Search Result
Results for "Antigen-presenting Cell Function Inhibitors" in MCE Product Catalog:
9691
Inhibitors & Agonists
31
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-118355
-
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-U00439
-
-
- HY-124040
-
BI-1950
|
Integrin
|
Inflammation/Immunology
|
BI-1950 is a highly potent lymphocyte function associated antigen-1 (LFA-1) inhibitor. LFA-1 is an essential component in normal immune system function and a target for drug discovery.
|
-
- HY-16697
-
CID 16020046
|
GPR55
|
Cancer
|
CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.
|
-
- HY-W012037
-
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-D0195
-
-
- HY-101903A
-
BMS-309403 sodium
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-101903
-
BMS-309403
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-14771A
-
-
- HY-14771
-
-
- HY-100196
-
Pyrroloquinoline quinone
PQQ; Methoxatin
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Pyrroloquinoline quinone (PQQ), a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone is an essential nutrient for mammals and is important for immune function.
|
-
- HY-109128
-
Danicamtiv
MYK-491
|
Myosin
|
Cancer
|
Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.
|
-
- HY-100196A
-
Pyrroloquinoline quinone disodium salt
PQQ disodium salt; Methoxatin disodium salt
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Pyrroloquinoline quinone disodium salt, a redox co-factor, is an anionic, redox-cycling orthoquinone. Pyrroloquinoline quinone disodium salt is isolated from cultures of methylotropic bacteria and tissues of mammals. Pyrroloquinoline quinone disodium salt is an essential nutrient for mammals and is important for immune function.
|
-
- HY-110086
-
RWJ 50271
|
Integrin
|
Inflammation/Immunology
|
RWJ 50271 is an selective and orally active inhibitor of lymphocyte function-associated antigen-1/intercellular adhesion molecule-1(LFA-1/ICAM-1) interaction with an IC50 of 5.0 μM (HL60 cells). RWJ 50271 inhibits LFA-1/ICAM-1-mediated cell adhesion.
|
-
- HY-13813
-
Blebbistatin
|
Myosin
|
Others
|
Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function.
|
-
- HY-19694
-
BRD7552
|
Others
|
Endocrinology
|
BRD7552, a potent PDX1 transcription factor inducer, upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases insulin expression. PDX1 is a key transcription factor involved in pancreas development and β cell function.
|
-
- HY-N7119
-
Cimicifugoside
|
Others
|
Inflammation/Immunology
|
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function.
|
-
- HY-131005
-
-
- HY-P0121
-
ReACp53
|
MDM-2/p53
|
Cancer
|
ReACp53 could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.
|
-
- HY-135827
-
MSC2360844
|
PI3K
|
Cancer
Inflammation/Immunology
|
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases.
|
-
- HY-P1271
-
Catestatin
|
nAChR
|
Cardiovascular Disease
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-135827A
-
-
- HY-P1271A
-
Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-135813
-
LtaS-IN-1
|
Bacterial
|
Infection
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-N1419
-
Vaccarin
|
AMPK
|
Metabolic Disease
|
Vaccarin is an active flavonoid glycoside associated with various biological functions. Vaccarin significantly promote wound healing and endothelial cells and fibroblasts proliferation in the wound site. Vaccarin ameliorates insulin resistance and steatosis by activating the AMPK signaling pathway.
|
-
- HY-121879
-
-
- HY-100894
-
Biotin-VAD-FMK
|
Caspase
|
Cancer
|
Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
|
-
- HY-126666
-
PNU-159682 carboxylic acid
|
ADC Cytotoxin
|
Cancer
Inflammation/Immunology
|
PNU-159682 carboxylic acid (compound 53) is a potent ADCs cytotoxin and encodes a member of the C-type lectin/C-type lectin-like domain (CTL/CTLD) superfamily. PNU-159682 carboxylic acid has protein fold and diverse functions, such as cell adhesion, cell-cell signalling, glycoprotein turnover, and roles in inflammation and immune response.
|
-
- HY-111969
-
BT18
|
Others
|
Neurological Disease
|
BT18 is a molecule mimic with function similar to glial cell line-derived neurotrophic factor (GDNF). BT18 shows an effect on GDNF family receptor GFRα1 and RET receptor tyrosine kinase RetA function.
|
-
- HY-124653
-
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-U00439A
-
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-125957
-
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-N0712
-
Typhaneoside
|
Autophagy
|
Inflammation/Immunology
Cardiovascular Disease
|
Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
|
-
- HY-P3139
-
TPP-1
|
PD-1/PD-L1
|
Cancer
|
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function.
|
-
- HY-P0276
-
GIP, human
Gastric Inhibitory Peptide (GIP), human
|
Insulin Receptor
|
Metabolic Disease
|
GIP, human, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
|
-
- HY-P0276A
-
GIP, human TFA
Gastric Inhibitory Peptide (GIP), human TFA
|
Insulin Receptor
|
Metabolic Disease
|
GIP, human TFA, a peptide hormone consisting of 42 amino acids, is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP, human TFA acts as an incretin hormone released from intestinal K cells in response to nutrient ingestion.
|
-
- HY-P3139A
-
TPP-1 TFA
|
PD-1/PD-L1
|
Cancer
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function.
|
-
- HY-117071
-
-
- HY-N0667
-
-
- HY-W017443
-
-
- HY-121793
-
Roemerine
(-)-Roemerine
|
P-glycoprotein
|
Cancer
|
Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells.
|
-
- HY-19344
-
Lifitegrast
SAR 1118; SHP-606
|
Integrin
|
Inflammation/Immunology
|
Lifitegrast (SAR 1118) is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
|
-
- HY-P0300
-
-
- HY-19373
-
-
- HY-B0228
-
-
- HY-117383
-
NGI-1
ML414
|
Virus Protease
|
Cancer
|
NGI-1 (ML414) is a potent oligosaccharyltransferase (OST) inhibitor, directly targeting and blocking the function of the OST catalytic subunits STT3A and STT3B. NGI-1 is a cell permeable inhibitor and can effectively reduce virus infectivity without affecting cell viability.
|
-
- HY-N6727
-
Gliotoxin
Aspergillin
|
Apoptosis
PKA
NF-κB
Bacterial
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
|
-
- HY-107193
-
Bacitracin
|
Bacterial
Antibiotic
|
Infection
|
Bacitracin is a polypeptide antibiotic used for staphylococcal infections. Bacitracin functions as an inhibitor of cell wall biosynthesis through its binding to the undecaprenyl pyrophosphate. The combination of bacitracin with other antibiotics has been efficient to be used as a topical agent.
|
-
- HY-14397A
-
Indomethacin sodium hydrate
Indometacin sodium hydrate
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
Indomethacin sodium hydrate (Indometacin sodium hydrate) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin sodium hydrate disrupts autophagic flux by disturbing the normal functioning of lysosomes.
|
-
- HY-14397
-
Indomethacin
Indometacin
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
|
-
- HY-136583
-
28-Epirapamycin
|
Others
|
Others
|
28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells.
|
-
- HY-50730
-
Asparagusic acid
|
Parasite
|
Infection
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-115292
-
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-137497
-
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-16673
-
PSN632408
|
GPR119
|
Metabolic Disease
|
PSN632408, a selective, orally active GPR119 agonist, shows similar potency to OEA at both recombinant mouse and human GPR119 receptors (EC50=5.6 and 7.9 uM, respectively). PSN632408 can stimulate β-cell replication and improve islet graft function. PSN632408 has the potential for the research of obesity and related metabolic disorders.
|
-
- HY-136110
-
-
- HY-109030
-
-
- HY-134654
-
MRTX849 analog 24
|
Others
|
Cancer
|
MRTX849 analog 24 is an alkyne-containing click probe analogue of KRAS G12C inhibitor MRTX849, which is used to research MRTX849 function.
|
-
- 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-113965
-
CUR61414
|
Hedgehog
Smo
Apoptosis
|
Inflammation/Immunology
|
CUR61414 is a novel, potent and cell permeable Hedgehog signaling pathway inhibitor (IC50 =100-200 nM). CUR61414 is a small-molecule aminoproline class compound and selectively binds to smoothened (Smo) with a Ki value of 44 nM. CUR-61414 can induce apoptosis in cancer cells without affecting neighboring non-tumor cells.
|
-
- HY-N4058
-
Helichrysetin
|
Apoptosis
|
Cancer
|
Helichrysetin, isolated from the flowers of Helichrysum odoratissimum, is an ID2 (inhibitor of DNA binding 2) inhibitor, and suppresses DCIS (ductal carcinoma in situ) formation. Helichrysetin possess strong inhibitory effects on cell growth and is capable of inducing apoptosis in A549 cells.
|
-
- HY-B0293A
-
Butoconazole
|
Fungal
|
Infection
|
Butoconazole, an imidazole antifungal agent, is active against Candida spp. and effective against vaginal infections due to Candida albicans. Butoconazole is presumed to function as other imidazole derivatives via inhibition of steroid synthesis.
|
-
- HY-17561
-
G-418 disulfate
Geneticin sulfate; Antibiotic G-418 sulfate
|
Bacterial
Antibiotic
|
Infection
|
G-418 disulfate (Geneticin sulfate), is an aminoglycoside antibiotic, inhibits protein synthesis in eukaryotes and prokaryotes. G-418 disulfate is commonly used as a selective agent for eukaryotic cells.
|
-
- HY-136610
-
Chlorpyrifos-oxon
|
AChE
|
Neurological Disease
|
Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.
|
-
- HY-101606
-
-
- HY-131344
-
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-15564
-
AR 231453
|
GPR119
|
Metabolic Disease
|
AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
|
-
- 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-14397S
-
Indomethacin-D4
Indometacin-D4
|
COX
Autophagy
|
Cancer
Inflammation/Immunology
|
Indomethacin-D4 (Indometacin-D4) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
|
-
- HY-131140
-
BD750
|
JAK
STAT
|
Cancer
Inflammation/Immunology
|
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
|
-
- HY-B0103
-
-
- HY-B0103A
-
-
- HY-110088
-
SCH529074
|
MDM-2/p53
|
Cancer
|
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).
|
-
- 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-N1255
-
Scoulerine
(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
|
Cancer
|
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells.
|
-
- HY-18728
-
-
- HY-17473
-
Embelin
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
|
-
- HY-B1430
-
-
- HY-U00441
-
DPBQ
|
MDM-2/p53
Apoptosis
|
Cancer
|
DPBQ activates p53 and triggers apoptosis in a polyploid-specific manner, but does not inhibit topoisomerase or bind DNA. DPBQ elicits expression and phosphorylation of p53 and this effect is specific to tetraploid cells.
|
-
- HY-101255
-
ODQ
|
Guanylate Cyclase
Apoptosis
|
Cancer
|
ODQ is a potent and selective soluble guanylyl cyclase (sGC, nitric oxide-activated enzyme) inhibitor. ODQ enhances the pro-apoptotic effects of Cisplatin in human mesothelioma cells.
|
-
- 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-19555
-
Seco Rapamycin
Secorapamycin A
|
Others
|
Others
|
Seco Rapamycin (Secorapamycin A) is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-136394
-
Diafenthiuron
|
Others
|
Others
|
Diafenthiuron is a thiourea compound commonly used pesticide. Diafenthiuron inhibits mitochondrial functioning in insect pests.
|
-
- HY-119881
-
-
- HY-133770
-
-
- HY-N0774
-
Isofraxidin
|
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
|
-
- HY-110249
-
CINPA1
|
Others
|
Metabolic Disease
|
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
|
-
- HY-P1784
-
Secretin, canine
|
Src
|
Endocrinology
|
Secretin, canine is an endocrine hormone that stimulates the secretion of bicarbonate-rich pancreatic fluids. Secretin, canine can regulates gastric chief cell function and paracellular permeability in canine gastric monolayers by a Src kinase-dependent pathway.
|
-
- HY-12346
-
FH1
NSC 12407; BRD-K4477
|
Others
|
Others
|
FH1 (NSC 12407) enhances hepatocyte functions, and promotes the differentiation of induced pluripotent stem (iPS)-derived hepatocytes toward a phenotype more mature and the maturation of well-differentiated cultures of hepatocyte-like cells (iHeps).
|
-
- HY-125039
-
N-Acetyl lysyltyrosylcysteine amide
|
Glutathione Peroxidase
|
Neurological Disease
Cardiovascular Disease
|
N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation.
|
-
- HY-120504
-
N-Acetyltyramine
|
Bacterial
|
Cancer
Infection
|
N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells.
|
-
- HY-113216
-
-
- HY-16689
-
VU 0240551
|
Potassium Channel
|
Others
|
VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission.
|
-
- HY-114657A
-
Benproperine phosphate
|
Arp2/3 Complex
|
Cancer
Inflammation/Immunology
|
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis.
|
-
- HY-N8441
-
Neriifolin
17β-Neriifolin
|
Na+/K+ ATPase
Apoptosis
|
Cancer
Inflammation/Immunology
|
Neriifolin, a CNS-penetrating cardiac glycoside, is an inhibitor of the Na +, K +-ATPase. Neriifolin can target beclin 1, inhibits the formation of LC3-associated phagosomes and ameliorates experimental autoimmune encephalomyelitis (EAE) development. Neriifolin induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells[2.
|
-
- HY-15989A
-
SM-164 Hydrochloride
|
IAP
Apoptosis
|
Cancer
|
SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- HY-15989
-
SM-164
|
IAP
Apoptosis
|
Cancer
|
SM-164 is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP.
|
-
- HY-N6811
-
1-Octacosanol
|
Others
|
Others
|
1-Octacosanol is a straight-chain aliphatic 28-carbon fatty alcohol with well-known anti-fatigue function.
|
-
- HY-B1221
-
Flufenamic acid
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-N6717
-
Tentoxin
|
Others
|
Infection
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-135336A
-
-
- 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-100739
-
RA190
|
Proteasome
|
Cancer
|
RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
|
-
- 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-B1305
-
-
- HY-116767
-
BLT-1
Block lipid transport-1
|
HCV
|
Metabolic Disease
Inflammation/Immunology
|
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor. BLT-1 has pro-inflammatory functions through neutrophil recruitment.
|
-
- HY-19356
-
Rocaglamide
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-105019A
-
Melflufen hydrochloride
Melphalan flufenamide hydrochloride
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-105019
-
Melflufen
Melphalan flufenamide
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
Melflufen (Melphalan flufenamide), a dipeptide prodrug of Melphalan, is an alkylating agent. Melflufen shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen induces irreversible DNA damage and cytotoxicity in MM cells.
|
-
- HY-122295
-
Dehydroleucodine
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Dehydroleucodine is a sesquiterpene lactone isolated from Gynoxys verrucosa. Dehydroleucodine is a mast cell stabilizer that inhibits tmast cell degranulation induced by compound 48/80. Dehydroleucodine inudces cells apoptosis, and has gastric ulcer inhibition and antileukemic effects.
|
-
- HY-15583
-
-
- HY-100750
-
-
- HY-10366
-
-
- HY-135328
-
-
- HY-N1403
-
Tigogenin
|
Others
|
Metabolic Disease
|
Tigogenin, one of steroidal sapogenins, is widely used for synthesizing steroid drugs. Tigogenin inhibits adipocytic differentiation and induces osteoblastic differentiation in mouse bone marrow stromal cells.
|
-
- HY-122716
-
PTGR2-IN-1
|
Others
|
Others
|
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
|
-
- HY-109187A
-
Posenacaftor sodium
PTI-801 sodium
|
CFTR
|
Inflammation/Immunology
|
Posenacaftor (PTI-801) sodium is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor sodium is used for the research of cystic fibrosis (CF).
|
-
- HY-135801
-
Arachidonyl alcohol
|
Others
|
Metabolic Disease
|
Arachidonyl alcohol is a long-chain primary fatty alcohol. Arachidonyl alcohol is used as a substrate for the production of several ether lipids possessing beneficial functions.
|
-
- HY-122181A
-
OTS186935 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells.
|
-
- HY-13811
-
NSC697923
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
|
-
- HY-P0073
-
-
- HY-B0030
-
D-Cycloserine
|
iGluR
Bacterial
Antibiotic
|
Infection
Neurological Disease
|
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research.
|
-
- HY-101030
-
MBM-17
|
Apoptosis
|
Cancer
|
MBM-17 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM. It effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-100965
-
-
- HY-122470
-
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-B1493
-
Bentiromide
|
Others
|
Endocrinology
|
Bentiromide is a peptide that is broken down in the pancreas by chymotrypsin. The bentiromide test is an excellent means of confirming the diagnosis of pancreatic exocrine insufficiency by outpatient test of chymotrypsin function.
|
-
- HY-N2459
-
Peonidin chloride
YGM-6 chloride
|
COX
|
Cancer
|
Peonidin chloride is an O-methylated anthocyanidin that functions as a primary plant pigment, endowing purplish-red hues to flowers such as the peony, from which it takes its name, as well as berries and vegetables. Peonidin chloride exhibits chemopreventive, as well as anti-inflammatory activities on cancer cells in vitro, blocking COX-2 expression and transformation in JB6 P+ mouse epidermal cells.
|
-
- HY-130680
-
Syk-IN-3
|
Syk
|
Cancer
|
Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
|
-
- HY-136123
-
Tubulin inhibitor 8
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
Tubulin inhibitor 7
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
|
-
- HY-136121
-
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-18621A
-
OTS514 hydrochloride
|
TOPK
Apoptosis
|
Cancer
|
OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.
|
-
- HY-10655A
-
Palosuran hydrochloride
ACT-058362 hydrochloride
|
Urotensin Receptor
|
Cardiovascular Disease
|
Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats.
|
-
- HY-10655
-
Palosuran
ACT-058362
|
Urotensin Receptor
|
Cardiovascular Disease
|
Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats.
|
-
- HY-B1005
-
8-Hydroxyquinoline
8-Quinolinol
|
Bacterial
Antibiotic
|
Cancer
|
8-Hydroxyquinoline (8-Hydroxyquinoline) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-50910
-
Temsirolimus
CCI-779
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model.
|
-
- HY-N3415
-
Kumatakenin
|
Apoptosis
|
Cancer
|
Kumatakenin, a flavonoid that is isolated from cloves shows the effect of inducing apoptosis in ovarian cancer cells.
|
-
- HY-13624A
-
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13624
-
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-N7695
-
Physalin B
|
Apoptosis
Autophagy
|
Cancer
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro.
|
-
- HY-100579
-
Ferrostatin-1
|
Ferroptosis
Fungal
|
Cancer
|
Ferrostatin-1, a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibit cell death. Antifungal Activity.
|
-
- HY-18621
-
OTS514
|
TOPK
Apoptosis
|
Cancer
|
OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells. OTS514 induces cell cycle arrest and apoptosis.
|
-
- HY-N0469
-
-
- HY-N2599
-
Taraxerol acetate
|
COX
Apoptosis
|
Cancer
|
Taraxerol acetate is a COX-1 and COX-2 inhibitor with IC50 values of 116.3 μM and 94.7 μM, respectively. Taraxerol acetate the has the anticancer potential and induces cell apoptosis.
|
-
- HY-19980
-
PRIMA-1Met
APR-246
|
MDM-2/p53
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
PRIMA-1Met restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1Met also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
|
-
- HY-100360
-
MS049
|
Histone Methyltransferase
|
Cancer
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
|
-
- HY-100360A
-
MS049 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells.
|
-
- HY-B0795
-
MHY1485
|
mTOR
Autophagy
|
Cancer
|
MHY1485 is a potent cell-permeable mTOR activator that targets the ATP domain of mTOR. MHY1485 inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.
|
-
- HY-138407
-
-
- HY-16981
-
SB-332235
|
CXCR
|
Inflammation/Immunology
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.
|
-
- HY-B1014
-
-
- HY-122534
-
Mensacarcin
|
Mitochondrial Metabolism
ADC Cytotoxin
Apoptosis
|
Cancer
|
Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
|
-
- HY-124771
-
RH01386
|
Others
|
Metabolic Disease
|
RH01386 is a small molecule that can prevent ER stress-induced β cell dysfunction and death, and inhibits proapoptotic gene expression. RH01386 restores ER stress-impaired glucose-stimulated insulin secretion responses. RH01386 has the potential for type 2 diabetes treatment.
|
-
- 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-14454
-
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-129390
-
Orelabrutinib
ICP-022
|
Btk
|
Cancer
|
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
|
-
- HY-19992
-
3-Bromopyruvic acid
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities.
|
-
- HY-101030A
-
MBM-17S
|
Apoptosis
|
Cancer
|
MBM-17S is a potent NIMA-related kinase 2 (Nek2) inhibitor, with an IC50 of 3 nM. MBM-17S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-17S shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-122590
-
Glabrescione B
|
Gli
|
Cancer
|
Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells.
|
-
- HY-B0132A
-
Norfloxacin hydrochloride
MK-0366 hydrochloride
|
Bacterial
Antibiotic
|
Infection
|
Norfloxacin hydrochloride (MK-0366 hydrochloride) is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria, which functions by inhibiting DNA gyrase.
|
-
- HY-B0132
-
-
- HY-W010483A
-
-
- HY-W010483
-
-
- HY-B0325
-
-
- HY-13686
-
PQ401
|
IGF-1R
Apoptosis
|
Cancer
|
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
|
-
- HY-13917A
-
PND-1186 hydrochloride
VS-4718 hydrochloride; SR-2516 hydrochloride
|
FAK
Apoptosis
|
Cancer
|
PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis.
|
-
- HY-13917
-
PND-1186
VS-4718; SR-2516
|
FAK
Apoptosis
|
Cancer
|
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis.
|
-
- HY-135858
-
SARS-CoV-IN-3
|
SARS-CoV
Parasite
HIV
|
Infection
|
SARS-CoV-IN-3 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-3 shows anti-Coronavirus activity with an EC50 of 3.6 μM in Vero cells. SARS-CoV-IN-3 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 11.7 and 20.4 nM; and IC90s of 29.19 and 56 nM; respectively. SARS-CoV-IN-3 reduces HIV-1-induced cytopathic effect with an EC50 of 10 μM in MT-4 cells.
|
-
- HY-P0023
-
Cyclo(-RGDfK)
|
Integrin
|
Cancer
|
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-15284
-
Prasugrel
PCR 4099
|
P2Y Receptor
|
Cardiovascular Disease
|
Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-15284A
-
Prasugrel hydrochloride
PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and prodrug, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-138540
-
1-Dodecylimidazole
N-Dodecylimidazole
|
Fungal
|
Cancer
|
1-Dodecylimidazole (N-Dodecylimidazole) is a lysosomotropic detergent and a cytotoxic agent. 1-Dodecylimidazole causes cell death by its acid-dependent accumulation in lysosomes, disruption of the lysosomal membrane, and releaseof cysteine proteases into the cytoplasm. 1-Dodecylimidazole has hypocholesterolaemic activity and broad-spectrum antifungal activity.
|
-
- HY-P3143A
-
BMSpep-57 hydrochloride
|
PD-1/PD-L1
|
Cancer
|
BMSpep-57 hydrochloride is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 hydrochloride binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 hydrochloride facilitates T cell function by in creasing IL-2 production in PBMCs.
|
-
- HY-135745
-
Sulfentrazone
|
Others
|
Others
|
Sulfentrazone is a phenyl triazolinone herbicide used for control of certain broadleaf and grass weed species. Sulfentrazone inhibits protoporphyrinogen oxidase, resulting in the disruption of lipid cell membranes.
|
-
- 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-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-18681
-
Voxelotor
GBT 440
|
Others
|
Cardiovascular Disease
|
Voxelotor (GBT 440) is a potent inhibitor of haemoglobin S (HbS) polymerization. Voxelotor has the potential for sickle cell disease (SCD) treatment.
|
-
- HY-B0158
-
-
- HY-114436
-
MRTX-1257
|
Ras
|
Cancer
|
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
|
-
- HY-P0023A
-
Cyclo(-RGDfK) TFA
|
Integrin
|
Cancer
|
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface.
|
-
- HY-N0732
-
Jolkinolide B
|
Apoptosis
|
Cancer
|
Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells.
|
-
- HY-135328S
-
-
- HY-136348
-
ML338
|
Bacterial
|
Infection
|
ML338 is a selective small molecule inhibitor probe of non-replicating Mycobacterium tuberculosis bacilli and is against the non-replicating M. tuberculosis with IC90 and IC99 values of 1 μM and 4 μM, respectively by CFU. ML338 is a invaluable tool for identifying both essential functions and vulnerabilities of the M. tuberculosis bacilli in the nutrient deprivation states. ML338 can be used for the study of M. tuberculosis chemotherapy.
|
-
- HY-119339
-
SX-682
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2. SX-682 can block tumor myeloid-derived suppressor cells (MDSCs) recruitment and enhance T cell activation and antitumor immunity.
|
-
- HY-N0729
-
Linoleic acid
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism .
|
-
- HY-118630
-
Vacuolin-1
|
PIKfyve
Autophagy
|
Cancer
|
Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca 2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation.
|
-
- HY-18563
-
4-Phenoxybenzylamine
|
HCV
|
Infection
|
4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
|
-
- HY-B0873
-
Uniconazole
|
Cytochrome P450
|
Others
|
Uniconazole is a plant growth regulator that functions by inhibiting cytochrome P450 707As (Ki=68 nM), a family of enzymes that catabolize Abscisic acid, and thus, suppress gibberellin and sterol biosynthesis.
|
-
- HY-108618
-
BC11-38
|
Phosphodiesterase (PDE)
|
Endocrinology
|
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
|
-
- HY-50896
-
Erlotinib
CP-358774; NSC 718781; OSI-774
|
EGFR
Autophagy
|
Cancer
|
Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
|
-
- HY-N7006
-
-
- HY-15597
-
Salinomycin
Procoxacin
|
Bacterial
Wnt
β-catenin
Mitophagy
Autophagy
Apoptosis
Antibiotic
|
Cancer
|
Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin (Procoxacin) shows selective activity against human cancer stem cells.
|
-
- HY-N5021
-
Anhydrosafflor yellow B
AHSYB
|
Others
|
Neurological Disease
|
Anhydrosafflor yellow B (AHSYB) is a quinochalcone C-glycoside isolated from Carthamus tinctorius. Anhydrosafflor yellow B inhibits ADP-induced platelet aggregation, exhibits significant anti-oxidative effects in vitro, and possesses certain activity against H2O2-induced cytotoxicity in cultured PC12 cells and primary neuronal cells.
|
-
- HY-15284B
-
Prasugrel (Maleic acid)
PCR 4099 (Maleic acid)
|
P2Y Receptor
|
Cardiovascular Disease
|
Prasugrel (PCR 4099) Maleic acid is a thienopyridine and prodrug, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-B0517
-
Mepivacaine
|
Sodium Channel
|
Neurological Disease
|
Mepivacaine is an amide-type local anesthetic agent. Mepivacaine binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-137471
-
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-135276
-
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.
|
-
- HY-70002S
-
-
- HY-103269
-
BAI1
|
Bcl-2 Family
Apoptosis
|
Cancer
|
BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death.
|
-
- HY-N0854
-
Alisol F
|
HBV
|
Infection
|
Alisol F is a triterpene isolated from Alisma orientalis, has immunosuppressive and anti-virus functions. Alisol F exhibits inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the HepG2.2.15 cell line with an IC50 of 0.6 μM.
|
-
- HY-N6985
-
Baccatin III
|
Others
|
Cancer
|
Baccatin III is a natural product isolated from Pacific yew tree and related species. Baccatin III reduces tumor progression by inhibiting the accumulation and suppressive function of MDSCs.
|
-
- HY-18959
-
CWP232228
|
β-catenin
Wnt
|
Cancer
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
|
-
- HY-19747
-
HPOB
|
HDAC
Apoptosis
|
Cancer
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
|
-
- 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-136312
-
17-DMAP-GA
|
Others
|
Cancer
|
17-DMAP-GA, a Geldanamycin (HY-15230) analogue, is an inhibitor of HSP90. 17-DMAP-GA causes cell cycle abnormalities.
|
-
- HY-19826
-
-
- HY-N6076
-
Tenuifoliside A
|
ERK
|
Neurological Disease
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-12072
-
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-W028690
-
DNMDP
|
Phosphodiesterase (PDE)
|
Cancer
|
DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
|
-
- HY-B0294
-
Flubendazole
|
Parasite
Microtubule/Tubulin
Apoptosis
|
Cancer
Infection
|
Flubendazole is a safe and efficacious anthelmintic drug, which is widely used for anthelmintic to human, rodents and ruminants. Flubendazole exerts anticancer activities by mechanisms including inhibition of microtubule function. Flubendazole induces p53-mediated apoptosis and arrests G2/M cell cycle.
|
-
- HY-N0530
-
Dryocrassin ABBA
Dryocrassin
|
Influenza Virus
Bacterial
|
Infection
|
Dryocrassin ABBA (Dryocrassin) is a flavonoid natural product derived from Dryopteris crassirhizoma, with antiviral and antibacterial activities. Dryocrassin ABBA exhibits antiviral activity against H5N1 avian influenza virus. Dryocrassin ABBA inhibits the coagulase activity of Staphylococcus aureus vWbp. Dryocrassin ABBA suppresses immunostimulatory function of dendritic cells and prolongs skin allograft survival.
|
-
- HY-P3143
-
BMSpep-57
|
PD-1/PD-L1
|
Cancer
|
BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs.
|
-
- HY-135008
-
J14
|
Reactive Oxygen Species
|
Cancer
|
J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death.
|
-
- HY-129937A
-
GNE-987
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
|
-
- HY-D0889
-
-
- HY-133570
-
17-AEP-GA
|
HSP
ADC Cytotoxin
|
Cancer
|
17-AEP-GA, an HSP90 antagonist, is a potent inhibitor of glioblastoma cell proliferation, survival, migration and invasion. ADCs Toxin.
|
-
- HY-131394
-
5-Hydroxymethyl-2’-deoxycytidine
5hmdC
|
Others
|
Cancer
|
5-Hydroxymethyl-2’-deoxycytidine (5hmdC) is an oxidation derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA. 5-Hydroxymethyl-2’-deoxycytidine may serve as a marker of irreversibly damaged cells.
|
-
- HY-14273
-
Isavuconazole
BAL-4815; RO-0094815
|
Fungal
Cytochrome P450
Antibiotic
|
Infection
|
Isavuconazole (BAL-4815) is a triazole prodrug with antifungal activity against yeasts, molds, and dimorphic fungi. Isavuconazole inhibits ergosterol biosynthesis and results in the disruption of fungal membrane structure and function. Isavuconazole is a moderate inhibitor of CYP3A4.
|
-
- HY-136528
-
RA-9
|
Deubiquitinase
Apoptosis
|
Cancer
|
RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
|
-
- HY-103349
-
PETCM
|
Caspase
Apoptosis
|
Cancer
|
PETCM is an activator of caspase-3 and acts as an cytochrome c (cyto c)-dependent manner. PETCM promotes Apaf-1 oligomerization and induces cell apoptosis in HeLa cells.
|
-
- HY-101519
-
BETd-260
ZBC 260
|
PROTAC
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
BETd-260 (ZBC 260) is a potent PROTAC BET degrader, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-W011303
-
Phytosphingosine
|
Apoptosis
|
Cancer
|
Phytosphingosine is a phospholipid and has anti-cancer activities. Phytosphingosine induces cell apoptosis via caspase 8 activation and Bax translocation in cancer cells.
|
-
- HY-108523
-
LG100754
UVI 2112
|
RAR/RXR
|
Metabolic Disease
|
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR.
|
-
- HY-N0671
-
Rhapontin
Rhaponiticin
|
Apoptosis
|
Cancer
|
Rhapontin (Rhaponiticin), a component of rhubarb (Rheum officinale Baillon), induces apoptosis resulting in suppression of proliferation of human stomach cancer KATO III cells.
|
-
- HY-10591
-
-
- HY-111360
-
SPL-707
|
γ-secretase
|
Inflammation/Immunology
|
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
|
-
- HY-B0551
-
-
- HY-B0551A
-
-
- HY-125729
-
-
- HY-14743B
-
Golotimod hydrochloride
SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-18702
-
Targocil
|
Bacterial
|
Infection
|
Targocil functions as a bacteriostatic inhibitor of wall teichoic acid (WTA) biosynthesis which can inhibit the growth of methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) with MIC90s of 2 μg/ mL for both MRSA and MSSA.
|
-
- HY-U00283
-
-
- HY-14291
-
-
- HY-136453
-
-
- HY-N2026A
-
Propylparaben sodium
Propyl parahydroxybenzoate sodium; Propyl 4-hydroxybenzoate sodium
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
Propylparaben sodium (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben sodium is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben sodium disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben sodium also decreases sperm number and motile activity in rats.
|
-
- HY-104037
-
Cintirorgon
LYC-55716
|
ROR
|
Cancer
|
Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
|
-
- HY-N2026
-
Propylparaben
Propyl parahydroxybenzoate; Propyl 4-hydroxybenzoate
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats.
|
-
- HY-16558
-
Butein
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
|
-
- HY-134771
-
YM-341619
AS1617612
|
STAT
|
Inflammation/Immunology
|
YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.
|
-
- 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-111838A
-
ZZW-115 hydrochloride
|
Apoptosis
|
Cancer
|
ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-111838
-
ZZW-115
|
Apoptosis
|
Cancer
|
ZZW-115 is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 induces tumor cell death by necroptosis and apoptosis. Anticancer activity.
|
-
- HY-101029
-
MBM-55
|
Apoptosis
|
Cancer
|
MBM-55 is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55 shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55 shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-15649
-
UNC1215
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
UNC1215 is a potent and selective inhibitor for the methyllysine (Kme) reading domain function of L3MBTL3 with a Kd value of 120 nM and an IC50 of 40 nM. UNC1215 has the potential to treat malignant brain tumor.
|
-
- HY-130122
-
MG-277
|
PROTAC
Apoptosis
|
Cancer
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
|
-
- HY-N1039A
-
Manool
|
Others
|
Cancer
|
Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
|
-
- HY-12501A
-
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-N7707
-
Sandacanol
|
Apoptosis
|
Cancer
|
Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells.
|
-
- HY-N2534
-
Karanjin
|
AMPK
Apoptosis
|
Cancer
|
Karanjin is a major active furanoflavonol constituent of Fordia cauliflora. Karanjin induces GLUT4 translocation in skeletal muscle cells by increasing AMPK activity. Karanjin can induce cancer cell death through cell cycle arrest and enhance apoptosis.
|
-
- HY-B0517A
-
Mepivacaine hydrochloride
|
Sodium Channel
|
Neurological Disease
|
Mepivacaine hydrochloride is an amide-type local anesthetic agent. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.
|
-
- HY-19555A
-
Seco Rapamycin sodium salt
Secorapamycin A monosodium
|
Others
|
Others
|
Seco Rapamycin sodium salt is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-136895
-
AZ12672857
|
Prostaglandin Receptor
|
Cancer
|
AZ12672857 is an orally active inhibitor of EphB4 (IC50=1.3 nM) and Src kinases. AZ12672857 shows good inhibition of proliferation of c-Src transfected 3T3 cells (IC50=2 nM) as well as autophosphorylation of EphB4 in transfected CHO-K1 cells (IC50=9 nM).
|
-
- HY-131018
-
-
- HY-107523
-
WAY-213613
|
EAAT2
|
Neurological Disease
|
WAY-213613 is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s are 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.
|
-
- HY-107523A
-
WAY-213613 hydrochloride
|
EAAT2
|
Neurological Disease
|
WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC50 of 85 nM EAAT2. It displays 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s are 5 and 3.8 μM, respectively). WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function.
|
-
- HY-14521
-
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-14521B
-
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-100490
-
Rilmenidine
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
|
-
- HY-127170
-
3-Hydroxycoumarin
|
Others
|
Others
|
3-hydroxycoumarin is a potent and redox inhibitor of human 15-LOX-1. 3-hydroxycoumarin is recently demonstrated to protect sea urchin reproductive cells against ultraviolet B damage.
|
-
- HY-14291A
-
-
- HY-127039
-
-
- HY-127034
-
-
- HY-15162
-
Monomethyl auristatin E
MMAE; SGD-1010
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
|
-
- HY-134653
-
5-Ph-IAA
|
Others
|
Cancer
|
5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.
|
-
- HY-W013274
-
CPTH2
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).
|
-
- HY-B1468
-
-
- HY-15036
-
Diclofenac
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac 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, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-15038
-
Diclofenac potassium
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac potassium 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, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac potassium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-123943
-
STING agonist-4
|
STING
|
Cancer
|
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function.
|
-
- HY-12892
-
SKI-178
|
SPHK
Apoptosis
|
Cancer
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines.
|
-
- HY-101867
-
AU1235
|
Bacterial
|
Cancer
Infection
|
AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane.
|
-
- HY-135856
-
SARS-CoV-IN-2
|
SARS-CoV
Parasite
HIV
|
Infection
|
SARS-CoV-IN-2 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-2 shows anti-Coronavirus activity with an EC50 of 1.9 μM in Vero cells. SARS-CoV-IN-2 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 21.5 and 30 nM; and IC90s of 51.0 and 99.9 nM; respectively. SARS-CoV-IN-2 reduces HIV-1-induced cytopathic effect with an EC50 of 2.9 μM in MT-4 cells. Antimalarial and Antiviral Activities.
|
-
- HY-124675
-
MYCMI-6
NSC354961
|
c-Myc
Apoptosis
|
Cancer
|
MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis.
|
-
- HY-N0805A
-
Alisol B
|
Others
|
Metabolic Disease
|
Alisol B is a potentially novel therapeutic compound for bone disorders by targeting the differentiation of osteoclasts as well as their functions.
|
-
- HY-10018
-
-
- HY-N0230
-
-
- HY-131058
-
Muscotoxin A
|
ADC Cytotoxin
|
Cancer
|
Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
|
-
- HY-15036A
-
Diclofenac diethylamine
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac diethylamine 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, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-15037
-
Diclofenac Sodium
GP 45840
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac Sodium (GP 45840) 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, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-121282A
-
Mepazine hydrochloride
Pecazine hydrochloride
|
MALT1
Apoptosis
|
Cancer
|
Mepazine hydrochloride (Pecazine hydrochloride) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine hydrochloride affects viability of ABC-DLBCL cells by enhancing apoptosis.
|
-
- HY-D0226
-
Quinizarin
1,4-Dihydroxyanthraquinone
|
DNA/RNA Synthesis
Fungal
|
Cancer
Infection
|
Quinizarin (1,4-Dihydroxyanthraquinone), a part of the anticancer agents such as Doxorubicin, Daunorubicin, and Adriamycin, interacts with DNA by intercalating mode (Kd=86.1 μM). Quinizarin is used as a fungicide and pesticide chemical and has shown the ability to inhibit tumor cell growth.
|
-
- HY-121282
-
Mepazine
Pecazine
|
MALT1
Apoptosis
|
Cancer
|
Mepazine (Pecazine) is a potent and selective MALT1 protease inhibitor with IC50s of 0.83 and 0.42 μM for GSTMALT1 full length and GSTMALT1 325-760, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
|
-
- 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-B0640A
-
-
- 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-129388B
-
CC-90011 benzenesulfonate
LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-14743
-
Golotimod
SCV 07; Gamma-D-glutamyl-L-tryptophan
|
Bacterial
STAT
|
Infection
Inflammation/Immunology
|
Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
|
-
- HY-12290
-
Arg-Gly-Asp-Ser
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function, decreases systemic inflammation via inhibition of collagen-triggered activation of leukocytes and attenuates expression of inflammatory cytokines, iNOS and MMP-9.
|
-
- HY-14373
-
CB30865
ZM 242421
|
NAMPT
|
Cancer
|
CB30865 (ZM 242421) is a nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with potent cytotoxicity. CB30865 is highly potent against a variety of human tumour cell lines (IC50 values in the 1-10 nM range).
|
-
- HY-12501
-
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-N0128
-
Sclareol
|
Apoptosis
|
Cancer
|
Sclareol is isolated from Salvia sclarea with anticarcinogenic activity. Sclareol shows strong cytotoxic activity against mouse leukemia (P-388), human epidermal carcinoma (KB) cells and human leukemia cell lines. Sclareol induces cell apoptosis.
|
-
- HY-101029A
-
MBM-55S
|
Ribosomal S6 Kinase (RSK)
DYRK
Apoptosis
|
Cancer
|
MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.
|
-
- HY-129995
-
TSHR antagonist S37b
|
TSH Receptor
|
Endocrinology
|
TSHR antagonist S37b is the less effective enantiomer of TSHR antagonist S37a (HY-129995A). TSHR antagonist S37b shows only a minor effect for thyrotropin receptor (TSHR) inhibition. TSHR antagonist S37b can be used for the research of thyroid function.
|
-
- HY-101058
-
-
- HY-B0640
-
-
- HY-19867A
-
Burixafor hydrobromide
TG-0054 hydrobromide
|
CXCR
|
Inflammation/Immunology
Cardiovascular Disease
Endocrinology
|
Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well water soluble anti-angiogenic drug that is of potential value in treating choroid neovascularization. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction.
|
-
- HY-101076
-
L-690488
|
Phosphatase
|
Metabolic Disease
|
L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330.
|
-
- HY-137295
-
Ingenol 3,20-dibenzoate
|
PKC
Apoptosis
|
Inflammation/Immunology
|
Ingenol 3,20-dibenzoate is a potent protein kinase C (PKC) isoform-selective agonist. Ingenol 3,20-dibenzoate induces selective translocation of nPKC-delta, -epsilon, and -theta and PKC-mu from the cytosolic fraction to the particulate fraction and induces morphologically typical apoptosis through de novo synthesis of macromolecules. Ingenol 3,20-dibenzoate increases the IFN-γ production and degranulation by NK cells, especially when NK cells are stimulated by NSCLC cells.
|
-
- HY-129388
-
CC-90011 Methylbenzenesulfonate
LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity.
|
-
- HY-70002
-
-
- HY-113914
-
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-P1066
-
Apelin-17(human, bovine)
|
HIV
|
Infection
|
Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-122181B
-
OTS186935 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells.
|
-
- HY-B1897A
-
Menadione bisulfite sodium
Menadione sodium bisulfite; Vitamin K3 sodium bisulfite
|
Others
|
Infection
|
Menadione bisulfite (sodium) is used as an agent to induce acute oxidative stress, and to function as a plant-defense activator against several pathogens.
|
-
- HY-16998
-
SR2211
|
ROR
|
Inflammation/Immunology
|
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
|
-
- HY-136373
-
Metazachlor
|
Others
|
Others
|
Metazachlor is a herbicide of the chloroacetamide class. Metazachlor is an inhibitor of the synthesis of long chain fatty acids and has an effect on cell division or tissue differentiation in the germinating and emerging weed target species.
|
-
- HY-120139
-
KMH-233
|
Others
|
Cancer
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
|
-
- HY-14674
-
CP-724714
|
EGFR
Apoptosis
|
Cancer
|
CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
|
-
- HY-19617A
-
EGFR-IN-1 hydrochloride
|
EGFR
|
Cancer
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-135869
-
Mito-apocynin (C11)
|
Mitochondrial Metabolism
|
Neurological Disease
|
Mito-apocynin (C11), an orally active mitochondria-targeted triphenylphosphonium (TPP)-based compound, is synthesized by conjugating the Apocynin moiety with a TPP + cation. Mito-apocynin (C11) selectively targets mitochondria, and shows neuroprotective effect. Mito-apocynin (C11) prevents hyposmia and corrects deficits in motor function.
|
-
- HY-B2028
-
Propargite
|
Parasite
|
Infection
|
Propargite is a pesticide used to kill mites. Propargite induces β-cell necrosis preceded by DNA damage. Propargite induces MIN6 cell death with an IC50 of 1 μM.
|
-
- HY-119906
-
Conglobatin
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo.
|
-
- HY-13963
-
ZCL278
|
Ras
|
Cancer
|
ZCL278 is a selective Cdc42 modulator that directly binds to Cdc42 and inhibits its functions with Kd of 11.4 μM for Cdc42-ZCL278 affinity in surface plasmon resonance (SPR) experiment.
|
-
- HY-108847
-
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-18981
-
Decursin
(+)-Decursin
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
Decursin ((+)-Decursin) is a cytotoxic agent and a potent protein kinase C activator from the Root of Angelica gigas. Decursin inhibits tumor growth, migration, and invasion in gastric cancer by down-regulating CXCR7 expression. Decursin inhibits the growth of HepG2 cells via Hippo/YAP signaling pathway.
|
-
- HY-121638
-
CU-3
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-16196
-
ENMD-1198
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-109198
-
Zandelisib
|
PI3K
|
Cancer
|
Zandelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic.
|
-
- HY-15398A
-
5,6-trans-Vitamin D3
5,6-trans-Cholecalciferol; 5,6-trans-Colecalciferol
|
VD/VDR
|
Metabolic Disease
|
5,6-trans-Vitamin D3 (5,6-trans-Cholecalciferol;5,6-trans-Colecalciferol) is a photoproduct of vitamin D3. Vitamin D3 is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
|
-
- HY-P1066A
-
Apelin-17(human, bovine) TFA
|
HIV
|
Infection
|
Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-B0503
-
2-Thiouracil
Thiouracil
|
Others
|
Endocrinology
Cancer
|
2-Thiouracil (Thiouracil) is an antithyroid compound. 2-Thiouracil can function as a highly specific melanoma seeker. 2-Thiouracil is a selective inhibitor of neuronal nitric oxide synthase (nNOS) with a Ki of 20 μM.
|
-
- 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-N7496
-
Odoroside A
|
Apoptosis
|
Cancer
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-122181
-
OTS186935
|
Histone Methyltransferase
|
Cancer
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells.
|
-
- HY-108640
-
HLI373
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-108640A
-
HLI373 dihydrochloride
|
MDM-2/p53
Parasite
Apoptosis
|
Cancer
Infection
|
HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
|
-
- HY-118607
-
VU041
|
Potassium Channel
|
Infection
|
VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5 μM and 1.7 μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7 μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function.
|
-
- HY-P0002A
-
-
- HY-B1204
-
-
- HY-P0002
-
-
- HY-W015878
-
-
- HY-Y0271
-
Urea
Carbamide; Carbonyldiamide
|
Endogenous Metabolite
|
Cardiovascular Disease
Cancer
|
Urea is a powerful protein denaturant via both direct and indirect mechanisms. A potent emollient and keratolytic agent. Used as a diuretic agent. Blood urea nitrogen (BUN) has been utilized to evaluate renal function. Widely used in fertilizers as a source of nitrogen and is an important raw material for the chemical industry.
|
-
- HY-125531
-
Dactylorhin A
|
Others
|
Others
|
Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
|
-
- HY-19617B
-
EGFR-IN-1 TFA
|
EGFR
|
Cancer
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-19617
-
EGFR-IN-1
|
EGFR
|
Cancer
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.
|
-
- HY-15178
-
Oglemilast
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-P9949
-
Reslizumab
Sch 55700
|
Interleukin Related
|
Inflammation/Immunology
|
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab inhibits IL-5-dependent cell proliferation, with an IC50 value of approximately 91.1pM. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively.
|
-
- HY-N4010
-
Iriflophenone
|
Others
|
Cancer
|
Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation.
|
-
- HY-125209A
-
TH5427 hydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells.
|
-
- HY-129997
-
Luteolinidin chloride
|
Others
|
Inflammation/Immunology
|
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
|
-
- HY-N0656
-
Usnic acid
|
Bacterial
|
Cancer
Infection
|
Usnic acid, a lichen-derived secondary metabolite, has a unique dibenzofuran skeleton. Usnic acid has excellent anticancer and antimicrobial properties. Usnic acid significantly inhibits RANKL-mediated osteoclast formation and function by reducing the transcriptional and translational expression of NFATc1.
|
-
- HY-N4114
-
Picrocrocin
|
Apoptosis
|
Cancer
|
Picrocrocin, an apocarotenoid found in the flowers of Cochliobolus sativus. Picrocrocin shows anticancer effect. Picrocrocin exhibits growth inhibitory effects against SKMEL-2 human malignant melanoma cells.
|
-
- HY-N0069
-
Solamargine
Solamargin; δ-Solanigrine
|
P-glycoprotein
Apoptosis
|
Cancer
|
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition. Solamargine significantly inhibits migration and invasion of HepG2 cells by down-regulating MMP-2 and MMP-9 expression and activity.
|
-
- HY-102022
-
α-Galactosylceramide
α-GalCer; KRN7000
|
Others
|
Cancer
Inflammation/Immunology
|
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
|
-
- 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-135855
-
SARS-CoV-IN-1
|
SARS-CoV
Parasite
|
Infection
|
SARS-CoV-IN-1 is an effective inhibitor of SARS-CoV replication. SARS-CoV-IN-1 shows anti-Coronavirus activity with an EC50 of 4.9 μM in Vero cells. SARS-CoV-IN-1 inhibits the 3D7 and W2 strains of P. falciparum with IC50s of 15.4 and 133.2 nM; and IC90s of 25.7 and 459.1 nM; respectively. Antimalarial and antiviral activities.
|
-
- HY-B0887
-
Permethrin
NRDC-143
|
Parasite
|
Infection
|
Permethrin (NRDC-143) is an insecticide, acaricide, and insect repellent; functions as a neurotoxin, affecting neuron membranes by prolonging sodium channel activation.
|
-
- HY-B0325S
-
-
- HY-B1409
-
-
- HY-N7634
-
Tectol
|
Farnesyl Transferase
Parasite
|
Cancer
Infection
|
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM. Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM.
|
-
- HY-136594
-
BODIPY aminoacetaldehyde
BAAA
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
|
-
- HY-N0595
-
Genistin
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Metabolic Disease
|
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.
|
-
- HY-110147A
-
SSM3 tetraTFA
|
Others
|
Infection
|
SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro.
|
-
- HY-12830
-
M-110
|
Pim
|
Cancer
|
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
|
-
- HY-W011916
-
Muramic acid
|
Bacterial
|
Others
|
Muramic acid is a component in many Gram-positive bacterial cell walls, as marker for Gram-positive bacteria.
|
-
- HY-18773
-
Oct3/4-inducer-1
|
Oct3/4
|
Inflammation/Immunology
|
Oct3/4-inducer-1 (compound 2) is a potent Oct3/4 inducer. Oct3/4-inducer-1 promotes expression and stabilization of Oct3/4, and enhances its transcriptional activity in diverse human somatic cells.
|
-
- HY-131042
-
NNMTi
|
Others
|
Metabolic Disease
|
NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues. NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice.
|
-
- HY-112234
-
L-Sepiapterin
Sepiapterin
|
Endogenous Metabolite
|
Cancer
|
L-Sepiapterin (Sepiapterin) is a precursor of the endothelial nitric oxide synthase (eNOS) cofactor tetrahydrobiopterin (BH4). L-Sepiapterin improves endothelial dysfunction in small mesenteric arteries from db/db mice, and induces angiogenesis. L-Sepiapterin inhibits cell proliferation and migration of ovarian cancer cells via down-regulation of p70 S6K-dependent VEGFR-2 expression.
|
-
- 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-12378
-
BQ-123
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-P0206
-
-
- HY-113061
-
Pseudouridine
|
Endogenous Metabolite
|
Others
|
Pseudouridine, the most abundant modified nucleoside in non-coding RNAs, enhances the function of transfer RNA and ribosomal RNA by stabilizing RNA structure.
|
-
- HY-W013706
-
-
- HY-B0923
-
Danthron
Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- HY-U00382
-
-
- HY-100746
-
STF-62247
|
Autophagy
|
Cancer
|
STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively).
|
-
- HY-131961
-
Triciferol
|
VD/VDR
HDAC
|
Cancer
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
|
-
- HY-125801
-
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-100608
-
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-102084
-
LMT-28
|
Interleukin Related
|
Inflammation/Immunology
|
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
|
-
- HY-100612
-
T16Ainh-A01
|
Chloride Channel
|
Others
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-15160A
-
TAK-960 hydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-15160B
-
TAK-960 dihydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-15160
-
TAK-960
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-11062
-
Icilin
AG-3-5
|
TRP Channel
|
Cancer
Neurological Disease
|
Icilin (AG-3-5) is an agonist of nonselective cation channel TRPM8, with antiproliferative activity. Icilin activates currents only in wild type TRPM8 and in the presence of Ca 2+. Icilin can induce G1 arrest in prostate cancer cells.
|
-
- HY-N4192
-
Toringin
|
Others
|
Cancer
Cardiovascular Disease
|
Toringin, a bioflavonoid, is isolated from the bark of Docyniopsis tschonoski. Toringin progressively decreases not only the cis-effect of the expanded CTG repeats but cytotoxicity as well. Exposure to isosakuranetin, Toringin rescues PC12 neuronal cells. Flavonoids are efficacious for ameliorating the RNA gain of function caused by expanded CTG repeats, and have various biological activities and beneficial actions against cancers, coronary heart disease, among other pathologies.
|
-
- HY-12378A
-
BQ-123 TFA
|
Endothelin Receptor
|
Cardiovascular Disease
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
|
-
- HY-12646A
-
Rhosin
|
Ras
Apoptosis
|
Cancer
|
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
|
-
- HY-12646
-
Rhosin hydrochloride
|
Ras
Apoptosis
|
Cancer
|
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
|
-
- HY-N7676
-
Marein
|
AMPK
HDAC
|
Metabolic Disease
Neurological Disease
Cardiovascular Disease
|
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC50 of 100 µM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.
|
-
- HY-103661
-
BI-6C9
|
Mitochondrial Metabolism
Apoptosis
|
Neurological Disease
|
BI-6C9 is a highly specific BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from mitochondrial apoptosis inducing factor (AIF) release and caspase-independent cell death in neurons.
|
-
- HY-15160C
-
TAK-960 monohydrochloride
|
Polo-like Kinase (PLK)
|
Cancer
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.
|
-
- HY-N8098
-
Pulchinenoside E2
|
Others
|
Cancer
|
Pulchinenoside E2 (Compound 8) is a triterpene saponin isolated from the roots of Pulsatilla chinensis. Pulchinenoside E2 shows cytotoxic to HL-60 cells with an IC50 value of 2.6 µg/mL.
|
-
- HY-B1777
-
-
- HY-N0785
-
-
- HY-10984
-
Pomalidomide
CC-4047
|
Ligand for E3 Ligase
Apoptosis
|
Cancer
|
Pomalidomide is the third-generation immunomodulatory agent, functions through interacting with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
|
-
- HY-B2172
-
Vitamin K
|
Others
|
Cardiovascular Disease
|
Vitamin K is a group of fat soluble vitamins, important for the function of numerous proteins within the body, such as the coagulation factors, osteocalcin and matrix-Gla protein.
|
-
- HY-W007355
-
-
- HY-101953
-
-
- HY-113485
-
Melanin
|
Endogenous Metabolite
|
Others
|
Melanin is a unique pigment with myriad functions. It is multifunctional, providing defense against environmental stresses such as ultraviolet (UV) light, oxidizing agents and ionizing radiation.
|
-
- HY-B0315
-
-
- HY-115452
-
G5-7
|
JAK
Apoptosis
|
Cancer
|
G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr 1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.
|
-
- HY-129328
-
Magnesium glycinate
Magnesium bisglycinate; Magnesium diglycinate
|
Others
|
Others
|
Magnesium glycinate (Magnesium bisglycinate), the magnesium salt of glycine, is a nutrient supplement. Magnesium glycinate has satisfactory physico-chemical properties and bioactivities. Metal glycinate chelates are formed by glycine and metal compounds through chemical reactions. Magnesium is an essential mineral that plays a critical role in the human body. Magnesium takes part in the process of energy metabolism and assists the maintenance of normal muscle function.
|
-
- HY-N0569
-
-
- HY-15473A
-
MLN120B dihydrochloride
ML120B dihydrochloride
|
IKK
|
Cancer
Inflammation/Immunology
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-N3446
-
IVHD-valtrate
|
Apoptosis
|
Cancer
|
IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research.
|
-
- HY-135774
-
6-Hydroxybenzbromarone
|
Drug Metabolite
Phosphatase
|
Cardiovascular Disease
|
6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting.
|
-
- HY-114356
-
BPI-9016M
|
c-Met/HGFR
|
Cancer
|
BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
|
-
- HY-119198
-
NSC745885
|
Apoptosis
Histone Methyltransferase
|
Cancer
|
NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers.
|
-
- HY-B0932
-
Levocarnitine propionate hydrochloride
L-Propionylcarnitine chloride; ST-261
|
Others
|
Others
|
Levocarnitine propionate hydrochloride (L-Propionylcarnitine chloride; ST-261) is used to treat the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.
|
-
- HY-19642
-
Glesatinib
MGCD265
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
|
-
- HY-19642A
-
Glesatinib hydrochloride
MGCD265 hydrochloride
|
TAM Receptor
c-Met/HGFR
|
Cancer
|
Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
|
-
- HY-110177
-
SP-100030
|
NF-κB
|
Inflammation/Immunology
|
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
|
-
- HY-W011338
-
Benzyl butyl phthalate
|
Aryl Hydrocarbon Receptor
|
Cancer
|
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
|
-
- HY-13007A
-
PF-3758309 hydrochloride
|
PAK
Apoptosis
|
Cancer
|
PF-3758309 hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
|
-
- HY-19313
-
LLY-507
|
Histone Methyltransferase
|
Cancer
|
LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes.
|
-
- HY-13007
-
PF-3758309
|
PAK
Apoptosis
|
Cancer
|
PF-3758309 is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
|
-
- HY-18522
-
AA26-9
|
Phospholipase
|
Metabolic Disease
|
AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
|
-
- HY-113962
-
7α,25-Dihydroxycholesterol
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
-
- HY-12011
-
HA14-1
|
Bcl-2 Family
|
Cancer
|
HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
|
-
- HY-136498
-
T-705RMP
|
Drug Metabolite
|
Infection
|
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
|
-
- HY-101437
-
-
- HY-111804
-
-
- HY-14781
-
-
- HY-N2530
-
-
- HY-100490B
-
Rilmenidine phosphate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-19686
-
Ipsapirone
TVX Q 7821 free base
|
5-HT Receptor
|
Neurological Disease
|
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function.
|
-
- HY-16399
-
Pladienolide B
|
Apoptosis
|
Cancer
|
Pladienolide B is a potent cancer cell growth inhibitor that targets the SF3B1 subunit of the spliceosome. Pladienolide B exerts antitumor activities mediated through the inhibition of pre-mRNA splicing. Pladienolide B induces apoptosis.
|
-
- HY-P1208
-
PG-931
|
Melanocortin Receptor
|
Inflammation/Immunology
|
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
|
-
- HY-P1208A
-
PG-931 TFA
|
Melanocortin Receptor
|
Inflammation/Immunology
|
PG-931 TFA, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R(IC50=2.4 nM). PG-931 TFA can reverse haemorrhagic shock and prevent multiple organ damage in vivo.
|
-
- HY-103697
-
Gardiquimod
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-118341
-
Clitocine
|
Apoptosis
Bcl-2 Family
|
Cancer
|
Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
|
-
- HY-12319
-
Cardiogenol C
|
β-catenin
Wnt
|
Cancer
|
Cardiogenol C is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
|
-
- HY-12319A
-
Cardiogenol C hydrochloride
|
β-catenin
Wnt
|
Cardiovascular Disease
|
Cardiogenol C hydrochloride is a potent cell-permeable pyrimidine inducer which prompts the differentiation of ESCs into cardiomyocytes (EC50=100 nM). Cardiogenol C hydrochloride also acts cardiomyogenic on already lineage-committed progenitor cell types with a limited degree of plasticity. Cardiogenol C hydrochloride is a useful cardiomyogenic agent and can be used as a tool to improve cardiac repair by cell transplantation therapy in animal models.
|
-
- HY-N6802
-
Tigloylgomisin H
|
Others
|
Cancer
|
Tigloylgomisin H is a lignan isolated from the fruits of S. chinensis, can induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H functions as a monofunctional inducer that specifically upregulates phase II detoxification enzyme NQO1 through the NF-E2-related factor 2 (Nrf2)-ARE pathway, thus represents a potential liver cancer prevention agent.
|
-
- HY-130709
-
PROTAC CDK2/9 Degrader-1
|
PROTAC
CDK
|
Cancer
|
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 µM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand.
|
-
- HY-129099
-
N-Desmethyltamoxifen
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-129099A
-
N-Desmethyltamoxifen hydrochloride
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
|
Cancer
|
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.
|
-
- HY-N7262
-
Hydroxyvalerenic acid
|
Others
|
Cancer
|
Hydroxyvalerenic acid is isolated from Verbena officinalis, has a low toxicity with IC50 values of 123 and 165 μM against GLC4 and COLO 320 cells, respectively.
|
-
- HY-15838
-
ID-8
|
DYRK
|
Cancer
|
ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
|
-
- HY-13894
-
Tyrphostin AG1296
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
|
-
- HY-N6848
-
Acetylseneciphylline N-oxide
|
Others
|
Infection
|
Acetylseneciphylline N-oxide is a pyrrolizine alkaloid that is seneciphylline in which the hydroxy hydrogen is replaced by an acetyl group and the tertiary amino function is oxidised to the corresponding N-oxide.
|
-
- HY-F0001
-
NADH disodium salt
Disodium NADH
|
Endogenous Metabolite
|
Others
|
NADH disodium salt is a coenzyme of a large number of oxidoreductases. NADH is a coenzyme that functions as a regenerating electron donor in catabolic processes including glycolysis, beta-oxidation and the citric acid cycle.
|
-
- HY-101437A
-
-
- HY-W013093
-
-
- HY-10593
-
IQ 1
|
Wnt
|
Cancer
|
IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on.
|
-
- HY-N4000
-
Digitonin
|
Others
|
Cancer
|
Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
|
-
- HY-N3119
-
Paeoniflorigenone
|
Apoptosis
|
Cancer
|
Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect.
|
-
- HY-133128
-
FM26
|
ROR
|
Cancer
|
FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
|
-
- HY-B0815
-
Chlorpyrifos
|
AChE
|
Neurological Disease
|
Chlorpyrifos is an organophosphate insecticide that is classified as a phosphorothionate. The oxon metabolite of Chlorpyrifos is an inhibitor of acetylcholinesterase (AChE), affecting neurological function in insects, humans, and other animals. The Chlorpyrifos oxon (CPO) metabolite is hydrolyzed by the plasma enzyme paraoxonase 1 (PON1), and susceptibility to neurotoxicity associated with CPO exposure is mitigated by PON1 overexpression.
|
-
- HY-P1064
-
Apelin-36(human)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-135680
-
I-OMe-Tyrphostin AG 538
I-OMe-AG 538
|
IGF-1R
|
Cancer
Metabolic Disease
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
|
-
- HY-70068
-
-
- HY-10251
-
BMS-599626
AC480
|
EGFR
|
Cancer
|
BMS-599626 (AC480) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC50s of 20 and 30 nM, respectively. BMS-599626 displays ~8-fold less potent to HER4 (IC50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy.
|
-
- HY-13297
-
PYZD-4409
|
E1/E2/E3 Enzyme
|
Cancer
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
|
-
- HY-103697A
-
Gardiquimod diTFA
|
Toll-like Receptor (TLR)
HIV
|
Cancer
Infection
|
Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
|
-
- HY-B1057S2
-
Nefopam D3
Fenazoxine D3
|
β-catenin
|
Neurological Disease
|
Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
|
-
- HY-P1126
-
Dolastatin 15
DLS 15
|
Microtubule/Tubulin
ADC Cytotoxin
Apoptosis
|
Cancer
|
Dolastatin 15 (DLS 15), a depsipeptide derived from Dolabella auricularia, is a potent antimitotic agent structurally related to the antitubulin agent Dolastatin 10. Dolastatin 15 induces cell cycle arrest and apoptosis in multiple myeloma cells. Dolastatin 15 can be used as an ADC cytotoxin.
|
-
- HY-136093A
-
IM156
HL156A; HL271 acetate
|
AMPK
|
Cancer
Neurological Disease
|
IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-A0067
-
Oxybenzone
Benzophenone 3
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
|
Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
|
-
- HY-B0902A
-
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-B0097
-
Floxuridine
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Cancer
Infection
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
|
-
- HY-17036
-
Naphthoquine phosphate
|
Parasite
|
Infection
|
Naphthoquine phosphate is a potent and orally active antimalarial agent. Naphthoquine phosphate has thorough killing function for various schizonts of plasmodia, including resistance of P. falciparum to Chloroquine.
|
-
- HY-15995
-
-
- HY-11029
-
-
- HY-117727
-
Leriglitazone
Hydroxypioglitazone
|
PPAR
|
Metabolic Disease
|
Leriglitazone (Hydroxypioglitazone), a metabolite of pioglitazone.
Leriglitazone (Hydroxypioglitazone) PioOH is a PPARγ agonist, stabilizes the PPARγ activation function-2 (AF-2) co-activator binding surface and enhances co-activator binding, affording slightly better transcriptional efficacy.
Leriglitazone (Hydroxypioglitazone) binds to the PPARγ C-terminal ligand-binding domain (LBD) with Ki of 1.2 μM,induces transcriptional efficacy of the PPARγ (LBD) with EC50
of 680 nM.
|
-
- HY-101870B
-
INCB053914 phosphate
|
Pim
|
Cancer
|
INCB053914 phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. INCB053914 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
|
-
- HY-136057
-
iFSP1
|
Ferroptosis
|
Cancer
|
iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).
|
-
- HY-136588
-
trans-R-138727MP
Prasugrel metabolite R-138727MP
|
P2Y Receptor
|
Cardiovascular Disease
|
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel (HY-15284). Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
|
-
- HY-16918
-
Heptamidine
SBi4211
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine (SBi4211) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-102011
-
BMS-1166
|
PD-1/PD-L1
|
Cancer
Inflammation/Immunology
|
BMS-1166 is a potent PD-1/PD-L1 immune checkpoint inhibitor. BMS-1166 induces dimerization of PD-L1 and blocks its interaction with PD-1, with an IC50 of 1.4 nM. BMS-1166 antagonizes the inhibitory effect of PD-1/PD-L1 immune checkpoint on T cell activation.
|
-
- HY-N2993
-
Polyporenic acid C
|
Apoptosis
|
Cancer
|
Polyporenic acid C is a lanostane-type triterpenoid isolated from P. cocos. Polyporenic acid C induces cell apoptosis through the death receptor-mediated apoptotic pathway without the involvement of the mitochondria. Polyporenic acid C is promising agent for lung cancer therapy.
|
-
- HY-N6036
-
Ganoderic acid F
|
Others
|
Cancer
|
Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
|
-
- HY-B0497B
-
-
- HY-P1064A
-
Apelin-36(human) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-13775
-
XL019
|
JAK
Apoptosis
|
Cancer
|
XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
|
-
- HY-131055
-
Mytoxin B
|
ADC Cytotoxin
PI3K
Apoptosis
|
Cancer
|
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway.
|
-
- 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-123076
-
Pifithrin-α, p-Nitro, Cyclic
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
|
-
- HY-113846
-
CMP-5 hydrochloride
|
Histone Methyltransferase
|
Cancer
|
CMP-5 hydrochloride is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 hydrochloride selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 hydrochloride prevents EBV-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-113498
-
Sphingomyelin
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.
|
-
- HY-100490A
-
Rilmenidine hemifumarate
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cancer
Cardiovascular Disease
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- 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-41404
-
Piperonylic acid
|
Cytochrome P450
|
Infection
|
Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase.
|
-
- HY-107372
-
-
- HY-125035
-
LCH-7749944
GNF-PF-2356
|
PAK
Apoptosis
|
Cancer
|
LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.
|
-
- HY-136979
-
RBN012759
|
PARP
|
Cancer
Inflammation/Immunology
|
RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.
|
-
- HY-B0252
-
Hydrochlorothiazide
HCTZ
|
TGF-beta/Smad
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
Hydrochlorothiazide (HCTZ), an orally active diuretic drug of the thiazide class, inhibits transforming TGF-β/Smad signaling pathway. Hydrochlorothiazide has direct vascular relaxant effects via opening of the calcium-activated potassium (KCA) channel. Hydrochlorothiazide improves cardiac function, reduces fibrosis and has antihypertensive effect.
|
-
- HY-N0633
-
-
- HY-12290A
-
Arg-Gly-Asp-Ser (TFA)
RGDS peptide (TFA); Fibronectin tetrapeptide (TFA)
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser (TFA) is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser (TFA) directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-16918A
-
Heptamidine dimethanesulfonate
SBi4211 dimethanesulfonate
|
Others
|
Cancer
Inflammation/Immunology
|
Heptamidine dimethanesulfonate (SBi4211 dimethanesulfonate) is a potent Pentamidine-related inhibitor of the calcium-binding protein S100B (Kd=6.9 μM), selectively kills melanoma cells with S100B over those without S100B. Heptamidine is a useful tool for the investigation of Myotonic dystrophy (DM).
|
-
- HY-131614
-
TPC2-A1-N
|
Calcium Channel
|
Others
|
TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-13919
-
Napabucasin
|
STAT
|
Cancer
|
Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
|
-
- HY-B1776
-
Spermidine
|
Endogenous Metabolite
|
Metabolic Disease
|
Spermidine maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-107846
-
Xylan
|
Others
|
Others
|
Xylan represents the main hemicellulose component in the secondary plant cell walls of flowering plants. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose.
|
-
- HY-B1776A
-
Spermidine trihydrochloride
|
Others
|
Metabolic Disease
|
Spermidine trihydrochloride maintains cell membrane stability, increases antioxidant enzymes activities, improving photosystem II (PSII), and relevant gene expression. Spermidine trihydrochloride significantly decreases the H2O2 and O2 .- contents.
|
-
- HY-100734
-
-
- HY-12276
-
MALT1 inhibitor MI-2
|
MALT1
|
Cancer
|
MALT1 inhibitor MI-2 is a MALT1 inhibitor (IC50=5.84 μM). MALT1 inhibitor MI-2 binds directly to MALT1, irreversibly suppresses protease function and is accompanied by NF-κB reporter activity suppression, c-REL nuclear localization inhibition, and NF-κB target gene downregulation. MALT1 inhibitor MI-2 shows nontoxic to animals.
|
-
- HY-10183
-
-
- HY-113756A
-
Latanoprost acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
|
-
- HY-18010
-
PCI 29732
|
Btk
BCRP
|
Inflammation/Immunology
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.
|
-
- HY-133654
-
2,3,3-Tribromopropenoic acid
|
Others
|
Others
|
2,3,3-Tribromopropenoic acid is a 2,3,3-Tribromo product based on propenoic acid. 2,3,3-Tribromopropenoic acid is a polar aromatic brominated disinfection byproduct during chlorination in water and shows cytotoxic potency in mammalian cell chronic cytotoxicity experiments.
|
-
- HY-101952
-
-
- HY-137179
-
Glyco-diosgenin
|
Others
|
Others
|
Glyco-diosgenin is a synthetic surfactant and detergent for extracting proteins from membranes for structure and function studies, and single-particle cryo-electron microscopy (cryoEM) studies of membrane proteins.
|
-
- HY-136093
-
HL271
IM156 hydrochloride; HL156A hydrochloride
|
AMPK
|
Cancer
Neurological Disease
|
HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-75564
-
Cyclo(Ala-Gly)
|
Endogenous Metabolite
|
Cancer
|
Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM.
|
-
- HY-12755
-
ML141
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
|
-
- HY-120137
-
CMP-5
|
Histone Methyltransferase
|
Cancer
|
CMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
|
-
- HY-128206
-
I3MT-3
HMPSNE
|
Hippo (MST)
|
Metabolic Disease
|
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
|
-
- HY-108556
-
RWJ-56110
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
RWJ-56110 is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis.
|
-
- HY-13968
-
JW 55
|
PARP
|
Cancer
|
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
|
-
- HY-B1836
-
Mildronate
Meldonium; MET-88; Quaterin
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
|
-
- HY-N4298
-
Epitheaflagallin 3-O-gallate
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
Epitheaflagallin 3-O-gallate is a minor polyphenol in black tea. Epitheaflagallin 3-O-gallate exhibits versatile physiological functions in vivo and in vitro, including antioxidative activity, pancreatic lipase inhibition, Streptococcus sorbinusglycosyltransferase inhibition, and an inhibiting effect on the activity of matrix metalloprotease-1 and -3 and their synthesis by human gingival fibroblasts.
|
-
- HY-Y0248A
-
-
- HY-125018
-
QM31
SVT016426
|
Caspase
|
Cancer
|
QM31 (SVT016426), a cytoprotective agent, is a selective inhibitor of Apaf-1. QM31 inhibits the formation of the apoptosome (IC50=7.9μM), the caspase activation complex composed by Apaf-1, cytochrome c, dATP and caspase-9. QM31 exerts mitochondrioprotective functions and interferes with the intra-S-phase DNA damage checkpoint.
|
-
- HY-121087
-
BCI-215
|
Phosphatase
|
Cancer
|
BCI-215 is a potent and tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor. BCI-215 has cytotoxicity for tumor cells but not normal cells.
|
-
- HY-19832
-
SC66
|
Akt
Apoptosis
|
Cancer
|
SC66 is an Akt inhibitor, reduces cell viability in a dose- and time-dependent manner, inhibits colony formation and induces apoptosis in hepatocellular carcinoma (HCC) cells.
|
-
- HY-114410
-
CCI-006
|
Mitochondrial Metabolism
|
Cancer
|
CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells.
|
-
- HY-134130
-
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-13306
-
Pyrintegrin
|
Integrin
|
Metabolic Disease
|
Pyrintegrin is an β1-integrin agonist and a 2,4-disubstituted pyrimidine that promotes embryonic stem cells survival. Pyrintegrin enhances cell-extracellular matrix (ECM) adhesion-mediated integrin signaling. Pyrintegrin can be used as a podocyte-protective agent and has robustly adipogenic.
|
-
- HY-136314
-
DBCO-PEG4-VC-PAB-MMAE
|
Drug-Linker Conjugates for ADC
|
Cancer
|
DBCO-PEG4-VC-PAB-MMAE consists a ADC linker (DBCO-PEG4-VC-PAB) and a tubulin polymerization inhibitor MMAE (HY-15162). DBCO-PEG4-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs). MMAE is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization.
|
-
- 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-P0172A
-
ATI-2341 TFA
|
CXCR
|
Cancer
Inflammation/Immunology
Endocrinology
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-P0172
-
ATI-2341
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).
|
-
- HY-19331
-
WZB117
|
GLUT
|
Cancer
|
WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.
|
-
- HY-103637
-
Vimirogant
VTP-43742
|
ROR
|
Inflammation/Immunology
|
Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.
|
-
- HY-103637A
-
Vimirogant hydrochloride
VTP-43742 hydrochloride
|
ROR
|
Inflammation/Immunology
|
Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
|
-
- HY-N1713
-
-
- HY-W015399
-
4-Methylcinnamic acid
|
Fungal
|
Infection
|
4-Methylcinnamic acid, a Cinnamic acid analog, can be used as a intervention catalyst for overcoming antifungal tolerance. 4-Methylcinnamic acid can improve the potency of cell wall-disrupting agents.
|
-
- HY-136242
-
UT-34
|
Androgen Receptor
|
Cancer
Endocrinology
|
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
|
-
- HY-N2028
-
Demethylwedelolactone
|
Others
|
Cancer
|
Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsin inhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell.
|
-
- HY-W011404
-
Tributyrin
Glyceryl tributyrate
|
Apoptosis
|
Metabolic Disease
|
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
|
-
- HY-N7626
-
Eleutherol
|
Fungal
Glucosidase
|
Infection
|
Eleutherol is a naphthalene isolated from E. americana with antifungal activities. Eleutherol is against yeasts Candida albicans, C. tropicalis, Saccharomyces cerevisiae and Cryptococcus neoformans with MIC values between 7.8 µg/mL and 250 µg/mL. Eleutherol inhibits α-glucosidase function with an IC50>1.00 mM.
|
-
- HY-B1836A
-
Mildronate dihydrate
Meldonium dihydrate; MET-88 dihydrate; Quaterin dihydrate
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
|
-
- HY-13915
-
NSC348884
|
Apoptosis
|
Cancer
|
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines.
|
-
- HY-P1185
-
Antagonist G
|
Vasopressin Receptor
Apoptosis
|
Cancer
|
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy.
|
-
- HY-123905
-
LIN28 inhibitor LI71
|
MicroRNA
|
Cancer
|
LIN28 inhibitor LI71 is a potent and cell-permeable LIN28 inhibitor, which abolishes LIN28-mediated oligouridylation with an IC50 of 7 uM. LIN28 inhibitor LI71 directly binds the cold shock domain (CSD) to suppress LIN28’s activity against let-7 in leukemia cells and embryonic stem cells.
|
-
- HY-116894
-
Rotundifuran
|
Apoptosis
|
Cancer
|
Rotundifuran, a labdane type diterpene, is isolated from Vitex rotundifolia. Rotundifuran can inhibit the cell cycle progression and induce apoptosis in human myeloid leukaemia cells.
|
-
- HY-B0411
-
Domperidone
R33812
|
Dopamine Receptor
|
Neurological Disease
|
Domperidone (R33812) is a selective dopamine-2 receptor antagonist. Domperidone acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
|
-
- HY-13673
-
Goserelin
ICI 118630
|
GnRH Receptor
Apoptosis
|
Cancer
Endocrinology
|
Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-19619
-
m-3M3FBS
|
Phospholipase
Apoptosis
|
Cancer
|
m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.
|
-
- HY-P1185A
-
-
- HY-10046
-
-
- HY-50908
-
Ridaforolimus
MK-8669; Deforolimus; AP23573
|
mTOR
Autophagy
|
Cancer
|
Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells.
|
-
- HY-N7019
-
19-Hydroxybufalin
|
Others
|
Cancer
|
19-Hydroxybufalin is a bufadienolide, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells.
|
-
- HY-125965
-
BioA-IN-13
|
Bacterial
|
Infection
|
BioA-IN-13 is a potent, cell permeable and whole-cell active inhibitor of Mycobacterium tuberculosis BioA enzyme.
|
-
- HY-B0862
-
Pendimethalin
|
Others
|
Others
|
Pendimethalin is an herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin inhibits cell division and cell elongation.
|
-
- HY-W013699
-
Chlorhexidine diacetate
|
Bacterial
Antibiotic
|
Infection
|
Chlorhexidine diacetate is a biguanide disinfectant with rapid bactericidal activity against both Gram-positive and Gram-negative organism. The antibacterial effect of chlorhexidine diacetate is related to its action on the bacterial cell membrane and to precipitation of intracellular contents.
|
-
- HY-B0986
-
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-P1201
-
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-113950
-
-
- HY-15518
-
LCL161
|
IAP
|
Cancer
|
LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
|
-
- HY-17362
-
Vancomycin hydrochloride
|
Bacterial
Autophagy
Antibiotic
|
Infection
Cancer
|
Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
|
-
- HY-100395
-
F16
|
Apoptosis
|
Cancer
|
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
|
-
- HY-101511
-
TTT-28
|
P-glycoprotein
|
Cancer
|
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
|
-
- HY-10583
-
Y-27632 dihydrochloride
|
ROCK
Apoptosis
|
Cancer
|
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
|
-
- HY-108556A
-
RWJ-56110 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
|
-
- HY-B0430
-
D-Pantothenic acid
pantothenate; vitamin B5
|
Others
|
Others
|
D-Pantothenic acid is an essential trace nutrient that functions as the obligate precursor of coenzyme A (CoA). D-Pantothenic acid plays key roles in myriad biological processes, including many that regulate carbohydrate, lipid, protein, and nucleic acid metabolism.
|
-
- HY-13673A
-
Goserelin acetate
ICI-118630 acetate
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-17571A
-
Oxytocin acetate
α-Hypophamine acetate; Oxytocic hormone acetate
|
Oxytocin Receptor
|
Endocrinology
|
Oxytocin acetate is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
|
-
- 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-P1345
-
TLQP-21
|
Complement System
|
Endocrinology
Neurological Disease
|
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-W008344
-
2-Chloroadenosine
|
Others
|
Others
|
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes.
|
-
- HY-109566
-
-
- HY-N0438
-
Pimpinellin
|
Apoptosis
|
Cancer
|
Pimpinellin is a constituent of Cyrtomium fortumei (J.). Pimpinellin inhibits the growth of tumor cells via the induction of tumor cell apoptosis.
|
-
- HY-114313
-
-
- HY-100036
-
MK-4101
|
Smo
Apoptosis
Hedgehog
|
Cancer
|
MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 µM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 µM for mouse cells; IC50 of 1 µM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.
|
-
- HY-100195
-
SAR-020106
|
Checkpoint Kinase (Chk)
|
Cancer
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer drugs.
|
-
- HY-P1065
-
Apelin-36(rat, mouse)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- HY-P1201A
-
Cyclosomatostatin TFA
|
Somatostatin Receptor
|
Cancer
|
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-112314
-
AZD0424
|
Src
Bcr-Abl
Apoptosis
|
Cancer
|
AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.
|
-
- HY-W019870A
-
Glufosinate
|
Others
|
Neurological Disease
|
Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity.
|
-
- HY-138537
-
NF-κB-IN-1
|
IKK
|
Cancer
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells.
|
-
- HY-122502
-
Pyrazofurin
|
DNA/RNA Synthesis
|
Cancer
|
Pyrazofurin, a pyrimidine nucleoside analogue with antineoplastic activity, inhibits cell proliferation and DNA synthesis in cells by inhibiting uridine 5'-phosphate (UMP) synthase. Pyrazofurin is an active, sensitive orotate-phosphoribosyltransferase inhibitor with IC50s between 0.06-0.37 µM in the three squamous cell carcinoma (SCC) cell lines Hep-2, HNSCC-14B and HNSCC-14C.
|
-
- HY-B0430A
-
D-Pantothenic acid sodium
Sodium pantothenate; Vitamin B5 sodium
|
Apoptosis
|
Metabolic Disease
|
D-Pantothenic acid sodium (Sodium pantothenate) is an essential trace nutrient that functions as the obligate precursor of coenzyme A (CoA). D-Pantothenic acid sodium plays key roles in myriad biological processes, including many that regulate carbohydrate, lipid, protein, and nucleic acid metabolism.
|
-
- HY-121018
-
Daltroban
BM-13505; SKF 96148
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
|
-
- HY-15826
-
-
- HY-12826
-
IMB-XH1
|
Bcl-2 Family
Bacterial
|
Cancer
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1). IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively.
|
-
- HY-135784
-
OSMI-2
|
Acyltransferase
|
Metabolic Disease
|
OSMI-2 (Compound 1b) is a cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-2 increases detained intron splicing in cells.
|
-
- HY-U00177
-
GDP366
|
Survivin
|
Cancer
|
GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
|
-
- HY-15184
-
Elaiophylin
Azalomycin B; Gopalamicin; Efomycin E
|
Autophagy
|
Cancer
|
Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
|
-
- HY-114926
-
KT185
|
MAGL
|
Neurological Disease
|
KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
|
-
- HY-112716
-
-
- HY-19637
-
SW044248
|
Topoisomerase
|
Cancer
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
|
-
- HY-114170
-
ML604440
|
Proteasome
|
Inflammation/Immunology
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-136383
-
AZA1
Rac1/Cdc42-IN-1
|
Ras
Apoptosis
|
Cancer
|
AZA1 is a potent dual inhibitor of Rac1 and Cdc42. AZA1 induces prostate cancer cells apoptosis and inhibits prostate cancer cells proliferation, migration and invasion.
|
-
- 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-15771A
-
Tirabrutinib hydrochloride
ONO-4059 hydrochloride; GS-4059 hydrochloride
|
Btk
|
Cancer
|
Tirabrutinib (ONO-4059) hydrochloride is a selective and novel inhibitor of BTK with IC50 2.2 nm, Tirabrutinib binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.
|
-
- HY-10126
-
Barasertib-HQPA
AZD2811; INH-34; AZD1152-HQPA
|
Aurora Kinase
Apoptosis
|
Cancer
|
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-109520
-
Glatiramer acetate
|
Others
|
Inflammation/Immunology
|
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
|
-
- 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-136234
-
9-cis-β-Carotene
|
Others
|
Others
|
9-cis-β-Carotene, a precursor of retinal, is cleaved by beta-carotene oxygenase 1 (BCMO1) to produce 9-cis-retinal. 9-cis-β-Carotene inhibits photoreceptor degeneration and restores retinal function in vivo. 9-cis-β-Carotene has the potential for the study of congenital stationary night blindness and fundus albipunctatus.
|
-
- HY-103193
-
NKH477
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
|
Cardiovascular Disease
|
NKH477 (Colforsin dapropate hydrochloride) is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts.
|
-
- HY-103238
-
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
|
-
- HY-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-110193
-
SPP-86
|
RET
|
Cancer
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
|
-
- HY-21141
-
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-15648F
-
GSK-J4 hydrochloride
|
Histone Demethylase
|
Cancer
|
GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
|
-
- HY-112062
-
POL1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
|
-
- HY-B0982
-
-
- HY-12743A
-
-
- HY-12743
-
K-7174
|
Others
|
Inflammation/Immunology
|
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
|
-
- HY-P1345A
-
TLQP-21 TFA
|
Complement System
|
Endocrinology
Neurological Disease
|
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
|
-
- HY-114503
-
NSAH
|
DNA/RNA Synthesis
|
Cancer
|
NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively.
|
-
- HY-101055
-
Kinetin riboside
N6-Furfuryladenosine
|
Apoptosis
|
Cancer
|
Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.
|
-
- HY-101524
-
-
- HY-15405
-
Teriflunomide
A77 1726
|
Others
|
Inflammation/Immunology
|
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
|
-
- HY-W019870
-
Glufosinate ammonium
|
Others
|
Neurological Disease
|
Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity.
|
-
- HY-P1065A
-
Apelin-36(rat, mouse) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
|
-
- 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-108716
-
CBS9106
SL-801
|
CRM1
Apoptosis
|
Cancer
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells.
|
-
- HY-103489
-
PI-273
|
PI4K
Apoptosis
|
Cancer
|
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
|
-
- 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-15304
-
-
- HY-P0151
-
-
- HY-12797
-
GF 15
|
Others
|
Cancer
|
GF 15 is a potent inhibitor of centrosomal clustering in tumor cells.
|
-
- HY-103359
-
Ceranib1
|
Others
|
Cancer
|
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.
|
-
- HY-N4171
-
Dihydrocucurbitacin B
|
Others
|
Inflammation/Immunology
|
Dihydrocucurbitacin B, a triterpene isolated from Cayaponia tayuya roots, inhibits nuclear factor of activated T cells (NFAT), induces cell cycle arrested in the G0 phase, and inhibits delayed type hypersensitivity.
|
-
- HY-112914
-
-
- HY-10127
-
Barasertib
AZD1152
|
Aurora Kinase
Apoptosis
|
Cancer
|
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-15694
-
SMIP004
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
|
-
- HY-135785
-
OSMI-3
|
Acyltransferase
|
Metabolic Disease
|
OSMI-3 (Compound 2b) is a potent, long-lasting, and cell-permeable O-linked N-acetylglucosamine transferase (OGT) inhibitor. Cells contain a large nuclear pool of partially spliced OGT transcript, and OSMI-3 increases detained intron splicing in cells.
|
-
- HY-15004
-
AUZ 454
K03861
|
CDK
|
Cancer
|
AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
|
-
- HY-118224
-
BPH-715
|
Parasite
|
Infection
|
BPH-715 is a bisphosphonate, inhibits Plasmodium liver-stage growth, with an IC50 of 10 μM for Plasmodium exoerythrocytic forms in HepG2 cells.
|
-
- HY-114322
-
VZ185
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
VZ185 is a potent, fast, and selective VHL based dual degrader probe of BRD9 and BRD7 with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC50s of 3 nM and 40 nM, respectively.
|
-
- HY-N2292
-
Kinsenoside
|
Keap1-Nrf2
Apoptosis
|
Inflammation/Immunology
|
Kinsenoside is a main active component isolated from plants of the genus Anoectochilus, and exhibits many biological activities and pharmacological effects. Kinsenoside rescues the nucleus pulposus cells (NPCs) viability under oxidative stress and protects against apoptosis, senescence and mitochondrial dysfunction in a Nrf2-dependent way.
|
-
- HY-103006
-
NAI-N3
|
Others
|
Others
|
NAI-N3 is a RNA acylation reagent that enables RNA purification. NAI-N3 is a dual-function SHAPE (selective 2-hydroxyl acylation and profiling experiment) probe (RNA structure probe and enrichment).
|
-
- HY-100406
-
(S)-MCPG
(+)-MCPG
|
mGluR
|
Neurological Disease
|
(S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning.
|
-
- HY-Y0445A
-
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-10846
-
-
- HY-15700
-
-
- HY-131615
-
TPC2-A1-P
|
Sodium Channel
|
Others
|
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-16662
-
Oncrasin-1
|
Ras
Apoptosis
|
Cancer
|
Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells.
|
-
- HY-17511
-
Potassium oxonate
Potassium azaorotate; Potassium otastat
|
Others
|
Metabolic Disease
|
Potassium oxonate is an inhibitor of uricase, inhibits the phosphorylation of 5-FU to 5-fluorouridine-5'-monophosphate catalyzed by pyrimidine phosphoribosyl-transferase in a different manner from allopurinol in cell-free extracts and intact cells in vitro.
|
-
- HY-N6745
-
Citreoviridin
|
Na+/K+ ATPase
Apoptosis
|
Infection
Cardiovascular Disease
|
Citreoviridin, a toxin from Penicillium citreoviride NRRL 2579, inhibits brain synaptosomal Na +/K +-ATPase whereas in microsomes, both Na +/K +-ATPase and Mg 2+-ATPase activities are significantly stimulated in a dose-dependent manner. Citreoviridin inhibits cell proliferation and enhances apoptosis of human umbilical vein endothelial cells.
|
-
- HY-119738
-
OSMI-1
|
Acyltransferase
|
Metabolic Disease
|
OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.
|
-
- HY-12458
-
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-110115
-
TC-Mps1-12
|
Mps1
|
Cancer
|
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM.
|
-
- 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-N1931
-
Epifriedelanol
|
Others
|
Cancer
|
Epifriedelanol is a triterpenoid isolated from the root bark of Ulmus davidiana, with antitumor activity. Epifriedelanol inhibits cellular senescence in human primary cells.
|
-
- 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-N6602
-
α-Solanine
|
Apoptosis
|
Cancer
|
α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
|
-
- HY-A0068
-
Aurothioglucose
Gold thioglucose
|
Others
|
Cancer
|
Aurothioglucose (Gold thioglucose) is a well known active-site inhibitor of TrxR1, inhibited TrxR1 activity in HeLa cell cytosol but had no effect on the viability of the cells.
|
-
- 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-13668
-
-
- HY-N2420
-
Flavokawain A
|
Apoptosis
|
Cancer
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N0504
-
-
- HY-10222
-
Ixabepilone
BMS-247550; Aza-epothilone B
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
|
-
- HY-B0293
-
Butoconazole nitrate
RS 35887
|
Fungal
|
Infection
|
Butoconazole nitrate (RS 35887), an imidazole antifungal agent, is active against Candida spp. and effective against vaginal infections due to Candida albicans. Butoconazole nitrate is presumed to function as other imidazole derivatives via inhibition of steroid synthesis.
|
-
- HY-11030
-
-
- HY-B2078A
-
Eprazinone dihydrochloride
|
Neurokinin Receptor
|
Inflammation/Immunology
|
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen.
|
-
- HY-135383B
-
(Z)-Pitavastatin calcium
|
Others
|
Metabolic Disease
|
(Z)-Pitavastatin calcium is the Z-Isomer of Pitavastatin hemicacium. Pitavastatin calcium is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin calcium inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells.
|
-
- HY-N6782
-
Oligomycin
|
ATP Synthase
Fungal
Antibiotic
|
Cancer
Infection
|
Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
|
-
- HY-10498
-
Lexibulin
CYT-997
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
|
-
- HY-10498A
-
Lexibulin dihydrochloride
CYT-997 dihydrochloride
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
Lexibulin dihydrochloride (CYT-997 dihydrochloride) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin dihydrochloride induces cell apoptosis and induces mitochondrial ROS generation in GC cells.
|
-
- HY-B1596
-
-
- HY-18965
-
-
- HY-100498
-
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-18679
-
TC-N 22A
|
mGluR
|
Neurological Disease
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-N0171A
-
-
- HY-138239
-
WEE1-IN-3
|
Wee1
|
Cancer
|
WEE1-IN-3 is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. WEE1-IN-3 has anticancer activities.
|
-
- HY-121497
-
3-Methoxybenzamide
3-MBA
|
PARP
Bacterial
|
Cancer
|
3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells. 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum).
|
-
- HY-17371
-
Oxaliplatin
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Autophagy
|
Cancer
|
Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and causes cell death. Oxaliplatin time-dependently inhibits human melanoma cell lines C32 and G361 with IC50 values of 0.98 μM and 0.14 μM, respectively. Oxaliplatin induces cell autophagy.
|
-
- HY-121802
-
Dynarrestin
|
Hedgehog
|
Cancer
|
Dynarrestin is a aminothiazole inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin rapidly and reversibly inhibits dynein 1-driven microtubule gliding in vitro plus a range of dynein 1- and 2-dependent processes in cells without affecting ATP hydrolysis and interfering with ciliogenesis. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells.
|
-
- HY-13721
-
Phenoxodiol
Idronoxil; Dehydroequol; Haginin E
|
Caspase
Apoptosis
Topoisomerase
|
Cancer
|
Phenoxodiol, a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. This agent also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21 WAF1 via a p53 independent manner.
|
-
- HY-16658B
-
Z-VAD-FMK
Z-VAD(OH)-FMK
|
Caspase
|
Cancer
|
Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM.
|
-
- HY-N6744
-
Chaetoglobosin A
|
Apoptosis
|
Cancer
Infection
|
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
|
-
- HY-77813
-
-
- HY-111425
-
SSE15206
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
SSE15206 is a microtubule polymerization inhibitor (GI50 = 197 nM in HCT116 cells) that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.
|
-
- HY-120215
-
KT203
|
MAGL
|
Metabolic Disease
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
|
-
- HY-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-100636
-
Gefitinib N-oxide
|
EGFR
|
Cancer
|
Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
|
-
- HY-120177
-
KT182
|
MAGL
|
Others
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
|
-
- HY-12873
-
RBC8
|
Ras
|
Cancer
|
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
|
-
- HY-B0497
-
Niclosamide
BAY2353
|
STAT
Parasite
Antibiotic
|
Infection
Cancer
|
Niclosamide (BAY2353) is an orally bioavailable chlorinated salicylanilide, with anthelmintic and potential antineoplastic activity. Niclosamide (BAY2353) inhibits STAT3 with IC50 of 0.25 μM in HeLa cells and inhibits DNA replication in a cell-free assay.
|
-
- HY-127002A
-
Squarunkin A hydrochloride
|
Src
|
Cancer
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
|
-
- HY-17571
-
Oxytocin
α-Hypophamine; Oxytocic hormone
|
Oxytocin Receptor
|
Endocrinology
|
Oxytocin (α-Hypophamine; Oxytocic hormone) is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
|
-
- HY-N7509
-
2,3-Dihydroxy-4-methoxyacetophenone
Gallacetophenone-4-methyl ether
|
Others
|
Neurological Disease
|
2,3-Dihydroxy-4-methoxyacetophenone is a neuroprotective compound from Cynenchum paniculatum. 2,3-Dihydroxy-4-methoxyacetophenone improves cognitive function and may has the potential for the treatment of Alzheimer's disease research.
|
-
- HY-B0702
-
-
- HY-126679
-
Apoptolidin
|
ATP Synthase
Apoptosis
|
Cancer
|
Apoptolidin is a polyketide isolated from Nocardiopsis bacteria. Apoptolidin is a selective mitochondrial F1FO ATPase inhibitor. Apoptolidin is an apoptosis inducer and induces apoptotic cell death in cells transformed with the adenovirus type 12 oncogenes including ElA (IC50=10-17 ng/ml) but not in normal cells.
|
-
- HY-134582
-
dCBP-1
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on PROTAC. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression.
|
-
- HY-106420
-
-
- HY-P1629
-
Temporin A
|
Bacterial
Fungal
Antibiotic
|
Infection
|
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
|
-
- HY-P0069A
-
-
- HY-P1286
-
-
- HY-B0313
-
-
- HY-B1300
-
-
- HY-21972
-
-
- HY-18632A
-
-
- HY-15648B
-
GSK-J4
|
Histone Demethylase
Apoptosis
|
Cancer
|
GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
|
-
- HY-N1506
-
Ganodermanontriol
|
Others
|
Cancer
|
Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity.
|
-
- HY-B0790
-
TAI-1
|
Apoptosis
|
Cancer
|
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
|
-
- HY-N2486
-
-
- HY-118660
-
Anhydrotetracycline hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
Anhydrotetracycline hydrochloride, a tetracycline biosynthetic precursor, is a potent competitive broad-spectrum tetracycline destructase enzymes inhibitor. Anhydrotetracycline hydrochloride is an effector for tetracycline controlled gene expression systems in eukaryotic cells.
|
-
- HY-12425
-
-
- HY-N3558
-
Ceanothic acid
Emmolic acid
|
Others
|
Cancer
|
Ceanothic acid (Emmolic acid) is a ring-A homologue of betulinic acid. Ceanothic acid inhibits OVCAR-3, HeLa, and FS-5 cells with the cell survival of 68%, 65%, and 81%, respectively.
|
-
- HY-12842
-
UC-112
|
IAP
Apoptosis
|
Cancer
|
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
|
-
- HY-136351
-
THZ-P1-2
|
Autophagy
|
Cancer
|
THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
|
-
- HY-N4053
-
Heraclenin
|
Others
|
Inflammation/Immunology
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-120836
-
AOH1160
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
AOH1160 is a potent, first-in-class, orally available small molecule proliferating cell nuclear antigen (PCNA) inhibitor, interferes with DNA replication, blocks homologous recombination-mediated DNA repair, causes cell-cycle arrest and induces apoptosis. AOH1160 selectively kills many types of cancer cells (mean GI50=330 nM) without causing significant toxicity to a broad range of nonmalignant cells.
|
-
- HY-15609
-
-
- HY-117650A
-
RG7834
RO 7020322
|
HBV
|
Infection
|
RG7834 (RO 7020322) is a highly selective and orally bioavailable HBV inhibitor, potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively, in dHepaRG Cells.
|
-
- HY-106101
-
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- HY-120548
-
KBU2046
|
Others
|
Cancer
|
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
|
-
- HY-129492
-
GNF4877
|
DYRK
GSK-3
|
Metabolic Disease
|
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells).
|
-
- HY-12462
-
WS3
|
Others
|
Inflammation/Immunology
|
WS3 is a novel proliferative molecule that promotes pancreatic β cell proliferation in rodent and human primary islets. WS3 can be used for the research of type 1 diabetes.
|
-
- HY-126378
-
LSP-249
|
Others
|
Inflammation/Immunology
|
LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasma kallikrein inhibitor under the study for angioedema, with an EC50 less than 100 nM in cell.
|
-
- HY-N4219
-
-
- HY-15894
-
-
- HY-N1516
-
Ganoderenic acid D
|
Apoptosis
|
Cancer
|
Ganoderenic acid D is a triterpene identified from the effective compounds of Ganoderma lucidum extract (GLE). Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
|
-
- HY-122214
-
AC-73
|
Autophagy
|
Cancer
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells. AC-73 is also an anti-proliferative drug and an inducer of autophagy in leukemic cells.
|
-
- HY-A0098
-
Tunicamycin
|
Bacterial
Fungal
Influenza Virus
Antibiotic
|
Cancer
Infection
Inflammation/Immunology
|
Tunicamycin is a mixture of homologous nucleoside antibiotic that inhibits N-linked glycosylation and blocks GlcNAc phosphotransferase (GPT). Tunicamycin causes accumulation of unfolded proteins in cell endoplasmic reticulum (ER) and induces ER stress, and causes blocking of DNA synthesis and cell cycle arrest in G1 phase. Tunicamycin inhibits gram-positive bacteria, yeasts, fungi, and viruses and has anti-cancer activity.Tunicamycin increases exosome release in cervical cancer cells.
|
-
- HY-101567
-
BMS-986158
|
Epigenetic Reader Domain
|
Cancer
|
BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.
|
-
- HY-103002
-
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-117102
-
ANI-7
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
|
-
- HY-B0496
-
PMSF
Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride
|
Cathepsin
|
Others
|
PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
|
-
- HY-13307
-
JK184
|
Hedgehog
|
Cancer
|
JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells.
|
-
- HY-16695
-
-
- HY-100755
-
-
- HY-P1286A
-
-
- HY-129337
-
Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
-
- HY-108900
-
Leu-AMS
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-32340
-
Lexacalcitol
KH1060
|
VD/VDR
|
Cancer
Inflammation/Immunology
|
Lexacalcitol (KH1060), a vitamin D analog, is potent regulators of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases.
|
-
- HY-108295
-
Pivagabine
CXB-722
|
GABA Receptor
|
Neurological Disease
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain.
|
-
- HY-N6020B
-
Butin
|
Others
|
Inflammation/Immunology
Cardiovascular Disease
|
Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities. Butin significantly alleviates myocardial infarction and improves heart function, together with prevents diabetes-induced cardiac oxidative damage in rat.
|
-
- HY-F0004
-
β-Nicotinamide mononucleotide
β-NM; NMN
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
β-nicotinamide mononucleotide (β-NM) is a product of the nicotinamide phosphoribosyltransferase (NAMPT) reaction and a key NAD(+) intermediate. The pharmacological activities of β-nicotinamide mononucleotide include its role in cellular biochemical functions, cardioprotection, diabetes, Alzheimer's disease, and complications associated with obesity.
|
-
- HY-B0840
-
Chlorfenapyr
|
Others
|
Others
|
Chlorfenapyr is a pyrrole pro-insecticide that is metabolized in vivo into CL 303268 by mixed function oxidases. Chlorfenapyr is active against a variety of insects including those susceptible and resistant to pyrethroid and organophosphate insecticides. Formulations containing Chlorfenapyr have been used to control termites and in agriculture to control various insects.
|
-
- HY-N6624
-
Skullcapflavone II
|
Bacterial
|
Inflammation/Immunology
|
Skullcapflavone II, a flavonoid derived from Scutellaria baicalensis, has anti-inflammatory, anti-microbial activities. Skullcapflavone II regulates osteoclast differentiation, survival, and function. Skullcapflavone II exerts potent antimicrobial activity against M. aurum and M. bovis BCG.
|
-
- HY-14590
-
-
- HY-50895S
-
Gefitinib D8
ZD1839 D8
|
EGFR
Autophagy
|
Cancer
|
Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
|
-
- HY-101413
-
Iberin
NSC 321801
|
Apoptosis
Endogenous Metabolite
Bacterial
|
Cancer
|
Iberin (NSC 321801), a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. Iberin inhibits cell survival with an IC50 of 2.3 μM in HL60 cell. Iberin induces apoptosis.
|
-
- HY-128522
-
ARS-1323-alkyne
|
Ras
|
Cancer
|
ARS-1323-alkyne, a switch-II pocket (S-IIP) inhibitor, is a conformational specific chemical reporter of KRAS G12C nucleotide state in living cells.
|
-
- HY-N6626
-
-
- HY-N0726
-
Dracorhodin perchlorate
Dracohodin perochlorate
|
Apoptosis
|
Cancer
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis.
|
-
- HY-N4285
-
-
- HY-112055
-
DIM-C-pPhOH
|
Apoptosis
|
Cancer
|
DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
|
-
- HY-131183
-
PROTAC PD-1/PD-L1 degrader-1
|
PROTAC
PD-1/PD-L1
|
Inflammation/Immunology
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
|
-
- HY-137658
-
Purine riboside triphosphate
PTP
|
Nucleoside Antimetabolite/Analog
|
Others
|
Purine riboside triphosphate is a triphosphate derivative of purine riboside. Purine riboside is a naturally occurring base analog which closely resembles adenosine. Purine riboside inhibits carcinogenic growth. Purine riboside strongly inhibits RNA and DNA synthesis in different cancer ascites cells.
|
-
- HY-119751
-
Hematein
|
Casein Kinase
Akt
Wnt
Apoptosis
|
Cancer
|
Hematein is a oxidation product of hematoxylin acted as a dye. Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells.
|
-
- HY-N6734
-
K-252b
|
PKC
|
Infection
|
K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely .
|
-
- 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-129065
-
Nourseothricin sulfate
Streptothricin sulfate
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Nourseothricin sulfate (Streptothricin sulfate) is a broad-spectrum antibiotic that destroys the outer membrane of Gram-negative bacteria and is a dominant selective marker for Fonsecaea pedrosoi. Nourseothricin sulfate inhibits protein biosynthesis in prokaryotic cells and strongly inhibits the growth of eukaryotes like fungi and can also be used as a elective marker for a wide range of organisms including bacteria, yeast, filamentous fungi, and plant cells.
|
-
- HY-12726A
-
-
- HY-111446
-
-
- HY-12726
-
-
- HY-N7654
-
(-)-Epipodophyllotoxin
|
Apoptosis
|
Cancer
|
(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro.
|
-
- HY-B2145
-
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-114300
-
DSP-0565
|
Others
|
Neurological Disease
|
DSP-0565 (compound 17a) is a strong, broad-spectrum anti-epileptic drug (AED) candidate with unique GABAergic function. DSP-0565 shows anti-convulsant activity in various models (scPTZ, MES, 6 Hz and amygdala kindling) with good safety margin.
|
-
- HY-101953S
-
β-Apo-13-carotenone D3
D'Orenone D3
|
Others
|
Cancer
|
β-Apo-13-carotenone D3 is the deuterium labeled β-Apo-13-carotenone. β-Apo-13-carotenone (D'Orenone) is a naturally occurring β-apocarotenoid functioned as an antagonist of RXRα.
|
-
- HY-N2920
-
β-Amyrenonol
11-Oxo-β-amyrin
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.
|
-
- HY-11030A
-
-
- HY-116282D
-
-
- HY-116282C
-
-
- HY-116282A
-
-
- 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-116282B
-
-
- HY-19095
-
TNP-351
|
Antifolate
|
Cancer
|
TNP-351 is an antifolate. TNP-351, a dihydrofolate reductase (DHFR) inhibitor, has potent antitumor activity against not only leukemia cells but also solid tumor cells in vitro and in vivo.
|
-
- HY-120635
-
-
- HY-131036
-
MAO-IN-M30 dihydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease.
|
-
- HY-115537
-
NAE-IN-M22
|
Apoptosis
|
Cancer
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo.
|
-
- HY-10585A
-
Valproic acid sodium salt
Sodium Valproate
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
|
-
- HY-100415
-
UKI-1
UKI-1C
|
PAI-1
Ser/Thr Protease
|
Infection
Cancer
|
UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
|
-
- HY-N2567
-
(±)-Decursinol
|
Bacterial
|
Cancer
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-135960
-
BO-264
|
FGFR
Apoptosis
|
Cancer
|
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.
|
-
- HY-101561
-
Avapritinib
BLU-285
|
c-Kit
PDGFR
|
Cancer
|
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
|
-
- HY-19324
-
-
- HY-19563
-
-
- HY-12053A
-
-
- HY-D0850
-
Tartaric acid disodium dihydrate
Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate
|
Phosphatase
|
Cancer
|
Tartaric acid disodium dihydrate is a Acid phosphatase inhibitor, is a sodium salt used in buffers for molecular biology and cell culture applications.
|
-
- HY-13541
-
ADH-1
|
Others
|
Cancer
|
ADH-1, an N-cadherin antagonist, inhibits N-cadherin mediated cell adhesion.
|
-
- HY-B0535
-
-
- HY-B0312
-
-
- HY-15723
-
NSC 23766
|
Ras
|
Cancer
|
NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
|
-
- HY-12053
-
-
- HY-16268
-
Kartogenin
KGN
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
|
-
- HY-17406
-
Tolcapone
Ro 40-7592
|
COMT
Amyloid-β
|
Neurological Disease
|
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-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-100236
-
Madrasin
DDD00107587
|
Others
|
Cancer
|
Madrasin (DDD00107587) is a splicing inhibitor that prevents formation of both splicing intermediates and products in vitro and interferes with one or more early steps in the pathway of spliceosome assembly. Madrasin also can inhibit pre-mRNA splicing in vitro and modify splicing of endogenous pre-mRNA in cells.
|
-
- HY-122571
-
Retro-2
|
Filovirus
Parasite
Autophagy
|
Cancer
Infection
|
Retro-2 is a selective inhibitor of retrograde protein trafficking at the endosome-trans-Golgi network interface. Retro-2 is an ebolavirus (EBOV) infection inhibitor with an EC50 of 12.2 µM in HeLa cells. Retro-2 induces cell autophagy.
|
-
- HY-17372
-
Rofecoxib
MK 966
|
COX
|
Inflammation/Immunology
Cancer
|
Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
|
-
- HY-15416
-
-
- HY-N1990
-
Gypenoside XLIX
|
PPAR
|
Inflammation/Immunology
Cardiovascular Disease
|
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
|
-
- HY-126324
-
IV-23
|
Apoptosis
|
Cancer
|
IV-23 (Compound 20) is a potent Noxa mediated apoptosis inducer, and it is a promising anticancer agent with potential. IV-23 inhibits cell growths in vitro and in vivo, reduces colony formation, arrests cell cycle at M phase, and induces esophageal squamous cell carcinoma (ESCC).
|
-
- HY-W011434
-
Triglycidyl isocyanurate
TGIC; Teroxirone
|
MDM-2/p53
Apoptosis
|
Cancer
Inflammation/Immunology
|
Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities. Triglycidyl isocyanurate inhibits the growth of non-small-cell-lung cancer cells via p53 activation. Triglycidyl isocyanurate induces cell apoptosis. Triglycidyl isocyanurate can be used for cancer research.
|
-
- HY-15894A
-
BQ-788
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM.
|
-
- HY-W009749
-
L-Cystathionine
|
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
|
L-Cystathionine is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine plays an important role in cardiovascular protection.
|
-
- HY-N0171B
-
Beta-Sitosterol (purity>75%)
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>75%) includes 75% β-sitosterol and 10% campesterol. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>75%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-106934
-
Peldesine
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-106934A
-
Peldesine dihydrochloride
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-100303A
-
FR194738
|
Others
|
Metabolic Disease
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-16904
-
RI-2
|
RAD51
|
Cancer
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-100004
-
-
- HY-114305
-
A1874
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-109049
-
Adavivint
SM04690; Lorecivivint
|
Wnt
|
Inflammation/Immunology
Cancer
|
Adavivint (SM04690; Lorecivivint) is a potent and selective inhibitor of canonical Wnt signaling, with an EC50 of 19.5 nM via a high-throughput TCF/LEF-reporter assay in SW480 colon cancer cells.
|
-
- HY-16191
-
ELR510444
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
|
-
- HY-13057
-
O6BTG-octylglucoside
Glucose-conjugated MGMT inhibitor
|
DNA Methyltransferase
|
Cancer
|
O6BTG-octylglucoside is a potent O 6-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC50s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.
|
-
- HY-12521
-
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
|
-
- HY-101664
-
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- 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-136833
-
-
- HY-115686
-
-
- HY-130254
-
Src Inhibitor 3
|
Src
|
Cancer
Inflammation/Immunology
|
Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling.
|
-
- HY-15355
-
Loviride
R 89439
|
Reverse Transcriptase
HIV
|
Infection
|
Loviride (R 89439) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), with an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
|
-
- HY-111475
-
-
- HY-19702
-
-
- HY-131007
-
FFN270 hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
|
FFN270 hydrochloride, a fluorescent tracer of norepinephrine, is a fluorescent substrate of the norepinephrine and vesicular monoamine transporters. FFN270 hydrochloride exhibits two resolved absorption/excitation maxima depending on solvent pH (FFN270 ex: 320 nm or 365 nm, em: 475 nm) and can function as ratiometric fluorescent pH-sensors.
|
-
- HY-D0147
-
Resorufin pentyl ether
Pentoxyresorufin
|
Bacterial
|
Infection
|
Resorufin pentyl ether (Pentoxyresorufin) is a Resazurin (HY-111391) analogue. Resorufin pentyl ether can function as a substrate probe to characterize and differentiate between a variety of inducers of cytochromes P-450. Resorufin pentyl ether has bactericidal activity against N. gonorrhoeae.
|
-
- 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-76474
-
BAY 61-3606
|
Syk
Apoptosis
|
Cancer
Inflammation/Immunology
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-14985
-
BAY 61-3606 dihydrochloride
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-10225
-
Belinostat
PXD101; PX105684
|
HDAC
Autophagy
|
Cancer
|
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
|
-
- HY-100693
-
-
- HY-13541A
-
-
- HY-101071A
-
Monastrol
(±)-Monastrol
|
Kinesin
Apoptosis
|
Cancer
|
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
|
-
- HY-18664
-
-
- HY-B0535A
-
-
- HY-19971
-
ML239
|
Others
|
Cancer
|
ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.
|
-
- HY-N0171
-
Beta-Sitosterol (purity>80%)
β-Sitosterol (purity>80%); 22,23-Dihydrostigmasterol (purity>80%)
|
Endogenous Metabolite
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Beta-Sitosterol (purity>80%) includes β-sitosterol (≥80%), stigmasterol, campesterol and brassicasterol mainly. Beta-Sitosterol is a plant sterol. Beta-Sitosterol (purity>98%) interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation.
|
-
- HY-12762
-
QS11
|
Others
|
Cancer
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-10218
-
Everolimus
RAD001; SDZ-RAD
|
mTOR
FKBP
Autophagy
Apoptosis
|
Cancer
|
Everolimus (RAD001) is a Rapamycin derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
|
-
- HY-15003
-
ATH686
|
FLT3
Apoptosis
|
Cancer
|
ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects.
|
-
- HY-117819
-
TMP920
|
ROR
|
Inflammation/Immunology
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-100853
-
IWP-O1
|
Porcupine
Wnt
|
Cancer
|
IWP-O1 is a highly potent Porcupine (Porcn) inhibitor, with an EC50 of 80 pM in L-Wnt-STF cells. IWP-O1 prevents the secretion of Wnt proteins. IWP-O1 suppresses the phosphorylation of Dvl2/3 and LRP6 in HeLa cells.
|
-
- HY-N3023
-
3,4-Dihydroxybenzylamine hydrobromide
NSC 263475 hydrobromide
|
DNA/RNA Synthesis
|
Cancer
|
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
|
-
- HY-107856
-
5-Fluorouridine
|
Others
|
Cancer
|
5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
|
-
- HY-124617A
-
AMXT-1501 tetrahydrochloride
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells. Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines.
|
-
- HY-102064
-
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-P1454
-
Fz7-21
Ac-LPSDDLEFWCHVMY-NH2
|
Wnt
|
Cancer
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2), a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-N1150
-
Thymidine
DThyd; NSC 21548
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Others
|
Thymidine, a specific precursor of deoxyribonucleic acid, is used as a cell synchronizing agent. Thymidine is a DNA synthesis inhibitor that can arrest cell at G1/S boundary, prior to DNA replication.
|
-
- HY-128607
-
Mcl1-IN-9
|
Bcl-2 Family
|
Cancer
|
Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
|
-
- HY-N6601
-
Pomolic acid
Randialic acid A
|
Apoptosis
|
Cancer
|
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
|
-
- HY-P1103
-
CTCE-9908
|
CXCR
|
Cancer
|
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
|
-
- HY-100321
-
-
- HY-19553
-
-
- HY-128595
-
MT-4
|
Others
|
Cancer
|
MT-4 blocks the TG2/FN complex at the interface between cancer cells and the tumor niche. MT-4 inhibits the adhesion of ovarian cancer (OC) cells to the peritoneum.
|
-
- HY-126075A
-
WS-383
|
E1/E2/E3 Enzyme
|
Cancer
|
WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
|
-
- HY-50909
-
Perifosine
KRX-0401; NSC 639966; D21266
|
Akt
Autophagy
Apoptosis
|
Cancer
|
Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
|
-
- HY-N2403
-
-
- HY-12682
-
Glutaminase C-IN-1
Compound 968
|
Glutaminase
|
Cancer
|
Glutaminase C-IN-1 (Compound 968) is an allosteric inhibitor of Glutaminase C that inhibits cancer cell growth without affecting their normal cellular counterparts.
|
-
- HY-100541
-
INH6
|
Apoptosis
|
Cancer
|
INH6 is a potent Nek2/Hec1 inhibitor; inhibits the growth of HeLa cells with an IC50 of 2.4 μM.
|
-
- HY-19352
-
-
- HY-13062
-
-
- HY-N7452
-
-
- HY-103111
-
MMPIP hydrochloride
|
mGluR
|
Neurological Disease
|
MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
|
-
- HY-107503
-
MMPIP
|
mGluR
|
Neurological Disease
|
MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice.
|
-
- HY-N5130
-
Effusol
|
Others
|
Neurological Disease
|
Effusol, a phenolic constituent from Juncus effuses, exhibits potent scavenging activity for DPPH and ABTS radicals, with IC50 values of 79 μM and 2.73 μM, respectively. Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline.
|
-
- HY-P2499
-
BAD (103-127) (human), FAM-labeled
|
Bcl-2 Family
|
Cancer
|
BAD (103-127) (human), FAM-labeled is a FAM-labeled human BAD (103-127) (HY-P2468). BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL.
|
-
- HY-113354
-
Anserine
|
Endogenous Metabolite
|
Neurological Disease
|
Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice.
|
-
- HY-B0944
-
Pidotimod
|
Bacterial
|
Inflammation/Immunology
|
Pidotimod is an orally active dipeptide immunostimulant with immunomodulatory properties on the adaptive and the innate immune responses. Pidotimod increases macrophage activity and humoral immune functions. Pidotimod can be used for the research of chronic bronchitis, chronic obstructive pulmonary disease (COPD), bronchiectasis, and chronic idiopathic urticaria,et al.
|
-
- HY-101849
-
Fasentin
|
GLUT
|
Cancer
Cardiovascular Disease
|
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.
|
-
- HY-126585
-
SAICAR
|
Endogenous Metabolite
|
Cancer
|
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions.
|
-
- HY-108476
-
INDY
|
DYRK
|
Cancer
|
INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells.
|
-
- HY-13018
-
MRT67307
|
IKK
ULK
Autophagy
|
Cancer
Inflammation/Immunology
|
MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
|
-
- HY-11005
-
BX-912
|
PDK-1
Apoptosis
|
Cancer
|
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis.
|
-
- HY-103397
-
Nanaomycin A
|
DNA Methyltransferase
Parasite
|
Cancer
Infection
|
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
|
-
- HY-13018A
-
-
- HY-125840
-
Belzutifan
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
|
-
- HY-P1318
-
Ac-RYYRIK-NH2
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-12810
-
EHop-016
|
Ras
|
Cancer
|
EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor. EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac, Rac-activated PAK1, lamellipodia formation, and cell migration.
|
-
- HY-10585
-
Valproic acid
VPA; 2-Propylpentanoic Acid
|
HDAC
Autophagy
Mitophagy
HIV
Notch
|
Cancer
|
Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
|
-
- HY-131904
-
POMHEX
|
Enolase
Apoptosis
|
Cancer
Metabolic Disease
|
POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific inhibitor of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis inhibitor.
|
-
- HY-W016099
-
3-Methyl-2-quinoxalinecarboxylic acid
MQCA
|
Others
|
Cancer
|
3-Methyl-2-quinoxalinecarboxylic acid (MQCA), an important N-oxide reductive metabolite of Quinocetone or Olaquindox, potently inhibits the growth of Chang liver cells through S phase arrest of the cell cycle.
|
-
- HY-110182
-
SP-141
|
MDM-2/p53
|
Cancer
|
SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells.
|
-
- HY-136195
-
TL13-110
|
ALK
|
Cancer
|
TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
|
-
- HY-136194
-
TL13-22
|
ALK
|
Cancer
|
TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
|
-
- HY-130608
-
Mutated EGFR-IN-3
|
EGFR
|
Cancer
|
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
|
-
- HY-P1454A
-
Fz7-21 TFA
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-101597
-
NVX-207
|
Apoptosis
|
Cancer
|
NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP.
|
-
- HY-117388
-
THI0019
|
Integrin
|
Inflammation/Immunology
|
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
|
-
- HY-P0069
-
D-JNKI-1
AM-111; XG-102
|
JNK
|
Others
|
D-JNKI-1 (AM-111) is a highly potent and cell-permeable peptide inhibitor of JNK.
|
-
- HY-U00458
-
K-80003
TX-803
|
Akt
|
Cancer
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-114361
-
-
- HY-101073
-
-
- HY-135846
-
PDD00031705
|
Others
|
Cancer
|
PDD00031705 is a benzimidazolone core cell-inactive inhibitor of Poly (ADP-ribose) glycohydrolase (PARG).
|
-
- HY-16691
-
-
- HY-12409
-
-
- HY-15773
-
-
- HY-101465
-
-
- HY-N6693
-
Valinomycin
NSC 122023
|
Bacterial
Apoptosis
Antibiotic
Autophagy
|
Infection
|
Valinomycin (NSC 122023) is a cyclic depsipeptide antibiotic first isolated from Streptomyces fulvissimus, act as a potassium selective ionophore. Valinomycin (NSC 122023) inhibits lymphocyte proliferation by its effects on the cell membrane, and induces apoptosis in CHO cells. Valinomycin induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
|
-
- HY-50895
-
Gefitinib
ZD1839
|
EGFR
Autophagy
|
Cancer
|
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
|
-
- HY-B0240
-
Disulfiram
Tetraethylthiuram disulfide; TETD
|
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
|
Metabolic Disease
Cancer
|
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells[1-4].
|
-
- HY-50895A
-
Gefitinib hydrochloride
ZD-1839 hydrochloride
|
EGFR
|
Cancer
|
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
|
-
- 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-135231
-
NL-1
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway.
|
-
- HY-12204
-
PFK-015
|
Autophagy
|
Cancer
|
PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.
|
-
- HY-12622
-
HSP70-IN-1
|
HSP
|
Cancer
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.
|
-
- HY-12444
-
Y15
FAK Inhibitor 14
|
FAK
|
Cancer
|
Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth.
|
-
- HY-112445
-
-
- HY-100303
-
-
- HY-124873
-
SERCA2a activator 1
|
Calcium Channel
|
Cardiovascular Disease
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
|
-
- HY-135318
-
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-129168
-
USP7-IN-5
|
Deubiquitinase
|
Cancer
|
USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
|
-
- HY-129169
-
USP7-IN-6
|
Deubiquitinase
|
Cancer
|
USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
|
-
- HY-P1318A
-
Ac-RYYRIK-NH2 TFA
|
Opioid Receptor
|
Neurological Disease
|
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
|
-
- HY-N4201
-
β-Hydroxyisovalerylshikonin
|
EGFR
Src
|
Cancer
|
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
|
-
- HY-112823
-
Almonertinib
HS-10296
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
|
-
- HY-112823B
-
Almonertinib hydrochloride
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.
|
-
- HY-P1746A
-
Protein Kinase C (19-31) (TFA)
PKC (19-31) (TFA)
|
PKC
|
Inflammation/Immunology
|
Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-P1746
-
Protein Kinase C (19-31)
PKC (19-31)
|
PKC
|
Inflammation/Immunology
|
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-12757
-
YHO-13177
|
BCRP
|
Cancer
|
YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
|
-
- HY-117421A
-
-
- HY-117421
-
-
- HY-B0392
-
-
- HY-16657
-
-
- HY-119808
-
-
- HY-126075
-
WS-383 free base
|
E1/E2/E3 Enzyme
|
Cancer
|
WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
|
-
- HY-100012
-
CBR-5884
|
Others
|
Cancer
|
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
|
-
- HY-N6733
-
Aphidicolin
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase.
Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus.
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
|
-
- HY-133016
-
M8891
|
Others
|
Cancer
Cardiovascular Disease
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
|
-
- HY-101297
-
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-N6791
-
KT5823
|
PKA
PKC
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
|
-
- HY-N6682
-
Cytochalasin D
Zygosporin A; NSC 209835
|
Arp2/3 Complex
Bacterial
Antibiotic
YAP
|
Infection
|
Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
|
-
- HY-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-P1932
-
-
- HY-111793
-
NUCC-390
|
CXCR
|
Neurological Disease
|
NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo.
|
-
- HY-111793A
-
NUCC-390 dihydrochloride
|
CXCR
|
Neurological Disease
|
NUCC-390 dihydrochloride is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 dihydrochloride induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100 (HY-10046). NUCC-390 dihydrochloride promotes nerve recovery of function after neurodegeneration in vivo.
|
-
- HY-P2468
-
BAD (103-127) (human)
|
Bcl-2 Family
|
Cancer
|
BAD (103-127) (human), the 25-mer Bad peptide, is derived from the BH3 domain of BAD, can antagonize the function of Bcl-xL. BAD (103-127) (human) is reported to have almost 800-fold higher affinity for Bcl-XL than the 16-mer peptide.
|
-
- HY-16214
-
FX-11
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell and a Ki value of 8 μM.
|
-
- HY-13229
-
BOC-D-FMK
|
Caspase
Apoptosis
|
Cancer
|
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
|
-
- HY-12688
-
Succinyl phosphonate
|
Endogenous Metabolite
Reactive Oxygen Species
|
Neurological Disease
|
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-15465A
-
-
- HY-17353
-
-
- HY-13506
-
M344
D 237; MS 344
|
HDAC
|
Cancer
|
M344 (D 237) is an inhibitor of histone deacetylase (IC50=100 nM) and an inducer of terminal cell fifferentiation.
|
-
- HY-16107
-
-
- HY-19725
-
-
- HY-13623A
-
Entecavir monohydrate
BMS200475 monohydrate; SQ34676 monohydrate
|
HBV
|
Infection
|
Entecavir monohydrate (BMS200475 monohydrate; SQ34676 monohydrate) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
|
-
- HY-15465
-
KN-93
|
CaMK
Autophagy
|
Cancer
|
KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
|
-
- 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.
|
-
- HY-13623
-
Entecavir
BMS200475; SQ34676
|
HBV
|
Infection
|
Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.
|
-
- HY-P9902
-
Pembrolizumab
MK-3475; Lambrolizumab
|
PD-1/PD-L1
|
Cancer
|
Pembrolizumab is a humanized antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
|
-
- HY-108248
-
-
- HY-100861
-
C-11
|
ADC Cytotoxin
|
Cancer
|
C-11 is a tubulin inhibitor and acts as a ADC cytotoxin, displays cytotoxicity for carcinoma cell lines.
|
-
- HY-17024
-
-
- HY-100269
-
-
- HY-12454
-
DM4
|
Microtubule/Tubulin
|
Cancer
|
DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody drug conjugate.
|
-
- HY-10455
-
-
- HY-13744
-
Rubitecan
RFS 2000; 9-Nitrocamptothecin
|
Topoisomerase
|
Cancer
|
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
|
-
- HY-N6932
-
-
- HY-111588
-
-
- HY-B1700A
-
Mivacurium dichloride
|
nAChR
|
Neurological Disease
|
Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
|
-
- HY-12681
-
CCT251545
|
Wnt
|
Cancer
|
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
|
-
- 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-13326
-
ASP3026
|
ALK
Apoptosis
|
Cancer
|
ASP3026 is a potent, selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 induces apoptosis of tumor cells. ASP3026 can be used for the research of non-small cell lung cancer (NSCLC).
|
-
- HY-108701
-
Nampt-IN-3
|
NAMPT
HDAC
Autophagy
Apoptosis
|
Cancer
|
Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
|
-
- HY-116147
-
Ceranib-2
|
LPL Receptor
Apoptosis
|
Cancer
|
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.
|
-
- HY-118482
-
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-125911
-
Gossypin
|
NF-κB
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
Gossypin is a flavone isolated from Hibiscus vitifolius and has antioxidant, antiinflammatory, anticancer, anticataract, antidiabetic, analgesic and hepatoprotective activities. Gossypin inhibits NF-κB and NF-κB-regulated gene expression. Gossypin inhibits RANKL-induced osteoclastogenesis both in mouse primary bone marrow cells and RAW 264.7 cells in vitro.
|
-
- HY-136555
-
GSK717
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
|
-
- HY-N0293
-
Paeoniflorin
Peoniflorin
|
HSP
|
Neurological Disease
|
Paeoniflorin (Peoniflorin), a heat shock protein-inducing compound and a pinane monoterpene glycoside with various bioactivities, such as anticancer effects, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, reducing blood viscosity and anti-inflammatory activity. paeoniflorin protects PC12 cells from MPP + and acidic damage via autophagic pathway.
|
-
- HY-12326A
-
c-di-AMP sodium
Cyclic diadenylate sodium; Cyclic-di-AMP sodium
|
STING
Bacterial
Endogenous Metabolite
|
Inflammation/Immunology
|
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
|
-
- HY-122815
-
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-111640
-
3'-Azido-3'-deoxy-5-methylcytidine
|
HIV
Reverse Transcriptase
|
Infection
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells.
|
-
- HY-107407
-
SB-218078
|
Checkpoint Kinase (Chk)
CDK
PKC
Apoptosis
|
Cancer
|
SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest.
|
-
- 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-N2600
-
Kuwanon H
|
Bombesin Receptor
|
Cancer
|
Kuwanon H is a flavonoid isolated from Morus bombycis, which acts as a potent non-peptide bombesin receptor antagonist. Kuwanon H selectively inhibits binding of gastrin releasing peptide CRP to GRP-preferring recepotr, with a Ki value of 290 nM in cells.
|
-
- HY-128605
-
PD-1-IN-22
|
PD-1/PD-L1
|
Cancer
|
PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction inhibitor with an IC50 of 92.3 nM.
|
-
- HY-100111
-
-
- HY-W011044
-
CID 5951923
|
KLF
|
Cancer
|
CID 5951923 is a potent inhibitor of Krüppel-like factor 5 (KLF5), with an IC50 of 603 nM. CID 5951923 can inhibit proliferation of cancer cells in vitro.
|
-
- HY-13991
-
CCG-1423
|
Ras
|
Cancer
|
CCG-1423 is a novel inhibitor of RhoA/C-mediated gene transcription that is capable of inhibiting invasion of PC-3 prostate cancer cells in a Matrigel model of metastasis.
|
-
- HY-16667
-
HLM006474
|
Others
|
Cancer
|
HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
|
-
- HY-100223
-
-
- HY-115570
-
GW406108X
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
|
-
- HY-115510
-
SPR inhibitor 3
SPRi3
|
Others
|
Inflammation/Immunology
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-12688A
-
Succinyl phosphonate trisodium salt
|
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Metabolic Disease
Neurological Disease
|
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-122615
-
SPOP-IN-6b
|
Others
|
Cancer
|
SPOP-IN-6b is a speckle-type POZ protein (SPOP) inhibitor extracted from patent CN 107141287, SPOP-B-88.
|
-
- HY-111418
-
-
- HY-12808
-
-
- HY-18665
-
-
- HY-17602
-
Amcasertib
BBI503
|
Others
|
Cancer
|
Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.
|
-
- HY-14394
-
TBB
NSC 231634; Casein Kinase II Inhibitor I
|
Casein Kinase
|
Cancer
|
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
|
-
- HY-13257
-
Thiazovivin
|
ROCK
|
Cancer
|
Thiazovivin is a potent ROCK inhibitor, which can protect human embryonic stem cells. Thiazovivin improves the efficiency of iPSC generation.
|
-
- HY-101405
-
-
- HY-13867
-
-
- HY-112125A
-
-
- HY-N0125
-
-
- HY-17567B
-
Heparin Lithium salt
|
Autophagy
|
Others
|
Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII). Heparin Lithium salt significantly inhibits exosome-cell interactions.
|
-
- HY-101523
-
Cdc7-IN-1
|
CDK
|
Cancer
|
Cdc7-IN-1 (Compound 13) is a highly potent, selective and ATP competitive inhibitor of Cdc7 kinase, with an IC50 value of 0.6 nM at 1 mM ATP and with slow off-rate characteristics. Cdc7-IN-1 potently inhibits Cdc7 activity in cancer cells, and effectively induces cell death.
|
-
- 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-17406S
-
Tolcapone D7
Ro 40-7592 D7
|
COMT
Amyloid-β
|
Neurological Disease
|
Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-N6843
-
Arnicolide D
|
Caspase
PI3K
Akt
mTOR
STAT
|
Cancer
|
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner.
|
-
- HY-N4100
-
Trilobatin
|
HIV
SGLT
|
Infection
|
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
|
-
- HY-N2515
-
Ginsenoside Rk1
|
NF-κB
PI3K
JAK
Apoptosis
|
Cancer
Inflammation/Immunology
|
Ginsenoside Rk1 is a unique component created by processing the ginseng plant (mainly Sung Ginseng, SG) at high temperatures.
Ginsenoside Rk1 has anti-inflammatory effect, suppresses the activation of Jak2/Stat3 signaling pathway and NF-κB.
Ginsenoside Rk1 has anti-tumor effect, antiplatelet aggregation activities, anti-insulin resistance, nephroprotective effect, antimicrobial effect, cognitive function enhancement, lipid accumulation reduction and prevents osteoporosis.
Ginsenoside Rk1 induces cell apoptosis by triggering intracellular reactive oxygen species (ROS) generation and blocking PI3K/Akt pathway.
|
-
- HY-112257
-
S-23
|
Androgen Receptor
|
Metabolic Disease
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats.
|
-
- HY-137498
-
EBOV/MARV-IN-1
|
Others
|
Infection
|
EBOV/MARV-IN-1 is a potent inhibitor of Ebola virus (EBOV) and Marburg virus (MARV), with broad-spectrum activity (EC50=0.31, and 0.82 µM, respectively) and low cytotoxicity (SI>100) in HeLa cells.
|
-
- HY-77293
-
(E)-[6]-Dehydroparadol
|
Apoptosis
Keap1-Nrf2
|
Cancer
|
(E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells.
|
-
- HY-119402
-
BCL6-IN-8c
|
Bcl-2 Family
|
Cancer
|
BCL6-IN-8c is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay.
|
-
- HY-B0990
-
Thiostrepton
|
Bacterial
Antibiotic
|
Infection
|
Thiostrepton is a thiazole antibiotic which selectively inhibits FOXM1. FOXM1 binds to YAP/TEAD complex. YAP/TEAD/FOXM1 complex binding at regulatory regions of genes governing cell cycle may impact cell proliferation.
|
-
- HY-N7526
-
Naphthazarin
DHNQ; 5,8-Dihydroxy-1,4-naphthoquinone
|
Apoptosis
|
Cancer
Neurological Disease
|
Naphthazarin (DHNQ) is a naturally occurring compound. Naphthazarin is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. Naphthazarin triggers apoptosis and has anti-tumor effects.
|
-
- HY-P1428
-
RFRP-1(human)
|
Neuropeptide Y Receptor
|
|
RFRP-1(human) is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-17552
-
sn-Glycero-3-phosphocholine
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
AChE
Endogenous Metabolite
|
Neurological Disease
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolera |