Search Result
Results for "
HT29
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121199
-
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Apoptosis
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Cancer
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Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage .
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-
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- HY-75564
-
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Endogenous Metabolite
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Cancer
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Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM .
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-
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- HY-101524
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TC13172
2 Publications Verification
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Mixed Lineage Kinase
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Cancer
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TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells .
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-
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- HY-160170
-
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Necroptosis
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Cancer
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Necrosis inhibitor 3 (compound B3) is a poteng inhibitor of necrosis, with the IC50 value of 0.29 nM in HT29 cells .
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-
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- HY-159795
-
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PF-07799933; ARRY-440
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Raf
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Cancer
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Claturafenib ( PF-07799933) is an inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in HT29 cells with an IC50 value of 1.6 nM .
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-
-
- HY-161628
-
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Topoisomerase
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Cancer
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Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
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-
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- HY-161361
-
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Mixed Lineage Kinase
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Cancer
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MLKL-IN-7 (compound 9) is a MLKL inhibitor, and shows anti-necroptosis activity in HT-29 cells with the IC50 of 148.4 nM .
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-
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- HY-139062
-
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C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
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Others
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Cancer
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C6 Urea Ceramide (C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells, but not in MEFs lacking neutral ceramidase. At concentrations of 5 and 10 μM, it inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but not in noncancerous RIE-1 cells. C6 Urea Ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116 cells, but not in RIE-1 cells. When administered at doses of 1.25, 2.5, and 5 mg/kg for five days, it reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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-
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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-123707
-
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Microtubule/Tubulin
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Cancer
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KPU-300 (compound 6b) is a tubulin inhibitor. KPU-300 has potent cytotoxicity with an IC50 value of 7.0 nM against HT-29 cells .
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-
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- HY-146274
-
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
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-
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- HY-126779
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Fungal
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Cancer
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Stictic acid is a secondary metabolite that can be isolated from the lichen Lobaria pulmonaria (L.) Hoffm. Stictic acid inhibits growth of human colon adenocarcinoma HT-29 cells (IC50: 29.29 μg/mL) .
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-
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- HY-139206
-
-
-
- HY-146778
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis .
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-
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- HY-W727999
-
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Apoptosis
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Cancer
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Koenimbine is an anticancer agent that can be obtained from the leaves and fruits of Murraya koenigii. Koenimbine can induce apoptosis and necrosis in HT-29 and SW48 cells. Koenimbine can be used in the research of cancer .
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-
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- HY-N12430
-
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Others
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Cancer
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Marsdenoside A (compound 7) is a Marsdenoside isolated from Alocasia genus. Marsdenoside A has a weak growth inhibitory effect on two tumor cell lines, MGC-803 and HT-29, with IC50 >50 μg/mL.
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-
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- HY-N8462
-
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Scutebatin C
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Others
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Cancer
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6-O-Nicotinoylscutebarbatine G is an alkaloid that can be isolated from Scutellaria barbata.6-O-Nicotinoylscutebarbatine has cytotoxic activities against HONE-1, KB and HT29 cells with IC50s of 3.1, 2.1 and 5.7 μM, respectively .
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-
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- HY-N8387
-
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Ras
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Cancer
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Neogrifolin is an inhibitor of KRAS. Neogrifolin suppress KRAS expression in human colon cancer cells. Neogrifolin has anti-cell viability activity against HeLa, SW480 and HT29 cells wih IC50s of 24.3, 34.6, and 30.1 μM, respectively .
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-
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- HY-N3123
-
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Dihydrooxochelerythrine
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Others
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Cancer
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Oxychelerythrine is an alkaloid that can be isolated from Zanthoxylum integrifoliolum. Oxychelerythrine exhibits cytotoxicity against P-388 and HT-29 cell lines with ED50s of 3.25 and 5.48 μg/mL, respectively .
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-
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- HY-N8225
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(-)-Manassantin B
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Others
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Others
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Manassantin B (compound 6) is a kind of lignan. Manassantin B can be isolated from the ethyl acetate extract of the roots of Saururus chinensis. Manassantin B has cytotoxicities against HT-29 with an IC50 value of 12 μM .
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-
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- HY-164467
-
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Wnt
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Cancer
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CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
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-
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- HY-107664
-
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Neurotensin Receptor
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Neurological Disease
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SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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-
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- HY-107664A
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Neurotensin Receptor
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Neurological Disease
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SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
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-
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- HY-146505
-
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Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species
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Cancer
|
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Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice .
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-
-
- HY-12855A
-
Lys05
2 Publications Verification
Lys01 trihydrochloride
|
Autophagy
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Cancer
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Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
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-
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- HY-N3057
-
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Others
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Cancer
|
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Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
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-
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- HY-147348
-
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Others
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Cancer
|
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4-Formylcolchicine is a potent anticancer agent. 4-Formylcolchicine shows cytotoxicity activity with IC50 values of 1.007, 0.128, 0.054 µM for A549, HT-29, HCT116 cells, respectively .
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-
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- HY-157963
-
-
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- HY-160811
-
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VEGFR
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Cancer
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hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM .
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-
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- HY-13734
-
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IV-2
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Others
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Cancer
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PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
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-
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- HY-122675
-
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Others
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Cancer
|
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ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
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-
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- HY-N12437
-
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Others
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Cancer
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Marsdenoside B (compound 8) is a Marsdenoside isolated from Alocasia genus. Marsdenoside B inhibits the growth of tumor cell lines MGC-803 and HT-29 with IC50s of 25.6 μg/mL and 32.4 μg/mL, respectively.
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- HY-130602
-
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PROTACs
MEK
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Cancer
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MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively .
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- HY-N8934
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Others
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Cancer
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6β-Hydroxytomentosin, a sesquiterpenoid, can be found in flowers of Inula japonica. 6β-Hydroxytomentosin exhibits weak cytotoxicities against A549, SK-OV-3, HepG-2 and HT-29 cell lines .
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-
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- HY-157085
-
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HSP
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Cancer
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BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
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-
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- HY-13620
-
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LU 79553
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Others
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Cancer
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Elinafide is an anticancer agent with a naphthalimide structure that targets DNA. Elinafide interferes with cell metabolism by inserting a planar ring into the DNA double helix and interacting with enzymes through its side chain. The IC50 value of Elinafide for HT-29 cells is 0.014 μM .
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-
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- HY-14444
-
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NPI-2358
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Microtubule/Tubulin
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Cancer
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Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells . Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells .
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- HY-156775
-
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Others
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Cancer
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Antitumor agent-119 (compound 13K) is a 2-benzoxazolyl hydrazone derivative with anticancer activities. Antitumor agent-119 inhibits the cell growth of Butkitt, CCRF-CEM, HeLa, and HT-29 with IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM, respectively .
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-
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- HY-161614
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 44 (Compound 26r) is an inhibitor for tubullin. Tubulin inhibitor 44 exhibits cytotoxicity in cancer cells NCI-H460, BxPC-3 and HT-29, with IC50s of 0.96, 0.66 and 0.61 nM, respectively .
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-
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- HY-149952
-
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ATM/ATR
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Cancer
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ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers .
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-
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- HY-N1631
-
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1-Hydroxyrutaecarpine
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Others
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Others
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1-Hydroxyrutaecarpine (compound 1a) is a hydroxy-derivative of rutaecarpine. 1-Hydroxyrutaecarpine shows cytotoxicities with ED50s of 3.72, 7.44 µg/mL for P-388 and HT-29 cells, respectively. 1-Hydroxyrutaecarpine shows antiplatelet activity .
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-
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- HY-B1714A
-
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Others
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Cancer
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NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
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-
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- HY-N10132
-
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nAChR
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Infection
Neurological Disease
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Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
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-
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- HY-169074
-
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Thalidomide-N-methylpiperazine is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-N-methylpiperazine can be used to synthesize PROTAC MLKL Degrader-2 (HY-169072) to exhibit antinecroptotic activity on human cell lines and effectively degrade MLKL in the HT-29 xenograft mouse model .
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-
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- HY-147725
-
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization .
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-
-
- HY-147727
-
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
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-
-
- HY-163806
-
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HDAC
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Neurological Disease
Cancer
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NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
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-
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- HY-N3057R
-
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Others
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Cancer
|
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Pinostrobin chalcone (Standard) is the analytical standard of Pinostrobin chalcone. This product is intended for research and analytical applications. Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
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-
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- HY-12855
-
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Autophagy
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Cancer
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Lys01, a dimeric form of Chloroquine (HY-17589A), is an autophagy inhibitor. Lys01 inhibits cell viability of 1205Lu, c8161, LN229, HT-29 cells with IC50s of 3.6, 3.8, 7.9, 6.0 μM. Lys01 can be used for anticancer research .
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-
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- HY-P3116
-
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Bacterial
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Cancer
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Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
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- HY-B1714
-
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Others
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Cancer
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NSC 601980 analog is the analog of the NSC601980, NSC601980 shows antitumor activity in the yeast screening experiment, which can inhibit cell proliferation in the COLO 205 and HT29 with Log GI 50 of -6.6 and -6.9 respectively.
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-
- HY-156098
-
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c-Met/HGFR
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Cancer
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c-Met-IN-19 (Compound 21j) is a c-Met inhibitor (IC50: 1.99 nM). c-Met-IN-19 shows cytotoxicity against A549, HT-29, SGC-7901, MDA-MB-231 cells with IC50s of 0.25, 0.36, 0.98, 0.76 μM .
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-
- HY-155240
-
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Tyrosinase
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Cancer
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Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
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- HY-161282
-
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Carbonic Anhydrase
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Neurological Disease
Cancer
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hCAII-IN-10 (compound 11d) is hCA II inhibitor with the IC50s of 14 nM and 29.2 μM for hCA II and hCA I, respectively. hCAII-IN-10 inhibits cell growth against HT-29 cells with the IC50 of 74 μM. hCAII-IN-10 shows strongly lowered intraocular pressure in the glaucomatous rabbit eye model .
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-
- HY-163390
-
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RIP kinase
Necroptosis
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Inflammation/Immunology
Cancer
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RIP1 kinase inhibitor 9 (compound SY-1) is a selective RIP kinase inhibitor. RIP1 kinase inhibitor 9 effectively suppresses the central inflammatory response induced by epilepsy. RIP1 kinase inhibitor 9 inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC50 of 7.04 nM .
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-
- HY-N1261
-
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Others
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Cancer
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Scutebarbatine B shows significant cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, with IC50 values in the range 3.5-8.1 mM [1]<
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- HY-155203
-
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Apoptosis
Reactive Oxygen Species
Ferroptosis
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Cancer
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Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM .
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- HY-N1655
-
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Others
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Cancer
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2,3-Dihydroamentoflavone 7,4'-dimethyl ether is a biflavonoid, which can be isolated from the aerial parts of Selaginella delicatula. 2,3-Dihydroamentoflavone 7,4'-dimethyl ether exhibits cytotoxicities against P-388 and HT-29 cell lines, with ED50 (median effective dose) values of 3.50 and 5.25 µg/mL, respectively .
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- HY-151541
-
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Mixed Lineage Kinase
Necroptosis
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Neurological Disease
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MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM . MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151542
-
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Mixed Lineage Kinase
Necroptosis
RIP kinase
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Neurological Disease
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MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM . MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-153863
-
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MEK
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Cancer
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MS934 is a novel improved VHL-recruiting MEK 1/2 degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma .
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- HY-157740
-
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HDAC
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Cancer
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XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 .
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- HY-139248
-
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Others
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Cancer
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Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) .
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- HY-120528
-
-
- HY-120528A
-
-
- HY-115949
-
|
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Others
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Cancer
|
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Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively .
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- HY-155152
-
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P-glycoprotein
BCRP
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Cancer
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P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
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- HY-157516
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CDK
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Cancer
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CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .
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-
- HY-162721
-
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Others
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Cancer
|
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Anticancer agent 242 (7) possesses anticancer activity in A2780 (IC50 = 0.24 μM, ovarian adenocarcinoma), A2780cis (IC50 = 0.45 μM, resistant derivative of A2780), CCD18Co (IC50 = 0.59 μM, non-malignant human fibroblasts), A549 (IC50 = 0.32 μM, lung carcinoma), HT29 (IC50 = 0.26 μM, colorectal adenocarcinoma), and MCF7 (IC50 = 0.55 μM, breast adenocarcinoma) .
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-
- HY-100753
-
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STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis .
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-
- HY-149511
-
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c-Met/HGFR
Apoptosis
PDGFR
|
Cancer
|
|
MET/PDGFRA-IN-2 (compound 8h) is a MET and PDGFRA protein inhibitor. MET/PDGFRA-IN-2 induces cell apoptosis. MET/PDGFRA-IN-2 inhibits proliferation of MET-positive cells (IC50s: 9.7, 6.1, 12.0, 11.5, 8.6, 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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-
- HY-156375
-
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Pyruvate Kinase
PDK-1
|
Cancer
|
|
PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
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-
- HY-163692
-
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Microtubule/Tubulin
Apoptosis
|
Cancer
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Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
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-
- HY-118899
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Others
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Cancer
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XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
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-
- HY-161900
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 22 (QR-5) is an apoptosis inducer with IC50 values of 63.1 and 46.5 μM for colon cancer cell lines SW480 and HT29, respectively. Apoptosis inducer 22 induces apoptosis by inhibiting the Wnt/β-catenin axis in colon cancer cells. Apoptosis inducer 22 can be used in anti-colon cancer research.
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-
- HY-123237
-
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|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
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-
- HY-115950
-
|
|
Others
|
Cancer
|
|
Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively .
|
-
- HY-N6002
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 µM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer .
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-
- HY-P1435A
-
|
|
NADPH Oxidase
|
Cancer
|
|
NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
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-
- HY-149510
-
|
|
c-Met/HGFR
Apoptosis
PDGFR
|
Cancer
|
|
MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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-
- HY-161863
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
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-
- HY-149302
-
|
|
Apoptosis
Autophagy
Histone Acetyltransferase
|
Cancer
|
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively .
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells .
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-
- HY-156792
-
|
|
Others
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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-
- HY-N12820
-
|
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Others
|
Cancer
|
|
3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C can be isolated from Alocasia cucullata (Lour.) G. Don. 3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C has moderate tumor cells inhibitory activity against MGC-803 and HT-29 cells with IC50 values of 45.6 and 28.4 μg/mL, respectively .
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-
- HY-161852
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
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-
- HY-103387
-
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COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects .
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-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
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-
- HY-N7175
-
|
9,11-Dehydroergosterol peroxide; 9(11)-DHEP
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
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-
- HY-155780
-
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COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
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-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
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-
- HY-155781
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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-
- HY-162927
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
p53-MDM2-IN-6 (Compound 10a), a LSM-83177 hydrazone analog, is a potent p53-MDM2 inhibitor with an IC50 value of 11.08 µg/mL. p53-MDM2-IN-6 arrests the cell cycle in the S phase and induces early and late Apoptosis with antiproliferative activity against HT29 cell lines with an IC50 value of 10.44 µg/mL. p53-MDM2-IN-6 inhibits p53-MDM2 interaction with increment in p-53 level and decrease the expression of GST enzymes. p53-MDM2-IN-6 is promising for research of colorectal cancer .
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-
- HY-149523
-
|
|
Apoptosis
NO Synthase
Caspase
|
Inflammation/Immunology
Cancer
|
|
Anticancer agent 157 (compound 15) is a NO inhibitor (IC50=0.62 μg/mL) with anti-inflammatory and anticancer activities. Anticancer agent 157 can bind to iNOS (inducible NO synthase) and caspase 8, causing nuclear fragmentation and chromatin condensation, inducing apoptosis. Anticancer agent 157 inhibits HT29 colon cancer cells (IC50=2.45 μg/mL), Hep-G2 liver cancer cells (IC50=3.25 μg/mL), and B16-F10 murine melanoma cells (IC50=3.84 μg/mL) .
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-
- HY-148239
-
-
- HY-147312
-
|
|
Others
|
Cancer
|
|
GSK-1520489A is a PKMYT1 (active protein kinase) inhibitor (IC50=115 nM, Ki=10.94 nM) .
|
-
- HY-N11692
-
|
9-Hydroxystearic acid; 9-HSA
|
HDAC
|
Cancer
|
|
9-Hydroxyoctadecanoic acid (9-HSA) is an HDAC1 inhibitor that inhibits ∼66.4% HDAC1 enzymatic activity at 5 μM. 9-Hydroxyoctadecanoic acid shows anticancer activity .
|
-
- HY-119665
-
|
|
AMPK
mTOR
|
Cancer
|
|
Asteltoxin is an inhibitor for extracellular vesicles (EV), which exhibits inhibitory effects towards mitochondrial ATP synthase and mTORC1 activation .
|
-
- HY-155602
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC50s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells .
|
-
- HY-148253
-
|
|
RIP kinase
|
Neurological Disease
Inflammation/Immunology
|
|
TP-030-1 is an inhibitor of RIPK1. TP-030-1 inhibits hRIPK1 with a Ki value of 3.9 nM and inhibits mRIPK1 with an IC50 value of 4.2 μM. TP-030-1 can be used for the research of inflammatory diseases and neurodegenerative diseases .
|
-
- HY-119892
-
|
NSC 320846; BAY-H 2049
|
Topoisomerase
|
Cancer
|
|
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
|
-
- HY-132003
-
|
|
Akt
|
Cancer
|
|
Wortmannin-Rapamycin Conjugate 1 (compound 7c) is a furan ring-opened derivative of wortmannin-rapamycin conjugate with potent antitumor activities and a fine water solubility. Wortmannin-Rapamycin Conjugate 1 can inhibit the AKT phosphorylation in the tumor and can be used for cancer research .
|
-
- HY-161353
-
|
|
c-Met/HGFR
P-glycoprotein
|
Cancer
|
|
c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC50 = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent .
|
-
- HY-122185
-
|
|
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 211 (AK301) can inhibit tubulin polymerization. Anticancer agent 211 can block the division of human colon cancer cells. Anticancer agent 211 can increase the sensitivity of human colon cancer cells to apoptotic ligands and promote cell apoptosis .
|
-
- HY-141478
-
|
|
ATM/ATR
|
Cancer
|
|
Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity .
|
-
- HY-150755
-
|
|
Topoisomerase
COX
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway .
|
-
- HY-153604
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
|
-
- HY-162569
-
|
|
Apoptosis
Necroptosis
|
Cancer
|
|
Ru-TRZ2 is a potent ruthenium-based chemotherapeutic agent. Ru-TRZ2 induces apoptosis and necroptosis. Ru-TRZ2 shows antitumor activity .
|
-
- HY-136530
-
|
|
KLF
|
Cancer
|
|
SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer .
|
-
- HY-120574
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
|
-
- HY-101089
-
-
- HY-109963
-
-
- HY-146029
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 3 (Compound 3) is an apoptosis inducer that selectively triggers apoptosis and late-apoptosis. Apoptosis inducer 3 shows cytotoxicity against cancer cells .
|
-
- HY-N9588
-
|
|
Others
|
Cancer
|
|
Pedaliin is a bioactive component obtained from the ethanol extract of Sesame (Sesamum indicum L.) leaves (SLs). Pedaliin shows in vitro antioxidant and anti-colon cancer efficacy with radical scavenging activity and ferric reducing antioxidant power (FRAP) .
|
-
- HY-123143
-
|
MLN576
|
Topoisomerase
|
Cancer
|
|
XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
|
-
- HY-160169
-
-
- HY-160169A
-
-
- HY-B1296S1
-
-
- HY-B1296
-
|
(±)-Promethazine
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Promethazine is an orally active histamine receptor antagonist . Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects .
|
-
- HY-147722
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-8 (compound 7i) is a potent and selective hCAIX inhibitor with IC50s of 1.99, 0.024, 1.10 µM for CAII, CAIX, CAVA respectively. hCAIX-IN-8 shows anti-proliferation activity with low toxicity. hCAIX-IN-8 decreases the epithelial to mesenchymal transitions and induces apoptosis. hCAIX-IN-8 inhibits cell migration and colonization potential .
|
-
- HY-114569
-
|
|
Ras
Cyclin G-associated Kinase (GAK)
Autophagy
|
Cancer
|
|
6-CEPN is a RAS inhibitor. 6-CEPN can inhibit RAS activation by binding to Icmt binding sites. 6-CEPN has anticancer activity. 6-CEPN can block cancer cells in the G1 phase. 6-CEPN can induce autophagy and necrosis of Cancer cells (Icmt: isovalerylcysteine carboxymethyltransferase) .
|
-
- HY-161860
-
|
|
Bacterial
|
Cancer
|
|
Antibacterial agent 233 (Compound 7c) exhibits inhibitory efficacy against Helicobacter pylori with MIC of 0.4-1.6 μg/mL. Antibacterial agent 233 inhibits jack bean urease (IC50 is 0.27 μg/mL), changes the permeability of H. pylori cell membrane, causes the leakage of cellular contents. Antibacterial agent 233 exhibits metabolic stability in whole blood and artificial gastric fluid. Antibacterial agent 233 exhibits antitumor efficacy against U2OS in mice .
|
-
- HY-168115
-
|
|
FLT3
PDGFR
|
Cancer
|
|
Multi-kinase inhibitor 4 (compound 14) is an orally active inhibitor of FLT1, KDR, FLT3, FLT4, PDGFRα, PDGFRβ, with IC50s of 1.97 nM, 1.04 nM, 0.33 nM, 1.44 nM, 0.18 nM, 0.89 nM. Multi-kinase inhibitor 4 plays an important role in cancer research .
|
-
- HY-12003
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-13755
-
Sulforaphane
Maximum Cited Publications
42 Publications Verification
|
HDAC
Keap1-Nrf2
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
|
Inflammation/Immunology
Cancer
|
|
Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
|
-
- HY-13755A
-
|
L-Sulforaphane
|
Keap1-Nrf2
Bcl-2 Family
Caspase
Reactive Oxygen Species
NF-κB
|
Inflammation/Immunology
Cancer
|
|
(R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses .
|
-
- HY-108344
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
|
-
- HY-150772
-
|
|
Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
|
-
- HY-159124
-
|
|
Sirtuin
|
Cancer
|
|
YZL-51N is a selective SIRT7 inhibitor with IC50 value of 12.71 μM. YZL-51N disrupts SIRT7 enzyme activity by occupying the NAD + binding pocket, thereby weakening DNA damage repair and inhibiting cancer cell survival. YZL-51N possesses anti-tumor activity and can be used in cancer research .
|
-
- HY-146756
-
|
|
Bacterial
|
Infection
|
|
22-((4-Methoxyphenyl)urea-1-yl)-22-deoxypleuromutilin (compound 6n) is an antibacterial pleuromutilin derivative against Gram-positive pathogens (GPPs) and Mycoplasma pneumoniae .
|
-
- HY-147803
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects .
|
-
- HY-15995
-
|
TubA
|
ADC Cytotoxin
Antibiotic
Microtubule/Tubulin
|
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-123611
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RX-5902
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DNA/RNA Synthesis
Apoptosis
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Cancer
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Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
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- HY-122872
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p38 MAPK
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Cancer
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MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM .
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- HY-162704
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PROTACs
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Cancer
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JMV7048 is an effective PROTAC degrader targeting PXR (Pregnane X Receptor) with a DC50 of 379 nM. JMV7048 induces the polyubiquitination and degradation of PXR protein by recruiting E3 CRBN ubiquitin ligase and the 26S proteasome. JMV7048 significantly enhances the sensitivity of colon cancer stem cells to chemotherapy by reducing the expression of PXR protein in these cells, thereby significantly delaying cancer recurrence in vivo. JMV7048 is composed of the PXR agonist JMV6944 (HY-162738), linker (HY-162736), and Thalidomide 5-fluoride (HY-W087383) (Red: JMV6944; Blue: Thalidomide 5-fluoride ligand; Black: linker) .
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- HY-110374
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Epigenetic Reader Domain
Apoptosis
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Cancer
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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism .
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- HY-163677
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PROTACs
PI3K
Akt
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Cancer
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ARM165 is a heterobifunctional molecule. ARM165 degrades the PIK3CG proteins, inhibits PI3Kγ-Akt signaling pathway, and thus exhibits antileukemia efficacy. ARM165 inhibits proliferations of AML cells, with IC50 <1 μM. (Pink: ligand for target protein PI3Kγ inhibitor AZ2 (HY-111570); Black: linker; Blue: ligand for E3 ligase Pomalidomide (HY-10984))
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- HY-163678
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E3 Ligase Ligand-Linker Conjugates
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Cancer
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Pomalidomide-CO-C7-NH-CO-C3-COOH is a conjugate of a ligand for E3 ligase and a linker. Pomalidomide-CO-C7-NH-CO-C3-COOH can be used for synthesis of PROTAC degrader ARM165 (HY-163677) .
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Product Name |
Target |
Research Area |
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- HY-P3116
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Bacterial
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Cancer
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Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
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- HY-P1435A
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NADPH Oxidase
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Cancer
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NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-121199
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- HY-75564
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- HY-126779
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- HY-N8225
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- HY-121458
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- HY-W727999
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- HY-N12430
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- HY-N8462
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- HY-N8387
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- HY-N3123
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- HY-N3057
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- HY-N12437
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- HY-N8934
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- HY-N10132
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- HY-N3057R
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- HY-N1261
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- HY-N1655
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- HY-N6002
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- HY-N12820
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- HY-N7175
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9,11-Dehydroergosterol peroxide; 9(11)-DHEP
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Structural Classification
Classification of Application Fields
Source classification
Solanum lyratum Thunberg
Solanaceae
Plants
Disease Research Fields
Steroids
Cancer
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Apoptosis
Endogenous Metabolite
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5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
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- HY-N11692
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- HY-N9588
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Flavonoids
Sesamum indicum Linn.
Pedaliaceae
Plants
Isoflavones
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Others
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Pedaliin is a bioactive component obtained from the ethanol extract of Sesame (Sesamum indicum L.) leaves (SLs). Pedaliin shows in vitro antioxidant and anti-colon cancer efficacy with radical scavenging activity and ferric reducing antioxidant power (FRAP) .
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- HY-13755
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- HY-13755A
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* This product has been "discontinued".
Optimized version of product available:
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Product Name |
Chemical Structure |
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- HY-B1296S1
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Promethazine-d4 is a deuterated-labeled promethazine (HY-B0781). Promethazine is an orally active H1 receptor and mAChR antagonist with antihistamine (H1), sedative, antiemetic, anticholinergic, and anti-motion sickness properties .
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Product Name |
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Classification |
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- HY-125387
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Alkynes
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TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
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Product Name |
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Classification |
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- HY-160066
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Aptamers
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SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
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