Search Result
Results for "Anti mir ™ mirna Inhibitors" in MCE Product Catalog:
9892
Inhibitors & Agonists
16
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
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- HY-15843
-
|
MIR96-IN-1
|
MicroRNA
Apoptosis
|
Cancer
|
|
MIR96-IN-1 targets the Drosha site in the miR-96 hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively.
|
-
- HY-19731
-
-
- HY-U00439
-
-
- HY-135276
-
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Targaprimir-96
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells.
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- HY-15861
-
|
Targapremir-210
TGP-210
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targapremir-210 (TGP-210) is a potent and selective miR-210 inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM).
|
-
- HY-50751
-
|
Linifanib
ABT-869; AL-39324
|
PDGFR
VEGFR
FLT3
c-Fms
c-Kit
Autophagy
Apoptosis
|
Cancer
|
|
Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
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-
- HY-122575
-
|
Aurintricarboxylic acid
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway.Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
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- HY-126295
-
-
- HY-U00273
-
-
- 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.
|
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- HY-126131
-
|
anti-TB agent 1
|
Bacterial
|
Infection
|
|
anti-TB agent 1 is a potent and orally active anti-tuberculosis agent, with MICs of < 2 nM against the Mtb strains H37Rv, rRMP and rINH.
|
-
- HY-B0268A
-
|
Enoxacin hydrate
Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Infection
Cancer
|
|
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
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- HY-B0268
-
|
Enoxacin
AT 2266; CI 919
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Cancer
Infection
|
|
Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
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- HY-B0185A
-
|
Lidocaine hydrochloride
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative commonly used to anesthetize. hydrochloride is a a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
|
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- HY-B0185
-
|
Lidocaine
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative commonly used to anesthetize. Lidocaine is a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
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- HY-131233
-
|
Anti-virus agent 1
|
Others
|
Infection
|
|
Anti-virus agent 1 (compound 4i), a phosphoramidate prodrug of GS-5734 (HY-104077; Remdesivir), has potent antiviral activity. Anti-virus agent 1 is used for the research of coronavirus and Ebola virus (EBOV).
|
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- HY-P9917
-
|
Tocilizumab
Anti-Human IL6R, Humanized Antibody
|
Interleukin Related
|
Cancer
Inflammation/Immunology
|
|
Tocilizumab (Anti-Human IL6R, Humanized Antibody) is an anti-human interleukin-6 receptor (IL-6R) neutralizing antibody, prevents binding of IL-6 to the IL-6R, thereby inhibiting both classic and trans-signaling. Tocilizumab (Anti-Human IL6R, Humanized Antibody) can be used for the treatment of rheumatoid arthritis. Tocilizumab is remarkablely effective for the study of severe COVID-19 (coronavirus disease).
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- HY-17624
-
|
Framycetin
Neomycin B; Fradiomycin B
|
Antibiotic
Bacterial
|
Infection
|
|
Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
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- HY-U00314
-
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- HY-131005
-
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- HY-17624A
-
|
Framycetin sulfate
Neomycin B sulfate; Fradiomycin B sulfate
|
Antibiotic
Bacterial
|
Infection
|
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Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
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- HY-U00301
-
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- HY-116716
-
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PIN1 inhibitor API-1
|
MicroRNA
|
Cancer
|
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PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development.
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- HY-101729
-
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- HY-131445
-
|
RJW100
|
MicroRNA
|
Cancer
Endocrinology
|
|
RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c promoter.
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- HY-100574A
-
|
Cl-amidine hydrochloride
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Cancer
Inflammation/Immunology
|
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Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
|
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- HY-100574
-
|
Cl-amidine
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Cancer
Inflammation/Immunology
|
|
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
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- HY-121879
-
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- HY-P9909
-
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- HY-100574B
-
|
Cl-amidine TFA
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Cancer
Inflammation/Immunology
|
|
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
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- 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.
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- HY-U00439A
-
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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.
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- HY-P9801
-
|
Anti-Spike-RBD mAb
SARS-CoV-2 (2019-nCoV) Spike RBD Antibody
|
SARS-CoV
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Infection
|
|
Anti-Spike-RBD mAb is a CHO cell derived human monoclonal IgG1 antibody. Blocking the interaction of Spike protein and ACE2. Anti-Spike-RBD mAb is a potential therapeutic approach for SARS-CoV-2 treatment.
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- HY-19373
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- HY-P9803
-
|
Anti-SARS-80R mAb
SARS-80R; SARS Antibody-80R
|
SARS-CoV
|
Infection
|
|
Anti-SARS-80R mAb (SARS-80R) is a human monoclonal IgG1 antibody produced in CHO cells. Anti-SARS-80R mAb can specifically bind to Spike (S1) protein to prevent SARS virus infection of susceptible cells.
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- HY-P9806
-
|
Anti-MERS-D12 mAb
MERS-D12; MERS Antibody-D12
|
SARS-CoV
|
Infection
|
|
Anti-MERS-D12 mAb (MERS-D12; MERS Antibody-D12) is a human monoclonal IgG1. Anti-MERS-D12 mAb binds directly to the DPP4 interacting region of the MERS-CoV Spike receptor binding domain (RBD) and effect neutralization by directly blocking receptor binding.
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- HY-N3977
-
|
Grifolic acid
|
GPR120
|
Inflammation/Immunology
|
|
Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
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- 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.
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- 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.
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- HY-108730
-
-
- HY-P9805
-
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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.
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- HY-P9804
-
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Anti-MERS-2E6 mAb
MERS-2E6; MERS Antibody-2E6
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SARS-CoV
|
Infection
|
|
Anti-MERS-2E6 mAb (MERS-2E6; MERS Antibody-2E6), a human neutralizing antibody IgG1 (CHO expressed) that can compete for the binding of the virus Spike protein to the receptor (CD26), thereby inhibiting virus invasion into host cells.
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- 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.
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- 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-18728
-
-
- 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.
|
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- HY-P9906
-
|
Bevacizumab
Anti-Human VEGF, Humanized Antibody
|
VEGFR
|
Cancer
|
|
Bevacizumab, a humanized monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity.
|
-
- HY-15583
-
-
- HY-P9802
-
|
Anti-Spike-RBD Single Domain mAb
SARS-CoV-2 (2019-nCoV) Single-Domain Antibodies; Humanized Single Domain Antibody
|
SARS-CoV
|
Infection
|
|
Anti-Spike-RBD Single Domain mAb is a CHO cell derived Alpaca monoclonal VHH-huFc antibody, specifically binds to SARS-CoV-2 RBD with high affinity.
|
-
- HY-P9807
-
-
- HY-P9907
-
|
Trastuzumab
Anti-Human HER2, Humanized Antibody
|
EGFR
|
Cancer
|
|
Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
- HY-P9908
-
-
- 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-125959
-
|
Ucf-101
|
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Ucf-101 is a selctive and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
|
-
- HY-B1479C
-
-
- HY-B1479
-
-
- HY-B1479B
-
-
- HY-N0018
-
|
Daidzin
Daidzoside; NPI-031D; Daidzein 7-O-glucoside
|
Mitochondrial Metabolism
Reverse Transcriptase
|
Others
|
|
Daidzin is an isoflavone that has anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.
|
-
- HY-100618
-
-
- HY-Y1825
-
|
Benzimidazole
|
Bacterial
Fungal
Influenza Virus
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Benzimidazole is a heterocyclic aromatic organic compound and acts as an important pharmacophore in medicinal chemistry. Benzimidazole derivatives have been reported to possess various biological activities such as anti-cancer, anti-viral, anti-bacterial, anti-fungal, anti-helmintic, anti-inflammatory, proton pump inhibitor and anti-coagulant property.
|
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- HY-B1436
-
-
- HY-W013332
-
-
- HY-W013332A
-
-
- HY-N3848
-
-
- HY-N0250
-
-
- HY-N2032
-
|
Euphorbiasteroid
|
AMPK
|
Cancer
Infection
Metabolic Disease
|
|
Euphorbiasteroid is a tricyclic diperpene of Euphorbia lathyris L., inhibits tyrosinase, and increases the phosphorylation of AMPK, with anti-cancer, anti-virus, anti-obesity and multidrug resistance-modulating effect.
|
-
- HY-111621
-
|
DC661
|
Autophagy
Apoptosis
|
Cancer
|
|
DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
|
-
- HY-117737A
-
|
RRD-251
|
Raf
Apoptosis
|
Cancer
|
|
RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.
|
-
- HY-P1009
-
|
Z-YVAD-FMK
|
Caspase
|
Cancer
|
|
AA-Z-YVAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor with anti-inflammatory and anti-tumor activities.
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-
- HY-B0289
-
-
- HY-N0720
-
|
Neobavaisoflavone
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.
|
-
- HY-N2127
-
|
Pinostrobin
|
Ser/Thr Protease
|
Inflammation/Immunology
|
|
Pinostrobin is a flavonoid can be found in many plants, and has anti-oxidant, anti-inflammatory, anti-cancer and neuroprotective properties. Pinostrobin is a potent PCSK9 inhibitor and inhibits the catalytic activity of PCSK9. Pinostrobin is a promising agent for cholesterol regulation and lipid management.
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- HY-N0184A
-
-
- HY-N0472
-
-
- HY-N0400
-
-
- HY-100350
-
-
- HY-P9911
-
|
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
|
|
Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- HY-10529
-
-
- HY-14934
-
-
- HY-N0773
-
|
Isovitexin
Saponaretin; Homovitexin
|
JNK
NF-κB
|
Inflammation/Immunology
|
|
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-10249A
-
-
- HY-107454
-
|
OSS_128167
|
Sirtuin
HBV
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
OSS_128167 is a potent selective sirtuin 6 (SIRT6) inhibitor with IC50s of 89 μM, 1578 μM and 751 μM for SIRT6, SIRT1 and SIRT2, respectively. OSS_128167 has anti-HBV activity that inhibits HBV transcription and replication. OSS_128167 has anti-acncer, anti-inflammation and anti-viral effects.
|
-
- HY-N6258
-
|
Kahweol
|
AMPK
Apoptosis
|
Metabolic Disease
|
|
Kahweol is one of the consituents of the coffee from Coffea Arabica with anti-inflammatory anti-angiogenic, and anti-cancerous activities. Kahweol inhibits adipogenesis and increase glucose uptake by AMP-activated protein kinase (AMPK) activation. Kahweol induces apoptosis.
|
-
- HY-Y0892
-
-
- HY-N2192
-
-
- HY-136718
-
|
CLEFMA
|
Apoptosis
|
Cancer
|
|
CLEFMA is a curcuminoid with antitumor activity. CLEFMA inhibits tumor growth is associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.
|
-
- HY-119369
-
-
- HY-13025
-
-
- HY-12511
-
|
SKF-86002
|
p38 MAPK
|
Inflammation/Immunology
|
|
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
|
-
- HY-N1377
-
|
Nevadensin
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive.
|
-
- HY-17361
-
|
Etofenamate
|
Others
|
Inflammation/Immunology
|
|
Etofenamate, a non-steroid anti-inflammatory drug (NSAID) and a non-selective COX inhibitor, possesses analgesic, anti-rheumatic, antipyretic and anti-inflammatory properties. Etofenamate is used in the research for osteoarthritis, arthritis and other inflammatory diseases.
|
-
- HY-N0790
-
|
Lupeol
Clerodol; Monogynol B; Fagarasterol
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC).
|
-
- HY-N4116
-
|
Xanthyletin
|
Fungal
|
Cancer
Infection
|
|
Xanthyletin is a coumarin isolated from Citrus, with anti-tumor and anti-bacterial activities. Xanthyletin also inhibits symbiotic fungus cultivated by leaf-cutting ants.
|
-
- HY-N0575
-
-
- HY-117260
-
-
- HY-N2000
-
|
Bellidifolin
|
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Bellidifolin is a xanthone isolated from the stems of Swertia punicea, with hepatoprotective, hypoglycemic, anti-oxidation, anti-inflammatory and antitumor activities. Bellidifolin also acts as a viral protein R (Vpr) inhibitor.
|
-
- HY-N6884
-
-
- HY-W013478
-
-
- HY-13727
-
-
- HY-14812
-
-
- HY-B0483
-
-
- HY-N0714A
-
-
- HY-N5077
-
|
Sinapine
|
AChE
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-N0889
-
|
Ginkgetin
|
Wnt
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC50 of 5.92 μΜ.
|
-
- HY-N6714
-
|
Alternariol
|
Topoisomerase
|
Cancer
Infection
|
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
|
-
- HY-N7015
-
|
Zerumbone
|
HSV
|
Infection
|
|
Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity.
|
-
- HY-N0004
-
|
Oridonin
NSC-250682; Isodonol
|
Akt
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.
|
-
- HY-N0804
-
|
Narirutin
|
Bacterial
|
Inflammation/Immunology
|
|
Narirutin, one of the active constituents isolated from Citrus unshiu, has antioxidant and anti-inflammatory activities. Narirutin is a shikimate kinase inhibitor with anti-tubercular potency.
|
-
- 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-32736
-
|
Triptonide
NSC 165677; PG 492
|
Wnt
β-catenin
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Triptonide (NSC 165677; PG 492) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.
|
-
- HY-114335
-
|
Triphala
|
NF-κB
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Triphala, an Ayurvedic polyherbal formulation comprising of equiproportional fruit parts of Terminalia chebula, Terminalia bellerica, and Phyllanthus emblica. Triphala inhibits NF-κB activation. Triphala exerts antifungal action. Anti-adipogenic, anti-inflammatory, and anti-neoplastic activities.
|
-
- HY-N0108
-
|
Physcion
Parietin; Rheochrysidin
|
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
|
-
- HY-N5077B
-
|
Sinapine hydroxide
|
AChE
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-N0450
-
|
Sinapine thiocyanate
|
P-glycoprotein
AChE
|
Cancer
|
|
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-15721
-
-
- HY-103672
-
-
- HY-U00406
-
-
- HY-13727A
-
-
- HY-B0811
-
-
- HY-W015007
-
|
Metyrosine
|
COX
|
Cardiovascular Disease
|
|
Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
|
-
- HY-N0484
-
|
Liensinine
|
Autophagy
Mitophagy
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
|
-
- HY-16278
-
|
Pradigastat
LCQ-908
|
Acyltransferase
|
Metabolic Disease
|
|
Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.
|
-
- HY-N6849
-
|
InteriotherinA
|
HIV
|
Infection
Metabolic Disease
|
|
Interiotherin A is a lignan with a dibenzocyclooctadiene skeleton isolated from Kadsura interior. Interiotherin A inhibits HIV replication to exhibit anti-HIV activity, it has a role as a metabolite and an anti-HIV agent.
|
-
- 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-115550
-
-
- HY-U00345
-
-
- HY-B0105A
-
-
- HY-17484
-
-
- HY-N5011
-
|
5,7-Dimethoxyflavone
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor.
|
-
- HY-W009156
-
-
- HY-16126
-
-
- HY-101655
-
|
COX-2-IN-2
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.
|
-
- HY-104075
-
|
R916562
|
TAM Receptor
VEGFR
|
Cancer
|
|
R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis.
|
-
- HY-N0346A
-
-
- HY-B0482
-
|
Acemetacin
TVX 1322
|
COX
|
Inflammation/Immunology
|
|
Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
|
-
- HY-14586
-
|
Irosustat
STX64; BN83495; 667-Coumate
|
Others
|
Cancer
|
|
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
|
-
- HY-P0052A
-
-
- HY-14947
-
|
Balamapimod
MKI 833
|
MEK
|
Cancer
|
|
Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
|
-
- HY-12053A
-
-
- HY-14857
-
-
- HY-U00048
-
-
- HY-108986
-
-
- HY-B0386
-
-
- HY-12053
-
-
- 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-117319
-
-
- HY-N6894
-
|
Pseudocoptisine acetate
Isocoptisine acetate
|
AChE
|
Inflammation/Immunology
|
|
Pseudocoptisine (Isocoptisine) acetate is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine acetate inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects.
|
-
- HY-N4288
-
-
- HY-N6894A
-
|
Pseudocoptisine chloride
Isocoptisine chloride
|
AChE
|
Inflammation/Immunology
|
|
Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and anti-amnestic effects.
|
-
- HY-N2597
-
-
- HY-102007
-
|
Gamitrinib TPP
|
HSP
|
Cancer
|
|
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-13737
-
|
R1530
|
VEGFR
FGFR
Apoptosis
|
Cancer
|
|
R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with Kds of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC50s of 10 nM and 28 nM, respectively.
|
-
- HY-N6656
-
-
- HY-13077
-
-
- HY-106579
-
|
Tiaprofenic acid
|
COX
|
Inflammation/Immunology
|
|
Tiaprofenic acid is an orally active nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory and analgesic potency. Tiaprofenic acid inhibits prostaglandin synthesis by suppressing cyclo-oxygenase (COX). Tiaprofenic acid can be used in the treatment of rheumatic diseases.
|
-
- HY-P2470
-
-
- HY-111783
-
-
- HY-19556
-
-
- HY-B0481
-
|
Miglitol
BAY1099; BAY-m1099
|
Others
|
Metabolic Disease
|
|
Miglitol is an oral anti-diabetic drug that acts by inhibiting the ability of the patient to breakdown complex carbohydrates into glucose.
|
-
- HY-109018
-
-
- HY-103128
-
-
- HY-105028
-
|
Tenidap
CP-66248
|
COX
|
Inflammation/Immunology
|
|
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
|
-
- HY-N2302
-
-
- HY-N0192
-
|
Arbutin
β-Arbutin
|
Tyrosinase
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
|
-
- HY-B0715
-
|
Pentoxifylline
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
|
-
- HY-N0126
-
-
- HY-13696
-
-
- HY-17485
-
|
Alminoprofen
EB-382
|
Phospholipase
COX
|
Inflammation/Immunology
|
|
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2.
|
-
- HY-N4187
-
-
- 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-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-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-128580
-
|
FAK inhibitor 2
|
FAK
|
Cancer
|
|
FAK inhibitor 2 is a potent focal adhesion kinase (FAK) inhibitor with an IC50 of 0.07 nM, with antitumor and anti-angiogenesis activities.
|
-
- HY-N7089
-
|
Benzoyleneurea
|
Bacterial
|
Infection
|
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-102007A
-
|
Gamitrinib TPP hexafluorophosphate
|
HSP
|
Cancer
|
|
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-W016586
-
|
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-111950
-
|
(-)-Ibuprofenamide
(R)-Ibuprofenamide
|
Others
|
Inflammation/Immunology
|
|
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
|
-
- HY-W016586A
-
|
Acivicin hydrochloride
AT-125 hydrochloride; U-42126 hydrochloride
|
Parasite
|
Cancer
Infection
|
|
Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N0439
-
-
- HY-B0494
-
-
- HY-109056
-
|
Elsulfavirine
|
HIV
|
Infection
|
|
Elsulfavirine is a reverse transcriptase inhibitors for HIV-1 infection and is a new anti-HIV drug.
|
-
- HY-121632
-
|
Quinoclamine
|
NF-κB
|
Cancer
|
|
Quinoclamine, a naphthoquinone derivative, is a NF-κB inhibitor. Quinoclamine exhibits anti-cancer activity.
|
-
- HY-12559
-
|
Alisporivir
Debio-025; DEB-025
|
HCV
|
Infection
|
|
Alisporivir (Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-17509
-
-
- HY-16125
-
|
Carboxyamidotriazole Orotate
L-651582 Orotate; CAI Orotate
|
Calcium Channel
|
Cancer
Inflammation/Immunology
|
|
Carboxyamidotriazole Orotate (L-651582 Orotate) is the orotate salt form of Carboxyamidotriazole (CAI), an orally bioavailable signal transduction inhibitor. Carboxyamidotriazole Orotate is a cytostatic inhibitor of nonvoltage-operated calcium channels and calcium channel-mediated signaling pathways. Carboxyamidotriazole Orotate shows anti-tumor, anti-inflammatory and antiangiogenic effects.
|
-
- 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-N0232
-
|
Psoralidin
|
COX
Lipoxygenase
Notch
Reactive Oxygen Species
Bacterial
|
Cancer
|
|
Psoralidin, isolated from the seed of Psoralea corylifolia, is a dual inhibitor of COX-2 and 5-LOX, regulates ionizing radiation (IR)-induced pulmonary inflammation.Anti-cancer, anti-bacterial, and anti-inflammatory properties. Psoralidin significantly downregulates NOTCH1 signaling. Psoralidin also greatly induces ROS generation.
|
-
- HY-N3187
-
-
- HY-N0570
-
-
- HY-N1581
-
|
Quassin
Nigakilactone D
|
Parasite
|
Infection
Endocrinology
|
|
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity.
|
-
- HY-N0589
-
-
- HY-16172
-
|
DMAPT
Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
|
DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
|
-
- HY-135408
-
-
- HY-138247
-
-
- HY-B0212
-
|
Sulfapyridine
|
Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Sulfapyridine, a major metabolite of Sulfasalazine, is a sulfonamide antibiotic agent. Sulfapyridine inhibits recombinant P. carinii dihydropteroate synthetase (DHPS) with an IC50 of 0.18 μM. Sulfapyridine has antibacterial, anti-inflammatory and anti-rheumatic activities.
|
-
- HY-112712
-
|
Cyclophilin inhibitor 1
|
HCV
|
Infection
|
|
Cyclophilin inhibitor 1 is a potent and orally bioavailable cyclophilin A inhibitor, with a Kd of 5 nM, shows effective anti-HCV activity, with an EC50 of 98 nM for HCV 2a.
|
-
- HY-126482
-
|
Telomerase-IN-2
|
Telomerase
|
Cancer
|
|
Telomerase-IN-2 is a telomerase inhibitor, and inhibits telomerase activity by decreasing expression of dyskerin, with an IC50 of 0.89 µM. Anti-cancer activity.
|
-
- HY-N5015
-
|
Rosmanol
|
Others
|
Inflammation/Immunology
Cancer
|
|
Rosmanol could inhibit the oxidation of low density lipoprotein (LPL) and significantly inhibit lipopolysaccharide induced iNOS and COX-2 expression, with anti-inflammatory effect.
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-N6980
-
|
Licorice glycoside C2
|
Others
|
Cancer
Infection
|
|
Licorice glycoside C2 is a oleanane-type triterpene oligoglycoside isolated from Glycyrrhiza uralensis. Various biological activities are associated with licorice extracts, such as anti-viral, anti-microbial, antioxidant, anti-inflammatory, anti-ulcer, anti-cancer and anti-HIV effects.
|
-
- HY-N0820
-
-
- HY-14621
-
|
Zingerone
Vanillylacetone; Gingerone
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antilipolytic, antidiarrhoeic, antispasmodic and anti-tumor properties. Zingerone alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways. Zingerone acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.
|
-
- HY-N6722
-
-
- HY-13075
-
-
- HY-N1089
-
-
- HY-14398
-
-
- HY-B0105
-
-
- HY-B0367
-
-
- HY-101481
-
-
- HY-P0052
-
-
- HY-17629
-
-
- HY-Y0189
-
|
Methyl Salicylate
Wintergreen oil
|
COX
|
Inflammation/Immunology
|
|
Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
|
-
- HY-B0578
-
|
Loxoprofen
|
COX
|
Inflammation/Immunology
|
|
Loxoprofen is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
|
-
- HY-B0578A
-
|
Loxoprofen sodium
|
COX
|
Inflammation/Immunology
|
|
Loxoprofen sodium is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
|
-
- HY-N0452
-
-
- HY-108966
-
|
Kushenol C
|
Beta-secretase
|
Inflammation/Immunology
|
|
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
|
-
- HY-15273
-
-
- HY-N4233
-
|
Bisabolangelone
|
p38 MAPK
|
Inflammation/Immunology
|
|
Bisabolangelone, a sesquiterpene derivative, is isolated from the roots of Osterici Radix. Bisabolangelone possesses anti-inflammatory properties, which inhibits LPS-stimulated inflammation through the blocking of NF-kappaB and MAPK pathways in macrophages. Bisabolangelone has anti-ulcer activities.
|
-
- HY-N1934
-
-
- HY-N0211
-
|
Cyasterone
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
|
-
- HY-N0327
-
|
Lobetyolin
|
Apoptosis
Xanthine Oxidase
|
Metabolic Disease
|
|
Lobetyolin, a bioactive compound, is derived from Codonopsis pilosula. Lobetyolin has anti-inflammatory, anti-oxidative and xanthine oxidase inhibiting activities. Lobetyolin also induces the apoptosis via the inhibition of ASCT2-mediated glutamine metabolism.
|
-
- HY-N7255
-
|
Cycloartenol
|
p38 MAPK
Apoptosis
|
Cancer
|
|
Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development.
|
-
- HY-N0485
-
|
Liensinine Diperchlorate
|
Autophagy
Mitophagy
|
Cardiovascular Disease
|
|
Liensinine Diperchlorate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlorate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlorate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
|
-
- HY-113951
-
-
- HY-101566A
-
|
Elimusertib hydrochloride
BAY 1895344 hydrochloride
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY 1895344) hydrochloride is a potent, orally available and selective ATR inhibitor, with IC50 of 7 nM. Anti-tumor activity.
|
-
- HY-N0516
-
|
Casticin
Vitexicarpin
|
STAT
|
Inflammation/Immunology
|
|
Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-N2263
-
|
Skimmin
Umbelliferone glucoside
|
Others
|
Inflammation/Immunology
|
|
Skimmin (Umbelliferone glucoside) is a coumarin found in Hydrangea paniculata, inhibits immune complex deposition, with anti-inflammatory activity.
|
-
- HY-B1153A
-
-
- HY-100495
-
-
- HY-N2401
-
-
- HY-109082
-
-
- HY-P1034
-
|
DAPTA
D-Ala-peptide T-amide; Adaptavir
|
CCR
HIV
|
Infection
Endocrinology
|
|
DAPTA is a synthetic peptide, functions as a viral entry inhibitor by targeting selectively CCR5, and shows potent anti-HIV activities.
|
-
- HY-U00022
-
-
- HY-N1405
-
|
Cucurbitacin I
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-13755
-
|
Sulforaphane
|
HDAC
Keap1-Nrf2
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
|
-
- HY-14904A
-
|
Umifenovir hydrochloride
|
Influenza Virus
SARS-CoV
|
Infection
|
|
Umifenovir hydrochloride is a potent, orally active broad-spectrum antiviral with activity against a number of enveloped and non-enveloped viruses. Umifenovir hydrochloride is used as an anti-influenza virus agent. Umifenovir hydrochloride could effectively inhibit the fusion of virus with host cells. Umifenovir hydrochloride is an efficient inhibitor of SARS-CoV-2 in vitro. Anti-inflammatory activity.
|
-
- HY-N6641
-
|
Monascin
|
Others
|
Cancer
Inflammation/Immunology
|
|
Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor).
|
-
- HY-14818A
-
|
Laninamivir octanoate
CS-8958
|
Influenza Virus
|
Infection
|
|
Laninamivir octanoate (CS-8958), a prodrug of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses.
|
-
- HY-126331
-
-
- HY-N2393
-
-
- HY-114454
-
|
INH14
|
IKK
|
Cancer
Inflammation/Immunology
|
|
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
|
-
- HY-128463
-
-
- HY-N0261
-
|
Aurantio-obtusin
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Aurantio-obtusin is an anthraquinone isolated from Semen Cassiae, with anti-Inflammatory, anti-oxidative, anti-coagulating and anti-hypertension activities. Aurantio-obtusin relaxes systemic arteries through endothelial PI3K/AKT/eNOS-dependent signaling pathway in rats, thus acts as a new potential vasodilator. Aurantio-obtusin inhibits allergic responses in IgE-mediated mast cells and anaphylactic models and is potential for treatment for allergy-related diseases.
|
-
- HY-N7031
-
|
(±)-Vasicine
(±)-Peganine
|
Proton Pump
|
Inflammation/Immunology
|
|
(±)-Vasicine is the racemate of Vasicine. Vasicine (Peganine), isolated from Peganum harmala seeds, significantly inhibits H +-K +-ATPase activity in vitro with an IC50 of 73.47 μg/mL. Anti-ulcer activity. Vasicine shows significant anti-secretory, antioxidant and cytoprotective effect.
|
-
- HY-B1464
-
|
Cetylpyridinium chloride
|
Bacterial
HBV
|
Infection
Inflammation/Immunology
|
|
Cetylpyridinium chloride, a cationic quaternary ammonium compound, is an anti-bacterial agent with broad-spectrum activity. Cetylpyridinium chloride is an effective anti-HBV capsid assembly inhibitor with an IC50 of 2.5 μM. Cetylpyridinium chloride is used in pesticides and various types of mouthwashes, and other personal care products.
|
-
- HY-N2555
-
-
- HY-N0102
-
-
- HY-17592
-
|
Bithionol
|
Parasite
|
Cancer
|
|
Bithionol is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.
|
-
- HY-N6928
-
-
- HY-N7036
-
-
- HY-100039
-
|
YYA-021
|
HIV
|
Infection
|
|
YYA-021 is a small-molecule CD4 mimic that inhibits HIV entry, with high anti-HIV activity and low cytotoxicity.
|
-
- HY-N2415
-
|
Podophyllotoxone
|
Microtubule/Tubulin
|
Cancer
|
|
Podophyllotoxone is isolated from the roots of Dysosma versipellis and has anti-cancer activities.Podophyllotoxone is able to inhibit the tubulin polymerization.
|
-
- HY-128576
-
|
DS21360717
|
Others
|
Cancer
|
|
DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
|
-
- HY-103096
-
|
R162
|
Others
|
Cancer
|
|
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
|
-
- HY-135848
-
-
- HY-135658
-
-
- HY-N2224
-
|
Guaijaverin
|
Bacterial
|
Infection
|
|
Guaijaverin is a urease inhibitor with an IC50 of 120 μM. Guaijaverin shows antioxidant and anti-Streptococcus mutans activities.
|
-
- HY-Y0078
-
-
- HY-B0738
-
|
Dithranol
Anthralin
|
Others
|
Inflammation/Immunology
|
|
Dithranol (Anthralin) is an anthraquinone derivative, with potent anti-psoriatic effects. Dithranol can inhibit DNA replication and repair.
|
-
- HY-17390
-
-
- HY-101566
-
|
Elimusertib
BAY 1895344
|
ATM/ATR
|
Cancer
|
|
Elimusertib (BAY-1895344) is a potent, orally available and selective ATR inhibitor with an IC50 of 7 nM. Anti-tumor activity.
|
-
- HY-A0273
-
|
Propyphenazone
4-IsopropylAntipyrine; Isopropylphenazone
|
COX
|
Inflammation/Immunology
|
|
Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity, Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
|
-
- HY-17390A
-
-
- HY-78131B
-
-
- HY-17002
-
|
Suplatast (Tosilate)
IPD 1151T
|
Interleukin Related
|
Inflammation/Immunology
|
|
Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.
|
-
- HY-17507
-
|
Pantoprazole
BY1023; SKF96022
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-17507B
-
|
Pantoprazole sodium hydrate
BY1023 sodium hydrate; SKF96022 sodium hydrate
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-17507A
-
|
Pantoprazole sodium
BY1023 sodium; SKF96022 sodium
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-N0923
-
|
Corydaline
(+)-Corydaline; Corydalin
|
AChE
Enterovirus
Opioid Receptor
|
Neurological Disease
|
|
Corydaline ((+)-Corydaline), an isoquinoline alkaloid isolated from Corydalis yanhusuo, is an AChE inhibitor with an IC50 of 226 µM. Corydaline is a μ-opioid receptor (Ki of 1.23 µM) agonist and inhibits enterovirus 71 (EV71) replication (IC50 of 25.23 µM). Corydaline has anti-angiogenic, anti-allergic and gastric-emptying and antinociceptive activities.
|
-
- HY-18716
-
-
- 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-N0393
-
|
Glabridin
|
PPAR
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
|
-
- HY-N0328
-
-
- HY-N0448
-
|
10-Gingerol
|
Others
|
Cancer
Inflammation/Immunology
|
|
10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM.
|
-
- HY-14658
-
-
- HY-128587
-
|
Mevociclib
SY-1365
|
CDK
|
Cancer
|
|
Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors.
|
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
|
-
- HY-B0729
-
|
Polaprezinc
Zinc L-carnosine
|
Others
|
Inflammation/Immunology
|
|
Polaprezinc is an orally bioavailable chelate composed of zinc and L-carnosine, with potential gastroprotective, anti-oxidant, anti-ulcer and anti-inflammatory activities.
|
-
- HY-N0055
-
|
Chlorogenic acid
3-O-Caffeoylquinic acid; Heriguard; NSC-407296
|
HIF/HIF Prolyl-Hydroxylase
Reactive Oxygen Species
Bacterial
Influenza Virus
Endogenous Metabolite
|
Cancer
Infection
Inflammation/Immunology
|
|
Chlorogenic acid is a major phenolic compound in coffee and tea. It plays several important and therapeutic roles such as antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial, anti-hypertension.
|
-
- HY-17393
-
-
- HY-115604
-
|
Pitstop 2
|
Apoptosis
|
Cancer
|
|
Pitstop 2 is a clathrin inhibitor which inhibits clathrin-mediated endocytosis (CME) by associating with the terminal domain of clathrin. Pitstop 2 has the potential for anti-cancer research.
|
-
- HY-100437
-
|
HA15
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
HA15 is a potent and specific inhibitor of ER chaperone BiP/GRP78/HSPA5, inhibits the ATPase activity of BiP, with anti-cancerous activity.
|
-
- HY-N0862
-
-
- HY-32735
-
|
Triptolide
PG490
|
NF-κB
Apoptosis
|
Cancer
|
|
Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory and antiproliferative effects. Triptolide is a NF-κB activation inhibitor.
|
-
- HY-76251
-
-
- HY-16265
-
-
- HY-P1728A
-
-
- HY-19217
-
-
- HY-N0783
-
-
- HY-N4226
-
|
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid
|
Others
|
Inflammation/Immunology
Cancer
|
|
1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid is from Cordyceps bassiana, which is one of Cordyceps species with anti-oxidative, anti-cancer, anti-inflammatory, anti-diabetic, anti-obesity, anti-angiogenic, and anti-nociceptive activities. 1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid targets to block AP-1-mediated luciferase activity, implying it has an anti-inflammatory function.
|
-
- HY-107794
-
|
Clodronate disodium tetrahydrate
Disodium clodronate tetrahydrate
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain.
|
-
- HY-N1390
-
|
Syringaldehyde
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
|
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL. Anti-hyperglycemic and anti-inflammatory activities.
|
-
- HY-B0628B
-
|
Vinflunine ditartrate
|
Microtubule/Tubulin
|
Cancer
|
|
Vinflunine ditartrate is the first fluorinated microtubule inhibitor belonging to the Vinca alkaloids family. Vinflunine ditartrate has anti-angiogenic, vascular-disrupting and anti-metastatic activities. Vinflunine ditartrate can be used for the research of transitional cell carcinoma of the urothelial tract, non-small cell lung cancer, and carcinoma of the breast.
|
-
- HY-N1416
-
|
Pogostone
|
Bacterial
Apoptosis
Autophagy
|
Infection
Inflammation/Immunology
|
|
Pogostone is isolated from patchouli with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy.
|
-
- HY-N0103A
-
|
Sophocarpine monohydrate
|
Autophagy
Apoptosis
PI3K
Akt
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
|
-
- HY-N0103
-
|
Sophocarpine
|
Autophagy
Apoptosis
PI3K
Akt
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer.
|
-
- HY-N0408
-
|
Picroside II
|
NF-κB
Reactive Oxygen Species
Apoptosis
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
|
Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities.
picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways.
Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities.
|
-
- 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-105008
-
|
Secoisolariciresinol diglucoside
(S,S)-SDG; (S,S)-LGM2605
|
Others
|
Inflammation/Immunology
Neurological Disease
Cardiovascular Disease
|
|
Secoisolariciresinol diglucoside ((S,S)-SDG), the main lignan in wholegrain flaxseed, is known for its beneficial effects including anti-inflammatory, antioxidant, anti-mutagenic, anti-microbial, anti-obesity, hypolipidemic, and neuroprotective effects.
|
-
- HY-124858
-
|
SC99
|
STAT
JAK
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities.
|
-
- HY-B0335
-
|
Tolfenamic Acid
GEA 6414
|
COX
|
Inflammation/Immunology
Cancer
|
|
Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
|
-
- HY-N0389
-
|
Columbin
|
COX
Parasite
|
Inflammation/Immunology
|
|
Columbin is an orally active diterpenoid furanolactone from Calumbae radix, has anti-inflammatory and anti-trypanosomal effects. Columbin selectively inhibits COX-2 (EC50=53.1 μM) over COX-1 (EC50=327 μM).
|
-
- 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-19727A
-
-
- 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-17431
-
|
Fosamprenavir Calcium Salt
GW433908G
|
HIV
|
Infection
|
|
Fosamprenavir Calcium Salt (GW433908G) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
|
-
- HY-101570
-
|
Nedisertib
M3814
|
DNA-PK
|
Cancer
|
|
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity.
|
-
- HY-126330
-
|
SS-208
|
HDAC
|
Cancer
|
|
SS-208 is a selective HDAC6 inhibitor, with an IC50 of 12 nM. SS-208 possesses anti-tumor activity in melanoma.
|
-
- HY-135301
-
-
- HY-N2077
-
-
- HY-78726
-
|
Fosamprenavir
Amprenavir phosphate; GW 433908
|
HIV
|
Infection
|
|
Fosamprenavir (Amprenavir phosphate;GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, with improved solubility. Anti-HIV infection.
|
-
- HY-N0708
-
-
- HY-13065
-
|
Isobavachalcone
Corylifolinin; Isobacachalcone
|
Akt
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
|
|
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
|
-
- HY-123503
-
|
Salicortin
|
JNK
NF-κB
|
Inflammation/Immunology
Neurological Disease
|
|
Salicortin, a phenolic glycoside, has been isolated from many plants such as Populus and Salix species. Salicortin inhibits osteoclast differentiation and bone resorption by down-regulating JNK and NF-κB/NFATc1 signaling pathways. Salicortin has anti-amnesic, anti-adipogenic, and immune-modulatory activity.
|
-
- HY-N0162
-
|
Luteolin
Luteoline; Luteolol; Digitoflavone
|
Keap1-Nrf2
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
|
Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
|
-
- HY-135646
-
|
Eleutheroside B1
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities.
|
-
- HY-N0519
-
|
Calycosin
Cyclosin
|
Apoptosis
|
Cancer
|
|
Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.
|
-
- HY-N0741A
-
-
- HY-N0741
-
-
- HY-101737
-
-
- HY-123601
-
|
DHQZ 36
|
Parasite
|
Infection
|
|
DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity.
|
-
- HY-N2590
-
|
Lupenone
|
Others
|
Cancer
Infection
Inflammation/Immunology
|
|
Lupenone, isolated from Rhizoma Musae, belongs to lupane type triterpenoids. Lupenone shows various pharmacological activities including anti-inflammatory, anti-virus, anti-diabetes, anti-cancer, improving Chagas disease without major toxicity.
|
-
- HY-N0013
-
-
- HY-107470
-
-
- HY-15995
-
-
- HY-N0344
-
-
- HY-B0195
-
-
- 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-B0195A
-
-
- HY-118284
-
|
Vicagrel
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Vicagrel, an acetate derivative of Clopidogrel, is a P2Y12 platelet inhibitor potentially for the treatment of thrombosis, the substrate of carboxylesterase 2 (CES2). Vicagrel demonstrates a favorable safety profile and excellent anti-platelet activity, which could be an anti-platelet drug and for the unmet medical needs of cardiovascular diseases.
|
-
- HY-B0559
-
|
Nabumetone
BRL14777
|
COX
|
Inflammation/Immunology
Cancer
|
|
Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
|
-
- HY-N7630
-
-
- HY-17592A
-
|
Bithionol sulfoxide
|
Parasite
|
Cancer
|
|
Bithionol sulfoxide(Bitin-S) is a clinically approved anti-parasitic drug; has been shown to inhibit solid tumor growth in several preclinical cancer models.
|
-
- HY-17435
-
|
4'-Demethylepipodophyllotoxin
4'-O-demethylepipodophyllotoxin; 4'-DMEP
|
Microtubule/Tubulin
|
Cancer
|
|
4'-Demethylepipodophyllotoxin(4'-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.
|
-
- HY-111578
-
|
BDP-13176
|
Others
|
Cancer
|
|
BDP-13176 is a potent fascin 1 inhibitor, with a Kd of 90 nM and an IC50 of 240 nM. BDP-13176 has potential as an anti-metastatic agent.
|
-
- HY-N0021
-
-
- HY-N0181
-
-
- HY-117843
-
-
- HY-133019
-
-
- HY-N0551
-
|
Wedelolactone
|
Caspase
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
|
-
- HY-14645
-
|
(-)-DHMEQ
Dehydroxymethylepoxyquinomicin
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
(-)-DHMEQ (Dehydroxymethylepoxyquinomicin) is a potent, selective and irreversible NF-κB inhibitor that covalently binds to a cysteine residue. (-)-DHMEQ inhibits nuclear translocation of NF-κB and shows anti-inflammatory and anticancer activity.
|
-
- HY-N1425
-
|
Tiliroside
|
Others
|
Metabolic Disease
|
|
Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2 μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract.
|
-
- HY-103261
-
|
SCH28080
|
Proton Pump
|
Endocrinology
|
|
SCH28080 is a reversible, K +-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity.
|
-
- HY-N0828
-
|
Pterostilbene
|
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium. Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties. Pterostilbene blocks ROS production, also exhibits inhibitory activity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide.
|
-
- HY-N2542
-
-
- HY-N7044
-
-
- HY-N0007
-
|
Bisdemethoxycurcumin
Curcumin III; Didemethoxycurcumin
|
Apoptosis
Autophagy
|
Cancer
|
|
Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
|
-
- HY-B1215
-
-
- HY-B1048
-
|
Pasiniazid
Paraniazide; Pasiniazide; Isonicotinic acid hydrazide p-aminosalicylate
|
Others
|
Inflammation/Immunology
|
|
Pasiniazid is an anti-TB and anti-leprosy drug, used to treat various types of TB and leprosy.
|
-
- HY-19727
-
-
- HY-100734
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-136203
-
-
- HY-N0334
-
|
(+)-Magnoflorine
Magnoflorine; α-Magnoflorine; Thalictrine
|
Fungal
|
Infection
Metabolic Disease
|
|
(+)-Magnoflorine (Magnoflorine), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. (+)-Magnoflorine has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-N0535
-
|
(+)-Magnoflorine chloride
Magnoflorine chloride; α-Magnoflorine chloride; Thalictrine chloride
|
Fungal
|
Infection
Metabolic Disease
|
|
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-136204
-
-
- HY-B2114
-
|
Escin
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Escin, a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.
|
-
- HY-B0580
-
|
Ketorolac
RS37619
|
COX
|
Inflammation/Immunology
|
|
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-138558
-
-
- HY-124632
-
|
WJ460
|
Others
|
Cancer
|
|
WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF and exerts anti-metastatic activity in the nanomolar range in breast cancer cells.
|
-
- HY-126941
-
|
Hecogenin acetate
|
Opioid Receptor
|
Neurological Disease
|
|
Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
|
-
- 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-108261
-
|
Tomeglovir
BAY 38-4766
|
CMV
|
Infection
|
|
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
|
-
- HY-B1355A
-
-
- HY-13751
-
-
- HY-N0436
-
|
Engeletin
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.
|
-
- HY-N6998
-
|
Paederosidic acid
|
Apoptosis
|
Cancer
|
|
Paederosidic acid is isolated from P. scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis.
|
-
- HY-N7697C
-
-
- HY-N0141
-
|
Parthenolide
(-)-Parthenolide
|
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-107569
-
|
Garcinol
|
AChE
Histone Acetyltransferase
Apoptosis
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
|
|
Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 µM and 7.39 µM, respectively. Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity.
|
-
- HY-N1067
-
|
Xanthohumol
|
COX
Acyltransferase
Apoptosis
HSV
CMV
Influenza Virus
|
Cancer
Infection
|
|
Xanthohumol is one of the principal flavonoids isolated from hops, the inhibitor of diacylglycerol acetyltransferase (DGAT), COX-1 and COX-2, and shows anti-cancer and anti-angiogenic activities. Xanthohumol also has antiviral activity against bovine viral diarrhea virus (BVDV), rhinovirus, HSV-1, HSV-2 and cytomegalovirus (CMV).
|
-
- HY-W012126
-
|
2,6-Dichlorodiphenylamine
2,6-Dichloro-N-phenylaniline
|
Bacterial
|
Cancer
Infection
|
|
2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
|
-
- HY-130208
-
|
Thiodigalactoside
TDG
|
Galectin
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.
|
-
- HY-121636
-
|
Resolvin D2
RvD2
|
TRP Channel
|
Infection
Inflammation/Immunology
Neurological Disease
|
|
Resolvin D2 is a metabolite of docosahexaenoic acid (DHA), with anti-inflammatory, anti-infective activities. Resolvin D2 is a potent regulator of leukocytes and controls microbial sepsis. Resolvin D2 is a remarkably potent inhibitor of TRPV1 (IC50 = 0.1 nM) and TRPA1 (IC50 = 2 nM) in primary sensory neurons.
|
-
- HY-B0520A
-
|
Benztropine mesylate
Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
|
Dopamine Receptor
mAChR
Histamine Receptor
|
Cancer
Neurological Disease
|
|
Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.
|
-
- HY-N0313
-
|
Euphol
|
Endogenous Metabolite
MAGL
|
Inflammation/Immunology
|
|
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain.
|
-
- HY-135674
-
|
SR-318
|
p38 MAPK
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
|
-
- HY-16561
-
|
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-N2014
-
|
Verbenalin
|
Others
|
Infection
Inflammation/Immunology
|
|
Verbenalin is Verbena glycoside, with anti-inflammatory, anti-fungal anti-virus activities. Verbenalin can be used for the research of prostatitis. Verbenalin can reduce cerebral ischemia-reperfusion injury.
|
-
- HY-N6806
-
-
- HY-N2604
-
|
Loureirin C
|
Others
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Loureirin C, isolated from "Dragon’s blood", which is a deep red resin obtained from a variety of plant sources. The resin extracted from stems of Dracaena cochinchinensis is one such source of “dragon’s blood”, has a reputation for facilitating blood circulation and dispersing blood stasis. The resin has anti-bacterial, anti-spasmodic, anti-inflammatory, analgesic, anti-diabetic, and anti-tumor activities.
|
-
- HY-N0101
-
-
- HY-N0184
-
-
- HY-N1451
-
-
- HY-18234A
-
|
Leupeptin hemisulfate
|
Cathepsin
|
Inflammation/Immunology
|
|
Leupeptin hemisulfate is a membrane-permeable thiol protease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
|
-
- HY-137067
-
|
IMT1B
LDC203974
|
Others
|
Cancer
|
|
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects.
|
-
- HY-14471
-
|
Cetilistat
ATL-962
|
Others
|
Metabolic Disease
|
|
Cetilistat (ATL-962), an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
|
-
- HY-N0222
-
|
Avicularin
|
Others
|
Cancer
Inflammation/Immunology
|
|
Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
|
-
- HY-N0155
-
|
Nobiletin
|
ROR
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
|
-
- HY-15005B
-
|
Sofosbuvir impurity C
|
Others
|
Others
|
|
Sofosbuvir impurity C is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-100857
-
|
PrPSc-IN-1
|
Others
|
Neurological Disease
|
|
PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrP Sc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity.
|
-
- HY-16589
-
-
- HY-W019940
-
-
- HY-N9315
-
-
- HY-W028047
-
|
JFD01307SC
|
Bacterial
|
|
|
JFD01307SC is a glutamine synthetase inhibitor and anti-tuberculosis agent. JFD01307SC acts as a mimic of L-Glutamate and thus target enzymes involved in glutamine biosynthesis.
|
-
- HY-I0727
-
|
Sofosbuvir impurity E
|
Others
|
Others
|
|
Sofosbuvir impurity E is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-100757
-
|
CPUY074020
|
Histone Methyltransferase
|
Cancer
|
|
CPUY074020 is a potent and oral bioavailable inhibitor of histone methyltransferase G9a, with an IC50 of 2.18 μM. CPUY074020 possesses anti-proliferative activity.
|
-
- HY-N6860
-
|
Lucidenic acid C
|
MMP
|
Cancer
|
|
Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-N0248
-
|
Saikosaponin B2
|
HCV
|
Cancer
Infection
|
|
Saikosaponin B2 is an active component from Bupleurum kaoi root, acts as an entry inhibitor against HCV infection. Anti-cancer activity.
|
-
- HY-I0719
-
|
Sofosbuvir impurity B
|
Others
|
Others
|
|
Sofosbuvir impurity B is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-30219
-
-
- HY-116514
-
-
- HY-126296
-
-
- HY-116856
-
-
- HY-128599
-
|
NMS-P515
|
PARP
|
Cancer
|
|
NMS-P515 is a potent, orally active and stereospecific PARP-1 inhibitor, with a Kd of 16 nM and an IC50 of 27 nM (in Hela cells). Anti-tumor activity.
|
-
- HY-I0723
-
|
Sofosbuvir impurity D
|
Others
|
Others
|
|
Sofosbuvir impurity D is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-N0011
-
-
- HY-109588
-
|
NITD-349
|
Bacterial
|
Infection
|
|
NITD-349 is an MmpL3 inhibitor that shows highly potent anti-mycobacterial activity with MIC50 of 23 nM against virulent Mycobacterium tuberculosis H37Rv.
|
-
- HY-15605
-
|
Encorafenib
LGX818
|
Raf
|
Cancer
|
|
Encorafenib (LGX818) is a highly potent BRAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing BRAF V600E (EC50=4 nM).
|
-
- HY-129181
-
|
FGFR4-IN-4
|
FGFR
|
Cancer
|
|
FGFR4-IN-4 (compound 693) is a FGFR4 inhibitor with anti-tumor activity, extracted from patent WO2018113584A1.
|
-
- HY-N0252
-
-
- HY-108485
-
|
Damnacanthal
|
Src
Apoptosis
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.
|
-
- HY-N6039
-
-
- HY-111757
-
-
- HY-N0423
-
-
- HY-19909
-
|
NRC-2694
|
EGFR
|
Cancer
|
|
NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties.
|
-
- HY-N2437
-
-
- HY-B1214
-
-
- HY-P1539A
-
-
- HY-N2490
-
-
- HY-N1402
-
|
Oxysophoridine
Sophoridine N-oxide
|
Apoptosis
|
Inflammation/Immunology
|
|
Oxysophoridine (Sophoridine N-oxide) is a bioactive alkaloid extracted from the Sophora alopecuroides Linn. Oxysophoridine (Sophoridine N-oxide) shows anti inflammatory, anti oxidative stress and anti apoptosis effects.
|
-
- HY-B2230
-
-
- HY-N0334A
-
|
(+)-Magnoflorine iodide
Magnoflorine iodide; α-Magnoflorine iodide; Thalictrine iodide
|
Fungal
|
Infection
Metabolic Disease
|
|
(+)-Magnoflorine iodide (Magnoflorine iodide), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. (+)-Magnoflorine iodide has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-N0664
-
|
Aucubin
|
Bacterial
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
|
Aucubin, an iridoid glucoside, is isolated from Plantago asiatica, Eucommia ulmoides, the leaves of Aucuba japonica and more recently from butterfly larva. Aucubin has many biological activities, such as antioxidant, anti-aging, anti-inflammatory, antimicrobial, anti-fibrotic, anti-cancer, hepatoprotective, neuroprotective and osteoprotective effects.
|
-
- HY-B1452
-
|
Licofelone
ML-3000
|
COX
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins.
|
-
- HY-14658S
-
-
- HY-P1306
-
|
Obestatin(rat)
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-14374
-
|
GPP78
CAY10618
|
NAMPT
Autophagy
|
Cancer
Inflammation/Immunology
|
|
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects.
|
-
- HY-15505
-
|
RWJ-67657
JNJ 3026582
|
p38 MAPK
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. RWJ-67657 displays no activity at p38γ and p38δ, and exhibits cardio protective effect. Anti-inflammatory and anti-tumor activity.
|
-
- HY-111551
-
|
FT113
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo.
|
-
- 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-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
|
Suramin
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-131999
-
-
- HY-106423
-
|
Mivobulin
NSC 613862; (S)-(-)-NSC 613862
|
Microtubule/Tubulin
|
Cancer
|
|
Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity.
|
-
- HY-133511
-
|
MLS000544460
|
Phosphatase
|
Cancer
|
|
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity.
|
-
- HY-N0770
-
|
Isoliensinine
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells.
|
-
- HY-N0064
-
-
- HY-N2357
-
-
- HY-N2035
-
-
- HY-N0718
-
-
- HY-N7083
-
-
- HY-104015
-
-
- HY-N0362
-
-
- HY-N5010
-
-
- HY-112800
-
|
cyt-PTPε Inhibitor-1
|
Phosphatase
|
Metabolic Disease
|
|
cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
|
-
- HY-N7030
-
|
5,7,3',4'-Tetramethoxyflavone
|
Others
|
Infection
|
|
5,7,3',4'-Tetramethoxyflavone, one of the major polymethoxyflavones (PMFs) isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
|
-
- HY-N6871
-
-
- HY-128685
-
|
FD 12-9
Ac12Az9
|
P-glycoprotein
BCRP
|
Cancer
|
|
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
|
-
- HY-109587
-
|
BM635
|
Bacterial
|
Infection
|
|
BM635 is a MmpL3 inhibitor with outstanding anti-mycobacterial activity. BM635 has an MIC50 of 0.12 μM against M. tuberculosis H37Rv.
|
-
- HY-12460
-
-
- HY-125729
-
-
- HY-114162A
-
-
- HY-15307A
-
|
Belumosudil mesylate
KD025 mesylate; SLx-2119 mesylate
|
ROCK
|
Inflammation/Immunology
|
|
Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
|
-
- HY-I1196
-
|
Sofosbuvir impurity L
|
HCV
|
Infection
|
|
Sofosbuvir impurity L, 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-101312
-
-
- HY-114162
-
-
- HY-N0252A
-
-
- HY-15307
-
|
Belumosudil
KD025; SLx-2119
|
ROCK
|
Inflammation/Immunology
|
|
Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
|
-
- 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-N2193
-
|
Hirsutine
|
Apoptosis
|
Cancer
Infection
|
|
Hirsutine, an indole alkaloid of Uncaria rhynchophylla, exhibits anti-cancer activity. Hirsutine induces apoptosis and is a potent Dengue virus inhibitor exhibiting low cytotoxicity.
|
-
- HY-13751A
-
-
- HY-N0622
-
-
- HY-101191
-
|
Ecteinascidin 770
Ecteinascidine 770; Et-770
|
Apoptosis
|
Cancer
|
|
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
|
-
- HY-N0405
-
|
Orientin
|
Others
|
Cancer
Neurological Disease
|
|
Orientin is a naturally occurring bioactive flavonoid that possesses diverse biological properties, including anti-inflammation, anti-oxidative, anti-tumor, and cardio protection. Orientin is a promising neuroprotective agent suitable for therapy for neuropathic pain.
|
-
- HY-126562
-
-
- HY-106628
-
|
Sudoxicam
|
COX
|
Inflammation/Immunology
|
|
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.
|
-
- HY-N3085
-
|
Phellamurin
|
P-glycoprotein
Apoptosis
|
Cancer
Metabolic Disease
|
|
Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity.
|
-
- HY-136124
-
|
Cetilistat impurity 1
|
Others
|
Others
|
|
Cetilistat impurity 1 is an impurity of Cetilistat. Cetilistat, an inhibitor of pancreatic lipase, acts as an effective anti-obesity agent. Cetilistat inhibits rat and human pancreatic lipase activity with IC50s of 54.8 nM, and 5.95 nM, respectively.
|
-
- HY-13685
-
|
Miltefosine
HePC; Hexadecyl phosphocholine
|
Akt
HIV
|
Infection
Cancer
|
|
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
|
-
- 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-B0619
-
|
Zaltoprofen
CN100
|
COX
|
Inflammation/Immunology
|
|
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
|
-
- HY-N0587
-
|
Demethylzeylasteral
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
|
-
- HY-N0547
-
|
Nomilin
|
Others
|
Metabolic Disease
|
|
Nomilin is a limonoid compound obtained from the extracts of citrus fruits. Nomilin is an anti-obesity and anti-hyperglycemic agent .
|
-
- HY-N4137
-
-
- HY-N0628
-
-
- HY-N0180
-
-
- HY-N8091
-
|
Lehmannine
|
Bacterial
|
Cancer
Infection
|
|
Lehmannine is a quinolizidine bioalkaloid isolated from S. alopecuroides L, has antibacterial, anti-inflammatory and anti-tumor activities.
|
-
- HY-U00063
-
-
- HY-N0073
-
-
- HY-135190
-
-
- HY-117506
-
|
(S)-SBFI-26
|
FABP
|
Neurological Disease
|
|
(S)-SBFI-26 is the (S) enantiomer of SBFI-26, an anti-nociceptive agent binds to anandamide transporters FABP5 and FABP7. (S)-SBFI-26 has anti-nociceptive and anti-inflammatory effects.
|
-
- 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-N7576
-
|
Anemarrhenasaponin Ia
|
Others
|
Inflammation/Immunology
|
|
Anemarrhenasaponin Ia, isolated from Anemarrhenae rhizome, inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation. Anemarrhenasaponin Ia is an useful anti-inflammation reagent.
|
-
- HY-I0515
-
|
Sofosbuvir impurity K
|
HCV
|
Infection
|
|
Sofosbuvir impurity K, 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-I0512
-
|
Sofosbuvir impurity I
|
HCV
|
Infection
|
|
Sofosbuvir impurity I, 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-I0513
-
|
Sofosbuvir impurity N
|
HCV
|
Others
|
|
Sofosbuvir impurity N, 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-114481
-
|
Imidazole ketone erastin
IKE
|
Ferroptosis
|
Cancer
|
|
Imidazole ketone erastin is a potent, selective, and metabolically stable inhibitor of the cystine-glutamate antiporter, system xc - and an activator of ferroptosis. Imidazole ketone erastin has anti-tumor activity.
|
-
- HY-18342
-
|
Diflunisal
MK-647
|
COX
|
Inflammation/Immunology
Cancer
|
|
Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
|
-
- HY-I0938
-
|
Sofosbuvir impurity H
|
HCV
|
Infection
|
|
Sofosbuvir impurity H, 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-15230
-
-
- HY-B1130
-
|
Isoxicam
|
COX
|
Inflammation/Immunology
|
|
Isoxicam is an orally active, long-acting, non-steroidal anti-inflammatory agent for the research of arthritis. Isoxicam is a nonselective inhibitor of COX-1 and COX-2.
|
-
- HY-I0975
-
|
Sofosbuvir impurity J
|
HCV
|
Infection
|
|
Sofosbuvir impurity J, 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-N1380
-
-
- HY-I0735
-
|
Sofosbuvir impurity M
|
HCV
|
Infection
|
|
Sofosbuvir impurity M, 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-N2270
-
-
- HY-I0406
-
|
Sofosbuvir impurity F
|
HCV
|
Infection
|
|
Sofosbuvir impurity F, 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-112732B
-
|
Sparfosic acid trisodium
|
Others
|
Cancer
Metabolic Disease
|
|
Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis.
|
-
- HY-P1104A
-
|
FC131 TFA
|
CXCR
HIV
|
Infection
|
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
|
-
- HY-114277A
-
|
Sotorasib racemate
AMG-510 racemate
|
Ras
|
Cancer
|
|
Sotorasib (AMG-510) racemate is the racemate of Sotorasib (AMG-510). AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
|
-
- HY-I0408
-
|
Sofosbuvir impurity G
|
Others
|
Others
|
|
Sofosbuvir impurity G, 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-13571A
-
-
- HY-18974
-
-
- HY-N1382
-
|
Asperuloside
|
NO Synthase
|
Inflammation/Immunology
|
|
Asperuloside is an iridoid isolated from Hedyotis diffusa, with anti-inflammatory activity. Asperuloside inhibits inducible nitric oxide synthase (iNOS), suppresses NF-κB and MAPK signaling pathways.
|
-
- HY-N1372A
-
|
Fangchinoline
|
HIV
FAK
Apoptosis
Autophagy
|
Cancer
Infection
|
|
Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
|
-
- HY-112724
-
|
SHR0302
|
JAK
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
|
-
- HY-121537
-
|
CAY10404
|
COX
Akt
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.
|
-
- HY-N0376
-
|
Liquiritin
|
Reactive Oxygen Species
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Liquiritin, a flavonoid isolated from Glycyrrhiza, is a potent and competitive AKR1C1 inhibitor with IC50s of 0.62 μM, 0.61 μM, and 3.72μM for AKR1C1, AKR1C2 and AKR1C3, respectively. Liquiritin efficiently inhibits progesterone metabolism mediated by AKR1C1 in vivo. Liquiritin acts as an antioxidant and has neuroprotective, anti-cancer and anti-inflammatory activity.
|
-
- HY-N6961
-
|
Lapachol
|
Bacterial
Fungal
Influenza Virus
Parasite
|
Cancer
Infection
Inflammation/Immunology
|
|
Lapachol is a naphthoquinone that was first isolated from Tabebuia avellanedae (Bignoniaceae). Lapachol shows anti-abscess, anti-ulcer, antileishmanial, anticarcinomic, antiedemic, anti-inflammatory, antimalarial, antiseptic, antitumor, antiviral, antibacterial, antifungal and pesticidal activities.
|
-
- HY-129055
-
|
Isoeleutherin
|
Fungal
|
Inflammation/Immunology
|
|
Isoeleutherin is a naphthopyran derivative isolated from E. americana Merr. Et Heyne with anti-fungal, anti-viral, and anti-tumor activities. Isoeleutherin plays an important role in selective modulation of T helper cell-mediated immune responses.
|
-
- HY-N7046
-
|
Silybin B
|
Amyloid-β
|
Cancer
Neurological Disease
|
|
Silybin B, a flavonolignan separated from Silybum marianum, has anti-tumor activity. Silybin B is the most potent antifibrillogenic and anti-oligomeric component of silymarin and proposes it as a promising anti Alzheimer’s disease drug candidate.
|
-
- HY-128766
-
|
CHK1-IN-4
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity.
|
-
- HY-10454
-
|
Delanzomib
CEP-18770
|
Proteasome
NF-κB
Apoptosis
|
Cancer
|
|
Delanzomib (CEP-18770) is a potent and orally active chymotrypsin-like activity of the proteasome inhibitor with an IC50 of 3.8 nM. Delanzomib inhibits NF-κB activity, induces cancer cell apoptotic, and has strong antiangiogenic and anti-cancer activities.
|
-
- HY-N0114
-
|
Evodiamine
(+)-Evodiamine; d-Evodiamine
|
Others
|
Cancer
|
|
Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.
|
-
- HY-N0512
-
|
Loganin
Loganoside
|
Apoptosis
|
Cancer
|
|
Loganin, a major iridoid glycoside obtained from Corni fructus, has been shown to have anti-inflammatory and anti-shock effects.
|
-
- HY-15097
-
-
- HY-N2343
-
-
- HY-N0100
-
-
- HY-N0271
-
-
- HY-107818
-
|
4-Hydroxychalcone
|
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
|
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity. 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice.
|
-
- HY-12383
-
|
Pelubiprofen
|
COX
|
Inflammation/Immunology
Neurological Disease
|
|
Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
|
-
- HY-P1306A
-
|
Obestatin(rat) TFA
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-N0763
-
|
Angelicin
Isopsoralen
|
Apoptosis
Virus Protease
|
Cancer
|
|
Angelicin, a furocoumarin naturally occurring tricyclic aromatic compound, structurally related to psoralens, is reported to have anti-cancer, antiviral, anti-inflammatory activity.
|
-
- HY-N8536
-
|
Papyracillic acid
|
Fungal
Bacterial
|
Infection
|
|
Papyracillic acid, a fungal metabolite, a Penicillic acid analog, is a nonselective herbicide. Papyracillic acid has anti-bacterial, anti-fungal, nematicidal, and phytotoxic effects.
|
-
- HY-133153S
-
-
- HY-112920
-
|
TM-25659
|
Others
|
Metabolic Disease
|
|
TM-25659 is a transcriptional co-activator with PDZ-binding motif (TAZ) modulator. Anti-osteoporotic and anti-obesity activities.
|
-
- HY-100599
-
-
- HY-B0138
-
|
Ketorolac tromethamine salt
Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt
|
COX
|
Inflammation/Immunology
|
|
Ketorolac tromethamine salt (RS37619 tromethamine salt) is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-N0738
-
-
- HY-13324
-
|
Bardoxolone methyl
RTA 402; NSC 713200; CDDO Methyl ester
|
Keap1-Nrf2
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
|
-
- HY-135654
-
-
- HY-N7688
-
-
- HY-107795
-
-
- HY-135957
-
-
- HY-N0133
-
|
Tangeretin
Tangeritin; NSC53909; NSC618905
|
Notch
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tangeretin (Tangeritin), a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several disease models, and is a Notch-1 inhibitor.
|
-
- HY-120832
-
|
Azt-pmap
|
HIV
|
Infection
|
|
Azt-pmap, a nucleoside analogue, is an aryl phosphate derivative of AZT. Azt-pmap shows anti-HIV activity. AZT is a nucleoside reverse transcriptase inhibitor (NRTI) for HIV infection.
|
-
- HY-N1200
-
-
- HY-B2175
-
|
Aspirin Aluminum
Aluminum diacetylsalicylate
|
Others
|
Inflammation/Immunology
|
|
Aspirin Aluminum is a novel intermolecular compound which can inhibit gastrointestinal mucosal disorders induced by NSAIDs (non-steroidal anti-inflammatory agents) extracted from patent WO 2010064441 A1.
|
-
- HY-126121
-
-
- HY-N0872
-
-
- HY-110244
-
|
Tilfrinib
|
Others
|
Cancer
|
|
Tilfrinib (compound 4f) is a potent and selective inhibitor of breast tumor kinase (Brk) with an IC50 of 3.15 nM, which displays anti-proliferative activity and acts as a promising antitumor agent.
|
-
- HY-N0737
-
-
- HY-N1482
-
|
Methyl palmitate
|
Others
|
Inflammation/Immunology
|
|
Methyl palmitate, an acaricidal compound occurring in green walnut husks, inhibits phagocytic activity and immune response. Methyl palmitate also posseses anti-inflammatory and antifibrotic effects.
|
-
- HY-119500
-
-
- HY-130603
-
|
DCZ0415
|
NF-κB
Apoptosis
|
Cancer
|
|
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.
|
-
- HY-12912
-
|
KDU691
|
PI4K
Parasite
|
Infection
|
|
KDU691, an imidazopyrazine with potent anti-parasitic activity against blood stage schizonts, gametocytes and liver stages, is a Plasmodium PI4K inhibitor. KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.
|
-
- HY-114200
-
|
Imrecoxib
BAP-909
|
COX
|
Inflammation/Immunology
|
|
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
|
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-100898
-
|
OGT 2115
|
Others
|
Cancer
|
|
OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity.
|
-
- HY-122219
-
|
R243
|
CCR
|
Inflammation/Immunology
|
|
R243 is a potent and selective CCR8 antagonist. R243 inhibits CCL1/CCR8 interaction and inhibits CCR8 signaling and chemotaxis. R243 has antinociceptive and anti-inflammatory effects.
|
-
- HY-B1893
-
-
- HY-N0580
-
-
- HY-133127
-
|
AR453588
|
Glucokinase
|
Metabolic Disease
|
|
AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.
|
-
- HY-N0748
-
-
- HY-133127A
-
-
- HY-N1579
-
-
- HY-106541
-
|
Neticonazole
|
Fungal
|
Cancer
Infection
|
|
Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole has anti-infection and anti-cancer effects.
|
-
- HY-128365
-
-
- HY-N4103
-
|
Fucosterol
|
PARP
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
|
Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.
|
-
- HY-129440
-
|
N-(p-Coumaroyl) Serotonin
|
PDGFR
|
Metabolic Disease
Inflammation/Immunology
|
|
N-(p-Coumaroyl) Serotonin is a polyphenol isolated from the seeds of safflower and has antioxidative, anti-atherogenic and anti-inflammatory properties. N-(p-Coumaroyl) Serotonin inhibits PDGF-induced on phosphorylation of PDGF receptor and Ca 2+ release from sarcoplasmic reticulum. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo and is usually used for the atherosclerosis research.
|
-
- HY-N2259
-
|
Curcumenol
(+)-Curcumenol
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Curcumenol ((+)-Curcumenol) is a potent CYP3A4 inhibitor with an IC50 of 12.6 μM, which is one of constituents in the plants of medicinally important genus of Curcuma zedoaria, with neuroprotection, anti-inflammatory, anti-tumor and hepatoprotective activities. Curcumenol ((+)-Curcumenol) suppresses Akt-mediated NF-κB activation and p38 MAPK signaling pathway in LPS-stimulated BV-2 microglial cells.
|
-
- HY-119367
-
|
ODM-203
|
FGFR
VEGFR
|
Cancer
|
|
ODM-203 is a potent FGFR and VEGFR families inhibitor with IC50s of 11, 16, 6, 35 nM towards recombinant FGFR1, FGFR2, FGFR3 and FGFR4 as well as 26, 9, 5 nM towards VEGFR1, VEGFR2 and VEGFR3, respectively. ODM-203 exhibits strong anti-tumor activity and induces anti-tumor immunity.
|
-
- HY-N2500
-
|
Deoxypodophyllotoxin
|
Microtubule/Tubulin
Apoptosis
Autophagy
|
Infection
Cardiovascular Disease
|
|
Deoxypodophyllotoxin (DPT), a derivative of podophyllotoxin, is a lignan with potent antimitotic, anti-inflammatory and antiviral properties isolated from rhizomes of Sinopodophullumhexandrum (Berberidaceae). Deoxypodophyllotoxin, targets the microtubule, has a major impact in oncology not only as anti-mitotics but also as potent inhibitors of angiogenesis. Deoxypodophyllotoxin induces cell autophagy and apoptosis. Deoxypodophyllotoxin evokes increase of intracellular Ca 2+ concentrations in DRG neurons.
|
-
- HY-18992
-
|
AS2444697
|
IRAK
|
Inflammation/Immunology
|
|
AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.
|
-
- 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-131259
-
-
- HY-136640
-
|
BCL6-IN-4
|
Bcl-2 Family
|
Cancer
|
|
BCL6-IN-4 is a potent B-cell lymphoma 6 (BCL6) inhibitor with an IC50 of 97 nM. BCL6-IN-4 has anti-tumor activities.
|
-
- HY-N3925
-
-
- HY-126294
-
|
JAK1-IN-7
|
JAK
|
Inflammation/Immunology
|
|
JAK1-IN-7 is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
|
-
- HY-124646
-
|
KIRA-7
|
IRE1
|
Inflammation/Immunology
|
|
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
|
-
- HY-128669
-
|
Abemaciclib metabolite M2
LSN2839567
|
CDK
|
Cancer
|
|
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity.
|
-
- HY-N6644
-
|
Crocin III
|
Others
|
Cancer
Inflammation/Immunology
|
|
Crocin III is a crocetin from saffron (Crocus sutivus L.). Crocetins inhibit cell growth of tumor cells and has anti-inflammatory activity. Crocins serve as spices and coloring agents.
|
-
- HY-N7275
-
-
- HY-N0493
-
-
- HY-131258
-
-
- HY-131260
-
-
- HY-N2410
-
|
N-trans-Feruloyltyramine
N-feruloyltyramine; Moupinamide
|
COX
|
Inflammation/Immunology
|
|
N-trans-Feruloyltyramine (N-feruloyltyramine), an alkaloid from Piper nigru, is an inhibitor of COX1 and COX2, with potential antioxidant properties. N-trans-Feruloyltyramine possesses anti-inflammatory activity.
|
-
- HY-129188
-
|
CCT369260
|
Bcl-2 Family
|
Cancer
|
|
CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM.
|
-
- HY-17643
-
|
Oteseconazole
VT-1161
|
Fungal
Cytochrome P450
|
Infection
|
|
Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51.
|
-
- HY-N4184
-
|
Licoflavone B
|
Parasite
|
Infection
|
|
Licoflavone B is a flavonoid isolated from Glycyrrhiza inflata, inhibits S. mansoni ATPase (IC50, 23.78 µM) and ADPase (IC50, 31.50 µM) activity. Anti-schistosomiasis activity.
|
-
- HY-N3115
-
|
Palbinone
|
Others
|
Inflammation/Immunology
|
|
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
|
-
- HY-N2593
-
|
Isorhapontigenin
|
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation.
|
-
- HY-B0418A
-
-
- HY-16293
-
-
- HY-N1422
-
|
Hecogenin
|
Others
|
Infection
Inflammation/Immunology
|
|
Hecogenin is a steroid saponin isolated from Agave sisalana and is a selective inhibitor of human UDP-glucuronosyltransferases. Hecogenin has a wide spectrum of pharmacological activities, including anti-inflammatory, antifungal and gastroprotective effects.
|
-
- HY-136450
-
|
Triclabendazole sulfoxide
TCBZ-SO
|
Parasite
BCRP
|
Infection
|
|
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP.
|
-
- HY-B0945
-
-
- HY-106859
-
-
- HY-B0994
-
-
- HY-N4109
-
|
Decursinol
|
Others
|
Cancer
Inflammation/Immunology
|
|
Decursinol, isolated from the roots of Angelica gigas, possesses antinociceptive effect with orally bioavailability. Decursinol possesses anti-tumor and anti-metastasis activity.
|
-
- HY-N4068
-
|
Glucoraphanin
|
Reactive Oxygen Species
|
Cancer
|
|
Glucoraphanin, a natural glucosinolate found in cruciferous vegetable, is a stable precursor of the Nrf2 inducer sulforaphane, which possesses antioxidant, anti-inflammatory, and anti-carcinogenic effects.
|
-
- HY-N5135
-
|
Liriopesides B
Nolinospiroside F
|
Others
|
Others
|
|
Liriopesides B (Nolinospiroside F) is a steroidal saponin isolated from Ophiopogon japonicas. Liriopesides B has anti-oxidative and anti-aging effects.
|
-
- HY-D0803
-
|
Thymoquinone
|
Others
|
Inflammation/Immunology
|
|
Thymoquinone is a nature product isolated from N. sativa. Thymoquinone possess antioxidant, anti-inflammatory, anti-cancer, antitumor activities and hepatoprotective properties.
|
-
- HY-U00151
-
-
- HY-N0207
-
-
- HY-N0558
-
|
Alnustone
|
Others
|
Inflammation/Immunology
|
|
Alnustone, a non-phenolic diarylheptanoid found in herbs and spices, is a constituent of Curcuma xanthorrhiza. Alnustone displays anti-emetic and anti-inflammatory activities.
|
-
- HY-N7700
-
-
- HY-B1320
-
|
Meclofenamate sodium
Meclofenamic acid sodium
|
Gap Junction Protein
|
Inflammation/Immunology
|
|
Meclofenamic acid sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-111549
-
|
Bragsin1
|
Others
|
Cancer
|
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
|
-
- HY-17401
-
|
Ranolazine dihydrochloride
CVT 303 dihydrochloride; RS 43285
|
Calcium Channel
Sodium Channel
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
|
-
- HY-N2036
-
|
Mosloflavone
|
Enterovirus
Bacterial
|
Infection
|
|
Mosloflavone is a flavonoid isolated from Scutellaria baicalensis Georgi with anti-EV71 activity. Mosloflavone inhibits VP2 virus replication and protein expression during the initial stage of virus infection and inhibits viral VP2 capsid protein synthesis. Mosloflavone is a promising biocide and inhibits P. aeruginosa virulence and biofilm formation.
|
-
- HY-B1099
-
|
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- HY-N0289
-
-
- HY-17596A
-
|
Closantel sodium
|
Parasite
|
Infection
|
|
Closantel sodium is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel sodium is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel sodium inhibits the O. volvulus L3 to L4 molt of developing.
|
-
- HY-112847A
-
|
Sulfosuccinimidyl oleate sodium
Sulfo-N-succinimidyl oleate sodium
|
Mitophagy
|
Inflammation/Immunology
|
|
Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
|
-
- HY-114147
-
-
- HY-17596
-
|
Closantel
|
Parasite
|
Infection
|
|
Closantel is a halogenated salicylanilide with a potent anti-parasitic activity. Closantel is a potent and highly specific Onchocerca volvulus chitinase (OvCHT1) inhibitor with an IC50 of 1.6 μM and a Ki of 468 nM. Closantel inhibits the O. volvulus L3 to L4 molt of developing.
|
-
- HY-N0158
-
|
Oxymatrine
|
TGF-beta/Smad
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Oxymatrine, an alkaloid from the roots of Sophora species, with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.
|
-
- HY-112847
-
|
Sulfosuccinimidyl oleate
Sulfo-N-succinimidyl oleate
|
Mitophagy
|
Inflammation/Immunology
|
|
Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
|
-
- 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-100775
-
|
Setogepram sodium salt
PBI-4050 sodium salt
|
GPR40
GPR84
|
Metabolic Disease
Inflammation/Immunology
|
|
Setogepram sodium salt (PBI-4050 sodium salt) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram sodium salt decreases renal, liver and pancreatic fibrosis. Setogepram sodium salt exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
|
-
- HY-N3963
-
-
- HY-100888
-
|
Simurosertib
TAK-931
|
CDK
|
Cancer
|
|
Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity.
|
-
- HY-101354
-
-
- HY-B0890
-
|
Zomepirac sodium salt
McN-2783-21-98
|
PGE synthase
|
Inflammation/Immunology
|
|
Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
|
-
- HY-P1404
-
|
R8-T198wt
|
Pim
|
Cancer
|
|
R8-T198wt is a cell-permeable carboxyl-terminal p27 Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
|
-
- HY-N7095
-
|
Ceftezole
CTZ
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
|
-
- HY-15356
-
-
- HY-N6261
-
|
Epimagnolin B
|
Others
|
Inflammation/Immunology
|
|
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
|
-
- HY-N7096
-
|
Ceftezole sodium
CTZ sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
|
-
- HY-13603
-
|
Crolibulin
EPC2407
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity.
|
-
- HY-50903
-
|
Rivaroxaban
BAY 59-7939
|
Factor Xa
|
Cardiovascular Disease
|
|
Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-N7512
-
|
Asimilobine
|
Dopamine Receptor
5-HT Receptor
Parasite
|
Cancer
Infection
|
|
Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
|
-
- HY-108570
-
|
AUDA
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
AUDA (compound 43) is a potent soluble epoxide hydrolase (sEH) inhibitor with IC50s of 18 and 69 nM for the mouse and human sEH, respectively. AUDA has anti-inflammatory activity.
|
-
- HY-B0253
-
|
Piroxicam
CP-16171
|
COX
|
Inflammation/Immunology
Cancer
|
|
Piroxicam (CP-16171) is a non-steroidal anti-inflammatory drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for human monocyte COX-1 and COX-2, respectively.
|
-
- HY-W016645
-
-
- HY-N2905
-
|
Aurantiamide acetate
Asperglaucide
|
Cathepsin
|
Inflammation/Immunology
|
|
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases.
|
-
- HY-B0961
-
|
Merbromin
Mercury dibromofluorescein disodium salt; ZP1
|
Bacterial
|
Others
|
|
Merbromin acts as a topical antiseptic for minor cuts and scrapes and as a biological dye. Merbromin is a potent inhibitor against Zika virus (ZIKV) replication. Merbromin shows anti-ZIKV potency through ZIKVpro inhibition.
|
-
- HY-12352A
-
|
HJC0416 hydrochloride
|
STAT
Apoptosis
|
Cancer
|
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.
|
-
- HY-122903A
-
|
(-)-TK216
|
DNA/RNA Synthesis
|
Cancer
|
|
(-)-TK216 is an enantiomer of TK216 (HY-122903). TK216 is an orally active and potent E26 transformation specific (ETS) inhibitor. (-)-TK216 has anti-cancer activity.
|
-
- HY-N0826
-
-
- HY-108704
-
|
CT-721
|
Bcr-Abl
|
Cancer
|
|
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities.
|
-
- HY-N0637
-
-
- HY-120327
-
|
KY-226
|
Phosphatase
|
Metabolic Disease
Neurological Disease
|
|
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
|
-
- 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-129601
-
|
MYCi975
NUCC-0200975
|
c-Myc
|
Cancer
Inflammation/Immunology
|
|
MYCi975 (NUCC-0200975) is an orally active MYC inhibitor, which disrupts MYC/MAX interaction, promotes MYC T58 phosphorylation and MYC degradation, and impairs MYC driven gene expression. MYCi975 (NUCC-0200975) exhibits potent anti-tumor efficacy with good tolerability, increases tumor immune cell infiltration, and sensitizes tumors to anti-PD1 immunotherapy.
|
-
- HY-N5003
-
-
- HY-N0799
-
|
Protodioscin
|
Endogenous Metabolite
|
Cancer
|
|
Protodioscin, a major steroidal saponin in dioscoreae rhizome, has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
|
-
- HY-B1285
-
|
Dimercaprol
2,3-Dimercapto-1-propanol; Dithioglycerol
|
HIV
|
Infection
|
|
Dimercaprol (2,3-Dimercapto-1-propanol) is an anti-heavy metal-poisoning drug, which exhibits anti-HIV activity.
|
-
- HY-W013573
-
-
- HY-101907
-
-
- HY-N7292
-
-
- HY-14615
-
|
[6]-Gingerol
(S)-(+)-[6]Gingerol; 6-Gingerol
|
AMPK
Apoptosis
|
Cancer
|
|
[6]-Gingerol is an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
|
-
- HY-B1137
-
|
Ramifenazone
IsopropylaminoAntipyrine
|
Others
|
Inflammation/Immunology
|
|
Ramifenazone (Isopropylaminoantipyrine) is a pyrazole derivative and acts as a non-steroidal anti-inflammatory agent (NSAID). Ramifenazone has analgesic, antipyretic, anti-inflammatory and antimicrobial activities.
|
-
- HY-B0299
-
|
Oxibendazole
|
Parasite
Apoptosis
|
Infection
|
|
Oxibendazole is an effective benzimidazole anthelmintic and is against nema-tode infections. Oxibendazole can induces apoptosis and has anti-cancer and anti-inflammation activities.
|
-
- HY-131708A
-
|
FNDR-20123
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations.
|
-
- HY-N0120
-
|
(E/Z)-Polydatin
(E/Z)-Piceid
|
Others
|
Inflammation/Immunology
|
|
(E/Z)-Polydatin ((E/Z)-Piceid) is a monocrystalline compound originally isolated from the root and rhizome of Polygonum cuspidatum. (E/Z)-Polydatin has anti-platelet aggregation, anti-oxidative action of low-density lipoprotein (LDL), cardioprotective activity, anti-inflammatory and immune-regulating functions.
|
-
- HY-130001
-
|
CDK9-IN-9
|
CDK
|
Cancer
|
|
CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
|
-
- HY-B0144A
-
-
- HY-100544
-
|
FLLL32
|
STAT
JAK
Apoptosis
|
Cancer
|
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
- HY-15375
-
|
Allitinib
AST-1306; ALS 1306
|
EGFR
|
Cancer
|
|
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib is an anilino-quinazoline compound and has anti-cancer activity.
|
-
- HY-D0143
-
|
Quinine
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine is an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM.
|
-
- HY-12035
-
|
AMG-208
|
c-Met/HGFR
Cytochrome P450
|
Cancer
|
|
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity.
|
-
- HY-B0338A
-
-
- HY-U00229
-
-
- HY-N0176
-
-
- HY-101751
-
-
- HY-U00081
-
-
- HY-100142
-
-
- HY-N6880
-
|
Rabdosiin
(+)-Rabdosiin
|
Others
|
Infection
Inflammation/Immunology
|
|
Rabdosiin is a tetramer of caffeic acid isolated from the stem of Rabdosia japonica Hara. Rabdosiin possess anti-allergic activity, anti-HIV activity and inhibition on DNA topoisomerase.
|
-
- HY-N3297
-
-
- HY-N2994
-
-
- HY-N4322
-
-
- HY-N0474
-
-
- HY-14616
-
|
Shogaol
[6]-Shogaol; 6-Shogaol
|
Autophagy
|
Cancer
|
|
Shogaol ([6]-Shogaol), an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
|
-
- HY-12840
-
-
- HY-N0401
-
-
- HY-B0280
-
|
Ranolazine
CVT 303; RS 43285-003
|
Sodium Channel
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor.
|
-
- HY-N6580
-
|
Ginsenoside Rg4
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Ginsenoside Rg4 is a major protopanaxatriol type ginsenoside isolated from the leaves of Panax ginseng C. A. Meyer. The protopanaxatriol type ginsenosides (such as Ginsenoside Rg4) exhibits various biological activities including anti-septic, anti-diabetic, wound healing, immune-stimulatory, and anti-antioxidant activity.
|
-
- HY-N0615
-
|
Notoginsenoside R1
Sanchinoside R1; Sanqi glucoside R1
|
Amyloid-β
Apoptosis
|
Others
|
|
Notoginsenoside R1 (Sanchinoside R1), a saponin, is isolated from P. notoginseng. Notoginsenoside R1 exhibits anti-oxidation, anti-inflammatory, anti-angiogenic, and anti-apoptosis activities. Notoginsenoside R1 provides cardioprotection against ischemia/reperfusion (I/R) injury. Notoginsenoside R1 also provides neuroprotection in H2O2-induced oxidative damage in PC12 cells.
|
-
- HY-103019
-
|
(+)-BAY-1251152
|
CDK
|
Cancer
|
|
(+)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (+). (+)-BAY-1251152 is a potent and selective CDK9 inhibitor with an IC50 of 3 nM. (+)-BAY-1251152 has anti-tumour activity.
|
-
- HY-12628
-
|
GNE-618
|
NAMPT
|
Cancer
|
|
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
|
-
- HY-N0929
-
|
Hexahydrocurcumin
|
COX
Reactive Oxygen Species
|
Cancer
|
|
Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities.
|
-
- HY-B0580S
-
|
Ketorolac D5
|
COX
|
Inflammation/Immunology
|
|
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-114429
-
|
CB-6644
|
Others
|
Cancer
|
|
CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.
|
-
- HY-B0109
-
|
Dorzolamide
L671152; MK507
|
Carbonic Anhydrase
|
Cancer
|
Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-B0574
-
|
Mefenamic acid
|
COX
|
Inflammation/Immunology
|
|
Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-100870
-
|
ABX464
|
HIV
|
Infection
|
|
ABX464 is a potent anti-HIV agent. ABX464 inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.
|
-
- HY-14882A
-
-
- HY-B0109A
-
|
Dorzolamide hydrochloride
L671152 hydrochloride; MK507 hydrochloride
|
Carbonic Anhydrase
|
Others
|
Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-125759
-
|
3-Phenyltoxoflavin
|
HSP
|
Cancer
|
|
3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity.
|
-
- HY-N3797A
-
|
Echitamine chloride
|
Apoptosis
|
Cancer
|
|
Echitamine chloride is the major monoterpene indole alkaloid present in Alstonia with potent anti-tumour activity. Echitamine chloride induces DNA fragmentation and cells apoptosis. Echitamine chloride inhibits pancreatic lipase with an IC50 of 10.92 µM.
|
-
- HY-135145
-
|
CB-103
|
Notch
|
Cancer
|
|
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
|
-
- HY-117985B
-
-
- HY-100566
-
-
- HY-129600
-
|
MYCi361
NUCC-0196361
|
c-Myc
|
Cancer
|
|
MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy.
|
-
- HY-U00046
-
|
Apyramide
|
COX
|
Inflammation/Immunology
|
|
Apyramide is an anti-inflammatory agent (NSAID) and behaves as a prodrug of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
|
-
- HY-N0842
-
|
Bevirimat
PA-457; MPC-4326; YK FH312
|
HIV
|
Infection
|
|
Bevirimat (PA-457; MPC-4326; YK FH312) is an anti-HIV drug derived from a betulinic acid-like compound; is believed to inhibit HIV by a novel mechanism, so-called maturation inhibition.
|
-
- HY-116304
-
|
1G244
|
Dipeptidyl Peptidase
Apoptosis
|
Cancer
|
|
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.
|
-
- HY-123847
-
|
KPT-6566
|
Others
|
Cancer
|
|
KPT-6566, a potent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 of 640 nM and a Ki of 625.2 nM for PIN1 PPIase domain. Anti-cancer activity.
|
-
- HY-119970
-
|
Helenalin
|
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding.
|
-
- HY-13427
-
|
Allitinib tosylate
AST-1306 (TsOH)
|
EGFR
|
Cancer
|
|
Allitinib tosylate (AST-1306 (TsOH)) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib tosylate also inhibits ErbB4 with an IC50 of 0.8 nM. Allitinib tosylate is an anilino-quinazoline compound and has anti-cancer activity
|
-
- HY-N1535
-
|
Ponicidin
Rubescensine B
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
|
-
- HY-N0779A
-
|
Silybin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Silybin is a flavonolignan isolated from milk thistle (Silybum marianum) seeds. Silybin induces apoptosis and exhibits hepatoprotective, antioxidant, anti-inflammatory, anti-cancer activity.
|
-
- 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-N1181
-
-
- HY-N0205
-
|
Pulchinenoside C
Anemoside B4
|
Others
|
Cancer
|
|
Pulchinenoside C (Anemoside B4) is Pulsatilla koreana Nakai that have many numerous biological effects in vitro, including enhancing hypoglycemic, anti-tumor, neuroprotective and anti-angiogenic activity.
|
-
- HY-B0634
-
|
Aceclofenac
|
COX
|
Inflammation/Immunology
|
|
Aceclofenac is an orally active nonsteroidal anti-inflammatory drug (NSAID), with analgesic and anti-inflammatory properties. Aceclofenac is used for the research of osteoarthritis, ankylosing spondylitis, rheumatoid arthritis.
|
-
- 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-135396
-
|
(1S,2S)-Bortezomib
|
Proteasome
Apoptosis
|
Cancer
|
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans.
|
-
- HY-N2556
-
|
Tirucallol
|
Others
|
Inflammation/Immunology
|
|
Tirucallol, a tetracyclic triterpene, is isolated from Euphorbia lacteal latex. Tirucallol has topical anti-inflammatory effect. Tirucallol can suppress ear edema in the mouse model and inhibit nitrite production in lipopolysaccharide-stimulated macrophages.
|
-
- HY-15556A
-
-
- HY-N1963
-
|
Curzerene
|
Gutathione S-transferase
Apoptosis
|
Cancer
|
|
Curzerene is a sesquiterpene is isolated from the rhizome of Curculigo orchioides Gaertn with anti-cancer activity. Curzerene inhibits glutathione S-transferase A1 (GSTA1) mRNA and protein expression. Curzerene induces cell apoptosis.
|
-
- HY-13250
-
|
Silvestrol aglycone
|
Others
|
Cancer
|
|
Silvestrol aglycone is a Silvestrol analogue, inhibits protein translation initiation in cancer cells, with EC50s of 10 and 200 nM for myc-LUC and tub-LUC luciferase reporter protein translation, respectively. Anti-cancer activity.
|
-
- HY-15556
-
-
- HY-111192
-
|
IPR-803
|
Ser/Thr Protease
|
Cancer
|
|
IPR-803 is a potent inhibitor of the uPAR•uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity.
|
-
- HY-103159
-
|
1-Deazaadenosine
|
Adenosine Deaminase
|
Cancer
|
|
1-Deazaadenosine is a potent Adenosine deaminase (ADA) inhibitor with a Ki value of 0.66 μM. 1-Deazaadenosine exhibits anti-cancer activities in vitro and has the potential to be a chemotherapy agent for lymphoproliferative disorders.
|
-
- HY-136328
-
-
- HY-118139
-
|
Desmethyl Celecoxib
|
COX
|
Inflammation/Immunology
|
|
Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%.
|
-
- HY-N0802
-
|
Tenuigenin
Senegenin
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Tenuigenin is a major active component isolated from the root of the Chinese herb Polygala tenuifolia. Tenuigenin protects against S.aureus-induced pneumonia by inhibiting NF-κB activation. Tenuigenin has anti-inflammatory effect.
|
-
- HY-N6968
-
|
α-Humulene
Humulene; α-Caryophyllene
|
NO Synthase
COX
|
Inflammation/Immunology
|
|
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
|
-
- HY-N4108
-
|
Hypophyllanthin
|
P-glycoprotein
|
Cancer
Inflammation/Immunology
|
|
Hypophyllanthin is a major lignan in Phyllanthus spp, with strong anti-inflammatory activity. Hypophyllanthin directly inhibits P-glycoprotein (P-gp) activity and did not interfere with multidrug resistance protein 2 (MRP2) activity.
|
-
- HY-N0220
-
|
Dauricine
|
NF-κB
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Dauricine, a bisbenzylisoquinoline alkaloid in Asiatic Moonseed Rhizome, possesses anti-inflammatory activity. Dauricine inhibits cell proliferation and invasion, and induces apoptosis by suppressing NF-κB activation in a dose- and time-dependent manner in colon cancer.
|
-
- 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-128594
-
-
- HY-112437
-
-
- HY-131343
-
|
HBV-IN-4
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
|
-
- HY-13629
-
-
- HY-N1404
-
|
Sodium aescinate
|
Others
|
Cancer
Inflammation/Immunology
|
|
Sodium aescinate is a triterpene saponin derived from Aesculus hippocastanum seeds, with anti-inflammatory and antioxidant activities. Sodium aescinate inhibits hepatocellular carcinoma growth by targeting CARMA3/NF-κB pathway.
|
-
- HY-133916
-
|
G140
|
Others
|
Inflammation/Immunology
|
|
G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.
|
-
- HY-100763
-
|
Mcl1-IN-12
|
Bcl-2 Family
|
Cancer
|
|
Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity.
|
-
- HY-15187
-
|
Filanesib
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.
|
-
- HY-B1394
-
|
Khellin
|
EGFR
|
Cancer
Cardiovascular Disease
|
|
Khellin is a furochromone that can be isolated from Ammi visnuga L.. Khellin is an EGFR inhibitor with an IC50 of 0.15 µM. Khelline has anti-proliferative activity in vitro. Khellin has antispasmodic and coronary vasodilator effects.
|
-
- HY-135236
-
|
OXFBD04
|
Epigenetic Reader Domain
|
Cancer
|
|
OXFBD04 is a potent and selective BRD4 inhibitor with an IC50 of 166 nM. OXFBD04 is a potent BET bromodomain ligand with additional modest affinity for the CREBBP bromodomain. OXFBD04 has anti-cancer activity.
|
-
- HY-76948
-
|
5-R-Rivaroxaban
|
Factor Xa
|
Cardiovascular Disease
|
|
5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
|
-
- HY-B0275
-
|
Oxytetracycline
|
Bacterial
HSV
Endogenous Metabolite
Antibiotic
|
Infection
|
|
Oxytetracycline is an antibiotic belonging to the tetracycline class. Oxytetracycline potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline also possesses anti-HSV-1 activity.
|
-
- HY-136427
-
|
KRM-III
|
Others
|
Inflammation/Immunology
|
|
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
|
-
- HY-D0143B
-
|
Quinine hemisulfate hydrate
|
Parasite
Potassium Channel
|
Infection
|
|
Quinine hemisulfate hydrate, an alkaloid derived from the bark of the cinchona tree, acts as an anti-malaria agent. Quinine hemisulfate hydrate is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV, with an IC50 of 169 μM.
|
-
- HY-16590
-
|
X-376
|
ALK
c-Met/HGFR
|
Cancer
|
|
X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
|
-
- HY-136220
-
|
AHR antagonist 5
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR antagonist 5, a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018195397, example 39, has an IC50 of < 0.5 µΜ. AHR antagonist 5 significantly inhibits tumor growth combined with checkpoint inhibitor anti-PD-1.
|
-
- HY-10253
-
|
AG1024
Tyrphostin AG 1024
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
|
-
- HY-B0275A
-
|
Oxytetracycline hydrochloride
|
Bacterial
HSV
Antibiotic
Endogenous Metabolite
|
Infection
|
|
Oxytetracycline hydrochloride is an antibiotic belonging to the tetracycline class. Oxytetracycline hydrochloride potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline hydrochloride is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline hydrochloride also possesses anti-HSV-1 activity.
|
-
- HY-B1203
-
-
- HY-77036
-
-
- HY-B0338
-
-
- HY-100286
-
-
- HY-U00149
-
-
- HY-U00100
-
-
- HY-100146
-
-
- HY-B1047
-
-
- HY-101573
-
-
- HY-101748
-
-
- HY-B0766
-
-
- HY-129189
-
|
RAS GTPase inhibitor 1
|
Ras
|
Cancer
|
|
RAS GTPase inhibitor 1 (example 51) is a RAS GTPase inhibitor with anti-tumor activity, extracted from patent WO2018212774A1. RAS GTPase inhibitor 1 (example 51) exhibits an EC50 less than 1 μM for at least one nucleotide exchange and an IC50 less than 1 μM in H727 cells.
|
-
- HY-Y0073
-
|
4-Hydroxyacetophenone
P-hydroxyacetophenone
|
HBV
|
Infection
Inflammation/Immunology
|
|
4-Hydroxyacetophenone (P-hydroxyacetophenone) is a key hepatoprotective and choleretic compound in Artemisia capillaris and A. morrisonensis, also has an anti-hepatitis B virus effect and anti-inflammatory effect.
|
-
- HY-N6049
-
-
- HY-N0363
-
|
(+)-Columbianetin
(S)-Columbianetin
|
Others
|
Infection
Inflammation/Immunology
|
|
(+)-Columbianetin is an isomer of Columbianetin. Columbianetin is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory activity.
|
-
- HY-N2281
-
-
- HY-N0639
-
|
Punicalin
|
HBV
|
Infection
Inflammation/Immunology
|
|
Punicalin is a hydrolyzable tannin isolated from Punica granatum L. or the leaves of Terminalia catappa L.. Punicalin is a anti-hepatitis B virus (HBV) agent and has anti-inflammatory activity.
|
-
- HY-N6892
-
|
3'-O-Acetylhamaudol
|
Others
|
Cancer
|
|
3'-O-Acetylhamaudol, isolated from Angelica japonica roots, exhibits anti-tumor activity through dual actions, anti-angiogenesis and intestinal intraepithelial lymphocyte activation.
|
-
- HY-100775A
-
|
Setogepram
PBI-4050
|
GPR40
GPR84
|
Metabolic Disease
Inflammation/Immunology
|
|
Setogepram (PBI-4050) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84. Setogepram (PBI-4050) decreases renal, liver and pancreatic fibrosis. Setogepram (PBI-4050) exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions.
|
-
- HY-13516
-
|
Aloperine
|
Apoptosis
Autophagy
Filovirus
HIV
|
Cancer
Infection
Inflammation/Immunology
|
|
Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties.
Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China. Aloperine induces apoptosis and autophagy in HL-60 cells.
|
-
- HY-N4042
-
|
Hirsutenone
|
PI3K
ERK
|
Cancer
Inflammation/Immunology
|
|
Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity.
|
-
- HY-126350
-
|
CL2-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types.
|
-
- HY-126390
-
|
(E/Z)-BCI
NSC 150117
|
Phosphatase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
|
-
- HY-101282
-
|
Glutaminyl Cyclase Inhibitor 3
|
Amyloid-β
|
Neurological Disease
|
|
Glutaminyl Cyclase Inhibitor 3 (compound 212 ), a designed anti-Alzheimer’s compound, is a potent human Glutaminyl Cyclase (GC) inhibitor, with an IC50 of 4.5 nM. Glutaminyl Cyclase-IN-1 (compound 212) significantly reduced the brain concentrations of pyroform Aβ and total Aβ and restored cognitive functions.
|
-
- HY-N6074
-
|
Soyasapogenol B
|
Autophagy
Apoptosis
|
Cancer
|
|
Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer.
|
-
- HY-N0363A
-
|
(+)-Columbianetin acetate
(S)-Columbianetin acetate
|
Others
|
Infection
Inflammation/Immunology
|
|
(S)-Columbianetin acetate is an isomer of Columbianetin. Columbianetin is a phytoalexin associated with celery (Apium graveolens) resistance to pathogens during storage. Columbianetin exhibits excellent anti-fungal and anti-inflammatory activity.
|
-
- HY-W015820
-
|
Phthalide
|
Others
|
Inflammation/Immunology
|
|
Phthalide is a promising chemical scaffold with a potent anti-inflammatory efficacy. Phthalide can be used to synthesize a variety of phthalide derivatives including anti-inflammatory agent, antimicrobial, antioxidant.
|
-
- HY-N0332
-
-
- HY-N0370
-
|
Bergapten
5-Methoxypsoralen
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Bergapten is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. Bergapten is inhibitory towards mouse and human CYP isoforms.
|
-
- HY-B0348
-
|
Liranaftate
Piritetrate; M-732
|
Fungal
|
Infection
|
|
Liranaftate (Piritetrate) is a squalene epoxidase inhibitor with anti-fungicidal activities. Liranaftate can be used for the research of dermatophytes. Liranaftate also suppresses fungal element-promoted production of IL-8 and experimental inflammation.
|
-
- HY-N0737A
-
|
Harmine
Telepathine
|
DYRK
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
|
-
- HY-109011
-
|
Rosiptor
AQX-1125
|
Phosphatase
|
Cancer
|
|
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects. Rosiptor (AQX-1125) inhibits Akt phosphorylation, inflammatory mediator production and leukocyte chemotaxis in vitro.
|
-
- 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-136526
-
|
BCR-ABL-IN-3
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity.
|
-
- HY-15028
-
|
ATB-346
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
ATB-346 an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2) ATB-346 possesses antiinflammatory and antinociceptive activities.
|
-
- HY-122521
-
|
Sootepin D
|
NF-κB
|
Inflammation/Immunology
|
|
Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
|
-
- HY-126681
-
|
SC-VC-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SC-VC-PAB-MMAE is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker SC-VC-PAB.
|
-
- HY-113772
-
|
Inflachromene
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Inflachromene, a microglial inhibitor, binds to HMGB1 and HMGB2 and exerts anti-inflammatory effects. Inflachromene effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage. Inflachromene can be used for the research of neuroinflammatory disorders.
|
-
- HY-N0746
-
|
Oxysophocarpine
|
Others
|
Cancer
|
|
Oxysophocarpine is an alkaloid extracted from Siphocampylus verticillatus. Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems. Oxysophocarpine inhibits the growth and metastasis of oral squamous cell carcinoma (OSCC).
|
-
- HY-112434
-
-
- HY-15044
-
|
NU1025
|
PARP
|
Cancer
Neurological Disease
|
|
NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer drugs. NU1025 has anti-cancer and neuroprotective activity.
|
-
- HY-15136
-
-
- HY-123055
-
|
Adenosine dialdehyde
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Adenosine Dialdehyde, a purine nucleoside analogue, is an irreversible inhibitor of S-adenosylhomocysteine hydrolase (SAH) (IC50=40 nM). Adenosine Dialdehyde exhibits potent anti-tumor activity in vivo and can be used for the cancer research.
|
-
- HY-100846
-
|
JQEZ5
|
Histone Methyltransferase
|
Cancer
|
|
JQEZ5 is a potent and selective EZH2 lysine methyltransferase inhibitor. JQEZ5 SAM-competitive inhibition of polycomb repressive complex 2 (PRC2) with an IC50 of 80 nM. JQEZ5 has anti-tumor effects.
|
-
- HY-N0120A
-
|
Polydatin
Piceid
|
Autophagy
Apoptosis
Mitophagy
|
Inflammation/Immunology
Cancer
|
|
Polydatin (Piceid), extracted from the roots of Polygonum cuspidatum Sieb, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
|
-
- HY-15575
-
|
VcMMAE
mc-vc-PAB-MMAE
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
|
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
|
-
- HY-14393
-
|
Emodin
Frangula emodin
|
SARS-CoV
Casein Kinase
Autophagy
|
Cancer
|
|
Emodin (Frangula emodin), an anthraquinone derivative isolated from genus Rheum and Polygonum, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
|
-
- HY-17476
-
-
- HY-U00258
-
-
- HY-B0288B
-
-
- HY-N0885
-
-
- HY-109098
-
-
- HY-B0288A
-
-
- HY-U00361
-
-
- HY-101694
-
-
- HY-14937
-
-
- HY-B0376
-
|
Mecarbinate
Dimecarbin; Dimecarbine; Dimekarbin
|
HCV
|
Infection
|
|
Mecarbinate is an anti-hepatitis C virus (HCV) agent.
|
-
- HY-113162
-
-
- HY-17470
-
|
Mizoribine
NSC 289637; HE 69
|
HCV
SARS-CoV
|
Inflammation/Immunology
|
|
Mizoribine (NSC 289637), an imidazole nucleoside, inhibits HCV RNA replication with IC50 of approximately 100 μM for anti-HCV activity. Immunosuppressant. Mizoribine, an IMPDH inhibitor, inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively.
|
-
- HY-13599
-
|
Cladribine
2-Chloro-2′-deoxyadenosine; CldAdo; 2CdA
|
Adenosine Deaminase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.
|
-
- 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-N1438
-
|
Hydroxygenkwanin
7-O-Methylluteolin
|
Others
|
Cancer
|
|
Hydroxygenkwanin (7-O-Methylluteolin), a natural flavonoid compound, is one of the main components of Lilac Daphne. Hydroxygenkwanin has anti-oxidant ability, anti-glioma ability and anticancer effect.
|
-
- HY-N2303
-
-
- HY-100933
-
-
- HY-W052512
-
|
Antitrypanosomal agent 1
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 1 is a potent and selective trypanothione reductase (TR) inhibitor with an IC50 of 3.3 μM. Antitrypanosomal agent 1 inhibits glutathione reductase (GR) (IC50=64.8 μM) and T. brucei (EC50=1 μM). Antitrypanosomal agent 1 has anti-trypanosomal activity.
|
-
- HY-121515
-
|
DPM-1001
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 is a potent, specific, orally bioavailable and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM, an an analog of the specific PTP1B inhibitor trodusquemine (MSI-1436; IC50=600 nM). DPM-1001 has anti-diabetic property.
|
-
- HY-N2204
-
|
Swertiajaponin
|
Tyrosinase
|
Inflammation/Immunology
|
|
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
|
-
- HY-14443
-
|
XMD8-92
|
ERK
Epigenetic Reader Domain
|
Cancer
|
|
XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity.
|
-
- HY-117145
-
|
Thiophene-2
TP2
|
Bacterial
|
Infection
|
|
Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis and rapidly leads to mycobacterial cell death. Thiophene-2 is active against Mycobacterium tuberculosis with a MIC value of 1 μM, and has potent anti-tuberculosis activity.
|
-
- HY-N4005
-
|
Isoastilbin
|
Bacterial
Tyrosinase
|
Infection
Neurological Disease
|
|
Isoastilbin is a dihydroflavonol glycoside compound in Rhizoma Smilacis glabrae and Astragalus membranaceus. Isoastilbin inhibits glucosyltransferase (GTase) with an IC50 value of 54.3 μg/mL, and also inhibits tyrosinase activity. Isoastilbin shows neuroprotective, antioxidation, antimicrobial and anti-apoptotic properties and has the potential for Alzheimer’s disease research.
|
-
- HY-18666
-
|
D77
|
HIV
|
Infection
|
|
D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).
|
-
- HY-131708
-
|
FNDR-20123 free base
|
HDAC
Parasite
|
Infection
|
|
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations.
|
-
- HY-10443A
-
|
Balapiravir hydrochloride
Ro 4588161 hydrochloride; R1626 hydrochloride
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir hydrochloride (Ro 4588161 hydrochloride; R1626 hydrochloride) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir hydrochloride has anti-HCV activity.
|
-
- HY-124711
-
|
TBOPP
|
Others
|
Cancer
|
|
TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with high affinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors.
|
-
- HY-N0836
-
|
Jervine
11-Ketocyclopamine
|
Hedgehog
Smo
|
Cancer
Inflammation/Immunology
|
|
Jervine (11-Ketocyclopamine) is a potent Hedgehog (Hh) inhibitor with an IC50 of 500-700 nM. Jervine is a natural teratogenic sterodial alkaloid from rhizomes of Veratrum album. Jervine has anti-inflammatory and antioxidant properties.
|
-
- HY-10443
-
|
Balapiravir
Ro 4588161; R1626
|
HCV
DNA/RNA Synthesis
|
Infection
|
|
Balapiravir (Ro 4588161; R1626) is an orally active prodrug of a nucleoside analogue inhibitor of the RNA-dependent RNA polymerase (RdRp) of HCV (R1479; 4'-Azidocytidine). Balapiravir has anti-HCV activity.
|
-
- HY-A0213A
-
|
Tiludronate disodium
Tiludronic Acid disodium
|
Proton Pump
|
Inflammation/Immunology
|
|
Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-100003
-
|
ML-210
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
ML-210 is a selective and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity.
|
-
- HY-100865
-
|
BPR1K871
DBPR114
|
FLT3
|
Cancer
|
|
BPR1K871 is a potent and selective dual FLT3/AURKA inhibitor with IC50s of 19 nM and 22 nM for FLT3 and AURKA, respectively, acts as a preclinical development candidate for anti-cancer therapy.
|
-
- HY-106409
-
|
Tefinostat
CHR-2845
|
HDAC
|
Cancer
|
|
Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
|
-
- HY-B1227
-
-
- HY-N7045
-
|
Isosilybin B
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
|
-
- HY-12686
-
-
- HY-13859
-
|
Clevudine
L-FMAU
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase.
|
-
- HY-N3014
-
|
Bruceine D
|
Notch
Apoptosis
|
Cancer
Infection
|
|
Bruceine D is a Notch inhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitory activity.
|
-
- HY-129768
-
|
CMLD012072
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
CMLD012072 is an amidino-rocaglates and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012072 can induce RNA clamping of eIF4A1 and eIF4A2 and possess potent anti-neoplastic activity.
|
-
- HY-N0499
-
|
Cyanidin Chloride
IdB 1027
|
Others
|
Cancer
|
|
Cyanidin Chloride (IdB 1027), a subclass of anthocyanin, displays antioxidant and anti-carcinogenesis properties. Cyanidin Chloride (IdB 1027) inhibits osteoclast formation, hydroxyapatite resorption, and receptor activator of NF-κB ligand (RANKL)-induced osteoclast marker gene expression.
|
-
- HY-100219
-
|
CB1151
|
VD/VDR
|
Cancer
|
|
CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM.
|
-
- HY-N6246
-
|
Asperulosidic Acid
|
NF-κB
ERK
|
Cancer
Inflammation/Immunology
|
|
Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd. Asperulosidic Acid (ASPA) has anti-tumor, anti-oxidant, and anti-inflammatory activities.
ASPA is related to the inhibition of inflammatory cytokines (TNF-α, IL-6) and mediators via suppression of the NF-κB and mitogen-activated protein kinase (MAPK) signaling pathways.
|
-
- HY-121054
-
|
Chalcone
|
Bacterial
|
Cancer
Inflammation/Immunology
|
|
Chalcone is isolated from Glycyrrhizae inflata and used to synthesize chalcone derivatives. Chalcone derivatives possess varied biological and pharmacological activity, including anti-inflammatory, antioxidative, antibacterial, anticancer, and anti-parasitic activities.
|
-
- HY-N0808
-
-
- HY-101021
-
|
Ascochlorin
Ilicicolin D
|
STAT
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ascochlorin (Ilicicolin D), an isoprenoid antibiotic, mediates its anti-tumor effects predominantly through the suppression of STAT3 signaling cascade. Ascochlorin induces apoptosis. Anti-inflammatory activity.
|
-
- HY-N2533
-
-
- HY-N7176
-
|
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide
|
Interleukin Related
|
Inflammation/Immunology
|
|
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
|
-
- HY-N0731
-
-
- HY-128695
-
-
- HY-B2044
-
-
- HY-13571
-
-
- HY-N0213
-
-
- HY-B0645
-
-
- HY-U00043
-
-
- HY-101754
-
-
- HY-101743
-
-
- HY-15385
-
|
Imexon
BM 06002
|
Others
|
Cancer
|
|
Imexon (BM 06002) is an iminopyrrolidone aziridine with anti-cancer activity.
|
-
- HY-B1383
-
-
- HY-129179
-
|
Bcl-2/Bcl-xl inhibitor 1
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2/Bcl-xl inhibitor 1 (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Bcl-2/Bcl-xl inhibitor 1 exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively.
|
-
- HY-N2477
-
|
Taraxerol
|
Apoptosis
NF-κB
|
Cancer
Inflammation/Immunology
|
|
Taraxerol is isolated from Abroma augusta L, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis.
|
-
- HY-N0063
-
|
Punicalagin
|
HBV
|
Cancer
Infection
Metabolic Disease
|
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects.
|
-
- 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-A0203
-
|
Pentosan Polysulfate
|
HIV
|
Infection
Inflammation/Immunology
|
|
Pentosan Polysulfate is an orally bioavailable medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate also displays a potent and selective anti-HIV activity. Pentosan Polysulfatecan be used for the research of interstitial cystitis.
|
-
- HY-N1954
-
|
Protostemonine
|
Others
|
Inflammation/Immunology
|
|
Protostemonine is an active alkaloid mainly isolated from the roots of Stemona sesslifolia, with anti-inflammatory activity. Protostemonine has anti-inflammatory effects on asthma and gram-negative bacteria-induced acute lung injury.
|
-
- HY-16349
-
|
Nimorazole
K-1900
|
Parasite
Antibiotic
|
Infection
Cancer
|
|
Nimorazole (K-1900), a 2-nitroimidazole, is a hypoxic cell-radiation sensitizer. Nimorazole has anti-infective and anti-protozoal against trichomoniasis. Nimorazole has the potential for head and neck cancer.
|
-
- HY-B1892
-
-
- HY-100382
-
|
FPTQ
|
mGluR
|
Others
|
|
FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
|
-
- HY-130518
-
|
Cdc7-IN-6
|
CDK
|
Cancer
|
|
Cdc7-IN-6 (compound I-D) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity.
|
-
- HY-N7656
-
|
5,7,8-Trimethoxyflavone
Norwogonin 5,7,8-trimethyl ether
|
Others
|
Inflammation/Immunology
|
|
5,7,8-Trimethoxyflavone (Norwogonin 5,7,8-trimethyl ether), isolated from Andrographis echioides, inhibits NO with an IC50 of 39.1 μM. 5,7,8-Trimethoxyflavone has anti-inflammatory activity.
|
-
- HY-15005A
-
|
PSI-7976
|
HCV
|
Infection
|
|
PSI-7976 is the isomer of PSI-7977. PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-N4121
-
|
Isocurcumenol
|
Estrogen Receptor/ERR
Apoptosis
|
|
|
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
|
-
- HY-14882
-
|
Cenicriviroc
TAK-652; TBR-652
|
CCR
HIV
|
Infection
Endocrinology
|
|
Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
|
-
- HY-N2463
-
|
Kushenol E
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity.
|
-
- HY-N6674
-
|
Diazepinomicin
ECO-4601; TLN-4601; BU 4664L
|
Ras
Apoptosis
|
Cancer
|
|
Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models.
|
-
- HY-B0336
-
|
Pranoprofen
|
COX
Apoptosis
PGE synthase
|
Cancer
Inflammation/Immunology
|
|
Pranoprofen is a non-steroidal anti-inflammatory agent (NSAID) for the research of keratitis or other ophthalmology diseases. Pranoprofen inhibit COX-1 and COX-2 enzymes, thus blocking arachidonic acid converted to eicosanoids and reducing prostaglandins synthesis.
|
-
- HY-119447
-
|
Mavacoxib
|
COX
|
Inflammation/Immunology
|
|
Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
|
-
- 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-N6679A
-
|
10,11-Dehydrocurvularin
|
HSP
TGF-beta/Smad
|
Cancer
Infection
|
|
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity.
|
-
- HY-103018
-
|
Gusacitinib
ASN-002
|
JAK
Syk
|
Cancer
|
|
Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
|
-
- HY-128577
-
|
NIC3
|
Others
|
Cancer
|
|
NIC3 is a selective nucleus accumbens-associated protein-1 (NAC1) inhibitor, binds to the conserved Leu-90 of NAC1, prevents its homodimerization, and leads to proteasomal NAC1 degradation. Anti-cancer activity.
|
-
- HY-15187B
-
|
Filanesib TFA
ARRY-520 TFA
|
Kinesin
|
Cancer
|
|
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity.
|
-
- HY-108969
-
|
Pyrazoloacridine
NSC 366140; PD 115934
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment.
|
-
- HY-12122A
-
-
- HY-112316
-
|
BAY1238097
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-130607
-
-
- HY-N8085
-
|
Icariside F2
|
NF-κB
|
Inflammation/Immunology
|
|
Icariside F2 is a potent NF-κB inhibitor with an IC50 value of 16.25 μM. Icariside F2 is an aromatic glycoside isolated from the leaves of E. ulmoides Oliver. Icariside F2 has anti-inflammatory activity.
|
-
- HY-136065
-
|
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-N2181
-
|
Acetylshikonin
|
Cytochrome P450
AChE
|
Cancer
Inflammation/Immunology
|
|
Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity.
|
-
- HY-122022
-
|
JR-AB2-011
|
mTOR
|
Cancer
|
|
JR-AB2-011 is a selective mTORC2 inhibitor with an IC50 value of 0.36 μM. JR-AB2-011 inhibits mTORC2 activity by blocking Rictor-mTOR association (Ki: 0.19 μM). JR-AB2-011 has anti-glioblastoma multiforme (GBM) properties.
|
-
- HY-135671
-
-
- HY-112698
-
|
CA-5f
|
Autophagy
Apoptosis
|
Cancer
|
|
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
|
-
- HY-W041489
-
|
Chelidonic acid
|
NF-κB
Caspase
|
Inflammation/Immunology
Cancer
|
|
Chelidonic acid is a component of Chelidonium majus L., used as a mild analgesic, an antimicrobial, an acentral nervous system sedative. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM.
|
-
- HY-13765
-
-
- HY-B0275B
-
|
Oxytetracycline dihydrate
|
Bacterial
HSV
Antibiotic
Endogenous Metabolite
|
Infection
|
|
Oxytetracycline dihydrate is an antibiotic belonging to the tetracycline class. Oxytetracycline dihydrate potent inhibits Gram-negative and Gram-positive bacteria. Oxytetracycline dihydrate is a protein synthesis inhibitor and prevents the binding from aminoacil-tRNA to the complex m-ribosomal RNA. Oxytetracycline dihydrate also possesses anti-HSV-1 activity.
|
-
- HY-P0256
-
-
- HY-N7016A
-
-
- HY-N3005
-
|
Britannin
|
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Britannin, isolated from Inula aucheriana, is a sesquiterpene lactone. Britannin induces apoptosis and autophagy by activating AMPK regulated by ROS in liver cancer cells. Britannin has anti-proliferative and anti-inflammatory activities.
|
-
- HY-108472
-
-
- HY-B0154
-
-
- HY-N1984
-
|
Artemisic acid
Qing Hao acid; Artemisinic acid; Arteannuic acid
|
Bacterial
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect.
|
-
- HY-14289
-
|
Cimetidine
SKF-92334
|
Histamine Receptor
|
Cancer
Endocrinology
|
|
Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.
|
-
- HY-N7016
-
-
- 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-19827
-
|
Aeroplysinin 1
(+)-Aeroplysinin-1
|
Bacterial
HIV
Apoptosis
|
Cancer
Infection
|
|
Aeroplysinin 1 ((+)-Aeroplysinin-1), a secondary metabolite isolated from marine sponges, shows potent antibiotic effects on Gram-positive bacteria and exerts antiviral activity against HIV-1 (IC50=14.6 μM). Aeroplysinin 1 has anti-inflammatory, anti-angiogenic and anti-tumor activities. Aeroplysinin 1 induces apoptosis in endothelial cells.
|
-
- HY-N2040
-
|
(20R)-Protopanaxadiol
|
Others
|
Cancer
Infection
|
|
(20R)-Protopanaxadiol is a triterpenoid saponin metabolite of 20(R)-ginsenoside Rg3 in black ginseng. (20R)-Protopanaxadiol exhibits anti-tumor activity and cytotoxicity, and potently inhibits the growth of Helicobacter pylori.
|
-
- HY-A0213B
-
|
Tiludronate disodium hemihydrate
Tiludronic acid disodium hemihydrate
|
Proton Pump
|
Metabolic Disease
|
|
Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-135967
-
|
MTH1-IN-2
|
DNA/RNA Synthesis
|
Cancer
|
|
MTH1-IN-2 is a MutT homolog 1 (MTH1) inhibitor extracted from patent WO2016135138A1, Compound (6), MTH1-IN-2 can be used for the research of cancer. Anti-tumor activity.
|
-
- HY-N0072
-
|
Brazilin
|
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Brazilin is a red dye precursor obtained from the heartwood of several species of tropical hardwoods. Brazilin inhibits the cells proliferation, promotes apoptosis, and induces autophagy through the AMPK/mTOR pathway. Brazilin shows chondroprotective and anti-inflammatory activities.
|
-
- HY-112885A
-
-
- HY-B1799
-
|
Tolmetin
|
COX
|
Cancer
Inflammation/Immunology
|
|
Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID).
|
-
- HY-N0523
-
-
- HY-N0523A
-
-
- HY-19212
-
|
S-2474
|
COX
Lipoxygenase
|
Inflammation/Immunology
|
|
S-2474 is an inhibitor of COX-2 and 5-lipoxygenase (5-LO), with IC50s of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.
|
-
- HY-B0363
-
|
Nimesulide
R805
|
COX
|
Inflammation/Immunology
|
|
Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 nM-70 μM in a time-dependent manner, but it shows no effect on COX-1 (IC50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties.
|
-
- HY-19316
-
|
NU2058
O6-(Cyclohexylmethyl)guanine
|
CDK
|
Cancer
|
|
NU2058 (O6-(Cyclohexylmethyl)guanine) is a potent, competitive and guanine-based CDK inhibitor with IC50s of 17 μM and 26 μM for CDK2 and CDK1. NU2058 has anti-cancer activity.
|
-
- HY-112713
-
|
SMS2-IN-2
|
Others
|
Inflammation/Immunology
|
|
SMS2-IN-2 is a potent, highly selective and orally active sphingomyelin synthase 2 (SMS2) inhibitor, with IC50s of 100 nM and 56 μM for SMS2 and SMS1, respectively. Anti-chronic inflammatory activity.
|
-
- HY-B0421
-
-
- HY-N0156
-
-
- HY-N4312
-
-
- HY-N0796
-
-
- HY-19085
-
-
- HY-B2232
-
-
- HY-B0248
-
-
- HY-B0600
-
-
- HY-N0725
-
-
- HY-B1900
-
-
- HY-N6856
-
|
4-Hydroxycoumarin
|
Endogenous Metabolite
Bacterial
|
Infection
|
|
4-Hydroxycoumarin, a coumarin derivative, is one of the most versatile heterocyclic scaffolds and is frequently applied in the synthesis of various organic compounds. 4-Hydroxycoumarin possesses both electrophilic and nucleophilic properties. 4-Hydroxycoumarin derivatives are employed as the anticoagulant, antibacterial, antifungal, antiviral, antitumor, antiprotozoal, insecticidal, antimycobacterial, antimutagenic, antioxidant, anti-inflammatory agents, HIV protease inhibitors and tyrosine kinase inhibitors.
|
-
- HY-112616
-
|
NAMPT inhibitor-linker 2
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 2 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
|
-
- HY-129767
-
|
CMLD012612
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
CMLD012612 is an amidino-rocaglate containing a hydroxamate group and is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. CMLD012612 inhibits cell translation and is cytotoxic to NIH/3T3 cells with an IC50 value of 2 nM. CMLD012612 inhibits eukaryotic translation initiation by modifying the behavior of the RNA helicase (eIF4A) and possesses potent anti-neoplastic activity.
|
-
- 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-N7766
-
|
Rubropunctatin
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Rubropunctatin, an orange azaphilone pigment, is isolated from the extracts of Monascus pilosus-fermented rice (red-mold rice). Rubropunctatin has anti-inflammatory, immunosuppressive and antioxidative effects, and also exhibits anti-tumor activity.
|
-
- HY-A0203A
-
|
Pentosan Polysulfate Sodium
|
HIV
|
Infection
Inflammation/Immunology
|
|
Pentosan Polysulfate Sodium is an orally bioavailable, semi-synthetic medication with anti-inflammatory and pro-chondrogenic properties. Pentosan Polysulfate Sodium also is a potent and selective anti-HIV agent. Pentosan Polysulfate Sodium is used for the treatment of interstitial cystitis.
|
-
- HY-N2080
-
|
Songorine
|
GABA Receptor
|
Cancer
|
|
Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
|
-
- HY-N1353
-
-
- HY-N2010
-
-
- HY-N0295
-
|
Protocatechualdehyde
Catechaldehyde; Protocatechuic aldehyde; Rancinamycin IV
|
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
|
|
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent.
|
-
- HY-17463
-
|
Prednisolone
|
Glucocorticoid Receptor
Endogenous Metabolite
|
Endocrinology
|
|
Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.
|
-
- HY-P1717B
-
|
AMY-101 acetate
Cp40 acetate
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
|
AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
|
-
- 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-N2571
-
|
Corydine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine.
|
-
- HY-N0814
-
|
Phytic acid
Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
|
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-17474
-
|
Parecoxib
SC 69124
|
COX
|
Cancer
Inflammation/Immunology
|
|
Parecoxib (SC 69124) 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 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-133669
-
|
DDR1-IN-5
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity.
|
-
- HY-109523
-
|
Cerivastatin sodium
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-128588
-
|
STAT3-IN-3
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research.
|
-
- HY-N0462
-
|
Corilagin
|
Reverse Transcriptase
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Corilagin, a gallotannin, is isolated from Caesalpinia coriaria (Jacq.) Willd. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.
|
-
- HY-103022
-
|
Repotrectinib
TPX-0005
|
ROS
Trk Receptor
ALK
|
Cancer
|
|
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
|
-
- HY-P1717
-
|
AMY-101
Cp40
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
|
AMY-101 (Cp40), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 (Cp40) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
|
-
- HY-133670
-
|
DDR1-IN-6
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 9.7 nM. DDR1-IN-6 has anti-cancer activity.
|
-
- HY-108361
-
|
CCG-203971
|
Ras
|
Inflammation/Immunology
Cancer
|
|
CCG-203971 is a second-generation Rho/MRTF/SRF pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC50 =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC50 of 4.2 μM. Potential anti-metastasis Agent.
|
-
- HY-129458
-
|
Cerivastatin
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-N2532
-
|
Diphyllin
|
HIV
Proton Pump
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM. Diphyllin is active against vesicular stomatitis virus (VSV) and influenza virus. Diphyllin is a vacuolar type H +-ATPase (V-ATPase) inhibitor with an IC50 value of 17 nM and inhibits lysosomal acidification in human osteoclasts. Diphyllin inhibits NO production with an IC50 of 50 μM and has anticancer and anti-inflammatory activities.
|
-
- HY-124909
-
|
(6R)-FR054
|
Apoptosis
|
Cancer
|
|
(6R)-FR054 is an active isomer of FR054. FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect. FR054induces endoplasmic reticulum (ER) stress and a ROS-dependent apoptosis.
|
-
- HY-130794
-
|
ALK/ROS1-IN-1
|
ALK
ROS
|
Cancer
|
|
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
|
-
- HY-15321
-
|
Etoricoxib
MK-0663; L-791456
|
COX
|
Inflammation/Immunology
Cancer
|
|
Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
|
-
- HY-123242
-
|
FTI-2153
|
Farnesyl Transferase
|
Cancer
|
|
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.
|
-
- HY-14860A
-
-
- HY-110398
-
|
5,6,7-Trimethoxyflavone
Baicalein trimethyl ether
|
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
|
-
- HY-112436
-
|
Trk-IN-4
PF-6683324 isomer
|
Trk Receptor
|
Neurological Disease
|
|
Trk-IN-4 (PF-6683324 isomer) is a potent pan-Trk inhibitor in cell-based assays with
IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.
|
-
- HY-14860
-
|
1-Deoxynojirimycin
Duvoglustat
|
Glucosidase
PI3K
|
Metabolic Disease
|
|
1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.
|
-
- HY-126241
-
|
RV01
|
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
|
|
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
|
-
- HY-N6866
-
|
Gomisin N
|
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
Gomisin N, isolated from Schisandra chinensis, produces beneficial sedative and hypnotic bioactivity. Gomisin N has the potential for use in the treatment of allergy. Gomisin N is an anti-cancer drug candidate capable of inhibiting the proliferation and inducing the apoptosis in cancer.
|
-
- HY-122818
-
|
bpV(phen) trihydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-13693
-
-
- HY-N4097
-
|
Incensole
|
Others
|
Neurological Disease
|
|
Incensole, a 14-membered diterpenoid, is isolated from both essential oils and resins of frankincense. Incensole has shown anti-inflammatory and anti-depression activities due to their ability to activate ion channels in the brain to alleviate anxiety or depression.
|
-
- HY-W010271
-
-
- HY-N0677
-
-
- HY-N0188
-
|
Esculin
|
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
Esculin, a fluorescent coumarin glucoside, is an active ingredient of ash bark. Esculin ameliorates cognitive impairment in experimental diabetic nephropathy (DN), and exerts anti‑oxidative stress and anti‑inflammatory effects, via the MAPK signaling pathway.
|
-
- HY-P0256A
-
-
- HY-N0705
-
-
- HY-N0281
-
|
Daphnetin
7,8-Dihydroxycoumarin
|
EGFR
PKA
PKC
Autophagy
Parasite
|
Inflammation/Immunology
Cancer
|
|
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative isolated from plants of the Genus Daphne, is a protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin (7,8-dihydroxycoumarin) is a secondary metabolite of plants used in folk medicine to counter inflammatory and allergic diseases, also has has the potential in the treatment of coagulation disorders, rheumatoid arthritis with anti-malarian and anti-pyretic properties.
|
-
- HY-N0060B
-
|
(E)-Ferulic acid
(E)-Coniferic acid
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
|
(E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
|
-
- HY-N0619A
-
|
cis-Mulberroside A
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-N0212
-
|
Peimine
Verticine; Dihydroisoimperialine
|
Others
|
Inflammation/Immunology
|
|
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.
|
-
- HY-U00344
-
-
- HY-B0779
-
-
- HY-128689
-
-
- HY-N6941
-
-
- HY-16509
-
-
- HY-N2123
-
-
- HY-P0183
-
-
- HY-B0370
-
-
- HY-101488
-
-
- HY-U00337
-
-
- HY-U00169
-
-
- HY-B0270
-
-
- HY-107427
-
|
PF-3644022
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
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- HY-15486
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Salubrinal
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Phosphatase
HSV
Autophagy
Apoptosis
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Cancer
Infection
Inflammation/Immunology
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Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
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- HY-112615
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NAMPT inhibitor-linker 1
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NAMPT
Drug-Linker Conjugates for ADC
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Cancer
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NAMPT inhibitor-linker 1 is a drug-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
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- HY-B1640
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Ethacrynic acid
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Gutathione S-transferase
NF-κB
Calcium Channel
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Cancer
Inflammation/Immunology
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Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
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- HY-129943
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Benzothiohydrazide
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Bacterial
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Infection
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Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2).
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- HY-N3074
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Hexahydrofarnesyl acetone
6,10,14-Trimethyl-2-pentadecanone
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Bacterial
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Infection
Inflammation/Immunology
|
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Hexahydrofarnesyl acetone (6,10,14-Trimethyl-2-pentadecanone), a sesquiterpene isolated from Launaea mucronata, is the major constituents of the essential oil. Hexahydrofarnesyl acetone has antibacterial, anti-nociceptive and anti-inflammation activities.
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-
- HY-N0595
-
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Genistin
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
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Estrogen Receptor/ERR
Apoptosis
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Cancer
Metabolic Disease
|
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Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway.
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-
- HY-N0677B
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-
- HY-N7148
-
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γ-Tocopherol
D-γ-Tocopherol; (+)-γ-Tocopherol
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COX
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Cancer
Inflammation/Immunology
|
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γ-Tocopherol (D-γ-Tocopherol) is a potent cyclooxygenase (COX) inhibitor. γ-Tocopherol is a naturally occurring form of Vitamin E in many plant seeds, such as corn oil and soybeans. γ-Tocopherol possesses antiinflammatory properties and anti-cancer activity.
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-
- HY-122312
-
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BAY-8002
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Monocarboxylate Transporter
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Cancer
|
|
BAY-8002 is a potent, selective, orally active inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 of 85 nM in the MCT1-expressing DLD-1 cells, displays excellent selectivity against MCT4. Anti-tumor activity.
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- HY-N2230
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