Search Result
Results for "
disease
" in MedChemExpress (MCE) Product Catalog:
9595
Inhibitors & Agonists
142
Biochemical Assay Reagents
833
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-147108
-
|
|
Mitochondrial Metabolism
|
Cancer
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Mitochondria degrader-1 (example 5) is a potent mitochondria degrader. Mitochondria degrader-1 induces the degradation of the injured mitochondria by the autophagy mechanism. Mitochondria degrader-1 can be used for the research of neurodegenerative disease, cancer, inflammatory disease, age-related disease, metabolic disease, mitochondrial disease or Down's disease.
|
-
- HY-137431A
-
|
(R)-BAY-2433334
|
Others
|
Cardiovascular Disease
|
|
(R)-Asundexian ((R)-BAY-2433334) is the enantiomer of Asundexian (HY-137431). (R)-Asundexian can be used in studies of cardiovascular disease (especially thrombotic or thromboembolic disease), edema, and ophthalmic disease.
|
-
- HY-P4040
-
-
- HY-122105
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
JNJ-40255293 is a high-affinity human A 2A receptor antagonist with a KiKi of 7.5 nM. JNJ-40255293 can be used in the research of neurodegenerative diseases such as Parkinson's disease.
|
-
- HY-153427
-
|
|
Tau Protein
|
Neurological Disease
|
|
Tau protein aggregation-IN-1 (Compound 0c) is a Tau protein aggregation inhibitor. Tau protein aggregation-IN-1 can be used in the study of protein folding disorders such as Alzheimer's disease, dementia, Parkinson's disease, Huntington's disease and prion-based spongiform encephalopathies.
|
-
- HY-132594A
-
-
- HY-132594
-
-
- HY-118284
-
|
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P2Y Receptor
|
Cardiovascular Disease
|
|
Vicagrel is a potent, safe and orally active antiplatelet agent, which works by irreversibly inhibiting P2Y12 receptor. Vicagrel can be used for the research of blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
|
-
- HY-W011246
-
|
HP 029; Hydroxytacrine maleate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Velnacrine maleate (HP 029) is an orally active cholinesterase inhibitor that can be used for the research of Alzheimer's disease.
|
-
- HY-16743
-
|
Venglustat; SAR402671; GZ402671
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-16743B
-
|
Venglustat succinate; SAR402671 succinate; GZ402671 succinate
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Ibiglustat (Venglustat) succinate is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat succinate can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-16743A
-
|
Venglustat (L-Malic acid); SAR402671 (L-Malic acid); GZ402671 (L-Malic acid)
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Ibiglustat (Venglustat) L-Malic acid is an orally active, brain-penetrant glucosylceramide synthase (GCS) inhibitor. Ibiglustat L-Malic acid can be used for the research of Gaucher disease type 3, Parkinson's disease associated with GBA mutations, Fabry disease, GM2 gangliosidosis, and autosomal dominant polycystic kidney disease.
|
-
- HY-107337
-
-
- HY-P99356
-
|
BIIB054; Anti-Alpha-synuclein Reference Antibody (cinpanemab)
|
α-synuclein
|
Neurological Disease
|
|
Cinpanemab (BIIB054) is a human-derived monoclonal antibody that binds to α-synuclein. Cinpanemab can be used for the research of Parkinson's disease.
|
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- HY-40294
-
|
|
Monoamine Oxidase
GSK-3
LRRK2
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
Indazole, also called isoindazole, a heterocyclic aromatic organic compound. Its derivatives display a broad variety of biological activities including anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour properties. Indazole and its derivatives can be used for research of cancer, neurological disorders, cardiovascular diseases, gastrointestinal diseases.
|
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- HY-P2699
-
|
GrTx; ω-GsTx SIA
|
Calcium Channel
|
Neurological Disease
|
|
ω-Grammotoxin SIA (GrTx) is P/Q and N-type voltage-gated Calcium channels inhibitor. ω-Grammotoxin SIA is also a protein toxin that can be obtained from spider venom. ω-Grammotoxin SIA has the potential to study neurological diseases as well as cardiovascular diseases.
|
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- HY-147240
-
|
|
Others
|
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
Acloproxalap is a quinoline-based aldehyde scavenger that can be used in studies of diseases with toxic aldehyde accumulation, such as inflammatory diseases of the eye and skin, respiratory diseases such as pneumonia, organ diseases, and viral infection-related syndromes.
|
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- HY-147579
-
|
|
TAM Receptor
|
Cancer
Infection
Inflammation/Immunology
|
|
Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
|
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- HY-149268
-
|
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JNK
|
Neurological Disease
|
|
JNK3 inhibitor-6 (Compound A53) is a selective JNK3 Inhibitor (IC50=78 nM). JNK3 inhibitor-6 has neuroprotective effect, and can used for research of neurodegenerative diseases.
|
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- HY-149439
-
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- HY-145584
-
|
JPI-547/OCN-201
|
PARP
|
Neurological Disease
Cardiovascular Disease
|
|
Nesuparib is a potent inhibitor of PARP. Nesuparib is useful for the research of neuropathic pain, neurodegenerative disease, and cardiovascular disease (extracted from patent WO2016200101A2).
|
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- HY-147578
-
|
|
TAM Receptor
|
Cancer
Infection
Inflammation/Immunology
|
|
Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals.
|
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- HY-150018
-
|
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mAChR
|
Neurological Disease
|
|
N-Demethyl MK-6884 (compound 34) is a potent M4 mAChR allosteric modulator. N-Demethyl MK-6884 can be used in the studies of alzheimer's disease and other diseases mediated by the M4 mAChR.
|
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- HY-P5852
-
|
Alpha-conotoxin EIIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin EIIB (Alpha-conotoxin EIIB) is a toxin peptide that can be obtained from Conus ermineus. α-Conotoxin EIIB binds to nAChR (Ki=2.2 nM). α-Conotoxin EIIB can be used in the study of neurological diseases such as schizophrenia, drug addiction, Alzheimer's disease, and Parkinson's disease.
|
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- HY-90009B
-
-
- HY-113639
-
|
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Proteasome
|
Neurological Disease
|
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A-933548 is a potent and selective inhibitor of calpain, with a Ki of 18 nM. A-933548 can be used for the research of Alzheimer's disease.
|
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- HY-48869
-
-
- HY-15976
-
|
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Others
|
Neurological Disease
|
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P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease.
|
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- HY-119378
-
|
CX 295
|
Apoptosis
Proteasome
|
Neurological Disease
|
|
AK 295 (CX 295) is a calpain inhibitor that inhibits apoptosis through a calpain-dependent pathway. AK 295 improves neurological function in a rat model of spinal cord injury (SCI). AK 295 can be used in the study of neurodegenerative diseases, such as bulbar amyotrophy, stroke, Alzheimer's disease, Parkinson's disease, multiple sclerosis.
|
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- HY-121340
-
|
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Others
|
Neurological Disease
|
|
Emylcamate is a potent muscle relaxant. Emylcamate has the potential for the research of neurological diseases.
|
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- HY-144399
-
|
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Others
|
Neurological Disease
|
|
CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 has the potential for the research of neurodegenerative disease including Alzheimer's disease.
|
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- HY-144399A
-
|
|
Others
|
Neurological Disease
|
|
CD33 splicing modulator 1 (Compound 1) hydrochloride is a CD33 splicing modulator. CD33/Siglec 3 is a myeloid lineage cell surface receptor that is known to regulate microglia activity. CD33 splicing modulator 1 hydrochloride increases exon 2 skipping in cellular mRNA pools. CD33 splicing modulator 1 hydrochloride has the potential for the research of neurodegenerative disease including Alzheimer's disease.
|
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- HY-B1680
-
-
- HY-103499
-
|
|
Others
|
Neurological Disease
|
ZK 93426 (hydrochloride) is a benzodiazepine antagonist. ZK 93426 (hydrochloride) can be used for the research of neurological disease.
|
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- HY-135601
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
Cinacalcet metabolite M4 is a metabolite of Cinacalcet. Cinacalcet is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease.
|
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- HY-P5007
-
|
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Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
Copeptin (human) is a diagnostic and prognostic biomarker for cardiovascular disease (CVD). Copeptin (human) is also the carboxyl terminus of the arginine vasopressin (AVP) precursor peptide. Copeptin (human) can be used in the study of cardiovascular disease.
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- HY-144682
-
|
|
Others
|
Neurological Disease
|
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O-GlcNAcase-IN-4 is a O-GlcNAcase inhibitor extracted from patent WO2018140299A1 Formulaic Ic. O-GlcNAcase-IN-4 can be used for the research of neurodegenerative diseases and disorders, such as Alzheimer's disease.
|
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- HY-105545
-
|
(+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide
|
mAChR
|
Neurological Disease
|
|
Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinity muscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease.
|
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- HY-N2916
-
|
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Glutaminase
|
Neurological Disease
|
|
Barbinervic acid is a glutaminase inhibitor with an IC50 of 14 μM. Barbinervic acid can be used for the study of neurodegenerative diseases.
|
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- HY-154798
-
|
|
iGluR
|
Neurological Disease
|
|
AMPA receptor modulator-5 (Example 217) is an AMPA receptor modulator. AMPA receptor modulator-5 can be used for research of neurological disease.
|
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- HY-115919
-
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- HY-123176
-
|
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Others
|
Neurological Disease
|
|
GYKI-13380 is an appetite suppressant. GYKI-13380 has the potential for the research of neurology diseases.
|
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- HY-156771
-
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- HY-100411
-
MLi-2
4 Publications Verification
|
LRRK2
|
Neurological Disease
|
|
MLi-2 is an orally active and highly selective LRRK2 inhibitor with an IC50 of 0.76 nM. MLi-2 has the potential for Parkinson’s disease.
|
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- HY-147233
-
|
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Sirtuin
|
Neurological Disease
|
|
MIND4-19 is a potent SIRT2 inhibitor with an IC50 value of 7.0 μM. MIND4-19 can be used for researching Huntington's disease.
|
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- HY-P1362A
-
|
Amyloid β Peptide (42-1)(human) TFA
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (42-1), human TFA is the inactive form of Amyloid β Peptide (1-42). β-Amyloid (42-1), human TFA is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
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- HY-147296
-
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- HY-121949
-
|
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Others
|
Neurological Disease
|
|
U-0521 is the inhibitor of the catechol-O-methyltransferase (COMT). U-0521 has the potential for the research of Parkinson's disease.
|
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- HY-B1786A
-
|
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
(E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease.
|
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- HY-147134
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 10 (compound 14a) is a highly potent GSK-3β inhibitor with an IC50 value of 80.5 nM. GSK-3β inhibitor 10 can be used for researching Alzheimer’s disease.
|
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- HY-144776
-
|
|
NAMPT
|
Neurological Disease
Cancer
|
|
NAT is an initial hit of NAMPT activator. NAMPT is the rate-limiting enzyme in the NAD salvage pathway, which makes it an attractive target for the research of many diseases associated with NAD exhaustion such as neurodegenerative diseases.
|
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- HY-113969
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer's disease and Parkinson's disease.
|
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- HY-144764
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT1A antagonist 1 (compound 6f) is a potent and selective antagonist of 5-HT1A receptor, with a Ki of 35 nM. 5-HT1A antagonist 1 can be used for the research of CNS diseases.
|
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- HY-153569
-
|
|
ROCK
|
Others
|
|
ROCK-IN-7 (compound 9) is a ROCK kinase inhibitor. ROCK-IN-7 can be used for research in ocular diseases (such as glaucoma and retinal diseases).
|
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- HY-132821A
-
|
E2027 maleate
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Irsenontrine (E2027) maleate is an orally active and selective phosphodiesterase 9 (PDE9) inhibitor. Irsenontrine maleate can be used for the research of neurological diseases.
|
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- HY-19490A
-
|
(S)-AQW-051
|
nAChR
|
Neurological Disease
|
|
(S)-VQW-765 ((S)-AQW-051) is an orally active, selective and effective α7 nicotinic ACh receptor (nAChR) partial agonist. (S)-VQW-765 has potential applications in cognitive disorders related to neurological diseases, such as Alzheimer's disease or schizophrenia.
|
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- HY-B0484A
-
|
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Others
|
Cardiovascular Disease
|
|
Buflomedil is an orally active vasoactive agent. Buflomedil is an α1-, α2-adrenolytic compound. Buflomedil can be used for research of cardiovascular disease, such as peripheral vascular disease.
|
-
- HY-153815
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 11 (compound 3) is an agonist of GLP Receptor. GLP-1 receptor agonist 11 can be used in the study of diseases such as diabetes and non-alc. fatty liver disease.
|
-
- HY-132821
-
-
- HY-147576
-
|
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
|
Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC50 of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
|
-
- HY-147577
-
|
|
TAM Receptor
|
Cancer
Inflammation/Immunology
|
|
Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals.
|
-
- HY-147976
-
|
|
Glucosidase
|
Metabolic Disease
Neurological Disease
|
|
Glucocerebrosidase-IN-1 (compound 11a) is a potent and selective GCase (glucocerebrosidase) inhibitor, with an IC50 of 29.3 μM and a Ki of 18.5 μM. Glucocerebrosidase-IN-1 can be used for the research of Gaucher disease (GD) and Parkinson’s disease (PD).
|
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- HY-110019A
-
|
cis-Lu 19-005
|
Others
|
Neurological Disease
|
|
cis-Indatraline (cis-Lu 19-005) hydrochloride is an active compound. cis-Indatraline (cis-Lu 19-005) hydrochloride can be used for the research of neurodegenerative diseases.
|
-
- HY-149888
-
-
- HY-152111
-
-
- HY-148108
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-27 (compound 8c) is an AChE inhibitor (IC50=0.19 µM). AChE-IN-27 can be used in studies of neurological diseases such as alzheimer's disease, dementia, ataxia and myasthenia gravis.
|
-
- HY-122908
-
|
AZD5718
|
FLAP
|
Cardiovascular Disease
|
|
Atuliflapon (AZD5718) is an orally active inhibitor of FLAP (5‑Lipoxygenase activating protein), with an IC50 of 2 nM. Atuliflapon is used in the study for coronary artery disease.
|
-
- HY-N7745
-
|
Glucopsychosine; Lyso-Gb1
|
Others
|
Metabolic Disease
|
|
Glucosylsphingosine (lyso-Gb1) is a deacylated form of glucosylceramide and is also degraded by the glucocerebrosidase. Glucosylsphingosine is a very promising, reliable and specific biomarker for monitoring Gaucher disease.
|
-
- HY-109507
-
|
Ceredase
|
Others
|
Metabolic Disease
|
|
Alglucerase (Ceredase) is a modified form of human placental glucocerebrosidase used as enzyme in the research of glucocerebrosidase deficiency, such as Gaucher's disease.
|
-
- HY-W040146
-
|
Propiopromazine hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease.
|
-
- HY-145317
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-2 (compoubd 22) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of <0.6 nM. LRRK2-IN-2 can be used for the research of Parkinson's disease.
|
-
- HY-103424
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 dihydrochloride is a selective dopamine D4 receptor agonist. A-412997 dihydrochloride improves cognitive performance in rats and can be used in the research of psychiatric diseases.
|
-
- HY-147976A
-
|
|
Glucosidase
|
Neurological Disease
|
|
Glucocerebrosidase-IN-1 (compound 11a) hydrochloride is a potent and selective GCase (glucocerebrosidase) inhibitor, with an IC50 of 29.3 μM and a Ki of 18.5 μM. Glucocerebrosidase-IN-1 hydrochloride can be used for the research of Gaucher disease (GD) and Parkinson’s disease (PD).
|
-
- HY-146068
-
|
|
Others
|
Neurological Disease
|
|
AEP-IN-1 (Compound 13e) is a CNS agent-like non-covalent inhibitor of asparagine endopeptidase (AEP), with the IC50 of 89 nM. AEP-IN-1 can be used for the research of numerous neurological diseases such as Alzheimer’s disease (AD).
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-
- HY-153595
-
|
|
Others
|
Cardiovascular Disease
|
DAPK-IN-2 is a DAPK inhibitor. DAPK-IN-2 can be used for the research of cerebral infarction and ischemic diseases.
|
-
- HY-146456
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
A1AR antagonist 3 (compound 13) is a selective adenosine 1 (A1) receptor antagonist with Kis of 9.69 nM and 0.529 nM for human A1 and rat A1, respectively. A1AR antagonist 3 can be used for researching neurological diseases.
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-
- HY-120644
-
|
|
Others
|
Cardiovascular Disease
|
|
BMS-919373 is a selective, potent IKur current blocker. BMS-919373 can be used for the research of cardiovascular diseases.
|
-
- HY-101321
-
-
- HY-145318
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-3 (compoubd 24) is a potent, selective, orally active and brain-penetrant inhibitor LRRK2, with IC50 of 2.6 nM in human PBMCs. LRRK2-IN-3 can be used for the research of Parkinson's disease.
|
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
EGFR
|
Neurological Disease
|
|
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease.
|
-
- HY-105170B
-
|
|
nAChR
|
Neurological Disease
|
|
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease.
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-
- HY-129738
-
|
|
Others
|
Cardiovascular Disease
|
|
I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases.
|
-
- HY-13410
-
|
LY246708 oxalate
|
mAChR
|
Neurological Disease
|
|
Xanomeline oxalate (LY246708 oxalate) is a potent and selective muscarinic receptor agonist (SMRA) and stimulates phosphoinositide hydrolysis in vivo. Xanomeline oxalate can be used for the research of Alzheimer’s disease.
|
-
- HY-107660
-
|
|
Sirtuin
|
Neurological Disease
|
|
SIRT2-IN-8 is a potent SIRT2 inhibitor. SIRT2-IN-8 can be used for Huntington’s and Parkinson’s diseases research.
|
-
- HY-P3909
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Biotinyl-Ahx-Amyloid β-Protein (1-42) ammonium is a N-terminally biotin-labeled Amyloid β-Protein (1-42). Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease.
|
-
- HY-151536
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
meso-Benzothiazole-BODIPY 505/515 is a boron dipyrromethenes (BODIPY) -based fluorescent probediseases, lysosomal storage diseases and neural degeneration diseases.
|
-
- HY-109514
-
|
|
Others
|
Metabolic Disease
|
|
Imiglucerase (Cerezyme) is a recombinant human glucocerebrosidase, ameliorates systemic manifestations such as hepatosplenomegaly, anemia, thrombocytopenia and skeletal abnormalities in patients with type 1 (non-neuronopathic) and type 3 (chronic neuronopathic) Gaucher's disease.
|
-
- HY-153688
-
|
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Neurotensin Receptor
|
Neurological Disease
|
|
SORT-PGRN interaction inhibitor 3 (Compound 13) is a SORT-PGRN interaction inhibitor (IC50: 0.17 μM). SORT-PGRN interaction inhibitor 3 can be used for research of neurodegenerative diseases.
|
-
- HY-W015514
-
|
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Others
|
Neurological Disease
|
|
N-(3-Aminopropyl)cyclohexylamine, a cyclohexylamine derivative, acts as a selective and competitive inhibitor of spermine synthase. N-(3-Aminopropyl)cyclohexylamine can be used for the research of neurological diseases.
|
-
- HY-101321A
-
|
|
Itk
|
Neurological Disease
|
|
Immepip dihydrobromide is a H3 agonist. Immepip dihydrobromide can reduce cortical histamine release. Immepip dihydrobromide can be used for the research of neurological diseases.
|
-
- HY-155830
-
-
- HY-P1060
-
|
|
Amyloid-β
|
Neurological Disease
|
|
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.
|
-
- HY-B1363
-
|
Bendrofluazide
|
Others
|
Cardiovascular Disease
|
|
Bendroflumethiazide is an orally active diuretic. Bendroflumethiazide is an antihypertensive agent. Bendroflumethiazide has the potential for the research of arterial hypertensive disease.
|
-
- HY-W062697
-
|
HTL0014242
|
mGluR
|
Neurological Disease
|
|
HTL14242 (HTL0014242) is an advanced and orally active mGlu5 NAM with a pKi and a pIC50 of 9.3 and 9.2, respectively. HTL14242 can be used for the research of parkinson’s disease.
|
-
- HY-128057
-
-
- HY-P4281
-
-
- HY-P5835
-
|
|
Potassium Channel
|
Neurological Disease
|
|
δ-Dendrotoxin is a K + channel blocker that can be obtained from the venom of the black mamba snake. δ-Dendrotoxin can be used in the study of neurological diseases.
|
-
- HY-156662
-
|
|
Casein Kinase
|
Metabolic Disease
|
|
Casein kinase 1δ-IN-7 (compound 497) is a Casein kinase 1δ inhibitor. Casein kinase 1δ-IN-7 can be used in the study of neurodegenerative disorders such as Alzheimer's disease.
|
-
- HY-P1060A
-
|
|
Amyloid-β
|
Neurological Disease
|
|
LPYFD-NH2 TFA, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 TFA can be used for the research of Alzheimer’s disease.
|
-
- HY-153878
-
|
|
Others
|
Neurological Disease
|
|
BCAT-IN-4 (Compound 1) is a BCAT inhibitor. BCAT-IN-4 exhibits a moderate ability to inhibit hBCATc with IC50 value of 2.35 μM. BCAT-IN-4 can be used for the research of neurodegenerative diseases.
|
-
- HY-145905
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-1 is a potent and selective D4R antagonist with an IC50 of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease.
|
-
- HY-117184
-
-
- HY-144762
-
-
- HY-105445
-
-
- HY-132821B
-
|
(R)-E2027
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine (HY-132821), is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC50 value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases.
|
-
- HY-153766
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
PDE5-IN-9 (Compound 59) is a PDE5 inhibitor (IC50: 11.2 μM). PDE5-IN-9 shows interaction with Gln 817, Tyr 612, and Ala 767 amino acid residues. PDE5-IN-9 can be used for research of cardiovascular disease.
|
-
- HY-144681
-
|
|
Tau Protein
|
Neurological Disease
|
|
LY3372689 (Formulaic Ia) is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.
|
-
- HY-14936
-
|
MCC-977
|
Thrombin
|
Cardiovascular Disease
|
|
Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease.
|
-
- HY-B0590
-
|
Ro 1-9569
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
|
-
- HY-B0590E
-
|
Ro 1-9569 mesylate
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease.
|
-
- HY-P4308
-
|
|
Prolyl Endopeptidase (PREP)
|
Neurological Disease
|
|
Z-Pro-Pro-aldehyde-dimethyl acetal is a potent inhibitor of prolyl endopeptidase (PREP), a cytoplasmic serine endoprotease (IC50= 12 nM). Z-Pro-Pro-aldehyde-dimethyl acetal plays an important role in cognitive dysfunction in aging and neurodegenerative diseases including Alzheimer's disease.
|
-
- HY-14838
-
|
BIA 5-453
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
|
-
- HY-N2195
-
|
(+)-Nootkatone
|
Others
|
Neurological Disease
|
|
Nootkatone, a neuroprotective agent from Vitis vinifera, has antioxidant and anti-inflammatory effects. Nootkatone improves cognitive impairment in lipopolysaccharide-induced mouse model of Alzheimer's disease.
|
-
- HY-14838A
-
|
BIA 5-453 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM. Etamicastat can be used in the research of cardiovascular diseases.
|
-
- HY-132582
-
|
BIIB080; ISIS 814907
|
Tau Protein
|
Neurological Disease
|
|
IONIS-MAPTRx (BIIB080) is the first Tau-lowering antisense oligonucleotide (ASO). IONIS-MAPTRx has the potential for the research of Alzheimer Disease.
|
-
- HY-156677
-
|
|
METTL3
|
Cancer
|
|
STC-15 (example 70) is an orally active METTL3 inhibitor used in the study of proliferative diseases such as cancer and autoimmune diseases.
|
-
- HY-128442
-
|
Phenyl hydrogen sulfate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phenyl sulfate is an orally active gut microbiota-derived metabolite. Phenyl sulfate induces albuminuria and podocyte damage in experimental models of diabetes. Phenyl sulfate can be used as a disease marker and future therapeutic target in diabetic kidney disease.
|
-
- HY-146478
-
|
|
Adenosine Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A1/A3 AR antagonist 1 (compound 10) is a potent adenosine 1 (A1) and adenosine 3 (A3) receptor dual antagonist with Kis of 36.7 nM, 25.4 nM and 1.47 nM for human A1, human A3 and rat A1, respectively. A1/A3 AR antagonist 1 can be used for researching kidney failure, inflammatory pulmonary diseases, and Alzheimer’s disease.
|
-
- HY-137447A
-
|
IRL752 fumarate
|
Others
|
Neurological Disease
|
|
Pirepemat (IRL752) fumarate is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat fumarate is used for the study of Parkinson's disease.
|
-
- HY-148382
-
-
- HY-W027553
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine is a pharmaceutically active compound which is a nootropic agent that acts as cholinesterase inhibitor and is used in research of Alzheimer disease.
|
-
- HY-112071
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Prenalterol is a selective β1-adrenergic receptor agonist. Prenalterol has no effect on gut smooth muscle contractile activity. Prenalterol can be used for researching cardiovascular disease.
|
-
- HY-P99163
-
|
ABBV-8E12; C2N-8E12
|
Microtubule/Tubulin
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanised anti-tau antibody that binds amino acids 25-30 near the N-terminal end of the tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates and reduces brain atrophy. Tilavonemab can be used in the study of Alzheimer's disease.
|
-
- HY-148187
-
|
|
NOD-like Receptor (NLR)
|
Infection
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
NLRP3-IN-11 is a NLR family pyrin domain containing 3 (NLRP3) proteins inhibitor. NLRP3-IN-11 has biological activity for NLRP3 with an IC50 value of <0.3 μM. NLRP3-IN-11 can be used for the researh of inflammatory and degenerative diseases including NASH, atherosclerosis and other cardiovascular diseases, Alzheimer's disease, Parkinson's disease, diabetes, gout, and numerous other autoinflammatory diseases.
|
-
- HY-153092
-
|
BI-685509
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
Avenciguat (BI-685509) is a potent and orally active sGC activator. Avenciguat restores cyclic guanosine monophosphate (cGMP) and improves functionality of nitric oxide (NO) pathways. Avenciguat can be used in research of chronic kidney disease (CKD) and diabetic kidney disease (DKD).
|
-
- HY-148650
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease.
|
-
- HY-119943
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
|
-
- HY-17387
-
|
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-151522
-
|
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT2-IN-10 (Compound 12) is a potent SIRT2 inhibitor with an IC50 of 1.3 μM. SIRT2-IN-10 can be used for the research of cancer and neurodegenerative disease.
|
-
- HY-144753
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-2 (Compound 13b) is a potent inhibitor of AChE/BChE (AChE IC50 = 0.96 ± 0.14 µM, BChE IC50 = 1.23 ± 0.23 µM). AChE/BChE-IN-2 has the potential for the research of AD diseases.
|
-
- HY-147846
-
-
- HY-137447
-
|
IRL752
|
Others
|
Neurological Disease
|
|
Pirepemat (IRL752) is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat (IRL752) is used for the study of Parkinson's disease.
|
-
- HY-136311
-
|
|
Others
|
Neurological Disease
|
|
NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease.
|
-
- HY-113303
-
|
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
FAPy-adenine is an oxidized DNA base. Fapy-adenine shows an increased trend levels in the Alzheimer's disease brain. Oxidized nucleosides are biochemical markers for tumors, aging, and neurodegenerative diseases.
|
-
- HY-153279
-
-
- HY-151616
-
|
|
Epoxide Hydrolase
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
|
sEH inhibitor-10 (Compound 37) is a selective soluble epoxide hydrolase (sEH) inhibitor (IC50=0.5 μM). sEH inhibitor-10 maintains high cycloeicosatrienoic acid (EETs) levels by inhibiting sEH, thereby reducing inflammation, regulating endothelial tone, improving mitochondrial function, and reducing oxidative stress. sEH inhibitor-10 has good research potential in metabolic, renal and cardiovascular diseases.
|
-
- HY-112266
-
|
|
AMPK
|
Neurological Disease
|
|
MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease.
|
-
- HY-149285
-
|
|
HDAC
|
Neurological Disease
|
|
NT160 is a highly potent class-IIa HDAC inhibitor with an IC50 value of 0.046 μM. NT160 can be used for the research of central nervous system diseases.
|
-
- HY-151370
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-26 (compound 4a) is an AChE (acetylcholinesterase) inhibitor with an IC50 value of 0.42 μM. AChE-IN-26 can be used for the research of Alzheimer’s disease.
|
-
- HY-107922
-
|
Isothazine hydrochloride; Lysivane hydrochloride; Parsidol hydrochloride
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ethopropazine (Isothazine) hydrochloride is a potent, selective BChE inhibitor and a poor AChE inhibitor. Ethopropazine hydrochloride is a phenothiazine compound with anticholinergic properties. Ethopropazine hydrochloride can be used for the research of Parkinson’s disease.
|
-
- HY-N8728
-
-
- HY-156429
-
|
|
LRRK2
|
Neurological Disease
|
|
MK-1468 is a high selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 0.8 nM. MK-1468 can be used in study Parkinson’s disease.
|
-
- HY-136733
-
|
Ac-Asp-Asn-Leu-Asp-CHO
|
Caspase
|
Infection
Neurological Disease
|
|
Ac-DNLD-CHO (Ac-Asp-Asn-Leu-Asp-CHO) is a Caspase-3/7 inhibitor (IC50: 9.89, 245 nM respectively; Ki app: 0.68, 55.7 nM respectively). Ac-DNLD-CHO can be used for research of caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases.
|
-
- HY-11070
-
-
- HY-106432A
-
|
SB-202026 hydrochloride; Memric hydrochloride
|
mAChR
|
Neurological Disease
|
|
Sabcomeline (SB-202026) hydrochloride is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline hydrochloride can be used for Alzheimer's disease research.
|
-
- HY-106432
-
|
SB-202026; Memric
|
mAChR
|
Neurological Disease
|
|
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research.
|
-
- HY-156358
-
-
- HY-143329
-
-
- HY-128477
-
|
Autophagy enhancer-67 inner salt
|
Autophagy
|
Neurological Disease
|
|
AUTEN-67 (inner salt), the inner salt form of AUTEN-67 (HY-117924), is an orally active autophagy-enhancing agent and MTMR14 inhibitor with potent antiaging and neuroprotective effects. AUTEN-67 (inner salt) hampers the progression of neurodegenerative symptoms in a drosophila model of Huntington's disease.
|
-
- HY-103283
-
|
GRP(18-27) (porcine)
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Neuromedin C porcine (GRP, 18-27, porcine) is a bombesin-like neuropeptide that can be obtained from porcine spinal cord. Neuromedin C porcine exhibits a potent contractile activity on rat uterus in the characteristic manner of bombesin. Neuromedin C porcine has research potential for neurological-related diseases.
|
-
- HY-142698
-
|
|
Others
|
Cardiovascular Disease
|
|
SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031).
|
-
- HY-B1084
-
|
|
Others
|
Others
|
|
Cinoctramide is an intermediate of pharmaceutical synthesis. Cinoctramide can be used for the research of autoimmune diseases.
|
-
- HY-B0203A
-
|
R 065824 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
|
-
- HY-B0203
-
|
R 065824
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
|
-
- HY-156180
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
DDC 3′-O-β-D glucuronide (compound 5) is a drug metabolite that can prevent the fibrillization and oligomerization of Aβ42. DDC 3′-O-β-D glucuronide has potential for the research of Alzheimer's disease.
|
-
- HY-151338
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-25 is a potent, selective and uncompetitive acetylcholinesterase (AChE) inhibitor (IC50=2.95 µM). AChE-IN-25 can be used in Alzheimer's disease research.
|
-
- HY-103162
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease.
|
-
- HY-156955
-
-
- HY-105647
-
|
Bufylline
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Ambuphylline (Bufylline) is a bronchodilator. Ambuphylline is a theophylline derivative possibly acting through phosphodiesterase inhibition. Ambuphylline can be used for the research of asthma and other lung diseases.
|
-
- HY-103405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
NGD94-1 is a specific dopamine D4 receptor antagonist. NGD94-1 can effectively reverse Phencyclidine-induced cognitive impairment in marmosets. NGD94-1 can be used in the study of psychiatric diseases.
|
-
- HY-125036
-
|
|
Others
|
Neurological Disease
|
|
MitoBloCK-11 is a new small molecule with a protein-binding target, Seo1. MitoBloCK-11 plays an important role in the delivery of PINK1 pathway. MitoBloCK-11 can be used in the study of autosomal recessive Parkinson's disease.
|
-
- HY-145888
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease.
|
-
- HY-N12075
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Dehydrodiscretamine chloride is a dual inhibitor of AChE and BChE with IC50s of 17.8 and 118.8 μM, respectively. Dehydrodiscretamine chloride has antioxidant activity. Dehydrodiscretamine chloride can be used in study Alzheimer’s disease.
|
-
- HY-P5856
-
|
|
nAChR
|
Neurological Disease
|
|
αA-Conotoxin PIVA is a selective mouse musclenAChR inhibitor with IC50 for adult and fetal mouse musclenAChR sub> values are 2.3 nM and 22 nM respectively. αA-Conotoxin PIVA can be used in the study of neurological diseases.
|
-
- HY-147574
-
|
|
TAM Receptor
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease.
|
-
- HY-119943A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease.
|
-
- HY-105003
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ST 1535 is a potent and orally active A2A adenosine receptor antagonist. ST 1535 shows antiparkinsonian activity and antitremorigenic effects. ST 1535 has the potential for the research of Parkinson’s disease.
|
-
- HY-100938
-
|
1-(3-Chlorophenyl)biguanide hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT3 agonist. m-CPBG hydrochloride can be used for the research of neurological disease.
|
-
- HY-157089
-
-
- HY-122495
-
|
rel-LY 141865 dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
rel-Quinpirole (rel-LY 141865) dihydrochloride, an ergot compound, is a selective dopamine (DA) D2 receptor agonist. rel-Quinpirole dihydrochloride can be used for research on neurological diseases.
|
-
- HY-116418
-
|
|
Endogenous Metabolite
Cannabinoid Receptor
|
Neurological Disease
|
|
Virodhamine is an endocannabinoid, it regulates neurotransmission by activating the cannabinoid (CB) receptors. Virodhamine is an antagonist of CB1 receptor and an agonist of CB2 receptor. Virodhamine induces megakaryocytic differentiation by triggering MAPK signaling and ROS production. Virodhamine can be used for the research of various neurological disorders such as Alzheimer's and Parkinson's diseases.
|
-
- HY-13720
-
|
LY127809 free base
|
Dopamine Receptor
|
Neurological Disease
|
|
Pergolide (LY127809 (free base)) is an ergot-derived orally active dopamine receptor agonist. Pergolide can be used for Parkinson disease research.
|
-
- HY-155628
-
|
|
iGluR
|
Others
|
|
AMPA receptor modulator-6 is an AMPA receptor positive allosteric modulator (PAM). AMPA receptor modulator-6 can be used in the study of neurological diseases.
|
-
- HY-107525
-
|
|
EAAT
|
Neurological Disease
|
|
(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases.
|
-
- HY-116868
-
|
Anecortave
|
PAI-1
|
Cardiovascular Disease
|
|
Anecortave acetate is a potent ocular angiostatic agent. Anecortave acetate inhibits neovascularization which is induced by many different angiogenic factors, and increases plasminogen activator inhibitor-1 (PAI-1) mRNA expression. Anecortave acetate can be used to research ocular neovascular diseases.
|
-
- HY-16748
-
|
ABT-126
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-P99452
-
|
SNDX-6352
|
c-Fms
|
Cancer
Inflammation/Immunology
|
|
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases.
|
-
- HY-148215
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-17 (Example 5) is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases.
|
-
- HY-148215A
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases.
|
-
- HY-117259
-
|
ALZ-801
|
Amyloid-β
|
Neurological Disease
|
|
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
|
-
- HY-P5845
-
|
α-RgIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin RgIA (α-RgIA) is a specific α9α10 nAChR antagonist. α-Conotoxin RgIA can be obtained from Conus regius venom. α-Conotoxin RgIA can be used in the study of neurological diseases.
|
-
- HY-P5864
-
|
|
Sodium Channel
|
Neurological Disease
|
|
μ-Conotoxin BuIIIA (Mu-Conotoxin BuIIIA) is a voltage-gated sodium channel (VGSC) blocker. μ-Conotoxin BuIIIA is a toxic peptide that can be obtained from the venom of Cone snails. μ-Conotoxin BuIIIA can be used in the study of neurological diseases.
|
-
- HY-151810
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases.
|
-
- HY-151809
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases.
|
-
- HY-123059
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
(Rac)-ICI-118551 hydrochloride is a selective β2-adrenergic receptor antagonist. (Rac)-ICI-118551 hydrochloride can inhibit dendrite ramification of hippocampal neurons in a mouse model of Alzheimer's disease.
|
-
- HY-100642
-
|
Ro 40-7591
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease.
|
-
- HY-126967A
-
|
1-P-GPA
|
Others
|
Metabolic Disease
|
|
1-Palmitoyl-sn-glycerol 3-phosphate (1-P-GPA) is an endogenous metabolite. 1-Palmitoyl-sn-glycerol 3-phosphate can be used for the research of non‐alcoholic fatty liver disease.
|
-
- HY-106000
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
GSK239512 is a potent and brain penetrated H3 receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD).
|
-
- HY-P99164
-
|
LY33003560
|
Microtubule/Tubulin
|
Neurological Disease
|
|
Zagotenemab (LY3303560) is a humanised anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research.
|
-
- HY-16748A
-
|
ABT-126 citrate
|
nAChR
|
Neurological Disease
|
|
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with high affinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease.
|
-
- HY-156550
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC50 value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases.
|
-
- HY-143465
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-5 is a potent and selective BChE inhibitor of hBChE over hAChE with an IC50 of 2.8 nM for BChE. BChE-IN-5 has the potential for the research of alzheimer’s disease.
|
-
- HY-146387
-
|
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-146155
-
|
|
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
TRPC4/5-IN-1 is a potent TRP channel 4/5 (TRPC4/5) inhibitor with IC50s of 2.06 μM and 0.54 μM, respectively. TRPC4/5-IN-1 can be used for proteinuric kidney diseases and skin inflammatory diseases research.
|
-
- HY-16759
-
|
MK-8931
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-156102
-
|
|
Bcr-Abl
|
Neurological Disease
|
|
c-ABL-IN-5 is a selective c-Abl inhibitor with neuroprotective effects. c-ABL-IN-5 has blood-brain barrier penetrability, metabolic stability and good pharmacokinetic properties. When c-ABL-IN-5 is labeled with [18F] (compound [18F]3), it can be used as a tracer to evaluate disease-modifying efficacy by complementary positron emission tomography (PET). c-ABL-IN-5 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD).
|
-
- HY-N10408
-
|
|
Apoptosis
Autophagy
|
Cancer
Neurological Disease
|
|
Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease.
|
-
- HY-107509
-
|
|
mGluR
|
Neurological Disease
|
|
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease.
|
-
- HY-149242
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease.
|
-
- HY-107524
-
|
|
EAAT
|
Neurological Disease
|
|
(±)-HIP-B is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-B is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-B can be used in the study of neurological diseases.
|
-
- HY-W083062
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases.
|
-
- HY-B0702
-
|
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Nicergoline, an ergoline derivative ester of bromonicotinic acid, is a potent, selective and orally active antagonist of α1A-adrenoceptor. Nicergoline has vasodilator effects. Nicergoline also has ameliorative effects on cognitive function in mouse models of Alzheimer's disease.
|
-
- HY-147608
-
|
|
c-Fms
|
Neurological Disease
|
|
CSF1R-IN-7 (Formula I) is a CSF-1R inhibitor. CSF1R-IN-7 can be used for Alzheimer’s disease research.
|
-
- HY-148253
-
|
|
RIP kinase
|
Inflammation/Immunology
Neurological Disease
|
|
TP-030-1 is an inhibitor of RIPK1. TP-030-1 inhibits hRIPK1 with a Ki value of 3.9 nM and inhibits mRIPK1 with an IC50 value of 4.2 μM. TP-030-1 can be used for the research of inflammatory diseases and neurodegenerative diseases.
|
-
- HY-149490
-
|
|
PKC
|
Neurological Disease
|
|
AJH-836 is an activator of Munc13-1 and PKC ε/α (Kd: 4.5 nM for PKCα) . AJH-836 triggers the translocation of Munc13-1 from the cytoplasm to the plasma membrane. AJH-836 can be used for research of neurodegenerative diseases.
|
-
- HY-125095
-
|
Tunodafil hydrochloride
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cardiovascular Disease
|
|
Yonkenafil (Tunodafil) hydrochloride, a novel phosphodiesterase 5 (PDE5) inhibitor, is effective in reducing cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area. Yonkenafil (Tunodafil) hydrochloride may improve cognitive function by modulating neurogenesis and has a potential therapeutic effect on Alzheimer's disease.
|
-
- HY-124063
-
-
- HY-16759A
-
|
MK-8931 TFA
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-147953
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease.
|
-
- HY-156031
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-19 (Compound 7b) is a para-substituted derivative of indone (7b) with inhibitory activity of butyryl cholinesterase (BChE) (IC50=0.04 μM). BChE-IN-19 improves cholinergic scheduling in the nervous system. BChE-IN-19 can be used against Alzheimer's disease.
|
-
- HY-14679
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK3β inhibitor II is an inhibitor of GSK3β. GSK3β inhibitor II can be used for research of Alzheimer’s disease (AD).
|
-
- HY-146386
-
|
|
Sirtuin
|
Cancer
Neurological Disease
|
|
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases.
|
-
- HY-16482
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD).
|
-
- HY-U00058
-
-
- HY-133712
-
|
Tunodafil
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Yonkenafil (Tunodafil), a novel phosphodiesterase 5 (PDE5) inhibitor, is effective in reducing cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area. Yonkenafil may improve cognitive function by modulating neurogenesis and has a potential therapeutic effect on Alzheimer's disease.
|
-
- HY-P3859
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Cys-Gly-Lys-Arg-Amyloid β-Protein (1-42) is a peptide fragment of amyloid β-protein (Aβ). Cys-Gly-Lys-Arg-Amyloid β-Protein (1-42) can be used in research of Alzheimer's disease.
|
-
- HY-144826
-
|
|
GSK-3
|
Neurological Disease
|
|
ZDWX-25 is a highly potent GSK-3β and DYRK1A dual inhibitor with an IC50 value of 71 nM for GSK-3β. ZDWX-25 possesses significant cytotoxic activities against SH-SY5Y and HL-7702 cells. ZDWX-25 can be used for researching alzheimer's disease.
|
-
- HY-P1061
-
|
|
STAT
Amyloid-β
|
Neurological Disease
|
|
Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
|
-
- HY-P99491
-
|
AVTX-007; CERC-007; MEDI 2338
|
Interleukin Related
|
Inflammation/Immunology
|
|
Camoteskimab (AVTX-007) is a fully human, high-affinity anti-IL-18 monoclonal antibody. Camoteskimab has the potential for the autoinflammatory diseases research, including adult-onset Still’s disease (AOSD).
|
-
- HY-P4895
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
(d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist. (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin can be used for the research of neurological disease.
|
-
- HY-P5863
-
|
Mamb-2
|
Sodium Channel
|
Neurological Disease
|
|
Mambalgin-2 (Mamb-2) is an acid-sensitive ion channels (ASICs) inhibitor and a venom peptide. Mambalgin-2 can be obtained from the venom of the African black mamba. Mambalgin-2 can be used in the study of pain and neurological diseases.
|
-
- HY-B0757A
-
|
Vitamin E Nicotinate
|
Reactive Oxygen Species
Endogenous Metabolite
|
Cardiovascular Disease
|
|
(±)-α-Tocopherol nicotinate, vitamin E - nicotinate, is an orally active fat-soluble antioxidant that prevents lipid peroxidation in cell membranes. (±)-α-Tocopherol nicotinate is hydrolysed in the blood to α -tocopherol and niacin and may be used in studies of related vascular diseases.
|
-
- HY-110135
-
|
|
IGF-1R
|
Others
|
|
NBI-31772 is the potent and nonselective inhibitor of IGFBP with a Ki value of 47 nM. NBI-31772 has the potential for the research of IGF-responsive diseases.
|
-
- HY-152264
-
|
|
CFTR
|
Inflammation/Immunology
|
|
CFTR activator 1 is a potent and selective CFTR activator, with an EC50 of 23 nM. CFTR activator 1 can be used to ameliorate dry eye disease.
|
-
- HY-107580
-
|
|
GPR109A
|
Cardiovascular Disease
Metabolic Disease
|
|
GPR109 receptor agonist-1 (Compound 3a) is a highly selective agonist of the human orphan G-protein-coupled receptor GPR109b, with the pEC50 of 6.4. GPR109 receptor agonist-1 can be used for the research of cardio-metabolic diseases.
|
-
- HY-103253
-
|
|
Others
|
Neurological Disease
|
|
LY231617 is a potent and blood-brain barrier penetrable antioxidant. LY231617 is a neuroprotective agent in brain, it can be used for the research of nervous disease.
|
-
- HY-N2043
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Huperzine B is a Lycopodium alkaloid isolated from Huperzia serrata and a highly selective acetylcholinesterase (AChE) inhibitor. Huperzine B can be uesd to can be used to improve Alzheimer's disease.
|
-
- HY-P1061A
-
|
|
STAT
Amyloid-β
Apoptosis
|
Neurological Disease
|
|
Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
|
-
- HY-N10151
-
|
|
Others
|
Cardiovascular Disease
|
|
Notoginsenoside R3 is an active principle components of P. notoginseng. Notoginsenoside R3 act as a signaling molecule that is associated with various physiological effects. P. notoginseng and its components are used as traditional Chinese medicine for cardiovascular disease.
|
-
- HY-N8453
-
|
Methyl 3,5-dicaffeoyl quinic acid
|
p38 MAPK
|
Neurological Disease
|
|
Macranthoin G is an inhibitor of p38 MAPK. Macranthoin G protects the cytotoxicity induced by Aβ or hydrogen peroxide in neuronal cells by downregulating p38 MAPK. Macranthoin G can used in study Alzheimer’s Disease.
|
-
- HY-P5841
-
|
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin LtIA is an α3β2 nAChR blocker (IC50=9.8 nM), that can be obtained from Conus litteratus venom. Alpha-Conotoxin LtIA can be used in the study of neurological diseases (such as Parkinson's disease, pain).
|
-
- HY-109150
-
|
IRL790
|
Dopamine Receptor
|
Neurological Disease
|
|
Mesdopetam (IRL790) is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease.
|
-
- HY-106392
-
|
NB-DGJ; N-(n-Butyl)deoxygalactonojirimycin
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
|
|
Lucerastat, the galactose form of Miglustat, is an orally-available inhibitor of glucosylceramide synthase (GCS). Lucerastat has the potential for Fabry disease study.
|
-
- HY-17020
-
-
- HY-130750
-
|
|
Reactive Oxygen Species
|
Neurological Disease
|
|
Phycocyanobilin, an orally active antioxidative agent, is an effective scavenger for various reactive oxygen species. Phycocyanobilin can be used for the research of Alzheimer’s disease.
|
-
- HY-P9930
-
|
AMG 145
|
Ser/Thr Protease
|
Metabolic Disease
Cancer
|
|
Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases.
|
-
- HY-154957
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-11 (Compound 9) is a brain-penetrant mTOR inhibitor (IC50: 21 nM for pS6). mTOR inhibitor-11 also inhibits pCHK1 and PDE4D with IC50s of 17.2 and 17.0 μM. mTOR inhibitor-11 can be used for research of CNS disease.
|
-
- HY-155058
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.3 channel inhibitor 1 (compound 15b) is a state-dependent voltage-gated sodium channel Nav1.3 inhibitor (IC50=20 nM). Nav1.3 channel inhibitor 1 can penetrate the blood-brain barrier and can be used in the research of nervous system diseases.
|
-
- HY-101207
-
|
|
GABA Receptor
|
Neurological Disease
|
|
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. NCS-382 has anticonvulsant and antisedative activity. NCS-382 is used in the related research of hereditary nervous system diseases.
|
-
- HY-101376
-
|
(+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an opioid receptor antagonist with Ki values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease.
|
-
- HY-143721
-
|
|
Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
|
SSAO inhibitor-2 (Compound 1) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 10-100 μM for human SSAO and MAO-A, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
|
-
- HY-17020A
-
-
- HY-146528
-
|
|
Others
|
Cancer
Neurological Disease
|
|
c-ABL-IN-3 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-3 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 50).
|
-
- HY-146530
-
|
|
Others
|
Cancer
Neurological Disease
|
|
c-ABL-IN-4 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-4 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2021048567A1, compound 54).
|
-
- HY-144108
-
|
|
HCV
|
Infection
|
|
HCV-IN-35 (Compound (R)-3h) is a potent inhibitor of HCV. HCV-IN-35 has the potential for the research infection diseases.
|
-
- HY-149605
-
|
|
Others
|
Metabolic Disease
|
|
KHK-IN-4 (compound 14) is a potent ketohexokinase (KHK) inhibitor. KHK-IN-4 can be used for fructose metabolic disease research.
|
-
- HY-101918
-
|
|
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-N6959
-
|
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
|
|
Osmundacetone is a natural product isolated from Osmundae Rhizoma, with neuroprotective and anti-apoptotic effects. Osmundacetone has DPPH scavenging activity and protects neurological cell from oxidative stress. Osmundacetone can be a potential agent for the research of neurodegenerative diseases.
|
-
- HY-109150A
-
|
IRL790 hemitartrate
|
Dopamine Receptor
|
Neurological Disease
|
|
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease.
|
-
- HY-10979
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
AN0128 is a boron-containing antibacterial and anti-inflammatory agent. AN0128 against S. aureus, S. epidermidis, P. acnes, B. subtilis with minimum inhibitory concentration (MIC) values of 1, 0.5, 0.3, 1 μg/mL. AN0128 can be used for the research of periodontal disease and cutaneous diseases.
|
-
- HY-136866
-
|
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-2 is a γ-secretase modulator extracted from patent WO2016070107, compound example 36. Aβ42-IN-2 has an IC50 of 6.5 nM for Αβ42. Aβ42-IN-2 can be used for the research of Alzheimer's disease.
|
-
- HY-143723
-
|
|
Monoamine Oxidase
|
Metabolic Disease
Cardiovascular Disease
Inflammation/Immunology
|
|
SSAO inhibitor-3 (Compound 2) is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor with IC50s of <10 nM, and 0.1-10 μM for human SSAO and AOC1, respectively. SSAO inhibitor-3 can be used for the research of atherosclerosis, diabetes and its complications, obesity, stroke, chronic kidney disease, retinopathy, chronic obstructive pulmonary disease (COPD), autoimmune diseases, multiple sclerosis, etc.
|
-
- HY-106616
-
|
BAY-g 2821; Edrul
|
Others
|
Cardiovascular Disease
|
|
Muzolimine (BAY-g 282) is a slow and long lasting diuresis agent. Muzolimine produces a diuresis in the loop of Henle and also shows anti-hypertensive effects. Muzolimine can be used for the research of cardiovascular disease.
|
-
- HY-W015546
-
|
BMAA hydrochloride; β-N-methylamino-L-alanine hydrochloride
|
Others
|
Neurological Disease
|
|
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.
|
-
- HY-P3858
-
|
|
Amyloid-β
|
Neurological Disease
|
|
(D-Asp1)-Amyloid β-Protein (1-42) is a peptide fragment of amyloid β-protein (Aβ). Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease.
|
-
- HY-B1371
-
|
Spiroperidol
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
Spiperone is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is a widely used pharmacological tool. Spiperone has the potential for the research of neurology diseases.
|
-
- HY-N8260
-
|
|
Others
|
Neurological Disease
|
|
Angeloylgomisin Q is a new dibenzocyclooctadiene lignan from the stems of Schisandra sphaerandra. Angeloylgomisin Q has the potential for alzheimer's disease research.
|
-
- HY-44154
-
|
|
Others
|
Metabolic Disease
|
|
PSB-CB5 is a potent and selective antagonist of GRP18. PSB-CB5 has the potential for the research of metabolic disease and obesity.
|
-
- HY-105327
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.
|
-
- HY-151208
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-16 is a selective monoamine oxidase B (MAO-B) inhibitor, with an IC50 of 1.55 µM. MAO-B-IN-16 can be used in the study of central nervous disorders, such as parkinson's disease.
|
-
- HY-14431
-
|
SAM-531; PF-05212365
|
5-HT Receptor
|
Neurological Disease
|
|
Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
|
-
- HY-156556
-
|
|
c-Fms
|
Cancer
Inflammation/Immunology
|
|
c-Fms-IN-14 (Example 76) is a c-Fms inhibitor with an IC50 value of 4 nM. c-Fms-IN-14 can be used for research of cancer and autoimmune diseases.
|
-
- HY-154958
-
|
|
mTOR
|
Neurological Disease
|
|
mTOR inhibitor-12 (Compound 11) is a selective brain penetrant mTOR inhibitor without genotoxicity risk. mTOR inhibitor-12 can be used for the research of CNS diseases.
|
-
- HY-P3846
-
|
|
Amyloid-β
|
Neurological Disease
|
|
(Glu20)-Amyloid β-Protein (1-42) is a slower fibrillizing variant of amyloid β-protein (Aβ). The Glu20 mutation reduces the aggregation propensity of Aβ42 and prevents accumulation of the slowly fibrillizing peptide. Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease.
|
-
- HY-P1387
-
|
|
Amyloid-β
Apoptosis
|
Neurological Disease
|
|
β-Amyloid (1-40) (rat) is a rat form of the amyloid β-peptide, which accumulates as an insoluble extracellular deposit around neurons, giving rise to the senile plaques associated with Alzheimer's disease (AD). β-Amyloid (1-40) (rat) increases 45Ca 2+ influx, induces neurodegeneration in the rat hippocampal neurons of the CA1 subfield. β-Amyloid (1-40) (rat) induces apoptosis. β-Amyloid (1-40) (rat) can be used for the research of Alzheimer's disease.
|
-
- HY-148475
-
-
- HY-P3244
-
|
|
Amyloid-β
|
Neurological Disease
|
|
D-KLVFFA is the inhibitor of Amyloid-β assembly, with the IC50 of 2.6 μM, that can be used in Alzheimer's disease study.
|
-
- HY-P3392A
-
|
ION373 sodium
|
FAP
|
Neurological Disease
|
|
Zilganersen sodium is a glial fibrillary acidic protein (GFAP) inhibitor. Zilganersen sodium can be used in Alexander disease (AxD) research.
|
-
- HY-109055
-
|
E2609
|
Beta-secretase
|
Neurological Disease
|
|
Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
|
-
- HY-147260B
-
|
(Rac)-SAGE-718
|
TRP Channel
|
Neurological Disease
|
|
(Rac)-Dalzanemdor ((Rac)-SAGE-718) is an isomer of Dalzanemdor (HY-147260). Dalzanemdor is an orally active and highly intrinsically active N-methyl-d-aspartate receptor (NMDAR)-positive allosteric modulator (PAM). Dalzanemdor can be used in the research of Huntington's disease.
|
-
- HY-P99399
-
|
RG 6100; RO7105705; MTAU-9937A
|
Tau Protein
|
Neurological Disease
|
|
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease.
|
-
- HY-115494
-
|
Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-123353
-
|
Neladenoson bialanate; BAY-1067197
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases.
|
-
- HY-122647
-
|
VU0652957; VU2957
|
mGluR
|
Neurological Disease
|
|
Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease.
|
-
- HY-139004
-
|
|
Casein Kinase
|
Neurological Disease
|
|
SGC-CK2-1 is a highly potent, ATP-competitive, and cell-active CK2 chemical probe with exclusive selectivity for both human CK2 isoforms, with IC50s of 36 and 16 nM for CK2α and CK2α′respectively in the nanoBRET assay. SGC-CK2-1 can be used for the research of neurodegenerative diseases.
|
-
- HY-119857
-
|
SIRT2 Inhibitor,Inactive Control
|
Sirtuin
|
Neurological Disease
|
|
AGK7 is a potent inhibitor of sirtuin 2 (SIRT2). AGK7 rescues alpha-synuclein toxicity and modified inclusion morphology in a cellular model of Parkinson's disease. AGK7 protects against dopaminergic cell death both in vitro and in a Drosophila model of Parkinson's disease.
|
-
- HY-17609
-
|
CR-845; FE-202845
|
Opioid Receptor
|
Neurological Disease
|
|
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease.
|
-
- HY-W017500
-
|
|
iGluR
|
Neurological Disease
|
|
N-Methyl-DL-aspartic acid is a glutamate analogue and a NMDA receptor agonist and can be used for neurological diseases research.
|
-
- HY-P99190
-
|
BMS-936557; MDX-1100
|
CXCR
|
Inflammation/Immunology
|
|
Eldelumab (BMS-936557) is a humanised anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease.
|
-
- HY-133589
-
|
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
Fulvine is a pyrrolizidine alkaloid isolated from the seeds of Crotalaria fulva. Fulvine is hepatotoxic and can be used to induce hypertensive pulmonary vascular disease in vivo.
|
-
- HY-147584
-
|
|
Btk
|
Cancer
Inflammation/Immunology
|
|
BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1).
|
-
- HY-128205
-
|
|
TRP Channel
|
Neurological Disease
|
|
BTD is a selective transient receptor potential canonical 5 (TRPC5) activator. BTD can be used for the research of neurological disease.
|
-
- HY-120419
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
PF9601N, an monoamine oxidase B (MAO-B) inhibitor, possesses neuroprotective properties in several in vitro and in vivo models of Parkinson's disease (PD). PF9601N can be used for the research of neurodegenerative diseases mediated by excitotoxicity. PF9601N is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N7950
-
|
|
Others
|
Metabolic Disease
|
|
16-Oxoalisol A is a triterpene in Rhizoma Alismatis. Rhizoma Alismatis is a commonly used traditional Chinese medicine (TCM). Rhizoma Alismatis can be used for the research of urinary tract diseases.
|
-
- HY-B0143A
-
|
Nicotinic acid hydrochloride; Vitamin B3 hydrochloride
|
Endogenous Metabolite
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
Niacin (Vitamin B3; Nicotinic acid) hydrochloride is an orally active B3 vitamin that is an essential nutrient for humans. Niacin hydrochloride plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin hydrochloride is also used in the study of cardiovascular diseases.
|
-
- HY-147938
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE-IN-19 (compound A15) is a highly potent AChE inhibitor with an IC50 value of 0.56 μM, also inhibits Aβ aggregation. AChE-IN-19 has potent neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE-IN-19 can be used for researching Alzheimer's disease.
|
-
- HY-116565
-
|
SUVN-D4010
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
|
-
- HY-N12019
-
-
- HY-W019710
-
|
|
HDAC
|
Neurological Disease
|
|
(E,E)-RGFP966 is a selective and CNS permeable HDAC3 inhibitor that can be used for the research of Huntington’s disease.
|
-
- HY-P99292
-
|
HuZAF; Anti-Human IFNG Recombinant Antibody
|
IFNAR
|
Inflammation/Immunology
|
|
Fontolizumab (HuZAF) is a humanized monoclonal anti-IFN-gamma antibody. Fontolizumab is an immunosuppressive agent. Fontolizumab can be used in research of Crohn’s disease.
|
-
- HY-75992
-
|
|
VD/VDR
|
Others
|
|
trans-Doxercalciferol is an isomer of Doxercalciferol. Doxercalciferol is a Vitamin D2 analog, acts as an activator of Vitamin D receptor, and prevent renal disease.
|
-
- HY-149339
-
|
|
NO Synthase
|
Neurological Disease
|
|
hnNOS-IN-2 (compound 17) is a human neuronal nitric oxide synthase (hnNOS) inhibitor with good metabolic stability. hnNOS-IN-2 can be used for research in neurodegenerative diseases.
|
-
- HY-121392
-
|
|
5-HT Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases.
|
-
- HY-147581
-
|
|
Btk
|
Cancer
Inflammation/Immunology
|
|
BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2).
|
-
- HY-146958
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research.
|
-
- HY-100723
-
|
|
Amyloid-β
|
Neurological Disease
|
|
THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease.
|
-
- HY-148132
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research.
|
-
- HY-143330
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease.
|
-
- HY-108681
-
|
|
Others
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a Ki of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease.
|
-
- HY-15800
-
|
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
|
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases.
|
-
- HY-108237
-
|
(+)-PHNO; Dopazinol
|
Dopamine Receptor
|
Neurological Disease
|
|
Naxagolide ((+)-PHNO; Dopazinol) is a potent dopamine D2 (Dopamine Receptor) agonist. Naxagolide has the potential for the research of parkinson's disease (PD).
|
-
- HY-156592
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research.
|
-
- HY-106579S
-
|
|
COX
|
Inflammation/Immunology
|
|
Tiaprofenic acid-d3 is a deuterium labeled Tiaprofenic acid. Tiaprofenic acid is a nonsteroidal anti-inflammatory agent (NSAID) mainly used in the treatment of rheumatic diseases[1].
|
-
- HY-19660
-
|
H-314-27
|
Thrombin
|
Cardiovascular Disease
|
|
Inogatran (H-314-27) is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
|
-
- HY-122761
-
|
|
mAChR
|
Neurological Disease
|
|
Quifenadine (Compound 3a), the hydroxyl-(diphenyl)methyl quinuclidine derivative, is a M3 receptor antagonist with an IC50 value > 1000 nM. Quifenadine can be used for the research of neurological disease.
|
-
- HY-145155
-
|
|
Proteasome
|
Neurological Disease
|
|
Calpain-2-IN-1 (Formula 1A) is a isoform-specific calpain-2 inhibitor with Kis of 181 nM and 7.8 nM for calpain-1, and calpain-2, respectively. Calpain-2-IN-1 can be used for the research of neurodegenerative diseases and other diseases of synaptic function.
|
-
- HY-122958
-
|
|
α-synuclein
|
Neurological Disease
|
|
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research.
|
-
- HY-155022
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-30 is an AChE inhibitor with an IC50 value of 4.4 μM. AChE-IN-30 has neuroprotective activity, and inhibits H2O2-induced apoptosis by suppressing intracellular ROS accumulation. AChE-IN-30 can be used for research of Alzheimer's disease.
|
-
- HY-111338
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent. Tacrine exhibits certain hepatotoxicity in some individuals. Tacrine can be used for researching Alzheimer's disease (AD).
|
-
- HY-N10742
-
|
|
Reactive Oxygen Species
|
Cardiovascular Disease
|
|
Maritimein is an aurone that can be isolated from Coreopsis tinctoria. Maritimein shows strong diphenyl(2,4,6-trinitrophenyl)iminoazanium (DPPH) radical-scavenging activity with an IC50 value of 4.12 μM. Maritimein can be used for the research of cardiovascular disease.
|
-
- HY-P3908
-
|
|
Amyloid-β
|
Neurological Disease
|
|
FITC-β-Ala-Amyloid β-Protein (1-42) ammonium is a FITC tagged Aβ1-42 monomer peptide. Aβ1-42 plays a key role in the pathogenesis of Alzheimer’s disease.
|
-
- HY-106902
-
|
|
Acyltransferase
|
Cardiovascular Disease
|
|
F-1394 is an orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor that inhibits dietary cholesterol absorption in mice. F-1394 can be used in cardiovascular disease research.
|
-
- HY-122957
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Huperzine C is an alkaloid isolated from Huperzia serrate. Huperzine C is an acetylcholinesterase (AChE) inhibotor, with an IC50 of 0.6 μM. Huperzine C can be used for the research of Alzheimer’s disease.
|
-
- HY-12866B
-
|
(R)-LOXO-101; (R)-ARRY-470
|
Trk Receptor
|
Cancer
Infection
Inflammation/Immunology
|
|
(R)-Larotrectinib is a potent TRK inhibitor with an IC50 value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases
|
-
- HY-153898
-
|
|
Others
|
Neurological Disease
|
|
rTRD01 is a TDP-43 ligand that binds to TDP-43’s RRM1 and RRM2 domains (Kd=89 uM for TDP-43102–269). rTRD01 partially disrupts TDP-43’s interaction with the hexanucleotide RNA repeat of the disease-linked c9orf72 gene. rTRD01 can be used for the research of neurodegenerative diseases.
|
-
- HY-120314
-
|
|
Others
|
Inflammation/Immunology
|
|
GEA 3162, oxatriazol derivative, is a NO-releasing compound. GEA 3162 can be used for the research of Inflammation diseases.
|
-
- HY-132596
-
-
- HY-P3392
-
|
ION373
|
FAP
|
Neurological Disease
|
|
Zilganersen (ION373) is a glial fibrillary acidic protein (GFAP) inhibitor, an antisense oligonucleotide. Zilganersen can be used in Alexander disease (AxD) research.
|
-
- HY-137553
-
|
SM934 free base
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
β-Aminoarteether (SM934 free base) is an Artemisinin derivative with orally active. β-Aminoarteether can be used for inflammation and autoimmune disease research, such as lupus diseases.
|
-
- HY-B1039
-
|
NA-872
|
Glucosidase
Autophagy
|
Metabolic Disease
Neurological Disease
|
|
Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
|
-
- HY-B1039A
-
|
NA-872 hydrochloride
|
Glucosidase
Autophagy
|
Metabolic Disease
Neurological Disease
|
|
Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
|
-
- HY-157090
-
-
- HY-N2807
-
-
- HY-143614
-
|
|
Others
|
Metabolic Disease
|
|
THR-β agonist 3 is a potent agonist of THR-β. THR-β agonist 3 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021129827A1, compound 6).
|
-
- HY-143613
-
|
|
Others
|
Metabolic Disease
|
|
THR-β agonist 2 is a potent agonist of THR-β. THR-β agonist 2 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021121210A1, compound 3).
|
-
- HY-150728
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease.
|
-
- HY-142917
-
|
|
Others
|
Metabolic Disease
|
|
THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72).
|
-
- HY-116565A
-
|
SUVN-D4010 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
|
-
- HY-47822
-
|
|
Sirtuin
|
Neurological Disease
|
|
WAY-354574 is an active molecule targeting deacetylase (Sirtuin) for the study of Huntington's disease (HD).
|
-
- HY-125125
-
|
|
Others
|
Neurological Disease
|
|
Danshenxinkun D is an anti-Alzheimer's disease (AD) candidate. Danshenxinkun D can significantly reverse the expression of PSEN1 and DRD2 mRNA in H2O2 treated PC12 cells. Danshenxinkun D can be used in the study of anti-Alzheimer's disease product candidate [1].
|
-
- HY-W104304
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
2-(3-Trifluoromethylphenyl)glycine hydrochloride is a precursor of substituted 2-acetamido-5-aryl-l, 2,4-triazolones. Substituted 2-acetamido-5-aryl-l, 2,4-triazolones are dual V1a/V2 receptor antagonists and can be used in cardiovascular disease research.
|
-
- HY-N11911
-
|
(-)-Verazine
|
Fungal
|
Infection
Neurological Disease
|
|
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases.
|
-
- HY-151387
-
|
|
Others
|
Neurological Disease
|
|
A2AAR antagonist 1 (compound 21a) is an A2AAR (adenosine A2A receptor) antagonist with a Ki value of 20 nM. A2AAR antagonist 1 shows high ligand efficiency, and it can be used for the research of neurodegenerative diseases.
|
-
- HY-153240
-
|
|
CXCR
|
Inflammation/Immunology
|
|
ACT-672125 is a potent CXCR3 antagonist with IC50 value of 239 nM in human blood. ACT-672125 has activity for hERG with IC50 value of 18μM. ACT-672125 can be used for the research of autoimmune diseases.
|
-
- HY-N7763
-
|
|
Glucosidase
|
Neurological Disease
|
|
Casuarictin is a potent and competitive α-glucosidase inhibitor with an IC50 of 0.21 μg/mL. Casuarictin is a presenilin stabilization factor like protein (PSFL) protein inhibitor. Casuarictin can be used for Alzheimer's disease research.
|
-
- HY-138935
-
|
BI-425809
|
GlyT
|
Neurological Disease
|
|
Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research.
|
-
- HY-101357A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.
|
-
- HY-142949
-
|
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
|
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4).
|
-
- HY-142950
-
|
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
|
ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1).
|
-
- HY-117861
-
|
|
Glucosidase
|
Metabolic Disease
|
|
ML198 is a glucocerebrosidase (GCase) modulator with an EC50 of 0.4 μM. ML198 is an activator and non-inhibitory chaperone of glucocerebrosidase. ML198 can be used for the research of Gaucher disease. ML198 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-156435
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau protein/α-synuclein-IN-1 is a dual inhibitor of tau protein and α-synuclein. tau protein/α-synuclein-IN-1 reduces α-syn inclusions development in M17D neuroblastoma cells. tau protein/α-synuclein-IN-1 can be used in study Alzheimer’s disease.
|
-
- HY-15800A
-
|
|
LRRK2
|
Inflammation/Immunology
Neurological Disease
|
|
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases.
|
-
- HY-120576
-
|
VU0405652
|
mAChR
|
Neurological Disease
|
|
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease.
|
-
- HY-B0143
-
|
Nicotinic acid; Vitamin B3
|
Autophagy
Endogenous Metabolite
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.
|
-
- HY-N12423
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Bis-(-)-8-demethylmaritidine, a natural alkaloid, is a potent acetylcholinesterase (AChE) inhibitor. Bis-(-)-8-demethylmaritidine can be used for Alzheimer's disease research.
|
-
- HY-15608
-
-
- HY-B0623A
-
|
SKF 101468 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Ropinirole (SKF 101468) hydrochloride is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
|
-
- HY-B0623
-
|
SKF 101468
|
Dopamine Receptor
|
Neurological Disease
|
|
Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease.
|
-
- HY-111935
-
|
|
Microtubule/Tubulin
|
Neurological Disease
|
|
3,3'-Diethyl-9-methylthiacarbocyanine iodide is a cyanine dye, also a tau aggregation inhibitor, with an IC50 value of 0.28 μM for tau. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can cause misfunction of the microtubule cytoskeleton. 3,3'-Diethyl-9-methylthiacarbocyanine iodide can be used for researching Alzheimer’s disease.
|
-
- HY-P1913
-
|
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Calcitonin Gene Related Peptide (CGRP) II, rat, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide (CGRP) II can be used in the research of cardiovascular diseases.
|
-
- HY-13206
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research.
|
-
- HY-149477
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
IHC3 is a competitive and reversible MAO-B inhibitor (IC50: 1.672 μM). IHC3 can interact with the amino acid Cys172 of MAO-B. IHC3 can be used for neurological diseases research.
|
-
- HY-N10283
-
-
- HY-108837
-
|
|
Others
|
Metabolic Disease
|
|
Agalsidase alfa has an amino acid sequence identical to that of native α-galactosidase A. Agalsidase alfa can be used for Fabry disease research.
|
-
- HY-P990007
-
|
PRA023; PRA-023
|
TNF Receptor
|
Inflammation/Immunology
|
|
Tulisokibart (PRA023) is a humanized IgG1-κ monoclonal antibody targeting to TNFSF15/TL1A. Tulisokibart can be used to study a variety of inflammatory/fibrotic diseases, such as Crohn's Disease (CD).
|
-
- HY-12947
-
|
|
MAP3K
|
Neurological Disease
|
|
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
|
-
- HY-112555
-
-
- HY-116020
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.
|
-
- HY-100642S
-
|
Ro 40-7591 d7
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-145906
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.
|
-
- HY-W587430
-
|
Glycolithocholate sulfate disodium; Sulfolithocholylglycine disodium; SLCG disodium
|
HIV
|
Infection
|
|
Glycolithocholic acid 3-sulfate (disodium) inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate (disodium) can be used for the research of HIV infection and gallbladder disease.
|
-
- HY-139066
-
|
Trichosanic acid
|
Others
|
Metabolic Disease
|
|
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and a ω-5 polyunsaturated fatty acid. Punicic acid has the potential for the research of various chronic diseases.
|
-
- HY-145712
-
|
|
FKBP
|
Cancer
|
|
ElteN378 is an inhibitors of FKBP12e. ElteN378 can be used in study Alzheimer disease, Parkinson disease, Amyotrophic Lateral Sclerosis, proliferation disorders and cancer.
|
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- HY-146527
-
|
|
Bcr-Abl
|
Cancer
Neurological Disease
|
|
c-ABL-IN-2 is a potent inhibitor of c-Abl. Activation of c-Abl has been implicated in various diseases, notably cancer. c-ABL-IN-2 has the potential for the research of neurodegenerative diseases (amyotrophic lateral sclerosis (ALS) and Parkinson’s disease (PD) and cancer (extracted from patent WO2020260871A1, compound 25). c-ABL-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146742
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARγ agonist 2 is a potent PPARγ partial agonist and can be used for metabolic disease research.
|
-
- HY-116969
-
|
Narthesterol
|
LXR
|
Metabolic Disease
|
|
22(R)-Hydroxycholesterol (Narthesterol) is an endogenous LXR agonist. 22(R)-Hydroxycholesterol (Narthesterol) can be used for tangier disease research.
|
-
- HY-145988
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases.
|
-
- HY-137789
-
|
LY 213829
|
COX
|
Cancer
|
|
Tazofelone (LY 213829) is a cyclooxygenase-II (COX-II) inhibitor. Tazofelone transform into sulfoxide and quinol metabolites is primarily mediated by CYP3A. Tazofelone can be used for the research of inflammatory bowel disease.
|
-
- HY-P1913A
-
|
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Calcitonin Gene Related Peptide (CGRP) II, rat TFA, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide (CGRP) II TFA can be used in the research of cardiovascular diseases.
|
-
- HY-150049
-
|
|
Amyloid-β
|
Neurological Disease
|
|
γ-Secretase modulator 13 (compound 4) is a gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 163 nM. γ-Secretase modulator 13 can be used in the study of Alzheimer's disease.
|
-
- HY-120686
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
S-14671 is a high-affinity 5-HT1A agonist (pKi=9.3). S-14671 can be used for research on neurological diseases, such as anti-anxiety, anti-depression, etc.
|
-
- HY-110325
-
|
|
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-P99022
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Gantenerumab is a fully human anti-amyloid-β (Aβ) IgG1 monoclonal antibody demonstrates sustained cerebral amyloid-β binding. Gantenerumab can be used for Alzheimer's disease research.
|
-
- HY-P5082
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein 4554W is an inhibitor of α-Synuclein (aSyn) aggregation with associated toxicity. α-Synuclein 4554W consists of GIVNGVKA sequences, previously identified through intracellular library screening. α-Synuclein 4554W reduces fibril formation of aSyn mutants assocaited with Parkinson’s disease.
|
-
- HY-15470
-
|
|
P2X Receptor
|
Neurological Disease
|
|
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.
|
-
- HY-15469
-
|
|
P2X Receptor
|
Neurological Disease
|
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.
|
-
- HY-136341
-
-
- HY-135006A
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Octahydroaminoacridine, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine can be used for Alzheimer's disease (AD) research.
|
-
- HY-124204
-
|
|
iGluR
|
Neurological Disease
|
|
LY 274614 is an orally active, competitive NMDA receptor antagonist. LY 274614 can be used for Neurological Disease study.
|
-
- HY-12452
-
-
- HY-111280
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
ST 198 is an orally active D3R antagonist. ST 198 can block the expression of nicotine-induced CPP at doses selective for D3R. ST 198 can be used for the research of neurological disease.
|
-
- HY-W263279
-
|
(E)-Wy-8678
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
|
-
- HY-103374
-
|
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-W004284
-
-
- HY-156552
-
-
- HY-128128
-
|
|
Others
|
Neurological Disease
|
|
ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
|
-
- HY-153730
-
|
|
Hedgehog
|
Inflammation/Immunology
|
|
Hedgehog IN-5 is an orally active small molecule inhibitor of the hedgehog pathway. Hedgehog IN-5 can be used for the research of fibrotic disease.
|
-
- HY-150702
-
|
|
MAGL
|
Inflammation/Immunology
Neurological Disease
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
|
-
- HY-135902
-
|
NSC 377363
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-135902A
-
|
NSC 377363 hydrochloride
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-117924
-
|
Autophagy enhancer-67
|
Autophagy
|
Neurological Disease
|
|
AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease.
|
-
- HY-153476
-
|
|
GCGR
|
Metabolic Disease
|
|
GIP/GLP-1 dual receptor agonist-1 (compound 4) is a GIP/GLP-1 receptor agonist. GIP/GLP-1 dual receptor agonist-1 can be used in the research of metabolic disorders and fatty liver diseases, including nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).
|
-
- HY-149329
-
|
|
Carbonic Anhydrase
|
Cancer
Neurological Disease
|
|
hCAIX/VII-IN-1 is a selective hCA VII/IX inhibitor. hCAIX/VII-IN-1 inhibit hCAⅠ, hCAⅡ, hCAⅣ, hCAⅦ and hCAⅨ with Ki values of 336.2 nM,185.8 nM, 1055 nM, 35.6 nM and 28.0 nM, respectively. hCAIX/VII-IN-1 can be used for the research of cancer and neurological diseases.
|
-
- HY-155085
-
|
|
Monoamine Oxidase
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
|
hAChE-IN-3 (compounds 5c) is a potent and blood-brain barrier permeable AChE, BuChE， MAO-B-IN-1 and BACE-1 inhibitor, with IC50 values of 0.44, 0.08, 5.15 and 0.38 μM, respectively. hAChE-IN-3 has antioxidant activity and metal chelating ability. In addition, hAChE-IN-3 can bind to peripheral anion sites, and affect β amyloid and reduce Alzheimer's-associated neurodegeneration. hAChE-IN-3 has the potential for the research of Alzheimer's disease.
|
-
- HY-143485
-
|
|
IRAK
|
Cancer
Inflammation/Immunology
|
|
IRAK4-IN-9 (compound 73) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-9 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer.
|
-
- HY-143486
-
|
|
IRAK
|
Cancer
Inflammation/Immunology
|
|
IRAK4-IN-10 (compound 75) is a potent IRAK4 inhibitor with an IC50 of 1.5 nM. IRAK4-IN-10 blocks MyD88 dependent signaling. IRAK4-IN-9 has the potential for the research of inflammatory diseases, autoimmune diseases, and cancer.
|
-
- HY-146137
-
-
- HY-111372
-
|
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-N10488
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC50 of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research.
|
-
- HY-150050
-
|
|
Amyloid-β
|
Neurological Disease
|
|
gamma-secretase modulator 5 (compound 22d) is a brain-penetrant gamma-secretase modulator (GSMs) that inhibits the production of the aggregated amyloid β-peptide Aβ42 with an IC50 value of 60 nM. gamma-secretase modulator 5 can be used in the study of Alzheimer's disease.
|
-
- HY-148385
-
|
|
Others
|
Cancer
|
|
Ganglioside GM2 is a human tumor antigen (OFA-I-1). Ganglioside GM2 is the major lysosomal storage compound of Tay-Sachs disease.
|
-
- HY-15280
-
|
|
PI3K
|
Inflammation/Immunology
|
|
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease.
|
-
- HY-P99485
-
|
AMG 139; MEDI2070
|
Interleukin Related
|
Inflammation/Immunology
|
|
Brazikumab (AMG 139) is a human IgG2 monoclonal antibody, selectively binds the p19 subunit of IL-23, with a KD of 0.138 nM for human IL-23. Brazikumab can be used for the research of Crohn's disease.
|
-
- HY-155833
-
|
|
PI3K
|
Cancer
Infection
Inflammation/Immunology
|
|
PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases.
|
-
- HY-111313
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease.
|
-
- HY-P99821
-
-
- HY-151539
-
-
- HY-150585
-
|
|
Amyloid-β
Cholinesterase (ChE)
Tau Protein
|
Neurological Disease
|
|
BuChE-IN-5 (compound 25b) is a potent BuChE inhibitor with an IC50 value of 1.94 μM. BuChE-IN-5 efficiently inhibits aggregation Aβ and tau protein in Escherichia coli. BuChE-IN-5 also has free radical scavenging capacity and antioxidant activity. BuChE-IN-5 can be used for researching Alzheimer’s disease.
|
-
- HY-18681
-
|
GBT 440
|
Others
|
Cardiovascular Disease
|
|
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
|
-
- HY-135006
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Octahydroaminoacridine succinate, a Tacrine analogue, is an acetylcholinesterse (AChE) and butyrylcholinesterase (BChE) inhibitor. Octahydroaminoacridine succinate can be used for Alzheimer's disease (AD) research.
|
-
- HY-122230
-
|
|
Integrin
|
Cardiovascular Disease
|
|
UR-3216 is a selective, and orally active platelet surface glycoprotein (GPIIb/IIIa) receptor antagonist. UR-3216 has the potential for cardiovascular diseases research.
|
-
- HY-156179
-
|
|
Amyloid-β
|
Neurological Disease
|
|
DDC 2′,3′-O-disulfate (compound 4) prevents the fibrillization and oligomerization of Aβ42. DDC 2′,3′-O-disulfate has the potential for Alzheimer's disease (AD) research.
|
-
- HY-114866
-
|
Lentinacin; D-Eritadenine; Lentysine
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
Eritadenine (Lentinacin) is a S-adenosyl-L-homocysteine hydrolase (SAHH) inhibitor. Eritadenine can be found in secondary metabolites of shiitake mushrooms. Eritadenine lowers blood cholesterol levels and can be used in cardiovascular disease research.
|
-
- HY-139974
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-2 (compound 22) is a potent inhibitor of BChE with a Ki of 0.099 μM. BChE-IN-2 is a pyrimidine and pyridine derivative. BChE-IN-2 has the potential for the research of Alzheimer’s disease (AD) .
|
-
- HY-151210
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-17 is a selective monoamine oxidase B (MAO-B) inhibitor with the IC50 value of 5.08 μM. MAO-B-IN-17 can be used in Parkinson’s disease research.
|
-
- HY-147644
-
|
|
Others
|
Neurological Disease
|
|
α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research.
|
-
- HY-149845
-
|
|
GSK-3
PROTACs
|
Neurological Disease
|
|
PROTAC GSK-3β Degrader-1 (compound 1) is a degrader targets GSK-3β degradation with an IC50 value of 833 nM. PROTAC GSK-3β Degrader-1 contains SB-216763 (a GSK-3β inhibitor), a PEG linker and a CRBN (E3 ligase liand). PROTAC GSK-3β Degrader-1 reduces the neurotoxicity induced by Aβ25-35 peptide and CuSO4. PROTAC GSK-3β Degrader-1 can be used to research in Alzheimer's disease.
|
-
- HY-14415
-
|
|
REV-ERB
|
Metabolic Disease
Neurological Disease
|
|
SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease.
|
-
- HY-132593
-
|
WVE-120101
|
Huntingtin
|
Neurological Disease
|
|
Rovanersen (WVE-120101) is an antisense oligonucleotide that specifically targets mutated mRNA copies of the huntington (HTT) gene without affecting healthy mRNA of HTT gene, thereby preventing the production of faulty Huntingtin protein. Rovanersen can be used for huntington’s disease research.
|
-
- HY-112855
-
|
|
LRRK2
|
Neurological Disease
|
|
PF-06447475 is a highly potent, selective, brain penetrant LRRK2 kinase inhibitor with IC50 values of 3 nM and 11 nM for WT LRRK and G2019S LRRK2, respectively. PF-06447475 can be used for parkinson's disease (PD) research.
|
-
- HY-151348
-
|
|
Beta-secretase
|
Neurological Disease
|
|
BACE1-IN-11 is a BACE1 inhibitor. BACE1-IN-11 has the BACE1 inhibitory activity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
|
-
- HY-149313
-
|
|
Amylases
|
Metabolic Disease
|
|
α Amylase-IN-1 (Compound 11) is an α-Amylase inhibitor with an IC50 value of 0.5509 μM. α Amylase-IN-1 has antioxidant activity with an IC50 value of 53.49 μM for scavenging DPPH free radicals. IC50 can be used in the study of diabetes and oxidative stress-related diseases.
|
-
- HY-149817
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-29, 3-OH pyrrolidine derivative, is an cholinesterase (ChE) inhibitor. AChE-IN-29 has cholinesterase inhibitory activity for hAChE, eeAChE and eqBChE with IC50 values of 0.25 μM, 0.23 μM and 0.72 μM, respectively. AChE-IN-29 can be used for the research of Alzheimer's disease.
|
-
- HY-P3648
-
|
AAPV-CMK
|
Elastase
|
Inflammation/Immunology
|
|
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases.
|
-
- HY-14418
-
|
ML-128
|
mGluR
|
Neurological Disease
|
|
VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
|
-
- HY-113641
-
-
- HY-143221
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
AS-Inclisiran is the antisense of Inclisiran. Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.
|
-
- HY-N10356
-
|
|
Others
|
Neurological Disease
|
|
4,27-Dimethyl withaferin A is a synthetic analog of withanolide natural products. 4,27-Dimethyl withaferin A has the potential for the research of neurodegenerative diseases (extracted from patent WO2015077780A1).
|
-
- HY-120296
-
-
- HY-13993B
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 hydrochloride is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 hydrochloride shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 hydrochloride has the potential for the research of parkinson's disease (PD).
|
-
- HY-13993
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 has the potential for the research of parkinson's disease (PD).
|
-
- HY-156601
-
|
|
Others
|
Others
|
|
Bexicaserin (Compound 3) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases.
|
-
- HY-152235
-
|
|
HDAC
|
Cancer
Neurological Disease
|
|
HDAC6-IN-15 is a selective histone deacetylase 6 (HDAC6) inhibitor. HDAC6-IN-15 has potent inhibitory activity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases.
|
-
- HY-15295
-
|
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-151173
-
-
- HY-150003
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
Aβ1-42 aggregation inhibitor 1 inhibits AChE (acetylcholinesterase) and BuChE (butyrylcholinesterase) with the IC50 value of 2.64 μM and 1.29 μM, respectively. Aβ1-42 aggregation inhibitor 1 inhibits self-mediated Aβ1-42 aggregation by 51.29% at a concentration of 25 μM. Aβ1-42 aggregation inhibitor 1 has the potential for the research of anti-Alzheimer's disease.
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases.
|
-
- HY-143475
-
-
- HY-143474
-
-
- HY-153333
-
|
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases.
|
-
- HY-146039
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease.
|
-
- HY-N10490
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Blestrin D is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 8.1 μM. Blestrin D can be isolated from Bletilla striata. Blestrin D can be used for the research of Alzheimer's disease (AD).
|
-
- HY-14338A
-
|
Lu AE58054 Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine Hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
|
-
- HY-14338
-
|
Lu AE58054
|
5-HT Receptor
|
Neurological Disease
|
|
Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
|
-
- HY-134661A
-
CVN424
1 Publications Verification
|
GPR6
|
Neurological Disease
|
|
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
|
-
- HY-132591
-
-
- HY-153433
-
|
|
Others
|
Neurological Disease
|
|
Serine Hydrolase inhibitor-21 (compound 8), a pyridine, is a serine hydrolase inhibitor with a Ki of 429 nM for BuChE. Serine Hydrolase inhibitor-21 has the potential for Alzheimer's disease research.
|
-
- HY-156032
-
|
|
GSK-3
|
Neurological Disease
|
|
PIMPC is a compound with antioxidant and metal-chelating properties. PIMPC is a novel inhibitor of glycogen synthase kinase 3 (GSK-3). PIMPC has potential anti-Alzheimer's disease effect.
|
-
- HY-13993A
-
|
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 Maleate is a potent, selective and activity-dependent NR2B subunit specific NMDA receptor antagonist. Ro 25-6981 Maleat shows anticonvulsant and anti-parkinsonian activity. Ro 25-6981 Maleate has the potential for the research of parkinson's disease (PD).
|
-
- HY-W416250
-
|
|
Others
|
Cardiovascular Disease
|
|
p-Cresol glucuronide, a metabolite of p-cresol, is a prototype protein-bound uremic toxin. p-Cresol glucuronide is associated with chronic kidney disease (CKD).
|
-
- HY-N11081
-
|
|
Others
|
Cardiovascular Disease
|
|
Hexanorcucurbitacin D is a cucurbitacin. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD).
|
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases.
|
-
- HY-118342
-
|
|
mAChR
|
Neurological Disease
|
|
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimer's disease.
|
-
- HY-120596
-
|
|
PPAR
|
Neurological Disease
|
|
PPARδ/γ agonist 1 sodium is a chemically unique and brain penetrant dual PPAR delta/gamma agonist. PPARδ/γ agonist 1 sodium can be used for the research of Alzheimer’s disease.
|
-
- HY-117608
-
|
|
DYRK
CDK
|
Cancer
Neurological Disease
|
|
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.
|
-
- HY-142778
-
|
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-10 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-10 has the potential for the research of neurodegenerative-related diseases such as Alzheimer's disease (AD), glaucoma, age-related macular degeneration (AMD), or cardiovascular diseases including atherosclerosis (extracted from patent WO2022001881A1, compound 4).
|
-
- HY-121826
-
-
- HY-P99185
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Bapineuzumab is an anti-β-amyloid protein (APP) monoclonal antibody. Bapineuzumab can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-144058
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1).
|
-
- HY-134398
-
|
6-Fu-ATP; KTP
|
Others
|
Neurological Disease
|
|
Kinetin triphosphate(6-Fu-ATP; KTP) is an ATP analogue that regulates or enhances kinase function with higher catalytic efficiency than its endogenous substrate, ATP. Kinetin triphosphate can be used in Parkinson's disease research.
|
-
- HY-147564
-
|
|
RET
|
Cancer
Neurological Disease
|
|
RET-IN-18 is a pyridone compound. is a potent inhibitor of RET. RET-IN-18 is a potent inhibitor of RET. RET-IN-18 has the potential for the research of diseases related to irritable bowel syndrome (IBS) and other gastrointestinal disorders, as well as cancers, and neurodegenerative diseases (extracted from patent WO2022017524A1, compound 1).
|
-
- HY-W011616
-
|
CDNG1/vuc230
|
Wnt
|
Cancer
Cardiovascular Disease
|
|
Cardionogen 1 (CDNG1/vuc230) is a Wnt signaling pathway inhibitor that slows down Myc-induced liver tumorigenesis. Cardionogen 1 treatment of zebrafish embryos before gastrulation inhibits cardiomyocyte formation, whereas treatment during or after gastrulation induces cardiomyocyte formation. Cardionogen 1 has potential in research into cancer and cardiovascular disease.
|
-
- HY-130795
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-P99405
-
|
PRX 002; RG 7935; RO 7046015
|
α-synuclein
|
Neurological Disease
|
|
Prasinezumab (PRX 002) is a humanized IgG1 monoclonal antibody directed against aggregated α-synuclein. Prasinezumab has the potential for Parkinson's disease research.
|
-
- HY-20457
-
-
- HY-144057
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-17 is a potent inhibitor of JAK. JAK-IN-17 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2021185305A1, compound 9-1).
|
-
- HY-W020050
-
|
|
Caspase
Glutaminase
Apoptosis
|
Cancer
Neurological Disease
|
|
Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
|
-
- HY-10096
-
|
|
GSK-3
|
Neurological Disease
|
|
TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease.
|
-
- HY-16747
-
|
SHP625 chloride; LUM001 chloride; Lopixibat chloride
|
Apical Sodium-Dependent Bile Acid Transporter
|
Metabolic Disease
|
|
Maralixibat (SHP625) chloride is an orally active ileal bile acid transporter (IBAT) inhibitor. Maralixibat chloride can be used for the research of rare cholestatic liver diseases including Alagille syndrome (ALGS), progressive familial intrahepatic cholestasis (PFIC) and biliary atresia.
|
-
- HY-134398A
-
|
6-Fu-ATP tetrasodium; KTP tetrasodium
|
Others
|
Neurological Disease
|
|
Kinetin triphosphate(6-Fu-ATP) tetrasodium is an ATP analogue that regulates or enhances kinase function with higher catalytic efficiency than its endogenous substrate, ATP. Kinetin triphosphate tetrasodium can be used in Parkinson's disease research.
|
-
- HY-147243
-
|
ANG-3070
|
VEGFR
PDGFR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.
|
-
- HY-W062700
-
|
|
Others
|
Neurological Disease
|
|
STS-E412 is a selective activator of tissue-protective EPO receptor (including EPOR and CD131). STS-E412 can be used for research of neurodegenerative diseases and organ protection.
|
-
- HY-156586
-
|
|
Tau Protein
|
Neurological Disease
|
|
ASN90 is a specific and orally active O-GlcNAcase (OGA) enzyme inhibitor with IC50 value of 10.2 nM. ASN90 can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies.
|
-
- HY-18286
-
|
|
TSH Receptor
|
Endocrinology
|
|
NCGC00229600 is an allosteric inverse agonist of thyrotropin receptor (TSHR). NCGC00229600 inhibits both TSH and stimulating antibody activation of TSHRs endogenously expressed in Graves' disease.
|
-
- HY-146345
-
|
|
Antibiotic
|
Infection
|
|
Antiviral agent 18 (Compound 5) is an anti-infection agent. Antiviral agent 18 results in good antiviral activity against murine norovirus. Antiviral agent 18 has the potential for the research of infectious and malignant diseases.
|
-
- HY-157087
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/MAO-B-IN-4 (compound 4a) is a selective dual AChE and MAO-B inhibitor. AChE/MAO-B-IN-4 shows no significant inhibition activity against BChE and h-MAO-A. AChE/MAO-B-IN-4 can be used for the Alzheimer’s disease (AD) research.
|
-
- HY-147387
-
|
|
CDK
Amyloid-β
|
Inflammation/Immunology
|
|
DSS30 is a P25/CDK5 inhibitor that reduces β-amyloid (Aβ) secretion by inhibiting amyloid precursor protein lyase 1 (BACEl) phosphorylation. DSS30 can be used in the study of neurodegenerative diseases such as Alzheimer's disease.
|
-
- HY-149010
-
|
|
Keap1-Nrf2
|
Neurological Disease
|
|
NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research.
|
-
- HY-142919
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
μ opioid receptor agonist 2 （Compound H-3）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases.
|
-
- HY-142918
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
μ opioid receptor agonist 1 （Compound H-1a）is an optically pure oxaspiro ring substituted pyrrolopyrazole derivative, acts as a MOR receptor agonist and can be used for the research of pain and pain related diseases.
|
-
- HY-P3140
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein (61-75) is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-155183
-
|
|
Adenosine Receptor
|
Cancer
Inflammation/Immunology
|
|
A3AR agonist 1 (Compound 12) is an A3AR agonist (Ki: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC50 value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc.
|
-
- HY-N0690
-
|
Schizandrin-C; Wuweizisu-C
|
Apoptosis
Virus Protease
Molecular Glues
|
Cancer
|
|
Schisandrin C (Schizandrin-C) is a phytochemical lignan isolated from Schizandra chinensis. Schisandrin C has diverse biological activities, including anticancer, anti-inflammatory and antioxidant effects. Schisandrin C is a molecular glue. Schisandrin C can be used for cancer, alzheimer’s disease, and liver diseases research. Schisandrin C induces cell apoptosis.
|
-
- HY-136459
-
|
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
|
-
- HY-P3507
-
|
ShK-186
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
|
-
- HY-156667
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
H4R antagonist 3 (Example 18) is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. H4R antagonist 3 can be used for the research of prevention of inflammatory, autoimmune, allergic, and ocular diseases.
|
-
- HY-124775
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
(S)-C33 is a potent and selective PDE9 (phosphodiesterase-9) inhibitor, with an IC50 of 11 nM. (S)-C33 can be used for central nervous system diseases and diabetes research.
|
-
- HY-155672
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease.
|
-
- HY-143313
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
Protease-Activated Receptor-1 antagonist 1 (Compound 13) is a protease-activated receptor-1 (PAR-1) antagonist with the IC50 of 3 nM by FLIPR technology. Protease-Activated Receptor-1 antagonist 1 can be used for the research of thrombotic cardiovascular, myocardial infarction, and peripheral arterial disease.
|
-
- HY-N8658
-
|
|
Others
|
Infection
Inflammation/Immunology
|
|
Epinodosin is a diterpenoid. Epinodosin has moderate cytotoxicity against HL-60 cells with IC50 value of 10.4 μM. Epinodosin can be used for the research of inflammatory diseases.
|
-
- HY-109001
-
|
ABT-957
|
Proteasome
|
Neurological Disease
|
|
Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-155708
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-13 (compound 5j) is a potent dual inhibitor of AChE and BChE with IC50s of 20.89 and 17.37 μM, respectively. AChE/BChE-IN-13 can be used in Alzheimer’s disease (AD) research.
|
-
- HY-P3140A
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein (61-75) TFA is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD).
|
-
- HY-143300
-
-
- HY-P3780
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Cys-Gly-Lys-Lys-Gly-Amyloid β-Protein (36-42) is the 36-42 fragment of Amyloid β-Protein. β-amyloid, a polypeptide made up of 36-43 amino acids, is the main component of amyloid plaques found in the brains of people with Alzheimer's disease. β-amyloid oligomers (Aβos) plays A key role in the progression of Alzheimer's disease (AD) by inducing neuronal damage and cognitive impairment.
|
-
- HY-B0311A
-
|
(S)-(-)-Carbidopa monohydrate
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa) monohydrate, a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa monohydrate is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa monohydrate inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-B0311
-
|
(S)-(-)-Carbidopa
|
Aryl Hydrocarbon Receptor
|
Cancer
Neurological Disease
|
|
Carbidopa ((S)-(-)-Carbidopa), a peripheral decarboxylase inhibitor, can be used for the research of Parkinson's disease. Carbidopa is a selective aryl hydrocarbon receptor (AhR) modulator. Carbidopa inhibits pancreatic cancer cell and tumor growth.
|
-
- HY-N8440
-
|
|
Others
|
Infection
|
|
Gibberellin A4 is a natural compound that can be isolated from Sphaceloma manihoticola. Gibberellin A4 is a causal agent of cassava superelongation disease.
|
-
- HY-120441
-
-
- HY-105934A
-
|
Emofolin sodium; 5-methyltetrahydrohomofolate sodium; NSC 139490 sodium
|
Antifolate
|
Cancer
Inflammation/Immunology
|
|
Ketotrexate sodium is an orally active antifolate and immunosuppressant. Ketotrexate sodium has good anti-inflammatory activity and is widely used in rheumatoid arthritis (RA). Ketotrexate sodium is used in research into cancer and autoimmune diseases.
|
-
- HY-128511
-
|
Piridoxylate
|
Others
|
Cardiovascular Disease
|
|
Piridoxilate (Piridoxylate), a glyoxylate derivative, is an anti-anoxic agent. Piridoxilate can be used in research on vascular diseases and coronary occlusion.
|
-
- HY-N6906
-
|
|
Others
|
Neurological Disease
|
|
Oleuroside is a phenolic secoiridoid in olive. Oleuroside can protect against mitochondrial dysfunction in models of early Alzheimer's disease and brain ageing.
|
-
- HY-130609A
-
|
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
|
-
- HY-P3507A
-
|
ShK-186 TFA
|
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease.
|
-
- HY-N10489
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD).
|
-
- HY-N10486
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-10 (compound 6) is a potent butyrylcholinesterase (BChE) mixed-type inhibitor with an IC50 value of 6.4 μM. BChE-IN-10 can be isolated from Bletilla striata. BChE-IN-10 can be used for the research of Alzheimer's disease (AD).
|
-
- HY-B0341
-
|
SG-75
|
Potassium Channel
|
Cardiovascular Disease
|
|
Nicorandil (SG-75) is a potent potassium channel activator and targets vascular nucleoside diphosphate-dependent K + channels and cardiac ATP-sensitive K + channels (KATP). Nicorandil is a nicotinamide ester with vasodilatory and cardioprotective effects and has the potential for angina and forischemic heart diseases.
|
-
- HY-B0955
-
|
Oxetacaine
|
HBV
|
Neurological Disease
|
|
Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.
|
-
- HY-15381
-
|
FTY720 phosphate
|
LPL Receptor
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.
|
-
- HY-143275
-
|
|
PI3K
|
Cancer
|
|
HL-8 is a PROTAC molecule targeting PI3K kinase. HL-8 has a significant and complete degradation effect on PI3K kinase at a concentration of 10 μM within 8 h. HL-8 has the potential for the research of cancer diseases.
|
-
- HY-B0160
-
|
FRG-8813
|
Histamine Receptor
|
Metabolic Disease
Endocrinology
|
|
Lafutidine (FRG-8813) is a histamine H2-receptor antagonist (H2RA), with proven gastric mucosal protective effects. Lafutidine can be used for the research of gastroesophageal reflux disease.
|
-
- HY-149102
-
-
- HY-N3345
-
|
|
Bacterial
|
Infection
|
|
Macrocarpal B is an antibacterial compounds. Macrocarpal B can be isolated from the branch of Eucalyptus globulus. Macrocarpal B can be used for the research of periodontal disease.
|
-
- HY-P1409
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases.
|
-
- HY-151963
-
|
|
PPAR
Glucocorticoid Receptor
|
Metabolic Disease
|
|
PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes.
|
-
- HY-P99859
-
|
LY3002813
|
Amyloid-β
|
Neurological Disease
|
|
Donanemab (LY3002813) is a humanized IgG1 monoclonal antibody directed at an N‐terminal pyroglutamate amyloid beta (Aβ) epitope. Donanemab has the potential for early Alzheimer's disease research.
|
-
- HY-145845
-
|
|
HDAC
Monoamine Oxidase
|
Neurological Disease
|
|
HDAC1/MAO-B-IN-1 is a potent, selective and cross the blood-brain barrier HDAC1/MAO-B inhibitor with IC50 values of 21.4 nM and 99.0 nM for HDAC1 and MAO-B, respectively. HDAC1/MAO-B-IN-1 has the potential for the research of Alzheimer’s disease.
|
-
- HY-145578
-
|
X842
|
Others
|
Inflammation/Immunology
|
|
Linaprazan glurate inhibits exogenously or endogenously stimulated gastric acid secretion. Linaprazan glurate exhibits several advantageous properties, such as fast onset, high in vivo potency and/or long duration of action. Linaprazan glurate is useful in the research of gastrointestinal inflammatory diseases and peptic ulcer diseases (extracted from patent WO2010063876A1).
|
-
- HY-103442
-
|
DAPH
|
EGFR
Amyloid-β
|
Cancer
Neurological Disease
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of Ca 2+ ions into neuronal cells, and dramatic inhibits and reverses the formation of β-amyloid (Aβ42) fibril aggregates associated with Alzheimer's disease.
|
-
- HY-121508
-
|
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603 (IT-603). IT-603 is a c-Rel inhibitor with an IC50 of 3 μM. IT-603 has anti-tumor activity. (E/Z)-IT-603 is a promising modulator of T-cell responses in the context of graft-versus-host disease (GVHD) and malignant diseases.
|
-
- HY-B0715
-
|
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
|
-
- HY-101277
-
|
PG-1016548; AKB-6548
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Vadadustat (PG-1016548) is a titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor. Vadadustat is an erythropoiesis-stimulating agent and has the potential for anemia treatment in chronic kidney disease in vivo.
|
-
- HY-150223
-
|
|
Small Interfering RNA (siRNA)
Ser/Thr Protease
|
Cardiovascular Disease
|
|
GalNAc unconjugated/naked Inclisiran is a double-stranded small interfering RNA (siRNA) without GalNAc conjugation. GalNAc unconjugated/naked Inclisiran inhibits the transcription of PCSK-9, and can be used for hyperlipidemia and cardiovascular disease (CVD) research.
|
-
- HY-19948
-
|
TRx0237 mesylate; Methylene blue leuco base mesylate
|
Amyloid-β
|
Neurological Disease
|
|
Leucomethylene blue (TRx0237) mesylate, an orally active second-generation tau protein aggregation inhibitor (Ki of 0.12 μM), could be used for the study of Alzheimer's Disease. Leucomethylene blue mesylate is a common reduced form of Methylene Blue, Methylene Blue is a member of the thiazine class of dyes.
|
-
- HY-151405
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Z164597606 is a selective BChE inhibitor (IC50: 1.3 and 1.7 μM for eqBChE and hBChE). Z164597606 forms a π-π stacking interaction with the amino acid Trp82 of hBChE. Z164597606 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-123704
-
|
|
5-HT Receptor
|
Neurological Disease
|
CGS-12066 (maleate) is a 5-HT receptor agonist. CGS-12066 has agonist effect for 5-HT1A , 5-HT1B ,5-HT1C and 5-HT1D with pEC50 values of 6.41, 7.56, 4.05 and 7.11, respectively. CGS-12066 can be used for the research of neurological disease.
|
-
- HY-124428
-
|
FK881
|
COX
|
Cardiovascular Disease
|
|
ASP6537 is a potent and selective rhCOX-1 inhibitor with an IC50 of 0.703 nM. ASP6537 has the potential for cardiovascular disease research.
|
-
- HY-144074
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease.
|
-
- HY-139725
-
|
|
CDK
|
Metabolic Disease
|
|
CDK5-IN-1, a potent CDK5 inhibitor, is against CDK5 activity less than 10 nM. CDK5-IN-1 is used for kidney diseases research.
|
-
- HY-124244
-
|
PPARδ/γ agonist 1
|
PPAR
|
Neurological Disease
|
|
DB-959 (PPARδ/γ agonist 1) is a potent dual PPAR delta/gamma inhibitor. DB-959 can be used for Alzheimer’s disease research.
|
-
- HY-121538
-
|
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-116090
-
|
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-148264
-
-
- HY-148112
-
|
|
Casein Kinase
|
Neurological Disease
|
|
Casein kinase 1δ-IN-1 (compound 822) is an inhibitor of casein kinase 1 delta (CK1δ), exhibits inhibition of greater than 5%. Casein kinase 1δ-IN-1 can be used for neurodegenerative disorders such as Alzheimer's disease research.
|
-
- HY-P4987
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
|
TRAP-7 is a thrombin receptor (PAR) activating peptide. TRAP-7 stimulates total inositol phosphate (IP) accumulation and phosphorylation of a specific endogenous substrate for activated PKC. TRAP-7 can be used in cardiovascular disease research.
|
-
- HY-156553
-
|
|
Btk
|
Cancer
Inflammation/Immunology
|
|
BTK-IN-27 (example 8) is a BTK inhibitor (IC50: 0.2 nM). BTK-IN-27 shows anti-proliferative activity in TMD8 cells (IC50: < 5 nM). BTK-IN-27 can be used for research of cancer, lymphoma, leukemia and immunological diseases.
|
-
- HY-155659
-
|
|
Others
|
Neurological Disease
|
|
4A7C-301 is a Nurr1 agonist with robust neuroprotective effects in vitro. 4A7C-301 significantly ameliorates neuropathological abnormalities and improves motor and olfactory dysfunctions in AAV2-mediated α-synuclein-overexpressing male mouse models. 4A7C-301 can be used for the research of Parkinson’s disease.
|
-
- HY-141511
-
|
|
Fluorescent Dye
|
Cancer
Neurological Disease
|
|
Coppersensor-1 (CS1) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu + with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu +) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases.
|
-
- HY-15452
-
|
EX-527
|
Sirtuin
|
Cancer
Inflammation/Immunology
|
|
Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease.
|
-
- HY-17623C
-
|
(R)-CJ-12420; (R)-RQ-00000004
|
Proton Pump
|
Metabolic Disease
|
|
(R)-Tegoprazan (example 3), a benzimidazole derivative, is a potent kidney H +/K +-ATPase inhibitor with an IC50 of 98 nM of canine kidney Na +/K +-ATPase. (R)-Tegoprazan has the potential for gastrointestinal diseases research.
|
-
- HY-N8598
-
|
|
Others
|
Cardiovascular Disease
|
|
Caulophine is a fluoroketone alkaloid isolated from Caulophyllum robustum MAXIM. Caulophine has antioxidant activity and the ability to protect cardiomyocytes from oxidative and ischemic damage, providing potential value for coronary heart disease research.
|
-
- HY-139293
-
|
|
Others
|
Cardiovascular Disease
|
|
PF-07059013 is an orally active and potent noncovalent modulator of sickled hemoglobin (HbS). PF-07059013 specifically binds to Hb with nanomolar affinity and displays strong partitioning into red blood cells (RBCs). PF-07059013 can be used for sickle cell disease (SCD) research.
|
-
- HY-W094474
-
|
hydrate/monohydrateortrihydrate
|
GSK-3
Apoptosis
|
Infection
Neurological Disease
|
|
Lithium chloride hydrate, an orally active mood stabilizer, is a potent virus inhibitor and effective immunomodulatory agent. Lithium chloride hydrate has antidepressant activity by inhibiting GSK3β and promoting neurogenesis. Lithium chloride hydrate alleviates cognition dysfunction and the symptoms of acute mania and depression. Lithium chloride hydrate can also be used for research of virus infection and Alzheimer's disease.
|
-
- HY-145443
-
|
|
Others
|
Cancer
|
|
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or researching cancer or tumor-related diseases.
|
-
- HY-107867
-
|
|
Others
|
Cardiovascular Disease
|
|
Clopidogrel sulfate is an antiplatelet agent. Specifically, Clopidogrel sulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. Clopidogrel sulfate can be used for research of heart disease and stroke.
|
-
- HY-145708
-
-
- HY-P3709
-
|
|
E1/E2/E3 Enzyme
|
Neurological Disease
|
|
TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
|
-
- HY-148133
-
|
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases.
|
-
- HY-13206A
-
|
|
mGluR
|
Neurological Disease
|
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research. MTEP is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N10397
-
|
|
CCR
|
Inflammation/Immunology
|
|
Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC50 = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases.
|
-
- HY-154851
-
|
|
GSK-3
CDK
Tau Protein
|
Neurological Disease
|
|
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research.
|
-
- HY-133011
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
|
-
- HY-P0198B
-
-
- HY-149349
-
|
|
Bacterial
|
Cancer
Infection
|
|
MtUng-IN-1 (Compound 18a) is a Uracil DNA glycosylase of Mycobacterium (MtUng) inhibitor (IC50: 300 μM). MtUng-IN-1 can be used for research of cancers and infectious diseases.
|
-
- HY-66010A
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cinepazide is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-13720A
-
|
Pergolide methanesulfonate; LY127809
|
Dopamine Receptor
|
Neurological Disease
|
|
Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research.
|
-
- HY-145585
-
|
|
iGluR
|
Neurological Disease
|
|
Onfasprodil is negative allosteric modulator of NR2B. Onfasprodil in combination with GABA receptor regulator has the potential for the research of Alzheimer's disease (extracted from patent CN111481543A).
|
-
- HY-70081A
-
|
U-95666E; PNU-95666
|
Dopamine Receptor
|
Neurological Disease
|
|
Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.
|
-
- HY-148908
-
|
|
Biochemical Assay Reagents
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
TNF-α-IN-8 (compound I-42) is a TNF-α inhibitor. TNF-α-IN-8 is an isoindole-imide compound. TNF-α-IN-8 can be used for the research of cancer, heart disease, osteoporosis, inflammatory, allergic and autoimmune diseases. TNF-α-IN-8 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-131417
-
|
|
MMP
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
cis-ACCP is an orally active antimetastatic matrix metalloproteinase-2 (MMP-2) selective inhibitor. cis-ACCP can inhibit MMP-2 and MMP-9 with IC50 values of 4 μM and 20 μM, respectively. cis-ACCP can be used for the research of a variety of chronic diseases.
|
-
- HY-107757
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GMQ is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ opens only ASIC3 but no other ASICs at pH 7.4. GMQ can be used for neurological disease research.
|
-
- HY-109193
-
|
IMR-687
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.
|
-
- HY-143464
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease.
|
-
- HY-N10443
-
|
|
Parasite
Apoptosis
Autophagy
Reactive Oxygen Species
|
Infection
|
|
Mammea A/BA has potent activity against Trypanosoma cruzi (T. cruzi). Mammea A/BA induces mitochondrial dysfunction, reactive oxygen species (ROS) production and DNA fragmentation, and increases number of acidic vacuoles. Mammea A/BA can induce apoptosis, autophagy and necrosis. Mammea A/BA can be used for researching chagas disease.
|
-
- HY-151281
-
|
|
TGF-β Receptor
|
Cancer
|
|
ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151275
-
|
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-151282
-
|
|
TGF-β Receptor
TGF-beta/Smad
|
Cancer
|
|
ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis.
|
-
- HY-103165
-
|
|
Adenosine Receptor
|
Cancer
Infection
|
|
PSB-0788 is a new selective high-affinity A2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases.
|
-
- HY-155300
-
|
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease.
|
-
- HY-44809A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Inflammation/Immunology
|
|
Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1).
|
-
- HY-148788
-
|
GBT-601; GBT-021601
|
Others
|
Others
|
|
Osivelotor is an allosteric modulator of haemoglobin S (HbS). Osivelotor can be used in the study of sickle cell disease (SCD).
|
-
- HY-N10487
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Bleformin A is a potent BChE inhibitor with an IC50 value of 5.2 μM. Bleformin A is a nature product that could be isolated from Bletilla striata. Bleformin A can be used for research of Alzheimer's disease (AD).
|
-
- HY-147135
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-3 (compound I-177) is a potent TEAD transcription factor inhibitor. TEAD-IN-3 can be used for the research of proliferative diseases (such as cancer) .
|
-
- HY-153011
-
-
- HY-N5077
-
|
|
Cholinesterase (ChE)
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-14399
-
|
CHF5074; CSP-1103
|
γ-secretase
Apoptosis
|
Neurological Disease
|
|
Itanapraced (CHF5074) is an orally active γ-secretase modulator and a non-steroidal anti-inflammatory derivative. Itanapraced reduces Aβ42 and Aβ40 secretion with IC50 values of 3.6 and 18.4 μM, respectively. Itanapraced inhibits cell apoptosis of hippocampal neurons induced by oxygen and glucose deprivation (OGD). Itanapraced can be used for the research of Alzheimer's disease.
|
-
- HY-145640
-
|
AZD4721; RIST4721
|
CXCR
|
Inflammation/Immunology
|
|
Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.
|
-
- HY-116541
-
|
ASM
|
Fungal
Bacterial
|
Infection
|
|
Acibenzolar-S-methyl (ASM) is a plant resistance inducer that mimics pathogen-host interactions and leads to systemic acquired resistance in plants. Acibenzolar-S-methyl helps reduce the use of pesticides and can be used in research to prevent plant diseases.
|
-
- HY-P3845
-
|
|
Amyloid-β
|
Neurological Disease
|
|
(Gly22)-Amyloid β-Protein (1-42) is a peptide fragment of amyloid β-protein (Aβ). Amyloid β-protein is the primary component of both vascular and parenchymal amyloid deposits in Alzheimer's disease. Mutation of Glu22 to Gly22 in Aβ can increase aggregation.
|
-
- HY-146757
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases.
|
-
- HY-147527
-
|
|
CDK
|
Inflammation/Immunology
|
|
CDK8-IN-5 is a potent CDK8 inhibitor with an IC50 of 72 nM. CDK8-IN-5 shows anti-inflammatory activities with 43% IL-10 enhancement rate. CDK8-IN-5 has the potential for the research of inflammatory bowel disease.
|
-
- HY-143615
-
|
|
RET
|
Cancer
|
|
RET-IN-10 is a potent inhibitor of RET. RET loss of function mutations leads to Hirschsprung's disease, while its gain of function mutations is associated with a variety of human tumors. RET-IN-10 has the potential for the research of cancer diseases (extracted from patent WO2021135938A1, compound 18).
|
-
- HY-150205
-
|
|
Others
|
Inflammation/Immunology
|
|
Succinate/succinate receptor antagonist 1 (compound 7a) is a succinate/succinate receptor antagonist. Succinate/succinate receptor antagonist 1 blocks succinate signaling in gingival tissue. Succinate/succinate receptor antagonist 1 inhibits the activation of succinate receptor 1 (SucnRl) with an IC50 value of 20 μΜ. Succinate/succinate receptor antagonist 1 can be used for the research of periodontal disease.
|
-
- HY-14280A
-
|
|
COMT
|
Neurological Disease
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone sodium salt can be used for the research of Parkinson's disease. Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-146272
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
Vasopressin V2 receptor antagonist 1 (Compound 4g) is a vasopressin V2 receptor (V2R) antagonist with a Ki of 3.8 nM. Vasopressin V2 receptor antagonist 1 can be used for autosomal dominant polycystic kidney disease (ADPKD) research.
|
-
- HY-N0702
-
|
|
Beta-secretase
Cholinesterase (ChE)
|
Neurological Disease
|
|
Tenuifolin is a triterpene isolated from Polygala tenuifolia Willd, has neuroprotective effects. Tenuifolin reduces Aβ secretion by inhibiting β-secretase. Tenuifolin improves learning and memory in aged mice by decreasing AChE activity and has the potential for Alzheimer’s disease (AD) treatment.
|
-
- HY-13204
-
|
KL 373 hydrochloride
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden hydrochloride has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-135825
-
|
|
Autophagy
|
Neurological Disease
|
|
TFEB activator 1 is an orally effective, mTOR-independent activator of TFEB. TFEB activator 1 significantly promotes the nuclear translocation of Flag-TFEB with an EC50 of 2167 nM. TFEB activator 1 enhances autophagy without inhibiting the mTOR pathway and has the potential for neurodegenerative diseases treatment.
|
-
- HY-13204A
-
|
KL 373
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. Biperiden has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-144619
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
|
-
- HY-131728
-
-
- HY-139560
-
-
- HY-136449
-
-
- HY-147321
-
|
|
Tau Protein
HBV
|
Infection
Neurological Disease
|
|
3'-DMTr-dG(iBu) is a nucleoside for the synthesis of nucleic acid, such as antiviral agents used in the research of viral infection (HBV, HDV), and oligonucleotides against Alzheimer’s disease and other tauopathies.
|
-
- HY-B0972
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Cinchophen is a potent and orally active non-steroidal anti-inflammatory agent, has analgesic and antimicrobial effects. Cinchophen can be used for the research of arthritis and some liver diseases.
|
-
- HY-P3709A
-
|
|
E1/E2/E3 Enzyme
|
Neurological Disease
|
|
TRAF6 peptide TFA is a specific TRAF6-p62 inhibitor. TRAF6 peptide TFA potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide TFA has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
|
-
- HY-N7887
-
-
- HY-N5077B
-
|
|
Cholinesterase (ChE)
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-P9967
-
|
BIIB037
|
Amyloid-β
|
Neurological Disease
|
|
Aducanumab (BIIB037), a human monoclonal antibody selective for aggregated forms of amyloid beta (Aβ). Aducanumab shows brain penetration, and can be used for Alzheimer's disease (AD) research.
|
-
- HY-113643
-
|
|
Calcium Channel
5-HT Receptor
|
Neurological Disease
|
|
Levemopamil hydrochloride is a blood-brain barrier penetrable calcium channel blocker and a 5-HT2 antagonist. Levemopamil hydrochloride can be used for temporary occlusion and neurological disease research.
|
-
- HY-153224
-
|
|
IRAK
|
Inflammation/Immunology
|
|
GLPG2534 is an orally active and selective IRAK4 inhibitor, with IC50 values of 6.4 nM and 3.5 nM for human and mouse IRAK4. GLPG2534 can be used for the research of inflammatory skin diseases.
|
-
- HY-N4113
-
|
|
Keap1-Nrf2
AMPK
|
Cancer
|
|
Glycycoumarin is a potent antispasmodic agent. Glycycoumarin is a major bioactive coumarin of licorice and exhibits antispasmodic activity. Glycycoumarin also has hepatoprotective effect. Glycycoumarin can be used for the research of abdominal pain and liver diseases.
|
-
- HY-151389
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-14 (compound 19c) is a selective butyrylcholinesterase (BChE) inhibitor with IC50s of 0.23 and 0.011 μM for eqBChE and hBChE, respectively. BChE-IN-14 shows good blood brain barrier permeation and primary cell safety. BChE-IN-14 is able to restore cognitive impairment in vivo, it can be used for the research of Alzheimer’s disease.
|
-
- HY-17368
-
|
S-Rivastigmine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-N7560
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
Neurological Disease
|
|
Safranal is an orally active main component of Saffron (Crocus sativus) and is responsible for the unique aroma of this spice. Safranal has neuroprotective and anti-inflammatory effects and has the potential for Parkinson’s disease research.
|
-
- HY-N11641
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Methyl ganoderate A acetonide, a lanostane triterpene, is a natural product that could be isolated from the fruiting bodies of Ganoderma lucidum. Methyl ganoderate A acetonide is a potent AChE inhibitor with an IC50 value of 18.35 μM. Methyl ganoderate A acetonide can be used in research of Alzheimer’s disease (AD).
|
-
- HY-109052
-
|
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment.
|
-
- HY-N3734
-
|
|
Beta-secretase
Phosphatase
|
Neurological Disease
|
|
Deoxyneocryptotanshinone, a natural tanshinone, is a high affinity BACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research.
|
-
- HY-U00341
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
ST4206 is a potent and orally active adenosine A2A receptor antagonist, with Kis of 12 nM and 197 nM for adenosine A2A receptor and adenosine A1 receptor, respectively. ST4206 has the potential for Parkinson׳s disease research.
|
-
- HY-P99471
-
|
UCB 0107
|
Tau Protein
|
Neurological Disease
|
|
Bepranemab (UCB 0107) is a humanized, full-length IgG4 monoclonal antibody that binds to a central tau epitope (amino acids 235-250). Bepranemab can be used for Alzheimer’s disease (AD) research.
|
-
- HY-66010
-
|
MD-67350
|
Calcium Channel
|
Cardiovascular Disease
|
|
Cinepazide Maleate (MD-67350) is a piperazine derivative and acts as a weak calcium channel blocker. Cinepazide Maleate is a potent vasodilator and can be used for the research of cerebrovascular diseases, including ischemic stroke, brain infarct et. al.
|
-
- HY-N8730
-
|
|
Others
|
Neurological Disease
|
|
7,8,3 ',4 '-Tetramethoxyflavone is an extract
isolated from natural pomegranate juice and seeds. 7,8,3 ',4' -Tetramethoxyflavone has a protective effect on the neurotoxicity of
paraquat-induced Parkinson's disease mouse model .
|
-
- HY-14280
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders.
|
-
- HY-149287
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC50 values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease.
|
-
- HY-149340
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
PD07 is an orally active AChE inhibitor (IC50: 0.29 μM for hAChE). PD07 also inhibits ChEs, BACE1 (IC50: 13.42 μM), and Aβ1–42 aggregation in in vitro. PD07 is an antioxidant, and shows DPPH inhibitory activity (IC50: 26.46 μM). PD07 improves memory and cognition in Scopolamine (HY-N0296)-induced amnesia rats. PD07 can be used for research of Alzheimer’s disease.
|
-
- HY-P3247
-
|
|
Insulin Receptor
|
Metabolic Disease
Neurological Disease
|
|
[D-Ala2]-GIP (human) is a GIP receptor agonist. [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
|
-
- HY-15545
-
-
- HY-146344
-
|
|
Antibiotic
|
Infection
|
|
Antiviral agent 17 (Compound 4) is an anti-infection agent. Antiviral agent 17 retains its antiviral effect in a human replicon assay (EC50 = 0.015 μM). Antiviral agent 17 results in good antiviral activity against murine norovirus. Antiviral agent 17 has the potential for the research of infectious and malignant diseases.
|
-
- HY-151952
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-12 is a specific NLRP3 inflammasome inhibitor. NLRP3-IN-12 reduces the release of IL-1β by targeting the NLRP3 protein, with an IC50 of 0.45 μM. NLRP3-IN-12 can be used for the research of inflammatory bowel disease.
|
-
- HY-149006
-
|
|
DAPK
|
Inflammation/Immunology
Cancer
|
|
CK156 is a highly selective death-associated protein kinase (DAPK) inhibitor with IC50s of 182 nM,34 μM, and 39 μM in the DRAK1 NanoBRET assay for DRAK1, CK2a1, and CK2a2, respectively. CK156 can be used for the research of autoimmune and inflammatory diseases.
|
-
- HY-114231B
-
|
ELX-02 disulfate; NB-124 disulfate
|
Others
|
Metabolic Disease
|
|
Exaluren (ELX-02) disulfate is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). Exaluren disulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
|
-
- HY-150058
-
|
|
Others
|
Neurological Disease
|
|
Bocconoline is a potent early endosome antigen 1 (EEA1) inhibitor. Bocconoline can be isolated from Macleaya cordata. Bocconoline can be used for the research of Parkinson’s disease (PD).
|
-
- HY-114231C
-
|
ELX-02 sulfate; NB-124 sulfate
|
Others
|
Metabolic Disease
|
|
Exaluren (ELX-02) sulfate is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). Exaluren sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.
|
-
- HY-103308
-
|
|
Potassium Channel
|
Neurological Disease
|
|
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
|
-
- HY-B0247
-
|
Torasemide
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
Torsemide (Torasemide) is an orally active loop diuretic. Torsemide has anti-aldosterone and vasodilatory effects. Torsemide also can be used for the research of heart failure, renal disease and hepatic cirrhosis.
|
-
- HY-120577
-
|
|
Others
|
Cardiovascular Disease
|
|
BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitory activity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF).
|
-
- HY-124609
-
|
|
Dopamine Transporter
Monoamine Oxidase
|
Neurological Disease
|
|
CAD031 is a derivative of the Alzheimer's disease (AD) targeting agent J147 (HY-13779) with neuroprotective and memory-enhancing properties. CAD031 enhances memory in mice, improves dendritic structure, and stimulates cell division in the germinal zone of the brain in aged mice. CAD031 is more active than J147 in human neural stem cell assays.
|
-
- HY-137472
-
|
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-142670
-
|
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-5 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-5 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 32).
|
-
- HY-142669
-
|
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-4 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-4 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2021228159A1, compound 38).
|
-
- HY-P1051
-
|
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (12-28) (Amyloid β-Protein (12-28)) is a peptide fragment of β-amyloid protein (β1-42). β1-42, a 42 amino acid protein , is the major component of senile plaque cores. β-Amyloid (12-28) shows aggregation properties. β-Amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-N1428C
-
|
Iron(III) citrate; Zerenex
|
Antibiotic
Reactive Oxygen Species
|
Metabolic Disease
|
|
Ferric citrate (Iron(III) citrate), an orally active iron supplement, is an efficacious phosphate binder. Ferric citratee can be used for iron deficiency anemia and chronic kidney disease (CKD) research.
|
-
- HY-149859
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions.
|
-
- HY-N1179
-
|
|
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Tanshinone IIB is a major active constituent of the roots of Salvia miltiorrhiza (Danshen) widely used for the research of stroke and coronary heart disease in Asian countries. Tanshinone IIB has a neuroprotective effect via inhibition of apoptosis.
|
-
- HY-N3702
-
|
|
Syk
|
Inflammation/Immunology
|
|
Dehydroabietinol is an abietane diterpenoid. Dehydroabietinol has kinase inhibition activity for spleen tyrosine kinase (SYK) with an IC50 value of 46.4 μM. Dehydroabietinol can be used for the research of immune-mediated disease.
|
-
- HY-14202
-
|
Ro 19-6327 hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-14201
-
|
Ro 19-6327
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-12176B
-
|
CGP 60536 fumarate; CGP60536B fumarate; SPP 100 fumarate
|
Renin
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Aliskiren fumarate is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren fumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-12176
-
|
CGP 60536; CGP60536B; SPP 100
|
Renin
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Aliskiren is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-153452
-
|
|
Ser/Thr Protease
|
Cardiovascular Disease
|
|
PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research.
|
-
- HY-149243
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-16 (compound 87) is a highly potent BChE inhibitor with an IC50 of 3.8 nM for hBChE. BChE-IN-16 has low cytotoxicity, potential CNS permeability, unique adaptability and can be used in Alzheimer's disease (AD) research.
|
-
- HY-111263
-
|
|
Amyloid-β
|
Neurological Disease
|
|
NIAD-4 is a fluorophore for optical imaging of amyloid-β (Aβ) in the central nervous system (CNS) for Alzheimer’s disease (AD). NIAD-4 binds to the same Aβ site with the binding affinity (Ki) of 10 nM.
|
-
- HY-151388
-
|
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
|
hMAO-B/MB-COMT-IN-1 is a dual MAO-B/MB-COMT inhibitor (IC50s: 2.5 μΜ for hMAO-B, 3.84 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-1 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-1 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD).
|
-
- HY-151390
-
|
|
Monoamine Oxidase
COMT
|
Neurological Disease
|
|
hMAO-B/MB-COMT-IN-2 is a dual MAO-B/MB-COMT inhibitor (IC50s: 4.27 μΜ for hMAO-B, 2.69 μΜ for MB-COMT). hMAO-B/MB-COMT-IN-2 protects cells against oxidative damage. hMAO-B/MB-COMT-IN-2 can be used in the research of neurodegeneration disease, such as Parkinson’s Disease (PD).
|
-
- HY-14179
-
PPQ-102
3 Publications Verification
CFTR Inhibitor
|
CFTR
|
Others
|
|
PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease.
|
-
- HY-153245
-
|
|
Btk
|
Cancer
Inflammation/Immunology
|
|
JNJ-64264681 is a potent, orally active, selective and irreversible covalent BTK inhibitor. JNJ-64264681 exhibits good pharmacokinetic characteristics and can be used for cancer and autoimmune diseases research.
|
-
- HY-147529
-
|
|
mGluR
|
Neurological Disease
|
|
mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice.
|
-
- HY-18137
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
|
-
- HY-P4911
-
|
|
CXCR
|
Cardiovascular Disease
|
|
SDF-1α (human) is a mononuclear cells chemoattractant that can bind to CXCR4. SDF-1α plays a central role in stem cell homing, retention, survival, proliferation, cardiomyocyte repair, angiogenesis and ventricular remodelling following myocardial infarction. SDF-1α (human) can be used in cardiovascular disease research.
|
-
- HY-148092
-
|
|
STAT
|
Cancer
Inflammation/Immunology
|
|
PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research[1].
|
-
- HY-156994
-
|
|
Others
|
Others
|
|
ASGPR ligand-1 is an asialoglycoprotein receptor (ASGPR) ligand compound. ASGPR ligand-1 can be used for kinds of diseases research.
|
-
- HY-116228
-
|
Caderofloxacin; CS-940
|
Bacterial
|
Infection
|
|
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases.
|
-
- HY-153593
-
|
|
Epigenetic Reader Domain
|
Cancer
|
BET bromodomain inhibitor 3 is BET bromodomain inhibitor. BET bromodomain inhibitor 3 has inhibitory effect against BrdT with Ki value of > 40 µM. BET bromodomain inhibitor 3 can be used for the research of contraception, cancer, and heart disease.
|
-
- HY-126362
-
|
|
Glucosidase
|
Others
|
|
ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease.
|
-
- HY-117661
-
|
|
SRPK
VEGFR
|
Cancer
Cardiovascular Disease
|
|
SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease.
|
-
- HY-11044
-
|
|
Histamine Receptor
|
Endocrinology
Inflammation/Immunology
Neurological Disease
|
|
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. PF-03654746 Tosylate reduces allergen-induced nasal symptoms. PF-03654746 Tosylate has potential for treatment of human cognitive disorders, improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD).
|
-
- HY-138281
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.
|
-
- HY-144032
-
|
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-9 (Compound 26) is a selective Tyk-2 inhibitor with IC50s of 0.076 and 1.8 nM for TYK2-JH2 and JAK1-JH2, respectively. Tyk2-IN-9 can be used for the research of inflammatory or autoimmune disease.
|
-
- HY-11017
-
|
ENA 713; SDZ-ENA 713
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Rivastigmine tartrate (ENA 713; SDZ-ENA 713) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively. Rivastigmine tartrate can pass the blood brain barrier (BBB). Rivastigmine tartrate is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease.
|
-
- HY-145428
-
|
|
Notch
γ-secretase
|
Cancer
|
|
BT-GSI is a γ-secretase inhibitor (GSI) and a bone-targeted Notch inhibitor. BT-GSI has dual anti-myeloma and anti-resorptive properties, which can be used for the research of multiple myeloma and associated bone disease. BT-GSI inhibits tumor growth and osteolytic disease progression.
|
-
- HY-148071
-
|
|
Others
|
Others
|
|
Epocholeone is a growth regulator. Epocholeone can control fungal or physiological diseases of crops.
|
-
- HY-146033
-
|
|
HPV
|
Cancer
|
|
HPV18-IN-1 (Compound H1) is a potent inhibitor of HPV18. HPV18-IN-1 prevents cervical cancer cells from premature cell procession and abnormal proliferation. HPV18-IN-1 supresses E7-Rb-E2F cellular pathway and DNA methylation. HPV18-IN-1 has the potential for the research of cancer diseases.
|
-
- HY-142779
-
|
|
Phospholipase
|
Metabolic Disease
Neurological Disease
|
|
Lp-PLA2-IN-11 is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Lp-PLA2 previously known as platelet- activating factor acetylhydrolase (PAF-AH), is a phospholipase A2 enzyme involved in hydrolysis of lipoprotein lipids or phospholipids. Lp-PLA2-IN-11 has the potential for the research of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease (extracted from patent WO2014114249A1, compound E145).
|
-
- HY-13733
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Procarbazine Hydrochloride is an orally active alkylating agent, with anticancer activity. Procarbazine Hydrochloride can be used in Hodgkin's disease research.
|
-
- HY-13733A
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Procarbazine is an orally active alkylating agent, with anticancer activity. Procarbazine can be used in Hodgkin's disease research.
|
-
- HY-144270
-
-
- HY-P1051A
-
|
Amyloid β-Protein (12-28) (TFA); Amyloid Beta-Peptide (12-28) (human) TFA; β-Amyloid protein fragment(12-28) TFA
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (12-28) (TFA) (Amyloid β-Protein (12-28) (TFA)) is a peptide fragment of β-amyloid protein (β1-42). β1-42, a 42 amino acid protein , is the major component of senile plaque cores. β-Amyloid (12-28) (TFA) shows aggregation properties. β-Amyloid (12-28) (TFA) has the potential for Alzheimer’s disease research.
|
-
- HY-B1487
-
|
Tricyclamol hydrochloride; (±)-Procyclidine hydrochloride
|
iGluR
mAChR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol, (±)-Procyclidine) hydrochloride , an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine hydrochloride can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-B1487A
-
|
Tricyclamol; (±)-Procyclidine
|
mAChR
iGluR
|
Neurological Disease
|
|
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy.
|
-
- HY-N12408
-
|
lyso-Gb3
|
Others
Calcium Channel
|
Cancer
|
|
Globotriaosylsphingosine (lyso-Gb3) inhibits the growth of fibroblasts, as well as their differentiation into myofibroblasts, and collagen expression. Globotriaosylsphingosine can be used for Fabry disease research.
|
-
- HY-157033
-
-
- HY-144324
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-6 (Compound 12a) is an optimal multifunctional ligand with significant inhibition of AChE (EeAChE, IC50 = 0.20 μM; HuAChE, IC50 = 37.02 nM) and anti-Aβ activity (IC50 = 1.92 μM for self-induced Aβ1-42 aggregation; IC50 = 1.80 μM for disaggregation of Aβ1-42 fibrils; IC50 = 2.18 μM for Cu2+-induced Aβ1-42 aggregation; IC50 = 1.17 μM for disaggregation of Cu2+-induced Aβ1-42 fibrils). AChE-IN-6 has the potential for the research of Alzheimer's disease.
|
-
- HY-146035
-
|
|
Cholinesterase (ChE)
Histamine Receptor
|
Neurological Disease
|
|
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease.
|
-
- HY-103033
-
|
|
Parasite
|
Infection
|
|
T.cruzi-IN-1 is a potent Trypanosoma cruzi inhibitor with an IC50 of 8 nM. T.cruzi-IN-1, a 4-trifluoromethyl substituted analog, has the potential for both the acute and chronic stages of Chagas disease.
|
-
- HY-144316
-
|
|
Cholinesterase (ChE)
GSK-3
|
Neurological Disease
|
|
ZLWH-23 is a selective AChE inhibitor (IC50=0.27 μM) with GSK-3β inhibitory property (IC50=6.78 μM). ZLWH-23 possesses selectivity for AChE over BChE (IC50=20.82 μM) and for GSK-3β over multi-kinases. ZLWH-23 has the potential for the research of Alzheimer's disease.
|
-
- HY-142059
-
-
- HY-148141
-
|
|
Complement System
|
Inflammation/Immunology
|
|
JPE-1375 is a complement C5a receptor 1 (C5aR1) antagonist. JPE-1375 effectively inhibits polymorphonuclear leukocyte mobilization (EC50=6.9 µM) and reduces TNF levels (EC50=4.5 µM) in mice. JPE-1375 can be used in studies of autoimmune and inflammatory diseases.
|
-
- HY-144087
-
|
|
JAK
|
Inflammation/Immunology
|
|
TYK2-IN-11 (Compound 5B) is a selective Tyk-2 inhibitor with IC50s of 0.016 and 0.31 nM for TYK2-JH2 and JAK1-JH2, respectively. TYK2-IN-11 can be used for the research of inflammatory or autoimmune disease.
|
-
- HY-153189
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research.
|
-
- HY-153904
-
|
|
Casein Kinase
|
Neurological Disease
|
|
Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM. Casein kinase 1δ-IN-5 shows neuroprotective and anti-inflammatory properties both in vitro. Casein kinase 1δ-IN-5 has the potential for neurodegenerative diseases research.
|
-
- HY-107901
-
|
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
|
-
- HY-122052
-
|
|
Others
|
Metabolic Disease
|
|
UK‑396082 is a potent thrombin activated fibrinolytic inhibitor (TAFI) inhibitor. UK‑396082 increases plasmin activity and induces a parallel decrease in ECM levels. UK‑396082 can be used in research of chronic kidney disease (CKD).
|
-
- HY-B1015
-
|
Ethosalamide
|
Others
|
Inflammation/Immunology
|
|
Etosalamide (Ethosalamide) is an antipyretic and analgesic agent. Etosalamide has anti-inflammatory activity and can be used for allergic disease research.
|
-
- HY-113616A
-
|
|
mAChR
|
Neurological Disease
|
|
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor with an EC50 of 0.11 μM. VU0364572 TFA has neuroprotective potential for preventing memory impairments and reducing neuropathology in Alzheimer’s Disease. VU0364572 TFA is CNS penetrant.
|
-
- HY-12282
-
|
|
LRRK2
|
Neurological Disease
|
|
GNE-9605 is a potent, orally active, selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor with an IC50 value of 18.7 nM. GNE-9605 inhibits LRRK2 Ser1292 autophosphorylation. GNE-9605 can be used in research of Parkinson's disease (PD) .
|
-
- HY-120970
-
|
|
Cholinesterase (ChE)
GABA Receptor
iGluR
|
Neurological Disease
|
|
Bis(7)-tacrine dihydrochloride is a dimeric AChE inhibitor derived from tacrine. Bis(7)-tacrine dihydrochloride prevents glutamate-induced neuronal apoptosis by blocking NMDA receptors. Bis(7)-tacrine dihydrochloride is a potent GABAAreceptor antagonist. Bis(7)-tacrine dihydrochloride has the potential for the research of Alzheimer's disease .
|
-
- HY-13204B
-
|
KL 373 lactate
|
mAChR
|
Neurological Disease
|
|
Biperiden (KL 373) lactate is an orally active non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors. Biperiden (KL 373) lactate inhibits acetylcholine and enhances dopamine signaling in the central nervous system. Biperiden (KL 373) lactate has the potential for the research of Parkinson's disease and other related psychiatric disorders.
|
-
- HY-N10701
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-11 (compound 1) is a potent is a dual AChE and BChE inhibitor with IC50 values of 70 and 71 μM for AChE and BChE, respectively. AChE/BChE-IN-11 is a natural product that could be isolated from the leaf of artichoke . AChE/BChE-IN-11 can be used in research of Alzheimer’s disease (AD) research.
|
-
- HY-137122
-
|
|
PIN1
|
Inflammation/Immunology
|
|
3-Pyridine toxoflavin (compound 49) is a PIN1 inhibitor. 3-Pyridine toxoflavin can be used for the research of immune disease proliferative disorder.
|
-
- HY-155487
-
|
|
ROR
|
Inflammation/Immunology
Neurological Disease
|
|
JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research.
|
-
- HY-10563
-
|
MCI-9042 free acid
|
5-HT Receptor
|
Infection
|
|
Sarpogrelate (MCI-9042) is a new, specific orally active 5-HT2 receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.
|
-
- HY-148068
-
|
|
STING
|
Cancer
Inflammation/Immunology
|
|
STING agonist-20 (compound 95) is a potent STING agonist used in the synthesis of XMT-2056. STING agonist-20 can be used as a vaccine adjuvant in the study of cancer and other inflammatory, immune diseases.
|
-
- HY-120274
-
-
- HY-W001601
-
|
|
iGluR
|
Neurological Disease
|
|
Budipine is an anti-parkinson agent. Budipine also is a substrate of P-glycoprotein (P-gp), is mediated the uptake into the brain by P-gp. Budipine also is N-methyl-d-aspartate (NMDA) antagonist, and has indirect dopaminergic effects through an improved dopamine release, the inhibition of monoamine oxidase type B (MAO-B). Budipine can be used for the research of CNS disorders include Parkinson disease.
|
-
- HY-70069
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.
|
-
- HY-151928
-
|
|
JNK
|
Neurological Disease
|
|
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitory activities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease.
|
-
- HY-145581
-
|
AZD4831
|
Glutathione Peroxidase
|
Cardiovascular Disease
|
|
Mitiperstat (AZD4831) is the potent inhibitor of myeloperoxidase (MPO). Mitiperstat is particularly useful in the research of prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions (extracted from patent US20160152623A1).
|
-
- HY-B0189
-
|
TAK-370; AS-4370
|
5-HT Receptor
Cytochrome P450
Potassium Channel
|
Neurological Disease
Cancer
|
|
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
|
-
- HY-B0189A
-
|
TAK-370 citrate; AS-4370 citrate
|
5-HT Receptor
Potassium Channel
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
|
-
- HY-151152
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).
|
-
- HY-10035
-
|
T-Type calcium channel inhibitor
|
Calcium Channel
|
Neurological Disease
|
|
TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
|
-
- HY-144669
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-144671
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-142777
-
|
|
Phospholipase
|
Neurological Disease
|
|
Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research.
|
-
- HY-142774
-
|
|
Phospholipase
|
Neurological Disease
|
|
Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research.
|
-
- HY-A0270
-
|
|
Others
|
Neurological Disease
|
|
Diphenidol is an orally active antiemetic. Diphenidol reduces abnormal neuropathic pain and TNF-α overexpression in rats following chronic compression injury. Diphenidol also has local anaesthetic activity and inhibits sodium currents. Diphenidol can be used in studies of meniere′s disease, anti-vertigo, antiemetic and analgesia.
|
-
- HY-109001A
-
|
(1S,2R)-ABT-957
|
Proteasome
|
Neurological Disease
|
|
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM.
|
-
- HY-12176A
-
|
CGP 60536 hydrochloride; CGP60536B hydrochloride; SPP 100 hydrochloride
|
Renin
Autophagy
|
Cancer
Cardiovascular Disease
|
|
Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hydrochloride can be used for the research of hypertension, cardiovascular diseases and cancer cachexia -.
|
-
- HY-144266
-
|
|
Glucosylceramide Synthase (GCS)
|
Metabolic Disease
Neurological Disease
|
|
Glucosylceramide synthase-IN-1 (T-036) a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 31 nM and 51 nM for human GCS and mouse GCS, respectively. Glucosylceramide synthase-IN-1 can be used for Gaucher's disease research.
|
-
- HY-146346
-
|
|
PROTACs
HDAC
|
Inflammation/Immunology
|
|
HD-TAC7 is a potent PROTAC HDAC degrader with IC50 values of 3.6 μM, 4.2 μM and 1.1 μM for HDAC1, HDAC2 and HDAC3, respectively. HD-TAC7 can decreases NF-κB p65 in RAW 264.7 macrophages. HD-TAC7 can be used for the research of inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD).
|
-
- HY-P3761
-
|
|
Caspase
|
Others
|
|
Ac-Tyr-Val-Lys-Asp-aldehyde is a caspase-1 inhibitor, can be used for disease research including anemia-associated to chronic diseases, chemotherapy-induced anemia and Diamond-Blackfan anemia.
|
-
- HY-10469
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease.
|
-
- HY-151483
-
|
|
Histone Demethylase
|
Cardiovascular Disease
|
|
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease.
|
-
- HY-146151
-
|
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
γ-Secretase modulator 12 (Compound 1a) is a γ-secretase modulator that can selectively decrease amyloid-β42 (Aβ42) levels (IC50 of 0.39 µM). γ-Secretase modulator 12 can be used for Alzheimer’s disease research. γ-Secretase modulator 12 has a good brain/plasma ratio (Kp, brain = 0.72) in mice.
|
-
- HY-N10384
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-17 (compound 1) is a potent AChE inhibitor with an IC50 value of 28.98 μM. AChE-IN-17 can significantly prevent H2O2-induced PC12 cell death, exhibiting excellent neuroprotective effect. AChE-IN-17 can be used for researching neurodegenerative diseases (NDs).
|
-
- HY-155773
-
|
|
FAAH
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
VU534 is a NAPE-PLD activator, with an EC50 of 0.30 μM. VU534 is dual inhibitors of FAAH and sEH (IC50 of 1.2 μM). VU534 increases efferocytosis in a NAPE-PLD dependent manner. VU534 has the potential for cardiometabolic diseases study [1] .
|
-
- HY-143438
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research.
|
-
- HY-115910
-
|
|
Cholinesterase (ChE)
Interleukin Related
|
Neurological Disease
|
|
Y13g is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals.
|
-
- HY-124729
-
|
|
ULK
Autophagy
|
Neurological Disease
|
|
BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment.
|
-
- HY-152112
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE/MAO-B-IN-2 is a potent AChE, BChE, and MAO-B enzymes inhibitor with IC50 values of 48.2 nM, 83.9 nM, and 31.2 nM, respectively. AChE/BChE/MAO-B-IN-2 has significant antioxidant activity, and can be used for Parkinson’s disease research.
|
-
- HY-115910A
-
|
|
Cholinesterase (ChE)
Interleukin Related
|
Neurological Disease
|
|
Y13g dihydrochloride is the potent inhibitor of both AChE and IL-6. Interleukin-6 (IL-6) and acetylcholinesterase (AChE) are two important targets implicated in progression of Alzheimer's Disease (AD). Y13g dihydrochloride reverses the STZ-induced memory deficit, and shows histopathology similarly as in normal animals.
|
-
- HY-B0384
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Temocapril hydrochloride is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril hydrochloride can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
|
-
- HY-100713
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Temocapril is an orally active angiotensin-converting enzyme (ACE) inhibitor. Temocapril can be used for the research of hypertension, congestive heart failure, acute myocardial infarction, insulin resistance, and renal diseases.
|
-
- HY-125495
-
|
|
Others
|
Inflammation/Immunology
|
|
Telmesteine is an amucolitic agent. Telmesteine has anti-protease activity. Telmesteine inhibits LPS-induced NO production in RAW264.7 cells. Telmesteine can be used for research of inflammation, such as acute and chronic bronchitis and obstructive airways disease.
|
-
- HY-123494
-
|
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
BRD0418 is a diversity-oriented synthesis (DOS) molecule that regulates the expression of tribbles pseudokinase 1. BRD0418 has the effect of causing hot lipoprotein metabolism from fat production to clearance. BRD0418 can be used in the study of coronary artery disease (CAD) .
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender specific neuroprotection in a Parkinson’s Disease rat model.
|
-
- HY-150069
-
|
|
Bcl-2 Family
Apoptosis
|
Metabolic Disease
|
|
UBX1325 is an Bcl-xL inhibitor that promotes apoptosis in senescent cells. UBX1325 is a potent anti-aging agent that can be used in studies of age-related eye diseases such as diabetic macular oedema (DME), age-related macular degeneration (AMD) and diabetic retinopathy (DR).
|
-
- HY-144373
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
IL-17 modulator 6 (compound 61) is a potent Interleukin 17 (IL-17) modulator (pIC50=9.1). IL-17 modulator 6 has the ability to inhibit IL-17 and can be used for the research of inflammatory and autoimmune diseases.
|
-
- HY-153905
-
|
|
Casein Kinase
|
Neurological Disease
|
|
Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
|
-
- HY-P1206
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. CH 275 acts as a potent and selective sst1 agonist (IC50=30.9 nM) and also displays IC50 values of 345 nM, >1 μM, >10 μM, >10 μM for human sst3, sst4, sst2 and sst5, respectively. CH 275 can be used for the research of alzheimer’s disease.
|
-
- HY-151488
-
|
|
Sirtuin
|
Cancer
Metabolic Disease
Neurological Disease
|
|
CypD-IN-4 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-4 has CypD affinity with an IC50 value of 0.057 μM. CypD-IN-4 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
|
-
- HY-151487
-
|
|
Sirtuin
|
Cancer
Metabolic Disease
Neurological Disease
|
|
CypD-IN-3 is a potent and subtype-selective cyclophilin D (CypD) inhibitor. CypD-IN-3 has CypD affinity with an IC50 value of 0.01 μM. CypD-IN-3 can be used for the research of several diseases including oxidative stress, neurodegenerative disorders, liver diseases, aging, autophagy and diabetes.
|
-
- HY-134968
-
|
|
Tau Protein
|
Neurological Disease
|
|
TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor with an IC50 of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies. TTBK1-IN-1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-136584
-
|
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
|
2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid is a ketone compound extracted from patent WO2002030860A2, compound example II-9. 2,2,14,14-Tetramethyl-8-oxopentadecanedioic acid can be used for the research of cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders.
|
-
- HY-143260
-
|
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 6 is a potent GSK-3β inhibitor with an IC50 value of 24.4 μM. GSK-3β inhibitor 6 shows high hepatocyte glucose uptake (38%). GSK-3β inhibitor 6 can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-D1168
-
|
|
Fluorescent Dye
|
Metabolic Disease
|
|
Oil Red O is a fat-soluble diazol dye, with a maximum absorption at 518 nm. Oil Red O stains neutral lipids and cholesteryl esters but not biological membranes. Oil Red O can be used for detecting and quantifying hepatic steatosis in mouse liver biopsies. Oil Red O staining efficiently helps to visualize the radical changes that occur in tissues as metabolic disease occurs and progresses.
|
-
- HY-149704
-
|
|
mAChR
|
Neurological Disease
|
|
M1/M2/M4 muscarinic agonist 1 (Compound 42) is a muscarinic M4/M1/M2 agonist with EC50 values of 6.5, 26 and 210 nM for M4/M1/M2, respectively. M1/M2/M4 muscarinic agonist 1 can be used for research on mental diseases, such as schizophrenia, delusion, etc.
|
-
- HY-W193545A
-
|
|
Others
|
Cancer
Inflammation/Immunology
|
|
EGR240 is a branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor. EGR240 can be used for the research of cancer, rheumatoid arthritis, and bone disease.
|
-
- HY-116100
-
-
- HY-100418
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-111 is a selective activator of potassium phannel KCa 3.1 , evokes KCa 3.1 membrane hyperpolarization in porcine endothelial cell. SKA-111 is capable of improving Bradykinin (HY-P0206)-induced coronary dilations in the isolated rat heart and can be used for cardiovascular disease research.
|
-
- HY-160002
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-27 (Compound 12c) is a monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-27 has potent and selective MAO-B inhibitory effect for hMAO-B with an IC50 values of 8.9 nM. MAO-B-IN-27 can be used for the research of parkinson's disease (PD).
|
-
- HY-N3383
-
|
Ligstroside
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
Ligustroside (Ligstroside), a secoiridoid derivative, has outstanding performance on mitochondrial bioenergetics in models of early Alzheimer's disease (AD) and brain ageing by mechanisms that may not interfere with Aβ production. Ligustroside significantly inhibits nitric oxide production in lipopolysaccharide-activated RAW264.7 macrophages.
|
-
- HY-125996
-
|
|
FXR
|
Inflammation/Immunology
|
|
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
|
-
- HY-P3410
-
|
|
SHP2
Phosphatase
|
Inflammation/Immunology
|
|
Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.
|
-
- HY-115744
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Mercaptoethylguanidine (MEG) dihydrobromide is selective inhibitor of the inducible nitric oxide synthase and peroxynitrite scavenger. Mercaptoethylguanidine (MEG) dihydrobromide has the potential for inflammatory bowel diseases research.
|
-
- HY-110237
-
|
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-B1365
-
-
- HY-12177
-
|
CGP 60536 hemifumarate; CGP60536B hemifumarate; SPP 100 hemifumarate
|
Renin
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
|
-
- HY-121765
-
|
N,S-Diacetyl-L-cysteine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Dacisteine (N,S-Diacetyl-L-cysteine) is a cysteine derivative and displays a less New Delhi metallo-beta-lactamase-1 (NDM-1) inhibitor with an IC50 value of 1000 μM. Dacisteine can be used for the treatment of cardiovascular and cerebrovascular diseases caused by platelet aggregation.
|
-
- HY-156438
-
|
|
NOD-like Receptor (NLR)
|
Neurological Disease
|
|
NT-0796 is a selective and CNS-penetrant NLRP3 inflammasome inhibitor with an IC50 of 0.32 nM in PBMC assay. NT-0796 is an isopropyl ester that undergoes intracellular conversion to NDT-19795, the carboxylic acid active species. NT-0796 has the potential for neuroinflammatory diseases research.
|
-
- HY-112678
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
TM6008 is a potent and orally active prolyl hydroxylase (PHD) inhibitor. TM6008 chelats transition metal (copper) and inhibits the autoxidation of ascorbic acid with an IC50 value is 0.57 μM. TM6008 exerts organ protection against ischemia in vivo and can be used for cerebrovascular disease research.
|
-
- HY-146405
-
|
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
nAChR antagonist 1 (compound B15) is an excellent α7 nAChR antagonist with an IC50 value of 3.3 μM. nAChR antagonist 1 can be used for researching schizophrenia, Alzheimer’s disease and inflammatory disorders.
|
-
- HY-147720A
-
|
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease.
|
-
- HY-143792
-
|
|
P-glycoprotein
|
Neurological Disease
|
|
HTT-D3 is a potent and orally active huntingtin (HTT) splicing modulator. HTT-D3 acts by promoting the inclusion of a pseudoexon containing a premature termination codon (stop-codon psiExon), leading to HTT mRNA degradation and reduction of HTT levels. HTT-D3 reduces p-glycoprotein (P-gp) efflux, and can be uesd for Huntington's disease research.
|
-
- HY-110279
-
|
|
GPR68
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive aliasing modulator (PAM) (pEC50=6.83) with a moderate antagonistic effect on A2A (Ki=220 nM). Ogerin inhibits the fear conditioning reflex in mice and also inhibits TGF-β-induced myofibroblast differentiation of fibroblasts from multiple organ systems. Ogerin can be used in the studies of fibrotic diseases and neurological disorders.
|
-
- HY-D0205A
-
-
- HY-44809
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
|
-
- HY-B0520A
-
|
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
Neurological Disease
|
|
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
|
-
- HY-144031S
-
-
- HY-117516
-
|
|
REV-ERB
|
Metabolic Disease
Neurological Disease
|
|
SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has high affinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders.
|
-
- HY-155774
-
|
|
Phospholipase
|
Metabolic Disease
|
|
APE-PLD (VU533) activator is a potent NAPE-PLD activator with an EC50 value of 0.30 µM. NAPE-PLD activator (VU533) can enhance NAPE-PLD activity and increase efferocytosis by macrophages. NAPE-PLD activator (VU533) can be used for cardiometabolic diseases research.
|
-
- HY-108828
-
|
rhGAA
|
Others
|
Others
|
|
Alglucosidase alfa is a hydrolytic lysosomal glycogen-specific recombinant human α-glucosidase product. Alglucosidase alfa can be used for Pompe disease research.
|
-
- HY-113489
-
|
14,15-EET
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
14,15-Epoxyeicosatrienoic acid (14,15-EET) is a metabolite of Arachidonic acid (HY-109590). 14,15-Epoxyeicosatrienoic acid is a potent inhibitor of in vivo platelet aggregation. 14,15-Epoxyeicosatrienoic acid facilitates astrocytic Aβ clearance. 14,15-Epoxyeicosatrienoic acid can be used for Alzheimer's Disease research.
|
-
- HY-18679
-
|
|
mGluR
|
Neurological Disease
|
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-137451A
-
|
(E/Z)-S-600918
|
P2X Receptor
|
Inflammation/Immunology
|
|
(E/Z)-Sivopixant ((E/Z)-S-600918) is a potent P2X3 receptor antagonist with an IC50 of 4 nM. (E/Z)-Sivopixant can be used for respiratory diseases research.
|
-
- HY-143726
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-8 (example 16), an aminoimidazopyridine, is a potent and selective RIPK1 inhibitor with an IC50 of 4 nM. RIPK1-IN-8 has the potential for inflammatory diseases research.
|
-
- HY-B0202A
-
|
SR-47436 hydrochloride; BMS-186295 hydrochloride
|
Angiotensin Receptor
Apoptosis
|
Metabolic Disease
Neurological Disease
|
|
Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.
|
-
- HY-120947
-
|
|
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-111262
-
|
|
11β-HSD
|
Metabolic Disease
Neurological Disease
|
|
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-107676
-
|
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-N10317
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Toddacoumalone is a natural inhibitor of phosphodiesterase 4 (PDE4) with moderate potency and imperfect agent-like properties. Toddacoumalone has the potential for the research of inflammatory diseases such as psoriasis.
|
-
- HY-16640
-
|
|
JAK
|
Inflammation/Immunology
|
|
TCJL37 is a potent, selective, and orally bioavailable TYK2 inhibitor with a Ki of 1.6 nM. TCJL37 can be used for the research of inflammatory bowel diseases (IBD).
|
-
- HY-122066
-
|
|
Others
|
Infection
|
|
NSC47924 is a laminin receptor (LR) inhibitor. NSC47924 affects 37/67 kDa LR cell surface localization and interaction with the cellular prion protein. NSC47924 can be used for testing prion diseases.
|
-
- HY-B2089
-
-
- HY-115986
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD).
|
-
- HY-148096
-
|
|
STAT
|
Cancer
Inflammation/Immunology
|
|
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer.
|
-
- HY-W281862
-
-
- HY-116815
-
|
|
Bacterial
|
Infection
Neurological Disease
|
|
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.
|
-
- HY-149235
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-12 (compound 13) is a PI3Kδ inhibitor (pIC50 = 5.8), with pKi values of 8.0/6.5/6.4/6.7 for PI3Kδ/γ/β/α, respectively. PI3Kδ-IN-12 can be used in the study of chronic respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD).
|
-
- HY-145430
-
|
|
Interleukin Related
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
IL-17A modulator-1 is a IL-17A modulator, extracted from patent WO2021239743+A1, example 9. IL-17A modulator-1 inhibits the biological action of IL-17A with a pIC50 of 8.2. IL-17A modulator-1 can be used for the research of diseases or disorders associated with modulation of IL-17A activity including diseases with an immune component or autoimmune pathol, cancer and neurodegenerative disorders.
|
-
- HY-124751
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Neurological Disease
|
|
YTX-465 is a stearoyl-CoA desaturase (Ole1/SCD) inhibitor. YTX-465 inhibits Ole1 and SCD1 with IC50s of 0.039 μM and 30.4 μM, respectively. YTX-465 can be used in the research of Parkinson’s disease and other synucleinopathies.
|
-
- HY-139308
-
|
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
T0467 activates parkin mitochondrial translocation in a PINK1-dependent manner in vitro. T0467 do not induce mitochondrial accumulation of PINK1in dopaminergic neurons. T0467 is a potential compound for PINK1-Parkin signaling activation, and can be used for parkinson's disease and related disorders research.
|
-
- HY-110125
-
|
CID 1261822
|
GPR55
|
Neurological Disease
|
|
ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.
|
-
- HY-144790
-
|
|
Amyloid-β
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu 2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease.
|
-
- HY-147565
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC50 of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer.
|
-
- HY-N2181
-
|
|
Cytochrome P450
Apoptosis
Bacterial
Autophagy
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Acetylshikonin is an oral active anti-cancer, anti-inflammatory, antioxidant, anti-fertility, antibacterial, and neuroprotective agent. Acetylshikonin is a inhibitor of acetylcholinase (AChE) (IC50=34.6 μM) and nonselective cytochrome P450. Acetylshikonin can induce Apoptosis and Autophagy in cancer cells. Acetylshikonin regulates blood glucose, liver fat metabolism, and renal fibrosis, and is used in the study of diabetes, diabetic nephropathy (DN), obesity, and nonalcoholic fatty liver disease (NAFLD).
|
-
- HY-F0004
-
|
β-NM; NMN
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD + intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
|
-
- HY-150503
-
|
|
HDAC
|
Neurological Disease
|
|
KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research.
|
-
- HY-105321
-
|
PBT 2
|
Bacterial
|
Neurological Disease
|
|
PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria.
|
-
- HY-107655
-
|
ABET
|
mAChR
|
Cardiovascular Disease
|
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research. Arecaidine but-2-ynyl ester (tosylate) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-152110
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
Dual AChE-MAO B-IN-5, indanone derivative, is a potent dual AChE/MAO-B inhibitior with IC50 values of 0.0224, 0.0412, and 0.1116 μM for AChE, MAO-B and MAO-A, respectively. Dual AChE-MAO B-IN-5 has antioxidant activity and prevents β-amyloid plaque aggregation. Dual AChE-MAO B-IN-5 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-107736
-
|
|
Others
|
Cancer
Inflammation/Immunology
|
|
AI-3 is a potent ARE (antioxidant response element) activator. AI-3 increases the NQO1 at the transcript levels and protein expression levels. AI-3 has the potential for the research of oxidative stress related diseases.
|
-
- HY-152227
-
|
|
PROTACs
JAK
|
Inflammation/Immunology
|
|
PROTAC TYK2 degradation agent1 is a potent and subtype-selective TYK2 degrader. PROTAC TYK2 degradation agent1 has TYK2 degradation activity with DC50 value of 14 nM. PROTAC TYK2 degradation agent1 can be used for the research of autoimmune disease.
|
-
- HY-145373
-
|
|
Btk
|
Inflammation/Immunology
|
|
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
|
-
- HY-N6625
-
|
|
Fungal
|
Infection
|
|
Chlorothalonil is a broad spectrum fungicide and is effective in protecting plants against fungal diseases caused mainly by Phytophthora infestans and Alternaria solani. Chlorothalonil is used for controlling of fungal foliar diseases of vegetables and crops.
|
-
- HY-143261
-
|
|
GSK-3
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
GSK-3β inhibitor 7 is a GSK-3β inhibitor with an IC50 value of 5.25 μM. GSK-3β inhibitor 7 is inserted into the ATP-binding binding pocket of GSK-3β and forms hydrogen-bond. GSK-3β inhibitor 7 shows high hepatocyte glucose uptake (83.5%), and can be used in the research of numerous diseases like diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder.
|
-
- HY-153564
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research.
|
-
- HY-107447
-
|
N-Deshydroxyethyl BMS-354825
|
Drug Metabolite
|
Cancer
Inflammation/Immunology
|
|
N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, Dasatinib is a multi-kinase inhibitor that potently inhibits Bcr-Abl, Src family and platelet-derived growth factor receptor kinases. N-Deshydroxyethyl Dasatinib can be used in cancer and immune disease research.
|
-
- HY-122605
-
|
CBA
|
TRP Channel
|
Cancer
Cardiovascular Disease
|
|
TRPM4-IN-1 (CBA) is a potent and selective inhibitor of the cation channel TRPM4, with an IC50 of 1.5 μM. TRPM4-IN-1 can be used for the research of cardiac diseases and prostate cancer.
|
-
- HY-139973
-
|
|
Amyloid-β
|
Neurological Disease
|
|
OAB-14, is a Bexarotene (HY-14171) derivative, improves Alzheimer's disease-related pathologies and cognitive impairments by increasing β-amyloid clearance in APP/PS1 mice. OAB-14 effectively ameliorates the dysfunction of the endosomal-autophagic-lysosomal pathway in APP/PS1 transgenic mice.
|
-
- HY-122080
-
|
|
Cholinesterase (ChE)
Beta-secretase
Amyloid-β
|
Neurological Disease
|
|
Memoquin is an anti-amyloid and anti-oxidant multi-target-directed ligand. Memoquin is an orally active inhibitor of BACE-1 and AChE with IC50 values of 108 and 1.55 nM, respectively. Memoquin is a cognitive enhancer that prevents the Aβ-induced neurotoxicity mediated by oxidative stress. Memoquin can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-N2908
-
|
Methyl atrarate
|
Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases.
|
-
- HY-148867
-
|
2-(Fluoromethoxy)-4'-(S-methylsulfonimidoyl)-1,1'-biphenyl
|
Dopamine Receptor
|
Neurological Disease
|
|
UCM-1306 is a potent and orally active human dopamine D1 receptor allosteric modulator (PAM). UCM-1306 increases the endogenous dopamine (DA) maximal effect both in human and mouse D1 receptors. UCM-1306 is not only for improving motor symptoms but also for addressing the key comorbid cognitive impairment associated with long-term Parkinson’s disease (PD).
|
-
- HY-13995A
-
|
|
FXR
Autophagy
|
Others
|
|
Sevelamer hydrochloride is an orally active and phosphate binding agent used for research of hyperphosphatemia with chronic kidney disease. Sevelamer hydrochloride consists of polyallylamine that is crosslinked with epichlorohydrin.
|
-
- HY-148795
-
-
- HY-134968A
-
|
|
Tau Protein
|
Neurological Disease
|
|
(R)-TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor. (R)-TTBK1-IN-1 is an enantiomer of TTBK1-IN-1 (HY-134968). (R)-TTBK1-IN-1 can be used in the research of alzheimer’s disease and related tauopathies. (R)-TTBK1-IN-1 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-32340
-
|
KH1060
|
VD/VDR
|
Cancer
Inflammation/Immunology
|
|
Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
|
-
- HY-116016
-
|
L-DOPA ethyl ester; Levodopa ethyl ester
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Etilevodopa (L-Dopa ethyl ester), an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine.
|
-
- HY-116016A
-
|
L-DOPA ethyl ester hydrochloride; Levodopa ethyl ester hydrochloride
|
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
|
Etilevodopa (L-Dopa ethyl ester) hydrochloride, an ethyl-ester proagent of Levodopa, is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Etilevodopa hydrochloride is used for the treatment of Parkinson disease (PD). Levodopa is the direct precursor of dopamine and is a suitable proagent as it facilitates CNS penetration and delivers dopamine.
|
-
- HY-144446
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD). BuChE-IN-1 shows low cytotoxicity and high blood brain barrier (BBB) permeability. BuChE-IN-1 is a promising BuChE inhibitor for the research of AD.
|
-
- HY-139727
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-151259
-
|
|
JAK
|
Cancer
|
|
TK4b is a Janus kinase (JAK) inhibitor with the IC50 values of 19.40 nM and 18.42 nM for JAK2 and JAK3, respectively. TK4b can be used in lymphoid-derived diseases and leukemia cancer research.
|
-
- HY-151258
-
|
|
JAK
|
Cancer
|
|
TK4g is a Janus kinase (JAK) inhibitor with the IC50 values of 12.61 nM and 15.80 nM for JAK2 and JAK3, respectively. TK4g can be used in lymphoid-derived diseases and leukemia cancer research.
|
-
- HY-139607
-
|
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research.
|
-
- HY-128382
-
|
E 151
|
Enterovirus
|
Infection
|
|
Brilliant black BN (E151) is an azo dye and a food colorant. Brilliant black BN is a promising antiviral agent against EV71 infection via inhibiting the interaction between EV71 and its cellular uncoating factor cyclophilin A. Brilliant black BN has the potential for the investigation of contagious disease.
|
-
- HY-113074
-
|
Glycolithocholate sulfate; Sulfolithocholylglycine; SLCG
|
HIV
Endogenous Metabolite
|
Infection
Inflammation/Immunology
|
|
Glycolithocholic acid 3-sulfate (SLCG) is a cholic acid derivative and a metabolite of glycolithocholic acid. Glycolithocholic acid 3-sulfate inhibits replication of HIV-1 in vitro. Glycolithocholic acid 3-sulfate can be used for the research of HIV infection and gallbladder disease.
|
-
- HY-12336
-
NIBR189
1 Publications Verification
|
EBI2/GPR183
|
Inflammation/Immunology
|
|
NIBR189 is an EBI2 (Epstein-Barr virus-induced gene 2) antagonist. NIBR189 inhibits human and mouse EBI2 with IC50s of 11 and 16 nM, respectively. NIBR189 can be used for the research of autoimmune diseases.
|
-
- HY-145150
-
|
|
TRP Channel
|
Metabolic Disease
|
|
TRPC5-IN-1 (Compound 6j) is a selective TRPC5 inhibitor with 50.5 % Inhibition for TRPC5 at 3 μM. TRPC5-IN-1 can be used for the research of chronic kidney disease (CKD).
|
-
- HY-150563
-
|
|
Monoamine Oxidase
Amyloid-β
|
Inflammation/Immunology
Neurological Disease
|
|
Neuroinflammatory-IN-2 is a potent anti-neuroinflammatory agent with an IC50 value of 10.30 μM for MAO-B, and 96.33% inhibition of Aβ1-42 aggregation at 25 μM. Neuroinflammatory-IN-2 has neuroprotective activity in H2O2-induced PC-12 cell injury. Neuroinflammatory-IN-2 also has biometal chelating abilities, antioxidant activity, anti-neuroinflammatory activity and appropriate BBB permeability. Neuroinflammatory-IN-2 can be used for researching Alzheimer’s disease.
|
-
- HY-130437
-
|
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease.
|
-
- HY-146727
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK3-IN-11 (Compound 12), a potent, noncytotoxic, irreversible, orally active JAK3 inhibitor with IC50 value of 1.7 nM, has excellent selectivity (>588-fold compared to other JAK isoforms), covalently bind to the ATP-binding pocket in JAK3. JAK3-IN-11 strongly inhibits JAK3-dependent signaling and T cell proliferation, is a promising tool for study autoimmune diseases.
|
-
- HY-156634
-
|
NYX-783
|
iGluR
|
Neurological Disease
|
|
Risevistinel (NYX-783) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
|
-
- HY-B1779
-
Sucrose
5 Publications Verification
D-(+)-Saccharose
|
Endogenous Metabolite
|
Metabolic Disease
Cancer
|
|
Sucrose (D-(+)-Saccharose) is a disaccharide which is composed of two monosaccharides, glucose and fructose. Sucrose can be applied in some animal models, including metabolic disease, obesity, diet on preference, and diabetes, et al.
|
-
- HY-148191
-
|
|
HIV Protease
|
Cancer
Infection
Inflammation/Immunology
Cardiovascular Disease
|
|
CL-197 is an orally active and long-acting purine anti-HIV nucleoside reverse transcriptase inhibitor (NRTI). CL-197 has potential effect on the research of viral, oncological and cerebrovascular diseases. CL-197 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N3963
-
|
(+)-Gomisin M2
|
HIV
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
|
Gomisin M2 ((+)-Gomisin M2) is a lignan isolated from the fruits of Schisandra rubriflora with anti-HIV activity (EC50 of 2.4 μM). Gomisin M2 exhibits anti-cancer and anti-allergic activities and has the potential for Alzheimer’s disease research.
|
-
- HY-P99238
-
|
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Rolinsatamab is a potent dual IL-4 and IL-13 inhibitor as a fully humanized bispecific monoclonal antibody. Rolinsatamab chimeric antigen receptor sequence T cell. Rolinsatamab can be used in research of immune disease.
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-
- HY-N1876
-
|
|
Others
|
Neurological Disease
|
|
Aromadendrane-4β,10α-diol is a sesquiterpene alcohol. Aromadendrane-4β,10α-diol significantly ameliorates the Aβ1-42 peptide-induced memory impairment. Aromadendrane-4β,10α-diol can be used for Alzheimer's disease (AD) research.
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-
- HY-136561
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Metabolic Disease
|
|
GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
|
-
- HY-149941
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent.
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-
- HY-151368
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research.
|
-
- HY-124476
-
|
|
Caspase
Glutaminase
Apoptosis
|
Cancer
|
|
Cystamine is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD) .
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-
- HY-121214
-
|
|
Mitochondrial Metabolism
|
Infection
|
|
Amisulbrom is a sulfonamide fungicide used to control oomycete diseases. Amisulbrom biochemically inhibits the cytochrome-bc1 complex of the mitochondrial electron transport system.
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-
- HY-145831
-
|
|
Cholinesterase (ChE)
|
Inflammation/Immunology
Neurological Disease
|
|
sEH/AChE-IN-1 (Compound 12a) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-1 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-1 has the potential for the research of Alzheimer's disease (AD).
|
-
- HY-16361A
-
|
CGP3466B; CGP3446 maleate; TCH346 maleate
|
Apoptosis
|
Metabolic Disease
Neurological Disease
|
|
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates Aβ1-42-induced tau acetylation, memory impairment, and locomotor dysfunction in mice. Omigapil maleate has the potential for the research of Alzheimer's disease. Omigapil maleate (CGP3446B maleate) is a apoptosis inhibitor. Omigapil maleate can be used for the research of congenital muscular dystrophy (CMD). Omigapil (maleate) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-132303
-
|
|
CETP
|
Metabolic Disease
Cardiovascular Disease
|
|
MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.
|
-
- HY-50707
-
|
(Rac)-T-Type calcium channel inhibitor
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Others
|
Neurological Disease
|
|
(Rac)-TTA-P2 is the inactive isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
|
-
- HY-10035A
-
|
|
Others
|
Neurological Disease
|
|
(R)-TTA-P2 is the inactive isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease.
|
-
- HY-115497
-
|
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
|
|
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).
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-
- HY-A0027
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Endocrinology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
|
-
- HY-A0027A
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
|
-
- HY-117006
-
|
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.
|
-
- HY-139727A
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
S(-)-Bisoprolol fumarate is a S(-)-enantiomer of Bisoprolol fumarate. Bisoprolol fumarate is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-P990008
-
|
|
Apoptosis
TNF Receptor
|
Inflammation/Immunology
|
|
Atrosab is a humanized IgG1 antagonistic anti-TNFR1 antibody. Atrosab inhibits TNF-mediated apoptosis induction and IL-6 and IL-8 production. Atrosab can be used for research of inflammatory disease.
|
-
- HY-125016
-
|
TAZ-K
|
YAP
|
Cardiovascular Disease
|
|
TT-10 (TAZ-K) is an activator of YES-associated protein (YAP)-transcriptional enhancer factor domain (TEAD) activity. TT-10 can be used for the research of heart diseases accompanied by cardiomyocyte loss.
|
-
- HY-15178
-
|
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-12820
-
|
Antibiotic-202
|
Bacterial
Antibiotic
|
Infection
|
|
Sibofimloc (Antibiotic-202) is a first-in-class, gut-restricted, orally active FimH adhesion inhibitor extracted from patent WO2014100158A1, Compound Example 202. Sibofimloc has anti-bacterial infective activity. Sibofimloc is developed for inflammatory bowel disease (IBD).
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-
- HY-103234
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research.
|
-
- HY-103234B
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research.
|
-
- HY-103234A
-
|
|
iGluR
|
Neurological Disease
|
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research.
|
-
- HY-145832
-
|
|
Cholinesterase (ChE)
|
Inflammation/Immunology
Neurological Disease
|
|
sEH/AChE-IN-2 (Compound 12b) is a dual inhibitor of the enzymes soluble epoxide hydrolase (sEH) and acetylcholinesterase (AChE). sEH/AChE-IN-2 provides cumulative effects against neuroinflammation and memory impairment. sEH/AChE-IN-2 has the potential for the research of Alzheimer's disease (AD).
|
-
- HY-136490
-
|
Galactosylsphingosine
|
PKC
|
Cancer
Neurological Disease
|
|
Psychosine (Galactosylsphingosine), a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell types including, most relevantly to globoid cell leukodystrophy (GLD), oligodendrocytes. Psychosine causes cell death at least in part via apoptosis. Psychosine also is an inhibitor of PKC.
|
-
- HY-N7698B
-
|
|
Others
|
Cancer
Inflammation/Immunology
|
|
Hexa-N-acetylchitohexaose is an inducer of disease resistance in crop plants, which could elicit an increase of lignification-related and antioxidative enzymes in soybean plants. Hexa-N-acetylchitohexaose is a substrate of lysozyme. Hexa-N-acetylchitohexaose shows antitumor effect.
|
-
- HY-B0731A
-
|
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
|
-
- HY-130452
-
|
|
NO Synthase
|
Neurological Disease
|
|
NOS1-IN-1 is a selective and cell-permeable nNOS inhibitor with a Ki of 120 nM. NOS1-IN-1 exhibits 2617-fold and 325-fold selectivity over eNOS (Ki=39 μM) and iNOS (Ki=325 μM) , respectively. NOS1-IN-1 can be used for the research of neurological disease, including cerebral palsy (CP).
|
-
- HY-156626
-
|
NYX-458; NYX-3054
|
iGluR
|
Neurological Disease
|
|
Nevadistinel (NYX-458; NYX-3054) is a positive allosteric modulator of N-methyl-D-aspartate (NMDA) receptor. Nevadistinel can be used to inhibit cognitive impairment associated with neurodegenerative diseases, such as mild cognitive impairment, mild Alzheimer's disease, Parkinson's disease, Lewy body disease.
|
-
- HY-147859
-
|
|
Amyloid-β
|
Neurological Disease
|
|
BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research.
|
-
- HY-N9239
-
|
|
Others
|
Others
|
|
Turmeronol A is a sesquiterpenoid compound.
Turmeronol A has anti-inflammatory activity. Turmeronol A prevents macrophage
activation and the production of inflammatory mediators by inhibiting the
activation of NFκB. Turmeronol A can be used to prevent chronic inflammatory
diseases .
|
-
- HY-142673
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-7 is a potent inhibitor of ATR. ATR is a class of protein kinases involved in genome stability and DNA damage repair, and is a member of the PIKK family. ATR-IN-7 has the potential for the research of ATR kinase-mediated diseases such as proliferative diseases and cancer (extracted from patent WO2021238999A1, compound 1).
|
-
- HY-139561
-
-
- HY-146195
-
-
- HY-N4005
-
|
|
Bacterial
Tyrosinase
|
Infection
Neurological Disease
|
|
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research.
|
-
- HY-B1806A
-
|
Pathilon chloride
|
mAChR
|
Inflammation/Immunology
Neurological Disease
|
|
Tridihexethyl (Pathilon) chloride is an orally active anticholinergic agent and mAChR antagonist, shows activities of antimuscarinic and anticholinergic. Tridihexethyl chloride shows pronounced antispasmodic and antisecretory effects on the gastrointestinal tract. Tridihexethyl chloride can be used in studies of peptic ulcer disease and acquired nystagmus .
|
-
- HY-11109
-
Resatorvid
Maximum Cited Publications
337 Publications Verification
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-α and IL-6 production with IC50s 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-15770
-
|
|
Integrin
|
Inflammation/Immunology
|
|
TR-14035 is a orally active dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune diseases.
|
-
- HY-146731
-
|
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders.
|
-
- HY-113089
-
|
H-Glu(H-Lys-OH)-OH; γ-Glu-ε-Lys
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Epsilon-(gamma-glutamyl)-lysine is an N(6)-acyl-L-lysine derivative. The enzyme tissue transglutaminase (tTg) helps the formation of epsilon-(gamma-glutamyl)lysine bonds between ECM components in some disease, such as non-diabetic kidney, glaucoma filtration.
|
-
- HY-149211
-
|
|
Cholinesterase (ChE)
Beta-secretase
Amyloid-β
|
Neurological Disease
|
|
AChE/BChE-IN-12 (compound 10b), a 3,5-dimethoxy analogue, is a potent AChE, BChE, and β-secretase-1 (BACE-1) inhibitor, with IC50 values of 2.57, 3.26, and 10.65 μM, respectively. AChE/BChE-IN-12 crosses the blood-brain barrier via passive diffusion and inhibits the self-aggregation of amyloid-β monomers. AChE/BChE-IN-12 can be used for Alzheimer’s disease (AD) research.
|
-
- HY-116044
