Search Result
Results for "A hd elite aromatase Inhibitors" in MCE Product Catalog:
9540
Inhibitors & Agonists
15
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-13632
-
|
Exemestane
FCE 24304; EXE
|
Aromatase
|
Cancer
Endocrinology
|
|
Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
|
-
- HY-14248
-
|
Letrozole
CGS 20267
|
Aromatase
Autophagy
|
Cancer
|
|
Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
|
-
- HY-N5012
-
|
Eurycomanone
Pasakbumin A
|
Others
|
Endocrinology
|
|
Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
|
-
- HY-N0292
-
|
Oleuropein
|
PPAR
Apoptosis
Aromatase
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
|
-
- HY-U00439
-
-
- HY-14247
-
|
Fadrozole hydrochloride
CGS 16949A; (Rac)-FAD286 hydrochloride
|
Aromatase
|
Cancer
|
|
Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
|
-
- HY-136063
-
|
Mefentrifluconazole
|
Fungal
Cytochrome P450
|
Infection
|
|
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM).
|
-
- HY-14247A
-
|
Fadrozole
CGS 16949A free base; (Rac)-FAD286
|
Aromatase
|
Cancer
|
|
Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
|
-
- HY-B0274
-
-
- HY-B0274A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-101382
-
|
GR 103691
|
Dopamine Receptor
|
Neurological Disease
|
|
GR 103691 is a potent, selective dopamine D3 receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites.
|
-
- HY-U00176
-
-
- HY-N7128
-
|
Flavanone
|
Aromatase
|
Cancer
|
|
Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase).
|
-
- 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-B0623A
-
|
Ropinirole hydrochloride
SKF 101468 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Ropinirole hydrochloride is a potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole hydrochloride has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole hydrochloride has no affinity for the D1 receptors. Ropinirole hydrochloride has the potential for Parkinson's disease.
|
-
- HY-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-B0845
-
|
Prochloraz
BTS 40542
|
Fungal
Estrogen Receptor/ERR
Androgen Receptor
Aryl Hydrocarbon Receptor
|
Infection
|
|
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50=40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s=25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50=1 μM).
|
-
- HY-14328
-
|
Sonepiprazole
PNU-101387G; U-101387G
|
Dopamine Receptor
|
Neurological Disease
|
|
Sonepiprazole (PNU-101387G) is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively.
|
-
- HY-125833
-
|
Alpha-Naphthoflavone
|
Aromatase
|
Cancer
|
|
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
|
-
- HY-131005
-
-
- HY-18719B
-
-
- HY-18719E
-
-
- HY-14782
-
|
Adoprazine
SLV313
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics.
|
-
- 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-121879
-
-
- 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-N8405
-
|
Isolimonexic acid
|
Aromatase
|
Cancer
|
|
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
|
-
- HY-19373
-
-
- 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-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-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-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-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-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-18728
-
-
- HY-B1558A
-
|
Bifemelane hydrochloride
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride 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-136092
-
|
Androsta-1,4,6-triene-3,17-dione
|
Aromatase
|
Endocrinology
Neurological Disease
|
|
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.
|
-
- HY-106019C
-
|
Liarozole dihydrochloride
R75251 dihydrochloride
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
|
-
- HY-130259
-
|
LC3-mHTT-IN-AN2
|
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-130258
-
|
LC3-mHTT-IN-AN1
|
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-15583
-
-
- HY-12054A
-
-
- HY-N0693
-
-
- 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-12054
-
|
Hesperadin
|
Aurora Kinase
Autophagy
Influenza Virus
Parasite
|
Cancer
|
|
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
|
-
- HY-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-13503
-
-
- 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-15720B
-
|
Glycyl H-1152 hydrochloride
|
ROCK
Aurora Kinase
CaMK
|
Neurological Disease
|
|
Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.
|
-
- HY-107426
-
|
Verrucarin A
Muconomycin A
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
|
-
- HY-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-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-N2221
-
-
- HY-N1447
-
-
- HY-18983
-
|
Calyculin A
(-)-Calyculin A
|
Phosphatase
|
Cancer
|
|
Calyculin A ((-)-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, 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 .
|
-
- HY-138294
-
|
RAS/RAS-RAF-IN-1
|
Ras
Raf
|
Cancer
|
|
RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
|
-
- 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-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-108486
-
|
Herbimycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-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-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-131907
-
|
LpxC-IN-5
|
Bacterial
|
Infection
|
|
LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively.
|
-
- 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-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-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-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-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-13254A
-
-
- HY-13254
-
|
A-674563
|
Akt
|
Cancer
|
|
A-674563 is a potent and selective Akt1 inhibitor with a Ki of 11 nM.
|
-
- HY-130841
-
|
Apcin-A
|
APC
Ligand for Target Protein for PROTAC
|
Cancer
|
|
Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257).
|
-
- HY-116090
-
|
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-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-127002A
-
|
Squarunkin A hydrochloride
|
Src
|
Cancer
|
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
|
-
- HY-N2498
-
-
- 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-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-N0466
-
-
- HY-13261
-
|
A66
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- 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-17387
-
|
(-)-Huperzine A
Huperzine A
|
AChE
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-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-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-19563
-
-
- 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-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-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-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-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-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-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-136072
-
|
QPX7728-OH disodium
|
Bacterial
|
Infection
|
|
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
|
-
- HY-19725
-
-
- HY-N6584
-
-
- 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-15764
-
|
A 419259
RK-20449
|
Src
|
Cancer
|
|
A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards the Src family with IC50 of 9 nM, <3 nM and <3 nM for Src, Lck and Lyn, respectively.
|
-
- 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-N2392
-
-
- HY-B0856
-
|
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
|
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-136071
-
-
- HY-136070
-
-
- 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-118773
-
|
MreB Perturbing Compound A22 hydrochloride
A22 hydrochloride
|
Bacterial
|
Inflammation/Immunology
|
|
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-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-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-N3389
-
-
- HY-107433
-
-
- HY-N7452
-
-
- 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-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-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-137473
-
|
Methyl pyropheophorbide-a
Pyropheophorbide-a methyl ester
|
Apoptosis
|
Cancer
|
|
Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth.
|
-
- 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-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-13020
-
-
- 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-101835
-
-
- HY-100599
-
-
- 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-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-105755
-
|
Antimycin A3
|
Mitochondrial Metabolism
Apoptosis
|
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-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-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-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-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-122135
-
-
- 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-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-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-112205
-
-
- 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-100558
-
|
Bafilomycin A1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Cancer
Infection
|
|
Bafilomycin A1 is a specific and reversible 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-11000
-
-
- HY-19422
-
-
- 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-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-107455
-
-
- HY-12507
-
-
- 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-N6073
-
|
Soyasapogenol A
|
Apoptosis
|
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-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-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-50880
-
-
- 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-117832
-
-
- HY-12468
-
|
A-1210477
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.
|
-
- 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-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-137563
-
|
A2793
|
Potassium Channel
|
Neurological Disease
|
A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1.
|
-
- HY-14164
-
-
- 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-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-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-12583
-
|
A-366
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
|
-
- HY-111417
-
-
- 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-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-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-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-14164A
-
-
- 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
Apoptosis
|
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-128553
-
-
- HY-100611
-
-
- HY-18303
-
|
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
|
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-131059
-
|
CBS1117
|
Influenza Virus
|
Infection
|
|
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process.
|
-
- 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-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-15005C
-
|
Sofosbuvir impurity A
|
HCV
|
Infection
|
|
Sofosbuvir impurity A, an diastereoisomer of Sofosbuvir, is the impurity of Sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
|
-
- 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-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-108706
-
|
KDM2A/7A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
|
-
- HY-13746B
-
-
- HY-13237
-
-
- HY-100183
-
-
- HY-112726
-
-
- 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-16576A
-
|
(Z)-SMI-4a
|
Pim
|
Cancer
|
|
(Z)-SMI-4a is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 µM. (Z)-SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. (Z)-SMI-4a has anticancer activity.
|
-
- 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-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-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-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-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-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-13036A
-
|
IBT6A
|
Btk
|
Cancer
|
|
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-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-13036B
-
|
IBT6A hydrochloride
|
Btk
|
Cancer
|
|
IBT6A hydrochloride 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-114267
-
|
Cbz-B3A
|
mTOR
|
Others
|
|
Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
|
-
- HY-B1202A
-
-
- HY-13339
-
-
- HY-B0093A
-
-
- HY-B0422
-
|
Nateglinide
A4166; Senaglinide
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-104064
-
|
1A-116
|
Ras
|
Cancer
|
|
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes .
|
-
- 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-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-134673A
-
|
UZH1a
|
Apoptosis
|
Cancer
|
|
UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1a can be used for epitranscriptomic modulation of cellular processes. UZH1a has antitumor activity. UZH1a also can be used as a chemical probe for studying METTL3.
|
-
- 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-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-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-109120
-
|
Odevixibat
A4250
|
Others
|
Metabolic Disease
|
|
Odevixibat (A4250) is a potent, selective and orally active inhibitor of the ileal bile acid transporter (IBAT). Odevixibat (A4250)decreases cholestatic liver and bile duct injury in mice model. Odevixibat (A4250) has the potential for the treatment of primary biliary cirrhosis.
|
-
- 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-17474A
-
|
Parecoxib Sodium
SC 69124A
|
COX
|
Inflammation/Immunology
Cancer
|
|
Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
|
-
- 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-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-10442
-
-
- HY-100431A
-
|
IMR-1A
|
Notch
Drug Metabolite
|
Cancer
|
|
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor 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
|
|
Infection
|
|
(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-P2265
-
|
SAH-SOS1A
|
Ras
|
|
|
SAH-SOS1A is a KRas/son of sevenless 1 (SOS1) interaction inhibitor. SAH-SOS1A binds within nucleotide binding pocket of KRas (Kd values ranges from 106 - 176 nM for wild type KRas and KRas mutants). SAH-SOS1A inhibits nucleotide binding to KRas in a concentration dependent manner.
|
-
- HY-N7613
-
-
- 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-130242
-
|
PXS-5120A
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).
|
-
- HY-B0597
-
-
- HY-103000
-
|
HSF1A
|
HSP
|
Cancer
Cardiovascular Disease
|
|
HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1). HSF1A also acts as a specific inhibitor of TRiC/CCT. Chaperonin TCP-1 ring complex (TRiC)/chaperonin containing TCP-1 (CCT) plays a pivotal role in toxin translocation and/or refolding.
|
-
- 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-N0853
-
-
- 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-N0873
-
|
Sagittatoside A
Icariin-A
|
Others
|
Others
|
|
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
|
-
- 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-114286
-
|
PXS-5153A
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5153A 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 could reduce crosslinks and ameliorates fibrosis.
|
-
- 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-B0579
-
-
- HY-16677A
-
-
- HY-N0134
-
-
- HY-15858
-
|
AP-III-a4
ENOblock
|
Enolase
|
Cancer
|
|
ENOblock(AP-III-a4) 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-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-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-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-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-N8395
-
|
Tunicamycin V
Tunicamycin A
|
Bacterial
|
Infection
|
|
Tunicamycin V (Tunicamycin A) is a nucleoside natural product that inhibits bacterial phospho-N-acetylmuramyl-pentapeptide transferase (MraY) with an IC50 of 0.35 μM. Tunicamycin V has antibacterial activties.
|
-
- 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-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-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-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-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-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-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-111388
-
|
SEL120-34A
|
CDK
|
Cancer
|
|
SEL120-34A 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-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-50877
-
-
- HY-131179
-
|
Influenza A virus-IN-1
|
Influenza Virus
|
Infection
|
|
Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
|
-
- HY-13235
-
-
- HY-122909
-
-
- HY-13470
-
-
- 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-13036C
-
|
(Rac)-IBT6A hydrochloride
|
Btk
|
Cancer
|
|
(Rac)-IBT6A hydrochloride is a racemate of IBT6A hydrochloride. 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-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-112569
-
-
- 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-N0476
-
|
Wilforlide A
Regelide; Abruslactone A
|
Others
|
Inflammation/Immunology
|
|
Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.
|
-
- 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-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-U00387
-
-
- HY-78727
-
-
- 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-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-15403
-
-
- HY-15403A
-
-
- HY-12143
-
-
- HY-12993
-
|
RSV604
A-60444
|
RSV
|
Infection
|
|
RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM).
|
-
- HY-106410A
-
|
Zabofloxacin hydrochloride
DW-224a
|
Bacterial
Topoisomerase
|
Infection
|
|
Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
|
-
- HY-13646A
-
-
- HY-13646
-
-
- 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-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-117391
-
-
- HY-112131
-
-
- HY-B0381B
-
-
- 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-131447
-
|
KY19382
A3051
|
GSK-3
|
Metabolic Disease
|
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
|
-
- HY-125741
-
|
GW768505A free base
|
VEGFR
|
Cancer
|
|
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity。
|
-
- HY-N0853A
-
-
- HY-N0875
-
-
- 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-B0492A
-
-
- HY-17448
-
-
- 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-N6732
-
|
K-252a
SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
PKC
PKA
CaMK
Trk Receptor
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
|
|
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-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-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-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-N7621
-
|
Bryonamide A
|
Others
|
Others
|
|
Bryonamide A is a natural compound isolated from red algae Bostrychia radicans (Rhodomelaceae).
|
-
- 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-100080
-
|
A-887826
|
Sodium Channel
|
Neurological Disease
|
|
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.
|
-
- HY-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-N6820
-
-
- HY-N0581
-
-
- HY-N0257
-
-
- HY-11079
-
-
- HY-P1539
-
-
- HY-N7679
-
-
- HY-N0659
-
-
- HY-113673
-
|
A-935142
|
Potassium Channel
|
Cardiovascular Disease
|
|
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
|
-
- 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-N2440
-
-
- 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
|
Infection
|
|
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-N0237
-
-
- 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-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-N1371
-
-
- HY-N6930
-
-
- HY-N0028
-
-
- 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-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-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-15568A
-
|
A-317491 sodium salt hydrate
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- 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-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-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-59201A
-
|
A-582941 dihydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
|
-
- HY-N0743
-
|
Senkyunolide A
|
Others
|
Cancer
|
|
Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
|
-
- HY-N7499
-
-
- 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-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-N2505
-
-
- HY-126252
-
|
A-9758
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
|
-
- 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-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-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-N4278
-
|
Huangjiangsu A
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Huangjiangsu A, pseudoprotodioscin, methyl protobioside, protodioscin, and protodeltonin, isolated from D. villosa.
Huangjiangsu A has hepatoprotective potential against H2O2-induced cytotoxicity and ROS generation and could be promising as potential therapeutic agents for liver diseases.
|
-
- HY-131448
-
|
A3334
|
Others
|
Metabolic Disease
|
|
A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH.
|
-
- 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-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-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-15568
-
|
A-317491
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- 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-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-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-14364
-
-
- HY-N6917
-
-
- 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-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 (hemolysis).
|
-
- 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-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-16589
-
-
- 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-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-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-104051
-
-
- HY-133246
-
-
- HY-101938
-
-
- HY-B0069
-
-
- HY-101785
-
-
- 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-B0492
-
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-131973
-
-
- HY-19487A
-
|
Ribocil B
Ribocil S enantiomer; ent-Ribocil A
|
Bacterial
|
Infection
|
|
Ribocil-B is the active S-isomer of ribocil which can inhibit flavin mononucleotide (FMN) with a KD of 6.6 nM.
|
-
- HY-111174A
-
-
- HY-102026
-
-
- HY-117319
-
-
- HY-13960
-
-
- HY-12424
-
|
Zotarolimus
ABT-578; A 179578
|
Others
|
Cancer
Cardiovascular Disease
|
|
Zotarolimus (ABT-578) is a derivative of rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis.
|
-
- HY-N1913
-
-
- HY-17590
-
-
- 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-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-18649
-
|
Galidesivir hydrochloride
BCX4430 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.
|
-
- 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-13768A
-
-
- HY-N0619A
-
|
cis-Mulberroside A
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-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-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-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-124596
-
|
CD161
NKR-P1A
|
Epigenetic Reader Domain
|
Cancer
|
|
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
|
-
- 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-15308
-
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-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-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-14261
-
-
- HY-N1724
-
-
- HY-15556A
-
-
- HY-15556
-
-
- HY-15662
-
|
Tulathromycin A
Tulathromycin; CP 472295
|
Antibiotic
Bacterial
|
Infection
|
|
Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 µM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects.
|
-
- HY-130665
-
|
TL12-186
|
PROTAC
CDK
|
Cancer
|
|
TL12-186 is a CRBN-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM).
|
-
- HY-12993B
-
|
RSV604 (R enantiomer)
A-60444 (R enantiomer)
|
RSV
|
Infection
|
|
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
|
-
- HY-112398
-
-
- HY-111098
-
-
- HY-N4146
-
-
- HY-19608
-
-
- HY-N6982
-
-
- HY-133777
-
|
Ciprofibrate impurity A
|
PPAR
|
Cancer
|
|
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha.
|
-
- 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-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-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-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.
|
-
- 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-112152
-
-
- HY-101582
-
-
- HY-101746
-
|
GSK376501A
|
PPAR
|
Metabolic Disease
|
|
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
|
-
- HY-19243
-
-
- HY-19477
-
-
- 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-N6915
-
-
- 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-124906
-
|
JAMI1001A
|
iGluR
|
Neurological Disease
|
|
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
|
-
- HY-B0519A
-
|
Tylosin
Tylosin A
|
Bacterial
Antibiotic
|
Infection
|
|
Tylosin (Tylosin A) is a macrolide antibiotic found naturally as a fermentation product of Streptomyces fradiae. Tylosin exerts potent antimicrobial activity against Gram-positive bacteria. Tylosin is widely used as a feed additive for promoting animal growth. Tylosin is used for veterinary purposes against bacterial dysentery and respiratory diseases in poultry, pigs and cattle.
|
-
- 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-14467
-
-
- HY-100672
-
-
- 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-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-N7614
-
|
Anemarrhenasaponin A2
Schidigerasaponin F2; Timosaponin AII
|
Others
|
Cardiovascular Disease
|
|
Anemarrhenasaponin A2 (Schidigerasaponin F2) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation.
|
-
- HY-N0692
-
|
Schisandrol B
Gomisin-A; TJN-101; Wuweizi alcohol-B
|
Reactive Oxygen Species
Cytochrome P450
Autophagy
|
Cancer
|
|
Schisandrol B (Gomisin-A) is a major active constituent of Schisandra sphenanthera with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities.
|
-
- 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-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-13032
-
-
- 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-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-136093
-
|
HL271
IM156 hydrochloride; HL156A hydrochloride
|
AMPK
|
Cancer
Neurological Disease
|
|
HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- 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 and orally active 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-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-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-138298
-
|
Trastuzumab deruxtecan
DS-8201; DS-8201a
|
EGFR
|
Cancer
|
|
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
|
-
- HY-P1505
-
-
- HY-P1788
-
-
- HY-B0422S
-
|
Nateglinide D5
A4166 D5; Senaglinide D5
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-101947
-
|
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.
|
-
- HY-16668
-
-
- HY-14262
-
|
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.
|
-
- 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-12993A
-
|
RSV604 racemate
A-60444 racemate
|
RSV
|
Others
|
|
RSV604 (A-60444) racemate is a racemic mixture, shows less potency against strains of respiratory syncytial virus (RSV) than the S-isomer.
|
-
- 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 (MPDL3280A) 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
-
|
Sitafloxacin hydrate
DU6859a hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Sitafloxacin (DU6859a) hydrate is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- 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-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-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-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-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-18679
-
|
TC-N 22A
|
mGluR
|
Neurological Disease
|
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-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
-
|
Sitafloxacin
DU6859a
|
Bacterial
Antibiotic
|
Infection
|
|
Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- 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.
|
-
- HY-N1118
-
-
- HY-136408
-
|
Malonyl Coenzyme A lithium
|
Others
|
Metabolic Disease
|
|
Malonyl Coenzyme A (lithium) is a coenzyme A derivative that is utilized in fatty acid and polyketide synthesis and in the transport of α-ketoglutarate across the mitochondrial membrane. Malonyl Coenzyme A (lithium) is formed by the Acetyl CoA Carboxylase-mediated carboxylation of acetyl CoA. Malonyl Coenzyme A (lithium) is exclusively used as the extender unit in the synthesis of bacterial aromatic polyketides.
|
-
- HY-B1017
-
-
- HY-N6993
-
|
25-O-Methylalisol A
|
Others
|
Metabolic Disease
|
|
25-O-Methylalisol A is a protostane triterpenoids isolated from Alisma orientale. The dried rhizomes of the aquatic plant Alisma orientale known as Rhizoma Alismatis is a common traditional Chinese medicine used for diuretic, anti-inflammatory, and hypolipidemic purposes, as well as the treatment of diabetes.
|
-
- HY-B0780
-
-
- HY-B0071A
-
-
- HY-B0723
-
|
Ospemifene
FC-1271a
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
|
-
- HY-N2220
-
-
- HY-P1594
-
-
- HY-P2318
-
|
Bac2A TFA
|
Fungal
|
|
|
Bac2A TFA is an antimicrobial and immunomodulatory peptide. Bac2A TFA is a linear variant of bactenecin and is very effective against fungal pathogens.
|
-
- HY-N1988
-
|
Cucurbitacin IIa
Hemslecin A
|
Survivin
Apoptosis
|
Cancer
|
|
Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells.
|
-
- HY-108271
-
|
Mogroside III-A1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside III-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.
|
-
- HY-B0197
-
-
- HY-103207
-
-
- HY-N2449
-
|
(±)-Licarin A
(±)-trans-Dehydrodiisoeugenol
|
Parasite
|
Infection
|
|
(±)-Licarin A ((±)-trans-Dehydrodiisoeugenol) is a dihydrobenzofuran neolignan, the resultant of an oxidative coupling reaction of isoeugenol and horseradish peroxidase (HRP) enzyme. (±)-Licarin A displays 58.7% parasite lysis and has an IC50 value of 100.8 µM for trypanocidal activity against trypomastigote forms of T. cruzi. And (±)-Licarin A shows 100% parasites mortality at 200 µM.
|
-
- HY-N2115
-
|
Araloside A
Chikusetsusaponin IV
|
Renin
|
Cardiovascular Disease
|
|
Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitory activity, with an IC50 of 77.4 μM.
|
-
- HY-B0455A
-
|
Lomefloxacin
SC47111A
|
Bacterial
Antibiotic
|
Infection
|
|
Lomefloxacin (SC47111A) is a broad-spectrum quinolone antibiotic, with antimicrobial activity. Lomefloxacin is used for the research of bronchitis, urinary tract infection, conjunctivitis, otitis externa, and otitis media.
|
-
- HY-N6694
-
-
- 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-122207
-
-
- HY-P1112
-
-
- HY-N9319
-
|
Fulvotomentoside A
Decaisoside E
|
Others
|
Others
|
|
Fulvotomentoside A (Decaisoside E) is a triterpenoid saponin compound isolated from the flowers of Lonicera fulvotomentosa Hsu et S.C. Cheng.
|
-
- HY-U00188
-
-
- HY-B0417A
-
-
- HY-13768
-
|
Topotecan
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87.
|
-
- HY-102024
-
-
- HY-12692
-
|
DO3A tert-Butyl ester
DO3A tert-butyl; DO3A-t-Bu-ester
|
Others
|
Others
|
|
DOTA tert-Butyl ester is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
|
-
- HY-P0088
-
-
- HY-100260
-
|
beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
|
HIV
|
Infection
|
|
beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.
|
-
- HY-113462
-
|
α-Carotene
|
Others
|
Cancer
|
|
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. α-Carotene is isolated from yellow-orange and dark-green vegetables.
|
-
- HY-P1505A
-
-
- HY-131615
-
|
TPC2-A1-P
|
Sodium Channel
|
Others
|
|
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-17442
-
-
- HY-103090
-
-
- HY-N0691
-
|
Schisandrin
Schizandrin; Schizandrol; Schizandrol-A
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats.
|
-
- HY-129995A
-
-
- HY-16973
-
|
Fluralaner
A1443; AH252723
|
Parasite
|
Infection
|
|
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
|
-
- HY-14111
-
-
- HY-P2230
-
|
Angstrom6
A6 Peptide
|
PAI-1
|
Cancer
|
|
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
|
-
- HY-12405
-
-
- HY-10171
-
|
NPS-2143 hydrochloride
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-10007
-
|
NPS-2143
SB-262470A
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-B0012A
-
-
- HY-P1112A
-
-
- HY-U00230
-
-
- HY-17621
-
-
- HY-10847B
-
|
SB-277011 hydrochloride
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-19555A
-
|
Seco Rapamycin sodium salt
Secorapamycin A monosodium
|
Others
|
Others
|
|
Seco Rapamycin sodium salt is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-107723
-
-
- HY-16566A
-
-
- HY-18776
-
-
- HY-18233
-
|
E1210
APX001A
|
Fungal
|
Infection
|
|
E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.
|
-
- HY-10847
-
-
- HY-15370A
-
-
- HY-N0258
-
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-101105A
-
-
- HY-131614
-
|
TPC2-A1-N
|
Calcium Channel
|
Others
|
|
TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-131152
-
-
- HY-N7401
-
-
- HY-13748
-
|
Silibinin
Silibinin A; Silymarin I
|
Autophagy
Reactive Oxygen Species
|
Cancer
|
|
Silibinin (Silibinin A), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
|
-
- HY-136269
-
-
- HY-P0236A
-
-
- HY-B0292A
-
-
- HY-101809
-
-
- HY-P1594A
-
-
- 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-N0812
-
-
- HY-103090A
-
-
- HY-12100
-
-
- HY-110258
-
|
ML334
LH601A
|
Keap1-Nrf2
|
Cancer
|
|
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
|
-
- HY-10847A
-
|
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-15644
-
|
Tyrphostin 23
Tyrphostin A23; RG-50810; AG 18
|
EGFR
|
Cancer
|
|
Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
|
-
- HY-N2481
-
|
Oroxylin A-7-O-glucuronide
Oroxyloside; Oroxylin A-7-O-β-D-glucuronide
|
Others
|
Neurological Disease
|
|
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity.
|
-
- HY-10895A
-
|
SB-334867 free base
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 free base (SB334867A free base) 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-13777
-
|
Zoledronic Acid
Zoledronate; CGP 42446; CGP42446A; ZOL 446
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
|
Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
|
-
- HY-13777A
-
|
Zoledronic acid monohydrate
Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
|
Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
|
-
- HY-N0604
-
-
- HY-107377
-
|
Benzo[a]pyrene
3,4-Benzopyrene
|
Others
|
Cancer
|
|
Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies.
|
-
- HY-14604
-
|
Xaliproden hydrochloride
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
|
-
- HY-N7087
-
|
Tulipalin A
α-Methylene butyrolactone
|
Drug Metabolite
|
|
|
Tulipalin A (α-Methylene butyrolactone) is a toxic glycoside isolated from the tulip bulbs. Tulipalin A is a causative allergen that induces Allergic contact dermatitides. Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells.
|
-
- HY-W006492
-
-
- HY-N7495
-
-
- HY-112057
-
-
- HY-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-136294
-
|
Cryptophycin 1
Cryptophycin A
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Cryptophycin 1 is a potent cytotoxic antimicrotubule agent which is isolated from Nostoc sp. Cryptophycin 1 can induce cells apoptosis, and exhibits antitumor activity and exceptional antiproliferative potency.
|
-
- HY-N2146
-
-
- 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-N0541
-
|
Pseudoginsenoside F11
Ginsenoside A1
|
Endogenous Metabolite
|
Others
|
|
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
|
-
- HY-N4088
-
-
- HY-15978
-
|
P7C3-A20
|
Others
|
Neurological Disease
|
|
P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
|
-
- HY-B0426A
-
-
- HY-B0515
-
-
- HY-100176
-
-
- HY-B0005
-
|
Toremifene citrate
Z-Toremifene citrate; NK 622; FC-1157a
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Infection
|
|
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-B0005A
-
|
Toremifene
Z-Toremifene; NK 622 free base; FC-1157a free base
|
Estrogen Receptor/ERR
|
Cancer
Infection
|
|
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-106199
-
-
- HY-124873
-
|
SERCA2a activator 1
|
Calcium Channel
|
Cardiovascular Disease
|
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
|
-
- HY-B1384
-
|
Retinyl palmitate
Vitamin A palmitate; Retinol palmitate
|
Endogenous Metabolite
|
Others
|
|
Retinyl palmitate is an ester of Retinol and is the major form of vitamin A found in the epidermis. Retinyl palmitate has been widely used in pharmaceutical and cosmetic formulations.
|
-
- HY-101915
-
-
- HY-14336A
-
|
SB 271046 Hydrochloride
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
|
-
- HY-101325
-
-
- HY-B1050
-
|
Gemifloxacin mesylate
SB-265805S; LB-20304a
|
Bacterial
|
Infection
|
|
Gemifloxacin mesylate is an oral broad-spectrum quinolone antibacterial agent, used in the treatment of acute bacterial exacerbation of chronic bronchitis, and mild-to-moderate pneumonia.
|
-
- HY-N0834
-
-
- HY-19995
-
-
- HY-131296
-
|
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
|
5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-N6686
-
|
Virginiamycin M1
Pristinamycin IIA; Ostreogrycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin IIA (RP 12536) is a macrocyclic lactone peptolide antibiotic, derived from Streptomyces pristinaespiralis, which is a member of the streptogramin A group of antibiotics.
|
-
- HY-N0855
-
|
Alisol G
Alisol-G; 25-Anhydroalisol A
|
Others
|
Others
|
|
Alisol G is a natural product extracted from Rhizoma Alismatis.
|
-
- HY-B2209A
-
|
Hydroxocobalamin monohydrochloride
Vitamin B12a monohydrochloride
|
Others
|
Metabolic Disease
|
|
Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia.
|
-
- HY-19655
-
-
- HY-N0206
-
|
Ardisiacrispin A
Deglucocyclamin; LTS-4; Saxifragifolin B
|
Others
|
Cancer
|
|
Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities.
|
-
- HY-B0976A
-
|
Fenoterol hydrobromide
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
|
-
- HY-113596
-
|
Acetyl Coenzyme A trisodium
Acetyl-CoA trisodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Acetyl Coenzyme A trisodium (Acetyl-CoA trisodium) is a central metabolic intermediate. Acetyl Coenzyme A trisodium is the actual molecule through which glycolytic pyruvate enters the tricarboxylic acid (TCA) cycle, is a key precursor of lipid synthesis, and is the sole donor of the acetyl groups for acetylation. Acetyl Coenzyme A trisodium acts as a potent allosteric activator of pyruvate carboxylase (PC).
|
-
- HY-101913
-
-
- HY-10512
-
-
- HY-136272
-
-
- HY-14778
-
-
- HY-14601
-
-
- HY-A0167
-
|
Gadopentetate dimeglumine
SH-L-451A; Gadopentetic acid dimeglumine salt
|
Others
|
Cancer
|
|
Gadopentetate dimeglumine (SH-L-451A) is used in combination with magnetic resonance imaging (MRI) to allow blood vessels, organs, and other non-bony tissues to be seen more clearly on the MRI.
|
-
- HY-U00321
-
-
- HY-B0723S
-
|
Ospemifene D4
FC-1271a D4
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
|
-
- HY-100290
-
-
- HY-N0056
-
-
- HY-136621
-
-
- HY-N0411
-
|
β-Carotene
Provitamin A; beta-Carotene
|
Endogenous Metabolite
ROS
Apoptosis
|
Cancer
Metabolic Disease
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
|
-
- HY-B0284S
-
-
- HY-136273
-
-
- HY-N0560
-
-
- HY-P0197
-
-
- HY-U00286
-
-
- HY-124874
-
|
(rel)-Asperparaline A
(rel)-Aspergillimide; (rel)-VM55598
|
nAChR
|
Neurological Disease
|
|
(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms.
|
-
- HY-B0933
-
|
Gadoteridol
SQ-32692; Gd-HP-DO3A
|
Others
|
Others
|
|
Gadoteridol is a gadolinium-based MRI contrast agent, used in the imaging of the central nervous system.
|
-
- HY-136274
-
-
- HY-15264
-
|
MC 1046
Impurity A of Calcipotriol
|
VD/VDR
|
Cancer
|
|
MC 1046(Impurity A of Calcipotriol) is an impurity of Calcipotriol; Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
|
-
- HY-B0197AS
-
-
- HY-N0510
-
|
Aristolochic acid A
Aristolochic acid I; TR 1736
|
NF-κB
|
Cancer
|
|
Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
|
-
- HY-N0045
-
-
- HY-14552A
-
-
- HY-107443
-
-
- HY-101355B
-
-
- HY-N7655
-
|
7-O-Methylbiochanin A
4',7-Dimethoxy-5-hydroxyisoflavone
|
Others
|
Others
|
|
7-O-Methylbiochanin A (4',7-Dimethoxy-5-hydroxyisoflavone) is an isoflavone derivative isolated from the roots of Lotus polyphyllos.
|
-
- HY-15459
-
-
- HY-11054
-
|
TH-237A
meso-GS 164
|
Others
|
Neurological Disease
|
|
TH-237A(meso-GS 164) is a novel neuroprotective agent exhibiting favorable permeation across the blood brain barrier.
|
-
- HY-105932
-
-
- HY-N8356A
-
|
9-cis-Vitamin A palmitate
9-cis-Retinyl palmitate
|
Endogenous Metabolite
|
Others
|
|
9-cis-Vitamin A palmitate (9-cis-Retinyl palmitate) is a 9-cis isomer formed by vitamin A palmitate in corn flakes. 9-cis-Vitamin A palmitate has a biological activity of 26% of all-trans-vitamin A palmitate, the most biologically ac-tive form of vitamin A.
|
-
- HY-12520A
-
-
- HY-N8356
-
|
13-cis-Vitamin A palmitate
13-cis-Retinyl palmitate
|
Endogenous Metabolite
|
Others
|
|
13-cis-Vitamin A palmitate (13-cis-Retinyl palmitate) is a 13-cis isomer formed by vitamin A palmitate in corn flakes. 13-cis-Vitamin A palmitate has a biological activity of 75% of all-trans-vitamin A palmitate, the most biologically ac-tive form of vitamin A.
|
-
- HY-100692
-
|
Lin28-let-7a antagonist 1
|
MicroRNA
|
Cancer
|
|
Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction.
|
-
- HY-B0277
-
-
- HY-P1031
-
-
- HY-U00130
-
-
- HY-N0410
-
-
- HY-107380A
-
|
PGlu-3-methyl-His-Pro-NH2 TFA
A-42872 TFA
|
Others
|
Endocrinology
|
|
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
|
-
- HY-125908
-
-
- HY-N5124
-
|
Meloside A
Isovitexin 2''-O-glucoside; Isovitexin 2''-O-β-D-glucoside
|
Others
|
Infection
|
|
Meloside A (Isovitexin 2''-O-glucoside) is a phenylpropanoid isolated from barley with antioxidant activity. In barley, phenylpropanoids have been described as having protective properties against excess UV-B radiation and have been linked to resistance to pathogens.
|
-
- HY-P0197A
-
-
- HY-17449
-
|
Fosbretabulin disodium
CA 4DP; CA 4P; Combretastatin A4 disodium phosphate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Fosbretabulin disodium (CA 4DP) is a tubulin destabilizing agent. Fosbretabulin disodium is the water soluble Combretastatin A4 prodrug that selectively targets endothelial cells, induces regression of nascent tumour neovessels, reduces tumour blood flow and causes central tumour necrosis.
|
-
- HY-15311
-
-
- HY-101735
-
|
(9Z,11E)-Prodlure
(9Z,11E)-Tetradecadien-1-yl acetate; Ferodin SL; Litlure A
|
Others
|
Endocrinology
|
|
(9Z,11E)-Prodlure ((9Z,11E)-Tetradecadien-1-yl acetate) is the main component of the sex pheromone of female Spodoptera littoralis.
|
-
- HY-112078
-
|
(S,R,S)-AHPC-Me
VHL ligand 2; E3 ligase Ligand 1A
|
Ligand for E3 Ligase
|
Cancer
|
|
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM.
|
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A
|
Endogenous Metabolite
|
Others
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-131344
-
|
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-136123
-
|
Tubulin inhibitor 8
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
|
Tubulin inhibitor 7
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-112851
-
-
- HY-112812
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-112722
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-101275
-
-
- HY-13278A
-
-
- HY-111370
-
|
mTOR inhibitor-2
|
mTOR
|
Cancer
|
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
|
-
- HY-119369
-
-
- HY-111412
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-130260
-
-
- HY-128703
-
-
- HY-138295
-
|
KRAS inhibitor-10
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- HY-112807
-
|
SGLT inhibitor-1
|
SGLT
|
Metabolic Disease
|
|
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-115514A
-
|
BRK inhibitor P21d hydrochloride
|
Others
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
|
-
- HY-128859
-
|
EMT inhibitor-2
|
Cytochrome P450
|
Metabolic Disease
|
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
|
-
- HY-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-128917
-
-
- HY-15182
-
-
- HY-112474
-
-
- HY-119372
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-128617
-
|
Legumain inhibitor 1
|
Others
|
Cancer
|
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
|
-
- HY-119937
-
-
- HY-15253
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-13973A
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135864
-
|
KRAS inhibitor-6
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
|
-
- HY-135866
-
|
KRAS inhibitor-8
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-135865
-
|
KRAS inhibitor-7
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-118810
-
-
- HY-B0884
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-104022
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-126328
-
|
PKC-theta inhibitor 1
|
PKC
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
|
-
- HY-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-131705
-
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-112270
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-15604A
-
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-50900
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-101791
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-P1398
-
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-10451S
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-112913
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-114309
-
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859A
-
|
Zidebactam sodium salt
WCK-5107 sodium salt
|
Bacterial
|
Infection
|
|
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-126331
-
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Infection
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-19707
-
-
- HY-112822
-
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ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-50706A
-
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Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-125997
-
|
BTK inhibitor 10
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
|
-
- HY-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-16062
-
|
ARQ 621
|
Kinesin
|
Cancer
|
|
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
|
-
- HY-119935
-
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-N8533
-
|
Sodium Camptothecin
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.
|
-
- HY-13985
-
-
- HY-12031A
-
-
- HY-U00453
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-13984
-
|
Mutant EGFR inhibitor
|
EGFR
|
Cancer
|
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-U00377
-
-
- HY-15217
-
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-119938
-
-
- HY-107994
-
-
- HY-70027A
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-128962
-
-
- HY-13278
-
-
- HY-112860
-
-
- HY-A0116S
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-124594
-
-
- HY-19731
-
-
- HY-101462
-
-
- HY-B0902A
-
|
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-101963
-
-
- HY-115213
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-112715
-
-
- HY-14165
-
-
- HY-124793A
-
|
GAK inhibitor 49 hydrochloride
|
Others
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.
|
-
- HY-19727A
-
-
- HY-129167
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-124793
-
|
GAK inhibitor 49
|
Others
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
|
-
- HY-B0879A
-
