Search Result
Results for "Aminopeptidase b Inhibitors" in MCE Product Catalog:
1169
Inhibitors & Agonists
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-120868
-
-
- HY-136614
-
|
H-Val-βNA
L-Valine β-naphthylamide
|
Others
|
Others
|
|
H-Val-βNA (L-Valine β-naphthylamide) can be used as an aminopeptidase and a Valine arylamidase substrate.
|
-
- HY-133125
-
|
ERAP1-IN-1
|
Others
|
Inflammation/Immunology
|
|
ERAP1-IN-1 is an endoplasmic reticulum aminopeptidase 1 (ERAP1) inhibitor. ERAP1-IN-1 competitively inhibits ERAP1 activity towards a nonamer peptide representative of physiological substrates.
|
-
- HY-U00439
-
-
- HY-115194
-
|
Amastatin hydrochloride
|
Aminopeptidase
Bacterial
|
Infection
|
|
Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase.
|
-
- HY-17624
-
|
Framycetin
Neomycin B; Fradiomycin B
|
Bacterial
|
Infection
|
|
Framycetin (Neomycin B), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
|
-
- HY-N0695
-
-
- HY-101932
-
-
- HY-17624A
-
|
Framycetin sulfate
Neomycin B sulfate; Fradiomycin B sulfate
|
Bacterial
|
Infection
|
|
Framycetin sulfate (Neomycin B sulfate), an aminoglycoside antibiotic, is a potent RNase P cleavage activity inhibitor with a Ki of 35 μM. Framycetin sulfate competes for specific divalent metal ion binding sites in RNase P RNA. Framycetin sulfate inhibits hammerhead ribozyme with a Ki of 13.5 μM. Framycetin sulfate, a 5″-azido neomycin B precursor, binds the Drosha site in miR-525 and is used for hepatic encephalopathy and enteropathogenic E. coli infections.
|
-
- HY-112462
-
-
- HY-113368
-
-
- HY-N2132
-
|
Flavokawain B
Flavokavain B
|
Apoptosis
|
Cancer
|
|
Flavokawain B (Flavokavain B) is a chalcone isolated from the root extracts of kava-kava plant and a potent apoptosis inducer for inhibiting the growth of various cancer cell lines. Flavokawain B (Flavokavain B) shows strong antiangiogenic activity. Flavokawain B (Flavokavain B) inhibits human brain endothelial cell (HUVEC) migration and tube formation with very low and non-toxic concentrations.
|
-
- HY-114269
-
-
- HY-14807
-
-
- HY-P1044
-
|
Spinorphin
LVV-hemorphin-4
|
Others
|
Neurological Disease
|
|
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect.
|
-
- HY-D0004
-
|
Azure B
Azure B chloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects.
|
-
- HY-125729
-
-
- 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-101995
-
|
Ridaifen-B
RID-B
|
Estrogen Receptor/ERR
Cannabinoid Receptor
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Ridaifen-B (RID-B) is a potent antagonist of estrogen receptor α (ERα) with IC50 of 52.4 nM, a tamoxifen derivative. Ridaifen-B is a high affinity, selective, inverse agonist at CB2 receptor (Ki=43.7 nM) over 17 folds CB1 receptor (Ki=732 nM). Ridaifen-B modulates G-protein (IC50=300 nM) and adenylyl cyclase activity with potency values predicted by CB2 affinity (IC50=134 nM). Ridaifen-B has anti-inflammatory, anti-cancer, and anti-osteoclastogenic effects.
|
-
- HY-P1043A
-
|
NGR peptide Trifluoroacetate
|
Aminopeptidase
|
Cancer
|
|
NGR peptide Trifluoroacetate containing the asparagine-glycine-arginine (NGR) motif is recognized by CD13/aminopeptidase N (APN) receptor isoforms that are selectively overexpressed in tumor neovasculature.
|
-
- HY-N0800
-
|
Protosappanin B
(-)-Protosappanin B
|
Apoptosis
|
Cancer
|
|
Protosappanin B is a phenolic compound extracted from Lignum Sappan. Anti-cancer activity. Protosappanin B induces apoptosis and causes G1 cell cycle arrest in human bladder cancer cells.
|
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- HY-N6261
-
|
Epimagnolin B
|
Others
|
Inflammation/Immunology
|
|
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
|
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- HY-N2303
-
-
- HY-107208
-
-
- HY-111320
-
|
Chrysomycin B
|
Bacterial
Antibiotic
|
|
|
Chrysomycin B is an antibiotic isolated from a strain of Streptomyces. Chrysomycin B causes DNA damage in the human lung adenocarcinoma A549 cell line and inhibits topoisomerase II. Chrysomycin B suppresses the growth of transplantable tumors in mice.
|
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- HY-101462
-
-
- HY-N6248
-
-
- HY-B0134
-
-
- HY-133108
-
-
- HY-N0660
-
-
- HY-N1453
-
|
Hypocrellin B
|
Apoptosis
|
Cancer
Infection
|
|
Hypocrellin B, a pigment isolated from the fungi Hypocrella bambusae and Shiraia bambusicola, is an apoptosis inducer. Hypocrellin B can be used as a photosensitizer for photodynamic therapy of cancer. Hypocrellin B also has antimicrobial and antileishmanial activities.
|
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- HY-15473
-
|
MLN120B
ML120B
|
IKK
|
Cancer
|
|
MLN120B (ML120B) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-15473A
-
|
MLN120B dihydrochloride
ML120B dihydrochloride
|
IKK
|
Cancer
Inflammation/Immunology
|
|
MLN120B dihydrochloride (ML120B dihydrochloride) is a potent, ATP competitive, and orally active inhibitor of IKKβ with an IC50 of 60 nM. MLN120B inhibits multiple myeloma cell growth in vitro and in vivo and also can be used for the research of rheumatoid arthritis.
|
-
- HY-N0811
-
|
Anemarsaponin B
|
NO Synthase
COX
NF-κB
|
Inflammation/Immunology
|
|
Anemarsaponin B is a steroidal saponin isolated from the rhizomes of A. asphodeloides (Liliaceae). Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
|
-
- 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-N6696
-
|
Aflatoxin B2
|
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
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- HY-N4189
-
|
Isocucurbitacin B
|
Others
|
Cancer
|
|
Isocucurbitacin B is a potent cytotoxic compound isolated from Helicteres rswa L. (Sterculiaceae). Isocucurbitacin B possesses anti-tumor acticity.
|
-
- HY-13992
-
|
AP20187
B/B Homodimerizer
|
FKBP
|
Metabolic Disease
|
|
AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein (FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
|
-
- HY-N1476
-
|
Heterophyllin B
|
PI3K
|
Cancer
|
|
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer.
|
-
- HY-N3388
-
-
- HY-N6037
-
|
Gardenin B
|
Apoptosis
|
Cancer
|
|
Gardenin B is a flavonoid isolated from Baccharis scandens. Gardenin B induces cell death in human leukemia cells involves multiple caspases.
|
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- HY-N3806
-
-
- HY-N0582
-
|
Qingyangshengenin B
|
Others
|
Neurological Disease
|
|
Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.
|
-
- HY-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-N6808
-
|
Rebaudioside B
|
Others
|
Others
|
|
Rebaudioside B is the minor constituent isolated from the leaves of Stevia rebaudiana Bertoni. Rebaudioside B tastes about 150 times sweeter than sucrose .
|
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- HY-N0429
-
|
Diosbulbin B
|
Others
|
Cancer
|
|
Diosbulbin B is a diterpene lactone isolated from D. bulbifera L., with anti-tumor activity. Diosbulbin B can induce liver injury.
|
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- HY-15335
-
-
- HY-N6780
-
|
Ophiobolin B
|
Fungal
|
Infection
|
|
Ophiobolin B, a sesterterpene metabolite of Helminthosporium oryzae, inhibits proton extrusion from maize coleoptiles. Ophiobolin B inhibits fusicoccin (FC) promoted proton extrusion, potassium uptake and cell enlargement. The MIC values with the antifungal effect of Ophiobolins B on different zygomycetes is 25–50 μg/mL.
|
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- HY-N4268
-
|
Tenuifoliside B
|
Others
|
Neurological Disease
|
|
Tenuifoliside B, a component isolated from Polygalae Radix, inhibits potassium cyanide (KCN)-induced hypoxia and scopolamine-induced memory impairment. Tenuifoliside B shows potential cognitive improvement and cerebral protective effects. Tenuifoliside B has potential to become an anti-AD lead compound.
|
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- HY-16937
-
-
- HY-15311
-
-
- HY-130999
-
|
Microcolin B
|
Others
|
Inflammation/Immunology
|
|
Microcolin B is an extremely potent unusual acylpeptide, proline-containing potent immunosuppressant. Microcolin B is isolated from blue-green alga Lyngbya majuscule.
|
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- HY-N7292
-
-
- HY-N0539
-
|
Calceolarioside B
|
Others
|
Cancer
|
|
Calceolarioside B is a natural product isolated from Stauntonia hexaphylla leaves. Calceolarioside B exhibits significant inhibitory activity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
|
-
- HY-N2148
-
|
Cytosporone B
Csn-B; Dothiorelone G
|
Others
|
Cancer
|
|
Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC50 of 0.278 nM.
|
-
- HY-N6701
-
|
Dihydrocytochalasin B
|
Arp2/3 Complex
|
Cancer
|
|
Dihydrocytochalasin B (H2CB) is a Cytokinesis inhibitor and changes the morphology of the cells, similar to that of cytochalasin B; does not inhibit glucose transport. Dihydrocytochalasin B (H2CB) disrupts the actin structure and inhibits the ability of growth factors to stimulate DNA synthesis, reversibly blocks initiation of DNA synthesis. Dihydrocytochalasin B (H2CB) inhibits active calcium transport and causes a Ca 2+increase in the mucosal scrapings.
|
-
- HY-A0248A
-
|
Polymyxin B1
|
Bacterial
|
Infection
|
|
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistant Gram-negative bacterial infections treatment.
|
-
- HY-126804
-
|
Safracin B
|
Antibiotic
|
Cancer
Infection
|
|
Safracin B, a tetrahydroisoquinoline (THIQ) alkaloid, is a naturally occurring antibiotic from Pseudomonas fluorescens. Safracin B exhibits broad spectrum antimicrobial and strong antitumor activities.
|
-
- HY-W018791
-
|
Bifendate
DDB
|
HBV
|
Infection
|
|
Bifendate (DDB) is a synthetic intermediate of Schisandrin C with anti-HBV efficacy in research of chronic hepatitis B.
|
-
- HY-N1280
-
|
Semilicoisoflavone B
|
Amyloid-β
|
Neurological Disease
|
|
Semilicoisoflavone B, an isoflavone, mainly derived from Glycyrrhiza uralensis Fisch.. Semilicoisoflavone B reduces amyloid β (Aβ) secretion by inhibiting β-secretase-1 (BACE1) expression and activity. Semilicoisoflavone B decreases BACE1 expression mainly through increasing PPARγ expression and inhibiting STAT3 phosphorylation.
|
-
- HY-126307
-
|
Urolithin B
|
NF-κB
JNK
ERK
Akt
AMPK
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
|
-
- HY-N3028
-
|
Taccalonolide B
|
Microtubule/Tubulin
|
Cancer
|
|
Taccalonolide B is microtubule stabilizer isolated from Tacca plantaginea, with antitumor activity. Taccalonolide B is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug-resistance protein (MRP7). Taccalonolide B inhibits growth of SK-OV-3 cells with an IC50 of 208 nM.
|
-
- 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-120501
-
|
B022
|
NF-κB
|
Inflammation/Immunology
|
|
B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor with a Ki of 4.2 nM. B022 protects liver from toxin-induced inflammation, oxidative stress, and injury.
|
-
- HY-P1178
-
|
Cyclotraxin B
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-N2043
-
|
Huperzine B
|
AChE
|
Neurological Disease
|
|
Huperzine B is a Lycopodium alkaloid isolated from Huperzia serrata and a highly selective acetylcholinesterase (AChE) inhibitor. Huperzine B can be uesd to can be used to improve Alzheimer's disease.
|
-
- HY-N0886
-
|
Aloin B
Aloin-B; Isobarbaloin
|
Others
|
Others
|
|
Aloin B is one isomer of Aloin; Aloin is a physiologically active anthraquinone present in aloe.
|
-
- HY-N6955
-
-
- HY-101749
-
-
- HY-N6074
-
|
Soyasapogenol B
|
Autophagy
Apoptosis
|
Cancer
|
|
Soyasapogenol B, an ingredient of soybean, exerts anti-proliferative, anti-metastatic activities. Soyasapogenol B triggers endoplasmic reticulum stress, which mediates apoptosis and autophagy in colorectal cancer.
|
-
- HY-10704
-
|
PTP1B-IN-1
PTP1B inhibitor
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
|
-
- HY-113331
-
|
Thromboxane B2
|
Others
|
|
|
Thromboxane B2 is a prostaglandin derivative that is released during anaphylaxis. Thromboxane B2 induces arterial contraction and platelet aggregation.
|
-
- HY-101855
-
|
Anle138b
|
Others
|
Neurological Disease
|
|
Anle138b is an oligomeric aggregation inhibitor. Anle138b is an oligomer modulator for neurodegenerative diseases such Parkinson's disease.
|
-
- HY-N4218
-
-
- HY-N3807
-
|
Enniatin B1
|
Acyltransferase
ERK
NF-κB
|
Cancer
Infection
Cardiovascular Disease
|
|
Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.
|
-
- 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-N1570
-
-
- HY-N2006
-
|
Ganoderic acid B
|
HIV Protease
|
Infection
|
|
Ganoderic acid B is a triterpene isolated from a mushroom Ganoderma lucidum. Ganoderic acid B inhibits the activation of Epstein-Barr virus (EBV) antigens as telomerase inhibitor. Ganoderic acid B is a moderately active inhibitor against HIV-1 protease.
|
-
- HY-P1114
-
|
2B-(SP)
|
GSK-3
|
Neurological Disease
|
|
2B-(SP) is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) is readily phosphorylated by both the α and β isoforms of GSK-3.
|
-
- HY-19505
-
|
TPA-023B
|
GABA Receptor
|
Neurological Disease
|
|
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
|
-
- HY-N6939
-
-
- HY-112051
-
-
- HY-N0796
-
-
- HY-N6719
-
|
Fumonisin B1
|
Acyltransferase
|
Infection
|
|
Fumonisin B1 is a mycotoxin produced from Fusarium moniliforme. Fumonisin B1 is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis. Fumonisin B1 is the most abundant and toxic fumonisin.
|
-
- HY-B0586
-
-
- HY-136453
-
-
- HY-N6786
-
|
Ochratoxin B
|
Others
|
Cancer
|
|
Ochratoxin B, a secondary metabolite of Aspergillus ochraceus, is the nonchlorinated analogue of the mycotoxin Ochratoxin A. Ochratoxin B has been shown to reduce the toxic effects of Ochratoxin A, and it is one of the most potent renal carcinogens in rodents.
|
-
- HY-N0753
-
|
Eupalinolide B
|
Others
|
Cancer
|
|
Eupalinolide B is a germacrane sesquiterpene isolated from Eupatorium lindleyanum. Eupalinolide B demonstrates potent cytotoxicity against A-549, BGC-823 and HL-60 tumour cell lines.
|
-
- HY-U00343
-
-
- HY-N4249
-
-
- HY-N2171
-
-
- HY-N2250
-
-
- HY-N6897
-
-
- HY-N1145
-
-
- HY-N3587
-
-
- HY-N6922
-
-
- HY-N0266
-
-
- HY-N7045
-
|
Isosilybin B
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
Isosilybin B, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity via inhibiting proliferation and inducing G1 phase arrest and apoptosis. Isosilybin B causes androgen receptor (AR) degradation.
|
-
- HY-N1243
-
|
Tubulysin B
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties.Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-116213
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-P0242
-
-
- HY-P0241
-
-
- HY-18219
-
-
- HY-136128
-
|
H3B-120
|
Potassium Channel
|
Cancer
|
|
H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity.
|
-
- HY-N0029
-
|
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-N7046
-
|
Silybin B
|
Amyloid-β
|
Cancer
Neurological Disease
|
|
Silybin B, a flavonolignan separated from Silybum marianum, has anti-tumor activity. Silybin B is the most potent antifibrillogenic and anti-oligomeric component of silymarin and proposes it as a promising anti Alzheimer’s disease drug candidate.
|
-
- HY-136556
-
-
- HY-N6690
-
|
Destruxin B
|
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
Infection
|
|
Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
|
-
- HY-N0307
-
|
Ciwujianoside B
|
Bcl-2 Family
|
Neurological Disease
|
|
Ciwujianoside B is isolated from Eleutherococcus senticosus leaf, is able to penetrate and work in the brain after the oral administration. Ciwujianoside B significantly enhances object recognition memory.
Ciwujianoside B shows radioprotective effects on the hematopoietic system in mice, which is associated with changes in the cell cycle, reduces DNA damage and down-regulates the ratio of Bax/Bcl-2 in bone marrow cells exposed to radiation.
|
-
- HY-135327
-
|
Amphotericin B methyl ester
|
HIV
Fungal
|
Infection
|
|
Amphotericin B methyl ester is the methyl ester derivative of the polyene antibiotic Amphotericin B (A634250). Amphotericin B methyl ester is the cholesterol-binding compound possesses significant antifungal activity. Amphotericin B methyl ester disrupts HIV-1 particle production and potently inhibits HIV-1 replication.
|
-
- HY-N6839
-
-
- HY-100462
-
-
- HY-N2016
-
|
Arteannuin B
|
SARS-CoV
Ferroptosis
|
Infection
|
|
Arteannuin B co-occurs with artemisinin, which is the potent antimalarial principle of the Chinese medicinal herb Artemisia annua (Asteraceae). Arteannuin B shows anti-SARS-CoV-2 potential with an EC50 of 10.28 μM.
|
-
- HY-N2099
-
|
Onjisaponin B
|
Autophagy
|
Neurological Disease
|
|
Onjisaponin B is a natural product derived from Radix Polygalae. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin in PC-12 cells, and exbibits potential therapeutic effects on Parkinson disease and Huntington disease.
|
-
- HY-N0366
-
|
Sennoside B
|
PDGFR
|
Cancer
|
|
Sennoside B is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside B can inhibit PDGF-stimulated cell proliferation by binding to PDGF-BB and its receptor and by down-regulating the PDGFR-beta signaling pathway.
|
-
- HY-128978
-
-
- HY-N4135
-
-
- HY-N0259
-
|
Epimedin B
|
Others
|
Others
|
|
Epimedin B, a component extracted from Epimedii Folium, is reported to have antiosteoporotic activity.
|
-
- HY-P0092
-
-
- HY-N0874
-
-
- HY-N2088
-
-
- HY-127018
-
|
Maltoheptaose
|
Others
|
Metabolic Disease
|
|
Maltoheptaose is an activator of phosphorylase B to prepare heptulose-2-phosphate. Maltoheptaose is a maltooligosaccharide contanins seven glucose units.
|
-
- HY-127018A
-
-
- HY-117391
-
-
- HY-P1349
-
-
- HY-135281
-
-
- HY-112596
-
-
- HY-N4219
-
-
- HY-108518
-
-
- HY-106783
-
|
Polymyxin B nonapeptide
|
Bacterial
Antibiotic
|
Infection
|
|
Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- HY-P1339
-
-
- HY-N3216
-
-
- 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-N5008
-
-
- HY-N4319
-
-
- HY-N1448
-
-
- HY-N7439
-
|
Mogroside VI B
|
PGC-1α
|
Metabolic Disease
|
|
Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription.
|
-
- HY-15695
-
-
- HY-P1178A
-
|
Cyclotraxin B TFA
|
Trk Receptor
|
Neurological Disease
|
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
|
-
- HY-N0333
-
-
- HY-A0248
-
-
- HY-101799
-
-
- HY-N1435
-
|
Oroxin B
|
Apoptosis
PI3K
PTEN
Autophagy
|
Cancer
|
|
Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent.
Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT.
Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
|
-
- HY-N0692
-
|
Schisandrol B
Gomisin-A; TJN-101; Wuweizi alcohol-B
|
Autophagy
|
Cancer
|
|
Schisandrol B (Gomisin-A;TJN-101;Wuweizi alcohol-B) is one of its major active constituents of traditional hepato-protective Chinese medicine, Schisandra sphenanthera.
|
-
- HY-12054A
-
-
- HY-12054
-
-
- HY-N0416
-
-
- HY-N2234
-
-
- HY-N2605
-
-
- HY-131099
-
|
Enduracidin B
|
Antibiotic
|
Infection
|
|
Enduracidin B is a major component of Enduracidin. Enduracidin is a polypeptide antibiotic produced by Streptomyces fungicides.
|
-
- HY-N2634
-
|
Uvarigranol B
|
Others
|
Others
|
|
Uvarigranol B, a polyoxygenated cyclohexene, is obtained from the roots of Uvaria grandiflora Roxb (Annonaceae).
|
-
- HY-N5052
-
-
- HY-122306
-
|
Ansatrienin B
Mycotrienin II
|
Antibiotic
Bacterial
|
Cancer
Infection
|
|
Ansatrienin B (Mycotrienin II) is an ansamycin antibiotic isolated from Streptomyces. Ansatrienin B is active against fungi and yeasts, but inactive against bacteria.Ansatrienin B displays antitumor antibiotic activity and can be used as an ADC Toxin.
|
-
- HY-15133
-
-
- HY-114314
-
|
BA-53038B
|
HBV
|
Infection
|
|
BA-53038B is a HBV core protein allosteric modulator (CpAM), binding to the HAP pocket and modulating HBV capsid assembly in a distinct manner, with an EC50 value of 3.32 μM.
|
-
- HY-108431
-
|
MN58b
|
Apoptosis
|
Cancer
|
|
MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity.
|
-
- HY-129545
-
-
- HY-P1114A
-
|
2B-(SP) (TFA)
|
GSK-3
|
Cancer
|
|
2B-(SP) TFA is a eIF2B-based substrate for glycogen synthase kinase-3 (GSK-3). 2B-(SP) TFA is readily phosphorylated by both the α and β isoforms of GSK-3.
|
-
- HY-N0373
-
|
Licochalcone B
|
Amyloid-β
|
Neurological Disease
|
|
Licochalcone B is an extract from the root of Glycyrrhiza inflate. Licochalcone B inhibits amyloid β (Aβ42) self-aggregation (IC50=2.16 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions.
|
-
- HY-N2124
-
|
Parishin B
|
Others
|
Cancer
|
|
Parishin B, a parishin derivative isolated from Gastrodia elata, may have antioxidant property.
|
-
- HY-N6819
-
-
- HY-N1432
-
|
Lirioprolioside B
|
Others
|
Cancer
|
|
Lirioprolioside B is a steroidal glycoside isolated from the underground organs of Liriope spicata var. prolifera.
|
-
- HY-131054
-
-
- HY-P1751
-
|
Ceratotoxin B
|
Bacterial
|
Infection
|
|
Ceratotoxins B is antibacterial peptide produced by the sexually mature females of Ceratitis capitata. Lytic and antibacterial activity .
|
-
- HY-A0040
-
-
- HY-136339
-
-
- HY-N2438
-
|
Methylophiopogonanone B
|
Ras
|
Others
|
|
Methylophiopogonanone B, homoisoflavonoid, is extracted from the root of Ophiopogon japonicas, shows high antioxidant ability. Methylophiopogonanone B increases GTP-Rho and acts via the Rho signaling pathway, inducing cell morphological change via actin cytoskeletal reorganization, including dendrite retraction and stress fiber formation.
|
-
- HY-B0684
-
|
Iopamidol
B-15000; SQ-13396
|
Others
|
Others
|
|
Iopamidol (B-15000; SQ-13396) is a nonionic, low-osmolar iodinated contrast agent.
|
-
- HY-N2393
-
-
- HY-N6784
-
-
- HY-100272
-
|
B220
|
HSV
CMV
|
Infection
Cancer
|
|
B220 is an antiviral agent which can inhibit the growth of HSV-1, HSV-2 and human cytomegalovirus (CMV).
|
-
- HY-100944
-
-
- HY-117289
-
-
- HY-N2218
-
-
- HY-B0490
-
-
- HY-107400
-
|
B I09
|
IRE1
|
Cancer
|
|
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
|
-
- HY-135890
-
-
- HY-N5135
-
|
Liriopesides B
Nolinospiroside F
|
Others
|
Others
|
|
Liriopesides B (Nolinospiroside F) is a steroidal saponin isolated from Ophiopogon japonicas. Liriopesides B has anti-oxidative and anti-aging effects.
|
-
- HY-104047
-
-
- HY-18227
-
|
B-Raf IN 1
|
Raf
|
Cancer
|
|
B-Raf IN 1 is a potent and selective B-Raf kinase inhibitor with an IC50 of 24 nM.
|
-
- HY-N0805
-
|
Alisol B 23-acetate
23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate
|
Others
|
Others
|
|
Alisol B 23-acetate, a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.
|
-
- HY-N0511
-
|
Aristolochic acid B
|
Others
|
Cancer
|
|
Aristolochic acid B is one of the major components of Aristolochic acids (AA) which are natural products derived from taxa in the Aristolochiaceae. Aristolochic acid is known to be a potent mutagen and carcinogen. Aristolochic acid B showes more carcinogenic risk than Aristolochic acid A in vivo.
|
-
- HY-N7384
-
-
- HY-N6916
-
-
- HY-100312
-
-
- HY-112596A
-
-
- HY-P0242A
-
-
- HY-112790
-
-
- HY-U00360
-
-
- 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-126246
-
|
CDC25B-IN-1
|
Phosphatase
|
Cancer
|
|
CDC25B-IN-1 (compound 4a) is a potent inhibitor of cell division cycle 25B (CDC25B) phosphatase, with a Ki of 8.5 μM. CDC25B-IN-1 potently inhibits cell proliferation and colony formation, causes an increase of the G2/M phase.
|
-
- HY-110259
-
-
- HY-112611
-
|
H3B-5942
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations.
|
-
- HY-N6256
-
-
- HY-14177A
-
-
- HY-14177
-
|
B-Raf inhibitor 1
|
Raf
|
Cancer
|
|
B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.
|
-
- HY-135646
-
|
Eleutheroside B1
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Eleutheroside B1, a coumarin compound, has a wide spectrum of anti-human influenza virus efficacy, with an IC50 value of 64-125 µg/ml. Eleutheroside B1 mediates its anti-influenza activity through POLR2A and N-glycosylation. Eleutheroside B1 inhibits the mRNA expression of several chemokine genes and the influenza nucleoprotein (NP) gene, and exhibits low cytotoxicity. Antiviral and anti-inflammatory activities.
|
-
- HY-N0247
-
-
- HY-15308
-
-
- HY-B0143
-
-
- HY-P1774
-
-
- HY-N6861
-
|
Lucidenic acid B
|
Apoptosis
|
Cancer
|
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
|
-
- HY-N0306
-
|
Hederasaponin B
|
Enterovirus
|
Infection
|
|
Hederasaponin B, isolated from Hedera helix, has broad-spectrum antiviral activity against various subgenotypes of Enterovirus 71 (EV71).
|
-
- HY-N6731
-
|
Hydrolyzed Fumonisin B2
|
Others
|
Infection
|
|
Hydrolyzed Fumonisin B2 (HFB2) is a hydrolysis product of fumonisins (HF), which retains biological activity. Hydrolyzed Fumonisin B2 (HFB2) exhibits phytotoxicity.
|
-
- HY-N0089
-
-
- HY-106783A
-
|
Polymyxin B nonapeptide TFA
|
Bacterial
|
Infection
|
|
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- HY-121513
-
|
Torcitabine
2'-Deoxy-L-cytidine
|
HBV
|
Infection
|
|
Torcitabine (2'-Deoxy-L-cytidine) is an antiviral agent. Torcitabine has the potential for chronic hepatitis B virus infection treatment.
|
-
- HY-N0082
-
-
- HY-101585
-
-
- HY-N6726
-
-
- HY-N7461
-
-
- HY-N4124
-
-
- HY-15756
-
|
PTP1B-IN-4
|
Phosphatase
|
Metabolic Disease
|
|
PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes.
|
-
- HY-N0901A
-
|
Corynoxine B
|
Autophagy
|
Cancer
|
|
Corynoxine B is an oxindole alkaloid isolated from Uncaria rhynchophylla (Miq.) Jacks (Gouteng in Chinese); a Beclin-1-dependent autophagy inducer.
|
-
- HY-N6672
-
-
- HY-115687
-
|
PDE4B-IN-2
|
Phosphodiesterase (PDE)
|
|
|
PDE4B-IN-2 is an orally active and selective PDE4B inhibitor (IC50=15 nM) and exhibits >100-fold selectivity for PDE4B over 4D. PDE4B-IN-2 regulates cAMP in inflammatory cells and inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. PDE4B-IN-2 reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. PDE4B-IN-2 also exhibits antidepressant-like effects.
|
-
- HY-N0479
-
|
Licarin B
(-)-Licarin B
|
PPAR
GLUT
|
Metabolic Disease
|
|
Licarin B, a nitric oxide production inhibitor extracted from the component of the seeds of Myristica fragrans, improves insulin sensitivity via PPARγ and activation of GLUT4 in the IRS-1/PI3K/AKT pathway.
|
-
- HY-113952
-
|
Actinonin
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
|
-
- HY-B0221
-
|
Amphotericin B
|
Fungal
Antibiotic
|
Infection
|
|
Amphotericin B is a polyene antifungal agent against a wide variety of fungal pathogens. It binds irreversibly to ergosterol, resulting in disruption of membrane integrity and ultimately cell death.
|
-
- HY-B0134B
-
-
- HY-B0134A
-
-
- HY-P1339A
-
-
- HY-133247
-
-
- HY-P1337
-
-
- HY-100241
-
-
- HY-N6868
-
-
- HY-17578
-
|
Pneumocandin B0
L-688786
|
Fungal
Antibiotic
|
Infection
|
|
Pneumocandin B0(L-688786), a key intermediate in the synthesis of the antifungal agent, Cancidas, has led to the identification of several materials with potential for improved performance.
|
-
- HY-N0704
-
|
Agrimol B
|
Sirtuin
PPAR
|
Metabolic Disease
|
|
Agrimol B is a polyphenol derived from Agrimonia pilosa Ledeb, suppresses adipogenesis via inducing SIRT1 translocation and expression, and reducing PPARγ expression.
|
-
- HY-N2345
-
|
Procyanidin B3
|
Histone Acetyltransferase
|
Cancer
|
|
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
|
-
- HY-N6615
-
|
Aflatoxin B1
|
Bacterial
Endogenous Metabolite
|
Cancer
Infection
|
|
Aflatoxin B1 (AFB1) is a Class 1A carcinogen, which is a secondary metabolite of Aspergillus flavus and A. parasiticus. Aflatoxin B1 (AFB1) mainly induces the transversion of G-->T in the third position of codon 249 of the p53 tumor suppressor gene, resulting in mutation.
|
-
- HY-18299B
-
|
(S)-Purvalanol B
(S)-NG 95
|
Others
|
Others
|
|
(S)-Purvalanol B is the S enantiomer of Purvalanol B. Purvalanol B is a cyclin-dependent kinase inhibitor.
|
-
- HY-129357
-
-
- HY-126318
-
|
Demethoxydeacetoxypseudolaric acid B analog
|
Others
|
Cancer
|
|
Demethoxydeacetoxypseudolaric acid B analog (Compound 13b) is semi-synthesized by efficient routines from Pseudolaric acid B. It has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM.
|
-
- HY-N6730
-
-
- HY-N1535
-
|
Ponicidin
Rubescensine B
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
|
-
- HY-N1362
-
|
Salvianolic acid B
Lithospermic acid B
|
Autophagy
|
Cardiovascular Disease
|
|
Salvianolic acid B is an active ingredient of Salvia miltiorrhiza, which has been widely applied in China for the management of various microcirculation-related disorders, such as cardiovascular disease, cerebrovascular disease, and diabetic vascular complication.
|
-
- HY-N4235
-
|
Angelol B
|
Others
|
Inflammation/Immunology
|
|
Angelol B is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model.
|
-
- HY-113380
-
-
- HY-N0639
-
|
Punicalin
|
HBV
|
Infection
Inflammation/Immunology
|
|
Punicalin is a hydrolyzable tannin isolated from Punica granatum L. or the leaves of Terminalia catappa L.. Punicalin is a anti-hepatitis B virus (HBV) agent and has anti-inflammatory activity.
|
-
- HY-N6013
-
|
Aloin(mixture of A&B)
|
MMP
Bacterial
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs).
|
-
- HY-114267
-
|
Cbz-B3A
|
mTOR
|
Others
|
|
Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
|
-
- HY-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-N4184
-
|
Licoflavone B
|
Parasite
|
Infection
|
|
Licoflavone B is a flavonoid isolated from Glycyrrhiza inflata, inhibits S. mansoni ATPase (IC50, 23.78 µM) and ADPase (IC50, 31.50 µM) activity. Anti-schistosomiasis activity.
|
-
- HY-B0017
-
|
Telbivudine
Epavudine; L-Thymidine; NV 02B
|
HBV
|
Infection
|
|
Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.
|
-
- HY-102090
-
-
- HY-12459
-
|
Pyrindamycin B
|
Bacterial
|
Infection
|
|
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both drug-sensitive and resistant cells of P388 leukemia in mice.
|
-
- HY-N3511
-
|
Triptonine B
|
HIV
|
Infection
|
|
Triptonine B, a sesquiterpene pyridine alkaloid that isolated from Tripterygium hypoglaucum and Tripterygium wilfordii, inhibits HIV replication in H9 lymphocytes with an EC50 value of <0.10 μg/mL.
|
-
- HY-P1490
-
-
- HY-N0467
-
-
- HY-18683
-
-
- HY-U00321
-
-
- HY-N0505
-
|
Rosiridin
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
|
-
- HY-A0008
-
-
- HY-101287
-
|
MPT0B392
|
Microtubule/Tubulin
JNK
Apoptosis
Caspase
|
Cancer
|
|
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
|
-
- HY-U00304
-
-
- HY-B1174
-
|
Bekanamycin
Kanamycin B
|
Bacterial
Antibiotic
|
Infection
|
|
Bekanamycin (Kanamycin B) is an aminoglycoside antibiotic produced by Streptomyces kanamyceticus, against an array of Gram-positive and Gram-negative bacterial strain.
|
-
- HY-N2397
-
-
- HY-N5041
-
-
- HY-N2113
-
|
Glaucocalyxin B
|
Autophagy
|
Cancer
|
|
Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 h.
|
-
- HY-117800
-
|
BJE6-106
B106
|
PKC
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
BJE6-106 (B106) is a potent, selective 3 rd generation PKCδ inhibitor with an IC50 of 0.05 μM and targets selectivity over classical PKC isozyme PKCα (IC50=50 μM). BJE6-106 (B106) induces caspase-dependent apoptosis. BJE6-106 (B106) possesses tumor-specific effect.
|
-
- HY-P1337A
-
-
- HY-B2209A
-
|
Hydroxocobalamin monohydrochloride
Vitamin B12a monohydrochloride
|
Others
|
Metabolic Disease
|
|
Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia.
|
-
- HY-N0864
-
|
Macranthoidin B
Macranthoiside I
|
Others
|
Cancer
|
|
Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
|
-
- HY-125702
-
|
Pulsatilloside E
Chinensioside B
|
Others
|
Others
|
|
Pulsatilloside E (Chinensioside B) is a triterpenoidal saponin isolated from the roots of Pulsatilla chinensis (Ranunculaceae).
|
-
- HY-126937
-
|
Ivermectin B1a
|
Parasite
SARS-CoV
|
Infection
|
|
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310). Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-16909
-
|
Leptomycin B
CI 940; LMB
|
CRM1
Fungal
Antibiotic
|
Cancer
Infection
|
|
Leptomycin B (CI 940; LMB) is a potent inhibitor of the nuclear export of proteins. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue. Leptomycin B is a potent antifungal antibiotic blocking the eukaryotic cell cycle.
|
-
- HY-111758
-
-
- HY-16637
-
-
- HY-101690
-
-
- HY-N0248
-
|
Saikosaponin B2
|
HCV
|
Cancer
Infection
|
|
Saikosaponin B2 is an active component from Bupleurum kaoi root, acts as an entry inhibitor against HCV infection. Anti-cancer activity.
|
-
- HY-N6738
-
-
- HY-I0719
-
|
Sofosbuvir impurity B
|
Others
|
Others
|
|
Sofosbuvir impurity B is an impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
|
-
- HY-16928
-
|
Cytochalasin B
Phomin
|
Arp2/3 Complex
|
Cancer
|
|
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
|
-
- HY-70020
-
|
Cevimeline
AF102B
|
mAChR
|
Neurological Disease
|
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
|
-
- HY-W054146
-
|
PTP1B-IN-9
|
Proteasome
|
Cancer
|
|
PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
|
-
- HY-N6723
-
|
Fumonisin B2
|
Acyltransferase
|
Infection
|
|
Fumonisin B2, a mycotoxin produced by Fusarium moniliforme in various grains, is a potent inhibitor of sphingosine N-acyltransferase (ceramide synthase) and disrupts de novo sphingolipid biosynthesis.
|
-
- HY-N1724
-
-
- HY-105118A
-
|
Zaldaride maleate
CGS-9343B; KW 5617
|
nAChR
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Zaldaride maleate (CGS-9343B) is a potent, orally active and selective inhibitor of calmodulin. Zaldaride maleate (CGS-9343B) inhibits CaM (calmodulin)-stimulated cAMP phosphodiesterase activity, with an IC50 of 3.3 nM. Zaldaride maleate (CGS-9343B) prevents estrogen-induced transcription activation by ER, reversibly blocks voltage-activated Na +, Ca 2+ and K + currents in PC12 cells and inhibits nAChR.
|
-
- HY-N0795
-
-
- 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-N0891
-
|
Tubeimoside II
Tubeimoside-B
|
Others
|
Cancer
|
|
Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.
|
-
- HY-N2236
-
|
Dipsanoside B
|
Others
|
Infection
|
|
Dipsanoside B is a novel tetrairidoid glucoside from Dipsacus asper. Dipsacus asper Wall., a perennial plant widespread in China, has been used in traditional Chinese medicine for hundreds of years as a tonic for refreshment, as a fissiparism promoter of the osseous cells, and as an embryo security agent, etc.
|
-
- HY-N6806
-
-
- HY-133016
-
|
M8891
|
Others
|
Cancer
|
|
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-B2226
-
-
- HY-B0315
-
-
- HY-N0784
-
|
Ginkgolide B
BN-52021
|
Endogenous Metabolite
|
Cancer
|
|
Ginkgolide B (BN-52021), an important active terpenoid from Ginkgo biloba leaves, is reported to increase cell viability and decrease cell apoptosis.
|
-
- HY-N6935
-
|
Sennidin B
|
HCV
Akt
GLUT
|
Infection
Metabolic Disease
|
|
Sennidin B, a stereoisomer isolated from the leaves of Cassia angustifolia, has lower activity than Sennidin A. Sennidin A inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation .
|
-
- HY-12546
-
|
Brevetoxin B
Brevetoxin-2; PbTx-2
|
Sodium Channel
|
|
|
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning.
|
-
- HY-P0111
-
|
Z-WEHD-FMK
|
Caspase
Cathepsin
|
Cancer
|
|
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
|
-
- HY-Y0073
-
|
4-Hydroxyacetophenone
P-hydroxyacetophenone
|
HBV
|
Infection
Inflammation/Immunology
|
|
4-Hydroxyacetophenone (P-hydroxyacetophenone) is a key hepatoprotective and choleretic compound in Artemisia capillaris and A. morrisonensis, also has an anti-hepatitis B virus effect and anti-inflammatory effect.
|
-
- HY-131152
-
-
- HY-N2301
-
-
- HY-P1791
-
|
Lactoferrin (17-41)
Lactoferricin B; Lfcin B
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
|
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities.
|
-
- HY-P1742
-
-
- HY-B1816
-
-
- HY-N6938
-
-
- HY-P1019A
-
-
- HY-N4328
-
-
- HY-114336
-
|
Enocyanin
|
Phosphatase
|
Inflammation/Immunology
|
|
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity.
|
-
- HY-131005
-
-
- HY-131107
-
-
- HY-13989
-
-
- HY-100660A
-
|
Cetirizine Impurity B dihydrochloride
|
Others
|
Others
|
|
Cetirizine Impurity B dihydrochloride is an impurity of Cetirizine dihydrochloride. Cetirizine, a second-generation antihistamine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1] [2] [3] .
|
-
- HY-15730
-
|
Poziotinib
HM781-36B; NOV120101
|
EGFR
Apoptosis
|
Cancer
|
|
Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity.
|
-
- HY-A0100
-
-
- HY-N0682
-
-
- HY-127105A
-
-
- HY-127105
-
-
- 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-18299
-
|
Purvalanol B
NG 95
|
CDK
|
Cancer
|
|
Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.
|
-
- HY-N0205
-
|
Pulchinenoside C
Anemoside B4
|
Others
|
Cancer
|
|
Pulchinenoside C (Anemoside B4) is Pulsatilla koreana Nakai that have many numerous biological effects in vitro, including enhancing hypoglycemic, anti-tumor, neuroprotective and anti-angiogenic activity.
|
-
- HY-113315
-
-
- HY-N0117
-
|
Indirubin
Couroupitine B; Indigo red; Indigopurpurin
|
Apoptosis
|
Cancer
|
|
Indirubin (Couroupitine B) is a purple 3,2- bisindole and a stable isomer of indigo isolated from Indigo naturalis (Apiaceae); anti-inflammatory and anticancer activities.
|
-
- HY-10264A
-
|
Edoxaban tosylate
DU-176b
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban tosylate (DU-176b) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- HY-18711A
-
|
SCR-1481B1
c-Met inhibitor 2
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
SCR-1481B1 (c-Met inhibitor 2) is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.
|
-
- HY-P1791B
-
|
Lactoferrin (17-41) (acetate)
Lactoferricin B acetate; Lfcin B acetate
|
Bacterial
Fungal
Apoptosis
|
Cancer
Infection
|
|
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities.
|
-
- HY-131003
-
|
Taletrectinib
DS-6051b; AB-106
|
ROS
|
Cancer
|
|
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
|
-
- HY-19487A
-
|
Ribocil B
Ribocil S enantiomer; ent-Ribocil A
|
Bacterial
|
Infection
|
|
Ribocil-B is the active S-isomer of ribocil which can inhibit flavin mononucleotide (FMN) with a KD of 6.6 nM.
|
-
- HY-P1495
-
-
- HY-P2323
-
-
- HY-A0279A
-
|
Pristinamycin IA
Mikamycin B; Mikamycin IA
|
Bacterial
|
Others
|
|
Pristinamycin IA (Mikamycin B;Mikamycin IA), a biologically active decapeptide isolated from the skin of the Australian frog Hyla caerulea, is a potent cholecystokinetic agent, and acts as a cholecystokinin receptor agonist.
|
-
- 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-121879
-
-
- HY-17029
-
-
- HY-P0117
-
|
Tat-NR2B9c
Tat-NR2Bct; NA-1
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
|
-
- HY-14452
-
|
Fatostatin
125B11
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin (125B11), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin decreases the transcription of lipogenic genes in cells. Fatostatin possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-B1915
-
|
Micronomicin
Gentamicin C2b; Antibiotic XK-62-2; Sagamicin
|
Bacterial
|
Infection
|
|
Micronomicin (Gentamicin C2b) is an aminoglycoside antibiotic, with antibacterial and bactericidal activities.
|
-
- HY-P1340
-
-
- HY-107608
-
-
- HY-P0117A
-
|
Tat-NR2B9c TFA
Tat-NR2Bct TFA; NA-1 TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2B9c TFA (Tat-NR2Bct TFA) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c TFA disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy.
|
-
- HY-116999
-
|
IR415
|
HBV
|
Infection
|
|
IR415 is a potent anti-HBV agent and inhibits HBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease. HBx: hepatitis B virus X protein.
|
-
- HY-10264B
-
|
Edoxaban tosylate monohydrate
DU-176b monohydrate
|
Factor Xa
Thrombin
|
Cardiovascular Disease
|
|
Edoxaban tosylate monohydrate (DU-176b monohydrate) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban tosylate monohydrate is an anticoagulant agent and can be used for stroke prevention. Edoxaban tosylate monohydrate is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban tosylate monohydrate has antithrombotic properties and has potential for thromboembolic diseases treatment.
|
-
- HY-111849
-
-
- HY-12838
-
|
Mirk-IN-1
Dyrk1B/A-IN-1
|
DYRK
|
Cancer
|
|
Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
|
-
- HY-P1340A
-
-
- HY-13779
-
|
J-147
|
Monoamine Oxidase
Dopamine Transporter
|
Neurological Disease
|
|
J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD).
|
-
- HY-14405A
-
|
Casopitant mesylate
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
|
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of substance P. Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).
|
-
- HY-19373
-
-
- 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-70020B
-
|
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- HY-121071
-
|
Ascamycin
|
Bacterial
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Ascamycin is a 5'-O-sulfonamide ribonucleoside antibiotic produced by Streptomyces sp. JCM9888. Ascamycin has a selective antibacterial activity against Xanthomonas species with MIC values of 0.4 μg/mL, 12.5 μg/mL and 12.5 μg/mL for Xanthomonas citri, Xanthomonas oryzae and Mycobacterium phlei, respectively.
|
-
- HY-N0044
-
-
- HY-14452A
-
|
Fatostatin hydrobromide
125B11 hydrobromide
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
Fatostatin hydrobromide (125B11 hydrobromide), a specific inhibitor of SREBP activation, impairs the activation of SREBP-1 and SREBP-2. Fatostatin hydrobromide binds to SCAP (SREBP cleavage-activating protein), and inhibits the ER-Golgi translocation of SREBPs. Fatostatin hydrobromide decreases the transcription of lipogenic genes in cells. Fatostatin hydrobromide possesses antitumor properties, and lowers hyperglycemia in ob/ob mice.
|
-
- HY-109058
-
|
Firibastat
QGC001; RB150
|
Aminopeptidase
|
Cardiovascular Disease
|
|
Firibastat (QGC001), an orally active brain penetrating prodrug of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
|
-
- 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-N0681
-
-
- 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-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-131003A
-
|
Taletrectinib free base
DS-6051b free base; AB-106 free base
|
ROS
|
Cancer
|
|
Taletrectinib (DS-6051b) free base is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants.
|
-
- HY-13292
-
|
Impurity B of Calcitriol
1β,25-Dihydroxyvitamin-D3; 1-Epicalcitriol
|
VD/VDR
|
Cancer
|
|
Impurity B of Calcitriol, Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ) is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- 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-N6847
-
-
- HY-N0604
-
-
- 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-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-N2142
-
-
- HY-124600
-
|
NVR 3-778
|
HBV
|
Infection
|
|
NVR 3-778 is a first-in-Class and oral bioavailable HBV CAM (capsid assembly modulator) belonging to the SBA (sulfamoylbenzamide) class, with anti-HBV activity.
|
-
- 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-18728
-
-
- HY-100499
-
|
Tyrphostin AG 528
Tyrphostin B66; AG 528
|
EGFR
|
Cancer
|
|
Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively.
Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2. Tyrphostin AG 528 is also an anticancer agent.
|
-
- HY-108307
-
|
Micronomicin sulfate
Gentamicin C2b sulfate; Antibiotic XK-62-2 sulfate; Sagamicin sulfate
|
Antibiotic
Bacterial
|
Infection
|
|
Micronomicin sulfate (Gentamicin C2b sulfate) is an aminoglycoside antibiotic isolated from Micromonospora. Micronomicin sulfate is a broad-spectrum antibiotic close to the gentamicin-type antibiotics, exhibits a high activity against Pseudomonas, Proteus, Klebsiella pneumoniae, Serratia, etc (MIC=0.001-8.3 μg/ml).
|
-
- HY-B1916
-
-
- HY-15583
-
-
- 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-121282
-
|
Mepazine
Pecazine
|
MALT1
Apoptosis
|
Cancer
|
|
Mepazine (Pecazine) is a potent and selective MALT1 inhibitor. Mepazine inhibits GSTMALT1 full length and GSTMALT1 325-760 with IC50s of 0.83 and 0.42 μM, respectively. Mepazine affects viability of ABC-DLBCL cells by enhancing apoptosis.
|
-
- HY-135827A
-
-
- HY-101621
-
-
- HY-P0298
-
-
- HY-P0298A
-
-
- HY-N6927
-
|
Isoforskolin
Coleonol B
|
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.
|
-
- HY-N0824
-
|
Syringin
Eleutheroside B
|
Autophagy
|
Cardiovascular Disease
|
|
Syringin is a main bioactive phenolic glycoside in Acanthopanax senticosus, with anti-osteoporosis activity. Syringin prevents cardiac hypertrophy induced by pressure overload through the attenuation of autophagy.
|
-
- HY-N0231
-
-
- HY-N0478
-
|
Neoline
Bullatine B
|
Others
|
Neurological Disease
|
|
Neoline, the active ingredient of processed aconite root (PA), alleviated oxaliplatin-induced peripheral neuropathy in mice. Neoline can be used as a marker compound to determine the quality of the PA products for the treatment of neuropathic pain.
|
-
- HY-103395
-
-
- HY-12307
-
|
(-)-Indolactam V
Indolactam V
|
PKC
|
Cancer
|
|
(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
|
-
- HY-114017
-
-
- HY-U00015
-
-
- HY-12312
-
-
- HY-15039
-
|
SSR240612
|
Bradykinin Receptor
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
SSR240612 is a potent, and orally active specific non-peptide bradykinin B1 receptor antagonist, with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.
|
-
- HY-109655
-
-
- HY-107018
-
|
AR-A 2
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- HY-16677A
-
-
- HY-N4185
-
-
- HY-N6651
-
|
Isocryptotanshinone
|
STAT
Phosphatase
|
Cancer
|
|
Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
|
-
- HY-113379
-
-
- HY-N0623
-
-
- HY-N0913A
-
|
Isomaltotriose
|
Others
|
Others
|
|
Isomaltotriose is a sugar from enzymic hydrolyzates of the dextran from Leuconostoc mesenteroides NRRL B-512.
|
-
- HY-14775
-
|
Nesbuvir
HCV-796
|
HCV
|
Infection
|
|
Nesbuvir is a nonnucleoside inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase.
|
-
- 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-101105A
-
-
- HY-10118
-
|
Filibuvir
|
HCV
|
Infection
|
|
Filibuvir is a potent, selective non-nucleoside inhibitor (NNI) of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase, and it binds noncovalently in the “Thumb 2” pocket of NS5B. In vitro, filibuvir is equipotent against genotype 1a and 1b replicons, with an EC50 of 59 nM.
|
-
- HY-101698
-
|
Alniditan
Alnitidan
|
5-HT Receptor
|
Neurological Disease
|
|
Alniditan is a potent 5-HT1B/1D receptors agonist, with IC50 of 1.7 and 1.3 nM in HEK 293 cells, and pKi value of 8.96 and 9.40 for 5-HT1B/1D receptors, respectively.
|
-
- HY-N6700
-
|
Aflatoxin M2
|
Others
|
Cancer
|
|
Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- HY-N6699
-
|
Aflatoxin M1
|
Bacterial
|
Cancer
Infection
|
|
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- 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-118651
-
|
Griseoluteic acid
|
Bacterial
|
Infection
|
|
Griseoluteic acid, a phenazine antibiotic, is originally isolated from S. griseoluteus. Griseoluteic acid is a breakdown product of griseolutein A and B.
|
-
- HY-P2328
-
-
- HY-B0450
-
-
- HY-N0253
-
|
Hederacoside C
Kalopanaxsaponin B
|
Bacterial
|
Infection
|
|
Hederacoside C is a principal active ingredient of Hedera helix leaf that can treat respiratory disorders, because of its expectorant, bronchodilator, antibacterial, and bronchospasmolytic effects.
|
-
- HY-100301
-
-
- HY-100014
-
|
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-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-19900
-
-
- HY-B0383A
-
-
- HY-12783
-
|
SCH 50911 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911 hydrochloride, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 hydrochloride antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
|
-
- 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-B0383
-
-
- HY-P2307
-
|
Tat-NR2Baa
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-P2307A
-
|
Tat-NR2Baa TFA
|
iGluR
NO Synthase
|
Neurological Disease
|
|
Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
|
-
- HY-12783A
-
|
SCH 50911
|
GABA Receptor
|
Neurological Disease
|
|
SCH 50911, (+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid, a selective, orally-active and competitive γ-Aminobutyric acid B GABA(B) receptor antagonist, binds to GABA(B) receptor with IC50 of 1.1 μM. SCH 50911 antagonizes GABA(B) autoreceptors, increasing the electrically-stimulated 3H overflow with an IC50 of 3 μM.
|
-
- HY-102087
-
|
JPM-OEt
|
Cathepsin
|
Cancer
|
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity.
|
-
- HY-12841
-
|
KHK-IN-1
|
Others
|
Metabolic Disease
|
|
KHK-IN-1 is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM; interacts with Asp-27B in the ATP-binding region of KHK.
|
-
- HY-N2111
-
-
- HY-19477
-
-
- HY-135865
-
|
KRAS inhibitor-7
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-12841A
-
|
KHK-IN-1 hydrochloride
|
Others
|
Others
|
|
KHK-IN-1 hydrochloride is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM, interacts with Asp-27B in the ATP-binding region of KHK.
|
-
- HY-112734
-
-
- HY-13998
-
|
Dasabuvir
ABT-333
|
HCV
|
Infection
|
|
Dasabuvir (ABT-333) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC50 between 2.2 and 10.7 nM.
|
-
- HY-N6698
-
|
Aflatoxin G2
|
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- HY-N3513
-
|
Mulberrin
Kuwanon C
|
Others
|
Cardiovascular Disease
|
|
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
|
-
- HY-19779
-
|
JTT 551
|
Phosphatase
|
Metabolic Disease
|
|
JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
|
-
- HY-133739
-
|
NBD-125
|
RAR/RXR
|
Cancer
|
|
NBD-125 (B-12), a berberine analogue, is an RXRα activator, with an IC50 of 31.10 μM in KM12C cell.
|
-
- HY-101385
-
-
- HY-125169
-
|
NSC 185058
|
Cathepsin
Autophagy
|
Cancer
|
|
NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC185058 markedly attenuates autophagic activity.
|
-
- HY-P1799
-
|
[pTyr5] EGFR (988-993)
|
Phosphatase
|
Others
|
|
[pTyr5] EGFR (988-993) is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).
|
-
- HY-B2082
-
-
- HY-101284
-
|
DMU2105
|
Cytochrome P450
|
Cancer
|
|
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
|
-
- HY-13527
-
-
- HY-101285
-
|
DMU2139
|
Cytochrome P450
|
Cancer
|
|
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
|
-
- HY-B2006
-
|
Fenvalerate
|
Phosphatase
Bacterial
|
Infection
|
|
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
|
-
- HY-10121
-
|
Asenapine
Org 5222
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
|
-
- HY-18596
-
|
SB-215505
|
5-HT Receptor
|
Neurological Disease
|
|
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
|
-
- HY-103154
-
|
SB228357
|
5-HT Receptor
|
Neurological Disease
|
|
SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.
|
-
- HY-B1129A
-
|
Dibekacin sulfate
|
Bacterial
|
Infection
|
|
Dibekacin sulfate is an aminoglycoside antibiotic derived from Kanamycin B (HY-B1174), has a broad-spectrum antibacterial activities. Dibekacin sulfate closely resembles Tobramycin (HY-B0441) structurally and is against some strains of Ps. Aeruginosa resistant to gentamicin.
|
-
- HY-P1799A
-
|
[pTyr5] EGFR (988-993) (TFA)
|
Phosphatase
|
Others
|
|
[pTyr5] EGFR (988-993) TFA is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) TFA is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).
|
-
- HY-17408
-
-
- HY-N0183
-
|
Formononetin
Biochanin B; Flavosil; Formononetol
|
FGFR
Apoptosis
|
Cancer
|
|
Formononetin (Formononetol; Flavosil) is a bioactive component extracted from the red clover; inhibits the proliferation of DU-145/PC-3 cells in a dose-dependent manner.
|
-
- HY-N0374
-
-
- HY-13859
-
-
- HY-106157
-
-
- HY-10966
-
|
SB-590885
|
Raf
|
Cancer
|
|
SB-590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, and has 11-fold greater selectivity for B-Raf over c-Raf, without inhibition to other human kinases.
|
-
- HY-N6650
-
-
- HY-101217
-
|
BI 689648
|
Cytochrome P450
|
Endocrinology
|
|
BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
|
-
- HY-15043
-
-
- HY-A0010
-
-
- HY-N0417
-
|
Cucurbitacin E
α-Elaterin; α-Elaterine
|
CDK
Autophagy
|
Cancer
|
|
Cucurbitacin E is a natural compound which from the climbing stem of Cucumic melo L. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
|
-
- HY-11004
-
|
AZ 628
|
Raf
Apoptosis
|
Cancer
|
|
AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
|
-
- HY-136071
-
-
- HY-136070
-
-
- HY-136072
-
|
QPX7728-OH disodium
|
Bacterial
|
Infection
|
|
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
|
-
- HY-N4096
-
|
Tsugaric acid A
|
Others
|
Inflammation/Immunology
|
|
Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
|
-
- HY-109080
-
|
Belvarafenib
HM95573; GDC-5573; RG6185
|
Raf
|
Cancer
|
|
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively.
|
-
- HY-N4289
-
|
3-Epiursolic Acid
|
Cathepsin
|
Cancer
|
|
3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B.
|
-
- HY-19383
-
|
Ertiprotafib
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-12694
-
-
- HY-136568
-
-
- HY-15648
-
-
- HY-13993
-
|
Ro 25-6981
|
iGluR
|
Neurological Disease
|
|
Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively.
|
-
- HY-15648D
-
-
- HY-19340
-
-
- HY-101036
-
|
Choline bitartrate
|
mAChR
|
Neurological Disease
|
|
Choline (bitartrate) is an essential nutrient, often associated with the B vitamins but not yet officially defined as a B vitamin. Choline (bitartrate) plays an important role in synthesis of the neurotransmitter acetylcholine.
|
-
- HY-106441A
-
|
Rislenemdaz
MK-0657; CERC-301
|
iGluR
|
Neurological Disease
|
|
Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
|
-
- HY-B2209B
-
|
Hydroxocobalamin acetate
|
Others
|
Metabolic Disease
|
|
Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia.
|
-
- HY-N2451
-
-
- HY-B2054
-
|
Tebufenozide
|
Apoptosis
|
Others
|
|
Tebufenozide is a nonsteroidal ecdysone agonist used to control pest. Tebufenozide has cytotoxic and induces apoptosis in HeLa and insect Tn5B1-4 cells.
|
-
- HY-10126
-
|
Barasertib-HQPA
AZD2811; INH-34; AZD1152-HQPA
|
Aurora Kinase
|
Cancer
|
|
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay, and shows 3700-fold selectivity for Aurora B over Aurora A.
|
-
- HY-10544
-
|
Tegobuvir
GS 333126; GS-9190
|
HCV
|
Infection
|
|
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
|
-
- HY-103350
-
-
- HY-14605
-
-
- HY-103129
-
|
SB-200646A
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
|
-
- HY-103129A
-
|
SB-200646
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.
|
-
- HY-12219A
-
|
MSI-1436 lactate
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-N1549
-
-
- HY-135659
-
|
BSH-IN-1
|
Bacterial
|
Infection
|
|
BSH-IN-1 is a potent and covalent inhibitor of gut bacterial recombinant bile salt hydrolases (BSHs) with IC50s of 108 nM and 427 nM for B. longum BSH (Gram positive) and B. theta BSH (Gram negative), respectively.
|
-
- HY-12219
-
|
MSI-1436
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-111767
-
|
BAY-545
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
|
-
- HY-109080A
-
|
Belvarafenib TFA
HM95573 TFA; GDC-5573 TFA; RG6185 TFA
|
Raf
|
Cancer
|
|
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv 600E and C-RAF respectively.
|
-
- HY-108539
-
|
CE3F4
|
Others
|
Metabolic Disease
|
|
CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC50s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.
|
-
- HY-126057S
-
|
(R)-Praziquantel D11
|
Parasite
5-HT Receptor
|
Infection
|
|
(R)-Praziquantel D11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.
|
-
- HY-11100
-
|
Asenapine maleate
Org 5222 maleate
|
5-HT Receptor
|
Neurological Disease
|
|
Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
|
-
- HY-17016
-
-
- HY-112543
-
-
- HY-13910A
-
-
- HY-12787
-
-
- HY-B0456
-
-
- HY-15463
-
|
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-B2223
-
-
- HY-B0988
-
-
- HY-12042
-
|
Pimasertib
AS703026; MSC1936369B
|
MEK
|
Cancer
|
|
Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
|
-
- HY-B0152
-
-
- HY-14462
-
-
- HY-N0432
-
|
Astragaloside I
Astrasieversianin IV; Cyclosieversioside B
|
Others
|
Others
|
|
Astragaloside I is a natural product isolated from Astragalus.
|
-
- 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-15419
-
|
RS-127445 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5 and 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
|
-
- HY-16687A
-
-
- HY-136299
-
|
Sepimostat
FUT-187 free base
|
iGluR
|
Neurological Disease
|
|
Sepimostat exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM.
|
-
- HY-126114
-
|
Lupeol acetate
|
Others
|
Inflammation/Immunology
|
|
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
|
-
- HY-12429
-
|
Beclabuvir
BMS-791325
|
HCV
|
Infection
|
|
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
|
-
- HY-15419A
-
|
RS-127445
|
5-HT Receptor
|
Neurological Disease
|
|
RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5 and 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
|
-
- HY-51424
-
|
PLX-4720
|
Raf
|
Cancer
|
|
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
|
-
- HY-N5132
-
|
(-)-Fenchone
|
Others
|
Others
|
|
(-)-Fenchone, a bicyclic monoterpene, is widely distributed in plants and found in essential oils from Thuja occidentalis. (-)-Fenchone is oxidized to 6-endo-hydroxyfenchone, 6-exo-hydroxyfenchone and 10-hydroxyfenchone derivatives by CYP2A6 and CYP2B6 in human liver microsomes with CYP2A6 playing a more important role than CYP2B6.
|
-
- HY-16687
-
-
- HY-125021
-
-
- HY-14886
-
-
- HY-12518
-
|
OF-1
|
Epigenetic Reader Domain
|
Cancer
|
|
OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor with Kd values of 100 nM/500 nM for BRPF1B/BRPF2; 39-fold selectivity over BRD4.
|
-
- HY-111430
-
-
- HY-13465
-
-
- HY-N2178
-
-
- HY-100029
-
|
Bay 41-4109
|
HBV
|
Infection
|
|
BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
|
-
- HY-50864
-
|
GDC-0879
|
Raf
|
Cancer
|
|
GDC-0879 is a potent and selective B-Raf inhibitor with an IC50 of 0.13 nM.
|
-
- HY-13910B
-
-
- HY-14390
-
-
- HY-100119
-
-
- HY-123960
-
|
Raphin1
|
Phosphatase
|
Neurological Disease
|
|
Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
|
-
- HY-123960A
-
|
Raphin1 acetate
|
Phosphatase
|
Neurological Disease
|
|
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease.
|
-
- HY-12294
-
|
PEAQX
NVP-AAM077
|
iGluR
|
Neurological Disease
|
|
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
|
-
- HY-130517
-
|
Cdc7-IN-5
|
CDK
|
Cancer
|
|
Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-15745A
-
|
PSI-7409 tetrasodium
|
HCV
|
Infection
|
|
PSI-7409 tetrasodium is an active 5'-triphosphate metabolite of sofosbuvir (PSI-7977), inhibiting HCV NS5B polymerases, with IC50s of 1.6, 2.8, 0.7 and 2.6 μM for GT 1b_Con1, GT 2a_JFH1, GT 3a, and GT 4a NS5B polymerases, respectively.
|
-
- HY-130617
-
|
Pomalidomide-amido-C1-Br
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Pomalidomide-amido-C1-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-amido-C1-Br can be used to design a B-Raf PROTAC degrader PROTAC B-Raf degrader 1 (HY-111758). PROTAC B-Raf degrader 1 has anti-cancer activity.
|
-
- HY-126741
-
|
Azadirachtin
|
Apoptosis
|
Others
|
|
Azadirachtin, one of the most promising botanical insecticides, is widely used for pest control. Azadirachtin induces apoptosis in insect cell lines, including Sf9, SL-1 and BTI-Tn-5B1-4.
|
-
- HY-14648
-
-
- HY-100279
-
|
RMI 10874
|
Others
|
Infection
Cancer
|
|
RMI 10874 is a tilorone analogue. Tilorone is a small-molecule, orally bioavailable antiviral agent. RMI 10874 completely abolishes lung colonization of an H-2 negative (GR9.B9) MCA-induced fibrosarcoma clone.
|
-
- HY-10558
-
-
- HY-U00263
-
-
- HY-107430
-
|
Oxythiamine
Hydroxythiamin
|
Others
|
Cancer
|
|
Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
|
-
- HY-112564
-
-
- HY-113493
-
-
- HY-13321
-
|
Anguizole
|
HCV
|
Infection
|
|
Anguizole is a small molecule inhibitor of HCV replication and alters NS4B's subcellular distribution.
|
-
- HY-112684
-
-
- HY-17425
-
-
- HY-13782
-
-
- HY-17425A
-
-
- HY-15951
-
|
ML167
CID44968231; NCGC00188654
|
CDK
|
Cancer
|
|
ML167 is a highly selective Cdc2-like kinase 4 (Clk4) inhibitor with IC50 of 136 nM, >10-fold selectivity for closely related kinases Clk1, Clk2, Clk3 and Dyrk1A/1B.
|
-
- HY-105185
-
|
Fidarestat
SNK 860
|
Aldose Reductase
|
Metabolic Disease
|
|
Fidarestat (SNK 860) is an inhibitor of aldose reductase, with IC50s of 26 nM, 33 μM, and 1.8 μM for aldose reductase, AKR1B10 and V301L AKR1B10, respectively; Fidarestat (SNK 860) has the potential to treat diabetic disease.
|
-
- HY-N6795
-
|
Leptomycin A
|
CRM1
HIV
|
Infection
|
|
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
|
-
- HY-15296
-
-
- HY-112711
-
|
LV-320
|
Autophagy
Cathepsin
|
Cancer
|
|
LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
|
-
- HY-103186
-
-
- HY-N7136
-
|
α-Terpinyl acetate
|
Cytochrome P450
|
Metabolic Disease
|
|
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
|
-
- HY-13409A
-
-
- HY-13409
-
-
- HY-12294A
-
|
PEAQX tetrasodium hydrate
NVP-AAM077 tetrasodium hydrate
|
iGluR
Apoptosis
|
Neurological Disease
|
|
PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).
|
-
- HY-19447A
-
|
Besifovir Dipivoxil maleate
LB80380 maleate
|
HBV
|
Infection
|
|
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral prodrug of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies[2]
|
-
- HY-116761
-
|
GSK467
|
Histone Demethylase
|
Cancer
|
|
GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
|
-
- HY-N0859
-
|
Schisanhenol
Schizanhenol; Gomisin-K3
|
Others
|
Cancer
|
|
Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
|
-
- HY-17374
-
-
- HY-10483
-
-
- HY-16465
-
-
- HY-B2229
-
-
- HY-B0531
-
-
- HY-19193
-
-
- HY-112089
-
|
LXH254
|
Raf
|
Cancer
|
|
LXH254 is a potent B/C RAF inhibitor extracted from patent WO2018051306A1, Compound A.
|
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-10179
-
-
- HY-U00252
-
-
- HY-129371
-
|
SPDV
|
ADC Linker
|
Cancer
|
|
SPDV is a cleavable ADC linker used for diagnosis and treatment of cancer or B cell proliferative diseas.
|
-
- 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-10128
-
-
- HY-129374
-
|
SPDH
|
ADC Linker
|
Cancer
|
|
SPDH is a cleavable ADC linker used for diagnosis and treatment of cancer or B cell proliferative diseas.
|
-
- HY-10482
-
-
- 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-109585
-
|
IRAK4-IN-7
|
IRAK
|
Cancer
Inflammation/Immunology
|
|
IRAK4-IN-7 is a selective, potent and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor, extracted from patent WO2015104688 (example 1). IRAK4-IN-7 has the potential for cancer and inflammatory diseases treatment.
|
-
- HY-15414
-
-
- HY-N0848
-
|
Epibrassinolide
24-Epibrassinolide; B1105; BP55
|
Apoptosis
|
Cancer
|
|
Epibrassinolide (24-Epibrassinolide) is a ubiquitously occurring plant growth hormone which shows great potential to alleviate heavy metals and pesticide stress in plants. Epibrassinolide is a potential apoptotic inducer in various cancer cells without affecting the non-tumor cell growth.
|
-
- HY-N0057
-
-
- HY-N0157
-
-
- HY-13442
-
|
Eribulin
B1939; E7389; ER-086526
|
Microtubule/Tubulin
|
Cancer
|
|
Eribulin (E7389) is a microtubule targeting agent that is used in the treatment of metastatic breast cancer. Eribulin (E7389) inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
|
-
- 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-15811
-
|
XMD8-87
ACK1-B19
|
Tyrosinase
|
Cancer
|
|
XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.
|
-
- HY-N0206
-
|
Ardisiacrispin A
Deglucocyclamin; LTS-4; Saxifragifolin B
|
Others
|
Cancer
|
|
Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities.
|
-
- HY-N0863
-
|
Methyl protodioscin
NSC-698790; Smilax saponin B
|
Apoptosis
|
Cancer
|
|
Methyl protodioscin(NSC-698790) is a furostanol bisglycoside with antitumor properties; shows to reduce proliferation, cause cell cycle arrest.
|
-
- HY-12451
-
-
- HY-109035
-
|
Inarigivir soproxil
SB9200
|
HCV
|
Infection
|
|
Inarigivir soproxil is an agonist of innate immunity and shows potent antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.
|
-
- HY-100034
-
|
NSC 663284
DA-3003-1
|
Phosphatase
Histone Methyltransferase
|
Cancer
|
|
NSC 663284 is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM).
|
-
- HY-100975
-
-
- HY-12639
-
|
Bephenium
|
Parasite
|
Infection
|
|
Bephenium is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis; B-type AChR activator.
|
-
- HY-100673
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-B1184
-
-
- HY-13782A
-
-
- HY-B1744
-
-
- HY-13210
-
-
- HY-111506
-
-
- HY-N0918
-
|
Desmethoxyyangonin
Demethoxyyangonin; 5,6-Dehydrokavain
|
Monoamine Oxidase
|
Others
|
|
Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.
|
-
- HY-15958
-
|
VBY-825
|
Cathepsin
|
Cancer
|
|
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.
|
-
- HY-B0255
-
-
- HY-12049
-
|
CCT129202
|
Aurora Kinase
|
Cancer
|
|
CCT129202 is an aurora kinase inhibitor with IC50s of 42, 198, and 227 nM for aurora A, B and C, respectively.
|
-
- HY-107836
-
|
Methiothepin mesylate
Metitepine mesylate; Ro 8-6837 mesylate
|
5-HT Receptor
|
Neurological Disease
|
|
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-15648H
-
|
GSK-J5 hydrochloride
|
Histone Demethylase
|
Cancer
|
|
GSK-J5 hydrochloride is a cell-permeable ester derivative of GSK J2 (HY-15648A), inactive. GSK-J5 hydrochloride is also an isomer of GSK-J4 (HY-15648B) and often used as a negative group.
|
-
- HY-10524
-
|
GSK1904529A
|
IGF-1R
|
Cancer
Endocrinology
|
|
GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
|
-
- HY-12291
-
|
HG6-64-1
HMSL 10017-101-1
|
Raf
|
Cancer
|
|
HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
|
-
- HY-P1565
-
|
Transdermal Peptide
TD 1 (peptide)
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
|
Transdermal Peptide (TD 1 peptide) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide can enhance the transdermal delivery of many macromolecules.
|
-
- HY-126298
-
|
RAF mutant-IN-1
|
Raf
|
Cancer
|
|
RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively.
|
-
- HY-N0646
-
|
Silydianin
|
Phosphatase
|
Cancer
|
|
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.
|
-
- HY-12962
-
|
NMDA-IN-1
|
iGluR
|
Neurological Disease
|
|
NMDA-IN-1 is a potent and NR2B-selective NMDA antagonist with Ki of 0.85 nM; NR2B Ca2+ influx IC50 is 9.7 nM; no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor.
|
-
- HY-N7038
-
|
Phytohemagglutinin
PHA-M
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Phytohemagglutinin (PHA-M), a lectin extract from the red kidney bean and a standard T cell mitogen, as an inhibitor of both T- and B-cell tumors. Phytohemagglutinin can inhibit incorporation of 3H-thymidine and mediate apoptosis of B- and T-cell tumor lines. Anti-tumor activity.
|
-
- HY-123872
-
|
MSC1094308
|
p97
|
Others
|
|
MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
|
-
- HY-15658
-
|
GSK2801
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK2801 is a potent, selective, orally active and cell active acetyl-lysine competitive BAZ2A and BAZ2B bromodomains inhibitor with Kd values of 136 nM and 257 nM, respectively. GSK2801 shows >50-fold selectivity for BAZ2A/B over BRD4.
|
-
- HY-12639A
-
-
- HY-12201
-
|
TAK-901
|
Aurora Kinase
|
Cancer
|
|
TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
|
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-13993A
-
-
- HY-N7256
-
|
Dihydrocephalomannine
|
Others
|
Cancer
|
|
Dihydrocephalomannine (compound 1b), an analogue of Paclitaxel, shows reduced cytotoxicity and tubulin binding compared to Paclitaxel.
|
-
- HY-W002314
-
-
- HY-10178
-
-
- HY-13910
-
-
- HY-121515
-
|
DPM-1001
|
Phosphatase
|
Metabolic Disease
|
|
DPM-1001 is a potent, specific, orally bioavailable and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM, an an analog of the specific PTP1B inhibitor trodusquemine (MSI-1436; IC50=600 nM). DPM-1001 has anti-diabetic property.
|
-
- HY-117639
-
|
AUT1
|
Potassium Channel
|
Cancer
|
|
AUT1 is a Kv3 potassium channel modulator, with pEC50s of 5.33 and 5.31 for human recombinant Kv3.1b and Kv3.2a, respectively, exhibits 10-fold lower potency at human recombinant Kv3.3 channel (pEC50, 4.5).
|
-
- HY-10847
-
-
- HY-15414A
-
-
- HY-16567
-
|
Asenapine hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
|
-
- HY-103355
-
|
YM022
|
CCR
|
Metabolic Disease
|
|
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
|
-
- HY-14151
-
|
Prucalopride
|
5-HT Receptor
|
Neurological Disease
|
|
Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.
|
-
- HY-112151A
-
|
EG01377 dihydrochloride
|
Complement System
|
Cancer
|
|
EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.
|
-
- HY-P1565A
-
|
Transdermal Peptide TFA
TD 1 (peptide) (TFA)
|
Na+/K+ ATPase
|
Others
|
|
Transdermal Peptide TFA (TD 1 peptide TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide TFA can enhance the transdermal delivery of many macromolecules.
|
-
- HY-110279
-
|
Ogerin
|
Others
|
Neurological Disease
|
|
Ogerin is a selective GPR68 positive allosteric modulator, with a pEC50 of 6.83. Ogerin shows inverse agonist and antagonist activity (Ki, 220 nM) at A2A receptoor and weak antagonist activity (Ki, 736 nM) at 5-HT2B receptor. Ogerin blocks recall in fear conditioning in mice.
|
-
- HY-112151
-
|
EG01377
|
Complement System
|
Cancer
|
|
EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects.
|
-
- HY-10469
-
-
- 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-100637
-
|
Hydroxybupropion
|
Adrenergic Receptor
nAChR
|
Neurological Disease
|
|
Hydroxybupropion is the major active metabolite of Bupropion. Hydroxybupropion is metabolized by CYP2B6.Bupropion is an atypical antidepressant and smoking-cessation agent. Hydroxybupropion inhibits norepinephrine uptake with an IC50 value of 1.7 μM. Hydroxybupropion is also a nACh receptor antagonis tis more potent than Bupropion .
|
-
- HY-136586
-
-
- HY-135676
-
-
- HY-12808
-
-
- HY-112623
-
-
- HY-13643
-
-
- HY-14605A
-
-
- HY-135675
-
-
- HY-113076
-
-
- HY-N2505
-
-
- HY-101634
-
|
ABT-072
|
HCV
|
Infection
|
|
ABT-072 is a nonnucleoside NS5B polymerase inhibitor and a candidate drug evaluated for treatment of hepatitis C virus.
|
-
- HY-128452
-
-
- HY-16465A
-
-
- HY-13253
-
|
AMG 900
|
Aurora Kinase
|
Cancer
|
|
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
|
-
- HY-108543
-
|
NSC 95397
|
Phosphatase
Apoptosis
|
Cancer
|
|
NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.
|
-
- HY-14348
-
-
- HY-15298C
-
|
Grazoprevir sodium salt
MK-5172 (sodium salt)
|
HCV
HCV Protease
|
Infection
|
|
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-15298B
-
|
Grazoprevir hydrate
MK-5172 (hydrate)
|
HCV
HCV Protease
|
|
|
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-125108
-
-
- HY-122054
-
|
BPK-29
|
Others
|
Cancer
|
|
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-15298
-
|
Grazoprevir
MK-5172
|
HCV Protease
HCV
|
Infection
|
|
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-P1390
-
|
d[Cha4]-AVP
|
Vasopressin Receptor
|
|
|
d[Cha4]-AVP is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
|
-
- HY-100942
-
-
- 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-122054A
-
|
BPK-29 hydrochloride
|
Others
|
Cancer
|
|
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
|
-
- HY-114641A
-
|
BIIL-260 hydrochloride
|
Leukotriene Receptor
|
Inflammation/Immunology
|
|
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM.
|
-
- HY-10559
-
|
Nelotanserin
APD125
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
- HY-15298A
-
|
Grazoprevir potassium salt
MK-5172 (potassium salt)
|
HCV
HCV Protease
|
Infection
|
|
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-101451
-
|
PBIT
|
Histone Demethylase
|
Cancer
|
|
PBIT is a specific inhibitor of the Jumonji AT-rich Interactive Domain 1 (JARID1) enzymes. PBIT inhibits JARID1B (KDM5B or PLU1) histone demethylase with an IC50 of about 3 μM . PBIT also inhibits JARID1A and JARID1C with IC50s of 6 μM and 4.9 μM, respectively.
|
-
- HY-B0910
-
|
Pyrithioxin
Pyritinol; Pyridoxine disulfide; Vitamin B6 disulfide
|
Endogenous Metabolite
|
Neurological Disease
|
|
Pyrithioxin is a neurodynamic compound, combined with a short period of hyperventilation (HV) was applied in cerebral infarct patients with Hemiplegia.
|
-
- HY-B0910A
-
|
Pyrithioxin dihydrochloride
Pyritinol dihydrochloride; Pyridoxine disulfide dihydrochloride; Vitamin B6 disulfide dihydrochloride
|
Others
|
Neurological Disease
|
|
Pyrithioxin dihydrochloride is a neurodynamic compound, combined with a short period of hyperventilation (HV) was applied in cerebral infarct patients with Hemiplegia.
|
-
- HY-B0441
-
|
Tobramycin
Nebramycin Factor 6; Deoxykanamycin B
|
Bacterial
Antibiotic
|
Infection
|
|
Tobramycin (Nebramycin Factor 6) is a parenterally administered, broad spectrum aminoglycoside antibiotic that is widely used in the treatment of moderate to severe bacterial infections due to sensitive organisms.
|
-
- HY-B0511
-
|
Biotin
Vitamin B7; Vitamin H; D-Biotin
|
Others
|
Metabolic Disease
|
|
Biotin is a water-soluble, enzyme co-factor present in minute amounts in every living cell.
|
-
- HY-N1405
-
|
Cucurbitacin I
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-15724
-
|
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK-1605786) is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
|
-
- HY-14660A
-
|
Dabrafenib Mesylate
GSK2118436 Mesylate; GSK 2118436B
|
Raf
|
Cancer
|
|
Dabrafenib Mesylate is a potent and selective Raf kinase inhibitor with IC50s of 0.6 and 5.0 nM for Raf V600E and c-Raf, respectively.
|
-
- HY-33914
-
-
- HY-112423
-
-
- HY-12003
-
|
SNS-314
SNS-314 Mesylate
|
Aurora Kinase
|
Cancer
|
|
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
|
-
- HY-126126
-
-
- HY-107444
-
-
- HY-10804
-
-
- HY-111500A
-
-
- HY-10825
-
-
- HY-100029A
-
|
Bay 41-4109 racemate
|
HBV
|
Infection
|
|
BAY 41-4109 racemate is the racemate of BAY 41-4109. BAY 41-4109 is a potent inhibitor of human hepatitis B virus (HBV) with an IC50 of 53 nM.
|
-
- HY-A0091A
-
-
- HY-B1232
-
-
- HY-P1390A
-
|
d[Cha4]-AVP TFA
|
Vasopressin Receptor
|
|
|
d[Cha4]-AVP TFA is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). d[Cha4]-AVP TFA stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.
|
-
- HY-103131
-
|
PNU-142633
|
5-HT Receptor
|
Neurological Disease
|
|
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.
|
-
- HY-16688
-
|
RU 24969
|
5-HT Receptor
|
Neurological Disease
|
|
RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.
|
-
- HY-15543A
-
-
- HY-103050
-
|
ML-030
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
|
-
- HY-15543
-
-
- HY-10847A
-
|
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-N6639
-
-
- HY-100744
-
-
- HY-10127
-
|
AZD1152
Barasertib
|
Aurora Kinase
|
Cancer
|
|
AZD1152 is a pro-drug of Barasertib-hQPA, which is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay.
|
-
- HY-10161
-
-
- HY-107496
-
-
- HY-10165
-
|
PSI-6130
R 1656
|
HCV
|
Infection
|
|
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
|
-
- HY-U00231
-
-
- HY-100350
-
-
- HY-122882
-
|
HOIPIN-8
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
|
HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.
|
-
- HY-16688B
-
|
RU 24969 hemisuccinate
|
5-HT Receptor
|
Neurological Disease
|
|
RU 24969 hemisuccinate is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion.
|
-
- HY-15414S
-
-
- HY-75800
-
|
Lomibuvir
VX-222
|
DNA/RNA Synthesis
HCV
|
Infection
|
|
Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
|
-
- HY-14711
-
|
Reversine
|
Aurora Kinase
Autophagy
|
Cancer
|
|
Reversine is a novel class of ATP-competitive Aurora kinase inhibitor with IC50s of 400, 500 and 400 nM for Aurora A, Aurora B and Aurora C, respectively.
|
-
- HY-10466
-
|
Daclatasvir
BMS-790052; EBP 883
|
HCV
|
Infection
|
|
Daclatasvir is a potent HCV NS5A protein inhibitor, with mean EC50 values of 50 and 9 pM against genotype 1a and 1b replicons, respectively.
|
-
- HY-70057
-
-
- HY-14574
-
-
- HY-19621
-
-
- 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-N0901
-
|
Corynoxine
|
Autophagy
|
Cancer
|
|
Corynoxine is an enantiomer of Corynoxine B; induces autophagy in different neuronal cell lines, including N2a and SHSY-5Y cells.
|
-
- HY-W007692
-
|
Acetylpyrazine
2-Acetylpyrazine
|
Others
|
Others
|
|
Acetylpyrazine (2-Acetylpyrazine) is fused to form many polycyclic compounds, as useful structures in pharmaceuticals and perfumes. Acetylpyrazine is a component of the folates (vitamin B compounds) .
|
-
- HY-103110A
-
|
ST1936 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human α2 adrenergic receptor.
|
-
- HY-W019939
-
|
Hydroxy-PEG10-Boc
|
ADC Linker
|
Cancer
|
|
Hydroxy-PEG10-Boc is extacted from patent CN108707228 (example 0024). Hydroxy-PEG10-Boc is a uncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Hydroxy-PEG10-Boc can be conjugated to Paclitaxel (HY-B0015) or docetaxel (HY-B0011).
|
-
- HY-P1163
-
|
D[LEU4,LYS8]-VP
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-112061
-
|
8-OH-DPAT
8-Hydroxy-DPAT
|
5-HT Receptor
|
Neurological Disease
|
|
8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
|
-
- HY-100764
-
|
YUKA1
|
Histone Demethylase
|
Cancer
|
|
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
|
-
- HY-108365
-
|
Gamithromycin
ML-1709460
|
Bacterial
Antibiotic
|
Infection
|
|
Gamithromycin is an antimicrobial agent which can inhibit the growth of MmmSC strains B237 and Tan8 with MICs of 0.00012 and 0.00006 μg/mL, respectively.
|
-
- HY-121161
-
-
- HY-111380
-
-
- HY-136266
-
|
HCV-IN-29
|
HCV
|
Cancer
|
|
HCV-IN-29 is a hepatitis C virus (HCV) inhibitor exacted from patent US8329159B2, compound 1e.
|
-
- HY-N5127
-
|
Nonacosane
|
Bacterial
|
Infection
|
|
Nonacosane, isolated from Baphia massaiensis, exhibits weak activities against E. coli, B. subtilis, P. aeruginosa and S. aureus.
|
-
- HY-136306
-
-
- HY-N0159
-
-
- HY-U00301
-
-
- HY-16355
-
|
NVP-QAV-572
|
PI3K
|
Cancer
|
|
NVP-QAV-572 is a PI3K inhibitor extracted from patent US7998990B2, Compound Example 8, has an IC50 of 10 nM.
|
-
- HY-10217
-
-
- HY-N6695
-
|
Aflatoxicol
Aflatoxin R0
|
Others
|
Cancer
|
|
Aflatoxin (Aflatoxin R0) is a metabolite of aflatoxin B1 produced from Rhizopus spp, and is mutagenic and carcinogenic mycotoxin.
|
-
- HY-B1618
-
-
- HY-B0152B
-
|
Adenine hemisulfate
6-Aminopurine hemisulfate; Vitamin B4 hemisulfate
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hemisulfate (6-Aminopurine hemisulfate) is a purine derivative with a variety of roles in biochemistry, including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), and protein synthesis, as a chemical component of DNA and RNA.
|
-
- HY-50946
-
-
- HY-B0152A
-
|
Adenine hydrochloride
6-Aminopurine hydrochloride; Vitamin B4 hydrochloride
|
DNA/RNA Synthesis
Endogenous Metabolite
|
Cancer
|
|
Adenine hydrochloride (6-Aminopurine hydrochloride) is a purine derivative with a variety of roles in biochemistry, including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD), and protein synthesis, as a chemical component of DNA and RNA.
|
-
- HY-N0680
-
-
- HY-15648A
-
|
GSK-J2
|
Histone Demethylase
|
Cancer
|
|
GSK-J2 is an isomer of GSK-J1 that does not have any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.
|
-
- HY-120327
-
|
KY-226
|
Phosphatase
|
Metabolic Disease
Neurological Disease
|
|
KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
|
-
- HY-P1163A
-
|
D[LEU4,LYS8]-VP TFA
|
Vasopressin Receptor
|
Neurological Disease
Cardiovascular Disease
|
|
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP TFA has weak antidiuretic, vasopressor, and in vitro oxytocic activities.
|
-
- HY-W011727A
-
|
Pyridoxal 5'-phosphate monohydrate
Pyridoxal phosphate monohydrate
|
Others
|
Neurological Disease
|
|
Pyridoxal 5'-phosphate hydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate hydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′‐phosphate (PMP).
|
-
- HY-107781
-
-
- HY-13056
-
|
SMND-309
|
Others
|
Neurological Disease
|
|
SMND-309 is a metabolite of salvianolic acid B, and exhibits neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats.
|
-
- HY-14121
-
-
- HY-103035
-
-
- HY-17568
-
|
Nonivamide
Pelargonic acid vanillylamide; Nonanoic acid vanillylamide; Pseudocapsaicin
|
TRP Channel
|
Neurological Disease
|
|
Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
|
-
- HY-N0529
-
-
- HY-15602
-
|
Ledipasvir
GS-5885
|
HCV
|
Infection
|
|
Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
|
-
- HY-112737
-
-
- HY-15591A
-
|
TMC647055 Choline salt
|
HCV
|
Infection
|
|
TMC647055 choline salt is a cell-permeating, selective HCV NS5B inhibitor, eliciting a mean IC50 of 34 nM, as assessed in the RdRp primer-dependent transcription assay.
|
-
- HY-16900
-
-
- HY-N0686
-
-
- HY-N1480
-
|
(-)-Fucose
6-Desoxygalactose; L-(-)-Fucose; L-Galactomethylose
|
Endogenous Metabolite
Parasite
|
Infection
Metabolic Disease
|
|
(-)-Fucose is classified as a member of the hexoses, plays a role in A and B blood group antigen substructure determination, selectin-mediated leukocyte-endothelial adhesion, and host-microbe interactions.
|
-
- HY-18964
-
|
MG-101
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
|
Proteasome
|
Cancer
|
|
MG-101 is a potent inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively.
|
-
- HY-N6798
-
|
Myriocin
|
HCV
Antibiotic
|
Infection
|
|
Myriocin, a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin strongly suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
|
-
- HY-136650
-
-
- HY-W074930
-
|
(S)-Tenofovir
(S)-GS 1278; (S)-PMPA; (S)-TDF
|
HIV
HBV
|
Infection
|
|
(S)-Tenofovir ((S)-GS 1278) is the less active S-enantiomer of Tenofovir. Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
|
-
- HY-112818
-
-
- HY-17561
-
|
G-418 disulfate
Geneticin sulfate; Antibiotic G-418 sulfate
|
Bacterial
Antibiotic
|
Others
|
|
G-418 (disulfate) is an aminoglycoside antibiotic similar in structure to gentamicin B1, which blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells.
|
-
- HY-12425
-
-
- HY-15426
-
-
- HY-124330
-
|
Tripolin A
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
|
-
- HY-17446
-
-
- HY-108896
-
-
- HY-128574
-
-
- HY-126975
-
-
- 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-14202
-
|
Lazabemide hydrochloride
Ro 19-6327 hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-14201
-
|
Lazabemide
Ro 19-6327
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease.
|
-
- HY-101509
-
|
HSL-IN-1
|
Others
|
Metabolic Disease
|
|
HSL-IN-1 (compound 24b) is a potent and orally active hormone sensitive lipase (HSL) inhibitor (IC50=2 nM) with a significantly reduced reactive metabolite liability.
|
-
- HY-W001909
-
|
Myosmine
|
nAChR
|
Metabolic Disease
|
|
Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.
|
-
- HY-100029B
-
-
- HY-130182
-
-
- HY-14660
-
|
Dabrafenib
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
|
-
- HY-10240
-
|
Mericitabine
RG 7128; R-7128; PSI 6130 diisobutyrate
|
HCV
|
Infection
|
|
Mericitabine (RG 7128; R-7128) is a nucleoside inhibitor of the HCV NS5B polymerase that acts as an RNA chain terminator and prevents elongation of RNA transcripts during replication.
|
-
- HY-B1234
-
|
Octinoxate
Octyl methoxycinnamate
|
Others
|
Others
|
|
Octinoxate is an organic compound that is an ingredient in some sunscreens and lip balms, primarily used is in sunscreens and other cosmetics to absorb UV-B rays from the sun, protecting the skin from damage.
|
-
- HY-101312
-
-
- HY-16900A
-
-
- HY-12219B
-
|
MSI-1701
|
Others
|
Metabolic Disease
|
|
MSI-1701 is an analogue of MSI-1436 which can control weight gain and blood glucose level extracted from patent US 7410959 B1.
|
-
- HY-101954
-
|
Inarigivir
ORI-9020; SB-9000
|
HBV
|
Infection
|
|
Inarigivir (ORI-9020;SB-9000) is a dinucleotide which can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus.
|
-
- HY-15701
-
-
- HY-70044
-
|
GSK-1070916
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-W018161
-
|
Hexadecanedioic acid
|
Endogenous Metabolite
|
Others
|
|
Hexadecanedioic acid is covalently linked to Sepharose 4B, shows better performance in terms of specificity than dye-based resins and could be used for depletion of SA from plasma samples.
|
-
- HY-15602B
-
|
Ledipasvir D-tartrate
GS-5885 D-tartrate
|
HCV
|
Infection
|
|
Ledipasvir D-tartrate is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
|
-
- HY-13008
-
-
- HY-15100
-
|
Balicatib
AAE581
|
Cathepsin
|
Inflammation/Immunology
|
|
Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.
|
-
- HY-W013266
-
-
- HY-136267
-
|
HCV-IN-30
|
HCV
|
Infection
|
|
HCV-IN-30 (compound 48) is a HCV NS5A replication complex inhibitor, with IC50s of 901 and 102 nM for genotypes 1a and 1b replicons, respectively.
|
-
- HY-13317S
-
|
Oseltamivir D3
|
Influenza Virus
|
Infection
|
|
Oseltamivir D3 is a deuterium labeled Oseltamivir. Oseltamivir is an influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively. Anti-influenza A and B agent.
|
-
- HY-13866
-
|
Ro 31-8220 mesylate
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate
|
PKC
|
Neurological Disease
Cardiovascular Disease
Cancer
|
|
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- HY-112776
-
|
BN82002
|
Phosphatase
|
Cancer
|
|
BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.
|
-
- HY-124295
-
|
MPT0E028
|
HDAC
Akt
Apoptosis
|
Cancer
|
|
MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
|
-
- HY-103138A
-
|
(Rac)-WAY-161503
|
5-HT Receptor
|
Metabolic Disease
Neurological Disease
|
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.
|
-
- HY-114204
-
|
GSK8814
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1.
|
-
- HY-B0371D
-
|
(S)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.
|
-
- HY-103152
-
-
- HY-13866A
-
|
Ro 31-8220
Bisindolylmaleimide IX
|
PKC
|
Neurological Disease
Cardiovascular Disease
|
|
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
|
-
- 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-126750
-
|
GNF362
|
Phosphatase
|
Inflammation/Immunology
|
|
GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
|
-
- HY-76772A
-
-
- HY-76772
-
|
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
|
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- 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-76772B
-
-
- HY-N3241
-
|
Mucrolidin
|
Bacterial
|
Infection
|
|
Mucrolidin is an eudesmane-type sesquiterpenoid isolated from aerial parts of homalomena occulta. Mucrolidin exhibits weak antibacterial activities when it compares to Rifampicin (HY-B0272).
|
-
- HY-111940
-
|
LUT014
|
Raf
|
Inflammation/Immunology
|
|
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .
|
-
- HY-109025
-
|
Baloxavir marboxil
S-033188
|
Influenza Virus
|
Infection
|
|
Baloxavir marboxil (S-033188) is a selective inhibitor of influenza cap-dependent endonuclease. Baloxavir marboxil, a potent antiviral agent, shows activity against influenza A and B virus.
|
-
- HY-111500
-
-
- HY-12846
-
|
CCT196969
|
Raf
|
Cancer
|
|
CCT196969 is a pan-Raf inhibitor, which inhibits B-Raf, BRaf V600E and CRAF with IC50s of 0.1, 0.04, and 0.01 μM, respectively.
|
-
- HY-129188
-
|
CCT369260
|
Bcl-2 Family
|
Cancer
|
|
CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits a IC50 of 520 nM.
|
-
- HY-131124
-
-
- HY-100595
-
|
Sodium stibogluconate
Stibogluconate trisodium nonahydrate
|
Phosphatase
|
Cancer
|
|
Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
|
-
- HY-111456
-
-
- HY-12866
-
|
Larotrectinib
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-133771AS
-
|
Nordoxepin D3 hydrochloride
Desmethyldoxepin D3 hydrochloride
|
Drug Metabolite
|
Neurological Disease
|
|
Nordoxepin D3 hydrochloride (Desmethyldoxepin D3 hydrochloride) is the deuterium labeled Nordoxepin hydrochloride. Nordoxepin hydrochloride is an active metabolite of Doxepin hydrochloride (HY-B0725), which is an orally active tricyclic antidepressant.
|
-
- HY-107321
-
|
Azosemide
|
NKCC
|
Metabolic Disease
|
|
Azosemide, a sulfonamide loop diuretic, is a potent NKCC1 inhibitor with IC50s of 0.246 µM and 0.197 µM for hNKCC1A and NKCC1B, respectively.
|
-
- HY-17416
-
-
- HY-B0471
-
-
- HY-B0365A
-
-
- HY-10081
-
|
GS-6201
CVT-6883
|
Adenosine Receptor
|
Inflammation/Immunology
|
|
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice.
|
-
- 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-B1658A
-
|
Frovatriptan succinate hydrate
|
5-HT Receptor
|
Neurological Disease
|
|
Frovatriptan succinate hydrate is a potent, high affinity, selective and orally active 5-HT1B, HT1D receptor agonist and a moderately potent 5-HT7 receptor agonist, with pKi values of 8.6, 8.4, and 6.7, respectively. Frovatriptan succinate hydrate is effective in treating the full spectrum of migraine including the associated symptoms of nausea, vomiting, photophobia, and phonophobia. Frovatriptan succinate hydrate can also be used as in mini-prophylaxis in menstrual migraine.
|
-
- HY-N0925
-
|
Tetrahydroberberine
Canadine
|
Dopamine Receptor
|
Neurological Disease
|
|
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
|
-
- HY-B0822
-
|
Fipronil
|
GABA Receptor
Cytochrome P450
|
Neurological Disease
|
|
Fipronil is an insecticide that acts as a selective antagonist of insect GABA receptors (IC50s = 30 nM and 1,600 nM for cockroach and rat receptors, respectively). Fipronil also inhibits desensitizing and non-desensitizing glutamate-induced chloride currents in cockroach neurons (IC500s = 800 nM and 10 nM, respectively). Fipronil induces activity of the cytochrome P450 (CYP) isoforms CYP1A1/2, CYP2B1/2, and CYP3A1/2 in isolated rat liver microsomes.
|
-
- HY-15472
-
-
- HY-30234
-
-
- HY-14200
-
|
(S)-Rasagiline
TVP1022; S-PAI
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) is the S-isomer of Rasagiline, which is an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor.
|
-
- HY-14777
-
|
Radiprodil
RGH-896
|
iGluR
|
Neurological Disease
|
|
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
|
-
- HY-B0250
-
|
Lamivudine
BCH-189
|
HIV
Reverse Transcriptase
|
Infection
|
|
Lamivudine (BCH-189) is a nucleoside reverse transcriptase inhibitors (NRTIs). Lamivudine (BCH-189) can inhibit HIV reverse transcriptase 1/2 and also the reverse transcriptase of hepatitis B virus.
|
-
- HY-30234A
-
-
- HY-14200A
-
|
(S)-Rasagiline mesylate
TVP1022 (mesylate); S-PAI mesylate
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) mesylate is the S-isomer of rasagiline, which is an anti-Parkinson drug, appears to have the same neuroprotective activity as the R-isomer, but is 1000-fold less active as an MAO-B inhibitor.
|
-
- HY-15789
-
|
Elbasvir
MK-8742
|
HCV
|
Infection
|
|
Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
|
-
- HY-100300
-
-
- HY-17587
-
|
4-Methylbenzylidene camphor
4-MBC; Enzacamene
|
AChE
|
Others
|
|
4-Methylbenzylidene camphor(4-MBC; Enzacamene)is an organic camphor derivative that is used in the cosmetic industry for its ability to protect the skin against UV, specifically UV B radiation.
|
-
- HY-15275
-
|
BMS-265246
|
CDK
|
Cancer
|
|
BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.
|
-
- HY-13784
-
|
Pirodavir
R77975
|
Enterovirus
|
Infection
|
|
Pirodavir is a potent, broad-spectrum picornavirus inhibitor, and is highly active against both group A and group B rhinovirus serotypes.
Pirodavir is very potent in a virus yield reduction assay (IC90=2.3 nM).
|
-
- HY-128606
-
-
- HY-B0150
-
|
Nicotinamide
Niacinamide; Nicotinic acid amide
|
Endogenous Metabolite
Sirtuin
|
Neurological Disease
Cancer
|
|
Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
|
-
- HY-18234A
-
|
Leupeptin hemisulfate
|
Cathepsin
|
Inflammation/Immunology
|
|
Leupeptin hemisulfate is a membrane-permeable thiolprotease inhibitor that inhibits Cathepsin B, Cathepsin H and Cathepsin L, and also impairs amphisome-lysosome fusion. Leupeptin hemisulfate also exhibits anti-inflammatory effect.
|
-
- HY-U00399
-
-
- HY-B0018
-
|
Docetaxal
10-Acetyl docetaxel; PNU-101383
|
Microtubule/Tubulin
|
Cancer
|
|
Docetaxal (10-Acetyl docetaxel; PNU-101383), an analog of Docetaxel (HY-B0011), is a microtubule disassembly inhibitor, with antimitotic activity. Docetaxal has cytotoxicity for murine leukemic cells.
|
-
- HY-130253
-
|
IRAK4-IN-6
|
IRAK
|
Cancer
|
|
IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma.
|
-
- HY-N7501
-
-
- HY-N6910
-
|
Pseudolaric Acid C2
|
Others
|
Metabolic Disease
|
|
Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats.
|
-
- HY-136219
-
|
Protein kinase affinity probe 1
|
Others
|
Others
|
|
Protein kinase affinity probe 1 is a novel protein kinase affinity probe for the functional identification of protein kinases (PKs). Protein kinase affinity probe 1 is a modified Purvalanol B (HY-18299) probe with 50% beads loading (Compound S3).
|
-
- HY-13318
-
|
Oseltamivir acid
GS 4071; Ro 64-0802; Oseltamivir carboxylate
|
Influenza Virus
Drug Metabolite
|
Infection
|
|
Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses.
|
-
- HY-136185
-
|
Atorvastatin Epoxy Tetrahydrofuran Impurity
|
Others
|
Others
|
|
Atorvastatin Epoxy Tetrahydrofuran Impurity is an impurity isolated oxidative degradation products of Atorvastatin (HY-B0589). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
|
-
- HY-N2391
-
-
- HY-B0441A
-
|
Tobramycin sulfate
Nebramycin Factor 6 sulfate; Deoxykanamycin B sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Tobramycin sulfate (Nebramycin Factor 6 sulfate) is a parenterally administered, broad spectrum aminoglycoside antibiotic that is widely used in the treatment of moderate to severe bacterial infections due to sensitive organisms.
|
-
- HY-13442A
-
|
Eribulin mesylate
B1939 mesylate; E7389 mesylate; ER-086526 mesylate
|
Microtubule/Tubulin
|
Cancer
|
|
Eribulin mesylate (E7389 mesylate) is a microtubule targeting agent that is used in the treatment of metastatic breast cancer. Eribulin mesylate (E7389 mesylate) inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
|
-
- HY-14850
-
|
Sograzepide
Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
|
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
|
-
- HY-118152
-
|
Org-12962
|
5-HT Receptor
|
Neurological Disease
|
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
|
-
- HY-19336
-
|
BAZ2-ICR
|
Epigenetic Reader Domain
|
Cancer
|
|
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
|
-
- HY-106136
-
|
TIK-301
PD-6735; LY-156735
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.
|
-
- HY-12882A
-
|
Ifenprodil tartrate
|
iGluR
Potassium Channel
|
Neurological Disease
|
|
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.
|
-
- HY-N0652
-
|
2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside
|
Others
|
Others
|
|
2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonum species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.
|
-
- HY-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-113134
-
-
- 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-109137
-
|
Selgantolimod
GS-9688
|
Toll-like Receptor (TLR)
HBV
|
Infection
|
|
Selgantolimod (GS-9688) is an orally active, potent and selective toll-like receptor 8 (TLR8) agonist for the treatment of hepatitis B virus (HBV) and human immunodeficiency virus (HIV) infection.
|
-
- HY-19447
-
|
Besifovir
LB80331
|
HBV
|
Infection
|
|
Besifovir (LB80331), a parent drug converted by LB80380, further metabolizes to its active form, LB80317. LB80380 is potent antiviral agent against hepatitis B virus (HBV) .
|
-
- HY-109586
-
-
- HY-118139
-
|
Desmethyl Celecoxib
|
COX
|
Inflammation/Immunology
|
|
Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%.
|
-
- HY-U00244
-
-
- 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-14165
-
-
- HY-12594
-
|
Paritaprevir
ABT-450; Veruprevir
|
HCV Protease
HCV
|
Infection
|
|
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
|
-
- HY-12529
-
|
Ro-3306
|
CDK
Apoptosis
|
Cancer
|
|
Ro-3306 is a potent and selective inhibitor of CDK1, with Kis of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.
|
-
- HY-101610
-
-
- HY-136093
-
|
HL271
|
AMPK
|
Neurological Disease
|
|
HL271, 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.
|
-
- HY-10468
-
|
NM107
2'-C-Methylcytidine; NM-107
|
HCV
|
Infection
|
|
NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM.
|
-
- HY-128343
-
|
KDM4-IN-2
|
Histone Demethylase
|
Cancer
|
|
KDM4-IN-2 (Compound 19a) is a potent and selective KDM4/KDM5 dual inhibitor with Kis of 4 and 7 nM for KDM4A and KDM5B, respectively.
|
-
- HY-U00213
-
|
Furaprofen
R803
|
HCV
|
Infection
|
|
Furaprofen (R803) is an effective HCV replication inhibitor. Furaprofen (R803) is substantially more potent against genotype 1a and 1b replicons (EC50, ~30 nM) than against the genotype 2a replicon (EC50, ~1,000 nM).
|
-
- HY-136464
-
|
β-catenin-IN-2
|
β-catenin
|
Cancer
|
|
β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer.
|
-
- HY-106235
-
|
LB80317
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
LB80317 is an active metabolite of LB80380 and suppresses the DNA synthesis of HBV with an EC50 of 0.5 μM. LB80317 has antiviral effect and has the potential for chronic hepatitis B treatment.
|
-
- HY-15777A
-
|
Ribociclib hydrochloride
LEE011 hydrochloride
|
CDK
|
Cancer
|
|
Ribociclib hydrochloride (LEE011 hydrochloride) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-136307S
-
|
Tizoxanide-D4 glucuronide
|
Parasite
|
Infection
|
|
Tizoxanide glucuronide-D4 is the deuterium labeled Tizoxanide glucuronide. Tizoxanide glucuronide is the metabolite of Nitazoxanide (HY-B0217) and is cell-permeable to inhibit asexual and sexual stages development of parasite C. parvum.
|
-
- HY-N0063
-
|
Punicalagin
|
HBV
|
Cancer
Infection
Metabolic Disease
|
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects.
|
-
- HY-10201S
-
-
- HY-135145
-
|
CB-103
|
Notch
|
Cancer
|
|
CB-103 is a first-in-class orally active notch signaling pathway inhibitor extracted from patent US9296682B2. CB-103 has anti-tumor activity.
|
-
- HY-113206
-
-
- HY-N3199
-
|
Neorauflavene
|
Bacterial
|
Infection
|
|
Neorauflavene is a phenolic neorautanenia isoflavanoid isolated from Neorautanenia edulis. Neorauflavene shows antibacterial activities against E. faecalis, S. suis, S. agalactiae, P. aeruginosa, B. subtilis, and R. anatipestifer.
|
-
- HY-10201S1
-
-
- HY-128759
-
|
DYRKs-IN-2
|
DYRK
|
Cancer
|
|
DYRKs-IN-2 (Example 132) is a potent DYRKs inhibitor with IC50s of 30.6 nM and 12.8 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-2 has antitumor activity.
|
-
- HY-N0840
-
|
Bruceantin
(-)-Bruceantin; NCI165563; NSC165563
|
Others
|
Cancer
|
|
Bruceantin(NSC165563) is first isolated from Brucea antidysenterica, a tree used in Ethiopia for the treatment of cancer, and activity was observed against B16 melanoma, colon 38, and L1210 and P388 leukemia in mice.
|
-
- HY-13962
-
-
- HY-P1441
-
|
Mambalgin 1
|
Sodium Channel
|
|
|
Mambalgin 1 is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
-
- HY-10895
-
|
SB-334867
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
|
-
- HY-136065A
-
|
bpV(phen) hydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) hydrate is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B. bpV(phen) hydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) hydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) hydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-136065
-
|
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
|
bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-12445
-
|
CDKI-73
|
CDK
Apoptosis
|
Cancer
|
|
CDKI-73 is a potent CDK9 inhibitor with Ki of 4 nM; shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).
|
-
- HY-15236
-
|
PSI-6206
RO 2433; GS-331007
|
HCV
|
Infection
|
|
PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
|
-
- 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-122700
-
|
Factor D inhibitor 6
|
Complement System
|
Inflammation/Immunology
|
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-107774
-
|
BMS-986163
|
iGluR
|
Neurological Disease
|
|
BMS-986163 is a negative allosteric modulator of GluN2B. The prodrug BMS-986163 rapidly converts to its active parent molecule BMS-986169 (Ki=4 nM, IC50=24 nM).
|
-
- HY-109025A
-
|
Baloxavir
Baloxavir acid; S-033447
|
Influenza Virus
|
Infection
|
|
Baloxavir (Baloxavir acid) is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.
|
-
- HY-10329
-
|
JNJ-7706621
|
Aurora Kinase
CDK
Apoptosis
|
Cancer
|
|
JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
|
-
- HY-B0602D
-
-
- HY-136093A
-
|
IM156
HL156A
|
AMPK
|
Neurological Disease
|
|
IM156 (HL156A), a chemical derivative of metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model.
|
-
- HY-W012982
-
-
- HY-15602D
-
|
Ledipasvir (diacetone)
GS-5885 diacetone
|
HCV
|
Infection
|
|
Ledipasvir diacetone (GS-5885 diacetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
|
-
- HY-113151
-
-
- HY-111547
-
|
M1001
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex.
|
-
- HY-15602A
-
|
Ledipasvir (acetone)
GS-5885 acetone
|
HCV
|
Infection
|
|
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
|
-
- HY-10290
-
|
MK-0674
|
Cathepsin
|
Metabolic Disease
|
|
MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S.
|
-
- HY-135679
-
-
- HY-A0261
-
|
Pentagastrin
ICI-50123
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
|
|
Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury.
|
-
- HY-128941
-
-
- 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-15463S1
-
|
Imatinib D4
STI571 D4; CGP-57148B D4
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib D4 (STI571 D4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
|
-
- HY-15463S
-
|
Imatinib D8
STI571 D8; CGP-57148B D8
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
|
Imatinib D8 (STI571 D8) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
|
-
- HY-12176
-
-
- HY-130716
-
-
- HY-P2093
-
|
S961
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-19910
-
|
Acoziborole
SCYX-7158; AN5568
|
Parasite
|
Infection
|
|
Acoziborole (SCYX-7158) is an effective, safe and orally active antiprotozoal agent for the research of human african trypanosomiasis (HAT). In the T. b. brucei S427 strain, the MIC value for SCYX-7158 is 0.6 µg/mL.
|
-
- HY-70069
-
-
- HY-15777
-
|
Ribociclib
LEE011
|
CDK
|
Cancer
|
|
Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-P2093B
-
|
S961 acetate
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-130515
-
|
Cdc7-IN-3
|
CDK
|
Cancer
|
|
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-19718
-
|
OTS964
|
TOPK
CDK
Apoptosis
|
Cancer
|
|
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
|
-
- HY-107477
-
|
GSK8573
|
Epigenetic Reader Domain
|
Cancer
|
|
GSK8573 (compound 23) is an inactive control compound for GSK2801. GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy.
|
-
- HY-15777C
-
|
Ribociclib succinate hydrate
LEE011 succinate hydrate
|
CDK
|
Cancer
|
|
Ribociclib succinate hydrate (LEE011 succinate hydrate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-15777B
-
|
Ribociclib succinate
LEE011 succinate
|
CDK
|
Cancer
|
|
Ribociclib succinate (LEE011 succinate) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-112254
-
|
ZINC03129319
|
Virus Protease
|
Infection
|
|
ZINC03129319 is a dengue virus (DENV) NS2B-NS3 protease inhibitor extracted from patent US20150141521A1, has inhibition constants (Ki1) of 92 μM and Ki3 of 20 μM.
|
-
- HY-10799
-
|
EG00229
|
Complement System
|
Cancer
|
|
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 μM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2.
|
-
- HY-12866A
-
|
Larotrectinib sulfate
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-103142
-
|
AS19
|
5-HT Receptor
|
Neurological Disease
|
|
AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
|
-
- 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-10238
-
|
Danoprevir
ITMN-191; R7227; RO5190591; RG7227
|
HCV Protease
HCV
|
Infection
|
|
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM).
|
-
- HY-P1441A
-
|
Mambalgin 1 TFA
|
Sodium Channel
|
|
|
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
-
- HY-B1101
-
|
Pimethixene
Pimetixene
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
|
-
- HY-10895A
-
|
SB-334867 free base
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
|
-
- HY-15504A
-
|
RGB-286638 free base
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-B1101A
-
|
Pimethixene maleate
Pimetixene maleate
|
5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
|
-
- HY-15504
-
|
RGB-286638
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-108697
-
|
PT2399
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
|
-
- HY-119933
-
|
RIPK1-IN-7
|
RIP kinase
|
Cancer
|
|
RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
|
-
- HY-102038
-
|
PC786
|
RSV
|
Infection
|
|
PC786 is an inhaled respiratory syncytial virus (RSV) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A (IC50 <0.09 to 0.71 nM) and RSV-B (IC50, 1.3 to 50.6 nM).
|
-
- HY-100678
-
-
- HY-129993
-
-
- HY-136459
-
|
NMDA receptor antagonist 2
|
iGluR
|
Neurological Disease
|
|
NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC50 and a Ki of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.
|
-
- HY-15590
-
|
AZ-23
AZ23; AZ 23
|
Trk Receptor
|
Cancer
|
|
AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.
|
-
- HY-P2093A
-
|
S961 TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-100540
-
|
Golgicide A
|
Enterovirus
|
Cancer
Infection
|
|
Golgicide A is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF), GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
|
-
- HY-103249
-
|
Reutericyclin
Reutericycline
|
Bacterial
Antibiotic
|
Infection
|
|
Reutericyclin (Reutericycline), a unique tetramic acid, is an antibiotic produced by some strains of Lactobacillus reuteri. Reutericyclin (Reutericycline) exhibits a broad inhibitory spectrum including Lactobacillus spp., Bacillus subtilis, B. cereus, Enterococcus faecalis, Staphylococcus aureus, and Listeria innocua.
|
-
- HY-44432
-
-
- HY-N2360
-
|
Hinokiflavone
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity.
|
-
- HY-12057
-
|
Vemurafenib
PLX4032; RG7204; RO5185426
|
Raf
Autophagy
|
Cancer
|
|
Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAF V600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
|
-
- 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-12881
-
|
Eliprodil
SL-820715
|
iGluR
|
Neurological Disease
|
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-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-128758
-
|
DYRKs-IN-1
|
DYRK
|
Cancer
|
|
DYRKs-IN-1 (Example 183) is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 9 nM and 5 nM for DYRK1B and DYRK1A, respectively. DYRKs-IN-1 has antitumor activity.
|
-
- HY-N6773
-
|
Cytochalasin A
|
HIV Protease
Fungal
|
Infection
|
|
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
|
-
- HY-126326
-
|
SWE101
|
Epoxide Hydrolase
|
Metabolic Disease
|
|
SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH.
|
-
- HY-113259
-
|
7α-Hydroxy-4-cholesten-3-one
|
Endogenous Metabolite
|
Metabolic Disease
|
|
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
|
-
- HY-105285
-
-
- HY-B0324A
-
|
Crystal Violet
Basic Violet 3; Gentian Violet; Methyl Violet 10B
|
Influenza Virus
Bacterial
|
Infection
|
|
Crystal violet (Basic Violet 3) is a triarylmethane dye. Crystal Violet (Gentian Violet) has antiviral effects against H1N1 and also has prominent bactericidal activities.
|
-
- HY-N0289
-
-
- HY-131254
-
-
- HY-B0602S
-
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
|
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
|
-
- HY-U00186
-
-
- HY-106408A
-
|
Salfaprodil
Neu2000 potassium
|
iGluR
|
Neurological Disease
|
|
Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death.
|
-
- HY-101490
-
-
- HY-101964
-
|
SPI-112
|
Phosphatase
|
Cancer
|
|
SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.
|
-
- HY-N3522
-
|
Platycoside E
|
Others
|
Inflammation/Immunology
|
|
Platycoside E is a platycodigenin-type saponin isolated from the root of Platycodon grandiflorum with haemolytic activity and adjuvant potential. Platycoside E promotes the production of the sera OVA-specific IgG2a and IgG2b antibody in the ovalbumin (OVA)-immunized mice.
|
-
- HY-100507
-
|
Avadomide
CC 122
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
|
-
- HY-B0602S1
-
-
- HY-11012
-
|
TDZD-8
GSK-3β Inhibitor I; NP 01139
|
GSK-3
|
Cancer
|
|
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
|
-
- HY-108323
-
|
CCR2 antagonist 4
Teijin compound 1
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-103362
-
|
CCR2 antagonist 4 hydrochloride
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
|
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-10399
-
|
Ladostigil
TV-3326
|
Monoamine Oxidase
AChE
|
Neurological Disease
|
|
Ladostigil is a dual inhibitor of monoamine oxidase (MAO) and acetylcholinesterase (AChE), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease.
|
-
- HY-131246
-
|
DM-01
|
Histone Methyltransferase
|
Cancer
|
|
DM-01 is a powerful and selective EZH2 inhibitor for the research of diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), and SNF5/INI-1/SMARCB1 genetically defined solid tumors.
|
-
- HY-19533
-
|
SCH 58261
|
Adenosine Receptor
|
Cancer
|
|
SCH 58261 is a potent, selective and competitive antagonist of adenosine A2A receptor with an IC50 of 15 nM, and displays 323-, 53- and 100-fold more selective for A2A receptor than A1, A2B, and A3 receptors, respectively.
|
-
- HY-136546
-
|
Stafia-1
|
STAT
|
Cancer
|
|
Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
|
-
- HY-103061
-
|
Dehydro-ZINC39395747
|
Others
|
Cardiovascular Disease
|
|
Dehydro-ZINC39395747 is a derivative of ZINC39395747. ZINC39395747 is a potent cytochrome b5 reductase 3 (CYB5R3) inhibitor with an IC50 of 9.14 μM and a Kd of 1.11 μM. ZINC39395747 can increase NO bioavailability in vascular cells.
|
-
- HY-13318S
-
|
Oseltamivir acid D3
GS 4071 D3; Ro 64-0802 D3; Oseltamivir carboxylate D3
|
Influenza Virus
|
Infection
|
|
Oseltamivir acid D3 (GS 4071 D3) is a deuterium labeled Oseltamivir acid. Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses.
|
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
|
-
- HY-114661
-
|
m-PEG4-Tos
|
PROTAC Linker
|
Cancer
|
|
m-PEG4-Tos is a derivative of silybin ethers, extracted from patent CN105037337A (compound III-b). m-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of Silymarin (HY-W043277).
|
-
- HY-135330
-
|
Lamivudine 13C,15N2
|
HIV
Reverse Transcriptase
|
Infection
|
|
Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus.
|
-
- HY-122487
-
|
Troriluzole
BHV-4157
|
Others
|
Neurological Disease
|
|
Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
|
-
- HY-100866B
-
|
F1324 acetate
|
Bcl-2 Family
|
Cancer
|
|
F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-12930
-
|
SPR719
VXc-486
|
Topoisomerase
Bacterial
|
Infection
|
|
SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple drug-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively.
|
-
- 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-P1508
-
|
Bactenecin
Bactenecin, bovine
|
Bacterial
Fungal
|
Infection
|
|
Bactenecin (Bactenecin, bovine) is a potent 12-aa looped antimicrobial peptide isolated from bovine neutrophils. Bactenecin inhibits the growth of bacteria and yeast, and kills the fungus Trichophyton rubrum. Bactenecin increass membrane permeability, inhibits the growth and biofilm formation of B. pseudomallei.
|
-
- HY-100246
-
-
- HY-100866
-
|
F1324
|
Bcl-2 Family
|
Cancer
|
|
F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-B0371B
-
|
(R)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
|
-
- HY-111926
-
-
- HY-106697
-
|
Statil
Ponalrestat
|
Aldose Reductase
|
Metabolic Disease
|
|
Statil (Ponalrestat) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Statil selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Statil inhibits the conversion of glucose to sorbitol.
|
-
- 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-15701B
-
|
ADH-503
(Z)-Leukadherin-1 choline
|
Complement System
|
Cancer
|
|
ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-119375
-
|
Syncytial Virus Inhibitor-1
|
Bacterial
|
Infection
|
|
Syncytial Virus Inhibitor-1 is a potent, orally bioavailable respiratory syncytial virus (RSV) fusion inhibitor with EC50s of 0.002 μM, 0.004 μM, and 0.002 μM for RSV Long, RSV A2, and RSV B strains, respectively.
|
-
- HY-117535
-
|
CDK2-IN-4
|
CDK
|
Cancer
|
|
CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM).
|
-
- HY-P2274
-
|
Argifin
|
Parasite
|
Infection
|
|
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively.
|
-
- HY-12457
-
|
Rachelmycin
CC-1065; NSC 298223
|
Antibiotic
|
Cancer
Infection
|
|
Rachelmycin (CC-1065; NSC 298223) is a potent naturally antibiotic isolated from Streptomyces zelensis. Rachelmycin binds non-covalently and covalently (N-3 adenine adduct) in the minor groove of B-form DNA. Rachelmycin has exceptionally potent antitumor activity.
|
-
- HY-126250
-
|
NPD-1335
|
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
|
|
NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death.
|
-
- HY-N6027
-
|
Cyclosporin C
|
Fungal
Bacterial
|
|
|
Cyclosporin C is a fungal metabolite that has been found in T. inflatum and has diverse biological activities, including antifungal, antiviral, and immunosuppressant properties. Cyclosporin C is active against isolates of B. cinerea, A. niger, and Alternaria, Mucor, and Penicillium species (MICs=0.1-5 μg/ml).
|
-
- HY-135750
-
|
VAF347
|
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
VAF347 is a cell permeable and highly affinity aryl hydrocarbon receptor (AhR) agonist and induces AhR signaling. VAF347 inhibits the development of CD14 +CD11b + monocytes from granulo-monocytic (GM stage) precursors. VAF347 has anti-inflammatory effects.
|
-
- HY-12467
-
|
OTS964 hydrochloride
|
TOPK
CDK
Apoptosis
|
Cancer
|
|
OTS964 hydrochloride is an orally active, high affinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM. OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.
|
-
- 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-10847B
-
|
SB-277011 hydrochloride
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-100866A
-
|
F1324 TFA
|
Bcl-2 Family
|
Cancer
|
|
F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
|
-
- HY-106408
-
|
Salfaprodil free base
Neu2000
|
iGluR
|
Neurological Disease
|
|
Salfaprodil free base (Neu2000) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil free base has excellent neuroprotection against NMDA- and free radical-induced cell death.
|
-
- HY-N7204
-
-
- HY-107514
-
|
(RS)-PPG
|
mGluR
|
Neurological Disease
|
|
(RS)-PPG is a potent and selective agonist for group III mGluRs. The EC50s of 5.2 μM, 4.7 μM, 185 μM, and 0.2 μM for hmGluR4a, hmGluR6, hmGluR7b, and hmGluR8a, respectively. Anticonvulsive and neuroprotective activity.
|
-
- HY-19921
-
|
JTK-853
|
HCV
|
Infection
|
|
JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 µM in genotype 1a H77 and 1b Con1 strains, respectively.
|
-
- HY-103354
-
|
Proglumide sodium
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
|
-
- HY-12422
-
|
Voruciclib
|
CDK
|
Cancer
|
|
Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
|
-
- HY-13953
-
|
JIB-04
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
JIB-04 is a pan-selective Jumonji histone demethylase inihibitor with IC50s of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D, respectively.
|
-
- HY-111101
-
|
AZ1495
|
IRAK
|
Cancer
|
|
AZ1495 (compound 28) is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Shows activity in treatment of mutant MYD88 L265P diffuse large B-cell lymphoma (DLBCL).
|
-
- HY-12422A
-
|
Voruciclib hydrochloride
|
CDK
|
Cancer
|
|
Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL).
|
-
- HY-15236S
-
|
PSI-6206 13CD3
RO-2433 13CD3; GS-331007 13CD3; Sofosbuvir metabolite GS-331007 13CD3
|
HCV
|
Others
|
|
PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
|
-
- HY-U00322
-
-
- HY-P0323
-
|
GP(33-41)
|
Arenavirus
|
Infection
|
|
GP(33-41), a 9-aa-long peptide, is the optimal sequence of the GP1 epitope of lymphocytic choriomeningitis virus, and can upregulate H-2D b molecules at the RMA-S (Db Kb) cell surface with a SC50 of 344 nM.
|
-
- HY-15777S
-
|
Ribociclib D6
LEE011 D6
|
CDK
|
Cancer
|
|
Ribociclib D6 (LEE011 D6) is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.
|
-
- HY-14531
-
|
Talarozole
R115866
|
RAR/RXR
Cytochrome P450
Autophagy
|
Inflammation/Immunology
|
|
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
|
-
- HY-15701A
-
|
(Z)-Leukadherin-1
ADH-503 free base
|
Complement System
|
Cancer
|
|
(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
|
-
- HY-B1330
-
|
Proglumide
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.
|
-
- HY-14520
-
|
Tetrahydrofolic acid
L-5,6,7,8-Tetrahydrofolic acid; L-Tetrahydrofolic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid.
|
-
- HY-118743
-
|
KMN-80
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
|
-
- 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-109112
-
|
Brilaroxazine
RP5063
|
Dopamine Receptor
5-HT Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
|
-
- HY-N0049
-
|
Nuciferine
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- HY-15703
-
|
QNZ46
|
iGluR
|
Neurological Disease
|
|
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).
|
-
- HY-19828
-
|
Herboxidiene
GEX1A
|
DNA/RNA Synthesis
|
Cancer
|
|
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
|
-
- HY-P1508A
-
|
Bactenecin TFA
Bactenecin, bovine TFA
|
Bacterial
Fungal
|
Infection
|
|
Bactenecin TFA (Bactenecin, bovine TFA) is a potent 12-aa looped antimicrobial peptide isolated from bovine neutrophils. Bactenecin TFA inhibits the growth of bacteria and yeast, and kills the fungus Trichophyton rubrum. Bactenecin TFA increass membrane permeability, inhibits the growth and biofilm formation of B. pseudomallei.
|
-
- HY-A0007
-
-
- HY-129911
-
|
FABP-IN-1
|
FABP
|
Inflammation/Immunology
|
|
FABP-IN-1 (Compounds 4b) is a high affinity fatty acid binding protein (FABP) inhibitor. FABP-IN-1 inhibits FABP3, FABP5, and FABP7 with Ki values of 0.69 μM, 0.55 μM and 0.67 μM, respectively. FABP-IN-1 displays potent antinociceptive effects.
|
-
- HY-W010130
-
-
- HY-16018
-
|
Ilorasertib
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
RET
|
Cancer
|
|
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
|
-
- HY-131328
-
|
BTK inhibitor 16
|
Btk
|
Cancer
|
|
BTK inhibitor 16 is a potent Bruton's tyrosine kinase (BTK) inhibitor extracted from patent WO2017103611A1, example 163b, with IC50s of <10 nM for BTK WT and BTK C81S, respectively. BTK inhibitor 16 shows low EGFR inhibition, with an IC50 ranging 1~10 μM.
|
-
- HY-P1115
-
|
AKTide-2T
|
Akt
|
Others
|
|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
-
- HY-50514
-
|
AT9283
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
|
-
- HY-B0964
-
-
- HY-16018A
-
|
Ilorasertib hydrochloride
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
RET
VEGFR
|
Cancer
|
|
Ilorasertib hydrochloride (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
|
-
- HY-N2106
-
|
Dehydroevodiamine
|
NF-κB
COX
PGE synthase
NO Synthase
|
Inflammation/Immunology
|
|
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
|
-
- HY-13628
-
|
Etalocib
LY293111; VML 295
|
Leukotriene Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [ 3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
|
-
- HY-15999A
-
|
Cerdulatinib hydrochloride
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies.
|
-
- HY-10014
-
|
R547
|
CDK
GSK-3
Apoptosis
|
Cancer
|
|
R547 is a potent, selective and oral orally bioavailable ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
|
-
- HY-116767
-
|
BLT-1
|
Others
|
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 has pro-inflammatory functions through neutrophil recruitment.
|
-
- HY-133669
-
|
DDR1-IN-5
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-5 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 7.36 nM. DDR1-IN-5 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 4.1 nM. DDR1-IN-5 has anti-cancer activity.
|
-
- HY-112698
-
|
CA-5f
|
Autophagy
Apoptosis
|
Cancer
|
|
CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
|
-
- HY-123812
-
-
- HY-111930
-
|
5-Iodo-indirubin-3'-monoxime
|
GSK-3
CDK
|
Cancer
|
|
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively.
|
-
- HY-133670
-
|
DDR1-IN-6
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-6 is a selective Discoidin Domain Receptor family, member 1 (DDR1) inhibitor with an IC50 of 9.72 nM. DDR1-IN-6 inhibits auto-phosphorylation DDR1b (Y513) with an IC50 of 9.7 nM. DDR1-IN-6 has anti-cancer activity.
|
-
- HY-P1115A
-
|
AKTide-2T TFA
|
Akt
|
Others
|
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position.
|
-
- HY-18768
-
|
NCT-501
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-15023
-
|
Cligosiban
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
|
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents.
|
-
- HY-N0527
-
|
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose
|
Influenza Virus
|
Infection
|
|
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
|
-
- HY-12661A
-
|
AMG PERK 44
|
PERK
Autophagy
|
Cancer
|
|
AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy.
|
-
- HY-124806
-
|
TTP-8307
|
Enterovirus
DNA/RNA Synthesis
HCV
|
Infection
|
|
TTP-8307 is a potent inhibitor of the replication of several rhino- and enteroviruses. TTP-8307 inhibits coxsackievirus B3 (CVB3; EC50=1.2 μM) and poliovirus by interfering with the synthesis of viral RNA. TTP-8307 exerts antiviral activity through oxysterol-binding protein (OSBP).
|
-
- HY-75502
-
-
- HY-101300
-
-
- HY-18161
-
|
CCT241736
|
FLT3
Aurora Kinase
|
Cancer
|
|
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
|
-
- HY-P2336
-
|
CCZ01048
|
Melanocortin Receptor
|
Cancer
|
|
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.
|
-
- HY-U00364
-
-
- HY-103354A
-
|
Proglumide hemicalcium
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
|
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.
|
-
- HY-12649
-
|
Y16
|
Ras
|
Cancer
|
|
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
|
-
- HY-P2336A
-
|
CCZ01048 TFA
|
Melanocortin Receptor
|
Cancer
|
|
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
|
-
- HY-116686
-
|
Inz-1
|
Cytochrome P450
Fungal
|
Infection
|
|
Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in the pathogenic fungus Candida albicans.
|
-
- HY-101254
-
|
Luzindole
N-0774
|
Melatonin Receptor
|
Neurological Disease
|
|
Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity.
|
-
- HY-103022
-
|
Repotrectinib
TPX-0005
|
ROS
Trk Receptor
ALK
|
Cancer
|
|
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
|
-
- HY-116423
-
|
JH295
|
Others
|
Cancer
|
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint.
|
-
- HY-18137
-
|
PF-04995274
|
5-HT Receptor
|
Neurological Disease
|
|
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
|
-
- HY-12177
-
-
- HY-136527
-
|
BMS-986251
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
|
-
- HY-122218
-
|
JHU-083
|
Glutaminase
|
Neurological Disease
|
|
JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
|
-
- HY-133551
-
|
WF-47-JS03
|
RET
|
Cancer
|
|
WF-47-JS03 is a potent RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, CCDC6-RET transfected LC-2/ad lung cancer cells, respectively.
|
-
- HY-B0602
-
|
Desvenlafaxine
O-Desmethylvenlafaxine
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
|
-
- HY-15394
-
-
- HY-18299A
-
|
Purvalanol A
NG-60
|
CDK
Autophagy
Apoptosis
|
Cancer
|
|
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
|
-
- HY-19333
-
|
OG-L002
|
Histone Demethylase
Monoamine Oxidase
HSV
|
Infection
|
|
OG-L002 is a potent and highly selective LSD1 inhibitor with an IC50 of 0.02 μM. OG-L002 is a potent monoamine oxidases (MAO) inhibitor with IC50s of 1.38 μM and 0.72 μM for MAO-A and MAO-B, respectively. OG-L002 potently inhibits the expression of HSV IE genes.
|
-
- HY-116171
-
|
(Rac)-Calpain Inhibitor XII
|
Proteasome
|
|
|
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM), with lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has been used to study the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury.
|
-
- HY-14873
-
|
Tonapofylline
BG 9928
|
Adenosine Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure.
|
-
- HY-122942
-
-
- HY-125733
-
|
Thiocillin I
|
Bacterial
|
Infection
|
|
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively.
|
-
- HY-N6801
-
|
Nivalenol
|
Caspase
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Nivalenol, classified as type B trichotecenes toxins produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol induces cell death through caspase-dependent mechanisms and via the intrinsic apoptotic pathway. Nivalenol affects the immune system, causes emesis, growth retardation, reproductive disorders and has a haematotoxic/myelotoxic effect.
|
-
- HY-116463C
-
-
- HY-118700
-
|
2-Iminobiotin
Guanidinobiotin
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively. 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage.
|
-
- HY-18263A
-
|
Elubrixin
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation.
|
-
- HY-18768A
-
|
NCT-501 hydrochloride
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-13247
-
|
Setrobuvir
ANA598
|
DNA/RNA Synthesis
HCV
SARS-CoV
|
Infection
|
|
Setrobuvir (ANA598) is an orally active non-nucleosidic HCV NS5B polymerase inhibitor. ANA-598 inhibits both de novo RNA synthesis and primer extension, with IC50s between 4 and 5 nM. Setrobuvir also shows excellent binding affinity to SARS-CoV-2 RdRp and induces RdRp inhibition.
|
-
- HY-122537A
-
|
Arotinolol
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
|
-
- HY-136573
-
|
5-Hydroxytoluene-2,4-disulphonic acid diammonium
|
Virus Protease
|
Infection
|
|
5-Hydroxytoluene-2,4-disulphonic acid diammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
|
-
- HY-136153
-
|
Amphotericin X1
|
Fungal
|
Infection
|
|
Amphotericin X1 is an 13-O-methyl derivative of Amphotericin B with good antifungal activity. Amphotericin X1 inhibits Candida albicans 33/079, C.parapsilosis 937A, Cryptococcus neoformans 451, Aspergillus niger 57A and A.fumigatus with MIC values of 1 μg/mL, 8 μg/mL, 1 μg/mL, 2 μg/mL and 2 μg/mL, respectively.
|
-
- HY-136575
-
|
4-Hydroxy-2-methylbenzenesulfonic acid ammonium
|
Virus Protease
|
Infection
|
|
4-Hydroxy-2-methylbenzenesulfonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
|
-
- HY-123033A
-
|
Nicotinamide riboside chloride
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
|
Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-103370
-
|
Talniflumate
BA 7602-06
|
Chloride Channel
|
Inflammation/Immunology
|
|
Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
|
-
- HY-B0602A
-
|
Desvenlafaxine succinate hydrate
O-Desmethylvenlafaxine succinate hydrate
|
Serotonin Transporter
|
Neurological Disease
|
|
Desvenlafaxine succinate hydrate, the succinate salt form of the isolated major active metabolite of Venlafaxine (HY-B0196), is an orally active and BBB penetrated 5-HT and norepinephrine reuptake inhibitor, with IC50 values of 47.3 nM and 531.3 nM for hSERT and hNET, respectively. Desvenlafaxine succinate hydrate shows weak binding affinity (62% inhibition at 100 μM) at the human dopamine (DA) transporter.
|
-
- HY-111544
-
|
EML741
|
Histone Methyltransferase
|
Cancer
|
|
EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.
|
-
- HY-114491
-
|
ERK-IN-1
|
Raf
ERK
|
Cancer
|
|
ERK-IN-1 (compound B) is a RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC (non-small celllung cancer), BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovanan cancer.
|
-
- HY-103171
-
|
BAY 60-6583
|
Adenosine Receptor
|
Inflammation/Immunology
Cardiovascular Disease
|
|
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.
|
-
- HY-P0162
-
|
HCV-IN-4
|
HCV
|
Infection
|
|
HCV-IN-4 is a potent and orally active HCV NS5A inhibitor, shows great potency against GT1a, GT2b, GT3a, GT1a Y93H and GT1a L31V, with EC90s of 3 pM, 0.3 nM, 0.01 nM, 0.5 nM and 0.02 nM, respectively.
|
-
- HY-136574
-
|
2-Hydroxy-4-methylbenzenesulphonic acid ammonium
|
Virus Protease
|
Infection
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2-Hydroxy-4-methylbenzenesulphonic acid ammonium is an impurity of Policresulen. Policresulen is a potent NS2B/NS3 protease inhibitor with an IC50 of 0.48 μg/mL. Policresulen effectively inhibits the replication of DENV2 virus in BHK-21 cells with an IC50 of 4.99 μg/mL. Policresulen acted as a competitive inhibitor of the protease, and slightly affected the protease stability.
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- HY-W014502
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