Search Result
Results for "A strong natural sfrp1 Inhibitors" in MCE Product Catalog:
8266
Inhibitors & Agonists
14
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-10858
-
|
WAY 316606
|
sFRP-1
|
Cancer
|
|
WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM.
|
-
- HY-N0560
-
-
- HY-N0716
-
-
- HY-U00439
-
-
- HY-N7591
-
|
Millepachine
|
Apoptosis
|
Cancer
|
|
Millepachine is a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against numerous human cancer cells both in vitro and in vivo.
|
-
- HY-17577
-
-
- HY-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-N6609
-
-
- HY-133541
-
|
Glucopiericidin A
|
GLUT
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts.
|
-
- 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-N6046
-
-
- HY-N7609
-
-
- HY-15087A
-
-
- HY-136064
-
-
- HY-N0856
-
|
Alisol C 23-acetate
23-O-Acetylalisol C; Alisol C monoacetate
|
Others
|
Cardiovascular Disease
|
|
Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
|
-
- HY-N0853
-
-
- 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-N2392
-
-
- HY-P1581
-
|
Ceratotoxin A
|
Bacterial
|
Infection
|
|
Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
|
-
- HY-N0005
-
|
Curcumin
Diferuloylmethane; natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Cancer
|
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-N0237
-
-
- HY-N0873
-
|
Sagittatoside A
Icariin-A
|
Others
|
Others
|
|
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
|
-
- HY-N0476
-
-
- HY-N6862
-
|
Lucideric acid A
|
MMP
|
Cancer
|
|
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-P2322
-
|
Iturin A
|
Fungal
|
|
|
IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
|
-
- HY-N0257
-
-
- HY-N4019
-
|
Maohuoside A
|
Others
|
Metabolic Disease
|
|
Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
|
-
- HY-12458
-
|
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-N0853A
-
-
- HY-136293
-
|
Mechercharmycin A
|
Apoptosis
|
Cancer
|
|
Mechercharmycin A is a cytotoxic substance isolated from marine-derived Thermoactinomyces sp. YM3-251. Mechercharmycin A exhibits relatively strong antitumor activity.
|
-
- HY-N6930
-
-
- HY-N0123
-
|
Aloin
Aloin-A; Barbaloin-A
|
Others
|
Cancer
|
|
Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.
|
-
- HY-N2228
-
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate
(-)-EGCG-3''-O-ME
|
Others
|
Cancer
|
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate is a natural product isolated from the tea leaf, with strong antioxidative activity. (-)-Epigallocatechin-3-(3''-O-methyl) gallate has a strong cytotoxic activity for rat cancer cells.
|
-
- HY-131005
-
-
- HY-N6017
-
|
Bakkenolide A
|
Others
|
Cancer
|
|
Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
|
-
- HY-N2440
-
-
- HY-113215
-
|
Allotetrahydrocortisol
5a-Tetrahydrocortisol
|
Endogenous Metabolite
|
Others
|
|
Allotetrahydrocortisol (5a-Tetrahydrocortisol) is a metabolite of Cortisol. Cortisol is the main glucocorticoid in human. It is produced in adrenal cortex and plays a crucial role in many physiological processes.
|
-
- HY-N0204
-
|
Pulchinenoside A
Anemoside A3
|
Others
|
Others
|
|
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
|
-
- HY-N7621
-
|
Bryonamide A
|
Others
|
Others
|
|
Bryonamide A is a natural compound isolated from red algae Bostrychia radicans (Rhodomelaceae).
|
-
- HY-W040129
-
|
Chromomycin A3
|
Bacterial
Fungal
Antibiotic
|
Cancer
Infection
|
|
Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
|
-
- HY-N3417
-
|
Kongensin A
|
HSP
RIP kinase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
|
-
- HY-N1438
-
|
Hydroxygenkwanin
7-O-Methylluteolin
|
Others
|
Cancer
|
|
Hydroxygenkwanin (7-O-Methylluteolin), a natural flavonoid compound, is one of the main components of Lilac Daphne. Hydroxygenkwanin has anti-oxidant ability, anti-glioma ability and anticancer effect.
|
-
- HY-N0875
-
-
- HY-N4210
-
|
Yadanziolide A
|
Others
|
Cancer
Infection
|
|
Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC50 of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects.
|
-
- HY-N6820
-
-
- HY-N6915
-
-
- HY-N2505
-
-
- HY-N1118
-
-
- HY-111830
-
|
Lignin
Lignine
|
Others
|
Others
|
|
Lignin (Lignine) is a natural complex biopolymer with biodegradable and biocompatible. Lignin is the main component of plant cell walls and is a renewable aromatic polymer. Lignin has strongly antioxidant activity.
|
-
- HY-108421
-
|
Xinjiachalcone A
|
Bacterial
|
Infection
|
|
Xinjiachalcone A is an active principle of Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori, with MIC values ranged from 12.5 to 50 µM for seventeen H. pylori strains.
|
-
- HY-18258
-
-
- HY-108485
-
|
Damnacanthal
|
Src
Apoptosis
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.
|
-
- HY-W012653
-
|
4'-Methylacetophenone
|
Others
|
Others
|
|
4′-methylacetophenone can be used as a fragrance material. 4′-Methylacetophenone is wildly occurs in volatile compounds in food and in some natural complex substances (NCS).
|
-
- HY-N0005S
-
-
- HY-136151
-
|
UNC10217938A
|
Others
|
Others
|
|
UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
|
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- HY-N7644
-
|
Comanthoside A
|
Others
|
Others
|
|
Comanthoside A is a plant derived natural flavonoid glycoside isolated from the leaves of Comanthosphace japonica. Comanthoside A also serves as a key intermediate for the synthesis of Comanthoside B and Linaroside.
|
-
- HY-121879
-
-
- HY-N6994
-
|
Isoasatone A
|
Others
|
Infection
|
|
Isoasatone A is a natural product isolated from the plant Heterotropa takaoi M., with anti-insect activity. Isoasatone A againsts S. litura by acting on cytochrome P450 monoxygenases and glutathione transferases.
|
-
- HY-N0410
-
-
- HY-130993
-
|
Isatropolone A
|
Parasite
|
Infection
|
|
Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
|
-
- HY-N1472
-
|
Levistolide A
|
Apoptosis
|
Cancer
|
|
Levistolide A (LA), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is used for treating cancer. Levistolide A can induce apoptosis via ROS-mediated ER stress pathway.
|
-
- HY-N0855
-
|
Alisol G
Alisol-G; 25-Anhydroalisol A
|
Others
|
Others
|
|
Alisol G is a natural product extracted from Rhizoma Alismatis.
|
-
- HY-12361
-
|
PF 1022A
|
Parasite
|
Infection
|
|
PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against Ascaridia galli in chickens. PF 1022A also can be used for angiostrongyliasis research.
|
-
- HY-41404
-
|
Piperonylic acid
|
Cytochrome P450
|
Infection
|
|
Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase.
|
-
- HY-N0819
-
|
Raddeanin A
|
Apoptosis
|
Cancer
|
|
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
|
-
- HY-N3517
-
-
- HY-N3516
-
-
- HY-N0841
-
|
Bruceine A
Dihydrobrusatol; NSC310616
|
Parasite
Antibiotic
|
Infection
|
|
Bruceine A(NSC310616; Dihydrobrusatol) is a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.
|
-
- HY-N6940
-
|
Prosapogenin A
Progenin III
|
Apoptosis
|
Cancer
|
|
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
|
-
- HY-114936
-
|
Piericidin A
AR-054
|
Bacterial
ADC Cytotoxin
Antibiotic
|
Cancer
Infection
Neurological Disease
|
|
Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.
|
-
- HY-N0325
-
|
DL-Methionine
|
Parasite
|
Infection
Inflammation/Immunology
|
|
DL-Methionine is an essential amino acid containing sulfur with oxidative stress defense effects. DL-Methionine can be used for animal natural feed. DL-Methionine also kills H. rostochiensis on potato plants.
|
-
- HY-N0056
-
-
- HY-19373
-
-
- 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-112906
-
-
- HY-W015371
-
|
Ethyl phenylacetate
|
Others
|
Others
|
|
Ethyl phenylacetate is a natural flavouring ingredien, and its sensory threshold is near 73 µg/L. Ethyl phenylacetate is a “greener" solvent with low toxicity. Ethyl phenylacetate is a non-mutagenic and is a Kosher food additive. Ethyl phenylacetate gives to the wines a strong honey-like character.
|
-
- HY-N0234
-
|
Bavachinin
7-O-Methylbavachin; Bavachinin A
|
Others
|
Inflammation/Immunology
|
|
Bavachinin(7-O-Methylbavachin) is a natural compound isolated from the Chinese herb Fructus Psoraleae;has potent anti-angiogenic activity.
|
-
- HY-13821
-
|
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-15459
-
-
- HY-N0441
-
-
- HY-135235
-
|
Cysteine thiol probe
|
Others
|
Others
|
|
Cysteine Thiol Probe is a thiol-based probe designed to label electrophilic natural products. Cysteine Thiol Probe possesses each of the characteristics of an ideal pharmacophore probe, and has a chromophore. Cysteine Thiol Probe is capable of engaging enone-, β-lactam-, and β-lactone-based electrophilic metabolites.
|
-
- HY-W017212
-
|
Methyl cinnamate
Methyl 3-phenylpropenoate
|
Tyrosinase
Bacterial
AMPK
|
Infection
Metabolic Disease
|
|
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
|
-
- HY-P0244
-
-
- HY-N0501
-
|
11-oxo-mogroside V
|
Reactive Oxygen Species
|
Metabolic Disease
|
|
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2 -, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
|
-
- HY-P0244A
-
-
- HY-N6707
-
|
Triacsin C
WS 1228A; FR 900190
|
Others
|
Infection
|
|
Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity. Triacsin C is found to be highly effective against rotavirus replication.
|
-
- 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-19720A
-
-
- HY-W008385
-
-
- HY-112860
-
-
- HY-N2326
-
|
(±)-Anatoxin A fumarate
|
nAChR
|
Neurological Disease
|
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
|
-
- HY-N6574
-
-
- HY-101873S
-
-
- HY-112543
-
|
S119-8
|
Influenza Virus
|
Infection
|
|
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV).
|
-
- 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-N0149
-
-
- HY-101073
-
-
- HY-N1916
-
|
Coniferyl ferulate
|
Gutathione S-transferase
P-glycoprotein
|
Cancer
|
|
Coniferyl ferulate, a strong inhibitor of glutathione S-transferase (GST) isolated from Radix Angelicae sinensis, reverses multidrug resistance and downregulates P-glycoprotein. Coniferyl ferulate shows strong inhibition of human placental GST with an IC50 of 0.3 μM.
|
-
- 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-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-11108
-
-
- HY-B1558A
-
|
Bifemelane hydrochloride
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
|
Bifemelane hydrochloride is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM, and it also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease.
|
-
- 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-B0134
-
-
- 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-18728
-
-
- HY-N1201
-
-
- HY-B0099
-
-
- HY-12054A
-
-
- HY-12054
-
-
- HY-P1290
-
|
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-15453
-
|
Devimistat
CPI-613
|
Apoptosis
|
Cancer
|
|
Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
|
-
- HY-111380
-
-
- HY-P1290A
-
|
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-15583
-
-
- HY-N0726
-
|
Dracorhodin perchlorate
Dracohodin perochlorate
|
Apoptosis
|
Cancer
|
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate (Dracohodin perochlorate) inhibits cell proliferation, induces cell cycle arrest and apoptosis [1].
|
-
- HY-20349
-
-
- HY-N1377
-
|
Nevadensin
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive.
|
-
- HY-N0243
-
-
- HY-N0077
-
|
Ginkgolic Acid
Ginkgolic acid (15:1); Ginkgolic acid I; Romanicardic acid
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
|
-
- HY-N0693
-
-
- HY-121222
-
|
alpha-Bisabolol
|
Apoptosis
|
Cancer
|
|
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
|
-
- 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-13503
-
-
- HY-15758
-
-
- HY-N2221
-
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-100876
-
|
GGTI298
|
Ras
Apoptosis
|
Cancer
|
|
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
|
-
- HY-I0096
-
-
- HY-N7039
-
-
- HY-13271
-
|
Tubastatin A Hydrochloride
Tubastatin A HCl; TSA HCl
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-18983
-
|
Calyculin A
(-)-Calyculin A
|
Phosphatase
|
Cancer
|
|
Calyculin A is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM.
|
-
- HY-B0183
-
-
- HY-100618
-
-
- HY-121450
-
|
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-N1447
-
-
- HY-10038
-
|
A 922500
DGAT-1 Inhibitor 4a
|
Acyltransferase
|
Metabolic Disease
|
|
A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
|
-
- 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-N2522
-
-
- HY-17387
-
|
(-)-Huperzine A
Huperzine A
|
AChE
Apoptosis
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A), an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
|
-
- HY-131123
-
-
- HY-W015175
-
-
- HY-P0311
-
|
LAH4
|
Bacterial
|
Infection
|
|
LAH4 is an antimicrobial peptide that strongly interacts with phospholipid membranes, exhibiting in vitro transfection efficiency.
|
-
- HY-N0897
-
|
Corylifol A
Corylifol-A; Corylinin
|
STAT
|
Others
|
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-N0859
-
|
Schisanhenol
Schizanhenol; Gomisin-K3
|
Others
|
Cancer
|
|
Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
|
-
- HY-N2150
-
|
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-119377
-
|
UPGL00004
|
Glutaminase
|
Cancer
|
|
UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
|
-
- HY-108486
-
|
Herbimycin A
|
Bacterial
Antibiotic
|
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL. Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-N2033
-
-
- HY-B0856
-
|
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
|
Validamycin A is an aminoglycoside agricultural antibiotic. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-15681
-
-
- HY-N2065
-
|
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-135376
-
|
Atorvastatin methyl ester
|
Others
|
Metabolic Disease
|
|
Atorvastatin methyl ester (Compound 2a) is a methyl esterified derivative of Atorvastatin. Atorvastatin methyl ester inhibits the 9-cis-RA-induced Gal4 reporter activity more strongly than Atorvastatin.
|
-
- HY-N7107
-
|
Fenchyl alcohol
|
Others
|
Infection
|
|
Fenchyl alcohol is a monoterpene alcohol in the essential oils isolated from Douglas fir needles, acts as a fragrance. Fenchyl alcohol strongly inhibits the rumen microbial activity of both sheep and deer.
|
-
- HY-119683
-
|
Epoxiconazole
|
Fungal
|
Infection
|
|
Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases.
|
-
- HY-16670
-
|
Dafadine-A
|
Cytochrome P450
|
Others
|
|
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
|
-
- HY-A0210
-
-
- HY-100558
-
|
Bafilomycin A1
(-)-Bafilomycin A1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Cancer
Infection
|
|
Bafilomycin A1 ((-)-Bafilomycin A1) is a specific inhibitor of vacuolar H +-ATPase (V-ATPase) with I50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
|
-
- HY-125916
-
|
Pseurotin A
|
Others
|
Cancer
|
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity.
|
-
- HY-13254A
-
-
- HY-16929
-
|
Latrunculin A
LAT-A
|
Arp2/3 Complex
|
Others
|
|
Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
|
-
- HY-136194
-
|
TL13-22
|
ALK
|
Cancer
|
|
TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
|
-
- HY-13271A
-
|
Tubastatin A
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-N2498
-
-
- HY-124330
-
|
Tripolin A
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
|
-
- HY-N6681
-
-
- HY-50903
-
|
Rivaroxaban
BAY 59-7939
|
Factor Xa
|
Cardiovascular Disease
|
|
Rivaroxaban (BAY 59-7939) is a highly potent，selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-13812
-
-
- HY-11011
-
|
A-770041
|
Src
|
Inflammation/Immunology
|
|
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
|
-
- HY-10454
-
|
Delanzomib
CEP-18770
|
Proteasome
NF-κB
Apoptosis
|
Cancer
|
|
Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.
|
-
- HY-N0466
-
-
- HY-12468
-
-
- HY-13261
-
|
A66
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- 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-N6796
-
|
Manumycin A
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
|
Cancer
Infection
|
|
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
|
-
- HY-N0505
-
|
Rosiridin
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
|
-
- HY-129337
-
|
Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
-
- HY-N0694
-
|
Schisantherin A
Gomisin-C; Schizantherin-A; Wuweizi ester-A
|
NF-κB
|
Inflammation/Immunology
|
|
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-N6773
-
|
Cytochalasin A
|
HIV Protease
Fungal
|
Infection
|
|
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
|
-
- HY-12583
-
-
- HY-16699
-
|
Nexturastat A
|
HDAC
|
Cancer
|
|
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.
|
-
- HY-Y0262
-
-
- HY-B0178A
-
-
- HY-U00005
-
-
- HY-N2182
-
-
- HY-B0183A
-
-
- HY-N0184A
-
-
- HY-N1950
-
|
Hispidulin
Dinatin
|
Pim
|
Cancer
|
|
Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.
|
-
- HY-N0125
-
-
- HY-N1405
-
|
Cucurbitacin I
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-19376
-
|
NAMI-A
|
FAK
|
Cancer
|
|
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.
|
-
- HY-19741
-
-
- HY-N1505
-
-
- HY-N0652
-
|
2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside
|
Others
|
Others
|
|
2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonum species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.
|
-
- HY-103397
-
|
Nanaomycin A
|
DNA Methyltransferase
Parasite
|
Cancer
Infection
|
|
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
|
-
- HY-110096
-
-
- HY-126406
-
-
- HY-N0935
-
-
- HY-N0788
-
-
- HY-N0787
-
-
- HY-N0426
-
-
- HY-N0916
-
-
- HY-N0321
-
-
- HY-19725
-
-
- HY-N6584
-
-
- HY-15595A
-
|
360A iodide
360 A iodide
|
G-quadruplex
Telomerase
|
Cancer
|
|
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-N1981
-
-
- HY-13557
-
-
- HY-15595
-
|
360A
|
G-quadruplex
Telomerase
|
Cancer
|
|
360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-16014
-
|
A-385358
|
Bcl-2 Family
|
Cancer
|
|
A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
|
-
- HY-N6687
-
|
Calcimycin
A-23187; Antibiotic A-23187
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
|
Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.
|
-
- HY-18621
-
|
OTS514
|
TOPK
Apoptosis
|
Cancer
|
|
OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
|
-
- HY-N4108
-
|
Hypophyllanthin
|
P-glycoprotein
|
Cancer
Inflammation/Immunology
|
|
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
|
-
- HY-N0647
-
|
Silychristin
|
Others
|
Endocrinology
|
|
Silychristin is an abundant flavonolignan present in the fruits of Silybum marianum, with antioxidant properties. Silychristin is a potent inhibitor of the thyroid hormone transporter MCT8, and elicits a strong inhibition of T3 uptake with an IC50 of 110 nM.
|
-
- HY-76948
-
|
5-R-Rivaroxaban
|
Factor Xa
|
Cardiovascular Disease
|
|
5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-14454
-
|
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-N6793
-
|
Phomopsin A
|
Microtubule/Tubulin
|
Cancer
|
|
Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin.
|
-
- HY-A0122
-
-
- HY-10614
-
|
A-966492
|
PARP
|
Cancer
|
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
|
-
- HY-N2300
-
-
- HY-100201
-
|
A-196
|
Histone Methyltransferase
|
Cancer
|
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
|
-
- HY-N3389
-
-
- HY-107433
-
-
- HY-N7452
-
-
- HY-118773
-
|
MreB Perturbing Compound A22 hydrochloride
A22 hydrochloride
|
Bacterial
|
|
|
MreB Perturbing Compound A22 (hydrochloride) is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 (hydrochloride) blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
|
-
- HY-N4058
-
|
Helichrysetin
|
Others
|
Cancer
|
|
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
|
-
- HY-N0867
-
-
- HY-N0854
-
-
- HY-N1765
-
-
- HY-50709
-
-
- HY-107833
-
|
A40926
|
Bacterial
|
Infection
|
|
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae.
|
-
- HY-N0862
-
-
- HY-N7082
-
|
D-Arabinose
|
Others
|
Infection
|
|
D-Arabinose, a monosaccharide, shows strong growth inhibition against the Caenorhabditis elegans with an IC50 of 7.5 mM.
|
-
- HY-113957
-
|
MPI_5a
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-N6781
-
|
Ophiobolin A
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-N0754
-
|
Eupalinolide A
|
HSP
|
Inflammation/Immunology
|
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-N6702
-
-
- HY-N1549
-
-
- HY-B0825A
-
|
Fenpyroximate
|
Parasite
|
Infection
|
|
Fenpyroximate is an acaricide and insecticide against many mites and insect pests of agricultural crops and ornamentals. Fenpyroximate is also a strong inhibitor of bovine heart mitochondrial NADH-ubiquinone oxidoreductase (complex I), binds to the ND5 subunit.
|
-
- HY-14682
-
|
GSK319347A
|
IKK
|
Inflammation/Immunology
|
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- HY-110195
-
|
Smurf1-IN-A01
A01
|
Others
|
Others
|
|
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
|
-
- HY-136195
-
|
TL13-110
|
ALK
|
Cancer
|
|
TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
|
-
- HY-13020
-
-
- HY-101835
-
-
- HY-17388
-
|
(±)-Huperzine A
|
AChE
|
Neurological Disease
|
|
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
|
-
- HY-N4185
-
-
- HY-10425
-
|
A-443654
|
Akt
|
Cancer
|
|
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
|
-
- HY-100599
-
-
- HY-N0365
-
|
Sennoside A
|
HIV
|
Infection
|
|
Sennoside A is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication.
|
-
- HY-15568A
-
-
- HY-15568
-
-
- HY-104064
-
-
- HY-105755
-
|
Antimycin A3
|
Mitochondrial Metabolism
|
Cancer
Infection
|
|
Antimycin A3, an antibiotic isolated from a number of Streptomyces species, shows antifungal activities. Antimycin A3 is a potent inhibitor of respiration. Antimycin A3 inhibits the electron transfer activity of ubiquinol-cytochrome c oxidoreductase. Antimycin A3 inhibits ATP-citrate lyase with a Ki value of 60.1 µM.
|
-
- HY-N4096
-
|
Tsugaric acid A
|
Others
|
Inflammation/Immunology
|
|
Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
|
-
- HY-N3925
-
-
- HY-114305
-
|
A1874
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-N2575
-
|
Hypocrellin A
|
PKC
|
Cancer
Infection
|
|
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).
|
-
- HY-101945
-
|
A-69412
|
Lipoxygenase
|
Inflammation/Immunology
|
|
A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
|
-
- HY-14644A
-
|
Apilimod mesylate
STA 5326 mesylate
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-14644
-
|
Apilimod
STA 5326
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
|
|
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-B1948
-
|
Diniconazole
Rac-diniconazole
|
Bacterial
|
Infection
|
|
Diniconazole is a newly developed fungicide strongly inhibited lanosterol 14 alpha-demethylation catalyzed by a yeast cytochrome P-450.
|
-
- HY-15097
-
-
- HY-N0100
-
-
- HY-N7207
-
-
- HY-N0611
-
-
- HY-N0941
-
-
- HY-N0866
-
-
- HY-N0457
-
-
- HY-B1856
-
|
Haloxyfop
|
Others
|
Metabolic Disease
|
|
Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea.
|
-
- HY-15405
-
|
Teriflunomide
A77 1726
|
Others
|
Inflammation/Immunology
|
|
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
|
-
- HY-11000
-
-
- HY-N5012
-
|
Eurycomanone
Pasakbumin A
|
Others
|
Endocrinology
|
|
Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
|
-
- 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-P1687
-
|
Siomycin A
|
Bacterial
Apoptosis
|
Cancer
|
|
Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
|
-
- HY-N2344
-
|
Procyanidin A1
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-19356
-
|
Rocaglamide
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-107406
-
|
Antimycin A1
|
Mitochondrial Metabolism
|
Cancer
|
|
Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
|
-
- HY-12507
-
-
- HY-107455
-
-
- HY-N6744
-
|
Chaetoglobosin A
|
Apoptosis
|
Cancer
Infection
|
|
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
|
-
- HY-101512
-
|
A-395
|
Histone Methyltransferase
|
Cancer
|
|
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
|
-
- HY-N6936
-
|
Sennidin A
|
HCV
Akt
GLUT
|
Infection
|
|
Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
|
-
- 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-112316
-
|
BAY1238097
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-50880
-
-
- HY-N6073
-
|
Soyasapogenol A
|
Others
|
Inflammation/Immunology
|
|
Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
|
-
- HY-N0168
-
-
- HY-N1369
-
|
Menthol
|
Others
|
Neurological Disease
|
|
Menthol is a natural analgesic compound. Menthol could cause a feeling of coolness due to stimulation of ‘cold’ receptors by inhibiting Ca ++ currents of neuronal membranes.
|
-
- HY-N0174
-
|
Cryptotanshinone
Cryptotanshinon; Tanshinone c
|
STAT
Autophagy
|
Cancer
|
|
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
|
-
- HY-N0054
-
-
- HY-N3033
-
-
- HY-18990
-
|
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-135780
-
-
- HY-117832
-
-
- HY-N7619
-
|
Xanthopurpurin
Purpuroxanthin
|
Others
|
Metabolic Disease
|
|
Xanthopurpurin, an anthraquinone glycoside, isolated from the roots of Rubia akane, shows mainly strong inhibition of collagen-induced platelet aggregation.
|
-
- HY-125098
-
-
- HY-N4287
-
|
Nordalbergin
|
Others
|
Cancer
|
|
Nordalbergin, a coumarin isolated from the wood bark of Dalbergia sissoo. Nordalbergin shows strong activity in the induction of differentiation of HL-60.
|
-
- HY-N4277
-
|
Methyl protogracillin
NSC-698793
|
Others
|
Cancer
|
|
Methyl protogracillin (NSC-698793), isolated from the roots of Dioscorea opposite Thunb, exhibits strong anti-cancer activity.
|
-
- HY-135378
-
-
- HY-100226
-
|
A-205804
|
Integrin
|
Inflammation/Immunology
|
|
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
|
-
- HY-N6795
-
|
Leptomycin A
|
CRM1
HIV
|
Infection
|
|
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
|
-
- HY-100540
-
|
Golgicide A
|
Enterovirus
|
Cancer
Infection
|
|
Golgicide A is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF), GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
|
-
- HY-100580
-
|
Asaraldehyde
Asaronaldehyde; Asaraldehyde; 2,4,5-trimethoxy-Benzaldehyde
|
COX
|
Inflammation/Immunology
|
|
Asarylaldehyde is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.
|
-
- HY-N1483
-
|
Guanfu base A
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-N0881
-
-
- HY-W012185
-
-
- HY-N1484
-
-
- HY-N0561
-
-
- HY-N0433
-
-
- HY-15764A
-
|
A 419259 trihydrochloride
RK 20449 trihydrochloride
|
Src
|
Cancer
|
|
A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
|
-
- HY-P0018
-
|
Pepstatin
Pepstatin A
|
Proteasome
HIV Protease
Autophagy
|
Infection
Cancer
|
|
Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-136532
-
|
ZT-1a
|
Others
|
Neurological Disease
|
|
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.
|
-
- HY-P0018A
-
|
Pepstatin Trifluoroacetate
Pepstatin A Trifluoroacetate
|
Proteasome
HIV Protease
|
Infection
|
|
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-N2112
-
|
Glaucocalyxin A
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
|
-
- HY-103706
-
|
ROC-325
|
Autophagy
Apoptosis
|
Cancer
|
|
ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
|
-
- HY-12406
-
|
VLX600
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
|
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity.
|
-
- HY-111458
-
-
- HY-100368A
-
-
- HY-100522
-
|
FMK 9a
|
Autophagy
|
Cancer
|
|
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
|
-
- HY-N2638
-
|
Ilexsaponin A
|
Others
|
Cardiovascular Disease
|
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes.
|
-
- HY-N2306A
-
|
Aclacinomycin A hydrochloride
Aclarubicin hydrochloride
|
Proteasome
Topoisomerase
|
Cancer
|
|
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
|
-
- HY-14164
-
-
- HY-N7043
-
|
Isosilybin A
|
Apoptosis
|
Cancer
|
|
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
|
-
- HY-N2298
-
|
Camellianin A
|
Apoptosis
|
Cancer
|
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-101143
-
-
- HY-18009
-
|
LFM-A13
|
Btk
Polo-like Kinase (PLK)
JAK
|
Cancer
|
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
|
-
- HY-N4317
-
|
Ethoxysanguinarine
|
Apoptosis
|
Cancer
|
|
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine inhibits viability and induces apoptosis of colorectal cancer cells by inhibiting protein phosphatase 2A (CIP2A).
|
-
- HY-N5017
-
|
Isochondrodendrine
Isochondrodendrin
|
Parasite
|
Infection
|
|
Isochondrodendrine ( Isochondrodendrin) is a class of bisbenzylisoquinoline alkaloid isolated from Isolona ghesquiereina. Isochondodendrine has strong antiplasmodial activity against Plasmodium falciparum.
|
-
- HY-136384
-
|
Diethofencarb
|
Fungal
|
Infection
|
|
Diethofencarb is a fungicide with strong activity against Botrytis cinerea and Benzimidazole-resistant strains of Botryis spp. Diethofencarb has a role as an antifungal agrochemical.
|
-
- HY-W009177
-
|
S-Methylglutathione
|
Others
|
Others
|
|
S-Methylglutathione is an S-substitued glutathione and a stronger nucleophile than GSH. S-Methylglutathione has inhibitory effect on glyoxalase 1.
|
-
- HY-N1923
-
-
- HY-15144
-
|
Trichostatin A
TSA
|
HDAC
|
Cancer
|
|
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
|
-
- HY-N5025
-
|
Bullatine A
|
P2X Receptor
|
Cancer
Inflammation/Immunology
|
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
|
-
- HY-100681
-
-
- HY-14164A
-
-
- HY-N2204
-
|
Swertiajaponin
|
Tyrosinase
|
Inflammation/Immunology
|
|
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
|
-
- HY-111756
-
|
BLM-IN-1
|
Apoptosis
|
Cancer
|
|
BLM-IN-1 (compound 29) is an effective Bloom syndrome protein (BLM) inhibitor, with a strong BLM binding KD of 1.81 μM and an IC50 of 0.95 μM for BLM. Induces DNA damage response, as well as apoptosis and proliferation arrest in cancer cells.
|
-
- HY-N0696
-
|
Sipeimine
Imperialine
|
Others
|
Others
|
|
Sipeimine is a natural product isolated from Fritillaria ussuriensis.
|
-
- HY-113268
-
-
- HY-N4101
-
-
- HY-B1000A
-
-
- HY-133642
-
-
- HY-N2476
-
-
- HY-N0843
-
-
- HY-N4234
-
-
- HY-N0432
-
|
Astragaloside I
Astrasieversianin IV; Cyclosieversioside B
|
Others
|
Others
|
|
Astragaloside I is a natural product isolated from Astragalus.
|
-
- HY-N0772
-
-
- HY-N0434
-
-
- HY-N1387
-
-
- HY-128553
-
-
- HY-N6860
-
|
Lucidenic acid C
|
MMP
|
Cancer
|
|
Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-100611
-
-
- HY-N6709
-
|
Zeranol
α-Zearalanol
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
|
-
- HY-18102
-
|
GLPG0492
|
Androgen Receptor
|
Others
|
|
GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.
|
-
- HY-101445A
-
|
(R)-Trolox
|
Tyrosinase
|
Cancer
|
|
(R)-Trolox is a water soluble vitamin E analogue and a competitive tyrosinase inhibitor with a Ki value of 0.83 mM and a ID50 value of 1.88 mM. The (R)-Trolox has stronger tyrosinase affinity than the (S) enantiomer (Ki value of 0.61 mM).
|
-
- HY-14347
-
|
EBE-A22
|
Others
|
Cancer
|
|
EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
|
-
- HY-N2959
-
|
Brevilin A
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
|
-
- HY-112373
-
|
Aurora Kinase Inhibitor 3
|
Aurora Kinase
|
Others
|
|
Aurora Kinase Inhibitor 3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50>10 μM. Aurora Kinase Inhibitor 3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket, and several induced structural changes in the active-site compared with other published AIK structures.
|
-
- HY-10029
-
|
Nutlin-3a
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
|
-
- 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-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-15613
-
|
Maritoclax
Marinopyrrole A
|
Bcl-2 Family
|
Cancer
|
|
Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
|
-
- HY-B0579
-
-
- HY-13746B
-
-
- HY-N6903
-
-
- HY-113440
-
-
- HY-N0668
-
|
Rubusoside
|
Others
|
Others
|
|
Rubusoside is a natural sweetener and a solubilizing agent with antiangiogenic and antiallergic properties.
|
-
- HY-N6817
-
-
- HY-N0213
-
-
- HY-Y0585
-
-
- HY-N4325
-
-
- HY-N2469
-
-
- HY-100528
-
|
Nanchangmycin
Nanchangmycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Nanchangmycin, a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
|
-
- HY-N0144
-
-
- HY-N0168A
-
-
- HY-13595
-
|
Chrysophanol
Chrysophanic acid
|
EGFR
|
Cancer
|
|
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
|
-
- HY-N6985
-
|
Baccatin III
|
Others
|
Cancer
|
|
Baccatin III is a natural product isolated from Pacific yew tree and related species. Baccatin III reduces tumor progression by inhibiting the accumulation and suppressive function of MDSCs.
|
-
- HY-N3513
-
|
Mulberrin
Kuwanon C
|
Others
|
Cardiovascular Disease
|
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-13237
-
-
- HY-100183
-
-
- HY-10794
-
-
- HY-30152
-
-
- HY-14247
-
-
- HY-17474A
-
-
- HY-100118
-
-
- HY-135809
-
|
A2764 dihydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
|
-
- HY-108254
-
|
Bisindolylmaleimide IV
Arcyriarubin A
|
PKC
CMV
|
Infection
|
|
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
|
-
- HY-112468
-
|
PNU112455A hydrochloride
|
CDK
|
Cancer
|
|
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
|
-
- HY-12521
-
|
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
|
GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
|
-
- HY-18303
-
|
AMG-47a
|
Src
|
Inflammation/Immunology
|
|
AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
|
-
- HY-18061
-
|
Ochromycinone
(Rac)-STA-21
|
STAT
Bacterial
|
Cancer
Infection
|
|
Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
|
-
- HY-N6601
-
|
Pomolic acid
Randialic acid A
|
Apoptosis
|
Cancer
|
|
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
|
-
- HY-106080A
-
|
Furegrelate sodium
U-63557A
|
Others
|
Cardiovascular Disease
|
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
|
-
- HY-19794
-
|
MP-A08
|
SPHK
|
Cancer
|
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
|
-
- HY-N1455
-
|
Falcarinol
Panaxynol; Carotatoxin
|
HSP
|
Cancer
|
|
Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.
|
-
- HY-B1202A
-
-
- HY-13339
-
-
- HY-B0093A
-
-
- HY-A0150
-
|
Alclometasone
7a-Chloro-16a-methyl prednisolone
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
|
-
- HY-100228A
-
-
- HY-N6020
-
|
(-)-Butin
|
Others
|
Inflammation/Immunology
|
|
(-)-Butin is the S enantiomer of Butin. Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities.
|
-
- HY-Y0366
-
-
- HY-126804
-
|
Safracin B
|
Antibiotic
|
Cancer
Infection
|
|
Safracin B, a tetrahydroisoquinoline (THIQ) alkaloid, is a naturally occurring antibiotic from Pseudomonas fluorescens. Safracin B exhibits broad spectrum antimicrobial and strong antitumor activities.
|
-
- HY-B1918
-
|
(+)-Bornyl acetate
|
Others
|
Others
|
|
(+)-Bornyl acetate is found in pichtae essential oil (Siberian fir needle oil). (+)-Bornyl acetate has a stronger inhibitory effect on root growth of Arabidopsis seedlings.
|
-
- HY-N0046
-
-
- HY-N0167
-
-
- HY-N0597
-
|
Panaxatriol
|
Others
|
Others
|
|
Panaxatriol is a natural product that can relieve myelosuppression induced by radiation injury.
|
-
- HY-N3524
-
-
- HY-113293A
-
-
- HY-N7704
-
-
- HY-N0156
-
-
- HY-N1366
-
|
Herniarin
7-Methoxycoumarin; Methyl umbelliferyl ether
|
Others
|
Cancer
|
|
Herniarin is a natural coumarin occurs in some flowering plants, with antitumor effect.
|
-
- HY-N0796
-
-
- HY-N0879
-
-
- HY-N5027
-
|
Oxyberberin
Berlambine; 8-Oxoberberine; Ketoberberine
|
Others
|
Infection
|
|
Berlambine is a natural alkaloid isolated from many plants.
|
-
- HY-N1958
-
-
- HY-N7257A
-
-
- HY-N2285
-
-
- HY-N7257
-
-
- HY-N0210
-
-
- HY-N6959
-
-
- HY-N6907
-
-
- HY-N6859
-
-
- HY-N0936
-
|
Coixol
6-Methoxy-2-benzoxazolinone; 6-MBOA
|
Others
|
Others
|
|
Coixol is a natural product extracted from Coix Lachryma-Jobi var.
|
-
- HY-N7037
-
-
- HY-N0900
-
-
- 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[1] [2] .
|
-
- HY-120994B
-
|
Sp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
|
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.
|
-
- HY-120994A
-
|
Rp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
|
-
- HY-120994
-
-
- HY-N6687B
-
|
Calcimycin hemimagnesium
A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium
|
Bacterial
Fungal
Apoptosis
Autophagy
|
Cancer
Infection
|
|
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces apoptosis.
|
-
- HY-N6687A
-
|
Calcimycin hemicalcium salt
A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
|
Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces apoptosis.
|
-
- HY-N0814
-
|
Phytic acid
Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-U00235
-
|
SR121566A
|
Integrin
|
Inflammation/Immunology
|
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-N0931
-
|
Santacruzamate A
CAY-10683
|
HDAC
|
Cancer
|
|
Santacruzamate A (CAY-10683) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM.
|
-
- HY-100790
-
|
Ciliobrevin A
HPI-4
|
Hedgehog
|
Cancer
|
|
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
|
-
- HY-117474
-
|
MJN110
|
MAGL
|
Neurological Disease
|
|
MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC50s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively. MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity.
|
-
- HY-112052
-
|
Aminomalonic acid
|
Endogenous Metabolite
|
Cancer
|
|
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis.
|
-
- HY-119917
-
|
Gossypetin
|
p38 MAPK
Bacterial
|
Cancer
Infection
|
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities.
|
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-N0737
-
-
- 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-P1184
-
-
- HY-N7203
-
-
- HY-N6976
-
|
Ascr#8
|
Others
|
Infection
|
|
Ascr#8 is an dauer-inducing ascaroside isolated from Caenorhabditis elegans, synergizes with ascr#2 and ascr#3, and strongly enhances male attraction.
|
-
- HY-119931
-
-
- HY-15790
-
|
Elobixibat
A 3309; AZD 7806
|
Others
|
Metabolic Disease
|
|
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
|
-
- HY-131182
-
|
DS-1971a
|
Sodium Channel
|
Neurological Disease
|
|
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
|
-
- HY-N4296
-
-
- HY-N0442
-
-
- HY-N0212
-
|
Peimine
Verticine; Dihydroisoimperialine
|
Others
|
Inflammation/Immunology
|
|
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.
|
-
- HY-N0519
-
|
Calycosin
Cyclosin
|
Apoptosis
|
Cancer
|
|
Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.
|
-
- HY-N6912
-
-
- HY-N2186
-
-
- HY-N2161
-
-
- HY-N1155
-
-
- HY-N0852
-
-
- HY-N7522
-
-
- HY-N2559
-
-
- HY-N2089
-
-
- HY-N0871
-
-
- HY-N0260
-
-
- HY-N7250
-
-
- HY-N0868
-
-
- HY-N1234
-
-
- HY-100431A
-
|
IMR-1A
|
Notch
Drug Metabolite
|
Cancer
|
|
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
|
-
- HY-B0220E
-
|
Erythromycin A dihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-18299A
-
|
Purvalanol A
NG-60
|
CDK
Autophagy
Apoptosis
|
Cancer
|
|
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
|
-
- HY-B0597
-
-
- HY-N0814A
-
|
Phytic acid dodecasodium salt hydrate
Inositol hexaphosphate dodecasodium salt hydrate; myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-N7613
-
-
- HY-N0139
-
-
- HY-10432
-
|
A 83-01
|
ALK
TGF-β Receptor
|
Cancer
|
|
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-16576
-
|
TCS-PIM-1-4a
SMI-4a
|
Pim
Apoptosis
|
Cancer
|
|
TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
|
-
- HY-108472
-
-
- HY-N2553
-
|
4-Deoxypyridoxine 5'-phosphate
|
LPL Receptor
|
Metabolic Disease
|
|
4-Deoxypyridoxine 5'-phosphate is a Pyridoxal 5'-phosphate analogue and a sphingosine 1-phosphate (S1P) inhibitor. 4-Deoxypyridoxine 5'-phosphate inhibits ornithine decarboxylase activity with a Ki of 60 μM. 4-Deoxypyridoxine 5'-phosphate is a competitive inhibitor of the activation of glutamate apodecarboxylase by Pyridoxal 5'-phosphate (Ki of 0.27 μM) and strongly inhibits glutamate-dependent labeling of glutamate decarboxylase.
|
-
- HY-12843
-
|
Bohemine
|
CDK
ERK
|
Cancer
|
|
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
|
-
- HY-105634
-
|
Nomegestrol
|
Progesterone Receptor
|
Endocrinology
|
|
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity.
|
-
- HY-N6704
-
|
Enniatin A1
|
ERK
Apoptosis
|
Cancer
|
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
|
-
- HY-109592
-
-
- HY-14929A
-
|
Migalastat hydrochloride
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-14595
-
|
Biochanin A
4-Methylgenistein; Olmelin
|
FAAH
Autophagy
|
Neurological Disease
Cancer
|
|
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
|
-
- HY-130613
-
|
MAC-545496
|
Bacterial
|
Infection
|
|
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA).
|
-
- HY-N4286
-
|
4-Methyldaphnetin
|
Apoptosis
|
Cancer
|
|
4-Methyldaphnetin is a precursor in the synthesis of derivatives of 4-methyl coumarin. 4-Methyldaphnetin has potent, selective anti-proliferative and apoptosis-inducing effects on several cancer cell lines. 4-Methyldaphnetin possesses radical scavenging property and strongly inhibits membrane lipid peroxidation.
|
-
- HY-128553A
-
|
(Rac)-Antineoplaston A10
|
Ras
Apoptosis
|
Cancer
|
|
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
|
-
- HY-13954
-
|
A 839977
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
|
-
- HY-N3557
-
|
Cauloside A
Leontoside A
|
Fungal
|
Infection
|
|
Cauloside A (Leontoside A) is a saponin isolated from Dipsacus asper roots. Cauloside A has potent antifungal activity.
|
-
- HY-N2252
-
-
- HY-N0372
-
|
Licochalcone A
Licochalcone-A
|
Autophagy
|
Cancer
|
|
Licochalcone A, a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, presents obvious anti-cancer effects.
|
-
- HY-P0216
-
-
- HY-15488
-
-
- HY-N1924
-
|
Crassicauline A
Crassicaulin A
|
Others
|
Neurological Disease
|
|
Crassicauline A (Crassicaulin A) is a bioactive alkaloid found in roots of Aconitum carmichaeli. Crassicauline A (Crassicaulin A) possesses feeding deterrent activity against T. castaneum adults with an EC50 of 1134.5 ppm.
|
-
- HY-107633
-
|
A 1120
|
Others
|
Metabolic Disease
|
|
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.
|
-
- HY-15488A
-
-
- HY-N1599
-
-
- HY-N2286
-
-
- HY-N3637
-
-
- 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-N2212
-
-
- HY-B1000
-
-
- HY-13930
-
|
Miquelianin
Quercetin 3-O-glucuronide; Quercetin 3-glucuronide
|
Endogenous Metabolite
|
Cancer
|
|
Miquelianin (Quercetin 3-O-glucuronide) is a metabolite of quercetin and a type of natural flavonoid.
|
-
- HY-N0695
-
-
- HY-N2200
-
-
- HY-N0748
-
-
- HY-N0744
-
-
- HY-W016289
-
|
Antiarol
3,4,5-Trimethoxyphenol
|
Others
|
Others
|
|
Antiarol (3,4,5-Trimethoxyphenol) is a natural compound isolated from Salmaliamalabaricum.
|
-
- HY-N0903
-
|
Dihydrochelerythrine
12,13-Dihydrochelerythrine
|
Fungal
|
Infection
|
|
Dihydrochelerythrine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal activity.
|
-
- HY-N6874
-
-
- HY-N4167
-
|
3-O-Methylgalangin
Galangin 3-methyl ether; 3-Methylgalangin
|
Others
|
Infection
|
|
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase.
|
-
- HY-P0219
-
|
Microcystin-LA
|
Phosphatase
|
Cancer
|
|
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
|
-
- HY-N4288
-
-
- HY-16677A
-
-
- HY-N0134
-
-
- HY-15858A
-
|
AP-III-a4 hydrochloride
ENOblock hydrochloride
|
Enolase
|
Cancer
|
|
AP-III-a4 hydrochloride (ENOblock hydrochloride) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
|
-
- HY-N3006
-
|
Sakuranetin
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Sakuranetin is a rice flavonoid phytoalexin, shows strong antifungal activity. Sakuranetin has anti-inflammatory and antioxidative activities. Sakuranetin ameliorates LPS-induced acute lung injury.
|
-
- HY-N6705
-
|
Tropodithietic acid
|
Bacterial
|
Infection
|
|
Tropodithietic acid is a sulfur-containing antibiotic produced by the marine bacterium Phaeobacter inhibens. Tropodithietic acid exhibits a strong antibiotic activity against a broad spectrum of bacteria including alpha- and gammaproteobacteria, flavobacteria and actinobacteria.
|
-
- HY-114170
-
|
ML604440
|
Proteasome
|
Inflammation/Immunology
|
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-P1076
-
|
CALP2
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
|
-
- HY-N2278
-
|
Kushenol A
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
|
-
- HY-10524
-
|
GSK1904529A
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
|
-
- HY-106101
-
|
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- HY-W002585
-
|
O6-Benzylguanine
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
|
-
- HY-N4202
-
-
- HY-N0573
-
-
- HY-N0007
-
|
Bisdemethoxycurcumin
Curcumin III; Didemethoxycurcumin
|
Apoptosis
Autophagy
|
Cancer
|
|
Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
|
-
- HY-131108
-
-
- HY-15733
-
|
Lucidin
NSC 30546
|
Others
|
Cancer
|
|
Lucidin (NSC 30546) is a natural component of Rubia tinctorum L. lucidin is mutagenic in bacteria and mammalian cells.
|
-
- HY-N1944
-
-
- HY-N0669
-
|
Stevioside
|
Others
|
Cancer
|
|
Stevioside is a natural sweetener extracted from leaves of Stevia rebaudiana, with anticancer activity.
|
-
- HY-N4279
-
|
Gentisin
|
Others
|
Others
|
|
Gentisin is a natural compound isolated from Gentianae radix (Gentianaceae) with mutagenic activities.
|
-
- HY-128387
-
-
- HY-N2446
-
|
Kakuol
|
Fungal
|
Infection
|
|
Kakuol is a natural compound isolated from the rhizomes of Asarum sieboldii. Antifungal activity.
|
-
- HY-N0902
-
|
Dihydrosanguinarine
13,14-Dihydrosanguinarine
|
Others
|
Infection
|
|
Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.
|
-
- HY-N7631
-
|
Combretol
|
Others
|
Others
|
|
Combretol is a natural compound isolated from the roots and leaves of the plant Cassipourea madagascariensis.
|
-
- HY-N0467
-
-
- HY-N1276
-
-
- HY-N0874
-
-
- HY-111174
-
-
- HY-B0958
-
|
Mupirocin
BRL-4910A; Pseudomonic acid
|
Bacterial
Antibiotic
|
Infection
|
|
Mupirocin (BRL-4910A) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin (BRL-4910A) apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
|
-
- HY-14137
-
-
- HY-122534
-
|
Mensacarcin
|
Mitochondrial Metabolism
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-B1816
-
-
- HY-112316A
-
|
(R)-BAY1238097
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
|
-
- HY-N0047
-
|
Polyphyllin I
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
|
-
- HY-111388A
-
|
SEL120-34A monohydrochloride
|
CDK
|
Cancer
|
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
|
-
- HY-135797A
-
|
DB1976 dihydrochloride
|
Apoptosis
|
Cancer
|
|
DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect.
|
-
- HY-12459
-
|
Pyrindamycin B
|
Bacterial
|
Infection
|
|
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice.
|
-
- HY-136295
-
-
- HY-N6783
-
|
Oligomycin C
|
Fungal
Antibiotic
|
Infection
|
|
Oligomycin C is a macrolide antibiotic produced by Streptomyces strains. Oligomycin C exhibits a strong activity against Aspergillus niger, Alternaria alternata, Botrytis cinerea and Phytophthora capsici but no activity toward bacteria.
|
-
- HY-103128
-
-
- HY-P0018B
-
|
Pepstatin Ammonium
Pepstatin A Ammonium
|
Proteasome
HIV Protease
|
Cancer
Infection
|
|
Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-100612
-
|
T16Ainh-A01
|
Chloride Channel
|
Others
|
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-129065
-
|
Nourseothricin sulfate
Streptothricin sulfate
|
Fungal
Bacterial
Antibiotic
|
Infection
|
|
Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells.
|
-
- HY-N2132
-
|
Flavokawain B
Flavokavain B
|
Apoptosis
|
Cancer
|
|
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations.
|
-
- HY-N1127
-
|
Tricin
|
CMV
|
Cancer
Infection
|
|
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
|
-
- HY-N7394A
-
|
(-)-Zuonin A
D-Epigalbacin
|
JNK
|
Cancer
|
|
(-)-Zuonin A (D-Epigalbacin), a naturally occurring lignin, is a potent, selective JNKs inhibitor, with IC50s of 1.7 μM, 2.9 μM and 1.74 μM for JNK1, JNK2 and JNK3, respectively.
|
-
- HY-80012
-
|
SJB3-019A
|
Deubiquitinase
|
Cancer
|
|
SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
|
-
- HY-N2110
-
|
Phellopterin
|
Others
|
Inflammation/Immunology
|
|
Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
|
-
- HY-112205A
-
|
RR-11a analog
|
Parasite
|
Infection
|
|
RR-11a analog is a potent and selective inhibitors of asparaginyl endopeptidases (AE) (Legumain), with IC50 values of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.
|
-
- HY-N0182
-
-
- HY-N4324
-
-
- HY-N1428
-
-
- HY-N0870
-
-
- HY-N6889
-
-
- HY-N0662
-
-
- HY-N4123
-
-
- HY-N4319
-
-
- HY-N7662
-
-
- HY-N0078
-
|
Ginkgolic Acid C13:0
Ginkgolic acid (13:0); Ginkgoneolic Acid; 6-Tridecylsalicylic acid
|
Others
|
Infection
|
|
Ginkgolic Acid (C13:0) is a natural anticariogenic agent in that it exhibits antimicrobial activity against S.
|
-
- HY-50877
-
-
- HY-N4142
-
-
- HY-N2380
-
-
- HY-112569
-
-
- HY-111388B
-
|
SEL120-34A HCl
|
CDK
|
Cancer
|
|
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-18963
-
|
Lavendustin A
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
|
-
- HY-13235
-
-
- HY-N0592
-
|
Demethyleneberberine
|
NF-κB
AMPK
|
Metabolic Disease
Inflammation/Immunology
|
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
|
-
- HY-107390A
-
|
AX-024 hydrochloride
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-107390
-
|
AX-024
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-122909
-
-
- HY-13470
-
-
- HY-U00387
-
-
- 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-13036
-
|
(Rac)-IBT6A
|
Btk
|
Cancer
|
|
(Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-107018
-
|
AR-A 2
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- HY-117391
-
-
- HY-N0636
-
|
Eriocitrin
|
Apoptosis
|
Cancer
|
|
Eriocitrin is a flavonoid isolated from lemon, which is a strong antioxidant agent. Eriocitrin could inhibit the proliferation of hepatocellular carcinoma cell lines by arresting cell cycle in S phase through up-regulation of p53, cyclin A, cyclin D3 and CDK6. Eriocitrin triggers apoptosis by activating mitochondria-involved intrinsic signaling pathway.
|
-
- HY-103586
-
|
GS-441524
|
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM.
|
-
- HY-W016586
-
|
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ−glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N0737A
-
|
Harmine
Telepathine
|
DYRK
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
|
-
- HY-N2995
-
|
Poricoic acid A
Poricoic acid A(F)
|
Others
|
Cancer
|
|
Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
|
-
- HY-78727
-
-
- HY-P1076A
-
|
CALP2 TFA
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
|
-
- HY-W018025
-
-
- HY-19828
-
|
Herboxidiene
GEX1A
|
DNA/RNA Synthesis
|
Cancer
|
|
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
|
-
- HY-P1184A
-
-
- HY-W008350
-
-
- HY-116284
-
-
- HY-W001963
-
-
- HY-N0860
-
-
- HY-N0571
-
-
- HY-N0537
-
|
Xylose
D-(+)-Xylose; (+)-Xylose; Wood sugar
|
Endogenous Metabolite
|
Others
|
|
Xylose, a natural product, can be catalyzed into xylulose by xylose isomerase, and it is the key step for anaerobic ethanolic fermentation of xylose.
|
-
- HY-N1899
-
-
- HY-N6260
-
-
- HY-W012980
-
-
- HY-N0887
-
-
- HY-17583
-
-
- HY-N0658
-
-
- HY-N2176
-
-
- HY-13863
-
|
Hydroxy-Dynasore
Dyngo-4a
|
Dynamin
|
Neurological Disease
|
|
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
|
-
- HY-12143
-
-
- HY-129997
-
|
Luteolinidin chloride
|
Others
|
Inflammation/Immunology
|
|
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
|
-
- HY-N0836
-
|
Jervine
11-Ketocyclopamine
|
Hedgehog
Smo
|
Cancer
Inflammation/Immunology
|
|
Jervine (11-Ketocyclopamine) is a potent Hedgehog (Hh) inhibitor with an IC50 of 500-700 nM. Jervine is a natural teratogenic sterodial alkaloid from rhizomes of Veratrum album. Jervine has anti-inflammatory and antioxidant properties.
|
-
- HY-12686
-
-
- HY-10442
-
-
- HY-13646A
-
-
- HY-13646
-
-
- HY-15403
-
-
- HY-N0691
-
|
Schisandrin
Schizandrol; Schizandrol-A; Wuweizi alcohol-A; Wuweizichun-A
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Schisandrin has various therapeutic effects on a range of medical conditions such as anti-asthmatic, anti-cancer, and anti-inflammatory effects.
|
-
- HY-15403A
-
-
- HY-B0389A
-
|
D-Glucose-13C6
Glucose-13C6
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Glucose-13C6 is a tracer used to trace glucose-related synthetic catabolism, is a low-cost alternative with the significant advantage that the sixth isotope of natural glucose has virtually zero natural abundance, which facilitates isotopomer analysis with <1% labeled glucose in the infusate.
|
-
- HY-70044
-
|
GSK-1070916
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-15891A
-
-
- HY-116474
-
|
Viridicatol
|
Fungal
|
Infection
|
|
Viridicatol, a quinolinone alkaloid, is isolated from the fermentation of an endophytic fungus Penicillium sp. R22 in Nerium indicum. Viridicatol has strong antifungal activity against Staphylococcus aureus with MIC value of 15.6 μg/mL.
|
-
- HY-N2108
-
|
7-Ethylcamptothecin
|
Others
|
Cancer
|
|
7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminate, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models.
|
-
- HY-112131
-
-
- HY-114286A
-
|
PXS-5153A monohydrochloride
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-B0381B
-
-
- HY-N0889
-
-
- HY-N2114
-
-
- HY-N6067
-
|
Primin
|
Bacterial
|
Cancer
Infection
|
|
Primin is a natural product stored in trichomes on leaves and stems of Primula obconica, with antimicrobial and antitumour properties.
|
-
- HY-N0424
-
|
Cycloastragenol
Cyclogalagenin; Cyclogalegenin; Cyclogalegigenin
|
Others
|
Others
|
|
Cycloastragenol, a natural tetracyclic triterpenoid, was first identified when screening Astragalus membranaceus extracts for active ingredients with antiaging properties.
|
-
- HY-N4106
-
-
- HY-N0140
-
-
- HY-N0362
-
-
- HY-N0418
-
-
- HY-N1318
-
-
- HY-N5098
-
-
- HY-W050154
-
|
Kojic acid
|
Parasite
|
Infection
|
|
Kojic acid is a natural substance produced by Aspergillus oryzae, also used as an anti-oxidant and radio-protective agent.
|
-
- HY-N2318
-
-
- HY-P1577
-
-
- HY-77813
-
-
- HY-N0722
-
-
- HY-101117
-
|
EED226
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model. EED226 is a potent, selective, and orally bioavailable EED inhibitor. EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays.
|
-
- HY-136443
-
|
4-Epitetracycline hydrochloride
|
Antibiotic
|
|
|
4-Epitetracycline hydrochloride is an epimer of the antibiotic tetracycline. Epimers of tetracycline form without catalysis and are considered degradation products. 4-Epitetracycline hydrochloride has decreased activity as an antibiotic or a Tet repressor effector but may have stronger toxic effects in animals.
|
-
- HY-N3918
-
|
γ-Fagarine
|
HCV
|
Infection
|
|
γ-Fagarine is a furoquinoline alkaloid naturally occurring in Rutae Herba. γ-Fagarine has strong anti-HCV activities with IC50 of 20.4 μg/mL and is also a sister chromatid exchanges (SCEs) inducer.
|
-
- HY-15881
-
|
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-N0288
-
-
- HY-N2345
-
|
Procyanidin B3
|
Histone Acetyltransferase
|
Cancer
|
|
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
|
-
- HY-N6715
-
|
Tenuazonic acid
|
Influenza Virus
Bacterial
|
Infection
|
|
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor.
|
-
- HY-A0126A
-
|
Epoprostenol sodium
Prostaglandin I2 sodium salt; Prostacyclin sodium salt; Flolan
|
Others
|
Cardiovascular Disease
|
|
Epoprostenol sodium (Prostaglandin I2 (sodium salt)), the synthetic form of the natural prostaglandin derivative prostacyclin (prostaglandin I2), is registered worldwide for the treatment of Pulmonary arterial hypertension (PAH). Epoprostenol sodium is used in pulmonary hypertension and transplantation as a potent inhibitor of platelet aggregation.
|
-
- HY-N0211
-
|
Cyasterone
|
EGFR
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
|
-
- HY-N0628
-
-
- HY-N2239
-
-
- HY-N3373
-
|
Loganetin
|
Bacterial
|
Infection
|
|
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
|
-
- HY-N7657
-
-
- HY-N2842
-
-
- HY-N7035
-
-
- HY-W010178
-
|
4-Methyloctanoic acid
|
Others
|
Others
|
|
4-Methyloctanoic acid is a natural compound mainly responsible for the characteristic goaty sheepy flavour of sheep and goat milk.
|
-
- HY-N6798
-
|
Myriocin
|
HCV
Antibiotic
|
Infection
|
|
Myriocin, a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin strongly suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
|
-
- HY-A0020
-
|
Eldecalcitol
ED-71; 2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3
|
VD/VDR
|
Metabolic Disease
|
|
Eldecalcitol (ED-71) is an orally active analogue of active vitamin D used in the treatment of osteoporosis. Eldecalcitol (ED-71) possesses a strong inhibitory effect on bone resorption and causes a significant increase in bone mineral density.
|
-
- HY-N2100
-
-
- HY-N4299
-
|
Caesappanin C
|
Others
|
Metabolic Disease
|
|
Caesappanin C, a biphenyl dimer from the ethanolic extract of the heartwood of Indonesian Caesalpinia sappan L., shows strong proliferation stimulating activity against the primary osteoblastic cells in vitro. Caesappanin C has the potential to stimulate bone formation and regeneration.
|
-
- HY-125747
-
|
Actinomycin X2
Actinomycin V
|
Bacterial
|
Cancer
Infection
|
|
Actinomycin X2 (Actinomycin V), produced by many Streptomyces sp., shows strong inhibition of MRSA with a minimum inhibitory concentration (MIC) value of 0.25 μg/mL. Actinomycin X2 can be used for cancer and bacterial infection.
|
-
- HY-N6011
-
|
9-Methoxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
|
9-Methoxycamptothecin (MCPT), isolated from Nothapodytes foetida, has antitumor activities through topoisomerase inhibition. 9-Methoxycamptothecin (MCPT) induces strong G2/M arrest and apoptosis in cancer.
|
-
- HY-B0492
-
-
- HY-B0492A
-
-
- HY-17448
-
-
- HY-N7058
-
|
cis-Jasmone
|
Others
|
Others
|
|
Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies.
|
-
- HY-U00185
-
-
- HY-N5120
-
|
Dihydrowithaferin A
2,3-Dihydrowithaferin A
|
AChE
|
Cancer
|
|
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE).
|
-
- HY-N0567
-
-
- HY-136466
-
|
A2ti-2
|
Virus Protease
|
Infection
|
|
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-136465
-
|
A2ti-1
|
Virus Protease
|
Infection
|
|
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-N4053
-
|
Heraclenin
|
Others
|
Inflammation/Immunology
|
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-N0739
-
|
Betaine hydrochloride
Betaine chloride
|
Others
|
Others
|
|
Betaine hydrochloride is a natural compound found in many foods and also an active methyl-donor which can maintain normal DNA methylation patterns.
|
-
- HY-N3670
-
|
Cycloolivil
Isoolivil
|
Others
|
Cardiovascular Disease
|
|
Cycloolivil (Isoolivil) is a natural polyphenolic compound with a significant radical scavenging activity present in olive tree. Antioxidant and Antiaggregant effects.
|
-
- HY-N0891
-
|
Tubeimoside II
Tubeimoside-B
|
Others
|
Cancer
|
|
Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.
|
-
- HY-N6069
-
-
- HY-N5128
-
-
- HY-B0923
-
|
Danthron
Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
|
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- HY-P1333
-
|
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-N2025
-
|
Oroxin A
|
PARP
Glucosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-N2420
-
|
Flavokawain A
|
Apoptosis
|
Cancer
|
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N7496
-
|
Odoroside A
|
Apoptosis
|
Cancer
|
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-N0239
-
-
- HY-N3051
-
-
- HY-50697
-
-
- HY-120295
-
|
A-192621
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cardiovascular Disease
|
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
|
-
- HY-N2416
-
|
Taccalonolide A
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
|
-
- HY-N7680
-
|
Neopuerarin A
|
Others
|
Metabolic Disease
|
|
Neopuerarin A is an isoflavones isolated from the water extraction of the dried roots of Pueraria lobata (Willd.). Neopuerarin A shows significant hepatoprotective effect.
|
-
- HY-N2606
-
-
- HY-N6065
-
|
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-N7028
-
|
Withanolide A
|
Others
|
Neurological Disease
|
|
Withanolide A, isolated from the indian herbal drug Ashwagandha (root of Withania somnifera), could regenerate neurites and reconstruct synapses in severely damaged neurons.
|
-
- HY-N0318
-
-
- HY-N0023
-
|
Cistanoside A
|
Others
|
Inflammation/Immunology
|
|
Cistanoside A is a phenylethanoid isolated from Cistanche deserticola, reduces NO accumulation, but shows no effect on iNOS mRNA, iNOS protein levels or iNOS activity. Anti-inflammatory effect.
|
-
- HY-131098
-
|
Enduracidin A
|
Antibiotic
|
Infection
|
|
Enduracidin A is a major component of Enduracidin. Enduracidin is a polypeptide antibiotic produced by Streptomyces fungicides.
|
-
- HY-N3201
-
-
- HY-N0581
-
-
- HY-11079
-
-
- HY-P1539
-
-
- HY-N7679
-
-
- HY-N0659
-
-
- HY-N5104
-
-
- HY-116941
-
|
A-381393
|
Dopamine Receptor
|
Neurological Disease
|
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM).
|
-
- HY-N6992
-
-
- HY-N1508
-
|
Ecliptasaponin A
|
Others
|
Inflammation/Immunology
|
|
Ecliptasaponin A , a pentacyclic triterpenoid saponin, is one of major compounds separated from Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant, and immunomodulatory.
|
-
- HY-N2175
-
-
- HY-N0081
-
|
(±)-Praeruptorin A
|
Calcium Channel
|
Infection
|
|
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker.
|
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
|
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
|
-
- HY-N2626
-
|
Epimedoside A
|
Others
|
Infection
|
|
Epimedoside A is a flavonoid isolated from the roots of Epimedium wushanense. Epimedoside A exhibits significant antioxidant activity in vitro.
|
-
- HY-N2281
-
-
- HY-N5057
-
|
Przewalskinic acid A
|
Others
|
Cardiovascular Disease
|
|
Przewalskinic acid A is a rare, water-soluble phenolic acid thus far only found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
|
-
- HY-N5087
-
-
- HY-12455
-
|
Duocarmycin A
|
ADC Cytotoxin
Apoptosis
Caspase
|
Cancer
|
|
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
|
-
- HY-N1371
-
-
- HY-N0028
-
-
- HY-108463
-
|
A-967079
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-N2155
-
-
- HY-131058
-
|
Muscotoxin A
|
ADC Cytotoxin
|
Cancer
|
|
Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
|
-
- HY-N2331
-
-
- HY-50662
-
-
- HY-N6776
-
|
Penitrem A
|
Potassium Channel
|
Cancer
Neurological Disease
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
|
-
- HY-N4084
-
|
Thonningianin A
|
Apoptosis
|
Cancer
|
|
Thonningianin A, an ellagitannin, is isolated from the methanolic extract of the African medicinal herb, Thonningia sanguinea. The antioxidant properties of Th A involve radical scavenging, anti-superoxide formation and metal chelation. Anti-cancer activities.
|
-
- HY-N2637
-
-
- HY-N2109
-
|
Macranthoidin A
|
Others
|
Metabolic Disease
|
|
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
|
-
- HY-N4236
-
|
Angelol A
|
Others
|
Others
|
|
Angelol A is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model.
|
-
- HY-N2249
-
-
- HY-N2524
-
-
- HY-133168
-
|
Englerin A
|
TRP Channel
|
Cancer
|
|
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
|
-
- HY-N0743
-
|
Senkyunolide A
|
Others
|
Cancer
|
|
Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
|
-
- HY-N7499
-
-
- HY-N6076
-
|
Tenuifoliside A
|
ERK
|
Neurological Disease
|
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-N4316
-
-
- HY-N4257
-
-
- HY-108013
-
-
- HY-125531
-
|
Dactylorhin A
|
Others
|
Others
|
|
Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
|
-
- HY-N2441
-
-
- HY-N2111
-
-
- HY-P2123
-
|
Colistin A
|
Bacterial
Antibiotic
|
Infection
|
|
Colistin A is a major component of Colistin. Colistin is a polymyxin antibiotic and can be used to combat infections caused by problematic gram-negative bacteria.
|
-
- HY-128851
-
|
Coenzyme A
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
|
-
- HY-12428
-
-
- HY-N0632
-
|
Esculentoside A
|
COX
NF-κB
|
Inflammation/Immunology
|
|
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta.
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2).
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
|
-
- HY-12761
-
-
- HY-U00225
-
-
- HY-126708
-
|
Luisol A
|
ADC Cytotoxin
|
Infection
|
|
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin.
|
-
- HY-18260
-
|
Bisphenol A
|
Endogenous Metabolite
|
Endocrinology
|
|
Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders.
|
-
- HY-100483
-
|
A-804598
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-N2017
-
-
- HY-N4318
-
-
- HY-N6593
-
-
- HY-N4223
-
|
Sibirioside A
|
Others
|
Metabolic Disease
|
|
Sibirioside A is a phenylpropanoid glycoside isolated from Scrophulariae Radix. Sibirioside A has the potential for the treatment of diabetes.
|
-
- HY-N4274
-
-
- HY-U00142
-
|
A-802715
|
Others
|
Cancer
|
|
A802715 is a methylxanthine derivative. A802715 has a TD50 (toxic dose of 50%) of 0.9-1.1 mM.
|
-
- HY-P1629
-
|
Temporin A
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
|
-
- HY-N2437
-
-
- HY-N2238
-
|
Dipsanoside A
|
Others
|
Metabolic Disease
|
|
Dipsanoside A is a novel tetrairidoid glucoside from Dipsacus asper. Dipsacus asper Wall., a perennial plant widespread in China, has been used in traditional Chinese medicine for hundreds of years as a tonic for refreshment, as a fissiparism promoter of the osseous cells, and as an embryo security agent, etc.
|
-
- HY-N0246
-
-
- HY-N6917
-
-
- HY-131103
-
-
- HY-N7692
-
|
Polyporusterone A
|
Others
|
Others
|
|
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells.
|
-
- HY-12149
-
|
A-867744
|
nAChR
Autophagy
|
Neurological Disease
|
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
|
-
- HY-N0673
-
|
Pseudolaric Acid A
|
Fungal
|
Infection
|
|
Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities.
|
-
- HY-N6997
-
|
Ceratamine A
|
Microtubule/Tubulin
|
Cancer
|
|
Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent. Ceratamine A exhibits cytotoxicity against human cancer cell lines.
|
-
- HY-N3163
-
-
- HY-118482
-
|
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-104040
-
|
MKC8866
|
IRE1
|
Cancer
|
|
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth.
|
-
- HY-N3032
-
|
Xanthatin
|
Apoptosis
VEGFR
Lipoxygenase
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Xanthatin is isolated from Xanthium strumarium leaves. Xanthatin exhibits strong antitumor activities against a variety of cancer cells through apoptosis persuasion and shows anti-inflammatory activities by inhibiting PGE2 synthesis and 5-lipoxygenase activity. Xanthatin is a potent and orally active inhibitor of VEGFR2 kinase activity with an IC50 of 3.8 μM and prominently blocks the phosphorylation of VEGFR2 at Tyr951 site. Xanthatin inhibits angiogenesis and has the potential for the investigation of breast cancer.
|
-
- HY-104051
-
-
- 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-135774
-
|
6-Hydroxybenzbromarone
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
|
-
- HY-119367
-
|
ODM-203
|
FGFR
VEGFR
|
Cancer
|
|
ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively. ODM-203 exhibits strong anti-tumor activity and induces anti-tumor immunity.
|
-
- HY-16589
-
-
- HY-133246
-
-
- HY-14660
-
|
Dabrafenib
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
|
-
- HY-N6732
-
|
K-252a
SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
PKC
PKA
CaMK
Trk Receptor
Autophagy
|
Infection
|
|
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
|
-
- HY-101938
-
-
- HY-B0069
-
-
- HY-N6013
-
|
Aloin(mixture of A&B)
|
MMP
Bacterial
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs).
|
-
- HY-100501
-
|
M2698
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
|
-
- HY-N0128
-
|
Sclareol
|
Apoptosis
|
Cancer
|
|
Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis.
|
-
- HY-N0563
-
|
Alizarin
|
Others
|
Others
|
|
Alizarin is a natural dye extracted from the roots of madder plant and has been widely used as a pigment in textile fabrics and paintings.
|
-
- HY-N0064
-
|
Macelignan
(+)-Anwulignan; Anwuligan
|
Bacterial
|
Neurological Disease
|
|
Macelignan(Anwuligan) is a natural compound isolated from Myristica fragrans Houtt; possesses therapeutic potentials against neurodegenerative diseases with oxidative stress and neuroinflammation.
|
-
- HY-N0882
-
|
Desacetylcinobufotalin
Deacetylcinobufotalin
|
Apoptosis
|
Cancer
|
|
Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
|
-
- HY-N0989
-
-
- HY-N6890
-
-
- HY-121295
-
|
Roseoflavin
|
Bacterial
|
Infection
|
|
Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.
|
-
- HY-N2622
-
|
Oxypeucedanin hydrate
(+)-Oxypeucedanin hydrate
|
Others
|
Cancer
|
|
Oxypeucedanin hydrate ((+)-Oxypeucedanin hydrate) is a natural product isolated from D. anethifolia. Prangol exhibits mild toxicity on fibroblasts and parental lymphoma cells.
|
-
- HY-B0433A
-
|
Quinine hydrochloride dihydrate
|
Parasite
|
Infection
|
|
Quinine Hydrochloride Dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.
|
-
- HY-N0714
-
|
Berbamine
|
NF-κB
Autophagy
|
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-B1071
-
-
- HY-B1071A
-
|
Lasalocid sodium
Lasalocid-A sodium; Ionophore X-537A sodium; Antibiotic X-537A sodium
|
Bacterial
Autophagy
Antibiotic
|
Cancer
Infection
|
|
Lasalocid sodium (Lasalocid-A sodium) treatment led to an increase in cell wall thickness, whilst the quantity and sugar composition of the cell wall remained unchanged in BY-2 cells.
|
-
- HY-N1956
-
|
Rubiadin-1-methyl ether
|
NF-κB
|
Metabolic Disease
|
|
Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
|
-
- HY-10529
-
-
- HY-101785
-
-
- HY-111174A
-
-
- HY-14852A
-
|
Tafamidis meglumine
Fx-1006A
|
Others
|
Neurological Disease
|
|
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis.
|
-
- HY-N4100
-
|
Trilobatin
|
HIV
SGLT
|
Infection
|
|
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
|
-
- HY-102026
-
-
- HY-117319
-
-
- HY-N0513
-
|
Loganic acid
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity.
|
-
- HY-N2203
-
-
- HY-110120
-
|
DSR-6434
|
Toll-like Receptor (TLR)
|
Cancer
|
|
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
|
-
- HY-N2996
-
|
Ganodermanondiol
|
HIV Protease
|
Infection
|
|
Ganodermanondiol is a melanogenesis inhibitor isolated from the Ganoderma lucidum.Ganodermanondiol exhibits potent cytoprotective effects on tert-butyl hydroperoxide-induced hepatotoxicity. Ganodermanondiol shows significant anti-HIV-1 protease activity with an IC50 of 90 μM. Ganodermanondiol exhibits a strong anticomplement activity against the classical pathway of the complement system with an IC50 of 41.7μM.
|
-
- HY-13960
-
-
- HY-N0610
-
-
- HY-B0914A
-
-
- HY-111911
-
-
- HY-B2188
-
-
- HY-U00097
-
-
- HY-109044
-
-
- HY-N3521
-
|
Platycoside G1
Deapi-platycoside E
|
Others
|
Others
|
|
Platycoside G1, a natural product found in Platycodon grandiflorum, is a triterpenoid saponin. Platycoside G1 has potent antioxidant activities.
|
-
- HY-N1166
-
|
Tephrosin
Deguelinol I; Hydroxydeguelin
|
EGFR
|
Cancer
|
|
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
|
-
- HY-W010533
-
-
- HY-W012999
-
|
Tiglic acid
|
Endogenous Metabolite
|
Others
|
|
Tiglic acid is a monocarboxylic unsaturated organic acid found in croton oil and in several other natural products. Tiglic aci has a role as a plant metabolite.
|
-
- HY-N0033
-
|
Poliumoside
|
Others
|
Metabolic Disease
|
|
Poliumoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 value of 4.6-25.7 μM.
|
-
- HY-Y0152
-
|
Cinchonine
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
|
Cancer
|
|
Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- HY-N1368A
-
-
- HY-17590
-
-
- HY-16059
-
-
- HY-13746
-
|
Sardomozide
CGP 48664; SAM-486A
|
Others
|
Cancer
|
|
Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
|
-
- HY-B1311
-
-
- HY-12424
-
|
Zotarolimus
ABT-578; A 179578
|
Others
|
Cancer
|
|
Zotarolimus is a tetrazole-containing Rapamycin analog which is used as animmunomodulator, and is useful in the treatment of restenosis, immune, and autoimmune diseases.
|
-
- HY-N1913
-
-
- HY-13768A
-
-
- HY-N6020B
-
|
Butin
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities. Butin significantly alleviates myocardial infarction and improves heart function, together with prevents diabetes-induced cardiac oxidative damage in rat.
|
-
- HY-N3000
-
|
6-Methoxydihydrosanguinarine
|
Others
|
Cancer
|
|
6-Methoxydihydrosanguinarine is an lkaloid isolated from the fruits of M.cordata. 6-Methoxydihydrosanguinarine shows strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μM and 0.54 μM, respectively.
|
-
- HY-N5142
-
|
α-Terpineol
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria.
α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption.
|
-
- HY-18649A
-
|
Galidesivir
BCX4430; Immucillin-A
|
DNA/RNA Synthesis
SARS-CoV
Filovirus
|
Infection
|
|
Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
|
-
- HY-100877
-
-
- HY-N4205
-
|
Tetrahydropiperine
|
Cytochrome P450
|
Cancer
|
|
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum. Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM).
|
-
- 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-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-N2574
-
|
Gitogenin
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
|
-
- HY-Y0790
-
|
Cuminaldehyde
|
Endogenous Metabolite
|
Cancer
|
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.
|
-
- 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-N0452
-
-
- HY-N0224
-
|
Epigoitrin
|
Influenza Virus
|
Infection
Cancer
|
|
Epigoitrin is a natural alkaloid from Isatis indigotica, with antiviral activities. Epigoitrin reduces susceptibility to influenza virus via mitochondrial antiviral signaling.
|
-
- HY-N2868
-
|
Andropanoside
|
Others
|
Metabolic Disease
|
|
Andropanoside is a natural product isolated and purified from the herbs of Andrographis paniculata. Andrographis paniculata possesses a protective activity against various liver disorders.
|
-
- HY-N4068
-
|
Glucoraphanin
|
Reactive Oxygen Species
|
Cancer
|
|
Glucoraphanin, a natural glucosinolate found in cruciferous vegetable, is a stable precursor of the Nrf2 inducer sulforaphane, which possesses antioxidant, anti-inflammatory, and anti-carcinogenic effects.
|
-
- HY-W007856
-
|
5-Methoxysalicylic acid
5-MeOSA
|
Others
|
Others
|
|
5-Methoxysalicylic acid (5-MeOSA) is a natural compound, used as a useful matrix in the MALDI MS analysis of oligonucleotides when combined with spermine.
|
-
- HY-N0713
-
-
- HY-14781
-
-
- HY-N0207
-
-
- HY-N0398
-
-
- HY-15511
-
|
Tyrphostin A9
Tyrphostin 9; Malonoben
|
VEGFR
Influenza Virus
|
Cancer
Infection
|
|
Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
|
-
- HY-12186
-
-
- HY-P1259
-
|
PR-39
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-101496
-
|
MT-DADMe-ImmA
MTDIA; Methylthio-DADMe-Immucillin A
|
Others
|
Cancer
|
|
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
|
-
- HY-N0346A
-
-
- HY-17499
-
|
EGFR-IN-12
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity.
|
-
- HY-19617B
-
|
EGFR-IN-1 TFA
|
EGFR
|
Cancer
|
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-10895
-
|
SB-334867
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
|
-
- HY-100014
-
|
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-129405
-
-
- HY-N0361
-
|
Dihydrocapsaicin
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.
|
-
- HY-17434
-
-
- HY-W015307
-
|
4-Ethyloctanoic acid
|
Others
|
Others
|
|
4-Ethyloctanoic acid is a natural compound first isolated from Saussurea lappa Clarke, widely used as a safe flavoring compound and acts as food additive.
|
-
- HY-N2487
-
-
- HY-N0777
-
-
- HY-N2370
-
-
- HY-121471
-
|
Chrysoeriol
|
Others
|
Metabolic Disease
|
|
Chrysoeriol, a natural flavonoid extracted from the tropical plant Coronopus didymus, exhibits potent antioxidant activity. Chrysoeriol shows significant inhibition of lipid peroxidation.
|
-
- HY-B0781
-
-
- HY-N1775
-
|
3',4'-Dihydroxyacetophenone
3,4-DHAP
|
Tyrosinase
|
Cancer
|
|
3',4'-Dihydroxyacetophenone (3,4-DHAP), isolated from Picea Schrenkiana Needles exhibits a strong suppressive action against tyrosinase activity, with an IC50 of 10 μM. 3',4'-Dihydroxyacetophenone (3,4-DHAP) is a vasoactive agent and antioxidant.
|
-
- HY-18085
-
-
- HY-15826
-
-
- HY-N6680
-
|
Virginiamycin S1
|
Bacterial
Antibiotic
|
Infection
|
|
Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections[1][2].
|
-
- HY-100943
-
|
Cinanserin hydrochloride
SQ 10643
|
5-HT Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
|
-
- HY-128717A
-
|
GSK3368715 dihydrochloride
EPZ019997 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
|
-
- HY-N6742
-
|
Borrelidin
Treponemycin
|
CDK
Parasite
Apoptosis
Antibiotic
|
Infection
|
|
Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei. Borrelidin (Treponemycin) is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM. Borrelidin (Treponemycin) is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM, and induces apoptosis of the tube-forming cells. Borrelidin (Treponemycin) has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum.
|
-
- HY-P1259A
-
|
PR-39 TFA
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
|
-
- HY-N6682
-
|
Cytochalasin D
Zygosporin A; NSC 209835
|
Arp2/3 Complex
Bacterial
Antibiotic
YAP
|
Infection
|
|
Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
|
-
- HY-N1724
-
-
- HY-14261
-
-
- HY-N2840
-
|
Allitol
Allodulcitol
|
Others
|
Cancer
Metabolic Disease
|
|
Allitol is a rare natural polyol that can be used as a sweetener. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS.
|
-
- HY-N0805
-
|
Alisol B 23-acetate
23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate
|
Others
|
Others
|
|
Alisol B 23-acetate (23-Acetylalismol B), a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.
|
-
- HY-N2561
-
|
Seneciphylline N-Oxide
|
Others
|
Cancer
|
|
Seneciphylline N-Oxide is a dehydrogenation product of Senecionine N-oxide. Seneciphylline N-Oxide is a natural compound isolated from root cultures of Senecio erucifolius (Asteraceae).
|
-
- HY-N0124
-
|
Dioscin
Collettiside III; CCRIS 4123
|
Autophagy
Apoptosis
|
Cancer
|
|
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines.
|
-
- HY-16686
-
|
α-Tocopherol phosphate
alpha-Tocopherol phosphate; TocP; vitamin E phosphate
|
Others
|
Others
|
|
α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
|
-
- HY-N0345
-
|
Liriope muscari baily saponins C
|
Others
|
Cancer
Inflammation/Immunology
|
|
Liriope muscari baily saponins C is one of major active compounds of L. muscari (Decne.) Baily. Liriope muscari baily saponins C possesses strong anti-inflammatory, immunopharmacological and cardioprotective activities. Liriope muscari baily saponins C has been studied as a candidate drug for cancer metastasis.
|
-
- HY-106410
-
|
Zabofloxacin
DW-224a Free base
|
Bacterial
Topoisomerase
|
Infection
|
|
Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
|
-
- HY-15308
-
-
- HY-15556
-
-
- HY-W046353
-
|
2-Methoxycinnamaldehyde
o-Methoxycinnamaldehyde
|
Apoptosis
|
Cancer
|
|
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration.
|
-
- HY-112398
-
-
- HY-111098
-
-
- HY-N4146
-
-
- HY-19608
-
-
- HY-N6982
-
-
- HY-103000
-
-
- HY-133777
-
-
- HY-N7597
-
|
Epimedoside
Korepimedoside A
|
Others
|
Others
|
|
Epimedoside is a flavonol glycoside, isolated from the aerial parts of Epimedium koreanum Nakai (Berberidaceae).
|
-
- HY-122815
-
|
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-75041
-
|
Calcitriol Impurities A
|
VD/VDR
|
Metabolic Disease
|
|
Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-N4133
-
-
- HY-B0911
-
|
Sodium copper chlorophyllin A
|
Others
|
Cancer
|
|
Sodium copper chlorophyllin A is a semi-synthetic mixture of water-soluble sodium copper salts derived from chlorophyll, primarily used as a food additive and in alternative medicine.
|
-
- HY-N5045
-
|
Jionoside A1
|
Others
|
Inflammation/Immunology
|
|
Jionoside A1 isolated from Radix Rehmanniae Praeparata displays dose dependent immune-enhancement activity and possesses moderate protective activities on H2O2-treated SH-SY5Y cells.
|
-
- HY-N0568
-
-
- HY-13032A
-
|
GSK 525768A
|
Others
|
Cancer
|
|
GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
|
-
- HY-B0343A
-
-
- HY-N6950
-
|
Hederacolchiside A1
|
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Cancer
Infection
|
|
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
|
-
- HY-N2264
-
|
Wulignan A1
|
Influenza Virus
|
Infection
|
|
Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities.
|
-
- HY-P1539A
-
-
- HY-107676
-
|
SIB-1553A
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-B1802A
-
-
- HY-100454
-
-
- HY-P2123A
-
-
- HY-107273
-
-
- HY-N5064
-
-
- HY-P1333A
-
|
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-15442
-
-
- HY-N7438
-
|
Mogroside VI A
|
Others
|
Others
|
|
Mogroside VI A, an isomer of Mogroside VI isolated from Luo Han Guo, exerts sweetness property. Mogroside VI A can be used for sweetener and/or taste modifier research.
|
-
- HY-112091
-
-
- HY-N5106
-
|
(E)-Flavokawain A
|
Apoptosis
|
Cancer
|
|
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
|
-
- HY-N2343
-
-
- HY-113573
-
|
Protosappanin A
PTA
|
JAK
STAT
|
Inflammation/Immunology
|
|
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.
|
-
- HY-103200
-
-
- HY-128973
-
-
- HY-N2172
-
-
- HY-111828
-
|
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-N0495
-
|
Aloenin
Aloenin A
|
Beta-secretase
|
Neurological Disease
|
|
Aloenin (Aloenin A) is a class of anthraquinones isolated from Aloe arborescens. Aloenin has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).
|
-
- HY-15995
-
-
- HY-N0150
-
|
Monensin sodium salt
Monensin A sodium salt
|
Bacterial
Sodium Channel
Antibiotic
|
Infection
Cancer
|
|
Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Monensin sodium salt is an ionophore that mediates Na +/H + exchange. Monensin sodium salt causes a marked enlargement of the MVBs and regulates exosome secretion.
|
-
- HY-103129
-
|
SB-200646A
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
|
-
- HY-101582
-
-
- HY-19243
-
-
- HY-101192
-
-
- HY-108434
-
|
Ceapin-A7
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
|
-
- HY-111398
-
-
- HY-113263
-
-
- HY-102064
-
|
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-N6079
-
-
- HY-N6942
-
|
Mogroside IV-A
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside IV-A, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N2167
-
-
- HY-B0519A
-
|
Tylosin
Tylosin A
|
Bacterial
Antibiotic
|
Infection
|
|
Tylosin (Fradizine; Tylocine; Tylosin A) is a broad spectrum antibiotic against Gram-positive organisms and a limited range of Gram-negative organisms.
|
-
- HY-128945
-
|
CL2A
|
ADC Linker
|
Cancer
Inflammation/Immunology
|
|
CL2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
|
-
- HY-100672
-
-
- HY-119744
-
|
BAY 38-7271
|
Cannabinoid Receptor
|
Neurological Disease
|
|
BAY 38-7271 is selective and highly potent and cannabinoid CB1/CB2 receptor agonist, with Kis of 1.85 nM and 5.96 nM for recombinant human CB1 receptor and CB2 receptor, respectively. BAY 38-7271 has strong neuroprotective properties.
|
-
- HY-D1117
-
|
NADA-green
NADA hydrochloride
|
Others
|
|
|
NADA-green, a fluorescent D-amino acid, suitable for labeling peptidoglycans in live bacteria. NADA-green is incorporated into bacterial cell walls during synthesis. NADA-green results in strong peripheral and septal labeling of taxonomically diverse bacterial cell populations without affecting growth rate. Excitation/emission λ ~450/555 nm.
|
-
- HY-108464A
-
|
Phenamil methanesulfonate
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
|
-
- HY-P2657
-
|
Verucopeptin
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-133646
-
|
Bromochloroacetonitrile
|
DNA/RNA Synthesis
|
Others
|
|
Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage.
|
-
- HY-N6018
-
-
- HY-N4000
-
|
Digitonin
|
Others
|
Cancer
|
|
Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
|
-
- HY-13938
-
|
Iretol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Iretol (2,4,6-trihydroxyanisole) is a a degradation product of a glucoside obtained from Iris Jorentina. Iretol is an intermediate in the synthesis of natural isoflavones, such as Tectorigenin, Irigenin and Caviunin.
|
-
- HY-N6965
-
-
- HY-N6829
-
|
Retusin
Quercetin-3,3',4',7-tetramethylether
|
Others
|
Infection
Inflammation/Immunology
|
|
Retusin (Quercetin-3,3',4',7-tetramethylether), a natural compound isolated from the leaves of Talinum triangulare, possesses antiviral and anti-inflammatory activities.
|
-
- HY-N1181
-
-
- HY-112542
-
|
Nemadectin
CL-287088; LL-F28249 α
|
Parasite
Antibiotic
|
Infection
|
|
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.
|
-
- HY-N2338
-
-
- HY-N5029
-
|
Isofebrifugine
|
Parasite
|
Infection
|
|
Isofebrifugine, isolated from a Chinese medicinal plant, Chang Shan (Dichroa febrifuga), is a natural quinazolinone alkaloid with important physiological activities and good pharmacological effects. Antimalarial effect.
|
-
- HY-U00450
-
-
- HY-N7011
-
-
- HY-N7624
-
|
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
-
- HY-15464D
-
|
(S)-Gossypol acetic acid
(S)-(+)-Gossypol acetic acid
|
Bcl-2 Family
|
Cancer
|
|
(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
|
-
- HY-N7124
-
|
Benzyl acetate
|
Others
|
Others
|
|
Benzyl acetate is a constituent of jasmin and of the essential oils of ylang-ylang and neroli. Natural sources of Benzyl acetate include varieties of flowers like jasmine (Jasminum), and fruits like pear, apple.
|
-
- HY-129039
-
|
Butyrolactone 3
|
Histone Acetyltransferase
|
Cancer
|
|
Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
|
-
- 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-N0146
-
-
- HY-136310
-
|
PIP4K-IN-a131
|
Others
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
|
-
- HY-136203
-
-
- HY-103700B
-
|
(Rac)-Azide-phenylalanine
|
Others
|
Others
|
|
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins.
|
-
- HY-N1283
-
|
Seneciphyllinine
|
Others
|
Metabolic Disease
|
|
Seneciphyllinine, a pyrrolizidine alkaloid, is isolated from the roots of Gynura japonica. Pyrrolizidine alkaloids are highly hepatotoxic natural chemicals that produce irreversible chronic and acute hepatotoxic effects on human beings.
|
-
- HY-N0849
-
|
Dictamine
Dictamnine; Dectamine
|
Apoptosis
Bacterial
Fungal
|
Infection
|
|
Dictamnine (Dictamine) has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells; A natural plant product has been reported to have antimicrobial activity against bacteria and fungi.
|
-
- HY-N6661
-
|
Verbenone
(-)-Verbenone
|
Others
|
Infection
|
|
Verbenone ((-)-Verbenone) is a natural terpene in leaves of the tree, Suregada zanzibariensis Verdc. Verbenone has anti-aggregation pheromone and interrupts the attraction of bark beetles to their aggregation pheromones.
|
-
- HY-B2114
-
|
Escin
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Escin, a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.
|
-
- HY-W002272
-
|
Isocytosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Isocytosine is a non-natural nucleobase and an isomer of cytosine. It is used in combination with Isoguanine in studies of unnatural nucleic acid analogues of the normal base pairs in DNA and used as a nucleobase of hachimoji RNA.
|
-
- 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-N0417
-
|
Cucurbitacin E
α-Elaterin; α-Elaterine
|
CDK
Autophagy
|
Cancer
|
|
Cucurbitacin E is a natural compound which from the climbing stem of Cucumic melo L. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
|
-
- HY-19644
-
|
GSK2256294A
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
|
-
- HY-15477A
-
|
YS-49 monohydrate
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-15477
-
|
YS-49
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-13032
-
-
- HY-101513
-
|
eIF4A3-IN-1
|
Eukaryotic Initiation Factor (eIF)
Autophagy
|
Cancer
|
|
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
|
-
- HY-N0240
-
|
Herbacetin
|
Others
|
Cancer
|
|
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
|
-
- HY-17389
-
|
Genipin
(+)-Genipin
|
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.
|
-
- HY-P2031
-
|
Phallacidin
|
Others
|
|
|
Phallacidin is a natural mycotoxin first isolated from the death cap mushroom, A. phalloides. Phallacidin binds filamentous actin (F-actin) like phalloidin (Item No. 18039), but contains a carboxyl group for coupling reactions.
|
-
- HY-N0360
-
|
Dihydrotanshinone I
|
SARS-CoV
|
Cardiovascular Disease
|
|
Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases. Dihydrotanshinone I exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-N0876
-
|
Arenobufagin
|
Others
|
Cancer
|
|
Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
|
-
- HY-N7029
-
|
3',4',5',5,7-Pentamethoxyflavone
|
Others
|
Cancer
|
|
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway.
|
-
- HY-N2445
-
|
Flavokawain C
|
Apoptosis
|
Cancer
|
|
Flavokawain C is a natural chalcone found in Kava root. Flavokawain C exerts cytotoxicity against human cancer cell lines, with an IC50 of 12.75 μM for HCT 116 cells.
|
-
- HY-N6038
-
|
Gartanin
|
Others
|
Cancer
|
|
Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells.
|
-
- HY-N7650
-
|
Dihydroseselin
|
Others
|
Others
|
|
Dihydroseselin is a 7-hydroxycoumarin (HY-N0573) derivative. 7-hydroxycoumarin is a natural product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent
|
-
- HY-N0163
-
-
- HY-N0370
-
|
Bergapten
5-Methoxypsoralen
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Bergapten is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. Bergapten is inhibitory towards mouse and human CYP isoforms.
|
-
- HY-N7614
-
|
Anemarrhenasaponin A2
Schidigerasaponin F2; Timosaponin AII
|
Others
|
Cardiovascular Disease
|
|
Anemarrhenasaponin A2 (Schidigerasaponin F2;Timosaponin AII) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation.
|
-
- HY-N0551
-
|
Wedelolactone
|
Caspase
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
|
-
- HY-110137A
-
|
Furamidine
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent.
|
-
- HY-136065A
-
|
bpV(phen) hydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) hydrate is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) hydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) hydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) hydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-136065
-
|
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-110137
-
|
Furamidine dihydrochloride
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
|
-
- HY-10252
-
|
NVP-ADW742
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
|
-
- HY-136093A
-
|
IM156
HL156A; HL271 acetate
|
AMPK
|
Cancer
Neurological Disease
|
|
IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-P9805
-
|
Anti-MERS-3A1 mAb
MERS-3A1; MERS Antibody-3A1
|
SARS-CoV
|
Infection
|
|
Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells.
Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor.
|
-
- HY-12838
-
|
Mirk-IN-1
Dyrk1B/A-IN-1
|
DYRK
|
Cancer
|
|
Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
|
-
- HY-106950
-
|
Fosfructose
Diphosphofructose; Esafosfan; FDP
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Fosfructose (Diphosphofructose;Esafosfan;FDP) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
|
-
- HY-13407
-
|
Gossypol
BL 193
|
Bcl-2 Family
|
Cancer
|
|
Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
|
-
- HY-18569
-
|
3-Indoleacetic acid
Indole-3-acetic acid; 3-IAA
|
Endogenous Metabolite
|
Others
|
|
3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division.
|
-
- HY-125699
-
|
Ochratoxin C
|
Fungal
|
|
|
Ochratoxin C is the ethyl ester analog of ochratoxin A, a mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant. Ochratoxin C rarely occurs as an initial natural contaminant due to a transformation from ochratoxin A.
|
-
- HY-N2572
-
|
Nepetin
6-Methoxyluteolin
|
Others
|
Inflammation/Immunology
|
|
Nepetin (6-Methoxyluteolin) is a natural flavonoid isolated from Eupatorium ballotaefolium HBK with potent anti-inflammatory activities. Nepetin inhibits IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43 μM, 3.42 μM and 4.17 μM, respectively in ARPE-19 cells.
|
-
- HY-18085S
-
|
Quercetin D5
|
PI3K
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
|
-
- HY-111532
-
|
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
|
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
|
-
- HY-N6257
-
|
Cafestol
|
ERK
PGE synthase
COX
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Cafestol, one of the major components of coffee, is a coffee-specific diterpene from. Cafestol is a ERK inhibitor for AP-1-targeted activity against PGE2 production and the mRNA expression of cyclooxygenase (COX)-2 in LPS-activated RAW264.7 cells. Cafestol has strong inhibitory activity on PGE2 production by suppressing the NF-kB activation pathway. Cafestol contributes to its beneficial effects through various biological activities such as chemopreventive, antitumorigenic, hepatoprotective, antioxidative and antiinflammatory effects.
|
-
- HY-N2050
-
-
- HY-N6850
-
|
Calenduloside E
|
HSP
Endogenous Metabolite
|
|
|
Calenduloside E (CE) is a natural pentacyclic triterpenoid saponin extracted from Aralia elata. Calenduloside E (CE) has anti-apoptotic potent by targeting heat shock protein 90 (Hsp90).
|
-
- HY-N5083
-
|
Saponarin
|
Others
|
Inflammation/Immunology
|
|
Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
|
-
- HY-N6969
-
|
Dicentrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates.
|
-
- HY-W011241
-
|
Cinchonine hydrochloride
(8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride
|
Apoptosis
Parasite
|
Cancer
|
|
Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural compound present in Cinchona bark. Cinchonine hydrochloride activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- 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[1] [2] .
|
-
- HY-18649
-
|
Galidesivir hydrochloride
BCX 4430 hydrochloride; Immucillin-A hydrochloride
|
DNA/RNA Synthesis
SARS-CoV
Filovirus
|
Infection
|
|
Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
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- HY-101947
-
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SMI-16a
PIM1/2 Kinase Inhibitor VI
|
Pim
|
Cancer
|
|
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
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-
- HY-126247
-
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BI-2852
|
Ras
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Cancer
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|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRAS G12D versus KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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- HY-N7020
-
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Cinobufaginol
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Others
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Cancer
|
|
Cinobufaginol is a natural bufadienolide isolated from toad venom which has been widely used for centuries in China to treat different diseases, especially for cancer. Cinobufaginol potently inhibits the activity against human nasopharyngeal carcinoma cell lines with IC50s of 803 μΜ and 1.270 μΜ for CNE-1 and CNE-2Z, respectively.
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- HY-P1505
-
-
- HY-P1788
-
-
- HY-16668
-
-
- HY-14262
-
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Vilazodone
EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
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-
- HY-N6882
-
-
- HY-N7247
-
|
Thiochrome
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
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-
- HY-N7117
-
-
- HY-N4093
-
|
Astringin
trans-Astringin
|
Others
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Cancer
|
|
Astringin (trans-Astringin) is a natural glycoside found in the bark of Picea sitchensis and Picea abies (Norway spruce), in Vitis vinifera cell cultures and in wine. Astringin has potent antioxidant capacity and cancer-chemopreventive activity.
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-
- HY-119412
-
|
Biliatresone
|
Others
|
Metabolic Disease
|
|
Biliatresone is a natural toxin isolated from Dysphania glomulifera and D. littoralis. Biliatresone, a 1,2-diaryl-2-propenone class of isoflavonoid, produces extrahepatic biliary atresia in a zebrafish model.
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-
- HY-N7072
-
-
- HY-114495
-
|
Caerulomycin A
Cerulomycin; Caerulomycin
|
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
|
-
- HY-126937
-
|
Ivermectin B1a
|
Parasite
SARS-CoV
|
Infection
|
|
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310). Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-112667
-
-
- HY-19555
-
|
Seco Rapamycin
Secorapamycin A
|
Others
|
Others
|
|
Seco Rapamycin (Secorapamycin A) is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-B0355
-
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-101437
-
-
- HY-P9904
-
|
Atezolizumab
MPDL3280A
|
PD-1/PD-L1
|
Cancer
|
|
Atezolizumab is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
|
-
- HY-108272
-
|
Mogroside II-A2
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside II-A2, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-101437A
-
-
- HY-100638
-
|
RPR132595A
NPC
|
Others
|
Cancer
|
|
RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
|
-
- HY-100673
-
-
- HY-N3502
-
-
- HY-B0395C
-
-
- HY-N0679
-
|
Retinyl acetate
Retinol acetate; Vitamin A acetate
|
Others
|
Cancer
|
|
Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities.
|
-
- HY-B0197A
-
-
- HY-135283
-
|
ABT-546
A-216546
|
Endothelin Receptor
|
Endocrinology
Cardiovascular Disease
|
|
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
|
-
- HY-B0284
-
-
- HY-N2214
-
|
7-O-Methylaloeresin A
|
Bacterial
|
Inflammation/Immunology
|
|
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae).
7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively.
7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively.
|
-
- HY-B0523A
-
-
- HY-108385
-
|
Ochratoxin A-D4
|
Others
|
Cancer
|
|
Ochratoxin A-D4 is the deuterium labeled Ochratoxin A. Ochratoxin A, a mycotoxin produced by several fungal species, causes nephrotoxicity and renal tumors in a variety of animal species.
|
-
- HY-108593
-
-
- HY-N1964
-
|
Gibberellic acid
Gibberellin A3
|
Others
|
Others
|
|
Gibberellic Acid is named after a fungus Gibberella fujikuroi . Gibberellic Acid regulates processes of plant development and growth, including seed development and germination, stem and root growth, cell division, and flowering time.
|
-
- HY-131103S
-
-
- HY-B0395
-
-
- HY-P0236
-
-
- HY-N6854
-
|
Mogroside I A1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside I A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
