Search Result
Results for "
Growth inhibition
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14792B
-
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Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride
|
PPAR
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Cancer
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Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
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-
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- HY-116392H
-
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Others
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Others
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D,L-erythro-PDMP hydrochloride is an erythro isomer of PDMP. D,L-erythro-PDMP hydrochloride causes growth inhibition of cultured rabbit skin fibroblasts. PDMP is an effective inhibitor of UDP-glucose:ceramide glucosyltransferase .
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- HY-119819
-
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Bacterial
Parasite
Antibiotic
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Infection
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Psicofuramine a nucleoside antibiotic and has the inhibition of xanthosine 5'-phosphate aminase. Psicofuranine also specifically inhibits GMP synthase, and interrupts parasite growth. Psicofuranine exhibits a dose-dependent inhibition of P. falciparum growth .
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-
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- HY-115965
-
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Bacterial
Antibiotic
|
Infection
|
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VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95% .
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-
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- HY-14754
-
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S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS
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Ras
Autophagy
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Cancer
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Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
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-
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- HY-N0671
-
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Rhaponiticin
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Apoptosis
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Cancer
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Rhapontin (Rhaponiticin), a component of rhubarb (Rheum officinale Baill), induces apoptosis resulting in suppression of proliferation of human stomach cancer KATO III cells .
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-
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- HY-107233
-
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Prosapogenin CP4
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Others
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Others
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Saponin CP4 is an oleanolic acid derivative which lacks a 23-OH. Saponin CP4 shows no growth inhibition .
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-
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- HY-116392G
-
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Others
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Others
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D,L-erythro-PDMP is an erythro isomer of PDMP. D,L-erythro-PDMP causes growth inhibition of cultured rabbit skin fibroblasts. PDMP is an effective inhibitor of UDP-glucose:ceramide glucosyltransferase .
|
-
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- HY-162881
-
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EGFR
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Cancer
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DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
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-
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- HY-115964
-
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Bacterial
Antibiotic
|
Infection
|
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VP-4556 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) agent. VP-4556 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 8 µg/mL. VP-4556 inhibits the growth of methicillin‐resistant Staphylococcus aureus with growth inhibition >95% .
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- HY-119113
-
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Others
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Cancer
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C 175 is a nitroacridine derivative with antitumor activity. C 175 inhibits the growth of HeLa cells monolayer (ED50=0.49 μM) .
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-
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- HY-N7082
-
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Others
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Infection
|
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D-Arabinose, a monosaccharide, shows strong growth inhibition against the Caenorhabditis elegans with an IC50 of 7.5 mM .
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-
-
- HY-W017401
-
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BIT
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Others
|
Infection
Cancer
|
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Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
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-
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- HY-N2871
-
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Apoptosis
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Cancer
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Angophorol is a flavonone compound. Angophorol exerts potential anticancer activity through growth inhibition and apoptosis in K562 cells .
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-
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- HY-W414724
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Others
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Others
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Methabenzthiazuron is a herbicide, which inhibits the plants' growth through inhibition of photosynthesis. Methabenzthiazuron can be used for weed control in cereal crops .
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- HY-U00177
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GDP366
1 Publications Verification
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Survivin
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Cancer
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GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
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-
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- HY-14792
-
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Efatutazone; CS-7017; RS5444
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PPAR
|
Cancer
|
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Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
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-
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- HY-D1472
-
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Fluorescent Dye
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Others
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Azure A eosinate is a dye for hematological and histological applications. Azure A eosinate can be used as new photosensitizer prototypes to determine growth inhibition of Candida albicans .
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-
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- HY-N12118
-
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Fungal
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Infection
|
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Piperanine is an antifungal agent. Piperanine shows growth inhibition against the fungus Cladosporium claspoirioides. Piperanine can be isolated from the fruits of Piper retrofractum .
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-
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- HY-153626
-
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Bacterial
Antibiotic
|
Infection
Inflammation/Immunology
|
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Chlamydia pneumoniae-IN-1 (compound 55), a benzimidazole, shows high activity against the bacterium. Chlamydia pneumoniae-IN-1 has 99% inhibition of C. pneumoniae Growth at 10 μM, and has 95% inhibition effect on the viability of the host cells at 10 μM. Chlamydia pneumoniae-IN-1 inhibits the growth of the CV-6 strain with a MIC of 12.6 μM. Chlamydia pneumoniae-IN-1 has antichlamydial efficiency .
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-
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- HY-N2105
-
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L-Dicentrine
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Fungal
Bacterial
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Infection
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(-)-Dicentrine is an aporphine alkaloid that can be isolated from the stem bark of Talauma arcabucoana. (-)-Dicentrine shows moderate growth inhibition against Staphylococcus aureus and
Candida albicans .
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- HY-150308
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PPAR
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Cancer
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SR10221, a noncovalent inverse agonist of PPARγ, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines .
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- HY-W506116
-
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Ostruthine
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Bacterial
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Infection
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Ostruthin (Ostruthine) is an antimycobacterial coumarin, that can be isolated from the roots of Peucedanum ostruthium. Ostruthin causes a marked inhibition of the growth of gram-positive micro-organisms .
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- HY-W021040R
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Fungal
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Infection
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Fludioxonil (Standard) is the analytical standard of Fludioxonil. This product is intended for research and analytical applications. Fludioxonil, a phenylpyrrole fungicide, has a strong inhibition on mycelia growth of S. sclerotiorum .
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- HY-W017401R
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Others
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Infection
Cancer
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Benzisothiazolone (Standard) is the analytical standard of Benzisothiazolone. This product is intended for research and analytical applications. Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibiting activity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
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-
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- HY-119737
-
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Acetolactate Synthase (ALS)
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Metabolic Disease
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Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase .
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- HY-P99590
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ACE-011
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TGF-β Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
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- HY-N10269
-
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Fungal
Endogenous Metabolite
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Infection
|
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Phomalactone, produced by the fungus Nigrospora sphaerica, specifically inhibits the mycelial growth of Phytophthora infestans, with an MIC value of 2.5 mg/L . Phomalactone is phytotoxic to Z. elegans and other plant species by inhibition of seedling growth and by causing electrolyte leakage from photosynthetic tissues of both Z. elegans leaves and cucumber cotyledons .
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- HY-120187
-
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Others
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Others
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DDCPPB-Glu (compound 3a) is a compound with anti-tumor activity, which has the activity of inhibiting tumor cell growth and prolonging survival. DDCPPB-Glu has growth inhibition effect on various tumor cell lines, can increase the survival time of leukemia mice, and has inhibitory effect on tumors such as colon cancer and lung cancer.
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- HY-W335972
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Phosphatase
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Others
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N-Lauryldiethanolamine is an antistatic agent with a strong inhibitory effect on cell growth at 30 µM, showing some lysosomotropic behavior. N-Lauryldiethanolamine is toxic at a concentration of ≥ 10 µM in the osteogenesis inhibition assay 。
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- HY-13603
-
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EPC2407
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Microtubule/Tubulin
Apoptosis
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Cardiovascular Disease
Cancer
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Crolibulin (EPC2407) is a tubulin polymerization inhibitor, with potent apoptosis induction and cell growth inhibition. Crolibulin has anti-tumor activity. Crolibulin also has cardiovascular toxicity and neurotoxicity .
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- HY-114228
-
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PROTACs
Epigenetic Reader Domain
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Cancer
|
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PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
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- HY-N3001
-
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STAT
VEGFR
Bcl-2 Family
Survivin
IAP
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Cancer
|
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Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells . Isolinderalactone suppresses the expression of B-cell lymphoma 2 (Bcl-2), survi
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- HY-122984
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Others
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Others
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Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test .
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- HY-135599
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Others
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Infection
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Lysine hydroxamate is an amino acid hydroxamate that inhibits the growth of Escherichia coli K-12. Of the other amino acid hydroxamates tested, only L-lysine hydroxamate reduced the growth rate. The inhibition of growth by L-serine hydroxamate could be rapidly reversed by adding L-serine to the bacterial culture or by removing the analog by filtration. This reversal was specific for L-serine. L-alanine, glycine, or adenine had no effect on the inhibited culture. There was no evidence for active transport of the analog.
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- HY-115908
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CDK
Apoptosis
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Cancer
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ZDLD13, a β-carboline, is an orally active and selective CDK4/CycD3 inhibitor with an IC50 value of 0.38 μM. ZDLD13 exhibits potent anti-HCT116 activity including inhibition of colony formation, inhibition of invasion and migration, inducing of apoptosis, and arresting of G1 phase in cell cycle. ZDLD13 shows significant tumor growth inhibition in HCT116 tumor xenograft model .
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- HY-162337
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Protoporphyrinogen IX oxidase
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Others
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PPO-IN-8 (Compound D4) is a phenyltriazolinone PPO inhibitor with an IC50 of 33 μg/L. PPO-IN-8 is a herbicide with a wide herbicidal spectrum and has good growth inhibition effect on dicotyledonous weeds .
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- HY-W414724R
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Others
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Others
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Methabenzthiazuron (Standard) is the analytical standard of Methabenzthiazuron. This product is intended for research and analytical applications. Methabenzthiazuron is a herbicide, which inhibits the plants' growth through inhibition of photosynthesis. Methabenzthiazuron can be used for weed control in cereal crops .
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- HY-168147
-
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Phosphodiesterase (PDE)
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Cancer
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Enpp-1-IN-24 (compund 7) is an ENPP1 inhibitor that, in combination with anti-PD-1 antibodies, achieves 77.7% tumor growth inhibition and improves survival in mouse models .
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- HY-13007
-
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PF-03758309
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PAK
Apoptosis
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Cancer
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PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
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- HY-13007B
-
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PF-03758309 dihydrochloride
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PAK
Apoptosis
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Cancer
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PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
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- HY-13007A
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PF-03758309 hydrochloride
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PAK
Apoptosis
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Cancer
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PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
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- HY-18634
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ZMC1
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MDM-2/p53
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Cancer
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NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
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- HY-154362A
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Others
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Cancer
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β-D-Ribofuranose, 3-deoxy-3-fluoro-, 1,2-diacetate 5-(4-methylbenzoate) (compound 25) displays potent tumor cell growth inhibition activity .
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- HY-N1513
-
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AP-1
NF-κB
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Cancer
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Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling .
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- HY-108431
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Apoptosis
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Cancer
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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 .
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- HY-116506
-
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RAR/RXR
Reactive Oxygen Species
Apoptosis
Autophagy
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Cancer
|
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Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation .
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- HY-161515
-
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NAMPT
Epigenetic Reader Domain
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Cancer
|
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BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
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- HY-10949
-
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E1/E2/E3 Enzyme
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Cancer
|
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SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF) Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF Met30 .
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-
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- HY-135549
-
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Fungal
Antibiotic
|
Infection
|
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Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species .
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- HY-151931
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Jasmonyl-ACC
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Others
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Metabolic Disease
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JA-ACC (Jasmonyl-ACC) is a derivative of 1-aminocyclopropane-1-carboxylic acid (ACC). ACC is the direct precursor of the plant hormone ethylene. JA-ACC inhibits root growth in Arabidopsis and the inhibition is independent of jasmonic acid (JA) signaling .
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- HY-P99818
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ACE-031
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TGF-β Receptor
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Metabolic Disease
|
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Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy .
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- HY-155047
-
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Bacterial
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Infection
|
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BDM91514 improves antibiotic potency through AcrB inhibition. BDM91514 prevents the growth of E. coliBW25113 (EC90: 8 μM) in the presence of 8 μg/mL Pyridomycin. BDM91514 has suitable plasma and microsomal stability .
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- HY-118528
-
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TGF-β Receptor
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Cancer
|
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TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells .
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- HY-155376
-
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mTOR
|
Cancer
|
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mTOR inhibitor-14 (compound 14c) is a potent mTOR inhibitor. mTOR inhibitor-14 also shows minimal CYP2C8 inhibition. mTOR inhibitor-14 can inhibit tumor growth .
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- HY-101571A
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-
- HY-16399
-
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Apoptosis
SF3B1
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Cancer
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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 .
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- HY-B1735
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Prostaglandin Receptor
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Cardiovascular Disease
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Picotamide is a combined inhibitor of thromboxane A2 (TxA2) synthase and receptor. Picotamide has antiplatelet activity. Picotamide promotes the reduction of microalbuminuria and the inhibition of growth of carotid plaques in diabetes. Picotamide can be used for researching acute or chronic cardiovascular diseases .
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- HY-P3156
-
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Fungal
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Infection
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Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
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- HY-119737R
-
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Acetolactate Synthase (ALS)
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Metabolic Disease
|
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Chlorsulfuron (Standard) is the analytical standard of Chlorsulfuron. This product is intended for research and analytical applications. Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase .
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- HY-118269
-
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c-Met/HGFR
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Cancer
|
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OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .
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- HY-120044
-
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Farnesyl Transferase
Ras
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Cancer
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L-739749 is a farnesyl transferase inhibitor. L-739749 inhibits the selective hypersensitivity of JMML cells to granulocyte-macrophage colony-stimulating factor (GM-CSF) by blocking the prenylation of Ras. L-739749 exhibits a strong inhibitory effect on the growth of primary human JMML cells in vitro .
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- HY-162471
-
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Others
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Cancer
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GSK_WRN3 is a selective inhibitor of WRN protease (IC50 = 8.6 μM). GSK_WRN3 displays a high degree of selectivity by forming a covalent binding to the Cys727 residue of the WRN protein. GSK_WRN3 reduces growth support for MSI tumor cells by inhibiting WRN protease activity, resulting in increased DNA double-strand breaks and cell growth inhibition .
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- HY-14375
-
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NAMPT
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Cancer
|
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CB 300919 is a quinazoline-based antitumour agent with high activity in the CH1 human ovarian tumour xenograft. CB 300919 has a continuous exposure (96 h) growth inhibition IC50 value of 2 nM in human CH1 ovarian tumor xenograft .
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- HY-108530
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RAR/RXR
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Cancer
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MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
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- HY-46568
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CDK
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Cancer
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CDK7/12-IN-1 is a selective CDK7/12 inhibitor with IC50s of 3 and 277 nM for CDK7 and CDK 12, respectively. CDK7 and CDK12 inhibition is an effective strategy to inhibit tumour growth .
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- HY-156566
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-B0133
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Pimaricin
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Fungal
Endogenous Metabolite
Antibiotic
Bacterial
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Infection
|
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Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
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- HY-113542
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(+)-Blasticidin A
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Bacterial
Antibiotic
Parasite
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Infection
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Blasticidin A ((+)-Blasticidin A) is an inhibitor of Aflatoxin production by Aspergillus parasiticus. Blasticidin A almost completely inhibits Aflatoxin production at 0.5 μM . Blasticidin A is a potent antibiotic produced by Streptomyces, inhibits Aflatoxin production without strong growth inhibition toward Aflatoxin-producing fungi .
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- HY-P99192
-
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LY2875358
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c-Met/HGFR
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Cancer
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Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer .
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- HY-113679
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Telomerase
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Metabolic Disease
Endocrinology
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Ceramides Mixture is an endogenous ceramide and consists of hydroxy and non-hydroxy fatty acid-containing ceramides. Ceramides Mixture is a main lipid component of the permeability barrier in epidermis. Ceramides Mixture is involved in the regulation of growth inhibition, cell cycle arrest, and modulation of telomerase activity .
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- HY-118061
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Others
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Infection
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VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
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- HY-N0282
-
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Microtubule/Tubulin
Apoptosis
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Inflammation/Immunology
Cancer
|
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Demecolcine is a potent mitotic inhibitor with an IC50 value of 2.4 μM for inhibition of tubulin polymerization. Colcemid (Demecolcine) can interact with tubulin dimers to induce anti-mitotic action and inhibit microtubule growth. Colcemid (Demecolcine) can be used for inflammatory disorders and cancer research .
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- HY-139664
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DNA Methyltransferase
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Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-100653
-
AZD5153
1 Publications Verification
|
Others
|
Cancer
|
|
AZD5153 (Compound 13) is a trivalent triazolpyrazine bromide domain (BRD), bromodomain and
extraterminal (BET) inhibitor. AZD5153 has down-regulated c-Myc gene and tumor growth inhibition activity. AZD5153 can be used in the study of BET small molecule inhibitors .
|
-
- HY-130326
-
|
Ru(η6-p-cymene)Cl2(pta)
|
Apoptosis
Caspase
|
Cardiovascular Disease
Cancer
|
|
RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model .
|
-
- HY-129510
-
|
|
EGFR
|
Cancer
|
|
4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-133680
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-P99215
-
|
Anti-EGFL7; RG 7414
|
VEGFR
|
Cancer
|
|
Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition .
|
-
- HY-155362
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-56 (compound 8l), an indazole derivative, is a potent tubulin polymerization inhibitor through interacting with the colchicine site, resulting in cell cycle arrest and cellular apoptosis. polymerization-IN-56 reduces cell migration and leads to more potent inhibition of tumor growth in vivo .
|
-
- HY-N0781
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-N4285
-
-
- HY-122984S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Diquat-d4 (dibromide)is the deuterium labeledDiquat (dibromide)(HY-122984) . Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test .
|
-
- HY-157029S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-157031S
-
|
|
Ras
|
Cancer
|
|
KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
|
-
- HY-18959
-
|
|
β-catenin
Wnt
|
Cancer
|
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs) .
|
-
- HY-144127
-
|
|
Androgen Receptor
|
Cancer
|
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
|
-
- HY-146806
-
|
|
MDM-2/p53
|
Cancer
|
|
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition .
|
-
- HY-20808
-
|
|
COX
|
Cancer
|
|
Antioxidant agent-15 (Compound 4) is a potent antioxidant inhibition activity, with the IC50 of 15.44 nM. Antioxidant agent-15 inhibits tumor cell growth in Hela, Hep G2 and Caco-2 cells, with the IC50 of 395.26, 400.4 and 24.6 nM, respectively .
|
-
- HY-122984R
-
|
|
Others
|
Others
|
|
Diquat (dibromide) (Standard) is the analytical standard of Diquat (dibromide). This product is intended for research and analytical applications. Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test .
|
-
- HY-120599A
-
|
VERU-111 hydrochloride; ABI-231 hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
Sabizabulin hydrochloride is a potent orally bioavailable microtubule inhibitor with activity that interacts with the colchicine binding site. Sabizabulin hydrochloride demonstrated significant inhibition of melanoma tumor growth with an average IC50 of 5.2 nM in melanoma and prostate cancer cell lines. Pharmacological screening of Sabizabulin hydrochloride shows it has a low risk of potential side effects .
|
-
- HY-150562
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-12954
-
|
NCH-51
|
HDAC
HIV
|
Infection
Cancer
|
|
PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 μM) .
|
-
- HY-136477
-
|
PGV-1
|
Apoptosis
COX
VEGFR
NF-κB
|
Cancer
|
|
Pentagamavunon-1 (PGV-1), a Curcumin analog with oral activity, targets on several molecular mechanisms to induce apoptosis including inhibition of angiogenic factors cyclooxygenase-2 (COX-2) and vascular endothelial growth factor (VEGF). PGV-1 inhibits NF-κB activation .
|
-
- HY-156568A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 TFA is a selective degrader of SMARCA2. SMD-3040 TFA contains SMARCA2/4 ligands, linker and VHL ligands and can be used for PROTAC drug synthesis. SMD-3040 TFA exhibits strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-124022
-
|
|
HDAC
|
Others
|
|
APHA Compound 8 (Compound 4) is a histone deacetylase (HDAC) inhibitor. APHA Compound 8 has antimouse HDAC1 activity with an IC50 value of 0.78 μM. APHA Compound 8, as antiproliferative and cytodifferentiating agent on MEL cells, shows dose-dependent growth inhibition and hemoglobin accumulation effects .
|
-
- HY-163533
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .
|
-
- HY-17406
-
|
Ro 40-7592
|
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
|
Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
|
-
- HY-124069
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
M-525 is a first-in-class, highly potent, irreversible and covalent menin-MLL protein-protein interaction inhibitor. M-525 binds to menin with an IC50 of 3 nM and achieves low nanomolar potencies in cell growth inhibition and in suppression of MLL regulated gene expression in MLL leukemia cells. Anti-leukemia activity .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-100549
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
(S)-Crizotinib is a potent and selective MTH1 (mutT homologue) inhibitor with an IC50 of 330 nM. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition, induces an increase in DNA single strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumour growth in animal models .
|
-
- HY-135111
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-14389
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
|
-
- HY-149292
-
|
|
Casein Kinase
|
Cancer
|
|
SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
|
-
- HY-112293
-
|
|
EGFR
|
Cancer
|
|
GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
|
-
- HY-135549R
-
|
|
Fungal
Antibiotic
|
Infection
|
|
Fluxapyroxad (Standard) is the analytical standard of Fluxapyroxad. This product is intended for research and analytical applications. Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species .
|
-
- HY-119213
-
|
|
Influenza Virus
|
Infection
|
|
BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth, and also exhibits inhibitory activity against some subtypes of influenza viruses. BMY-27709 acts early in the course of H1 and H2 virus infections, and exhibits antiviral activity through inhibition of hemagglutinin proteins. However, BMY-27709 has no effect on H3 subtype viruses and influenza B/Lee/40 viruses .
|
-
- HY-119618
-
|
|
Endogenous Metabolite
|
Cancer
|
|
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
|
-
- HY-B2049
-
|
|
Others
|
Infection
|
|
Triflumuron is a potent chitin synthesis inhibitor. Triflumuron shows the efficacy in emergence inhibition (EI) against Culex quinquefasciatus and Aedes albopictus, with EI50 values of 5.28 and 1.59 μg/L, respectively. Triflumuron can be used as an insecticide. Triflumuron represents a potential tool for the control of disease vectors in public health .
|
-
- HY-B2049R
-
|
|
Others
|
Infection
|
|
Triflumuron (Standard) is the analytical standard of Triflumuron. This product is intended for research and analytical applications. Triflumuron is a potent chitin synthesis inhibitor. Triflumuron shows the efficacy in emergence inhibition (EI) against Culex quinquefasciatus and Aedes albopictus, with EI50 values of 5.28 and 1.59 μg/L, respectively. Triflumuron can be used as an insecticide. Triflumuron represents a potential tool for the control of disease vectors in public health .
|
-
- HY-B0113S
-
|
H 16868-d3
|
Proton Pump
Bacterial
Autophagy
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
|
-
- HY-N0284
-
|
|
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .
|
-
- HY-145572
-
|
LY-3484356
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-113068
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
(rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-152225
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction .
|
-
- HY-145572A
-
|
LY-3484356 tosylate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-149985
-
|
|
Parasite
|
Infection
|
|
Antitrypanosomal agent 12 is a C20-phenylthiourea with trypanocidal and cytotoxic activities. Antitrypanosomal agent 12 shows antitrypanosomal activity with 50% growth inhibition (GI50) values of 0.22 μM. Antitrypanosomal agent 12 induces faster cell swelling in bloodstream-form trypanosomes than Salinomycin (HY-15597) .
|
-
- HY-163352
-
|
|
Others
|
Infection
|
|
Chitinase-IN-6 (Compound 4h) is a potent dual-Chitinase inhibitor, with Ki values of 1.82 and 2.00 μM against OfChtI and OfChi-h, respectively. Chitinase-IN-6 exhibits certain growth inhibition effects against Ostrinia furnacalis. Chitinase-IN-6 is a potential novel insecticide candidate friendly to nontarget organisms .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-118175
-
|
|
Others
|
Others
|
|
RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
|
-
- HY-167679
-
|
|
Others
|
Inflammation/Immunology
|
|
Scio-323 is an orally available p38 mitogen-activated protein kinase (MAPK) inhibitor with the potential to inhibit chronic inflammatory responses associated with polyethylene particles. Scio-323's oral inhibition pattern had a minimal effect on bone formation. Scio-323 administration inhibited net bone formation after the establishment of a chronic inflammatory response to polyethylene particles. Osteoblast-like activity remained low in all cases of Scio-323 inhibition. Scio-323 failed to improve bone growth in the presence of polyethylene particles .
|
-
- HY-155356
-
|
|
PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
|
-
- HY-163483
-
|
|
Parasite
|
Others
|
|
ELQ-598, as a prodrug, is converted into the active drug ELQ-596 upon oral administration. ELQ-598 demonstrates potent parasitic growth inhibition capabilities (IC50= 37 nM). ELQ-598 also shows low toxicity towards human cells (IC50= 19 μM). ELQ-598 can be used for research into babesiosis .
|
-
- HY-17593
-
|
CEM-101; OP-1068
|
Bacterial
Antibiotic
|
Infection
|
|
Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
|
-
- HY-115519
-
|
|
Casein Kinase
|
Cancer
|
|
(E/Z)-GO289 is a potent and selective casein kinase 2 (CK2) inhibitor (IC50=7 nM). (E/Z)-GO289 strongly lengthens circadian period. (E/Z)-GO289 exhibits cell type–dependent inhibition of cancer cell growth that correlated with cellular clock function .
|
-
- HY-139664A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-146467
-
|
|
Others
|
Cancer
|
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition .
|
-
- HY-163272
-
|
|
Glutathione Peroxidase
CDK
|
Cancer
|
|
GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC50 values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo .
|
-
- HY-B0133R
-
|
|
Fungal
Endogenous Metabolite
Antibiotic
Bacterial
|
Infection
|
|
Natamycin (Standard) is the analytical standard of Natamycin. This product is intended for research and analytical applications. Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research .
|
-
- HY-124403
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-116138
-
|
|
Others
|
Others
|
|
RG-14467 is an epidermal growth factor receptor tyrosine kinase inhibitor with activity that inhibits enzyme activity. RG-14467 has similar inhibition kinetics to Lavendustin-A, with a dissociation constant of 3.4μM for the initial rapidly formed complex and an overall dissociation constant estimated to be less than or equal to 30nM, and is a partially competitive inhibitor for ATP.
|
-
- HY-B0220H
-
|
|
DNA/RNA Synthesis
Bacterial
Antibiotic
|
Infection
|
|
Erythromycin hydrochloride is a protein synthesis inhibitor with activity against the growth of both Gram-negative and Gram-positive bacteria. Erythromycin hydrochloride is commonly used in biomedicine to inhibit diseases caused by bacterial infections. Erythromycin hydrochloride is also involved in the inhibition of mammalian mRNA splicing. The application range of erythromycin hydrochloride includes respiratory tract infections, skin infections, and other infections caused by sensitive bacteria .
|
-
- HY-18723
-
|
|
Piezo Channel
Akt
ERK
Potassium Channel
|
Cardiovascular Disease
|
|
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca 2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation .
|
-
- HY-111747
-
|
|
Bacterial
|
Infection
Cardiovascular Disease
|
|
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .
|
-
- HY-145388
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-134911
-
|
|
IRAK
CDK
|
Inflammation/Immunology
Cancer
|
|
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity .
|
-
- HY-400685
-
|
|
Others
|
Cancer
|
|
SMD-3040 intermediate-2 is an intermediate in the synthesis of SMD-3040 (HY-156568). SMD-3040 contains SMARCA2/4 ligands, linker and VHL ligands and is a selective SMARCA2 degrader. MD-3040 can be used for ADC drug synthesis and has strong tumor growth inhibition in tumor xenograft models .
|
-
- HY-N0282R
-
|
|
Microtubule/Tubulin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Colcemid (Standard) is the analytical standard of Colcemid. This product is intended for research and analytical applications. Colcemid (Demecolcine) is a potent mitotic inhibitor with an IC50 value of 2.4 μM for inhibition of tubulin polymerization. Colcemid (Demecolcine) can interact with tubulin dimers to induce anti-mitotic action and inhibit microtubule growth. Colcemid (Demecolcine) can be used for inflammatory disorders and cancer research .
|
-
- HY-111193
-
|
3-Chloroprocainamide
|
NF-κB
Apoptosis
|
Cancer
|
|
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
|
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-N0781R
-
|
|
Apoptosis
|
Cancer
|
|
Linderalactone (Standard) is the analytical standard of Linderalactone. This product is intended for research and analytical applications. Linderalactone is an important sesquiterpene lactone isolated from Lindera aggregata. Linderalactone inhibits cancer growth by modulating the expression of apoptosis-related proteins and inhibition of JAK/STAT signalling pathway. Linderalactone also inhibits the proliferation of the lung cancer A-549 cells with an IC50 of 15 μM .
|
-
- HY-W052289
-
|
|
Others
|
Cancer
|
|
Methyl 6-bromo-1H-indole-3-carboxylate is a marine-derived natural product with antitumor activity. Methyl 6-bromo-1H-indole-3-carboxylate showed growth inhibition against Staphylococcus epidermidis, exhibiting weak or moderate minimum inhibitory concentrations (MICs) .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-163510
-
|
|
Androgen Receptor
|
Cancer
|
|
AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
|
-
- HY-129510R
-
|
|
EGFR
|
Cancer
|
|
4-Methyl erlotinib (Standard) is the analytical standard of 4-Methyl erlotinib. This product is intended for research and analytical applications. 4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
|
-
- HY-B0113
-
|
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-113068S
-
|
|
Isotope-Labeled Compounds
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol-d3 is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol can also prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
|
-
- HY-W014316
-
|
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol .
|
-
- HY-B0113A
-
|
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria . Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-103257
-
|
NSC656158
|
Microtubule/Tubulin
|
Cancer
|
|
CHM-1, a microtubule-destabilizing agent, inhibits tubulin polymerization. CHM-1 is a potent and selective antimitotic antitumor activity against human hepatocellular carcinoma. CHM-1 induces growth inhibition and apoptosis via G2-M phase arrest in human hepatocellular carcinoma cells by activation of Cdc2 kinase activity .
|
-
- HY-121333
-
|
|
Antibiotic
Wnt
β-catenin
|
Infection
Neurological Disease
Cancer
|
|
Dinactin, an antibiotic ionophore produced by Streptomyces species, as an effective small molecule targeting Wnt/β-catenin signaling pathway in cancer cells. Dinactin shows marked inhibition of HCT-116 cell growth with an IC50 of 1.1 µM. Dinactin shows anti-proliferative activity against the cancer cells in apoptosis-independent manner. Dinactin is also an effective agent for the research of neuropathic pain .
|
-
- HY-156568
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM). SMD-3040 contains SMARCA2/4 ligand, linker and VHL ligand. SMD-3040 demonstrates excellent degradation selectivity for SMARCA2 protein over SMARCA4 protein.SMD-3040 achieves strong tumor growth inhibition in xenograft models .
|
-
- HY-W422288
-
|
(Rac)-Ketoconazol; (Rac)-R 41400
|
Fungal
Cytochrome P450
|
Infection
|
|
(Rac)-Ketoconazole ((Rac)-R 41400) is an antifungal imidazole compound with oral activity. (Rac)-Ketoconazole interferes with ergosterol synthesis by inhibiting cytochrome P450-dependent 14α-sterol demethylase (CYP51), a key enzyme on the fungal cell membrane, leading to membrane dysfunction and ultimately inhibition of fungal growth and reproduction. (Rac)-Ketoconazole is indicated for studies of fungal infections .
|
-
- HY-133680S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
β-Tocopherol-d4 is a deuterium labeled β-Tocopherol (HY-133680). β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-50878
-
Crizotinib
Maximum Cited Publications
66 Publications Verification
PF-02341066
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-17406S1
-
|
Ro 40-7592-d4
|
Isotope-Labeled Compounds
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
|
Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
|
-
- HY-144271
-
|
|
Raf
|
Cancer
|
|
RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-147187
-
|
|
STAT
Apoptosis
Bcl-2 Family
Survivin
|
Cancer
|
|
MNK8 is a potent STAT3 (signal transducer and activator of transcription 3) inhibitor. MNK8 inhibits STAT3 activation and reduced its DNA binding ability. MNK8 shows good growth inhibition against hepatocellular carcinoma (HCC) cells. MNK8 induces apoptosis in HCC cells. MNK8 reduces prosurvival proteins expression and migration/invasion of HCC cells .
|
-
- HY-139664B
-
|
|
Others
|
Cancer
|
|
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-50878B
-
|
PF-02341066 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
c-Met/HGFR
|
Cancer
|
|
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
|
-
- HY-121152
-
-
- HY-17406R
-
|
Ro 40-7592 (Standard)
|
COMT
Amyloid-β
Apoptosis
|
Neurological Disease
Cancer
|
|
Tolcapone (Standard) is the analytical standard of Tolcapone. This product is intended for research and analytical applications. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver . Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis . Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma .
|
-
- HY-133680R
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol (Standard) is the analytical standard of β-Tocopherol. This product is intended for research and analytical applications. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-B0067B
-
|
(R)-SM-5887
|
Others
|
Cancer
|
|
(R)-Amrubicin ((R)-SM-5887) is an anthracycline that effectively treats lung cancer by intercalating into DNA and inhibiting topoisomerase II activity, which consequently hampers DNA replication as well as RNA and protein synthesis, leading to cell growth inhibition and apoptosis. This compound exhibits superior anti-tumor efficacy compared to traditional anthracycline drugs while lacking the cumulative cardiac toxicity typically associated with this drug class.
|
-
- HY-119726
-
|
APX001; E1211
|
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Fosmanogepix (APX001) is a broad-spectrum agent against invasive fungal infections. Fosmanogepix (APX001) targets the conserved Gwt1 enzyme required for the localization of glycosylphosphatidylinositol-anchored mannoproteins in fungi. This inhibition prevents the appropriate localization of cell wall mannoproteins, which compromises cell wall integrity, biofilm formation, germ tube formation, and fungal growth. Fosmanogepix (APX001) can be used for invasive fungal infections research .
|
-
- HY-109583
-
|
4-Oxo-4-HPR
|
Apoptosis
Reactive Oxygen Species
Drug Metabolite
|
Cancer
|
|
4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
|
-
- HY-163125
-
|
|
VEGFR
|
Cancer
|
|
BHEPN is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). BHEPN has inhibition of VEGFR-2 with an IC50 value of 0.320 μM. BHEPN also exhibits remarkable cytotoxic effects against HepG2 and MCF-7 cancer cell lines, with IC50 values of 0.19 μM and 1.18 μM, respectively. BHEPN can be used for anticancer research .
|
-
- HY-N0284R
-
|
|
PI3K
Akt
|
Inflammation/Immunology
Cancer
|
|
Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .
|
-
- HY-12708
-
|
|
Dopamine Receptor
Cytochrome P450
Autophagy
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
|
-
- HY-B0407A
-
|
|
Dopamine Receptor
Autophagy
Cytochrome P450
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis .
|
-
- HY-145864
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC50 of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI50=1.6 µM). VEGFR-2-IN-12 has antitumor activity .
|
-
- HY-17593R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Solithromycin (Standard) is the analytical standard of Solithromycin. This product is intended for research and analytical applications. Solithromycin (CEM-101) is an orally bioavailable, effective antimicrobial agent, with IC50s for inhibition of cell viability, protein synthesis, and growth rate are 7.5 ng/mL, 40 ng/mL, and 125 ng/mL for Streptococcus pneumonia, Staphylococcus aureus, and Haemophilus influenzae, respectively. Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis .
|
-
- HY-122324
-
|
(+)-(S)-Tylophorine; DCB-3500; NSC-717335
|
Others
|
Cancer
|
|
Tylophorine and its analogs are benzoindole alkaloids, most of which are derived from Garcinia plants. Tylophorine analogs all show potent growth inhibition against human hepatocellular carcinoma HepG2 and human nasopharyngeal carcinoma KB cell lines. Tylophorine analogs can also induce increased albumin expression and inhibit α-fetoprotein expression in HepG2 cells, and have the potential to induce HepG2 cell differentiation .
|
-
- HY-119726A
-
|
APX001 (tautomerism); E1211 (tautomerism)
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Fosmanogepix tautomerism (APX001 tautomerism) is a broad-spectrum and orally active anti-invasive fungal compound. Fosmanogepix tautomerism targets the conserved Gwt1 enzyme required for the localization of glycosylphosphatidylinositol-anchored mannoproteins in fungi, and inhibition prevents proper localization of cell wall mannoproteins, thereby impairing cell wall integrity, biofilm formation, germ tube formation, and fungal growth. Fosmanogepix tautomerism can be used to study invasive fungal infections .
|
-
- HY-117247
-
|
|
DNA/RNA Synthesis
|
Infection
|
|
5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitory activity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .
|
-
- HY-15186
-
|
GDC-0068; RG7440
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-50878S
-
|
PF-02341066-d5
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-115446A
-
|
Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively .
|
-
- HY-N2484
-
|
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-151374
-
|
|
PKD
|
Cancer
|
|
3-IN-PP1 is a protein kinase D (PKD) inhibitor. 3-IN-PP1 has potent pan-PKD inhibitory activity for PKD1, PKD2 and PKD3 with IC50 values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer .
|
-
- HY-148443
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-9 (compound 57) is a silvestrol (HY-13251) analogue. eIF4A3-IN-9 interferes the assembling of eIF4F translation complex with EC50s of 29, 450 and 80 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-9 can be used for the research of human cancer pathogenesis .
|
-
- HY-148444
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-10 (compound 58) is a silvestrol (HY-13251) analogue. eIF4A3-IN-10 interferes the assembling of eIF4F translation complex with EC50s of 35 and 100 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-10 can be used for the research of human cancer pathogenesis .
|
-
- HY-148446
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-12 (compound 62) is a silvestrol (HY-13251) analogue. eIF4A3-IN-12 interferes the assembling of eIF4F translation complex with EC50s of 4, 70 and 5 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-12 can be used for the research of human cancer pathogenesis .
|
-
- HY-148448
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-14 (compound 51) is a silvestrol (HY-13251) analogue. eIF4A3-IN-14 interferes the assembling of eIF4F translation complex with EC50s of 40 and 50 nM for myc-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-14 can be used for the research of human cancer pathogenesis .
|
-
- HY-148449
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-15 (compound 52) is a silvestrol (HY-13251) analogue. eIF4A3-IN-15 interferes the assembling of eIF4F translation complex with EC50s of 11, 700 and 120 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-15 can be used for the research of human cancer pathogenesis .
|
-
- HY-148450
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-16 (compound 60) is a silvestrol (HY-13251) analogue. eIF4A3-IN-16 interferes the assembling of eIF4F translation complex with EC50s of 1, 30 and 1 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-16 can be used for the research of human cancer pathogenesis .
|
-
- HY-B0113R
-
|
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole (Standard) is the analytical standard of Omeprazole. This product is intended for research and analytical applications. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-161629
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
|
-
- HY-114211
-
|
|
Histone Methyltransferase
HSP
|
Cancer
|
|
SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity .
|
-
- HY-113068R
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
(rel)-β-Tocopherol (Standard) is the analytical standard of (rel)-β-Tocopherol. This product is intended for research and analytical applications. (rel)-β-Tocopherol is a relative configuration of β-Tocopherol.(±)-β-Tocopherol is a lipid-soluble form of vitamin E with antioxidant activity. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
|
-
- HY-113843
-
|
|
Others
|
Cancer
|
|
RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
|
-
- HY-135111R
-
|
|
Drug Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
4-Desmethoxy Omeprazole (Standard) is the analytical standard of 4-Desmethoxy Omeprazole. This product is intended for research and analytical applications. 4-Desmethoxy Omeprazole is the active metabolite of Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .
|
-
- HY-15186C
-
|
GDC-0068 tosylate; RG7440 tosylate
|
Organoid
Akt
Apoptosis
|
Cancer
|
|
Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
|
-
- HY-117807
-
|
|
Ras
|
Cancer
|
|
A-176120 is a potent inhibitor of farnesyltransferase, crucial for Ras protein farnesylation in cancer cells. It exhibits high selectivity for farnesyltransferase (IC50 1.2 ± 0.3 nM) over related enzymes like geranylgeranyltransferases and squalene synthase. Inhibition of Ras processing in H-ras and K-ras mutated cells demonstrates its efficacy in blocking Ras-mediated signaling. A-176120 shows anti-angiogenic effects by inhibiting vascular endothelial growth factor (VEGF) secretion and disrupting capillary formation in endothelial cells. In vivo studies reveal its ability to reduce tumor growth in Ras-transformed cells and enhance survival in animal models. These findings highlight A-176120 as a promising FPP analogue with potent anti-tumor and anti-angiogenic properties .
|
-
- HY-50878A
-
|
PF-02341066 hydrochloride
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-B0113S1
-
|
H 16868-d3-1
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-124653
-
|
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition .
|
-
- HY-10002A
-
|
1α,25-Dihydroxy-3-epi-vitamin-D3
|
VD/VDR
|
Others
|
|
(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3) is a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3). (1S)-Calcitriol exhibits potent vitamin D receptor (VDR)-mediated actions such as inhibition of keratinocyte growth or suppression of parathyroid hormone secretion .
|
-
- HY-144269
-
|
|
Raf
|
Cancer
|
|
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
|
-
- HY-148333
-
MS177
1 Publications Verification
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MS177 is an effective and fast-acting EZH2 degrader. MS177 is a PROTAC that consists of a CRBN ligand, linker, and a potent enzymatic EZH2 inhibitor C24 (C24 IC50): 12?nM). MS177 effectively depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. MS177 induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest .
|
-
- HY-148445
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-11 (compound 56) is a silvestrol (HY-13251) analogue. eIF4A3-IN-11 interferes the assembling of eIF4F translation complex with EC50s of 0.2, 4 and 0.3 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-11 can be used for the research of human cancer pathogenesis .
|
-
- HY-148447
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-13 (compound 75) is a silvestrol (HY-13251) analogue. eIF4A3-IN-13 interferes the assembling of eIF4F translation complex with EC50s of 0.6, 15 and 0.4 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-13 can be used for the research of human cancer pathogenesis .
|
-
- HY-148451
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-17 (compound 61) is a silvestrol (HY-13251) analogue. eIF4A3-IN-17 interferes the assembling of eIF4F translation complex with EC50s of 0.9, 15 and 1.8 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-17 can be used for the research of human cancer pathogenesis .
|
-
- HY-N6948S
-
|
|
Isotope-Labeled Compounds
|
Inflammation/Immunology
|
|
Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-B0113S4
-
|
H 16868-d3 sodium
|
Autophagy
Phospholipase
Proton Pump
Bacterial
Isotope-Labeled Compounds
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
|
-
- HY-50878R
-
|
|
Anaplastic lymphoma kinase (ALK)
c-Met/HGFR
ROS Kinase
Autophagy
|
Cancer
|
|
Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
|
-
- HY-161630
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
|
-
- HY-160708
-
|
|
Tie
|
Cancer
|
|
Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC50=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis .
|
-
- HY-161631
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
|
-
- HY-106963
-
|
LGD1550
|
RAR/RXR
|
Cancer
|
|
ALRT1550 (LGD1550) is a selective retinoic acid receptor (RAR) agonist that binds RARs with exceptional potency, with Kd values of approximately 1-4 nM. ALRT1550 exhibits anti-proliferative activity, with an IC50 value of 0.22 nM in UMSCC-22B squamous carcinoma cells. In a mouse tumor xenograft model, ALRT1550 inhibited tumor growth in a dose-dependent manner, achieving a maximum inhibition rate of 89%. ALRT1550 is applicable for research in the field of cancer .
|
-
- HY-130207
-
|
NSC-743380
|
Endogenous Metabolite
|
Cancer
|
|
Oncrasin-72 (NSC-743380) is an RNA polymerase II inhibitor with activity in inhibiting growth and inducing cell death in human cancer cells. Oncrasin-72 exhibits antitumor activity through JNK activation and STAT3 inhibition. Analytical method development and validation for Oncrasin-72 is essential for quantifying its concentration in biological fluids for pharmacokinetic studies. This method was able to successfully quantify Oncrasin-72 in different dose groups when applied in rat plasma .
|
-
- HY-B0996
-
|
NSC-17764
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
|
Hexetidine (NSC-17764) is an orally active antibacterial and antifungal agent with broad antibacterial and antifungal activity. Hexetidine combined with IPBC potentiates strong fungal growth inhibition properties. Hexetidine at concentrations greater than 0.1% can cause oral ulceration. Additionally, Hexetidine improves its plaque inhibiting activities combined with zinc and has been confirmed the effectiveness on purulent wound along with ultrasound. Hexetidine is a promising candidate for research in fungus-related diseases and soft tissue purulent-inflammatory
|
-
- HY-B0113S3
-
|
H 16868-13C,d3
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Infection
Metabolic Disease
Cancer
|
|
Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
|
-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-143487
-
|
|
Parasite
|
Infection
|
|
Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli .
|
-
- HY-13265
-
AR-42
2 Publications Verification
HDAC-42; OSU-HDAC42
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
|
-
- HY-124843
-
|
CLT-005
|
STAT
Apoptosis
|
Cancer
|
|
LLL3 (CLT-005) is a STAT3 inhibitor. LLL3 inhibits dimerization and phosphorylation of STAT3, thereby preventing intraconuclear transfer of STAT3 and inhibits the expression of STAT3 dependent genes, which encode proteins such as Bcl-xL and cyclin D1. In addition, LLL3 can induce cell growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells via the caspase pathway. LLL3 can be used in the study of STAT3 persistent activation types of cancer .
|
-
- HY-B0764B
-
|
Dibutyryl cAMP; DBcAMP
|
PKA
|
Neurological Disease
|
|
Bucladesine (DBcAMP) is a membrane permeable selective activator that activates cyclic adenosine phosphate dependent protein kinase A (PKA). The main regulatory mechanism of Bucladesine involves the cAMP/PKA signaling pathway. When Bucladesine activates PKA, it can promote a variety of cellular processes, including neurodevelopment, growth and plasticity. In particular, the cAMP/PKA signaling pathway plays a key role in the expression of long-term enhancement (LTP) and long-term inhibition (LTD), as well as in the formation of long-term memory in the hippocampus. Bucladesine can be used to study memory formation and neuroplasticity .
|
-
- HY-118792
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AHR activator 1 is an aryl hydrocarbon receptor activator with activity regulating fibroblast growth factor-2 (FGF2)-induced branching morphogenesis. AHR activator 1 prevents the formation of cellular branches by inhibiting AHR signaling. AHR activator 1 also associates with adhesion of dissociated linkers, suggesting the importance of dissociated linkers in the inhibition of branching by AHR agonists. Studies of AHR activator 1 reveal its functional role in mammary gland morphogenesis and play a role in inhibiting FGF-induced invasion .
|
-
- HY-118843
-
|
|
Potassium Channel
|
Infection
|
|
Lombazole is an antimicrobial compound with activity that inhibits cell membrane synthesis. Lombazole had little effect on K+ permeability in S. aureus. Lombazole inhibited only de novo synthesis of cell enclosure in S. aureus, and this effect occurred before growth was affected. The main effect of lombazole was through inhibition of lipid synthesis. Lombazole may have an effect on key steps in lipid biosynthesis, as inferred from the lack of changes in lipid patterns after treatment. Lombazole also inhibited the sterol C-14 demethylation step in Candida albicans .
|
-
- HY-164689
-
|
|
Others
|
Cancer
|
|
Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-158230
-
|
|
Topoisomerase
|
Cancer
|
|
SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells .
|
-
- HY-162873
-
|
|
MEK
Raf
|
Cancer
|
|
MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer .
|
-
- HY-167938
-
|
(E/Z)-CGC-11047
|
Others
|
Cancer
|
|
(E/Z)-PG-11047 ((E/Z)-CGC-11047) is a polyamine analog with potential application in lung cancer inhibition. (E/Z)-PG-11047 effectively inhibited the growth of non-small cell and small cell lung cancer cells. (E/Z)-PG-11047 exhibits significant biochemical effects in non-small cell lung cancer cells, resulting in significant downregulation of polyamine synthetase activity. (E/Z)-PG-11047 induces polyamine metabolism, resulting in a significant reduction in polyamine levels .
|
-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
|
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
|
-
- HY-158138
-
|
|
PARP
Topoisomerase
Apoptosis
|
Cancer
|
|
TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
|
-
- HY-50878AS
-
|
PF-02341066-d9 hydrochloride
|
c-Met/HGFR
Autophagy
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Isotope-Labeled Compounds
|
Cancer
|
|
Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
|
-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Others
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
|
-
- HY-107738
-
|
Z/E-Guggulsterone
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
Cancer
|
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
|
-
- HY-148452
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4A3-IN-18 (compound 74) is a silvestrol (HY-13251) analogue. eIF4A3-IN-18 interferes the assembling of eIF4F translation complex with EC50 values of 0.8, 35 and 2 nM for myc-LUC, tub-LUC and the growth inhibition for MBA-MB-231 cells. eIF4A3-IN-18 also has cytotoxicity to RMPI-8226 cells with an LC50 of 0.06 nM. eIF4A3-IN-18 can be used for the research of human cancer pathogenesis .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
|
-
- HY-N4314
-
|
4',5,6,7-Tetramethoxyflavone
|
Bacterial
COX
NO Synthase
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
- HY-W014316R
-
|
|
Bacterial
Fungal
|
Infection
|
|
5-Bromo-5-nitro-1,3-dioxane (Standard) is the analytical standard of 5-Bromo-5-nitro-1,3-dioxane. This product is intended for research and analytical applications. 5-Bromo-5-nitro-1,3-dioxane, an antimicrobial compound, is effective against Gram-positive and Gram-negative bacteria and fungi, including yeast. 5-Bromo-5-nitro-1,3-dioxane inhibits enzyme activity and subsequent inhibition of microbial growth by the oxidation of essential protein thiol .
|
-
- HY-162910
-
|
|
Xanthine Oxidase
HDAC
Autophagy
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition .
|
-
- HY-114312
-
MD-224
5 Publications Verification
|
PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-19542
-
|
C6-Cer; N-Hexanoylsphingosine
|
Apoptosis
|
Cancer
|
|
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
|
-
- HY-168012
-
|
|
Ras
Phosphatase
|
Cancer
|
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-138074
-
|
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
|
Milbemycin A4 oxime is a derivative of milbemycin A4 (Item No. 17155) and a component of Milbemycin Oxime (HY-B0778), compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/mL.1 Milbemycin A4 oxime (2.5 μg/mL) blocks efflux of Fluconazole (HY-B0101) from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate Rhodamine 123 (HY-D0816), in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-147826
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
- HY-N4314R
-
|
|
Bacterial
COX
NO Synthase
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
|
Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
- HY-12031B
-
|
|
Others
|
Inflammation/Immunology
|
|
(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
|
-
- HY-126287
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-15334
-
|
|
VEGFR
|
Cancer
|
|
CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
|
-
- HY-13590
-
|
|
Others
|
Cancer
|
|
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-117051
-
|
|
Others
|
Cancer
|
|
STA-2842 is a small molecule agent that inhibits heat shock protein 90 (HSP90) to treat autosomal dominant polycystic kidney disease (ADPKD). The disease is caused by inherited mutations in the PKD1 or PKD2 genes that aberrantly activate multiple signaling proteins and pathways that regulate cell proliferation. Through network construction, we found that many HSP90 client proteins associated with ADPKD are regulated by HSP90. STA-2842 induced degradation of these clients in Pkd1?/? primary kidney cells and in vivo. In experiments using conditional Cre-mediated in vivo knockout of Pkd1 in mice, we found that weekly administration of STA-2842 for 10 weeks significantly reduced initial renal cyst formation and kidney growth in mice and slowed disease progression in mice with pre-existing cysts. These improved disease phenotypes were accompanied by improvements in renal function markers and reductions in the expression and activity of HSP90 clients and their effectors, with the extent of this inhibition correlating with the extent of cyst expansion in individual animals. Pharmacokinetic analysis showed that HSP90 was overexpressed in cystic kidney tissue and HSP90 inhibitors were selectively retained in cystic tissue, which is similar to the situation in solid tumors. These results provide a preliminary basis for evaluating HSP90 inhibitors as therapeutic agents for ADPKD.
|
-
- HY-162816
-
|
|
PROTACs
MAP4K
|
Cancer
|
|
PROTAC PD-L1 degrader-2 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC PD-L1 degrader-2 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC PD-L1 degrader-2 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC PD-L1 degrader-2 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841) [1] .
|
-
-
-
HY-L044
-
|
|
550 compounds
|
|
Nucleoside and nucleotide analogues are synthetic, chemically modified compounds that have been developed to mimic their physiological counterparts in order to exploit cellular metabolism and subsequently be incorporated into DNA and RNA to inhibit cellular division and viral replication. In addition to their incorporation into nucleic acids, nucleoside and nucleotide analogues can interact with and inhibit essential enzymes such as human and viral polymerases (that is, DNA-dependent DNA polymerases, RNA-dependent DNA polymerases or RNA-dependent RNA polymerases), kinases, ribonucleotide reductase, DNA methyltransferases, purine and pyrimidine nucleoside phosphorylase and thymidylate synthase. These actions of nucleoside and nucleotide analogues have potential therapeutic benefits — for example, in the inhibition of cancer cell growth, the inhibition of viral replication as well as other indications.
MCE offers a unique collection of 550 nucleotide compounds including nucleotide, nucleoside and their structural analogues. MCE Nucleotide Compound Library is a useful tool to discover anti-cancer and antiviral drugs for high throughput screening (HTS) and high content screening (HCS).
|
-
-
HY-L067
-
|
|
688 compounds
|
|
Antibiotics are types of antimicrobial products used for the treatment and prevention of bacterial infections. Antibiotics can kill or inhibit bacterial growth. Although the target of an antibiotic is bacteria, some antibiotics also attack fungi and protozoans. However, antibiotics rarely have an effect on viruses. The major mechanism underlying antibiotics is the inhibition or regulation of enzymes involved in cell wall biosynthesis, nucleic acid metabolism and repair, protein synthesis, or disruption of membrane structure. Many of these cellular functions targeted by antibiotics are most active in multiplying cells. Since there is often overlap in these functions between prokaryotic bacterial cells and eukaryotic mammalian cells, it is not surprising that some antibiotics have also been found to be useful as anticancer agents.
MCE supplies a unique collection of 688 antibiotics, including penicillins, cephalosporins, tetracyclines, macrolides, etc. MCE Antibiotics Library is a useful tool for anti-bacterial or anti-cancer drugs discovery.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D1472
-
|
|
Dyes
|
|
Azure A eosinate is a dye for hematological and histological applications. Azure A eosinate can be used as new photosensitizer prototypes to determine growth inhibition of Candida albicans .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W698686
-
|
|
Cell Assay Reagents
|
|
β-Galactosyl-C18-ceramide is a bioactive molecule that promotes the regulation of nerve cells, regulates protein kinase C activity, and affects hormone receptors. β-Galactosyl-C18-ceramide is widely used in neuroscience research to explore its effects on nerve cell growth and function. The regulatory function of β-Galactosyl-C18-ceramide makes it a potential application prospect in compound development and disease inhibition.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10392B
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R TFA, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R TFA inhibits competitively the binding of β-catenin to TCF4. aStAx-35R TFA selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-P10603
-
|
|
Peptides
|
Infection
|
|
SP1 is an α-peptide encoded by the mating pheromone MFα1 gene in Candida albicans, which can induce cell growth arrest at the mating type locus MTLa in Candida albicans. SP1 can be used in the study of the prevention and treatment of Candida albicans infection .
|
-
- HY-P3156
-
|
|
Fungal
|
Infection
|
|
Syringomycin E is an antifungal cyclic lipodepsinonapeptide. Syringomycin E exhibits growth inhibition of Saccharomyces cerevisiae through interaction with the plasma membrane. Syringomycin E causes K + efflux, Ca 2+ influx, and changes in membrane potential, and is related to channel formation .
|
-
- HY-P4716
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Boc-D-Trp(For)-OH, containing the amino acid tryptophan, is synthesized by the ammonolysis of Boc-protected D-alanine, followed by cyclization to form a dipeptide with ninhydrin. Boc-D-Trp(For)-OH has pharmacological properties, including inhibition of growth hormone release, induction of sleep and antiinflammatory .
|
-
- HY-P10392
-
|
|
β-catenin
Wnt
|
Cancer
|
|
aStAx-35R, a stapled peptide, antagonizes nuclear form of β-catenin and inhibits Wnt signaling. aStAx-35R inhibits competitively the binding of β-catenin to TCF4. aStAx-35R selectively induces growth inhibition of Wnt-dependent cancer cells .
|
-
- HY-P2088
-
|
Des-N-tetramethyltriostin A
|
Peptides
|
Cancer
|
|
TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99590
-
|
ACE-011
|
TGF-β Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Sotatercept (ACE-011) is a soluble activin receptor 2A (ACVR2A) type IgG Fc fusion protein. Sotatercept combines activin and growth differentiation factor to try to restore the balance between growth promotion and growth inhibition signal pathways. Sotatercept has potential application in pulmonary arterial hypertension, anemia, bone loss, erythropoiesis, multiple myeloma (MM) osteolytic lesions .
|
-
- HY-P99192
-
|
LY2875358
|
c-Met/HGFR
|
Cancer
|
|
Emibetuzumab (LY2875358) is a humanized bivalent MET antibody (IgG4 type). Emibetuzumab shows high neutralization and internalization activities, resulting in inhibition of both HGF-dependent and HGF-independent MET pathway activation and tumor growth. Emibetuzumab can be used in study of cancer .
|
-
- HY-P99215
-
|
Anti-EGFL7; RG 7414
|
VEGFR
|
Cancer
|
|
Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition .
|
-
- HY-P99279
-
|
Anti-Human Phosphatidylserine Recombinant Antibody
|
Inhibitory Antibodies
|
Cancer
|
|
Bavituximab (Anti-Human Phosphatidylserine Recombinant Antibody) is a phosphatidylserine (PS)-targeting monoclonal antibody, suppresses tumor growth by targeting tumor vasculature and reactivating antitumor immunity. Bavituximab plus Paclitaxel (HY-B0015) and Carboplatin (HY-17393), have enhanced inhibition on non-small-cell lung cancer .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-P99925
-
|
REGN421
|
Notch
|
Metabolic Disease
Cancer
|
|
Enoticumab (REGN421, SAR153192) is an IgG1κ antibody targeting human Dll4. DLL4 is a ligand of the Notch signaling pathway and regulates fatty acid uptake through non-transcriptional regulation of macropinocytosis-dependent long-chain fatty acid uptake. Specific in vivo activity of Enoticumab in an ovarian xenograft model. EGN421 (2.5 mg/kg once weekly) resulted in 86% and 83% tumor growth inhibition in mouse subcutaneous TOV-112D or intraperitoneal A2780 human tumor xenograft models, respectively .
|
-
- HY-P99667
-
|
OMP-54F28; FZD8-Fc
|
Wnt
|
Cancer
|
|
Ipafricept (OMP-54F28; FZD8-Fc) is a first class recombinant fusion protein with the extracellular part of the human frizzled-8 receptor fused to a human IgG1 Fc fragment that binds Wnt ligands, which blocks Wnt signaling. Ipafricept reduces tumor growth and results in a decrease in both liver and lung metastases combined with Gemcitabine (HY-17026) in pancreatic cancer mouse models. Ipafricept shows solid tumor inhibition activity with well tolerance, such as desmoid tumor, germ cell cancer, ovarian cancer .
|
-
- HY-P99818
-
|
ACE-031
|
TGF-β Receptor
|
Metabolic Disease
|
|
Ramatercept (ACE-031) is a soluble ActRIIB receptor and can be used as a soluble activin receptor 2 (ACVR2) antagonist. Ramatercept inhibits the signal pathway of muscle growth inhibition and has potential application in muscle atrophy .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0671
-
-
-
- HY-N7082
-
-
-
- HY-N2105
-
-
-
- HY-N3001
-
-
-
- HY-N1513
-
-
-
- HY-116506
-
-
-
- HY-107233
-
-
-
- HY-N2871
-
-
-
- HY-N12118
-
-
-
- HY-N10269
-
-
-
- HY-B0133
-
-
-
- HY-N0282
-
-
-
- HY-133680
-
-
-
- HY-N0781
-
-
-
- HY-N4285
-
-
-
- HY-N0284
-
-
-
- HY-113068
-
-
-
- HY-B0133R
-
-
-
- HY-N0282R
-
-
-
- HY-N0781R
-
-
-
- HY-W052289
-
-
-
- HY-121152
-
-
-
- HY-133680R
-
-
-
- HY-N0284R
-
-
-
- HY-122324
-
|
(+)-(S)-Tylophorine; DCB-3500; NSC-717335
|
Apocynaceae
Source classification
Plants
Tylophora
|
Others
|
|
Tylophorine and its analogs are benzoindole alkaloids, most of which are derived from Garcinia plants. Tylophorine analogs all show potent growth inhibition against human hepatocellular carcinoma HepG2 and human nasopharyngeal carcinoma KB cell lines. Tylophorine analogs can also induce increased albumin expression and inhibit α-fetoprotein expression in HepG2 cells, and have the potential to induce HepG2 cell differentiation .
|
-
-
- HY-N2484
-
-
-
- HY-113068R
-
-
-
- HY-107738
-
Guggulsterone
Maximum Cited Publications
12 Publications Verification
Z/E-Guggulsterone
|
Triterpenes
Structural Classification
Classification of Application Fields
Terpenoids
Plants
Burseraceae
Disease Research Fields
Commiphora wightii
Cancer
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
|
-
-
- HY-N4314
-
|
4',5,6,7-Tetramethoxyflavone
|
Infection
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Plants
Compositae
Genista maderensis (Webb & Berthel.) Lowe
Inflammation/Immunology
Disease Research Fields
|
Bacterial
COX
NO Synthase
NF-κB
|
|
Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
|
-
-
- HY-N4314R
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Compositae
Genista maderensis (Webb & Berthel.) Lowe
|
Bacterial
COX
NO Synthase
NF-κB
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Scutellarein tetramethyl ether (Standard) is the analytical standard of Scutellarein tetramethyl ether. This product is intended for research and analytical applications. Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is a bioactive compound extracted from Eupatorium odoratum. Scutellarein tetramethyl ether exhibits anti-inflammatory, antibacterial, pro-coagulant, and anti-tumor activities. Scutellarein tetramethyl ether exerts its anti-inflammatory effects by modulating the NF-κB pathway and regulates bacterial resistance through the inhibition of efflux pumps. Additionally, Scutellarein tetramethyl ether accelerates coagulation time via the endogenous coagulation pathway. Studies have shown that Scutellarein tetramethyl ether can effectively inhibit the growth of the liver cancer cell line HepG2 (IC50= 20.08 μg/mL) .
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- HY-N6871
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Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
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Bacterial
IKK
Ferroptosis
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Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-157029S
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-B0113S
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1 Publications Verification
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Omeprazole-d3 is deuterium labeled Omeprazole. Omeprazole, a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].
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- HY-17406S1
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Tolcapone-d4 is the deuterium labeled Tolcapone. Tolcapone (Ro 40-7592) is a selective, orally active and powerful mixed (peripheral and central) COMT inhibitor with an IC50 of 773 nM in the liver[1]. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis[2]. Tolcapone induces oxidative stress leading to apoptosis and inhibition of tumor growth in neuroblastoma[3].
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- HY-50878S
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Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
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- HY-B0113S1
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Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-122984S
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Diquat-d4 (dibromide)is the deuterium labeledDiquat (dibromide)(HY-122984) . Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test .
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- HY-113068S
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β-Tocopherol-d3 is the deuterium labeled β-Tocopherol. β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol can also prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
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- HY-133680S
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β-Tocopherol-d4 is a deuterium labeled β-Tocopherol (HY-133680). β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol .
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- HY-N6948S
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Linalyl acetate-d6 is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S4
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Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM . Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria .Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor) .
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- HY-B0113S3
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Omeprazole- 13C,d3 is a 13C-labeled and deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
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- HY-50878AS
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Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
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Product Name |
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Classification |
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- HY-157029S
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Alkynes
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KRASG12D-IN-1 (compound 22) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-157031S
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Alkynes
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KRASG12D-IN-2 (compound 28) is a KRAS G12D Inhibitor. KRASG12D-IN-1 has dose-dependent anti-tumor efficacy in the AsPC-1 xenograft mouse models with a tumor growth inhibition .
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- HY-129510
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Alkynes
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4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers .
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- HY-W748514
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Alkynes
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(4-?(Bromomethyl)?phenyl)?(4-?(prop-?2-?yn-?1-?yloxy)?phenyl)?methanone is a compound with anticancer activity that can effectively inhibit the growth of tumor cells and shows potential application value in compound development. The compound has also been studied for the improvement of certain neuropathological conditions and as a candidate compound for anti-inflammatory inhibition.
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