Search Result
Results for "
antiproliferative effect
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-132258A
-
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IMGN853 (solution)
|
Antibody-Drug Conjugates (ADCs)
Antifolate
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Cancer
|
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Mirvetuximab soravtansine (IMGN853) solution is an anti-folate receptor α (FRα) antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A, and the drug-linker conjugate for ADC is sulfo-SPDB-DM4 (HY-101141). Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
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-
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- HY-103193
-
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Colforsin dapropate hydrochloride
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Adenylate Cyclase
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Cardiovascular Disease
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NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
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- HY-120400
-
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Histone Demethylase
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Cancer
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KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels .
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-
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- HY-B0965
-
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Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
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Infection
Neurological Disease
Cancer
|
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Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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-
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- HY-126247
-
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Ras
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Cancer
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BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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- HY-B0965A
-
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Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
Cancer
|
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Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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-
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- HY-15995
-
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TubA
|
Antibiotic
Microtubule/Tubulin
ADC Payload
Mitosis
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Cancer
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Tubulysin A (TubA) is an anticancer and antiangiogenic agent with anti-microtubule, anti-mitosis and anti-proliferative activity against a variety of cancer cells with IC50 values in the pmol range. It can induce apoptosis of cancer cells and has no effect on normal cells. Tubulysins are a group of potent cytotoxins consisting of nine members (A-I). Tubulysin A can synthesize ADC as ADC Cytotoxin .
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- HY-149898
-
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Transmembrane Glycoprotein
CD44
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Cancer
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HA-CD44 interaction inhibitor 1 is a CD44 inhibitor that can inhibit the interaction between Hyaluronic acid (HA) (HY-B0633A) and CD44. HA-CD44 interaction inhibitor 1 exerts an antiproliferative effect on CD44+ cancer cell lines. HA-CD44 interaction inhibitor 1 can be used for the research of cancer .
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-
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- HY-W016889
-
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Ras
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Cancer
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CFL-137 is a potent KRas G12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .
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-
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- HY-13591
-
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IB-MECA; CF-101
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Adenosine Receptor
Apoptosis
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Inflammation/Immunology
Cancer
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Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19 .
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- HY-122639
-
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NEKs
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Cancer
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ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
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- HY-124653
-
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J2
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HSP
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Cancer
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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 .
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- HY-N6635
-
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Fungal
|
Infection
Cancer
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trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
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- HY-N10264
-
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(+)-Avrainvillamide; CJ-17,665
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Antibiotic
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Infection
Cancer
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Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
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-
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- HY-N2693
-
-
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- HY-B0736A
-
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FI7056
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Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
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Infection
Cancer
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Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
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-
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- HY-18979
-
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Flavivirus
Dengue Virus
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Infection
Cancer
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Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities .
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- HY-N3119
-
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Apoptosis
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Cancer
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Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect .
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-
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- HY-W014118
-
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Environmental Pollutants
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Inflammation/Immunology
Cancer
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α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
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- HY-157844
-
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PROTACs
Histone Methyltransferase
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Cancer
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NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research .
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- HY-145264
-
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Epigenetic Reader Domain
PROTACs
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Cancer
|
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OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively .
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- HY-137756
-
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JAK
|
Cancer
|
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JAK2-IN-6, a multiple-substituted aminothiazole derivative, is a potent and selective JAK2 inhibitor with an IC50 of 22.86 μg/mL. JAK2-IN-6 shows no activity against JAK1 and JAK3. JAK2-IN-6 has anti-proliferative effect against cancer cells .
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- HY-111552
-
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Pim
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Cancer
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PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity .
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- HY-N12540
-
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MGDG
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DNA/RNA Synthesis
Apoptosis
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Others
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Monogalactosyldiacylglycerol (MGDG) is a galactolipid with anti-inflammatory and anticancer activities, which is found in photosynthetic organisms. Monogalactosyldiacylglycerol is a potent DNA polymerase inhibitor with pro-apoptotic activity. Monogalactosyldiacylglycerol inhibits the synthesis of LPS (HY-D1056)-induced inflammation-related proteins (Ex-FABP, Avidin, Serum Amyloid A). Monogalactosyldiacylglycerol exerts an anti-proliferative effect on chicken articular chondrocytes . Monogalactosyldiacylglycerol can be used in research related to osteoarthritis, cancer and inflammatory diseases .
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- HY-100933
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-
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- HY-169090
-
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DNA/RNA Synthesis
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Cancer
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TS-002902 is a selective small-molecule inhibitor of TUT4 and TUT7 enzymes, with IC50 values of 0.36 nM and 9.6 nM, respectively. TS-002902 induces an antiproliferative effect in FOCAD-deficient cancer cells. TS-002902 is applicable for research on FOCAD-deficient solid tumors (including glioblastoma, non-small cell lung cancer, and pancreatic cancer) .
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- HY-162100
-
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ULK
Autophagy
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Cancer
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MR-2088 is a reversible, ATP-competitive, and selective ULK1/2 inhibitor with pEC50 values of 8.3 and 8.7 respectively. MR-2088 effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with Trametinib (HY-10999) (MEK inhibitor) in vitro. MR-2088 can be used for non-small lung cell cancer (NSCLC) research .
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- HY-118858
-
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EAAT
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Neurological Disease
Cancer
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UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
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- HY-178161
-
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HDAC
Apoptosis
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Cancer
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HDAC degrader-2 is a selective HDAC degrader with a DC50 values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .
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- HY-157574
-
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TRP Channel
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Cancer
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TRPV6-IN-1 is a potent and selective TRPV6 inhibitor. TRPV6-IN-1 has anti-proliferative effect and can be used for the research of cancer .
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- HY-W041315
-
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Ras
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Cancer
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CFL-120 is a potent KRas G12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer .
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- HY-172911
-
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SHP2
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Cancer
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SHP2-IN-37 (compound C5) is a potent and selective SHP2 allosteric inhibitor with an IC50 of 0.023 μM. SHP2-IN-37 exhibits antiproliferative effect on KYSE-520 and MV-411 cells with IC50s of 6.97 and 0.67 μM, respectively
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- HY-113505
-
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Δ12-PGJ2
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Endogenous Metabolite
Apoptosis
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Cancer
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Delta-12-Prostaglandin J2 (Δ12-PGJ2) is a cyclopentenone prostaglandin (PG) with anti-proliferative effect on various tumor cell growth. Delta-12-Prostaglandin J2, a naturally occurring dehydration product of prostaglandin D2, is able to induce apoptosis in HeLa cells via caspase activation .
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- HY-126247B
-
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Drug Derivative
Ras
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Cancer
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(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
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- HY-139901
-
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Checkpoint Kinase (Chk)
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Cancer
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Chk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma .
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- HY-80013B
-
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CDK
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Cancer
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(E/Z)-THZ1 dihydrochloride is a selective inhibitor of CDK7 with an IC50 of 3.2 nM. (E/Z)-THZ1 dihydrochloride has antiproliferative effect .
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- HY-103367
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Checkpoint Kinase (Chk)
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Cancer
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CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
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- HY-119340
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Flavoneacetic acid
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Reactive Oxygen Species (ROS)
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Cancer
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Mitoflaxone (flavoneacetic acid) is a synthetic flavonoid compound with vascular targeting properties. Mitoflaxone exerts anti-proliferative effects on endothelial cells through a superoxide-dependent mechanism, this effect leads to changes in the permeability of tumor blood vessels, thereby exerting anti-tumor effects [1] [2] .
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- HY-B0736
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-
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- HY-149920
-
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Microtubule/Tubulin
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Cancer
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Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
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- HY-177755
-
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Molecular Glues
BCL6
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Cancer
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BCL6-IN-10 (Compound 6) is a selective partially degradable molecular glue inhibitor that targets the BTB domain of BCL6 with an IC50 of 4 nM. BCL6-IN-10 shows anti-proliferative effect in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6-IN-10 can be used for the research of cancer .
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- HY-144720
-
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SWI/SNF Complex
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Cancer
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BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .
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- HY-B0965AS
-
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Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
|
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Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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- HY-177270
-
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EGFR
Drug Derivative
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Cancer
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CHNQD-01281, a derivative of Brefeldin A (HY-16592), is a EGFR modulator. CHNQD-01281 has strong antiproliferative activities against cancer cells (IC50: 0.079 and 0.081 μM for T24 and J82 cells, respectively). CHNQD-01281 regulates both EGFR/PI3K/AKT and EGFR/ERK pathways and mediates the chemotactic effect of chemokines on immune effector cells. CHNQD-01281 remarkably inhibits tumor growth in T24 xenograft mice model and prolongs the survival time in MB49 allogeneic mice model via inducing infiltration of cytotoxic T cells .
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- HY-152536
-
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NO Synthase
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Cancer
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iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
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- HY-121458
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Apoptosis
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Cancer
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Nemorosone is the main component of the floral resin of Clusia rosea. Nemorosone has an antiproliferative effect on cancer cells. Nemorosone induces apoptosis in HT-29 and LoVo cells .
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- HY-101071
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(+)-Monastrol
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Kinesin
Mitosis
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Cancer
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(S)-Monastrol ((+)-Monastrol) is an allosteric inhibitor of the mitotic kinesin Eg5 that exhibits an antiproliferative effect against several cancer cell lines. (S)-Monastrol arrests mammalian cells in mitosis with monopolar spindles .
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- HY-170955
-
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Transmembrane Glycoprotein
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Cancer
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HA-CD44 interaction inhibitor 3 (compound 5d) is a Hyaluronic acid (HY-B0633A) (HA)-CD44 interaction inhibitor with antiproliferative activities. HA-CD44 interaction inhibitor 3 inhibits MDA-MB-231 (CD44++) cells and MCF-7 cells (CD44--) with EC50s of 4.24 μM and 14.74 μM, respectively. HA-CD44 interaction inhibitor 3 shows the potential for cancer research .
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- HY-P3223A
-
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Opioid Receptor
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Neurological Disease
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Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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- HY-153396
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Ceramidase
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Cancer
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Acid Ceramidase-IN-2 (compound 1) is an acid ceramidase inhibitor with potentially antiproliferative and cytostatic activities. Moreover, human acid ceramidase is overexpressed in prostate cancer cells, indicating potential anti-tumor effect of Acid Ceramidase-IN-2. And Acid Ceramidase-IN-2 hydrolysis can be inhibited by 3 a-ketoamides GT85, GT98 and GT99 inhibits in vitro .
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- HY-162106
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Ferroptosis
PROTACs
Glutathione Peroxidase
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Cancer
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PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
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- HY-126596
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Apoptosis
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Cancer
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Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
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- HY-177761
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Molecular Glues
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Cancer
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GSPT1 degrader-15 (Compound Lib-B-15O) is a potent and highly selective GSPT1 molecular gel degrader, with a DC50 of 154 nM. GSPT1 degrader-15 has almost no effect on the expression of other proteins. GSPT1 degrader-15 exhibits significant anti-proliferative activity against leukemia cells and lymphoma cells. GSPT1 degrader-15 can be used in leukemia and lymphoma research .
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- HY-156183
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MDM-2/p53
ERK
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Cancer
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Antiproliferative agent-37 (compound 10J) shows anti-proliferative effect by arresting the cells at the G2/M phase of the cell cycle .
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- HY-N10354
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Apoptosis
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Cancer
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27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
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- HY-114902
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Epigenetic Reader Domain
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Cancer
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Y02224 is a potent BRD4 inhibitor and exhibits reasonable antiproliferative effect on leukemia cells.Y02224 has the potential for? CRPC research .
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- HY-N10351
-
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Apoptosis
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Cancer
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27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
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- HY-155112
-
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Microtubule/Tubulin
FLT3
Bcr-Abl
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Cancer
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Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
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- HY-121866
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Topoisomerase
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Cancer
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Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
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- HY-161336
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Bacterial
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Cancer
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Alendronate prodrug-1(compound 2) is an inhibitor of farnesyl diphosphate synthase (FPPS). Alendronate prodrug-1 has an antiproliferative effect with an IC50 value of 34.0 μM .
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- HY-N10355
-
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Apoptosis
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Cancer
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27-TBDMS-4-Dehydrowithaferin A, a withaferin A derivative, exhibits potent antiproliferative effects on the tumor cells.27-TBDMS-4-Dehydrowithaferin A induces tumor cells apoptosis. 27-TBDMS-4-Dehydrowithaferin A is a anticancer agent .
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- HY-157460
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Epigenetic Reader Domain
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Cancer
|
|
BRD4 Inhibitor-29 (SQ-17) is a BRD4 inhibitor, with an IC50 of <100 nM. BRD4 Inhibitor-29 shows antiproliferative effect against prostate cancer cells .
|
-
- HY-118242
-
|
|
Estrogen Receptor/ERR
Calmodulin
|
Others
|
|
RU 45144 is an anti-estrogen compound that has the activity of antagonizing the binding of estrogen receptors to calmodulin. RU 45144 can inhibit the binding of estrogen receptors to calmodulin, and its effect is similar to that of tamoxifen. Its anti-estrogen effect may be related to specific side chains in the molecular structure, and the steroid skeleton may be involved in its anti-proliferative activity.
|
-
- HY-W016889R
-
|
|
Reference Standards
Ras
|
Cancer
|
|
CFL-137 is a potent KRasG12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer .
|
-
- HY-146197
-
|
|
Apoptosis
|
Cancer
|
|
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes .
|
-
- HY-157960
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
|
-
- HY-143280
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .
|
-
- HY-119827
-
|
F 860191
|
Topoisomerase
|
Cancer
|
|
Moflomycin (F 860191) is a compound with strong anti-leukemic activity and low mutagenicity. Moflomycin has an antiproliferative effect on the leukemic cell line HL60 in vitro (IC50=2.9 nM) . Moflomycin enhances topoisomerase II-induced DNA breaks and free radical production .
|
-
- HY-152193
-
|
|
Apoptosis
|
Cancer
|
|
ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression .
|
-
- HY-158076
-
|
|
IAP
|
Cancer
|
|
S2/IAPinh is a conjugate, which consist of an inhibitor for the apoptosis protein inhibitor (IAPinh) and a ligand for sigma 2 SW43. S2/IAPinh exhibits an anti-proliferative and apoptotic-inducing effect through degradation of the cellular inhibitor for apoptosis protein (clAP-1) .
|
-
- HY-P3223
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
|
-
- HY-168514
-
|
|
SOS1
EGFR
|
Cancer
|
|
SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC50s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .
|
-
- HY-146254
-
|
|
Carbonic Anhydrase
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
hCAIX-IN-12 is a potent hCAIX inhibitor with IC50 values of 0.74, 10.78 μM for CAIX and CAII, respectively. hCAIX-IN-12 shows antiproliferative effect and induces apoptosis. hCAIX-IN-12 increases ROS production. hCAIX-IN-12 has the potential for the research of colorectal cancer (CRC) .
|
-
- HY-173498
-
|
|
Adenosine Receptor
|
Cancer
|
|
AR ligand 40 (compound 19c) is an Adenosine A1 Receptor ligand with antagonist activity. AR ligand 40 exhibits antiproliferative effect on SW480, SW48, HCT116, K562, MDA-MB-231, and A549 cells with EC50s of 7, 10, 12, 13, 15 and 39 μM .
|
-
- HY-155766
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor, with an IC50 of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells with IC50 values below 0.3 nM .
|
-
- HY-N6635R
-
|
|
Reference Standards
Fungal
|
Infection
Cancer
|
|
trans-Nerolidol (Standard) is the analytical standard of trans-Nerolidol. This product is intended for research and analytical applications. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
|
-
- HY-150590
-
|
|
Proteasome
|
Cancer
|
|
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M .
|
-
- HY-161814
-
|
|
Apoptosis
|
Metabolic Disease
|
|
Apoptosis inducer 20 (12) causes G2/M cell cycle arrest and induction of apoptosis via caspase 3/7 activation, which occurred during M arrest. Apoptosis inducer 20 is a novel indolic benzenesulfonamide with anti-proliferative effect against a broad panel of cancer cell lines, which is proming for research of new anti-mitotic agents .
|
-
- HY-138185
-
|
SF 2738A
|
Bacterial
Apoptosis
|
Cancer
|
|
Collismycin A is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities, including antibacterial, antiproliferative, and neuroprotective properties. It is active against a variety of bacteria (MICs=6.25 and 100 μg/mL) and fungi (MICs=12.5-100 μg/mL). It inhibits proliferation of A549 lung, HCT116 colon, and HeLa cervical cancer cells (IC50s=0.3, 0.6, and 0.3 μM, respectively) and NIH373 fibroblasts (IC50=56.6 μM) but not MDA-MD-231 breast cancer cells (IC50=>100 μM). Collismycin A forms a complex with Fe(II) and Fe(III) at a 2:1 ratio, and the addition of iron ions inhibits the antiproliferative effect of collismycin A on HeLa cells, an effect that does not occur with the addition of zinc, manganese, copper, or magnesium ions.3 Collismycin A (1 μM) prevents apoptosis in the brain region of zebrafish larvae in a model of neuronal cell death induced by all-trans retinoic acid.
|
-
- HY-B0736AR
-
|
FI7056 (Standard)
|
Reference Standards
Fungal
Autophagy
Apoptosis
p38 MAPK
Microtubule/Tubulin
|
Infection
|
|
Sertaconazole (nitrate) (Standard) is the analytical standard of Sertaconazole (nitrate). This product is intended for research and analytical applications. Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells .
|
-
- HY-N15424
-
|
|
Apoptosis
Bcl-2 Family
|
|
|
Himachalol, a sesquiterpene, is an orally active antispasmodic and anticancer constituent found in the wood of Cedrus deodara. Himachalol has anti-proliferative activity against the melanoma cells, and induces apoptosis (decreases Bcl-2 level and increases Bax level). Himachalol has systemic hypotension and peripheral vasodilation effect. Himachalol inhibits Carbachol-induced spasm of the intestine. The LD50 of Himachalol in mice is 265 mg/kg (p.o.) and 247 mg/kg (i.p.) .
|
-
- HY-148821
-
|
|
PAK
MEK
PERK
|
Cancer
|
|
BJG-05-039 is a PAK1-selective degrader consisting of NVS-PAK1-1 (HY-100519) conjugated to Lenalidomide (HY-A0003). BJG-05-039 induces selective degradation of PAK1. BJG-05-039 inhibits phosphorylation of MEK S298, as well as inhibiting phosphorylation of ERK. BJG-05-039 has an anti-proliferative effect on PAK1-dependent cell lines .
|
-
- HY-B1690AR
-
|
|
Reference Standards
Antibiotic
Bacterial
Histamine Receptor
|
Infection
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-117540
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- HY-B0965AR
-
|
|
Reference Standards
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Neurological Disease
Cancer
|
|
Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-B0965S
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
Apoptosis
Bacterial
Autophagy
5-HT Receptor
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-B0965R
-
|
|
Reference Standards
Dopamine Receptor
Apoptosis
5-HT Receptor
Autophagy
Bacterial
|
Infection
Neurological Disease
Cancer
|
|
Thioridazine (hydrochloride) (Standard) is the analytical standard of Thioridazine (hydrochloride). This product is intended for research and analytical applications. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
|
-
- HY-115904
-
|
|
CDK
FLT3
|
Cancer
|
|
FLT3/CDK4-IN-1 is a potent, high selective and orally active FLT3/CDK4 dual inhibitor (IC50=11 and 7 nM for FLT3 and CDK4, respectively). FLT3/CDK4-IN-1 has antiproliferative activities against certain cancer cells. FLT3/CDK4-IN-1 has good antitumor effect in vivo .
|
-
- HY-169400
-
|
|
HDAC
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
|
-
- HY-N13130
-
|
|
Others
|
Cancer
|
|
(+)-Mollisacacidin is a flavan compound found in the root bark of Albizia glaberrima. (+)-Mollisacacidin exhibits no significant antiproliferative effect on cancer cells .
|
-
- HY-180607
-
|
|
Ras
|
Cancer
|
|
KRAS-IN-50 (Compound 136a) is a KRAS inhibitor. KRAS-IN-50 has an anti-proliferative effect on KRAS mutant cells. KRAS-IN-50 has anti-cancer activity against colon cancer .
|
-
- HY-149035
-
|
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model .
|
-
- HY-180198
-
|
|
Melatonin Receptor
|
Cancer
|
|
UCM1400 is a melatonin receptor (MT) subtype-selective modulator. UCM1400 shows agonistic effect for MT1 and antagonistic effect for MT2 with pKi values of 7.94 and 8.11. UCM1400 can inhibit the decrease in cAMP mediated by the MT2 receptor with a pIC50 of 7.87. UCM1400 exhibits anti-proliferative activity against human glioma cells and inhibit tumor growth. UCM1400 can be used for the research of cancer, such as glioma .
|
-
- HY-183553
-
|
|
Ras
|
Cancer
|
|
AUBE00 is an orally active, selective cyclic peptide pan-KRAS inhibitor. AUBE00 selectively binds to the OFF state of KRAS. AUBE00 exhibits anticancer activity against RAS wild-type colorectal cancer. The combination of AUBE00 with Cetuximab (HY-P9905) produces a synergistic antiproliferative effect .
|
-
- HY-N11737
-
|
|
Drug Derivative
|
Inflammation/Immunology
|
|
Monasfluore A is an azaphenanthrenone derivative with antioxidant activity. Monasfluore A inhibits LPS-induced nitric oxide production. Monasfluore A scavenges DPPH and superoxide anion free radicals. Monasfluore A exerts cellular antioxidant activity in oxidatively damaged colon adenocarcinoma cells. Monasfluore A shows no antiproliferative effect on human laryngeal cancer cells and colon adenocarcinoma cells .
|
-
- HY-176792A
-
|
|
PROTACs
Ras
Drug Isomer
|
Cancer
|
|
(R)-ACBI-4 is an isomer of ACBI-4 (HY-176792). ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader. ACBI-4 has significant anti-proliferative effect and potently degrades multiple KRAS mutants in cancer cells, such as KRASG12R .
|
-
- HY-180508
-
|
|
MDM-2/p53
Topoisomerase
|
Cancer
|
|
MDM2-IN-27 (Compound 20k) is an MDM2 inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has a certain topoisomerase I inhibitory activity and has a very weak inhibitory effect on topoisomerase IIα. MDM2-IN-27 exhibits significant anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma .
|
-
- HY-180509
-
|
|
Topoisomerase
MDM-2/p53
|
Cancer
|
|
Topoisomerase I/IIα-IN-1 (Compound 20i) is a Topoisomerase I/IIα inhibitor. MDM2-IN-27 can effectively block the inhibitory effect of MDM2 on p53, thereby activating the p53 pathway. MDM2-IN-27 has relatively poor anti-proliferative activity against breast cancer, colon cancer, and cutaneous squamous cell carcinoma .
|
-
- HY-128299
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
Cancer
|
|
ALDH3A1-IN-4 is a selective ALDH3A1 inhibitor with an IC50 of 0.2 μM. ALDH3A1-IN-4 binds to the aldehyde-binding pocket of ALDH3A1 via hydrophobic interactions and van der Waals forces. ALDH3A1-IN-4 acts as a chemosensitizer that sensitizes ALDH3A1-expressing cancer cells to the antiproliferative effect of mafosfamide, but does not produce a sensitizing effect on non-cancer cells that do not express ALDH3A1. ALDH3A1-IN-4 is applicable to research related to lung adenocarcinoma and glioblastoma .
|
-
- HY-103193R
-
|
Colforsin dapropate hydrochloride (Standard)
|
Reference Standards
Adenylate Cyclase
|
Cardiovascular Disease
|
|
NKH477 (Standard) is the analytical standard of NKH477 (HY-103193). This product is intended for research and analytical applications. NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
|
-
- HY-151436
-
|
|
CDK
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
|
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
|
-
- HY-173499
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
HLDA-212 (Compound 43) is a bifunctional small molecule targeting HaloTag-tagged protein (Target Protein, TP) and Aurora kinase A/B (AURKA/B, Effector Protein, EP). HLDA-212 binds to TP and EP to form a stable ternary complex (TP:RIPTAC:EP), inhibiting the cell-survival function of EP and inducing apoptosis in TP-expressing cancer cells. HLDA-212 shows antiproliferative activity (GI50 of 0.011 μM) in 293_HFL cells. HLDA-212 is promising for research of cancers with high TP expression (such as prostate cancer and hematological malignancies) .
|
-
- HY-N6651
-
|
|
STAT
Phosphatase
Apoptosis
Autophagy
p38 MAPK
EGFR
JAK
Bcl-2 Family
Survivin
Akt
mTOR
PARP
Caspase
Atg8/LC3
CDK
|
Cancer
|
|
Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation [1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC .
|
-
- HY-P3808
-
-
- HY-W014118R
-
|
|
Reference Standards
Environmental Pollutants
|
Cancer
|
|
α-Hexylcinnamaldehyde (Standard) is the analytical standard of α-Hexylcinnamaldehyde. This product is intended for research and analytical applications. α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
|
-
- HY-173059
-
|
|
CDK
|
Cancer
|
|
CDK12/13-IN-3 (Compound 12b) is the orally active inhibitor for CDK that inhibits CDK12 and CDK13 with IC50 of 107.4 nM and 79.4 nM. CDK12/13-IN-3 inhibits the phosphorylation of Ser2 on the CTD of RNA polymerase II, induces DNA damage, and downregulates the gene expression of DNA damage response (DDR). CDK12/13-IN-3 exhibits antiproliferative activity against multiple cancer cells with IC50 of nanomolar levels. CDK12/13-IN-3 exhibits antitumor effect in mouse models, exhibits good pharmacokinetic properties with an oral bioavailability of 53.6% .
|
-
- HY-149401
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFR WT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .
|
-
- HY-174382
-
|
|
Akt
mTOR
NF-κB
ROR
Apoptosis
|
Cancer
|
|
ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research .
|
-
- HY-156470
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-144451
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
|
-
- HY-181537
-
|
|
PROTACs
SNIPERs
YAP
IAP
|
Cancer
|
|
PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC50 of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .
|
-
- HY-170966
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
|
-
- HY-180817
-
|
|
CDK
Aurora Kinase
Apoptosis
|
Cancer
|
|
CDK2-IN-55 (Compound 12c) is a CDK2 inhibitor with an IC50 value of 4.7 nM. CDK2-IN-55 also has a strong inhibitory effect on CDK1 (IC50 = 26.3 nM), moderate inhibitory effects on Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM), and very weak inhibitory activities on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM). CDK2-IN-55 shows strong anti-proliferative activity against various cancer cell lines, inducing cell cycle arrest and apoptosis. CDK2-IN-55 can be used for research on colorectal cancer, lung cancer, and cervical cancer .
|
-
- HY-174302
-
|
|
Pim
HDAC
PARP
Apoptosis
|
Cancer
|
|
PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
|
-
- HY-173493
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
Akt
mTOR
|
Cancer
|
|
ALK-IN-31 (Compound Ld-10) is an orally active ALK inhibitor (IC50: 1135 nM). ALK-IN-31 exhibits excellent antiproliferative activity against lung cancer H2228 cells with an IC50 value of 1.35 μM. ALK-IN-31 induces apoptosis and arrests cell proliferation in the G0/G1 phase by affecting mitochondrial function. ALK-IN-31 exerts its anti-tumor effect by downregulating the expression of p-AKT and p-mTOR in the PI3K-AKT-mTOR signaling pathway downstream of ALK. ALK-IN-31 can be used in the study of non-small cell lung cancer (NSCLC) .
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- HY-N6871
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Bacterial
IKK
Ferroptosis
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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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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- HY-168131
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PROTACs
Histone Methyltransferase
Apoptosis
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Cancer
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PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751;Pink: EZH2 inhibitor Tazemetostat (HY-13803)) .
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- HY-179020
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PARP
VEGFR
DNA/RNA Synthesis
Apoptosis
Autophagy
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Cancer
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PARP/VEGFR3-IN-1 (Compound 18) is a dual PARP-VEGFR3 target inhibitor. Its IC50 values for PARP1, PARP2, and VEGFR3 are 0.0763, 0.0366, and 4.25 nM respectively. PARP/VEGFR3-IN-1 has no inhibitory effect on VEGFR1/2 and shows subtype selectivity. PARP/VEGFR3-IN-1 exhibits significant anti-proliferative activity in various cancer cells (leukemia, lung cancer, and triple-negative breast cancer). PARP/VEGFR3-IN-1 induces DNA damage and cell cycle arrest. PARP/VEGFR3-IN-1 triggers various forms of cell death by inducing apoptosis and autophagy. PARP/VEGFR3-IN-1 can be formulated into nanodelivery systems, significantly enhancing tumor targeting and therapeutic window .
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- HY-175213
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
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- HY-175849
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HyT
Anaplastic lymphoma kinase (ALK)
Apoptosis
STAT
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Cancer
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ALK degrader 1 is a potent, hydrophobic tag (HyT)-based degrader that induces ubiquitin-proteasome system (UPS)-dependent EML4-ALK degradation (DC50 = 0.13 μM). ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research .
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- HY-117991
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VEGFR
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Cancer
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DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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- HY-164393
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JAK
Bcr-Abl
Apoptosis
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Cancer
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ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
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- HY-W049881
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Dopamine Receptor
PI3K
Monoamine Oxidase
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Neurological Disease
|
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9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies .
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- HY-155232
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PI3K
Apoptosis
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Cancer
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PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies .
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- HY-111137
-
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XC-302 free base
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Akt
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Cancer
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Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
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- HY-13032B
-
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GSK 525762C; I-BET 762 besylate
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Epigenetic Reader Domain
ERK
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Cancer
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Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P3223A
-
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Opioid Receptor
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Neurological Disease
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Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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- HY-P3223
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Opioid Receptor
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Neurological Disease
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Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
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- HY-P3808
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N6871
-
|
|
Infection
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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-
- HY-N6635
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-
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- HY-N10264
-
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(+)-Avrainvillamide; CJ-17,665
|
Infection
Alkaloids
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Disease Research Fields
Indole Alkaloids
Source Classification
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Antibiotic
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Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
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-
- HY-N2693
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-
-
- HY-18979
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-
-
- HY-N3119
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-
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- HY-W014118
-
|
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Classification of Application Fields
Ketones, Aldehydes, Acids
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Environmental Pollutants
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α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
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-
- HY-N12540
-
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MGDG
|
Structural Classification
other families
Oplismenus burmannii
Plants
Lipid
Source Classification
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DNA/RNA Synthesis
Apoptosis
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Monogalactosyldiacylglycerol (MGDG) is a galactolipid with anti-inflammatory and anticancer activities, which is found in photosynthetic organisms. Monogalactosyldiacylglycerol is a potent DNA polymerase inhibitor with pro-apoptotic activity. Monogalactosyldiacylglycerol inhibits the synthesis of LPS (HY-D1056)-induced inflammation-related proteins (Ex-FABP, Avidin, Serum Amyloid A). Monogalactosyldiacylglycerol exerts an anti-proliferative effect on chicken articular chondrocytes . Monogalactosyldiacylglycerol can be used in research related to osteoarthritis, cancer and inflammatory diseases .
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-
- HY-N6651
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-
-
- HY-113505
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-
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- HY-121458
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-
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- HY-126596
-
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Quinones
Alkanna tinctoria (L.) Tausch
Plants
Naphthalene Quinones
Boraginaceae
Source Classification
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Apoptosis
|
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Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
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- HY-N10351
-
-
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- HY-N10355
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-
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- HY-N6635R
-
-
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- HY-N15424
-
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Cedrus deodara (Roxburgh) G. Don
Pinaceae
Terpenoids
Sesquiterpenes
Plants
Source Classification
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Apoptosis
Bcl-2 Family
|
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Himachalol, a sesquiterpene, is an orally active antispasmodic and anticancer constituent found in the wood of Cedrus deodara. Himachalol has anti-proliferative activity against the melanoma cells, and induces apoptosis (decreases Bcl-2 level and increases Bax level). Himachalol has systemic hypotension and peripheral vasodilation effect. Himachalol inhibits Carbachol-induced spasm of the intestine. The LD50 of Himachalol in mice is 265 mg/kg (p.o.) and 247 mg/kg (i.p.) .
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- HY-W014118R
-
|
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Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
Environmental Pollutants
|
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α-Hexylcinnamaldehyde (Standard) is the analytical standard of α-Hexylcinnamaldehyde. This product is intended for research and analytical applications. α-Hexylcinnamaldehyde is an O-acetyltransferase (OAT) inhibitor. α-Hexylcinnamaldehyde inhibits OAT-mediated bioactivation of nitroarene mutagens, exerts antimutagenic activity through demutagenic and bioantimutagenic mechanisms, and interferes with ATP-binding cassette (ABC) transporter function to reduce substrate efflux. α-Hexylcinnamaldehyde alters membrane permeability, fluidizes phospholipid membranes, exerts antioxidant effects, and enhances the antiproliferative effect of Doxorubicin on human cancer cells. α-Hexylcinnamaldehyde can be used in the research of colorectal adenocarcinoma, T-cell leukemia, and multidrug-resistant cancers .
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-
-
- HY-N13130
-
-
-
- HY-N11737
-
|
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
Drug Derivative
|
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Monasfluore A is an azaphenanthrenone derivative with antioxidant activity. Monasfluore A inhibits LPS-induced nitric oxide production. Monasfluore A scavenges DPPH and superoxide anion free radicals. Monasfluore A exerts cellular antioxidant activity in oxidatively damaged colon adenocarcinoma cells. Monasfluore A shows no antiproliferative effect on human laryngeal cancer cells and colon adenocarcinoma cells .
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| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0965AS
-
|
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Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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- HY-B0965S
-
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Thioridazine-d3 2-Sulfone is the deuterium labeled Thioridazine hydrochloride. Thioridazine hydrochloride, an orally active antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs) .
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