydrochloride XAC dihydrochloride	Adenosine Receptor	Neurological Disease
Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC₅₀ values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.

HY-121119

MRS 1523	Adenosine Receptor Calcium Channel	Inflammation/Immunology Neurological Disease Cardiovascular Disease
MRS 1523 is a potent and selective adenosine A₃ receptor antagonist with K_i values of 18.9 nM and 113 nM for human and rat A₃ receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A₁ and A_2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.

HY-10962

Momelotinib sulfate CYT387 sulfate salt	JAK Autophagy Apoptosis	Cancer
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀ of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC₅₀=155 nM).

HY-10343

Sotrastaurin AEB071	PKC	Inflammation/Immunology Cancer
Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with K_is of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.

HY-111342

HDAC8-IN-1
HDAC Cancer

HDAC8-IN-1 is a HDAC8 inhibitor with an IC₅₀ of 27.2 nM.

HY-136179

ZAP-180013	Tyrosinase	Inflammation/Immunology
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC₅₀ of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).

HY-118946

BPH-1358 NSC50460	Bacterial	Cancer Infection
BPH-1358 (NSC50460) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against *S. aureus* in vitro (MIC ~250 ng/mL).

HY-133084

ERK-IN-2	ERK	Cancer
ERK-IN-2 is a potent, highly seletive and orally active ERK2 inhibitor probe with an IC₅₀ value of 1.8 nM. ERK-IN-2 might lead to off-target toxicity and/or off-target activity at dose >10 μM.

HY-135299

CH6953755	Src	Cancer
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC₅₀ of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo.

HY-14648

Dexamethasone Hexadecadrol; Prednisolone F	Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic	Cancer Infection Endocrinology Inflammation/Immunology
Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection.

HY-N4125

Dehydroeburicoic acid monoacetate 3-O-Acetyldehydroeburicoic acid	Others	Inflammation/Immunology
Dehydroeburicoic acid monoacetate (Compound 18) is a lanostane triterpenoid isolated from Wolfiporia cocos.

HY-103492

CDK8-IN-1
CDK Cancer

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC₅₀ of 3 nM.
HY-12466

Z-DEVD-FMK
Caspase Cancer

Z-DEVD-FMK is a specific and irreversible caspase-3 inhibitor with IC₅₀ of 18 μM.

HY-133111S

3-Hydroxy agomelatine D3	5-HT Receptor	Neurological Disease
3-Hydroxy agomelatine D3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is a 5-HT_2C receptor antagonist with an IC₅₀ of 3.2 μM and a K_i of 1.8 μM.

HY-105185

Fidarestat SNK 860	Aldose Reductase	Metabolic Disease
Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC₅₀s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.

HY-135859

NH2-MPAA-NODA	Others	Cancer
NH2-MPAA-NODA is a nitroveratryl-based photocleavable linker, it has a NODA motif and a methyl phenyl acetic acid (MPAA) backbone. NH2-MPAA-NODA can be used as a radiolabel by labeling with ¹⁸F-fluoride.

HY-130001

CDK9-IN-9	CDK	Cancer
CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC₅₀ of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC₅₀ of 155 nM. CDK9-IN-9 has anti-cancer activity.

HY-118946B

BPH-1358 mesylate NSC50460 mesylate	Bacterial	Cancer Infection
BPH-1358 mesylate (NSC50460 mesylate) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively. BPH-1358 mesylate is active against *S. aureus* in vitro (MIC ~250 ng/mL).

HY-100486

BTTAA
Others Others

BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
HY-12794

Vps34-PIK-III
PI3K Autophagy Neurological Disease

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

HY-N3513

Mulberrin Kuwanon C	Others	Cardiovascular Disease
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC₅₀ value being 1.8 ±1.5 μM.

HY-N7140

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

HY-118946A

BPH-1358 free base NSC50460 free base	Bacterial	Cancer Infection
BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against *S. aureus* in vitro (MIC ~250 ng/mL).

HY-128776

Antitumor agent-19	Others	Cancer
Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC₅₀ values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.

HY-15527

Emapunil
AC-5216; XBD-173
Others Neurological Disease

Emapunil(AC-5216;XBD-173) is a translocator protein [TSPO (18 kDa)] ligand.
HY-13873

IKK-IN-1
IKK Inflammation/Immunology

IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.

HY-W008610

GBR 12783	Dopamine Receptor	Neurological Disease
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [³H]dopamine uptake by rat and mice striatal synaptosomes with IC₅₀s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats.

HY-128865

BPR1M97	Opioid Receptor	Neurological Disease
BPR1M97 is a dual-acting mu opioid receptor (MOP) and nociceptin-orphanin FQ peptide (NOP) receptor agonist with K_i values of 1.8 and 4.2 nM, respectively. BPR1M97 shows high potency and blood-brain barrier penetration, and produces potent antinociceptive effects.

HY-100968

GBR 12783 dihydrochloride	Dopamine Receptor	Neurological Disease
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [³H]dopamine uptake by rat and mice striatal synaptosomes with IC₅₀s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.

HY-103414

Raclopride	Dopamine Receptor	Neurological Disease
Raclopride is a dopamine D₂/D₃ receptor antagonist, which binds to D₂ and D₃ receptors with dissociation constants (K_is) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D₁ and D₄ receptors with K_is of 18000 nM and 2400 nM, respectively.

HY-110166

PD 90780	Others	Neurological Disease
PD 90780 is a non peptide antagonist of nerve growth factor (NGF) binding to the P75 NGF receptor, inhibits NGF-p75 NTR interaction with IC₅₀s values of 23.1 µM and 1.8 µM in PC12 cells and PC12 nnr5 cells, respectively .

HY-15343

CEP-33779
JAK Cancer

CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC₅₀ of 1.8±0.6 nM.
HY-16696

SN 2
TRP Channel Others

SN 2 is a novel and potent activator of TRPML3 ion channel with EC₅₀ of 1.8±0.13 μM.

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-101770

BTB-1
Microtubule/Tubulin Cancer

BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC₅₀ of 1.69 μM.

HY-111905

BRD7-IN-1	Epigenetic Reader Domain	Cancer
BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC₅₀s of 4.5 and 1.8 nM, respectively).

HY-P1542

Urotensin I Catostomus urotensin I	CRFR	Cardiovascular Disease Endocrinology
Urotensin I is, 41-aa neuropeptide, acts as an agonist of CRF receptor with pEC₅₀s of 11.46, 9.36 and 9.85 for human CRF₁, human CRF₂ and rat CRF_2α receptors in CHO cells, and K_is of 0.4, 1.8, and 5.7 nM for hCRF₁, rCRF_2α and mCRF_2β receptors, respectively.

HY-111905A

BRD7-IN-1 free base	Epigenetic Reader Domain	Cancer
BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC₅₀s of 4.5 and 1.8 nM, respectively).

HY-12278

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

HY-18325

AN-3485
Toll-like Receptor (TLR) Inflammation/Immunology

AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC₅₀ values ranging from 18 to 580 nM.

HY-19676

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

HY-130240

GCN2-IN-6	Eukaryotic Initiation Factor (eIF)	Cancer
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC₅₀ of 1.8 nM) and cellular assays (IC₅₀ of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC₅₀ of 0.26 nM (in enzymatic assay) and 230 nM (in cells).

HY-19765

GSK2798745	TRP Channel	Cardiovascular Disease
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC₅₀s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 is used in research for the treatment of pulmonary edema associated with congestive heart failure.

HY-17377

Vicriviroc maleate SCH-417690 maleate; SCH-D maleate	CCR HIV	Infection Endocrinology
Vicriviroc maleate (SCH-417690 maleate; SCH-D maleate) is a potent, selective, oral bioavailable and CNS penetrated antagonist of CCR5, with a K_i of 2.5 nM, and also inhibits HIV-1 in PBMC cells, with IC₉₀s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) and 10 nM (RU 570).

HY-136404

Melanin probe-1	Others	Cancer
Melanin probe-1 is an ¹⁸F-picolinamides based PET probe. Melanin probe-1 can be used for PET imaging of malignant melanoma. Melanin probe-1 exhibits high tumor targeting efficiency, excellent tumor imaging contrasts, desirable biodistribution patterns, and good in vivo stability.

HY-U00177

GDP366
Survivin Cancer

GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.

HY-15851

Revefenacin TD-4208; GSK1160724	mAChR	Inflammation/Immunology Cardiovascular Disease
Revefenacin (TD-4208; GSK1160724) is a potent mAChR antagonist; has a high affinity on M3 receptor with a K_i of 0.18 nM.

HY-18668

Integrin Antagonists 27
Integrin Cancer

Integrin Antagonists 27 is a small molecule integrin αvβ3 antagonist with binding affinity of 18 nM, as s novel anticancer agent.
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-112299

TAS6417
EGFR Cancer

TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC₅₀ values ranging from 1.1-8.0 nM.
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-100855

DC_C66	Histone Methyltransferase	Cancer
DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC₅₀ of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC₅₀=21 μM), PRMT6 (IC₅₀= 47μM), and PRMT5.

HY-19505

TPA-023B	GABA Receptor	Neurological Disease
TPA-023B is a high-affinity and orally active GABA_A receptor α2/α3 subtype (K_is of 0.73 nM/2 nM) partial agonist and a α1 subtype (K_i of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.

HY-10510

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

HY-10161

Tozasertib
VX 680; MK-0457
Aurora Kinase Autophagy Cancer

Tozasertib (VX 680; MK-0457) is an inhibitor of Aurora A/B/C kinases with K_is of 0.6, 18, 4.6 nM, respectively.

HY-13856

(R)-PS210	PDK-1	Cancer
(R)-PS210, the R enantiomer of PS210 (compound 4h-eutomer), is a substrate-selective allosteric activator of PDK1 with an AC₅₀ value of 1.8 μM. (R)-PS210 targets to the PIF-binding pocket of PDK1. PIF: The protein kinase C-related kinase 2 (PRK2)-interacting fragment.

HY-102070

NS13001	Potassium Channel	Neurological Disease
NS13001 is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC₅₀s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

HY-100443B

(-)-PX20606 trans isomer (-)-PX-102 trans isomer; (-)-PX-104	FXR Autophagy	Metabolic Disease
(-)-PX20606 trans isomer is a FXR agonist with EC₅₀s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.

HY-133740

MS117
Histone Methyltransferase Cancer

MS117 is a first-in-class and cell-active irreversible protein arginine methyltransferase 6 (PRMT6) covalent inhibitor, with an IC₅₀ of 18 nM.

HY-11109

Resatorvid TAK-242; CLI-095	Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy	Inflammation/Immunology Cancer
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-R and IL-6 production with IC_50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.

HY-135123

DC4SMe	ADC Cytotoxin	Cancer
DC4SMe, a phosphate prodrug of cytotoxic DNA alkylator DC4, can be used in the synthesis of Antibody-drug Conjugate (ADC). DC4SMe exhibits IC₅₀s of 1.9 nM, 2.9 nM, and 1.8 nM for Ramos, Namalwa, and HL60/s cancer cells, respectively. DC4SMe can be used for the targeted treatment of cancer.

HY-12076

BMS 777607 BMS 817378	c-Met/HGFR TAM Receptor	Cancer
BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC₅₀s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.

HY-111483

AZD-0364
ERK Cancer

AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC₅₀ of 0.6 nM.

HY-U00415

Benzamide Derivative 1	Dopamine Receptor mAChR	Neurological Disease
Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful in treatment of gastrointestinal disorders.

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-10221

Vorinostat SAHA; Suberoylanilide hydroxamic acid	HDAC Autophagy Mitophagy Filovirus	Cancer Infection
Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID₅₀ values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.

HY-50697

A-740003	P2X Receptor	Neurological Disease
A-740003 is a potent, selective and competitive P2X7 receptor antagonist with IC₅₀ values are 18 and 40 nM for rat and human P2X7 receptors, respectively.

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-13233B

Talabostat isomer mesylate	Others	Others
Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a K_i of 0.18 nM.

HY-17424

Penciclovir
BRL 39123; VSA 671
HSV Infection

Penciclovir is reported to be potent against HSV types 1 and 2 with IC₅₀ of 0.04-1.8 μg/mL and 0.06-4.4 μg/mL, respectively.
HY-111948

c-Fms-IN-7
c-Fms Cancer Inflammation/Immunology

c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC₅₀ of 18.5 nM.
HY-15732

BGB-102
JNJ-26483327
EGFR Cancer

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC₅₀s of 9.6 nM, 18 nM and 40.3 nM, respectively.

HY-100791

NSC23005 sodium	Others	Cancer
NSC23005 sodium is a novel and effective *p18* inhibitor (ED₅₀=5.21 nM) in promoting Hematopoietic stem cells (HSCs) expansion in both murine and human models.

HY-13319

JNK-IN-8
JNK Cancer

JNK-IN-8 is a potent JNK inhibitor with IC₅₀s of 4.7 nM, 18.7 nM, and 1 nM for JNK1, JNK2, and JNK3, respectively.

HY-117970

MMPI-1154	MMP	Cardiovascular Disease
MMPI-1154 is a promising novel cardio-cytoprotective imidazole-carboxylic acid (ICA) MMP-2 inhibitor(IC₅₀=6.6 μM) and can be used for the study of acute myocardial infarction. MMPI-1154 also inhibits the activity of MMP-13, MMP-1 and MMP-9 with IC₅₀s of 1.8 μM,10 μM, and 13 μM, respectively.

HY-B0573

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

HY-B0573B

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

HY-112584

JBSNF-000088 6-Methoxynicotinamide	Endogenous Metabolite	Metabolic Disease
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent Nicotinamide N-methyltransferase (NNMT) inhibitor with IC₅₀s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease.

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-100757

CPUY074020	Histone Methyltransferase	Cancer
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC₅₀ of 2.18 μM. CPUY074020 possesses anti-proliferative activity.

HY-14399

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

HY-U00435

Neoseptin 3
Toll-like Receptor (TLR) Cancer

Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation factor 2 (mTLR4/MD-2) agonist with an EC₅₀ of 18.5 μM.
HY-100531

DprE1-IN-2
Bacterial Infection

DprE1-IN-2 (compound 18) is a potent DprE1 inhibitor with an IC₅₀ of 28 nM. DprE1-IN-2 has antituberculosis effect.
HY-12835

S1P1 Agonist III
LPL Receptor Inflammation/Immunology

S1P1 Agonist III is a potent and orally active S1P1 agonist with EC50 of 18 nM; no activity on S1P3.

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-13205

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

HY-N6691

Veratridine 3-Veratroylveracevine	Sodium Channel	Neurological Disease
Veratridine (3-Veratroylveracevine), a alkaloid derived from plants in the family Liliaceae, is a sodium channel agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM.

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-B0573S

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

HY-P1274A

ShK-Dap22 TFA	Potassium Channel	Inflammation/Immunology
ShK-Dap22 TFA is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 TFA is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

HY-114414

HDACs/mTOR Inhibitor 1	HDAC mTOR Apoptosis	Cancer
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC₅₀s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.

HY-P1274

ShK-Dap22	Potassium Channel	Inflammation/Immunology
ShK-Dap22 is a potent Kv1.3-specific immunosuppressive Polypeptide. ShK-Dap22 is a selective Kv1.3 channel blocker with IC₅₀s of 23 pM, 1.8 nM, 10.5 nM, 37 nM, and 39 nM for mKv1.3, mKv1.1, hKv1.6, mKv1.4, and rKv1.2 channels, respectively.

HY-15186

Ipatasertib GDC-0068; RG7440	Akt	Cancer
Ipatasertib (GDC-0068) is a highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

HY-15065

Chembridge-5861528 TCS 5861528	TRP Channel	Neurological Disease
Chembridge-5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively).

HY-133126

hDDAH-1-IN-1	Others	Cancer Inflammation/Immunology
hDDAH-1-IN-1 (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a K_i of 18 µM.

HY-14949

Cevipabulin TTI-237	Microtubule/Tubulin	Cancer
Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [³H] vinblastine to tubulin, with an IC₅₀ of 18-40 nM for cytotoxicity in human tumor cell line.

HY-108570

AUDA	Epoxide Hydrolase	Inflammation/Immunology
AUDA (compound 43) is a potent soluble epoxide hydrolase (sEH) inhibitor with IC₅₀s of 18 and 69 nM for the mouse and human sEH, respectively. AUDA has anti-inflammatory activity.

HY-15186A

Ipatasertib dihydrochloride GDC-0068 dihydrochloride; RG-7440 dihydrochloride	Akt	Cancer
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

HY-12030

PIK-90
PI3K DNA-PK Cancer

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC₅₀s of 11, 18 and 13 nM, respectively.
HY-125872

KRAS G12C inhibitor 14
Ras Cancer

KRAS G12C inhibitor 14 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 17, has an IC₅₀ of 18 nM.

HY-59090

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

HY-136447

ASP4132	AMPK	Cancer
ASP4132 is an orally active, potent AMPK activator with an EC₅₀ of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.

HY-129059

Odapipam NNC 756	Dopamine Receptor	Neurological Disease
Odapipam (NNC 756) is a selective, high affinity and benzazepine dopamine D₁ receptor antagonist with a K_d of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer.

HY-P1602

Apidaecin IB
Bacterial Infection

Apidaecin IB is a insect antimicrobial peptide, with minimum inhibitory concentration (MIC) values of 8 μM for E. coli (ML35, O18K1H7 and ATCC 25922).

HY-133126A

hDDAH-1-IN-1 TFA	Others	Cancer Inflammation/Immunology
hDDAH-1-IN-1 TFA (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a K_i of 18 µM.

HY-14397

Indomethacin Indometacin	COX Bacterial Autophagy Antibiotic	Inflammation/Immunology Cancer
Indomethacin (Indometacin) is a potent and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.

HY-12304

IOX1	Histone Demethylase	Cancer
IOX1, 5-Carboxy-8-hydroxyquinoline, is a potent broad‐spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases. IOX1 inhibits KDM4C, KDM4E, KDM2A, KDM3A and KDM6B with IC₅₀ values of 0.6 μM, 2.3 μM, 1.8 μM, 0.1 μM and 1.4 μM, respectively. IOX1 also inhibits ALKBH5.

HY-131005

Ehp inhibitor 2
Ephrin Receptor Cancer

Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.

HY-U00448

ADDA 5 hydrochloride	Others	Cancer
ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC₅₀s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.

HY-100018

BAY1125976
Akt Cancer

BAY1125976 is a selective allosteric Akt1/Akt2 inhibitor; inhibits Akt1 and Akt2 activity with IC₅₀ values of 5.2 nM and 18 nM at 10 μM ATP, respectively.

HY-14949C

Cevipabulin fumarate TTI-237 fumarate	Microtubule/Tubulin	Cancer
Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [³H]NSC 49842 to tubulin, with an IC₅₀ of 18-40 nM for cytotoxicity in human tumor cell line.

HY-101923B

LYN-1604 dihydrochloride	ULK Autophagy Apoptosis	Cancer
LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

HY-100708

NSC632839	Deubiquitinase	Cancer
NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC₅₀s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.

HY-101923A

LYN-1604 hydrochloride	ULK Autophagy Apoptosis	Cancer
LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

HY-101923

LYN-1604
ULK Autophagy Apoptosis Cancer

LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC₅₀=18.94 nM) for the research of triple negative breast cancer (TNBC).

HY-18732A

L-NMMA acetate Tilarginine acetate; Methylarginine acetate	NO Synthase	Cardiovascular Disease
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The K_i values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.

HY-101943

LY 345899	Others	Cancer
LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC₅₀ values of 96 nM and 663 nM, respectively and a K_i of 18 nM for MTHFD1.

HY-12892

SKI-178	SPHK Apoptosis	Cancer
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC₅₀ concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.

HY-10961

Momelotinib CYT387	JAK Autophagy Apoptosis	Cancer
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

HY-110201

Estrogen receptor modulator 1	Estrogen Receptor/ERR	Cancer
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC₅₀ of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors.

HY-10959

RG7112 RO5045337	MDM-2/p53 E1/E2/E3 Enzyme	Cancer
RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC₅₀ of 18 nM and a K_D of 11 nM for binding to MDM2.

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-W015422

1,5-Isoquinolinediol	PARP	Metabolic Disease
1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC₅₀ of 0.18-0.37 µM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina.

HY-P0256

Apamin Apamine	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-B0274

Chlorprothixene	Dopamine Receptor Histamine Receptor Bacterial	Neurological Disease
Chlorprothixene is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

HY-P1401

Protein Kinase C (19-36)	PKC	Metabolic Disease
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC₅₀ of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response.

HY-15553A

Mibefradil dihydrochloride Ro 40-5967 dihydrochloride	Calcium Channel	Cardiovascular Disease
Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca²⁺ channels displaying IC₅₀s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.

HY-B0274A

Chlorprothixene hydrochloride	Dopamine Receptor Histamine Receptor Bacterial	Neurological Disease
Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

HY-128596

ALK-IN-6	ALK	Cancer
ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC₅₀ values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively.

HY-135619

DHODH-IN-4	Parasite Dihydroorotate Dehydrogenase DNA/RNA Synthesis	Infection Inflammation/Immunology
DHODH-IN-4 (compound 17) is a human and Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitor, with IC₅₀ values of 4 μM and 0.18 μM for PfDHODH and HsDHODH, respectively. DHODH-IN-4 (compound 17) possess antimalarial activity.

HY-P1441

Mambalgin 1	Sodium Channel
Mambalgin 1 is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-N6742

Borrelidin Treponemycin	CDK Parasite Apoptosis Antibiotic	Infection
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin (Treponemycin) is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC₅₀ of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor, with an IC₅₀ of 0.8 nM, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC₅₀s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum.

HY-111234

IDO-IN-11	Indoleamine 2,3-Dioxygenase (IDO)	Cancer
IDO-IN-11 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC₅₀s of 0.18 μM (Kinase) and 0.014 μM (Hela Cell), extracted from patent WO 2016041489 A1, compound 13.

HY-111427

CDK8/19-IN-1	CDK	Cancer
CDK8/19-IN-1 is a potent, selective and oral bioavailable CDK8/19 dual inhibitor, with IC₅₀s of 0.46 nM, 0.99 nM and 270 nM for CDK8, CDK19 and CDK9, respectively.

HY-75564

Cyclo(Ala-Gly)	Endogenous Metabolite	Cancer
Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC₅₀ values range from 9.5 to 18.1 μM.

HY-N4266

Vinaginsenoside R8	Others	Cardiovascular Disease
Vinaginsenoside R8, a triterpenoid glycoside isolated from the rhizomes of Panacis majoris. Vinaginsenoside R8 displays activities against adenosine diphosphate (ADP)-induced platelet aggregation (IC₅₀=25.18 μM).

HY-101281A

(Rac)-VU 6008667	mAChR	Neurological Disease
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC₅₀=1.8 μM, pIC₅₀= 5.75), has high CNS penetration.

HY-112908

RTS-V5
HDAC Proteasome Cancer

RTS-V5 is a dual HDAC/proteasome inhibitor with IC₅₀s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.

HY-101512

A-395	Histone Methyltransferase	Cancer
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC₅₀ of 18 nM.

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-15553

Mibefradil Ro 40-5967	Calcium Channel	Cardiovascular Disease
Mibefradil (Ro 40-5967) is a calcium channel blocker with moderate selectivity for T-type Ca²⁺ channels displaying IC₅₀s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively.

HY-P0256A

Apamin TFA Apamine TFA	Potassium Channel	Inflammation/Immunology Neurological Disease
Apamin TFA (Apamine TFA) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom), is known as a specifically selective blocker of Ca²⁺-activated K⁺ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity.

HY-P1441A

Mambalgin 1 TFA	Sodium Channel
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-121879

SHP836
Phosphatase Cancer

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

HY-P1215

HS024	Melanocortin Receptor	Metabolic Disease
HS024 is a selective MC4 receptor antagonist, with K_is of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.

HY-114200

Imrecoxib BAP-909	COX	Inflammation/Immunology
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC₅₀ value of 18 nM, it also inhibits COX1- activity with an IC₅₀ value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.

HY-P1215A

HS024 TFA	Melanocortin Receptor	Metabolic Disease
HS024 is a selective MC4 receptor antagonist, with K_is of 0.29, 3.29, 5.45, 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake.

HY-129681

MCL-1/BCL-2-IN-1
Bcl-2 Family Cancer

MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC₅₀s of 4.45 and 3.18 μM, respectively.

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-120062

TVB-3664	Fatty Acid Synthase (FASN)	Cancer
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC₅₀ values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.

HY-N2350

Cynaropicrin	MMP NF-κB TNF Receptor	Cancer
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC₅₀s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.

HY-101379A

8-Bromo-cGMP sodium	Calcium Channel	Neurological Disease
8-Bromo-cGMP sodium, a membrane-permeable analogue of cGMP, is a PKG (protein kinase G) activator and significantly inhibits Ca²⁺ macroscopic currents and impairs insulin release stimulated with high K⁺. 8-Bromo-cGMP sodium has antinociceptive effects.

HY-19231

DPI-3290 Org 41793	Opioid Receptor	Neurological Disease
DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with K_i values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity.

HY-101964

SPI-112	Phosphatase	Cancer
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC₅₀s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.

HY-128774

AM-6494	Beta-secretase	Neurological Disease
AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC₅₀=0.4 nM) with in vivo selectivity over BACE2 (IC₅₀=18.6 nM).

HY-100132

P300/CBP-IN-5	Histone Acetyltransferase	Cancer
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC₅₀ of 18.8 nM.

HY-14397S

Indomethacin-D4 Indometacin-D4	COX Autophagy	Inflammation/Immunology
Indomethacin-D4 (Indometacin-D4) is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC₅₀s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.

HY-77251

TAK1/MAP4K2 inhibitor 1	MAP4K MAP3K	Cancer
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC₅₀s of 41.1 nM and 18.2 nM, respectively.

HY-115661

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

HY-104008

ACY-957	HDAC	Others
ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC₅₀s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.

HY-W012399

2,5-Di-tert-butylhydroquinone	Lipoxygenase COX	Inflammation/Immunology
2,5-Di-tert-butylhydroquinone (DTBHQ), the indirect food additive, regulates the activity of 5-lipoxygenase as well as the activity of COX-2 (IC₅₀=1.8 and 14.1 for 5-LO and COX-2, respectively) .

HY-101908

BMS CCR2 22	CCR	Inflammation/Immunology Endocrinology
BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC₅₀ of 5.1 nM) and potent functional antagonism (calcium flux IC₅₀ of 18 nM and chemotaxis IC₅₀ of 1 nM).

HY-13007

PF-3758309	PAK Apoptosis	Cancer
PF-3758309 is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; *K_i*=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

HY-125851

TGFβRI-IN-2	ALK	Inflammation/Immunology
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC₅₀ and pEC₅₀ values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose.

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-128704A4

c-Kit-IN-3 maleate	c-Kit	Cancer
c-Kit-IN-3 maleate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC₅₀ of 4 nM. c-Kit-IN-3 maleate displays great potencies against c-KIT kinase and a broad spectrum of drug-resistant mutants in the biochemical assay. c-Kit-IN-3 maleate has improved bioavailability.

HY-19322B

PIM-447 dihydrochloride LGH447 dihydrochloride	Pim	Cancer
PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with K_i values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.

HY-125176

G907	Bacterial	Infection
G907 is a selective small-molecule antagonist of ATP-binding cassette (ABC) transporter, MsbA. It inhibits purified E. coli MsbA in amphipols with an IC₅₀ of 18 nM. G907 traps MsbA in an inward-facing, lipopolysaccharide-bound conformation by wedging into an architecturally conserved transmembrane pocket. Bactericidal activity.

HY-N1584

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

HY-19322

PIM447 LGH447	Pim Apoptosis	Cancer
PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with K_i values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.

HY-112144

TP0463518	HIF/HIF Prolyl-Hydroxylase	Metabolic Disease
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a K_i value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC₅₀s of 18 and 63 nM as well as monkey PHD2 with an IC₅₀ value of 22 nM.

HY-14874

Topiroxostat FYX-051	Xanthine Oxidase Cytochrome P450	Metabolic Disease
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC₅₀ value of 5.3 nM and a K_i value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.

HY-103265

ARL67156 trisodium salt	Phosphatase	Cardiovascular Disease
ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 trisodium salt is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with K_is of 11, 18 and 12 μM, respectively. ARL67156 trisodium salt prevents in vivo the development of calcific aortic valve disease.

HY-N2511

Trimyristin	AChE Phosphatase Endogenous Metabolite	Metabolic Disease
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC₅₀s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively.

HY-108425B

(Rac)-AMG8379 (Rac)-AMG8380	Sodium Channel	Neurological Disease
(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .

HY-15536

Cebranopadol GRT6005	Opioid Receptor	Neurological Disease
Cebranopadol is an analgesic NOP and opioid receptor agonist with K_is/EC₅₀s of 0.9 nM/13 nM, 0.7 nM/1.2 nM, 2.6 nM/17 nM, 18 nM/110 nM for human NOP, MOP, KOP and delta-opioid peptide (DOP) receptor, respectively.

HY-N1584A

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

HY-14722C

NVP-BSK805 trihydrochloride	JAK	Cancer
NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

HY-14722A

NVP-BSK805 dihydrochloride	JAK	Cancer
NVP-BSK805 dihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

HY-14722

NVP-BSK805	JAK	Cancer
NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively.

HY-13007A

PF-3758309 hydrochloride	PAK Apoptosis	Cancer
PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; *K_i*=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

HY-120028

GNE-207	Epigenetic Reader Domain Histone Acetyltransferase	Cancer
GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC₅₀ of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC₅₀ of 18 nM for MYC expression in MV-4-11 cells.

HY-125232

MS645	Epigenetic Reader Domain	Cancer
MS645 is a bivalent BET bromodomains (BrD) inhibitor with a K_i of 18.4 nM for BRD4-BD1/BD2. MS645 spatially constrains bivalent inhibition of BRD4 BrDs resulting in a sustained repression of BRD4 transcriptional activity in solid-tumor cells.

HY-19026

Siguazodan SKF 94836	Phosphodiesterase (PDE)	Cardiovascular Disease
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC₅₀ of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC₅₀ of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC₅₀ value of 4.2 μM.

HY-N4110

Friedelin	Cytochrome P450	Metabolic Disease
Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC₅₀ and K_ivalues of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC₅₀ and K_i values of 22.54 μM and 18.02 μM, respectively.

HY-101517

PI3K-IN-2	PI3K	Cancer
PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC₅₀=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC₅₀=13/190 nM, respectively).

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-13941B

1-Naphthyl PP1 hydrochloride 1-NA-PP 1 hydrochloride	Src	Cancer
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC₅₀s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.

HY-B1452

Licofelone ML-3000	COX Lipoxygenase Apoptosis	Cancer Inflammation/Immunology
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC₅₀=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.

HY-13941

1-Naphthyl PP1 1-NA-PP 1	Src	Cancer
1-Naphthyl PP1 (1-NA-PP 1) is a selective inhibitor of src family kinases. 1-Naphthyl PP1 inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC₅₀s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.

HY-112900

DC41SMe	ADC Cytotoxin	Cancer
DC41SMe, a DC1 derivative, shows cytotoxicity in Ramos, Namalwa, and HL60/s cells with IC₅₀s ranging from 18-25 pM. DC1, a simplified analogue of CC-1065, is an antibody conjugate of cytotoxic DNA alkylators for the targeted treatment of cancer.

HY-122337

Streptolydigin Portamycin	DNA/RNA Synthesis Bacterial	Infection
Streptolydigin (Portamycin) is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor with a K_i of 18 μM and a K_d of 15 μM. Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin possess potent antibacterial activity, particularly against anaerobes and some Gram-positive aerobes.

HY-124817

Col003	HSP	Inflammation/Immunology
Col003 is a selective and potent inhibitor of Hsp47 and competitively binds to the collagen binding site on Hsp47 (IC₅₀=1.8 μM). Col003 discourages the interaction of Hsp47 with collagen and inhibits collagen secretion by destabilizing the collagen triple helix. Col003 can be used for the investigation of fibrosis

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-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-17372

Rofecoxib MK 966	COX	Inflammation/Immunology Cancer
Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC₅₀s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC₅₀ > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).

HY-103131

PNU-142633	5-HT Receptor	Neurological Disease
PNU-142633 is a high affinity, selective and orally active 5-HT_1D receptor agonist with K_is of 6 nM and > 18 000 nM for human 5-HT_1D receptor and human 5-HT_1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

HY-N6009

8-Deoxygartanin	Parasite NF-κB	Infection
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE). 8-Deoxygartanin exhibits antiplasmodial activity with an IC₅₀ of 11.8 μM for the W2 strain of Plasmodium falciparum. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC₅₀ of 11.3 μM.

HY-124952

iKIX1	Fungal	Infection
iKIX1 is an antifungal agent and re-sensitizes drug-resistant C. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC₅₀ and K_i values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection.

HY-19485

XL-784	MMP	Cardiovascular Disease
XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC₅₀s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.

HY-19745

BMS-202	PD-1/PD-L1 Apoptosis	Cancer
BMS-202 is a potent and nonpeptidic PD-1/PD-L1 complex inhibitor with an IC₅₀ of 18 nM and a K_D of 8 μM. BMS-202 binds to PD-L1 and blocks human PD-1/PD-L1 interaction. BMS-202 has antitumor activity.

HY-103364A

C-021 dihydrochloride	CCR	Inflammation/Immunology
C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC₅₀s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [³⁵S]GTPγS from binding to the receptor with an IC₅₀ of 18 nM.

HY-128704

c-Kit-IN-3	c-Kit	Cancer
c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC₅₀s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.

HY-111372

Finerenone BAY 94-8862	Mineralocorticoid Receptor	Cardiovascular Disease
Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC₅₀=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease.

HY-N2512

1-Monomyristin	FAAH Bacterial Fungal Endogenous Metabolite Autophagy	Infection
1-Monomyristin, extracted from Serenoa repens, inhibits the hydrolysis of 2-oleoylglycerol (IC₅₀=32 μM) and fatty acid amide hydrolase (FAAH) activity (IC₅₀=18 μM). 1-Monomyristin shows antibacterial activity against Staphylococcus aureus and Aggregatibacter actinomycetemcomitans and also antifungal activity against Candida albicans.

HY-128704A1

c-Kit-IN-3 hydrochloride	c-Kit	Cancer
c-Kit-IN-3 hydrochloride (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC₅₀ of 4 nM) and a broad spectrum of drug-resistant mutants (IC₅₀ of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.

HY-W008344

2-Chloroadenosine	Others	Others
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent K_i=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent K_i=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.

HY-112160

XL-784 free base	MMP	Cardiovascular Disease
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC₅₀s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1，MMP-2，MMP-3，MMP-8，MMP-9，MMP-13，respectively.

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-10200

BMS-754807	IGF-1R Insulin Receptor	Cancer Endocrinology
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC₅₀=1.8 and 1.7 nM, respectively; K_i=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC₅₀ values of 6, 44, 7, 4, 9, and 25 nM, respectively.

HY-10019

Varenicline CP 526555	nAChR	Neurological Disease
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.

HY-128704A6

c-Kit-IN-3 L-tartrate	c-Kit	Cancer
c-Kit-IN-3 L-tartrate (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC₅₀s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 L-tartrate displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.

HY-130616

EGFR-IN-11	EGFR	Cancer
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC₅₀ of 18 nM for triple mutant EGFR^{L858R/T790M/C797S}. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

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-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-111546

BI-3663	PROTAC FAK	Cancer
BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation. BI-3663 inhibits PTK2 with an IC₅₀ of 18 nM. BI-3663 is a PROTAC that composes of BI-4464 (HY-124625) linked to Pomalidomide (HY-10984) with a linker. Anti-cancer activity.

HY-128704A7

c-Kit-IN-3 tartrate	c-Kit	Cancer
c-Kit-IN-3 tartrate (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC₅₀ of 4 nM) and a broad spectrum of drug-resistant mutants (IC₅₀ of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.

HY-108476

INDY	DYRK	Cancer
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC₅₀s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a K_i value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.

HY-15971A

AMD 3465 GENZ-644494	CXCR HIV	Infection Endocrinology
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC₅₀: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

HY-108425

AMG8379	Sodium Channel	Neurological Disease
AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC₅₀ of 3.1 nM.

HY-N0678

Icaritin Anhydroicaritin	Autophagy Apoptosis	Cancer
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium Genusis and potently inhibits proliferation of K562 cells (IC₅₀ of 8 µM) and primary CML cells (IC₅₀ of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis^[3.

HY-107589A

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

HY-107589

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

HY-10297

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

HY-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-12596

JNJ-26489112	Calcium Channel Sodium Channel Potassium Channel	Neurological Disease
JNJ-26489112, a CNS-active agent, exhibits broad-spectrum anticonvulsant activity in rodents against audiogenic, electrically-induced, and chemically-induced seizures. JNJ-26489112 inhibits voltage-gated Na⁺ channels and N-type Ca²⁺ channels, and is effective as a K⁺ channel opener. JNJ-26489112 has very weak inhibition of CA-II (IC₅₀=35 μM) and CA-I (18 μM).

HY-N1860

3-O-Methylquercetin	Phosphodiesterase (PDE)	Inflammation/Immunology
3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC₅₀ values of 31.9 μM， 86.9 μM， 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively.

HY-128656

LML134	Histamine Receptor	Neurological Disease Endocrinology
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with K_is of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.

HY-15971

AMD 3465 hexahydrobromide GENZ-644494 hexahydrobromide	CXCR HIV	Infection Endocrinology
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC₅₀: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

HY-128704A5

c-Kit-IN-3 D-tartrate	c-Kit	Cancer
c-Kit-IN-3 (D-tartrate) (Compound 18) is a potent c-KIT kinase inhibitor, which is potent and selective against BaF3-tel-c-KIT (IC₅₀ of 4 nM) and a broad spectrum of drug-resistant mutants (IC₅₀ of 8 nM for BaF3-tel-c-KIT-T670I) with improved bioavailability.

HY-117386

Methoxyfenozide	Bacterial
Methoxyfenozide, a diacylhydrazine insecticide, selectively binds to lepidopteran ecdysone receptors (EcRs) over dipteran EcRs with K_d values of 0.5 and 124 nM, respectively. Methoxyfenozide is lethal to neonatal larvae of S. exigua, S. frugiperda, T. ni, O. nubilalis, L. pomonella, H. zea, and H. virescens (LC₅₀s=0.35, 0.2, 0.11, 0.18, 0.21, 0.79, and 3.12 mg/L, respectively).

HY-133012

GFB-8438	TRP Channel	Neurological Disease
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.

HY-101762

TyK2-IN-2	JAK Phosphodiesterase (PDE)	Inflammation/Immunology
TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC₅₀s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC₅₀ of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.

HY-136092

Androsta-1,4,6-triene-3,17-dione	Aromatase	Endocrinology Neurological Disease
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a K_i of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.

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 IC₅₀s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.

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-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-111191

ONO-2952	Others	Neurological Disease
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with K_i of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.

HY-13233A

Talabostat mesylate Val-boroPro mesylate; PT100 mesylate	Dipeptidyl Peptidase	Cancer Inflammation/Immunology
Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC₅₀ < 4 nM; K_i = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC₅₀ = 560 nM), inhibits DPP8/9 (IC₅₀ = 4/11 nM; K_i = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC₅₀ = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.

HY-103360

J-113863	CCR	Inflammation/Immunology
J-113863 is a potent and selective CCR1 (CD18) antagonist with IC₅₀ values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC₅₀ of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC₅₀ of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.

HY-112429

HJB97	Epigenetic Reader Domain	Cancer
HJB97 is a high-affinity BET inhibitor with K_is of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity.

HY-103045

CMPD101	PKC ROCK	Cardiovascular Disease
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC₅₀ of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC₅₀s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure.

HY-13233

Talabostat Val-boroPro; PT100	Dipeptidyl Peptidase	Cancer Inflammation/Immunology
Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC₅₀ < 4 nM; K_i = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC₅₀ = 560 nM), inhibits DPP8/9 (IC₅₀ = 4/11 nM; K_i = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC₅₀ = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities.

HY-13522

Fimepinostat CUDC-907	PI3K HDAC Apoptosis	Cancer
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC₅₀ of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.

HY-112345

PD-089828	FGFR PDGFR EGFR Src	Cancer
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

HY-122582

TL13-12	PROTAC ALK	Cancer
TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC₅₀ values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).

HY-111754

DMX-5804	MAP4K	Cardiovascular Disease
DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC₅₀ of 3 nM, a pIC₅₀ of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC₅₀, 8.18), and TNIK/MAP4K7 (pIC₅₀, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.

HY-135809

A2764 dihydrochloride	Potassium Channel	Neurological Disease
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K⁺ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC₅₀=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.

HY-101514

β3-AR agonist 1	Adrenergic Receptor	Cardiovascular Disease Endocrinology
β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC₅₀=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).

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-N2214

7-O-Methylaloeresin A	Bacterial	Inflammation/Immunology
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae). 7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively. 7-O-Methylaloeresin A has antioxidant activities, gives IC₅₀ values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively.

HY-122203

PCS1055 dihydrochloride	mAChR AChE	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively.

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-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-130422

Tos-PEG4-t-butyl ester Tos-PEG4-Boc	PROTAC Linker	Cancer
Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) can be used in the synthesis of a series of PROTACs, such as BI-3663 (HY-111546). BI-3663 is a highly selective PTK2/FAK PROTAC, with cereblon ligands to hijack E3 ligases for PTK2 degradation, and inhibits PTK2 with an IC₅₀ of 18 nM.

HY-100513A

Dehydroaltenusin	Apoptosis DNA/RNA Synthesis	Cancer
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC₅₀ value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (K_i=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (K_i=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.

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-101261

ATPA	iGluR	Neurological Disease
ATPA is a selective glutamate receptor GluR5 activator with EC₅₀s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively.

HY-12307

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

HY-18340

(R)-CR8 CR8, (R)-Isomer	CDK Apoptosis	Cancer Neurological Disease
(R)-CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K.

HY-18340A

(R)-CR8 trihydrochloride CR8, (R)-Isomer trihydrochloride	CDK Apoptosis	Cancer Neurological Disease
(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC₅₀=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect. (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K.

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-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.

Cat. No.	Product Name	Type

HY-D1048

Cy7 DiC18
Fluorescent Dyes/Probes

Cy7 DiC18 is a lipophilic, near-infrared fluorescent cyanine dye used for staining membranes.

HY-D0083

DiI DiIC18(3)	Fluorescent Dyes/Probes
DiI (DiIC18(3)) is a lipophilic membrane dye that diffuses laterally to stain the entire cell. DiI is excited to emit orange-red fluorescence. The fluorescence is weak in water but strong and photostable when incorporated into membranes.

HY-D0903

DFO
9H-1,8-Diazafluoren-9-one
Fluorescent Dyes/Probes

DFO (9H-1,8-Diazafluoren-9-one) is a chemical that is used to find fingerprints on porous surfaces.
HY-D0193

Ponceau 4R
Acid Red 18; New Coccine
Dyes

Ponceau 4R is a synthetic colourant that may be used as a food colouring.

HY-D0969

3,3'-Dioctadecyloxacarbocyanine perchlorate DiO; DiOC18(3)	Fluorescent Dyes/Probes
3,3′-Dioctadecyloxacarbocyanine perchlorate is a green fluorescent lipophilic tracer, which is weakly fluorescent in water but highly fluorescent and quite photostable when incorporated into membranes.

HY-135009

2-Di-1-ASP	Fluorescent Dyes/Probes
2-Di-1-ASP (Compound 18a) is a mono-stryryl dye, and widely used as mitochondrial stain and groove-binding fluorescent probes for double-stranded DNA. 2-Di-1-ASP is selective for G-quadruplex (G4) and double-stranded DNA.

Cat. No.	Product Name	Type

HY-126712

ROS tracer precursor
Biochemical Assay Reagents

ROS tracer precursor is the precursor of [¹⁸F]ROStrace for the synthesis of ROStrace, which can be used for disease diagnosis.

Cat. No.	Product Name	Target	Research Area

HY-P1863

*α-Neoendorphin (1-8)*	Peptides	Neurological Disease
α-Neoendorphin (1-8) is a 8-amino acid peptide derived from the N-terminal of α-Neoendorphin. α-Neoendorphin is an endogenous opioid peptide.

HY-P1879

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

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

HY-P1039A

R18 TFA PHCVPRDLSWLDLEANMCLP TFA	Peptides	Cancer
R18 TFA is a peptide antagonists of 14-3-3, with a K_D of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1.

HY-P1476

Adrenocorticotropic Hormone (ACTH) (18-39), human CLIP (human)	Peptides	Metabolic Disease
Adrenocorticotropic Hormone (ACTH) (18-39), human is a corticotropinlike intermediate lobe peptide, which is produced in the melanotrophs of the intermediate lobe of the pituitary.

HY-P1476A

Adrenocorticotropic Hormone (ACTH) (18-39), human TFA CLIP (human) (TFA)	Peptides	Metabolic Disease
Adrenocorticotropic Hormone (ACTH) (18-39), human TFA is a corticotropinlike intermediate lobe peptide, which is is produced in the melanotrophs of the intermediate lobe of the pituitary.

HY-P0279

Systemin
Peptides Others

Systemin, an 18-amino acid polypeptide, has been isolated from tomato leaves that is a powerful inducer of over 15 defensive genes.