Search Result
Results for "ActiveIL-1 beta Inhibitors" in MCE Product Catalog:
9860
Inhibitors & Agonists
25
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-U00439
-
-
- HY-16702
-
-
- HY-16702A
-
-
- HY-N0550
-
|
β-Pinene
(-)-β-Pinene
|
Bacterial
|
Infection
|
|
β-Pinene ((-)-β-Pinene), a major component of turpentine, inhibit infectious bronchitis virus (IBV) with an IC50 of 1.32 mM. β-Pinene presents antimicrobial activity.
|
-
- HY-125586
-
|
β-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-N2337
-
-
- HY-D0886
-
-
- HY-B1837A
-
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β-Cyfluthrin
beta-Cyfluthrin
|
Calcium Channel
|
Infection
|
|
β-Cyfluthrin (beta-Cyfluthrin) is a type II synthetic pyrethroid and also an active ingredient of many insecticide products used for pestsin agriculture. β-Cyfluthrin is a neurotoxicant and affects calcium concentration in nervous tissue by inhibiting Ca 2+ ATPase involved in calcium transport.
|
-
- HY-107324
-
|
β-Elemene
(-)-β-Elemene; Levo-β-elemene
|
Apoptosis
|
Cancer
|
|
β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.
|
-
- HY-135386
-
-
- HY-Y1750
-
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-N5112A
-
-
- HY-N2454
-
-
- HY-P1286
-
-
- HY-133680
-
|
β-Tocopherol
|
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
|
-
- HY-N2513
-
|
β-Boswellic acid
|
Lipoxygenase
DNA/RNA Synthesis
|
Cancer
|
|
β-Boswellic acid is isolated from the gum resin of Boswellia serrate.
β-Boswellic acid is a nonreducing-type inhibitor of the 5-lipoxygenase (5-LO) product formation either interacting directly with the 5-LO or blocking its translocation. β-Boswellic acid inhibits the synthesis of DNA, RNA and protein in human leukemia HL-60 cells.
|
-
- HY-126144
-
-
- HY-135670A
-
-
- HY-124957
-
|
β-NETA
|
AChE
Apoptosis
|
Cancer
|
|
β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC50=76 μM) and cholinesterase (ChE; IC50=40 µM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC50=1 mM).
|
-
- HY-N0941
-
|
beta-Mangostin
β-Mangostin
|
Bacterial
Parasite
Apoptosis
|
Cancer
Infection
|
|
beta-Mangostin (β-Mangostin) is a xanthone compound present in Cratoxylum arborescens, with antibacterial and antimalarial activities. beta-Mangostin exhibits antimycobacterial activity against Mycobacterium tuberculosis with an MIC of 6.25 μg/mL. beta-Mangostin possesses in vitro antimalarial activity against Plasmodium falciparum, with an IC50 of 3.00 μg/mL. beta-Mangostin has potent anticancer activity against various cancers (such as hepatocellular carcinoma, leukaemic).
|
-
- HY-N1940
-
|
β-Anhydroicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
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β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
|
-
- HY-N2920
-
|
β-Amyrenonol
11-Oxo-β-amyrin
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.
|
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- HY-N7606
-
-
- HY-108059
-
-
- HY-P1084
-
-
- HY-136234
-
|
9-cis-β-Carotene
|
Others
|
Others
|
|
9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus.
|
-
- HY-107373
-
|
β-Chloro-L-alanine
L-β-Chloroalanine
|
Bacterial
|
Infection
|
|
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
|
-
- HY-U00272
-
|
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)-
Androst-4-ene-3β,17β-diol, dipropionate
|
Androgen Receptor
|
Metabolic Disease
Neurological Disease
|
|
Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- is the dipropanoate of 4-Androstenediol, a metabolite of testosterone.
|
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- HY-131005
-
-
- HY-114464
-
|
11-Beta-hydroxyandrostenedione
4-Androsten-11β-ol-3,17-dione
|
Endogenous Metabolite
|
Endocrinology
|
|
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
|
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- HY-P1286A
-
-
- HY-N2922
-
|
β-Amyrin
|
Others
|
Neurological Disease
|
|
β-Amyrin, an ingredient of the surface wax of tomato fruit and dandelion coffee, blocks amyloid β (Aβ)-induced long-term potentiation (LTP) impairment. β-amyrin is a promising candidate of treatment for AD.
|
-
- HY-138247
-
-
- HY-N5112B
-
|
β,β-Dimethylacrylshikonin
|
Others
|
Cancer
|
|
β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity.
|
-
- HY-U00325
-
-
- HY-19773
-
|
β-Lactamase-IN-1
|
Bacterial
|
Infection
|
|
β-Lactamase-IN-1 is an inhibitor of β-Lactamase extracted from patent WO2016027249A1, page 77. β-Lactamase-IN-1 can be used to prepare of tricyclic nitrogen containing compound. β-Lactamase-IN-1 can be used for the research of neisseria gonorrhea infection.
|
-
- HY-N2056
-
|
11-Keto-beta-boswellic acid
11-Keto-β-boswellic acid
|
Lipoxygenase
Leukotriene Receptor
NF-κB
|
Cancer
|
|
11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.
|
-
- HY-12452
-
-
- HY-136464
-
|
β-catenin-IN-2
|
β-catenin
|
Cancer
|
|
β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
|
-
- HY-103081
-
|
β-Glucuronidase-IN-1
|
Bacterial
|
Cancer
Infection
|
|
β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively.
|
-
- HY-W010231
-
|
β-Cyclocitral
|
Others
|
Others
|
|
β-Cyclocitral, a volatile oxidized derivative of β-carotene, is a grazer defence signal unique to the Cyanobacterium Microcystis. β-Cyclocitral, one of the predominant volatile terpenoid compounds, can upregulate the expression of defence genes to enhance excess light (EL) acclimation. β-Cyclocitral is a powerful repellent.
|
-
- HY-113351
-
-
- HY-16673
-
|
PSN632408
|
GPR119
|
Metabolic Disease
|
|
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
|
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- HY-N8549
-
-
- HY-114392
-
|
Gly-β-MCA
|
FXR
Autophagy
|
Metabolic Disease
|
|
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.
|
-
- HY-F0004
-
|
β-Nicotinamide mononucleotide
β-NM; NMN
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD(+) intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
|
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- HY-135594
-
|
4'-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
|
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- HY-135595
-
|
6-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Drug Metabolite
|
Metabolic Disease
|
|
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
|
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- HY-N3995
-
|
5β-Dihydrocortisol
|
Apoptosis
Drug Metabolite
|
Cancer
|
|
5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis.
|
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- HY-108693
-
-
- HY-P1084A
-
-
- HY-N0411
-
|
β-Carotene
Provitamin A; beta-Carotene
|
Endogenous Metabolite
ROS
Apoptosis
|
Cancer
Metabolic Disease
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
|
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- HY-P1051
-
|
β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
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- HY-P1522
-
-
- HY-N7682
-
|
β-Tomatine
|
Others
|
Others
|
|
β-Tomatine is a breakdown product of α-tomatine and a less fungitoxic compound. β-Tomatine can suppress plant defense responses.
|
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- HY-B0141
-
-
- HY-P1521
-
-
- HY-P0128
-
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β-Amyloid (25-35)
Amyloid beta-peptide (25-35); Aβ25-35; β-Amyloid peptide (25-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (25-35) (Amyloid beta-peptide (25-35)) is the fragment Aβ(25-35) of the Alzheimer's amyloid β-peptide, has shown neurotoxic activities in cultured cells.
|
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- HY-15679
-
-
- HY-P0179
-
-
- HY-P1046
-
|
β-Amyloid 1-15
Amyloid β-Protein (1-15)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-15) is a fragment of β-Amyloid peptide. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-N6652
-
|
1-beta-D-Arabinofuranosyluracil
Uracil 1-β-D-arabinofuranoside
|
Others
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties. 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells.
|
-
- HY-N6018
-
-
- HY-N6741
-
|
β-Zearalenol
|
Others
|
Infection
Endocrinology
|
|
β-Zearalenol is a non-steroidal estrogenic mycotoxin synthesized by Fusarium species. β-Zearalenol potentially influences transcription and effects gene expression on translational level.
|
-
- HY-136552
-
|
β-Bisabolene
|
Others
|
Cancer
|
|
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer.
|
-
- HY-N1484
-
-
- HY-N5053
-
-
- HY-P1772
-
-
- HY-50900
-
-
- HY-P1481A
-
-
- HY-P1468
-
|
β-Amyloid (1-28)
Amyloid β-Protein (1-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-P1466
-
|
β-Amyloid 1-16
Amyloid β-Protein (1-16)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
|
-
- HY-107201
-
|
β-Cyclodextrin
|
Influenza Virus
|
Infection
|
|
β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus H1N1 activities.
|
-
- HY-P1474
-
|
β-Amyloid (22-35)
Amyloid β-Protein (22-35)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35), the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-125849
-
-
- HY-113418
-
-
- HY-N4201
-
|
β-Hydroxyisovalerylshikonin
|
EGFR
Src
|
Cancer
|
|
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
|
-
- HY-N1968
-
-
- HY-N2274
-
|
23-Hydroxylongispinogenin
12-Oleanene-3β,16β,23,28-tetrol; 3β,16β-12-Oleanene-3, 16,23,28-tetrol
|
Others
|
Cancer
|
|
23-Hydroxylongispinogenin (12-Oleanene-3β,16β,23,28-tetrol) is extracted from Lysimachia heterogenea Klatt. Lysimachia heterogenea Klatt is a perennial herb, which is used as a folk medicine in subduing swelling and detoxicating in China. The effective fraction LH-1 of L. heterogene has antitumor activity.
|
-
- HY-128976
-
-
- HY-12780S
-
-
- HY-22306
-
-
- HY-P1880
-
-
- HY-P1891
-
-
- HY-P1879
-
-
- HY-P1893
-
-
- HY-113478
-
|
3β-Ursodeoxycholic acid
Isoursodeoxycholic acid
|
Others
|
Metabolic Disease
|
|
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA.
|
-
- HY-P1051A
-
|
β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-N1501
-
|
Beta-asarone
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties of
immunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease.
|
-
- HY-N6740
-
|
Beta-Zearalanol
|
Apoptosis
|
Metabolic Disease
|
|
Beta-Zearalenol is an mycotoxin produced by Fusarium spp, which causes apoptosis and oxidative stress in mammalian reproductive cells. Beta-Zearalenol is the derivative of zearalenone (ZEA) which can conjugate with glucuronic acid.
|
-
- HY-136344
-
-
- HY-N7683
-
|
Prunetin 5-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
|
|
Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes.
|
-
- HY-P1787
-
-
- HY-125773
-
|
β-cyano-L-Alanine
beta-cyano-l-alanine
|
Others
|
Neurological Disease
|
|
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
|
-
- HY-P1895
-
-
- HY-P1903
-
-
- HY-130842
-
-
- HY-N2182
-
-
- HY-136306
-
-
- HY-P1510
-
-
- HY-P1517
-
-
- HY-P1850
-
-
- HY-B1449
-
|
Uridine
β-Uridine
|
Endogenous Metabolite
|
Others
|
|
Uridine (β-Uridine) is a glycosylated pyrimidine-analog containing uracil attached to a ribose ring (or more specifically, aribofuranose) via a β-N1-glycosidic bond.
|
-
- HY-P1362
-
|
β-Amyloid (42-1), human
Amyloid β Peptide (42-1)(human)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). Amyloid β Peptide (1-42) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
-
- HY-N0087
-
|
Gambogic Acid
beta-Guttiferrin
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
|
-
- HY-N7635
-
-
- HY-N2188
-
-
- HY-131108
-
-
- HY-P0179A
-
-
- HY-N1415
-
-
- HY-P1474A
-
|
β-Amyloid (22-35) (TFA)
Amyloid β-Protein (22-35) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid 22-35 (Amyloid β-Protein 22-35) TFA, the residues 22-35 fragment ofβ-amyloid protein, has a cytotoxic effect on cultured neurons from the rat hippocampus in serum-free medium. β-Amyloid 22-35 TFA forms aggregates and typical amyloid fibrils resembling those of the β-amyloid protein in neutral buffer solution).
|
-
- HY-N7489
-
|
β-Hederin
|
Parasite
|
Infection
Inflammation/Immunology
|
|
β-Hederin, a saponin isolated from Hedera helix L.(Araliaceae), possesses antileishmanial activity. β-Hederin exhibits IC50 values of 1.5 μM, 68 nM and 4.57 μM in L. Mexicana promastigotes, L. mexicana amastigotes and THP1 cells, respectively.
|
-
- HY-N0338
-
-
- HY-N4034
-
-
- HY-N0181A
-
|
Lumisterol
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-121879
-
-
- HY-N6824
-
-
- HY-10133
-
-
- HY-101514
-
-
- HY-N7401
-
-
- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
|
-
- HY-P1854
-
|
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism [1].
|
-
- HY-N0180
-
-
- HY-P1502
-
|
β-Endorphin, human
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin, human, a prominent endogenous peptide, existing in the hypophysis cerebri and hypothalamus, is an agonist of opioid receptor, with preferred affinity for μ-opioid receptor and δ-opioid receptor; β-Endorphin, human exhibits antinociception activity.
|
-
- HY-141379
-
|
N-Bromoacetyl-β-alanine
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
N-Bromoacetyl-β-alanine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs. N-Bromoacetyl-β-alanine is also a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-137553A
-
-
- HY-P1053
-
-
- HY-136537A
-
-
- HY-N6851
-
|
Glycyrrhetic acid 3-O-β-D-glucuronide
|
Others
|
Inflammation/Immunology
|
|
Glycyrrhetic acid 3-O-β-D-glucuronide, isolated from glycyrrhiza, is an important derivative of glycyrrhizin (GL) with an anti -allergic activity. Glycyrrhetic acid 3-O-β-D-glucuronide (GAMG) shows that β‐glucuronidases (β‐GUS) are key GAMG-producing enzymes, displaying a high potential to convert GL directly into GAMG.Glycyrrhetic acid 3-O-β-D-glucuronide is valuable as a sweetener.
|
-
- HY-N2168
-
|
Pinoresinol 4-O-β-D-glucopyranoside
(+)-Pinoresinol 4-O-β-D-glucopyranoside
|
Others
|
Cardiovascular Disease
|
|
Pinoresinol 4-O-β-D-glucopyranoside ((+)-Pinoresinol 4-O-β-D-glucopyranoside) is the major active furofuran type lignans in Fructus Forsythiae. Pinoresinol 4-O-β-D-glucopyranoside shows antioxidant, blood pressure reducing, and cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitory effects.
|
-
- HY-N0171B
-
|
Beta-Sitosterol (purity>75%)
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-P2294
-
|
pm26TGF-β1 peptide
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-107670
-
|
Dihydro-β-erythroidine hydrobromide
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
|
-
- HY-N0171
-
|
Beta-Sitosterol (purity>80%)
β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)
|
Endogenous Metabolite
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-130269
-
|
β-Naphthoflavone-CH2-OH
β-NF-CH2-OH
|
Ligand for E3 Ligase
|
Cancer
|
|
β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) is a ligand for arylhydrocarbon receptor (AhR) E3 ligase. β-Naphthoflavone-CH2-OH can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1) that recruit the AhR E3 ligase complex by incorporating AhR ligands into chimeric molecules. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins [1].
|
-
- HY-128737
-
-
- HY-13555
-
|
β-Lapachone
ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
|
-
- HY-130256
-
|
β-NF-JQ1
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
β-NF-JQ1 is a PROTAC that recruits AhR E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
|
-
- HY-N3517
-
-
- HY-N3516
-
-
- HY-W015084
-
|
β-Ionone
|
Apoptosis
|
Cancer
|
|
β-Ionone, isolated from plant oils, is effective in the induction of apoptosis in gastric adenocarcinoma SGC7901 cells. Anti-cancer activity.
|
-
- HY-116284
-
-
- HY-112044
-
-
- HY-P1567
-
-
- HY-N2075
-
-
- HY-P1524
-
-
- HY-N4099
-
-
- HY-W012875
-
-
- HY-138322
-
-
- HY-N2100
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-N0406
-
|
2"-O-beta-L-galactopyranosylorientin
|
Others
|
Metabolic Disease
|
|
2"-O-beta-L-galactopyranosylorientin is extracted from the flowers of Trollius ledebouri. 2"-O-beta-L-galactopyranosylorientin involves transporter mediated efflux in addition to passive diffusion and is the substrate of multidrug resistance protein 2 (MRP2).
|
-
- HY-N5111
-
-
- HY-P1548
-
-
- HY-101953
-
-
- HY-P2283
-
-
- HY-B0708
-
-
- HY-P2294A
-
|
pm26TGF-β1 peptide TFA
|
TGF-β Receptor
|
Inflammation/Immunology
|
|
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-N2212
-
-
- HY-129993
-
-
- HY-U00391
-
-
- HY-N6904
-
-
- HY-P2290
-
|
Beta-defensin 1, pig
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-N7598
-
-
- HY-N0192
-
|
Arbutin
β-Arbutin
|
Tyrosinase
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
|
-
- HY-N2394
-
-
- HY-100084
-
-
- HY-19373
-
-
- HY-N3523
-
|
3-O-Beta-D-Glucopyranosylplatycodigenin
|
Others
|
Cancer
|
|
3-O-Beta-D-Glucopyranosylplatycodigenin is an oleanane-type triterpenoid isolated from roots of Platycodon grandiflorum. 3-O-Beta-D-Glucopyranosylplatycodigenin exhibits anti-proliferative activities against HSC-T6 cell line with an IC50 of 13.36 μM.
|
-
- HY-P0265
-
-
- HY-113949A
-
-
- HY-N6677
-
|
β-Apo-8'-carotenal
Apocarotenal
|
Cytochrome P450
|
Cancer
|
|
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.
|
-
- HY-P1378
-
-
- HY-P1548B
-
-
- HY-N2287
-
-
- HY-100260
-
|
beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
|
HIV
|
Infection
|
|
beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.
|
-
- HY-N2142
-
-
- HY-P1363
-
-
- HY-137553
-
|
β-Aminoarteether
SM934 free base
|
Others
|
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-N7176
-
|
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide
|
Interleukin Related
|
Inflammation/Immunology
|
|
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
|
-
- HY-N0171A
-
-
- HY-N5091
-
-
- HY-N6986
-
-
- HY-N0520
-
|
Calycosin-7-O-β-D-glucoside
|
Reactive Oxygen Species
|
Others
|
|
Calycosin-7-O-β-D-glucoside is an isoflavone isolated from Astragali Radix. Calycosin-7-O-β-D-glucoside has variety of biological activities, such as neuroprotective, cardioprotection, anti-inflammation, and antioxidative stress effects.
|
-
- HY-N7422
-
|
Kauran-16,17-diol
ent-Kauran-16β,17-diol
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
|
-
- HY-P1866
-
-
- HY-W015546
-
|
β-N-methylamino-L-alanine hydrochloride
BMAA hydrochloride
|
Others
|
Neurological Disease
|
|
β-N-methylamino-L-alanine hydrochloride (BMAA hydrochloride) is a neurotoxin produced by cyanobacteria. β-N-methylamino-L-alanine hydrochloride could cause amyotrophic lateral sclerosis (ALS) and possibly other neurodegenerative diseases.
|
-
- HY-P2290A
-
|
Beta-defensin 1, pig TFA
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Beta-defensin 1, pig TFA is an antimicrobial peptide found primarily in tongue mucosa of pig. Beta-defensin 1, pig TFA is active against bacteria such as Escherichia coli, Salmonella typhimurium, Listeria monocytogenes, Staphylococcus aureus, Bordetella pertussis and Candida albicans.
|
-
- HY-N2468
-
|
Xylobiose
1,4-β-D-Xylobiose; 1,4-D-Xylobiose
|
Others
|
Others
|
|
Xylobiose (1,4-β-D-Xylobiose; 1,4-D-Xylobiose) is a disaccharide of xylose monomers with a β-1, 4 bond between monomers.
|
-
- HY-43470
-
-
- HY-P1378A
-
-
- HY-N6938
-
-
- HY-11012
-
|
TDZD-8
GSK-3β Inhibitor I; NP 01139
|
GSK-3
|
Cancer
|
|
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
|
-
- HY-N6885
-
|
Puerarin-4'-O-β-D-glucopyranoside
|
Others
|
Cancer
|
|
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells.
|
-
- HY-N6911
-
-
- HY-N2451
-
-
- HY-N6879
-
-
- HY-N6260
-
-
- HY-P2313
-
|
Human β-defensin-2
HβD-2
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-2 (HβD-2) is a small cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by a number of epithelial cells.Human β-defensin-2 has antimicrobial activity against gram-negative bacteria and Candida, but not gram-positive Staphylococcus aureus. Human β-defensin-2 can be used for the study of colitis.
|
-
- HY-P1548A
-
-
- HY-101953S
-
|
β-Apo-13-carotenone D3
D'Orenone D3
|
Others
|
Cancer
|
|
β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
|
-
- HY-113320
-
|
Etiocholanolone
5β-Androsterone
|
GABA Receptor
|
Neurological Disease
|
|
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent neurosteroid positive allosteric modulator (PAM) of the GABAA receptor than its enantiomer form.
|
-
- HY-N6006
-
-
- HY-135103
-
|
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- HY-W010452
-
-
- HY-113378
-
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A
|
Endogenous Metabolite
|
Others
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-P0265A
-
-
- HY-N4088
-
-
- HY-B0406
-
|
Bethanechol
Carbamyl-β-methylcholine
|
mAChR
|
Neurological Disease
|
|
Bethanechol (Carbamyl-β-methylcholine), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-B0406A
-
|
Bethanechol chloride
Carbamyl-β-methylcholine chloride
|
mAChR
|
Neurological Disease
|
|
Bethanechol chloride (Carbamyl-β-methylcholine chloride), a parasympathomimetic agent, is a mAChR agonist that exerts its effects via directly stimulating the mAChR (M1, M2, M3, M4, and M5) of the parasympathetic nervous system.
|
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P1388
-
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-U00250
-
-
- HY-N2107
-
-
- HY-136329
-
-
- HY-125801
-
|
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-128974
-
|
N-Dodecyl-β-D-maltoside
Lauryl Maltoside
|
Others
|
Others
|
|
N-Dodecyl-β-D-maltoside (Lauryl Maltoside) is a derivatives of pyrene (Py), and it is a alkyl maltopyranoside detergent, especially in transporters and respiratory complexes. N-Dodecyl-β-D-maltoside has also been employed in applications such as in the purification and stabilization of RNA polymerase and detection of protein-lipid interactions.
|
-
- HY-N0230
-
-
- HY-111642
-
-
- HY-P2291
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-141131
-
-
- HY-141132
-
-
- HY-140012
-
-
- HY-B1192
-
|
Estradiol benzoate
β-Estradiol 3-benzoate; 17β-Estradiol 3-benzoate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. It exhibits mild anabolic and metabolic properties, and increases blood coagulability.
|
-
- HY-P1866A
-
-
- HY-A0058
-
-
- HY-N7715
-
|
Ferulic acid acyl-β-D-glucoside
Ferulic acid glucoside
|
Drug Metabolite
|
Others
|
|
Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid (HY-N0060). Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.
|
-
- HY-P2312
-
|
Human β-defensin-3
HβD-3
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-3 (HβD-3) is an antibiotic anti-microbial peptide produced by epithelial cells with antimicrobial activities and reduces the effect of inflammatory cytokine responses. Human β-defensin-3 is against different microbes with IC90 values of 6-25 μg/ml.
|
-
- HY-N2601
-
-
- HY-N0892
-
-
- HY-77591A
-
-
- HY-N0713
-
-
- HY-P2315
-
|
Human β-defensin-1
HβD-1
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
|
-
- HY-103687
-
|
Abiraterone metabolite 1
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-P1504
-
-
- HY-108652
-
-
- HY-P2291A
-
-
- HY-P1388A
-
-
- HY-N4180
-
|
Pennogenin 3-O-beta-chacotrioside
|
Autophagy
|
Cancer
|
|
Pennogenin 3-O-beta-chacotrioside is an active component isolated from Paris polyphylla, modulates autophagy via increasing the expressions of autophagy-related proteins LC3 and Beclin-1. Anti-colorectal cancer activity.
|
-
- HY-B1209
-
|
Etofylline
7-(β-Hydroxyethyl)theophylline
|
Others
|
Cardiovascular Disease
|
|
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
|
-
- HY-109564
-
-
- HY-77591
-
-
- HY-N7604
-
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-N0627
-
-
- HY-B0672
-
-
- HY-113013
-
|
Hydroxypyruvic acid
β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-N2094
-
|
Genipin 1-β-D-gentiobioside
Genipin 1-gentiobioside; Genipin 1-β-gentiobioside; Genipin gentiobioside
|
Others
|
Inflammation/Immunology
|
|
Genipin 1-β-D-gentiobioside (Genipin 1-gentiobioside) is one of the most abundant and bioactive iridoid glycosides in Gardenia jasminoides Ellis, which possesses hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.
|
-
- HY-B0151
-
|
Pregnenolone
3β-Hydroxy-5-pregnen-20-one
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication.
|
-
- HY-135588
-
-
- HY-136614
-
|
H-Val-βNA
L-Valine β-naphthylamide
|
Others
|
Others
|
|
H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.
|
-
- HY-A0083
-
|
Methacholine chloride
Acetyl-β-methylcholine chloride
|
mAChR
|
Others
|
|
Methacholine (Acetyl-β-methylcholine) chloride acts a muscarinic M3 receptor agonist in the parasympathetic nervous system. Methacholine chloride acts directly on acetylcholine receptors on smooth muscle causing contraction and airway narrowing. Methacholine challenges are widely used to measure airway hyperresponsiveness (AHR) as a diagnostic aid in the assessment of individuals with asthma-like symptoms and normal resting expiratory flow rates.
|
-
- HY-W007648
-
|
Methyl 3-aminopropanoate hydrochloride
β-Alanine methyl ester hydrochloride
|
Others
|
Others
|
|
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand.
|
-
- HY-P1504A
-
-
- HY-135955
-
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-111974
-
|
β-D-Glucopyranosyl abscisate
ABA-GE; (S)-cis,trans-Abscisic acid glucosyl ester
|
Others
|
Endocrinology
|
|
β-D-Glucopyranosyl abscisate (ABA-GE) is a hydrolyzable abscisic acid (ABA) conjugate that accumulates in the vacuole and presumably also in the endoplasmic reticulum. The deconjugation of β-D-Glucopyranosyl abscisate allows the rapid formation of free ABA in response to abiotic stress conditions such as dehydration and salt stress. β-D-Glucopyranosyl abscisate contributes to the maintenance of ABA homeostasis.
|
-
- HY-N7024
-
-
- HY-N2190
-
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-P2558
-
-
- HY-141133
-
-
- HY-N4179
-
-
- HY-141135
-
-
- HY-141127
-
-
- HY-N7035
-
-
- HY-N3811
-
-
- HY-B0770
-
|
Artemotil
β-Arteether; (+)-Arteether; Arteether
|
Parasite
|
Infection
Cancer
|
|
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys.
|
-
- HY-125033
-
|
EIDD-1931
β-D-N4-hydroxycytidine; NHC
|
SARS-CoV
Enterovirus
HCV
Topoisomerase
|
Infection
|
|
EIDD-1931 (Beta-d-N4-hydroxycytidine; NHC) is a novel nucleoside analog and behaves as a potent anti-virus agent. EIDD-1931 effectively inhibits the replication activity of venezuelan equine encephalitis virus (VEEV), Chikungunya virus (CHIKV) and hepatitis C virus (HCV).
|
-
- HY-18728
-
-
- HY-113949
-
-
- HY-N7681
-
|
Taxifolin 7-O-β-D-glucoside
Taxifolin 7-O-glucoside
|
Others
|
Others
|
|
Taxifolin 7-O-β-D-glucoside (Taxifolin 7-O-glucoside) is one of the main metabolites at the seed germination stage in Scutellaria baicalensis. Taxifolin 7-O-β-D-glucoside, a flavonoid, mainly exists in the episperm and participates in defending against pathogens and UV-damage.
|
-
- HY-N5039
-
-
- HY-N7003
-
|
28-Demethyl-β-amyrone
28-Norolean-12-en-3-one
|
Bacterial
|
Infection
|
|
28-Demethyl-β-amyrone (28-Norolean-12-en-3-one) is one of the main triterpenes from Pistacia lentiscus var. Chia. 28-Demethyl-β-amyrone is an antitoxin and can effectively for the toxic effects of Staphylococcal enterotoxins (SEs).
|
-
- HY-114760
-
|
Vanillic acid glucoside
Vanillic acid 4-β-D-glucoside
|
Others
|
Others
|
|
Vanillic acid glucoside (Vanillic acid 4-β-D-glucoside), a hydrolyzable tannin, is isolated from the fruits of C. annuum as well as the leaves of various additional plants. Vanillic acid glucoside can be phytotoxic against different species.
|
-
- HY-115365
-
-
- HY-133407
-
-
- HY-10512
-
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-111638
-
-
- HY-131086
-
-
- HY-N4008
-
-
- HY-136318
-
-
- HY-N6082
-
|
Rhein 8-Glucoside
Rhein 8-O-β-D-Glucopyranoside
|
Others
|
Metabolic Disease
|
|
Rhein 8-Glucoside (Rhein 8-O-β-D-Glucopyranoside) is an anthraquinone glycoside that has been found in rhubarb. Purgative activity.
|
-
- HY-130929
-
-
- HY-N7628
-
|
Cassiaside C
Toralactone 9-O-β-D-gentiobioside
|
Others
|
Metabolic Disease
|
|
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitory activity on advanced glycation end products (AGE) formation in vitro.
|
-
- HY-B1739
-
|
Pregnenolone monosulfate
3β-Hydroxy-5-pregnen-20-one monosulfate
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate can protect the brain from cannabis intoxication.
|
-
- HY-110189
-
|
Pregnenolone monosulfate sodium salt
3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt
|
Cannabinoid Receptor
Endogenous Metabolite
Autophagy
|
Neurological Disease
|
|
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
|
-
- HY-N5128
-
-
- HY-15583
-
-
- HY-N3893
-
-
- HY-P9911
-
|
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
|
|
Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- HY-131087
-
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-131096
-
-
- HY-107829
-
|
3-Aminopropionitrile fumarate (2:1)
Di-β-aminopropionitrile fumarate; β-Aminopropionitrile fumarate; β-Ammoniumpropionitrile hemifumarate
|
Others
|
Others
|
|
3-Aminopropionitrile fumarate (2:1) is a lathyrogen which inhibits crosslinking of collagen.
|
-
- HY-135591
-
-
- HY-N6958
-
-
- HY-113013A
-
|
Hydroxypyruvic acid lithium hydrate
β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-N5084
-
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM [1].
|
-
- HY-W018512
-
-
- HY-10009
-
-
- HY-N2174
-
-
- HY-N0578
-
|
Apigenin 7-glucoside
Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin
|
Reactive Oxygen Species
|
Cancer
|
|
Apigenin-7-glucoside (Apigenin-7-O-β-D-glucopyranoside) exhibits significant anti-proliferative and antioxidant activity and scavenges reactive oxygen species (ROS).
|
-
- HY-G0025
-
|
Tetrabenazine Metabolite
(-)-β-Dihydrotetrabenazine; (-)-β-HTBZ
|
Monoamine Transporter
Drug Metabolite
|
Neurological Disease
|
|
Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a high affinity (Ki=13.4 nM). Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders.
|
-
- HY-107819
-
-
- HY-141139
-
-
- HY-10590
-
-
- HY-U00424
-
-
- HY-N8441
-
|
Neriifolin
17β-Neriifolin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
|
-
- HY-13335
-
|
PKCβ inhibitor 1
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
|
-
- HY-17631A
-
-
- HY-B0381B
-
-
- HY-117432
-
-
- HY-N4128
-
|
4''-methyloxy-Daidzin
Daidzein 7-O-Β-D-glucoside 4''-O-methylate
|
Others
|
Inflammation/Immunology
|
|
4''-methyloxy-Daidzin (Daidzein 7-O-Β-D-glucoside 4''-O-methylate), an isoflavone methyl-glycoside, is isolated from Cordyceps militaris grown on germinated soybeans. Isoflavones possess immunomodulating and antiallergic activities.
|
-
- HY-19303
-
-
- HY-19383
-
|
Ertiprotafib
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-14879A
-
|
Avibactam sodium
NXL-104
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-14879B
-
|
Avibactam sodium hydrate
NXL-104 hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium hydrate (NXL-104 hydrate) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-N2481
-
|
Oroxylin A-7-O-glucuronide
Oroxyloside; Oroxylin A-7-O-β-D-glucuronide
|
Others
|
Neurological Disease
|
|
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity.
|
-
- HY-B1127
-
|
Betamipron
N-Benzoyl-β-alanine
|
Bacterial
Antibiotic
|
Others
|
|
Betamipron is a chemical compound which is used together with Panipenem to inhibit Panipenem uptake into the renal tubule and prevent nephrotoxicity.
|
-
- HY-18551
-
-
- HY-12292
-
|
IM-12
|
GSK-3
|
Cancer
|
|
IM-12 is an inhibitor of GSK-3β, with an IC50 of 53 nM, and also enhances Wnt signalling.
|
-
- HY-19050
-
-
- HY-128859
-
|
EMT inhibitor-2
|
Cytochrome P450
|
Metabolic Disease
|
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
|
-
- HY-W008566
-
-
- HY-14879
-
|
Avibactam free acid
NXL-104 free acid
|
Bacterial
Antibiotic
|
Infection
|
|
Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
|
-
- HY-N0845
-
-
- HY-P1189
-
|
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-14872
-
|
Tideglusib
NP031112
|
GSK-3
|
Neurological Disease
|
|
Tideglusib (NP031112) is an irreversible GSK-3 inhibitor with IC50s of 5 nM and 60 nM for GSK-3β WT (1 h preincubation) and GSK-3β C199A (1 h preincubation), respectively.
|
-
- HY-18173
-
|
AZD8329
|
Others
|
Metabolic Disease
|
|
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
|
-
- HY-18644
-
|
CWHM-12
|
Integrin
|
Cancer
|
|
CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
|
-
- HY-U00426
-
-
- HY-19676
-
|
Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
-
- HY-P1189A
-
|
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-129453
-
|
BOP sodium
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
|
-
- HY-112359
-
|
C-82
|
β-catenin
Wnt
|
Cancer
|
|
C-82 is a second-generation specific CBP/β-catenin antagonist, which inhibits the binding between β-catenin and CBP and increases the binding between β-catenin and p300.
|
-
- HY-17462
-
|
Adrenosterone
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
|
|
Adrenosterone ((+)-Adrenosterone) is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone also is a selective and competitive inhibitor of hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1).
|
-
- HY-13783
-
|
BIBF0775
|
TGF-β Receptor
|
Cancer
|
|
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
|
-
- HY-B1275A
-
-
- HY-59090
-
|
1-Azakenpaullone
1-Akp
|
GSK-3
|
Metabolic Disease
|
|
1-Azakenpaullone (1-Akp) is a highly selective and ATP-competitive inhibitor of glycogen synthase kinase-3 β (GSK-3β), with an IC50 value of 18 nM.
|
-
- HY-B1418
-
|
Tazobactam
CL-298741; YTR-830H
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam is a beta Lactamase Inhibitor with antibacterial activity
Target: Antibacterial
Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups.
|
-
- HY-136069
-
|
QPX7728
|
Bacterial
|
Infection
|
|
QPX7728 is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. QPX7728 inhibits key serine and metallo beta-lactamases at a nano molar range.
|
-
- HY-10403
-
-
- HY-118810
-
-
- HY-16143
-
|
Cilengitide TFA
EMD 121974 TFA
|
Integrin
Autophagy
|
Cancer
|
|
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.
|
-
- HY-B0320A
-
-
- HY-18748
-
|
BQR-695
NVP-BQR695
|
PI4K
Parasite
|
Infection
|
|
BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.
|
-
- HY-109008
-
|
Nacubactam
OP0595 free acid
|
Bacterial
|
Infection
|
|
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and class C β-lactamases. Nacubactam (OP0595 free acid) acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs.
|
-
- HY-128483
-
-
- HY-18055
-
-
- HY-18053
-
-
- HY-112502
-
|
MethADP
Adenosine 5'-(α,β-methylene)diphosphate
|
CD73
|
Cancer
|
|
MethADP is a specific CD73 inhibitor.
|
-
- HY-12743A
-
-
- HY-12743
-
|
K-7174
|
Others
|
Inflammation/Immunology
|
|
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
|
-
- HY-101275
-
-
- HY-B0445
-
|
NAD+
β-DPN; β-NAD; β-Nicotinamide Adenine Dinucleotide
|
Endogenous Metabolite
|
Metabolic Disease
|
|
NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
|
-
- HY-N0373
-
|
Licochalcone B
|
Amyloid-β
|
Neurological Disease
|
|
Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.
|
-
- HY-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-19306
-
|
SB-267268
|
Integrin
|
Cancer
|
|
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
|
-
- HY-100608
-
|
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-N0527
-
|
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose
|
Influenza Virus
|
Infection
|
|
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
|
-
- HY-N1280
-
|
Semilicoisoflavone B
|
Amyloid-β
|
Neurological Disease
|
|
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
|
-
- HY-19964
-
-
- HY-101091
-
-
- HY-50948
-
-
- HY-112045
-
|
PRI-724
|
Wnt
|
Cancer
|
|
PRI-724 is a selective inhibitor of the CBP/β-catenin interaction.
|
-
- HY-105661
-
-
- HY-16777
-
-
- HY-16752
-
|
Relebactam
MK-7655
|
Bacterial
|
Infection
|
|
Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.
|
-
- HY-15483
-
-
- HY-P1481
-
-
- HY-10985
-
|
Marizomib
Salinosporamide A; NPI-0052
|
Proteasome
|
Cancer
|
|
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-119706
-
|
Barbadin
|
Others
|
Others
|
|
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors.
|
-
- HY-101860
-
-
- HY-120697
-
|
MSAB
|
Wnt
β-catenin
|
Cancer
|
|
MSAB is a potent and selective inhibitor of Wnt/β-catenin signaling. MSAB binds to β-catenin promoting its degradation, and specifically downregulates Wnt/β-catenin target genes. MSAB exhibits potent anti-tumor effects selectively on Wnt-dependent cancer cells.
|
-
- HY-14126
-
-
- HY-103394
-
|
TC HSD 21
|
Others
|
Cancer
|
|
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
|
-
- HY-15721
-
-
- HY-103705
-
-
- HY-19930
-
-
- HY-130119
-
|
Integrin-IN-2
|
Integrin
|
Cancer
|
|
Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively.
|
-
- HY-N6640
-
|
2-O-Acetyl-20-hydroxyecdysone
20-Hydroxyeedysone 2-acetate
|
Others
|
Neurological Disease
|
|
2-O-Acetyl-20-hydroxyecdysone, an ecdysterones in insects and terrestrial plants, inhibits amyloid-β42 (Aβ42)-induced cytotoxicity. 2-O-Acetyl-20-hydroxyecdysone could decrease Aβ oligomer formation through promotion of fibrogenesis, transforming Aβ oligomers to the low-toxicity fibrils.
|
-
- HY-126047B
-
|
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-136393
-
|
IKK-IN-4
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
|
-
- HY-100445
-
-
- HY-15438
-
|
SB 415286
|
GSK-3
Apoptosis
|
Metabolic Disease
|
|
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
|
-
- HY-103374
-
|
Phenserine
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
AChE
Amyloid-β
|
Neurological Disease
|
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease.
|
-
- HY-13060
-
-
- HY-101444A
-
-
- HY-100944
-
-
- HY-107368
-
-
- HY-50949
-
-
- HY-A0256A
-
-
- HY-12704
-
-
- HY-15374
-
-
- HY-B0203A
-
-
- HY-B0203
-
-
- HY-N0074
-
|
Byakangelicol
|
COX
|
Inflammation/Immunology
|
|
Byakangelicol, isolated from Angelica dahurica, inhibits interleukin-1beta (IL-1beta) -induced prostaglandin E2 (PGE2) release in A549 cells mediated by suppression of cyclooxygenase-2 (COX-2) expression and the activity of COX-2 enzyme. Byakangelicol has therapeutic potential as an anti-inflammatory drug on airway inflammation.
|
-
- HY-12012
-
-
- HY-100445A
-
-
- HY-N0270
-
|
Ononin
Ononoside; Formononetin 7-O-β-D-glucopyranoside
|
Others
|
Others
|
|
Ononin is an isoflavonoid, is an additional growth inhibitor in soils associated with the weed, Pluchea lanceolata.
|
-
- HY-13671
-
|
LW6
HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
|
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-N0249
-
|
Saikosaponin C
|
Amyloid-β
|
Neurological Disease
|
|
Saikosaponin C is a bioactive component found in radix bupleuri, targets amyloid beta and tau in Alzheimer's disease. Saikosaponin C inhibits the secretion of both Aβ1-40 and Aβ1-42, and suppresses abnormal tau phosphorylation, but shows no effect on BACE1 activity and expression.
|
-
- HY-100207
-
|
CP21R7
CP21
|
GSK-3
|
Cancer
|
|
CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
|
-
- HY-19918A
-
|
Anatabine dicitrate
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potent α4β2 nAChR agonist. Anatabine dicitrate inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-N4186
-
-
- HY-13027
-
|
DAPT
GSI-IX
|
γ-secretase
Amyloid-β
Autophagy
Notch
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment.
|
-
- HY-100563
-
-
- HY-100563A
-
-
- HY-B0788A
-
-
- HY-B0788
-
|
LY2409881
|
IKK
|
Cancer
|
|
LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
|
-
- HY-A0256B
-
-
- HY-N2566
-
|
Euscaphic acid
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
|
-
- HY-112108
-
|
Chitosan oligosaccharide
COS
|
AMPK
|
Cancer
Metabolic Disease
|
|
Chitosan oligosaccharide (COS) is an oligomer of β-(1→4)-linked D-glucosamine. Chitosan oligosaccharide (COS) activates AMPK and inhibits inflammatory signaling pathways including NF-κB and MAPK pathways.
|
-
- HY-N0042
-
-
- HY-B1154
-
-
- HY-16294
-
|
LY2090314
|
GSK-3
|
Cancer
|
|
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
|
-
- HY-107790
-
|
5-Methoxyflavone
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
|
-
- HY-101090
-
-
- HY-P1420
-
|
TAT-cyclo-CLLFVY
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
|
-
- HY-P0118
-
|
Disitertide
P144
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-14428
-
|
ICG-001
|
β-catenin
Apoptosis
|
Cancer
|
|
ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
|
-
- HY-129492
-
|
GNF4877
|
DYRK
GSK-3
|
Metabolic Disease
|
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
|
-
- HY-101930
-
|
BMS-816336
|
Others
|
Metabolic Disease
|
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
|
-
- HY-15761
-
|
AZD2858
|
GSK-3
|
Neurological Disease
|
|
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
|
-
- HY-107126A
-
|
Ibrexafungerp citrate
MK 3118 citrate; SCY-078 citrate
|
Fungal
|
Infection
|
|
Ibrexafungerp citrate (MK 3118 citrate) is an orally active β-1,3-glucan synthesis inhibitor, with potential antifungal activity. Ibrexafungerp citrate is an investigational agent for the treatment of Candida and Aspergillus infections.
|
-
- HY-111931
-
-
- HY-16659
-
|
EHT 1864
|
Ras
|
Neurological Disease
Cancer
|
|
EHT 1864 is an inhibitor of Rac family small GTPases. EHT 1864 directly binds and impairs the ability of this small GTPase to engage critical downstream effectors required for growth transformation. The Kd values are 40, 50, 60, and 230 nM for Rac1, Rac1b, Rac2 and Rac3, respectively. EHT 1864 also potently inhibits other Rac-dependent transformation processes, Tiam1- and Ras-mediated growth transformation. EHT 1864 prevents Aβ 40 and Aβ 42 production in vivo.
|
-
- HY-N0722
-
-
- HY-101282
-
|
Glutaminyl Cyclase Inhibitor 3
|
Amyloid-β
|
Neurological Disease
|
|
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
|
-
- HY-124257
-
|
(R)-Citronellol
D-Citronellol; (R)-(+)-β-Citronellol
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
(R)-Citronellol (D-Citronellol) is an alcoholic monoterpene found in geranium essential oil. (R)-Citronellol inhibits degranulation of mast cells and does not affect caffeine bitterness perception. (R)-Citronellol can be used in decorative cosmetics, toiletries as well as in non-cosmetic products.
|
-
- HY-B1434
-
-
- HY-16321
-
-
- HY-103095
-
|
AAI101
|
Bacterial
|
Infection
|
|
AAI101 is an extended-spectrum β-lactamase inhibitor, against many resistant Gram-negative pathogens.
|
-
- HY-13019
-
|
BI605906
|
IKK
|
Others
|
|
BI605906 is a novel IKKβ inhibitor with an IC50 value of 380 nM when assayed at 0.1 mM ATP.
|
-
- HY-10344
-
-
- HY-100337
-
-
- HY-14281
-
|
Trilostane
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
|
-
- HY-50884
-
-
- HY-12014
-
-
- HY-76691
-
-
- HY-103241
-
|
Ro 90-7501
|
Amyloid-β
ATM/ATR
Phosphatase
Apoptosis
|
Cancer
Neurological Disease
|
|
Ro 90-7501 is an amyloid β42 (Aβ42) fibril assembly inhibitor that reduces Aβ42-induced cytotoxicity (EC50 of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.
|
-
- HY-P0118A
-
|
Disitertide TFA
P144 TFA
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-B0240
-
|
Disulfiram
Tetraethylthiuram disulfide; TETD
|
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
|
Metabolic Disease
Cancer
|
|
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
|
-
- HY-W010041
-
|
Scyllo-Inositol
|
Amyloid-β
Endogenous Metabolite
|
Neurological Disease
|
|
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.
|
-
- HY-135391
-
-
- HY-113914
-
|
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-B0927
-
|
Hydrastine
(-)-β-Hydrastine; (1R,9S)-β-Hydrastine
|
Others
|
Others
|
|
Hydrastine is a natural alkaloid which is present in Hydrastis canadensis and other plants of the ranunculaceae family.
|
-
- HY-N0410
-
-
- HY-126114
-
|
Lupeol acetate
|
Others
|
Inflammation/Immunology
|
|
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
|
-
- HY-100607A
-
-
- HY-101853
-
-
- HY-U00206
-
-
- HY-B0974
-
-
- HY-B0703
-
-
- HY-137315
-
|
TML-6
|
Amyloid-β
NF-κB
mTOR
Keap1-Nrf2
|
Neurological Disease
|
|
TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.
|
-
- HY-10016
-
|
E 2012
|
γ-secretase
|
Neurological Disease
|
|
E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
|
-
- HY-B0379A
-
|
Adiphenine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has narcotic and anticonvulsant effects.
|
-
- HY-128889
-
-
- HY-10873
-
|
N-Desethyl Sunitinib
SU-12662
|
Others
|
Cancer
|
|
N-Desethyl Sunitinib (SU-12662) is a metabolite of sunitinib. Sunitinib is a potent, ATP-competitive VEGFR, PDGFRβ and KIT inhibitor with Ki values of 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT, respectively.
|
-
- HY-N7115
-
|
Sultamicillin
|
Bacterial
Antibiotic
|
Infection
|
|
Sultamicillin is an orally active double prodrug of Ampicillin/Sulbactan. Sulbactam is a semisynthetic beta-lactamase inhibitor which, in combination with Ampicillin, extends the antibacterial activity of the latter to include some beta-lactamase-producing strains of bacteria that would otherwise be resistant.
|
-
- HY-B2230
-
-
- HY-N2147
-
|
Phorbol
4β-Phorbol
|
Others
|
Cancer
|
|
Phorbol is a highly toxic diterpene, whose esters have important biological properties.
|
-
- HY-13605
-
-
- HY-13605A
-
-
- HY-14823
-
-
- HY-13951
-
-
- HY-N0604
-
-
- HY-111055
-
|
BIP-135
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
|
-
- HY-14176
-
|
Compound E
|
γ-secretase
|
Cancer
|
|
Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
|
-
- HY-A0009
-
|
Galanthamine hydrobromide
Galantamine hydrobromide
|
AChE
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- HY-111184
-
|
PIK-108
|
PI3K
|
Cancer
|
|
PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
|
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-15770
-
|
TR-14035
|
Integrin
|
Inflammation/Immunology
|
|
TR-14035 is a 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 disease.
|
-
- HY-15509A
-
|
Semapimod tetrahydrochloride
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
|
|
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
|
-
- HY-17006
-
-
- HY-B0555A
-
-
- HY-12662
-
-
- HY-12075
-
-
- HY-P1613A
-
-
- HY-13226
-
|
Galunisertib
LY2157299
|
TGF-β Receptor
|
Cancer
|
|
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
|
-
- HY-N0283
-
-
- HY-104050
-
|
M-31850
|
Others
|
Metabolic Disease
|
|
M-31850 is a potent, selective and competitive β-hexosaminidase (Hex) inhibitor with IC50s of 6.0 µM and 3.1 µM for human HexA and human HexB, respectively. M-31850 also competitively inhibits β-N-acetyl-D-hexosaminidase OfHex2 with a Ki of 2.5 μM.
|
-
- HY-103442
-
|
CGP52411
DAPH
|
EGFR
Amyloid-β
|
Cancer
Neurological Disease
|
|
CGP52411 (DAPH) is a high selective, potent, orally active and ATP-competitive EGFR inhibitor with an IC50 of 0.3 μM. CGP52411 blocks the toxic influx of 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-15746
-
-
- HY-124607B
-
|
BRD3731
|
GSK-3
|
Metabolic Disease
Neurological Disease
|
|
BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders.
|
-
- HY-112799
-
|
DK419
|
Wnt
β-catenin
|
Cancer
|
|
DK419 is a potent and orally active Wnt/β-catenin signaling inhibitor, with an IC50 of 0.19 μM. DK419 reduces protein lelvels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin and induces production of pAMPK.
|
-
- HY-10336
-
|
Brivanib (alaninate)
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
|
-
- HY-108628
-
|
SU16f
|
PDGFR
|
Cancer
|
|
SU16f is a potent and selective PDGFRβ inhibitor with IC50s of 10 nM, 140 nM, 2.29 μM for PDGFRβ, PDGFR1, PDGFR2, respectively. Neutralization of PDGFRβ receptor by SU16f blocks the promoting role of GC-MSCs (gastric cancer-derived mesenchymal stem cells) conditioned medium in gastric cancer cell proliferation and migration.
|
-
- HY-B0158
-
-
- HY-N0702
-
|
Tenuifolin
|
Beta-secretase
AChE
|
Neurological Disease
|
|
Tenuifolin is a triterpene isolated from Polygala tenuifolia Willd, has neuroprotective effects. Tenuifolin reduces Aβ secretion by inhibiting β-secretase. Tenuifolin improves learning and memory in aged mice by decreasing AChE activity and has the potential for Alzheimer’s disease (AD) treatment.
|
-
- HY-16910
-
|
WIKI4
|
PARP
β-catenin
|
Cancer
|
|
WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2. WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM.
|
-
- HY-114454
-
|
INH14
|
IKK
|
Cancer
Inflammation/Immunology
|
|
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
|
-
- HY-18710
-
-
- HY-101130
-
-
- HY-12050
-
|
CP-673451
|
PDGFR
|
Cancer
|
|
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-12043
-
|
SB 525334
|
TGF-β Receptor
|
Cancer
|
|
SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
|
-
- HY-17579
-
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-50845
-
|
Avagacestat
BMS-708163
|
γ-secretase
Notch
|
Cancer
|
|
Avagacestat (BMS-708163) is a potent inhibitor of γ-secretase, with IC50s of 0.27 nM and 0.30 nM for Aβ42 and Aβ40 inhibition; Avagacestat (BMS-708163) also inhibits NICD (Notch IntraCellular Domain) with IC50 of 0.84 nM and shows weak inhibition of CYP2C19, with IC50 of 20 μM.
|
-
- HY-B1367
-
|
Carbenoxolone disodium
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
|
-
- HY-U00183
-
-
- HY-15102
-
|
MK-0429
L-000845704
|
Integrin
|
Inflammation/Immunology
Cancer
|
|
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
|
-
- HY-120859A
-
|
Zidebactam sodium salt
WCK-5107 sodium salt
|
Bacterial
|
Infection
|
|
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-P0299
-
|
LSKL, Inhibitor of Thrombospondin (TSP-1)
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.
|
-
- HY-P0299A
-
|
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
|
TGF-β Receptor
|
Cancer
|
|
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier.
|
-
- HY-B0452
-
-
- HY-19468
-
-
- HY-13076
-
|
CHIR-98014
|
GSK-3
|
Metabolic Disease
|
|
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
|
-
- HY-P0023
-
|
Cyclo(-RGDfK)
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-11102
-
-
- HY-18988
-
|
ETC-159
ETC-1922159
|
Porcupine
Wnt
|
Cancer
|
|
ETC-159 (ETC-1922159) is a potent, orally available PORCN inhibitor. ETC-159 inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
|
-
- HY-10256A
-
|
SB 203580 hydrochloride
RWJ 64809 hydrochloride
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
SB 203580 hydrochloride (RWJ 64809 hydrochloride) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 hydrochloride is an autophagy and mitophagy activator.
|
-
- HY-112619
-
|
TES-991
|
Others
|
Metabolic Disease
|
|
TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
|
-
- HY-136071
-
-
- HY-15837
-
|
SAR-260301
|
PI3K
|
Cancer
|
|
SAR-260301 is an orally available and selective PI3Kβ inhibitor with an IC50 of 23 nM.
|
-
- HY-N7111
-
|
Sultamicillin tosylate
|
Bacterial
|
Infection
|
|
Sultamicillin (tosylate) is a potent and orally active beta-lactamase inhibitor, an antibiotic with antibacterial activity. Sultamicillin (tosylate) is the tosylate salt of the double ester of sulbactam plus ampicillin.
|
-
- HY-100198
-
-
- HY-136070
-
-
- HY-16265
-
-
- HY-B0942
-
-
- HY-138617
-
|
AI-10-47
|
Others
|
Cancer
|
|
AI-10-47 is a small molecule inhibitor of CBFβ-RUNX binding, with an IC50 of 3.2 μM.
|
-
- HY-N9331
-
|
Cimicifugoside H-1
Cimicidanol-3-O-β-d-xyloside
|
Others
|
Metabolic Disease
|
|
Cimicifugoside H-1, a cyclolanostanol xyloside, is a major constituent of C. foetida L. extract. Cimicifugoside H-1 inhibits bone resorption and ovariectomy-induced bone loss.
|
-
- HY-10230
-
|
Midostaurin
PKC412; CGP 41251
|
PKC
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-125263
-
|
OP-1074
|
Estrogen Receptor/ERR
|
Cancer
|
|
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
|
-
- HY-P0023A
-
|
Cyclo(-RGDfK) TFA
|
Integrin
|
Cancer
|
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-111267
-
-
- HY-109103
-
|
Tegatrabetan
BC2059
|
β-catenin
|
Cancer
|
|
Tegatrabetan (BC2059) is a β-Catenin antagonist. Tegatrabetan disrupts the binding of β-catenin with the scaffold protein transducin β-like 1 (TBL1).
|
-
- HY-75385
-
-
- HY-112220
-
|
VIT-2763
|
Others
|
Metabolic Disease
|
|
VIT-2763, an oral ferroportin inhibitor, inhibits hepcidin binding to ferroportin and blocks iron efflux. VIT-2763 has the potential in the treatment of β-thalassemia.
|
-
- HY-100444
-
-
- HY-B0573
-
|
Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-B0573B
-
|
Propranolol
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
Endocrinology
|
|
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-131447
-
|
KY19382
A3051
|
GSK-3
|
Metabolic Disease
|
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
|
-
- HY-119037
-
|
UK-101
|
Proteasome
Apoptosis
|
Cancer
|
|
UK-101 is a potent and selective immunoproteasome β1i (LMP2) inhibitor with an IC50 value of 104 nM, displays 144- and 10-fold selectivity over β1c (IC50=15 μM) and β5 subunit (IC50=1 μM), respectivey. UK-101 induces cell apoptosis and can be used for the study of prostate cancer.
|
-
- HY-103200
-
-
- HY-100672
-
-
- HY-101085
-
|
SKL2001
|
Wnt
β-catenin
|
Cancer
|
|
SKL2001 is an agonist of the Wnt/β-catenin pathway, with anti-cancer activity. SKL2001 stabilizes intracellular β-catenin via disruption of the Axin/β-catenin interaction.
|
-
- HY-18959
-
|
CWP232228
|
β-catenin
Wnt
|
Cancer
|
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
|
-
- HY-137472
-
|
SAR502250
|
GSK-3
|
Neurological Disease
|
|
SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-101271
-
-
- HY-75385A
-
-
- HY-13535
-
|
ATN-161
|
Integrin
|
Cancer
|
|
ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
|
-
- HY-109190
-
|
Seralutinib
GB002; PK10571
|
PDGFR
|
Cardiovascular Disease
|
|
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
|
-
- HY-16276
-
-
- HY-W001941
-
|
D-Cystine
|
Others
|
Others
|
|
D-Cystine is the D-enantiomer of L-Cystine. D-Cystine inhibits L-aspartate-β-semialdehyde dehydrogenase (ASADH) from Escherichia coli.
|
-
- HY-13535A
-
-
- HY-13713
-
-
- HY-15147
-
|
XAV-939
|
β-catenin
PARP
|
Cancer
|
|
XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively).
|
-
- HY-129113
-
|
α-Chaconine
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-10453
-
|
Ixazomib
MLN2238
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-112182
-
|
UM-164
DAS-DFGO-II
|
Src
p38 MAPK
Autophagy
|
Cancer
|
|
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
|
-
- HY-111507
-
|
PDGFRα kinase inhibitor 1
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-10256
-
|
SB 203580
RWJ 64809
|
p38 MAPK
Autophagy
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
|
-
- HY-14300A
-
-
- HY-P2285
-
|
AC 253
|
Amyloid-β
|
|
|
AC 253 is an Amylin (AMY3) receptor antagonist, inhibiting andrenomedulin-stimulated cAMP production. AC 253 protects against oligomeric Aβ-induced increase in intracellular Ca2+, activation of PKA, MAPK, Akt and cFOS and cell death in neuronal cell culture. AC 253 blocks electrophysiological effects of Aβ.
|
-
- HY-112613
-
|
UCB9608
|
PI4K
|
Inflammation/Immunology
|
|
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
|
-
- HY-N0633
-
-
- HY-19717
-
|
DCVC
S-[(1E)-1,2-dichloroethenyl]--L-cysteine
|
TNF Receptor
|
Inflammation/Immunology
|
|
DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
|
-
- HY-W050031
-
|
(S)-3-Hydroxybutanoic acid
(S)-β-Hydroxybutanoic acid; L-(+)-3-Hydroxybutyric acid; L-β-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(S)-3-Hydroxybutanoic acid is a normal human metabolite, that has been found elevated in geriatric patients remitting from depression. In humans, 3-Hydroxybutyric acid is synthesized in the liver from acetyl-CoA, and can be used as an energy source by the brain when blood glucose is low.
|
-
- HY-A0295
-
-
- HY-W009009
-
|
L-838417
|
GABA Receptor
|
Neurological Disease
|
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
|
-
- HY-14300
-
-
- HY-N4326
-
-
- HY-W010201
-
|
Citronellol
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
|
Cancer
|
|
Citronellol ((±)-Citronellol) is a monoterpene Pelargonium capitatum. Citronellol ((±)-Citronellol) induces necroptosis of cancer cell via up-regulating TNF-α, RIP1/RIP3 activities, down-regulating caspase-3/caspase-8 activities and increasing ROS (reactive oxygen species) accumulation.
|
-
- HY-N2022
-
|
Castanospermine
|
Glucosidase
|
Cancer
|
|
Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
|
-
- HY-16665
-
|
iCRT 14
|
Wnt
|
Cancer
|
|
iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT), with IC50 of 40.3 nM against Wnt responsive STF16 luciferase.
|
-
- HY-75124
-
|
(Rac)-AZD 6482
(Rac)-KIN-193
|
PI3K
Autophagy
|
Cancer
|
|
(Rac)-AZD 6482 ((Rac)-KIN-193) is the racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
|
-
- HY-12325
-
|
GSK2194069
|
Others
|
Cancer
|
|
GSK2194069 is a potent and specific inhibitor of the β-ketoacyl reductase (KR) activity of hFAS with an IC50 of 7.7 ± 4.1 nM in an assay detecting released CoA.
|
-
- HY-100506
-
|
GLPG0187
|
Integrin
|
Cancer
|
|
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
|
-
- HY-108313
-
|
T-00127_HEV1
|
PI4K
|
Infection
|
|
T-00127_HEV1 is a phosphatidylinositol 4-kinase III beta (PI4KB) inhibitor with an IC50 of 60 nM.
|
-
- HY-B1643
-
-
- HY-N2215
-
-
- HY-10407
-
|
SU 5402
|
VEGFR
FGFR
PDGFR
|
Cancer
|
|
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
|
-
- HY-14503
-
|
MDR-1339
DWK-1339
|
Amyloid-β
|
Neurological Disease
|
|
MDR-1339 (DWK-1339) is an orally active and blood-brain-barrier-permeable Aβ-aggregation inhibitor, used in the research of Alzheimer's disease.
|
-
- HY-N6712
-
|
Thiolutin
Acetopyrrothin
|
Bacterial
Antibiotic
|
Infection
Metabolic Disease
|
|
Thiolutin (Acetopyrrothin) is a disulfide-containing antibiotic and anti-angiogenic compound produced by Streptomyces. Thiolutin inhibits the JAMM metalloproteases Csn5, Associated-molecule-with-the-SH3-Domain-of-STAM (AMSH) and Brcc36. Thiolutin is a potent and selective inhibitor of endothelial cell adhesion accompanied by rapid induction of Heat-shock protein beta-1 (Hsp27) phosphorylation.
|
-
- HY-110266
-
|
GN44028
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
|
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-120789
-
|
PF-06648671
|
γ-secretase
|
Neurological Disease
|
|
PF-06648671 is a novel, brain‐penetrable, and orally active γ‐secretase modulator (GSM). PF-06648671 reduces Aβ42 and Aβ40, with concomitant increases in Aβ37 and Aβ38 in vitro. PF-06648671 is used for the study of Alzheimer’s disease.
|
-
- HY-14951
-
|
Firategrast
SB 683699
|
Integrin
|
Neurological Disease
|
|
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-N0540
-
|
Cynaroside
Luteolin 7-glucoside; Luteolin 7-O-β-D-glucoside
|
Influenza Virus
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Cynaroside (Luteolin 7-glucoside) is a flavone, a flavonoid-like chemical compound. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-100538A
-
|
DTP3 TFA
|
DNA/RNA Synthesis
JNK
|
Cancer
|
|
DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
|
-
- HY-111930
-
|
5-Iodo-indirubin-3'-monoxime
|
GSK-3
CDK
|
Cancer
|
|
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
|
-
- HY-13289A
-
|
Nepicastat hydrochloride
SYN-117 hydrochloride; RS-25560-197 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-101930B
-
|
(R)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively [1].
|
-
- HY-N7697B
-
-
- HY-13438
-
|
AZD3839 free base
|
Beta-secretase
|
Cancer
|
|
AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor.
|
-
- HY-13862
-
|
AZD1080
|
GSK-3
|
Neurological Disease
|
|
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
|
-
- HY-14302
-
-
- HY-17453
-
-
- HY-10431
-
-
- HY-10452
-
|
Ixazomib citrate
MLN9708
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
|
-
- HY-10114
-
|
TGX-221
|
PI3K
|
Cancer
|
|
TGX-221 is a potent, selective, and cell membrane permeable inhibitor of the PI3K p110β catalytic subunit, used for cancer treatment.
|
-
- HY-50883
-
|
BMS 299897
|
γ-secretase
|
Neurological Disease
|
|
BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
|
-
- HY-112444
-
-
- HY-111365
-
|
TES-1025
|
Others
|
Metabolic Disease
|
|
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
|
-
- HY-50949A
-
-
- HY-W009168
-
|
Tazobactam sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Tazobactam sodium is an antibiotic of the beta-lactamase inhibitor class. Ceftolozane combines with Tazobactam, extends the activity of ceftolozane against many ESBL-producing Enterobacteriaceae and some Bacteroides spp..
|
-
- HY-10456
-
|
TAK-715
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
|
-
- HY-135674
-
|
SR-318
|
p38 MAPK
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
|
-
- HY-19807
-
|
Indirubin-3'-monoxime
Indirubin-3'-oxime
|
GSK-3
Lipoxygenase
|
Cancer
|
|
Indirubin-3'-monoxime is a potent GSK-3β inhibitor, and weakly inhibits 5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitory activities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
|
-
- HY-10580
-
|
GSK 3 Inhibitor IX
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-111760
-
|
NRX-252262
|
β-catenin
|
Cancer
|
|
NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCF β-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM.
|
-
- HY-130609A
-
|
Aβ42-IN-1 free base
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
|
-
- HY-136449
-
-
- HY-14652
-
-
- HY-107437
-
-
- HY-131166
-
|
Curdlan
|
Others
|
Others
|
|
Curdlan is a polysaccharide produced by bacteria and a homopolymer of glucose with β-1,3-glucosidic linkage.
|
-
- HY-B0573A
-
|
(S)-(-)-Propranolol hydrochloride
|
Adrenergic Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
(S)-(-)-Propranolol hydrochloride is a β-adrenergic receptor antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively. (S)-(-)-Propranolol hydrochloride the active enantiomer of propranolol and can be s used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-117388
-
|
THI0019
|
Integrin
|
Inflammation/Immunology
|
|
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
|
-
- HY-124290
-
|
Carotegrast methyl
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-130252
-
|
YQ128
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
|
-
- HY-13289
-
|
Nepicastat
SYN117; RS-25560-197
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).
|
-
- HY-18754
-
|
FR 167653 free base
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 free base, an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 free base is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
|
-
- HY-111424
-
|
BDP9066
|
Ras
|
Cancer
|
|
BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC50 of 64 nM for MRCKβ in SCC12 cells, Ki values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.
|
-
- HY-107531
-
|
A 1070722
|
GSK-3
|
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-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 prodrug 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-14649
-
|
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-15198
-
|
KG5
|
Raf
PDGFR
FLT3
c-Kit
|
Cancer
|
|
KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
|
-
- HY-B0573S
-
|
Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy.
|
-
- HY-120215
-
|
KT203
|
MAGL
|
Metabolic Disease
|
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
|
-
- HY-120177
-
|
KT182
|
MAGL
|
Others
|
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
|
-
- HY-10501
-
|
SU14813
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
|
-
- HY-10501A
-
-
- HY-14975
-
-
- HY-10514
-
|
BX795
|
PDK-1
IKK
Autophagy
|
Cancer
|
|
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
|
-
- HY-15614A
-
|
SC144 hydrochloride
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells.
|
-
- HY-10230S
-
|
Midostaurin-D5
PKC412-D5; CGP 41251-D5
|
Others
|
Cancer
|
|
Midostaurin-D5 (PKC412-D5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- HY-15614
-
|
SC144
|
Interleukin Related
Apoptosis
|
Cancer
|
|
SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.
|
-
- HY-119940
-
|
MC180295
(rel)-MC180295
|
CDK
|
Cancer
|
|
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
|
-
- HY-N6630
-
-
- HY-A0275
-
-
- HY-12216
-
-
- HY-135119
-
|
Salmeterol-D3
|
Adrenergic Receptor
|
Endocrinology
Inflammation/Immunology
|
|
Salmeterol-D3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
|
-
- HY-13904
-
|
Flumatinib
HHGV678
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
|
-
- HY-13013
-
|
(E)-SIS3
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
(E)-SIS3 is a potent and selective inhibitor of Smad3 with an IC50 of 3 μM for Smad3 phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts by TGF-β1.
|
-
- HY-13905
-
|
Flumatinib mesylate
HHGV678 mesylate
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
Flumatinib mesylate (HHGV678 mesylate) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
|
-
- HY-P1376
-
|
G-Protein antagonist peptide
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-136207
-
|
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-N0582
-
|
Qingyangshengenin B
|
Others
|
Neurological Disease
|
|
Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.
|
-
- HY-N7652
-
|
Terminolic acid
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity.
|
-
- HY-10974
-
|
MK-0752
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo.
|
-
- HY-18754A
-
|
FR 167653
FR 167653 sulfate
|
p38 MAPK
Autophagy
|
Endocrinology
|
|
FR 167653 (FR 167653 sulfate), an orally active and selective p38 MAPK inhibitor, is a potent suppressor of TNF-α and IL-1β production via specific inhibition of p38 MAPK activity. FR 167653 (FR 167653 sulfate) is effective in treating inflammation, relieving trauma and ischemia-reperfusion injury in vivo.
|
-
- HY-111911
-
-
- HY-103456
-
-
- HY-100935S
-
|
Cimaterol-D7
|
Adrenergic Receptor
|
Endocrinology
|
|
Cimaterol-D7 is the deuterium labeled Cimaterol. Cimaterol is a potent agonist of β-adrenergic receptors (pEC50s=8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively). Cimaterol has been used in farmed animals to increase carcass mass and to alter muscle and fat deposition.
|
-
- HY-10215
-
|
Luminespib
VER-52296; AUY922; NVP-AUY922
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
|
-
- HY-N2523
-
|
Gigantol
|
Wnt
|
Cancer
|
|
Gigantol is a bibenzyl compound derived from several medicinal orchids. Giganto shows promising therapeutic potential against cancer cells. Gigantol is a novel inhibitor of the Wnt/β-catenin pathway.
|
-
- HY-N7368
-
-
- HY-117771
-
|
DO34
|
Others
|
Metabolic Disease
|
|
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
|
-
- HY-B1189
-
-
- HY-14316A
-
|
Tebanicline dihydrochloride
Ebanicline dihydrochloride; ABT-594 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
|
-
- HY-13005
-
|
Fagomine
D-Fagomine
|
Others
|
Metabolic Disease
|
|
Fagomine is a mild glycosidase inhibitor. The Ki of the iminosugar Fagomine is 4.8 μM, 39 μM, and 70 μM for Amyloglucosidase (A.niger), β-Glucosidase (bovine), and Isomaltase (yeast), respectively.
|
-
- HY-13689
-
|
Go 6983
Gö 6983; Goe 6983
|
PKC
|
Cancer
|
|
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
|
-
- HY-78349
-
|
A 77-01
|
TGF-β Receptor
|
Cancer
|
|
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
|
-
- HY-12437
-
|
BDP5290
|
ROCK
|
Cancer
|
|
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
|
-
- HY-100760
-
|
Toxoflavin
Xanthothricin; Toxoflavine; PKF-118-310
|
β-catenin
|
Cancer
|
|
Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex, also acts as an inhibitor of KDM4A, with antitumor activity.
|
-
- HY-10401
-
-
- HY-N1431A
-
|
Tabersonine hydrochloride
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Tabersonine hydrochloride is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and is a potential therapeutic candidate for the treatment of ALI/ARDS.
|
-
- HY-N0001
-
-
- HY-16988A
-
-
- HY-A0070
-
-
- HY-16989
-
|
SR9009
|
Autophagy
|
Cancer
|
|
SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-108013
-
-
- HY-16988
-
|
SR9011
|
Autophagy
|
Cancer
|
|
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-A0070A
-
-
- HY-N1431
-
|
Tabersonine
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Tabersonine is an indole alkaloid mainly isolated from Catharanthus roseus. Tabersonine disrupts Aβ(1-42) aggregation and ameliorates Aβ aggregate-induced cytotoxicity. Tabersonine has anti-inflammatory activities and acts as a potential therapeutic candidate for the treatment of ALI/ARDS.
|
-
- HY-100469
-
|
LXRβ agonist-2
|
LXR
|
Cardiovascular Disease
|
|
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
|
-
- HY-119109
-
|
Laminaran
|
Others
|
Cancer
|
|
Laminaran is a neutral water-soluble β-1-3-glucan and a typical ligand for Dectin-1 isolated from the brown alga D. dichotoma, has potent immunomodulating, radioprotective, and anticancer activities. Laminaran is made up of β (1→3)-glucan with β (1→6)-branches and can be catalyzed by enzymes such as laminarinase (EC 3.2.1.6) that breaks the β (1→3) bonds. Laminaran is a promising immune stimulatory molecule for use in cancer immunotherapy.
|
-
- HY-P1376A
-
|
G-Protein antagonist peptide TFA
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide TFA competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
|
-
- HY-11001
-
|
PHA-793887
|
CDK
Apoptosis
|
Cancer
|
|
PHA-793887 is a potent, ATP-competitive CDK inhibitor, can inhibit Cdk2, Cdk1, Cdk4, and Cdk9 with IC50s of 8 nM, 60 nM, 62 nM and 138 nM, respectively, and also inhibits glycogen synthase kinase 3β with an IC50 of 79 nM.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-N0665
-
|
Specnuezhenide
(8E)-Nuezhenide
|
NF-κB
Wnt
|
Inflammation/Immunology
|
|
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).
|
-
- HY-103238
-
|
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
|
-
- HY-12383
-
|
Pelubiprofen
|
COX
|
Inflammation/Immunology
Neurological Disease
|
|
Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
|
-
- HY-18054
-
|
BVT 2733
|
Others
|
Inflammation/Immunology
|
|
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
|
-
- HY-P0178
-
|
LXW7
|
Integrin
|
Inflammation/Immunology
|
|
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-B0436
-
-
- HY-13815
-
|
KY02111
|
Wnt
|
Cardiovascular Disease
|
|
KY02111 is a canonical WNT signaling (β-catenin) inhibitor which promotes differentiation of hPSCs to cardiomyocytes. KY02111 can be used for the research of human cardiomyocyte regeneration.
|
-
- HY-B1100
-
-
- HY-16786
-
|
AI-10-49
|
Others
|
Cancer
|
|
AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.
|
-
- HY-13469
-
|
Debio 0932
CUDC-305
|
HSP
|
Cancer
|
|
Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
|
-
- HY-50673
-
|
Dactolisib
BEZ235; NVP-BEZ235
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2.
|
-
- HY-12826
-
|
IMB-XH1
|
Bcl-2 Family
Bacterial
|
Cancer
|
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1). IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively.
|
-
- HY-13205
-
|
Belnacasan
VX-765
|
Caspase
|
Inflammation/Immunology
|
|
Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
|
-
- HY-131040
-
|
NLRP3-IN-NBC6
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs).
|
-
- HY-B0849
-
|
Azoxystrobin
|
Fungal
Reactive Oxygen Species
Apoptosis
|
Infection
|
|
Azoxystrobin is a broad-spectrum β-methoxyacrylate fungicide. Azoxystrobin inhibits mitochondrial respiration by binding to the Qo site of the cytochrome bc1 complex and inhibiting electron transfer. Azoxystrobin induces the production of reactive oxygen species (ROS) and induces cell apoptosis.
|
-
- HY-135670
-
|
Glycosidase-IN-1
|
Others
|
Metabolic Disease
|
|
Glycosidase-IN-1 (Compound 9) is a glycosidase inhibitor synthesized from D-mannose. Glycosidase-IN-1 be used to synthesize some immunosuppressive agents and β-glucosidase inhibitors. Glycosidase-IN-1 has hypoglycemic activity.
|
-
- HY-12302
-
|
Kenpaullone
9-Bromopaullone; NSC-664704
|
CDK
GSK-3
|
Cancer
|
|
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
|
-
- HY-N0377
-
-
- HY-B1459
-
|
Dicloxacillin sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Dicloxacillin sodium is a narrow-spectrum β-lactam antibiotic of the penicillin family. Dicloxacillin sodium is active against β-lactamase-producing organisms such as Staphylococcus aureus.
|
-
- HY-107489
-
|
RO 4938581
|
GABA Receptor
|
Neurological Disease
|
|
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
|
-
- HY-100886
-
|
BAY1082439
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
|
-
- HY-N0012
-
|
Glycitin
Glycitein 7-O-β-glucoside
|
Influenza Virus
Bacterial
|
Cancer
Infection
|
|
Glycitin is a natural isoflavone isolated from legumes; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.Glycitin is antibacterial, antiviral and estrogenic.
|
-
- HY-N0203
-
|
Atractylenolide III
ICodonolactone; 8β-Hydroxyasterolide
|
Apoptosis
|
Cancer
|
|
Atractylenolide III is a major component of Atractylodes rhizome can induce apoptosis of the lung carcinoma cells.
|
-
- HY-N0176
-
-
- HY-N0610A
-
|
Cinnamic acid
3-Phenylacrylic acid; β-Phenylacrylic acid
|
Endogenous Metabolite
|
Cancer
|
|
Cinnamic acid has potential use in cancer intervention, with IC50s of 1-4.5 mM in glioblastoma, melanoma, prostate and lung carcinoma cells.
|
-
- HY-B1035
-
-
- HY-B1392
-
-
- HY-101658
-
-
- HY-101817
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-112331
-
|
SJ000291942
|
TGF-β Receptor
|
Cancer
|
|
SJ000291942 is an activator of the canonical bone morphogenetic proteins (BMP) signaling pathway. BMPs are members of the transforming growth factor beta (TGFβ) family of secreted signaling molecules.
|
-
- HY-14537
-
-
- HY-N3514
-
|
Kuwanon E
|
Others
|
Cancer
|
|
Kuwanon E is a flavonoid isolated from Morus alba, cytotoxic to human monocytic leukemic cell lines, and reduces the level of IL-1β.
|
-
- HY-103207
-
-
- HY-129630
-
-
- HY-16708A
-
|
ZLN024 hydrochloride
|
AMPK
|
Metabolic Disease
|
|
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-14933
-
|
Prinaberel
ERB-041
|
Estrogen Receptor/ERR
Wnt
Apoptosis
|
Cancer
|
|
Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis.
|
-
- HY-16708
-
|
ZLN024
|
AMPK
|
Metabolic Disease
|
|
ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-13520
-
|
Nocodazole
Oncodazole; R17934
|
Microtubule/Tubulin
Bcr-Abl
CRISPR/Cas9
Autophagy
Apoptosis
|
Cancer
|
|
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
|
-
- HY-13453
-
|
BAY 11-7082
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
|
-
- HY-14838
-
-
- HY-112157
-
-
- HY-10402
-
-
- HY-14838A
-
-
- HY-109052
-
|
Atabecestat
JNJ-54861911
|
Beta-secretase
|
Neurological Disease
|
|
Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
|
-
- HY-P0178A
-
|
LXW7 TFA
|
Integrin
|
Inflammation/Immunology
|
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
|
-
- HY-10472
-
|
LY2811376
|
Beta-secretase
|
Neurological Disease
|
|
LY2811376 is the first orally available non-peptidic β-secretase (BACE1) inhibitor with IC50 of 239 nM-249 nM, that acts to decrease Aβ secretion with EC50 of 300 nM, and demonstrates to have 10-fold selectivity towards BACE1 over BACE2, and more than 50-fold inhibition over other aspartic proteases including cathepsin D, pepsin, or renin.
|
-
- HY-122537A
-
|
Arotinolol
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-134130
-
|
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-17497A
-
-
- HY-102028
-
|
KY1220
|
Wnt
β-catenin
|
Cancer
|
|
KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway; with an IC50 of 2.1 μM in HEK293 reporter cells.
|
-
- HY-14399
-
-
- HY-121251
-
-
- HY-108437
-
|
exo-IWR-1
|
Wnt
|
Cancer
Infection
|
|
exo-IWR-1, an inactive stereoisomer of Endo-IWR-1, is a negative control of IWR-1 (HY-12238). IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-B0334
-
|
Sulbactam
CP45899
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.
|
-
- HY-13514
-
|
TG 100713
|
PI3K
|
Cancer
|
|
TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.
|
-
- HY-N0602
-
-
- HY-13493
-
|
AC710
|
PDGFR
c-Kit
FLT3
|
Cancer
|
|
AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-17044
-
|
Duvelisib
IPI-145; INK1197
|
PI3K
|
Cancer
|
|
Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
|
-
- HY-15190
-
|
NVP-HSP990
HSP-990
|
HSP
Apoptosis
|
Cancer
|
|
NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
|
-
- HY-14175
-
|
Begacestat
GSI-953
|
γ-secretase
|
Neurological Disease
|
|
Begacestat (GSI-953) is a selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase (IC50Aβ40=15 nM) for the treatment of Alzheimer's disease.
|
-
- HY-11035
-
|
WAY-262611
|
β-catenin
|
Cancer
|
|
WAY-262611 is a wingless β-Catenin agonist that increases bone formation rate with an EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also a Dkk1 inhibitor.
|
-
- HY-12113
-
|
Oprozomib
ONX 0912; PR-047
|
Proteasome
Autophagy
|
Cancer
|
|
Oprozomib (ONX 0912; PR047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM.
|
-
- HY-N1949
-
|
Homoplantaginin
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
|
-
- HY-B0334A
-
|
Sulbactam sodium
CP45899 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex.
|
-
- HY-13493A
-
|
AC710 Mesylate
|
PDGFR
|
Cancer
|
|
AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-18179
-
|
AZD2932
|
PDGFR
VEGFR
FLT3
c-Kit
|
Cancer
|
|
AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
|
-
- HY-10320
-
|
Doramapimod
BIRB 796
|
p38 MAPK
Raf
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
|
-
- HY-101752
-
-
- HY-U00016
-
-
- HY-100141
-
-
- HY-111413
-
-
- HY-B1486
-
-
- HY-18295
-
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
|
-
- HY-136866
-
|
Aβ42-IN-2
|
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-117482
-
|
BPN-15606
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
|
-
- HY-15174
-
|
Dactolisib Tosylate
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
|
-
- HY-108470
-
|
Ro5-3335
|
Others
|
Cancer
|
|
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.
|
-
- HY-12046
-
|
PIK-93
|
PI4K
PI3K
Virus Protease
|
Cancer
|
|
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
|
-
- HY-105272A
-
-
- HY-B1270
-
-
- HY-105272
-
|
Loreclezole
R 72063
|
GABA Receptor
|
Neurological Disease
|
|
Loreclezole, an antiepileptic compound, is a selective GABAA receptor modulator and acts as a positive allosteric modulator of β2 or β3-subunit containing receptors.
|
-
- HY-111413A
-
-
- HY-15356
-
-
- HY-10342
-
|
Enzastaurin
LY317615
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
|
-
- HY-136392
-
|
IKK-IN-3
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively.
|
-
- HY-15897
-
|
LDN-212854
|
TGF-β Receptor
|
Cancer
|
|
LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
|
-
- HY-103021
-
|
LY3200882
|
TGF-β Receptor
|
Cancer
Inflammation/Immunology
|
|
LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.
|
-
- HY-N0158
-
|
Oxymatrine
|
TGF-beta/Smad
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
|
-
- HY-U00205
-
-
- HY-113404
-
-
- HY-B1286
-
-
- HY-B1463
-
-
- HY-U00066
-
-
- HY-101691
-
-
- HY-100634
-
|
4-Hydroxypropranolol hydrochloride
(±)-4-hydroxy Propranolol hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-107589A
-
|
BIO5192 hydrate
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-107589
-
|
BIO5192
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-N7204
-
-
- HY-114320
-
|
BuChE-IN-TM-10
TM-10
|
AChE
|
Neurological Disease
|
|
BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease.
|
-
- HY-W015445
-
|
SD-169
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-N0815
-
|
Resibufogenin
Bufogenin; Recibufogenin
|
Others
|
Cancer
|
|
Resibufogenin, a component of huachansu, has been shown to exhibit the anti-proliferative effect against cancer cells, and this may be attributed to the degradation of cyclin D1 caused by the activation of GSK-3β.
|
-
- HY-15504A
-
|
RGB-286638 free base
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
|
RGB-286638
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-116446
-
|
Pironetin
|
Microtubule/Tubulin
|
Cancer
|
|
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.
|
-
- HY-10517
-
|
Orantinib
SU6668; TSU-68
|
PDGFR
FGFR
VEGFR
Apoptosis
|
Cancer
|
|
Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
|
-
- HY-10065
-
|
Axitinib
AG-013736
|
VEGFR
PDGFR
|
Cancer
|
|
Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
|
-
- HY-P0318
-
-
- HY-N0250
-
-
- HY-100711
-
|
Prodigiosin
Prodigiosine
|
Wnt
Bacterial
Fungal
Parasite
Apoptosis
|
Cancer
Infection
|
|
Prodigiosin (Prodigiosine) is a red pigment produced by bacteria as a bioactive secondary metabolite. Prodigiosin is a potent inhibitor of the Wnt/β-catenin pathway. Prodigiosin has antibacterial, antifungal, antiprotozoal, antimalarial, immunosuppressive, and anticancer properties.
|
-
- HY-16268
-
|
Kartogenin
KGN
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
|
-
- HY-112769
-
|
EX229
|
AMPK
|
Metabolic Disease
|
|
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
|
-
- HY-15244
-
|
Alpelisib
BYL-719
|
PI3K
|
Cancer
|
|
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
|
-
- HY-P0154
-
|
Epsilon-V1-2
ε-V1-2; EAVSLKPT
|
PKC
|
Inflammation/Immunology
|
|
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
|
-
- HY-19622
-
|
PF-9184
|
PGE synthase
|
Inflammation/Immunology
|
|
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
|
-
- HY-17406
-
|
Tolcapone
Ro 40-7592
|
COMT
Amyloid-β
|
Neurological Disease
|
|
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-B0422
-
|
Nateglinide
A4166; Senaglinide
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-N0044
-
-
- HY-10408
-
|
Ki20227
|
c-Fms
VEGFR
c-Kit
PDGFR
|
Inflammation/Immunology
|
|
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
|
-
- HY-135366
-
|
HPN-01
|
IKK
|
Inflammation/Immunology
|
|
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
|
-
- HY-N0619
-
|
Mulberroside A
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-16316
-
-
- HY-101585
-
-
- HY-U00278
-
|
Deloxolone
(3β,20β)-3-(3-Carboxy-1-oxopropoxy)olean-9(11)-en-29-oic acid
|
Others
|
Inflammation/Immunology
|
|
Deloxolone has the potential for inflammatory, ischemic and proliferative diseases treatment.
|
-
- HY-P1060
-
|
LPYFD-NH2
|
Amyloid-β
|
Neurological Disease
|
|
LPYFD-NH2, a pentapeptide, exerts some inhibitory effect on the aggregation of Aβ(1-42). LPYFD-NH2 can be used for the research of Alzheimer’s disease.
|
-
- HY-B1276A
-
-
- HY-100370
-
|
MRK-016
|
GABA Receptor
|
Cancer
|
|
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
|
-
- HY-131997
-
|
2'MeO6MF
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
|
-
- HY-13598
-
|
Valecobulin
CKD-516
|
Microtubule/Tubulin
|
Cancer
|
|
Valecobulin (CKD516) is a valine prodrug of (S516) and a vascular disrupting agent (VDA). Valecobulin is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
|
-
- HY-N2998
-
|
Ganoderenic acid A
|
Others
|
Metabolic Disease
|
|
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury.
|
-
- HY-50698
-
-
- HY-N0116
-
|
Hematoxylin
Natural Black 1; Haematoxylin
|
Amyloid-β
|
Others
|
|
Hematoxylin (Natural Black 1), a naturally occurring flavonoid compound derived from the logwood tree, Haematoxylon campechianum. Hematoxylin is a nuclear stain in histology and is also a potent Aβ42 fibrillogenesis inhibitor with an IC50 of 1.6 µM.
|
-
- HY-13223
-
|
Crenolanib
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-N0020
-
|
Echinacoside
|
Wnt
Reactive Oxygen Species
|
Neurological Disease
|
|
Echinacoside, one of the phenylethanoids isolated from the stems of Cistanche salsa, effectively inhibits Wnt/β-catenin signaling. Echinacoside elicits neuroprotection by activating Trk receptors and their downstream signal pathways. Antiosteoporotic activity.
|
-
- HY-15473
-
|
MLN120B
ML120B
|
IKK
|
Cancer
|
|
MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-15473A
-
|
MLN120B dihydrochloride
ML120B dihydrochloride
|
IKK
|
Cancer
Inflammation/Immunology
|
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-12903
-
|
Macozinone
PBTZ169
|
Bacterial
|
Infection
|
|
Macozinone (PBTZ169) is a bactericidal benzothiazinone and a potent DprE1 (decaprenylphosphoryl-β-d-ribose 2′-oxidase) inhibitor. Macozinone inhibits the essential flavoprotein DprE1 by forming a covalent bond with the active-site Cys387 residue. Macozinone has antituberculosis effect.
|
-
- HY-10255AS
-
|
Sunitinib D10
SU 11248 D10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-N6964
-
-
- HY-N0197
-
-
- HY-B0172
-
-
- HY-N0419
-
-
- HY-12762
-
|
QS11
|
Others
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-15597
-
|
Salinomycin
Procoxacin
|
Bacterial
Wnt
β-catenin
Mitophagy
Autophagy
Apoptosis
Antibiotic
|
Cancer
|
|
Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
|
-
- HY-111383
-
-
- HY-12009
-
|
Pazopanib Hydrochloride
GW786034 (Hydrochloride)
|
PDGFR
VEGFR
FGFR
c-Kit
c-Fms
Autophagy
|
Cancer
|
|
Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
|
-
- HY-B1238
-
|
Pronethalol
(±)-Pronethalo
|
Adrenergic Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias and limits the cerebral arteriovenous malformation (AVMs).
|
-
- HY-10337
-
|
Brivanib
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β.
|
-
- HY-50094
-
|
Pictilisib
GDC-0941
|
PI3K
Autophagy
Apoptosis
|
Cancer
|
|
Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
|
-
- HY-B1238A
-
-
- HY-12036
-
|
GSK1059615
|
PI3K
mTOR
Apoptosis
|
Cancer
|
|
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
|
-
- HY-N0439
-
-
- HY-14393
-
|
Emodin
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
|
Cancer
|
|
Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
|
-
- HY-19744
-
|
T6167923
|
MyD88
|
Inflammation/Immunology
|
|
T6167923 is a potent and selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with an 50 of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.
|
-
- HY-111386
-
-
- HY-33353
-
-
- HY-B0925
-
-
- HY-B0467
-
-
- HY-U00293
-
-
- HY-131145
-
-
- HY-101604
-
|
Atrimustine
Bestrabucil; KM2210
|
Others
|
Cancer
|
|
Atrimustine is a conjugate of chlorambucil and β-estradiol benzoate with the antitumor activity.
|
-
- HY-U00019
-
-
- HY-135391S
-
|
Ezetimibe phenoxy glucuronide-D4
Ezetimibe glucuronide-D4; Ezetimibe β-D-glucuronide-D4
|
Others
|
Metabolic Disease
|
|
Ezetimibe phenoxy glucuronide-D4 (Ezetimibe glucuronide-D4) is the deuterium labeled Ezetimibe phenoxy glucuronide. Ezetimibe phenoxy glucuronide is the active metabolite of Ezetimibe. Antihyperlipoproteinemic activity. Ezetimibe is a potent cholesterol absorption inhibitor.
|
-
- HY-P1060A
-
-
- HY-130778
-
|
N,N'-Diacetylchitobiose
|
Others
|
Others
|
|
N,N'-Diacetylchitobiose is a dimer of β(1,4) linked N-acetyl-D glucosamine. N,N'-Diacetylchitobiose is the hydrolysate of chitin and can be used as alternative carbon source by E. coli.
|
-
- HY-B1264
-
|
Celiprolol hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Celiprolol hydrochloride is a potent, selective and orally active antagonist of β1-andrenoceptor with partial β2 agonist activity, therefore it is a selective adrenoreceptor modulator (SAM). Celiprolol hydrochloride demonstrates antihypertensive and antianginal activity.
|
-
- HY-B0982
-
-
- HY-B0449
-
|
Methacycline hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
|
Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis.
|
-
- HY-B1276
-
-
- HY-117516
-
|
SR10067
|
Others
|
Neurological Disease
|
|
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
|
-
- HY-10912
-
|
Fexaramine
|
FXR
Autophagy
|
Others
|
|
Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
|
-
- HY-B0977
-
|
Dicloxacillin Sodium hydrate
Dicloxacillin sodium salt monohydrate
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Dicloxacillin Sodium hydrate (Dicloxacillin sodium salt monohydrate) is a narrow-spectrum β-Lactam antibiotic of the penicillin class, is used to treat infections caused by susceptible Gram-positive bacteria, active against beta-lactamase-producing organisms such as Staphylococcus aureus.
|
-
- HY-107688A
-
|
UB-165 fumarate
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
|
-
- HY-P1106
-
|
K41498
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study.
|
-
- HY-114263
-
|
NXT629
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
|
-
- HY-15506
-
|
TAK-593
|
PDGFR
VEGFR
|
Cancer
|
|
TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
|
-
- HY-16759
-
|
Verubecestat
MK-8931
|
Beta-secretase
|
Neurological Disease
|
|
Verubecestat (MK-8931) is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease.
|
-
- HY-13049
-
|
Cediranib maleate
AZD-2171 maleate
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-N2319
-
|
Dihydroergocristine mesylate
DHEC mesylate
|
Amyloid-β
|
Neurological Disease
|
|
Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively.
|
-
- HY-117937
-
|
BC-1215
|
Ligand for E3 Ligase
|
Inflammation/Immunology
|
|
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
|
-
- HY-N8537
-
|
Enfumafungin
|
Fungal
|
Infection
|
|
Enfumafungin, a triterpene glycoside, is isolated from extracts derived from an endophytic species of Hormonema. Enfumafungin is an antifungal compound that is acting on the fungal cell wall, as the (1,3)-beta-D-glucan synthase inhibitor. Enfumafungin is specific for yeasts and fungi (excluding Cryptococcus) and does not inhibit the growth of Bacillus subtilis.
|
-
- HY-13521
-
|
SB-505124
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-108847
-
|
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-16018
-
|
Ilorasertib
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
RET
|
Cancer
|
|
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
|
-
- HY-13521A
-
|
SB-505124 hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-107411
-
|
Bromoenol lactone
(6E)-Bromoenol lactone
|
Phospholipase
|
Inflammation/Immunology
|
|
Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca 2+ influx.
|
-
- HY-14299
-
-
- HY-100583
-
-
- HY-14299A
-
-
- HY-19737A
-
-
- HY-100699
-
-
- HY-13588
-
-
- HY-B0076
-
-
- HY-17503B
-
-
- HY-U00386
-
-
- HY-101973
-
-
- HY-P1269
-
|
α-Conotoxin AuIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
|
-
- HY-110160
-
|
Pozanicline dihydrochloride
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
|
-
- HY-107436
-
|
LE135
|
RAR/RXR
TRP Channel
|
Cancer
Neurological Disease
|
|
LE135 is a potent RAR antagonist that binds selectively to RARα (Ki of 1.4 μM) and RARβ (Ki of 220 nM), and has a higher affinity to RARβ. LE135 is highly selective over RARγ, RXRα, RXRβ and RXRγ. LE135 is also a potent TRPV1 and TRPA1 receptors activator with EC50s of 2.5 μM and 20 μM, respectively.
|
-
- HY-10205
-
|
Cediranib
AZD2171
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-10208
-
|
Pazopanib
GW786034
|
VEGFR
c-Kit
PDGFR
Autophagy
FGFR
|
Cancer
|
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
|
-
- HY-N6679A
-
|
10,11-Dehydrocurvularin
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
|
-
- HY-20180
-
|
Pictilisib dimethanesulfonate
GDC-0941 dimethanesulfonate; GDC-0941 2 MeSO3H salt
|
PI3K
Autophagy
Apoptosis
|
Cancer
|
|
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
|
-
- HY-16782
-
|
Pexmetinib
ARRY-614
|
p38 MAPK
Autophagy
|
Cancer
|
|
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
|
-
- HY-18676
-
|
OSU-T315
|
Integrin
Autophagy
Apoptosis
|
Cancer
|
|
OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
|
-
- HY-19999A
-
|
PF-CBP1 hydrochloride
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Neurological Disease
|
|
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
|
-
- HY-16561
-
|
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-101355B
-
-
- HY-12560A
-
|
PNU-282987
|
nAChR
|
Neurological Disease
|
|
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
|
-
- HY-P1269A
-
-
- HY-B0467B
-
-
- HY-100327
-
-
- HY-17495A
-
-
- HY-101804
-
-
- HY-101721
-
-
- HY-U00283
-
-
- HY-136435
-
-
- HY-10004
-
-
- HY-113201
-
-
- HY-17498
-
|
Atenolol
(RS)-Atenolol
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Atenolol ((RS)-Atenolol) is a cardioselective β1-adrenergic receptor blocker, with a Ki of 697 nM atβ1-adrenoceptor in guine pig left ventricle membrane. Atenolol can be used for the research of hypertension and angina pectoris.
|
-
- HY-103040
-
|
Zuranolone
|
GABA Receptor
|
Neurological Disease
|
|
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
|
-
- HY-N0506
-
|
Rosarin
|
Others
|
Neurological Disease
|
|
Rosarin is a cinnamyl alcohol glycoside isolated from Rhodiola rosea. Rosarin has anti-inflammatory and neuroprotective effects. Rosarin supresses the expression of the proinflammatory factors iNOS, IL-1 β, and TNF- α in the kidney and prefrontal cortex of brain in mice .
|
-
- HY-119689
-
|
Umibecestat
CNP520
|
Beta-secretase
|
Neurological Disease
|
|
Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively.
|
-
- HY-13598A
-
|
Valecobulin hydrochloride
CKD-516 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 (HY-130233) and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.
|
-
- HY-50937
-
|
ST 2825
|
MyD88
|
Inflammation/Immunology
|
|
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
|
-
- HY-108966
-
|
Kushenol C
|
Beta-secretase
|
Inflammation/Immunology
|
|
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
|
-
- HY-101457
-
|
JZP-430
|
MAGL
|
Metabolic Disease
|
|
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-19798
-
|
PI4KIIIbeta-IN-9
|
PI4K
PI3K
|
Cancer
|
|
PI4KIIIbeta-IN-9 is a potent PI4KIIIβ inhibitor with an IC50 of 7 nM. PI4KIIIbeta-IN-9 also inhibits PI3Kδ and PI3Kγ with IC50s of 152 nM and 1046 nM, respectively.
|
-
- HY-B0006A
-
|
Carvedilol phosphate hemihydrate
BM 14190 phosphate hemihydrate
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
|
-
- HY-10330
-
|
Toceranib
SU11654; PHA 291639E
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
|
-
- HY-112700
-
|
SHIP2-IN-1
|
Phosphatase
|
Neurological Disease
|
|
SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.
|
-
- HY-B0422S
-
|
Nateglinide D5
A4166 D5; Senaglinide D5
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-10330A
-
|
Toceranib phosphate
SU11654 phosphate; PHA 291639E phosphate
|
PDGFR
VEGFR
c-Kit
|
Cancer
|
|
Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
|
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-101115
-
|
PI3K-IN-6
|
PI3K
|
Cancer
|
|
PI3K-IN-6 (compound 20a) is an oral active and highly selective phosphoinositide 3-kinase (PI3K) β/δ inhibitor, with IC50 values of 7.8 nM/5.3 nM for PI3K β/δ, respectively. PI3K-IN-6 (compound 20a) has potential top treat phosphatase and tensin homolog (PTEN) feficient tumors.
|
-
- HY-100634S
-
|
4-Hydroxypropranolol D7 hydrochloride
(±)-4-hydroxy Propranolol D7 hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
|
|
4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
|
-
- HY-N0060B
-
|
(E)-Ferulic acid
(E)-Coniferic acid
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
|
(E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
|
-
- HY-N0619A
-
|
cis-Mulberroside A
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-107661
-
|
Arundic Acid
ONO-2506; (R)-2-Propyloctanoic acid
|
Others
|
Neurological Disease
|
|
Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid has the potential for stroke and Alzheimer’s disease research.
|
-
- HY-N0651
-
|
Spinosin
|
Others
|
Neurological Disease
|
|
Spinosyn a C-glycoside flavonoid isolated from the seeds of Zizyphus jujube, with neuroprotective effects. Spinosin inhibits Aβ1-42 production and aggregation via activating Nrf2/HO-1 pathway.
|
-
- HY-131081
-
|
γ-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin.
|
-
- HY-124607
-
|
(R)-BRD3731
|
GSK-3
|
Neurological Disease
|
|
(R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively.
|
-
- HY-N3413
-
|
Kushenol X
|
Others
|
Metabolic Disease
|
|
Kushenol X, a flavonoid compound isolated from the roots of Sophora flavescens. Kushenol X is a potent β-glucuronidase and human carboxylesterase 2 (hCE2) inhibitor with IC50s of 2.07 μM and 3.05 μM, respectively.
|
-
- HY-U00287
-
|
BACE-IN-1
|
Beta-secretase
|
Neurological Disease
|
|
BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
|
-
- HY-N2625A
-
|
Harmalol hydrochloride
|
Others
|
Others
|
|
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.
|
-
- HY-14773
-
-
- HY-Y0932
-
-
- HY-B1108
-
-
- HY-129029
-
|
Bisoprolol
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.
|
-
- HY-14602
-
|
Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
|
Amyloid-β
|
Cancer
|
|
Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects.
|
-
- HY-16579
-
|
Etifoxine hydrochloride
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-P0295
-
|
Gly-Arg-Gly-Asp-Ser
|
Integrin
|
Others
|
|
Gly-Arg-Gly-Asp-Ser is a pentapeptide that forms the cell-binding domain of a glycoprotein, osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin receptors αvβ3 and αvβ5 with estimated IC50 of ∼5 and ∼6.5 μM
|
-
- HY-100689
-
|
Propyl pyrazole triol
PPT
|
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
|
-
- HY-16579A
-
|
Etifoxine
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-N4195
-
|
Resveratroloside
trans-Resveratrol 4'-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
Cardiovascular Disease
|
|
Resveratroloside is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect.
|
-
- HY-I0352
-
-
- HY-B1076
-
-
- HY-N1459
-
-
- HY-N0343
-
|
Helicid
Helicide; Helicidum; 4-Formylphenyl-β-D-allopyranoside
|
Others
|
Neurological Disease
|
|
Helicid (Helicide) is a major constituent of Helicia nilgirica Bedd. Helicid has been used to treat psychoneurosis for its sedative-hypnotic and analgesic properties.
|
-
- HY-B1172
-
|
Lactulose
4-O-β-D-Galactopyranosyl-D-fructose
|
Others
|
Others
|
|
Lactulose is a non-absortable sugar used in the treatment of constipation and hepatic encephalopathy.
|
-
- HY-13894
-
|
Tyrphostin AG1296
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
|
-
- HY-119757
-
|
Tyrphostin AG1433
SU1433; AG1433
|
PDGFR
VEGFR
|
Cancer
|
|
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
|
-
- HY-77251
-
|
TAK1/MAP4K2 inhibitor 1
|
MAP4K
MAP3K
|
Cancer
|
|
TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
|
-
- HY-B0006
-
-
- HY-17406S
-
|
Tolcapone D7
Ro 40-7592 D7
|
COMT
Amyloid-β
|
Neurological Disease
|
|
Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-108264
-
|
TCS 21311
NIBR3049
|
JAK
PKC
GSK-3
|
Cancer
|
|
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
|
-
- HY-136072
-
|
QPX7728-OH disodium
|
Bacterial
|
Infection
|
|
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
|
-
- HY-131179
-
|
Influenza A virus-IN-1
|
Influenza Virus
|
Infection
|
|
Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
|
-
- HY-128773A
-
|
MRL-494 hydrochloride
|
Bacterial
|
Infection
|
|
MRL-494 hydrochloride, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 hydrochloride can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.
|
-
- HY-P1119
-
|
WRW4
|
Others
|
Neurological Disease
|
|
WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
|
-
- HY-16361A
-
|
Omigapil maleate
CGP3466B maleate
|
Apoptosis
|
Metabolic Disease
Neurological Disease
|
|
Omigapil maleate, an orally bioavailable GAPDH nitrosylation inhibitor, abrogates 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).
|
-
- HY-117541
-
|
Glycyl-glutamine
Glycyl-L-glutamine
|
Others
|
Neurological Disease
|
|
Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems. Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln).
|
-
- HY-70063
-
|
Buparlisib
BKM120; NVP-BKM120
|
PI3K
Apoptosis
|
Cancer
|
|
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
|
-
- HY-10432A
-
|
A 83-01 sodium salt
|
TGF-β Receptor
ALK
|
Cancer
|
|
A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-13308
-
-
- HY-N0366
-
|
Sennoside B
|
PDGFR
|
Cancer
|
|
Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
|
-
- HY-10331A
-
-
- HY-N2491
-
|
Deoxyelephantopin
|
NF-κB
|
Cancer
|
|
Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
|
-
- HY-103254
-
|
ML221
|
Others
|
Neurological Disease
|
|
ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
|
-
- HY-B0381A
-
-
- HY-14533
-
-
- HY-19334
-
-
- HY-N2146
-
-
- HY-B0381
-
-
- HY-10182B
-
|
CHIR-99021 trihydrochloride
CT99021 trihydrochloride
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 trihydrochloride (CT99021 trihydrochloride) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 trihydrochloride enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 trihydrochloride induces autophagy.
|
-
- HY-108359
-
|
Alsterpaullone
9-Nitropaullone; NSC 705701
|
CDK
GSK-3
|
Cancer
|
|
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders.
|
-
- HY-10182
-
|
CHIR-99021
CT99021
|
GSK-3
Wnt
β-catenin
Autophagy
|
Cancer
|
|
CHIR-99021 (CT99021) is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. CHIR-99021 shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. CHIR-99021 is also a potent Wnt/β-catenin signaling pathway activator. CHIR-99021 enhances mouse and human embryonic stem cells self-renewal. CHIR-99021 induces autophagy.
|
-
- HY-N7676
-
|
Marein
|
AMPK
HDAC
|
Metabolic Disease
Neurological Disease
Cardiovascular Disease
|
|
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
|
-
- HY-111932
-
|
Indirubin-5-sulfonate
|
CDK
GSK-3
|
Cancer
|
|
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK) inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively. Indirubin-5-sulfonate also shows inhibitory activity against GSK-3β.
|
-
- HY-N4285
-
-
- HY-14190
-
|
Valategrast
R-411 free base
|
Integrin
|
Inflammation/Immunology
|
|
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
|
-
- HY-19624
-
|
NVP-ACC789
ACC-789; ZK202650
|
VEGFR
PDGFR
|
Cancer
|
|
NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
|
-
- HY-10331
-
|
Regorafenib
BAY 73-4506
|
VEGFR
Autophagy
PDGFR
Raf
RET
|
Cancer
|
|
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
|
-
- HY-15177
-
|
PF-04691502
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
|
-
- HY-B1803A
-
|
Tracazolate hydrochloride
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity.
|
-
- HY-113402A
-
|
Gamma-glutamylcysteine TFA
γ-Glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.
|
-
- HY-112813
-
|
TUG-1375
|
Others
|
Metabolic Disease
|
|
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
|
-
- HY-N0569
-
-
- HY-P0295A
-
-
- HY-N4327
-
|
Eurycomalactone
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
|
-
- HY-16018A
-
|
Ilorasertib hydrochloride
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
RET
VEGFR
|
Cancer
|
|
Ilorasertib (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
|
-
- HY-B0116
-
