Search Result
Results for "
H460
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-112037
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IACS-010759
Maximum Cited Publications
26 Publications Verification
IACS-10759
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Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research .
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- HY-164388
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Caspase
Apoptosis
Autophagy
Necroptosis
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Cardiovascular Disease
Cancer
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Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
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- HY-N10503
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Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
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Cancer
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Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
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- HY-P99197
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CP-751871
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IGF-1R
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Cancer
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Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM .
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- HY-101089
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RHPS4
5 Publications Verification
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Telomerase
Apoptosis
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Cancer
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RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer .
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- HY-15259
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Acetyl-CoA Carboxylase
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Metabolic Disease
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CP-640186 is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 can also stimulate muscle fatty acid oxidation .
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- HY-137497
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Ras
Apoptosis
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Cancer
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KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
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- HY-P11115
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Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
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Inflammation/Immunology
Cancer
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CIGB-552 is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 can increase the level of protein COMMD1. CIGB-552 significantly inhibits the NF-κB signaling pathway. CIGB-552 can promote apoptosis of the tumor cells. CIGB-552 can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 has anti-inflammatory and anti-angiogenic effects. CIGB-552 can be used for the research of the lung cancer and colon cancer.
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- HY-116038
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Others
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Cancer
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Kulinone has cytotoxic effects against A549, H460 and HGC27 with IC50 values of 6.2, 7.8, 5.6 μg/mL .
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- HY-149265
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Reactive Oxygen Species (ROS)
TrxR
Ferroptosis
Apoptosis
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Cancer
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ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities .
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- HY-P3139
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PD-1/PD-L1
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Cancer
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TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
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- HY-112037A
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IACS-10759 hydrochloride
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Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research .
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- HY-136265
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Aminoacyl-tRNA Synthetase
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Cancer
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BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
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- HY-177554
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Biochemical Assay Reagents
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Cancer
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KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins .
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- HY-15259A
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Acetyl-CoA Carboxylase
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Metabolic Disease
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CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation .
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- HY-142095
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Histone Methyltransferase
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Cancer
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NSD3-IN-3 is a potent NSD3 inhibtor with an IC50 value of 1.86 μM. NSD3-IN-3 has anticancer activity and significantly inhibits the growth and proliferation of non-small cell lung cancer cell line H460 .
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- HY-168566
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HSP
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Cancer
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EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer .
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- HY-100690
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DNA/RNA Synthesis
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Cancer
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NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer .
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- HY-102066
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AZD-7451
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Trk Receptor
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Cancer
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Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
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- HY-16018A
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ABT-348 hydrochloride
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Aurora Kinase
PDGFR
VEGFR
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Cancer
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Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
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- HY-113638
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GS-456332
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Stearoyl-CoA Desaturase (SCD)
Apoptosis
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Cancer
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CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
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- HY-16018
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ABT-348
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Aurora Kinase
VEGFR
PDGFR
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Cancer
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Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
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- HY-145312
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ATM/ATR
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Cancer
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ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13) .
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- HY-151606
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Akt
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Cancer
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Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomesOsimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
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- HY-123298
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Src
Akt
Apoptosis
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Cancer
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Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
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- HY-161313
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Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
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- HY-168530
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PD-1/PD-L1
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Cancer
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PDL1 degrader-1 (compound PMT-O9-1A) is a potent PD-L1 degrader. PDL1 degrader-1 decreases the protein expression of PD-L1. PDL1 degrader-1 shows cytotoxicity. PDL1 degrader-1 shows anticancer activity .
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- HY-N0867
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HIV
ULK
Bcl-2 Family
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Infection
Cancer
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13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM .13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis .
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- HY-179149
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Polo-like Kinase (PLK)
Apoptosis
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Cancer
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PLK4-IN-6 (compound C05) is an PLK4 inhibitor (IC50 < 0.1 nM). PLK4-IN-6 has anti proliferative activity against various tumor cells, such as IMR-32 (IC50 = 0.948 μM), MCF-7 (IC50 = 0.979 μM), H460 (IC50 = 1.679 μM) cells. PLK4-IN-6 can significantly induce cell apoptosis and block the cell cycle. PLK4-IN-6 can be used for research on various types of cancer .
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- HY-142094
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Histone Methyltransferase
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Cancer
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NSD3-IN-2 is a potent NSD3 inhibitor with an IC50 value of 17.97 μM. NSD3-IN-2 inhibits the growth and proliferation of non-small cell lung cancer cell lines H460, H1299 and H1650 with anti-cancer activity .
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- HY-149086
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RAR/RXR
Apoptosis
PARP
Bcl-2 Family
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Cancer
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BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
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- HY-P10988
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Apoptosis
MDM-2/p53
Integrin
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Cancer
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LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
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- HY-N15267
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FAK
Akt
mTOR
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Cancer
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Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
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- HY-147768
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PI3K
Akt
Microtubule/Tubulin
MMP
Apoptosis
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Cancer
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PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin .
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- HY-163134
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DNA-PK
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Cancer
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DNA-PK-IN-12 (compound 31t) is an oral active DNA-PK inhibitor with the IC50 of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC50 of 33.28 μM, and shows antitumor activity in vivo .
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- HY-W103792
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HDAC
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Cancer
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4-Phenylcinnamic acid is a weak HDAC2 inhiibitor (IC50 > 5 μM). 4-Phenylcinnamic acid has weak cell growth inhibition against tumor cells .
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- HY-P11115A
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Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
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Cancer
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CIGB-552 TFA is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 TFA can increase the level of protein COMMD1. CIGB-552 TFA significantly inhibits the NF-κB signaling pathway. CIGB-552 TFA can promote apoptosis of the tumor cells. CIGB-552 TFA can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 TFA has anti-inflammatory and anti-angiogenic effects. CIGB-552 TFA can be used for the research of the lung cancer and colon cancer.
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- HY-101741
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A-289099
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Microtubule/Tubulin
Apoptosis
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Cancer
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A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
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- HY-P11102
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Bacterial
Fungal
HIV
Parasite
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Infection
Cancer
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Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
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- HY-147724
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-147728
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-169860
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BCRP
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Cancer
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BCRP-IN-2 has BCRP inhibitory activity and shows even greater inhibition of BCRP after activation by ultraviolet light. BCRP-IN-2 can be a valuable probe for studying the interactions of quinazolinamine derivatives with BCRP, as it stimulates ATP hydrolysis of the BCRP transport protein, increasing the accumulation of mitoxantrone (HY-13502) in H460/MX20 cells with BCRP overexpression .
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- HY-157564
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Apoptosis
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Cancer
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Antitumor agent-135 (Compound 13) is a potent antitumor agent. Antitumor agent-135 induces cell apoptosis, with IC50s of 3.79 , 10.55, 1.14, and 4.14 μM for NSCLC cell lines (A549, H460, PC-9, and PC-9/GR) .
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- HY-N12821
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Others
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Cancer
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Visamminol-3'-O-glucoside (Compound 4) is a chromone glycoside, which is initially isolated from Saposhnikovia divaricata. Visamminol-3'-O-glucoside exhibits weak cytotoxicity against cancer cells PC-3, SK-OV-3 and H460, with IC50s of 93.91, >100 and >100 μM, respectively .
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- HY-122552
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Integrin
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Cancer
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Chrysotobibenzyl can be isolated from stem of Dendrobium pulchellum. Chrysotobibenzyl inhibits lung cancer cell (H460 and H292) migration, invasion, filopodia formation via Cav-1, integrins β1, β3, and αν, and EMT suppressions. Chrysotobibenzyl also sensitizes lung cancer cell death mediated by Cisplatin (HY-17394) .
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- HY-173074
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Microtubule/Tubulin
MDM-2/p53
Apoptosis
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Cancer
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Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
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- HY-126803
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Antibiotic
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Infection
Cancer
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Saquayamycin B (compound 3) is a new angucycline antibiotic. Saquayamycin B has antitumor activities against a human lung (H-460) and a human breast cancer cell line (MCF-7) with GI50 values of 12.2 and 15.2 µM respectively .
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- HY-146454
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DNA/RNA Synthesis
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Cancer
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Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
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- HY-155039
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Drug Derivative
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Cancer
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Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
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- HY-164033
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Ramnodigin
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Apoptosis
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Cancer
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HOE 689 (Ramnodigin) is an analog of Digitoxin (HY-B1357). HOE 689 exhibits cytotoxicity to lung cancer cells and induces apoptosis in cancer cell NCI-H460 with an IC50 of 52 nM .
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- HY-N10877
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Others
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Cancer
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Chlorajapolide F is a nature product that could be isolated from the aerial part of Chloranthus japonicas. Chlorajapolide F has low cytotoxic activity against NCI-H460 and SMMC-7721 cell lines .
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- HY-139882
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- HY-147726
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
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- HY-176435
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mTOR
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Cancer
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mTOR inhibitor-28 (SM-3) is a potent mTOR inhibitor. mTOR inhibitor-28 inhibits A549, H292, and H460 cells with IC50s of 72.74, 67.66, and 43.24 μM, respectively .
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- HY-144337
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DNA Alkylator/Crosslinker
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Cancer
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DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
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- HY-169239
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MAGL
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Cancer
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MAGL-IN-20 (compound ±34) is a reversible monoacylglycerol lipase (MAGL) inhibitor. MAGL-IN-20 exhibits appreciable antiproliferative activities against several cancer cells, including H460, HT29, CT-26, Huh7 and HCCLM-3. .
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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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- HY-W560574
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Xanthine Oxidase
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Cancer
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Xanthine oxidase-IN-14 (Compound 3f) is an inhibitor for xanthine oxidase, with IC50 >100 μM. Xanthine oxidase-IN-14 inhibits proliferations of cancer cells MCF-7, NCI-H460 and SF-268, with IC50 greater than 150 μM .
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- HY-123020
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BDA-366 analog
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Bcl-2 Family
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Cancer
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CYD-2-88 (BDA-366 analog) is a BDA-366 (HY-101083) (Bcl2 BH4 antagonist) analog. CYD-2-88 (20 mg/kg, i.p.) inhibits tumor growth in NSCLC H460 xenografts mice .
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- HY-117872
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20-O-Acetylsartorypyrone D
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Fungal
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Infection
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Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
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- HY-147725
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Microtubule/Tubulin
|
Cancer
|
|
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-N10876
-
|
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Others
|
Others
|
|
8-epi-Chlorajapolide F (compound 1) a sesquiterpene that can be isolated from the aboveground part of the Chloranthus japonicus. 8-epi-Chlorajapolide has few cytotoxic to human cancer cell lines NCI-H460 and SMMC-7721 (IC50s>50 μg/mL) .
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-
- HY-147727
-
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Microtubule/Tubulin
|
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-144335
-
|
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DNA Alkylator/Crosslinker
|
Cancer
|
|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
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-
- HY-146274
-
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c-Met/HGFR
Apoptosis
|
Cancer
|
|
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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-
- HY-119694
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Fungal
|
Cancer
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Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
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-
- HY-155522
-
|
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Carbonic Anhydrase
|
Cancer
|
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
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-
- HY-162896
-
|
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DNA/RNA Synthesis
|
Cancer
|
|
And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research .
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- HY-169476
-
|
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Drug Derivative
|
Cancer
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|
Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
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-
- HY-P3139A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
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-
- HY-180183
-
|
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Epigenetic Reader Domain
|
Cancer
|
|
DLG-41 is a GAS41 YEATS domain inhibitor (IC50: 600 nM in AlphaLISA). DLG-41 potently disrupts the association of GAS41 YEATS with chromatin in cells. DLG-41 strongly enhances levels of CDKN1A. DLG-41 has anticancer activity against NSCLC .
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-
- HY-112749B
-
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Heme Oxygenase (HO)
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
|
Cancer
|
|
(3S,4R)-ME-344 is the (3S,4R)-enantiomer of ME-344 (HY-112749). ME-344 is a mitochondrial Heme oxygenase 1 (HO-1) inhibitor. ME-344 specifically binds and alters HO-1 structure, and increases HO-1 translocation from the rough endoplasmic reticulum to mitochondria, but only in drug-sensitive cells (such as H460 and SHP-77 cells). ME-344 decreases mitochondrial ATP production and induces ROS, with subsequent disruption of redox homeostasis and mitochondrial function. ME-344 has significant antitumor activity, and can be used for cancers like breast cancer research .
|
-
- HY-169262
-
|
|
Phospholipase
Apoptosis
|
Cancer
|
|
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
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-
- HY-124456
-
|
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Bacterial
|
Infection
|
|
Unguinol is a depsidone originally isolated from A. unguis. It is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50=42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation. Unguinol also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s=8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s=28.2, 50.8, and 44.3 μM, respectively).
|
-
- HY-145394
-
|
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CDK
|
Cancer
|
|
CDK7-IN-6 is a potent and selective cyclin-dependent kinase (CDK7) inhibitor (IC50≤100 nM), extracted from patent WO2019197549 A1, compound 210. CDK7-IN-6 is > 200-fold selective for CDK7 over CDK1, CDK2, and CDK5. CDK7-IN-6 can be used for the research of cancer .
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-
- HY-149968
-
|
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Histone Demethylase
Apoptosis
|
Cancer
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|
LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis .
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-
- HY-174314
-
|
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Ligands for Target Protein for PROTAC
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
WZH-15-125 is a potent ALK inhibitor. WZH-15-125 can effectively overcome drug resistance, especially compound ALK mutations. WZH-15-125 has an IC50 of 101.7 nM for the highly refractory G1202R/L1196M mutation that is resistant to Lorlatinib (HY-12215). WZH-15-125 can be used as a PROTAC target protein ligand to synthesize PROTAC WZH-17-002 (HY-174315). WZH-15-125 can be used in the research of non-small cell lung cancer .
|
-
- HY-138098
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
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-
- HY-157319
-
|
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PI3K
|
Cancer
|
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
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-
- HY-139090
-
|
28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin
|
Bacterial
HIV
Drug Derivative
|
Cancer
|
|
3-Oxobetulin acetate (28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin) is a derivative of betulin (HY-N0083), a cholesterol biosynthesis inhibitor. 3-Oxobetulin acetate inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL) and human MCF-7 breast cancer, SF-268 CNS cancer, H460 lung cancer, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL), but not BxPC-3 pancreatic cancer cells or DU145 prostate cancer cells (GI50s=>10 μg/mL for both). 3-Oxobetulin acetate inhibits the replication of X4-tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). 3-Oxobetulin acetate is also effective against Listeria donovani amastigotes.
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-
- HY-N10949
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|
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Others
|
Cancer
|
|
Viscosalactone B is a withanolide found in Withania somnifera. Viscosalactone B shows potent inhibitory activities to NCI-H460, HCT-116, MCF-7 and SF-268 cancer cells with IC50 values of 0.32, 0.47, 0.4 and 0.45 μg/mL. Viscosalactone B can be used for the research of cancer .
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-
- HY-161649
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
|
Cancer
|
|
hCYP1B1-IN-2 (compound 3n) is a potent human cytochrome P450 1B1 enzyme hCYP1B1 inhibitor. hCYP1B1-IN-2 shows the extremely potent anti-hCYP1B1 activity (IC50=0.040 nM) and blocks AhR transcription activity. hCYP1B1-IN-2 potently inhibits hCYP1B1 via a mix inhibition manner, showing a Ki value of 21.71 pM .
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-
- HY-156346
-
|
|
SARS-CoV
|
Infection
|
|
HCoV-OC43-IN-1 (Compound IV-16) is a coronavirus HCoV-OC43 inhibitor. HCoV-OC43-IN-1 has antiviral efficacy (EC50: 90 nM). HCoV-OC43-IN-1 inhibits the mRNA level and expression of viral nucleocapsid protein (NP) .
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-
- HY-N9489
-
|
|
Others
|
Cancer
|
|
Phoyunnanin E, isolated from Dendrobium venustum, possesses anti-migration activity. Phoyunnanin E can be used for the research of cancer .
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-
- HY-162711
-
|
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DNA/RNA Synthesis
|
Cancer
|
|
Methylbiocin is an ATP competitive inhibitor for human CMG helicase with an IC50 of 59 µM. Methylbiocin exhibits potential in cancer research .
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-
- HY-118988
-
|
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PPAR
Apoptosis
|
Cancer
|
|
CAY10506 is a PPARγ ligand that can induce cell death and ROS production in a PPARγ-dependent manner in vitro. CAY10506 exhibits radiosensitizing effects, enhancing γ-radiations-induced apoptosis and caspase-3-mediated poly (ADP-ribose) polymerase (PARP) cleavage. CAY10506 can be used in cancer research .
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-
- HY-150511
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity .
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-
- HY-179321
-
|
|
PROTACs
HDAC
|
Cancer
|
|
PROTAC HDAC4 Degrader-1 (compound SCT-1) is a potent and selective PROTAC HDAC4 degrader. PROTAC HDAC4 Degrader-1 reduces HDAC4 protein level, induces S phase cell cycle arrest, and inhibits cell colony formation, thereby inhibiting proliferation of the tumor cells. PROTAC HDAC4 Degrader-1 exhibits efficacy in a H460 mouse model. PROTAC HDAC4 Degrader-1 can be used for cancer research, such as lung cancer .
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-
- HY-150576
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-13 is a potent c-Met inhibitor with an IC50 value of 2.43 nM. c-Met-IN-13 shows excellent cytotoxicity for cancer cells. c-Met-IN-13 shows antiproliferative activity in a concentration- and time- dependent manner. c-Met-IN-13 has the potential for the research of cancer .
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-
- HY-150571
-
|
|
Topoisomerase
c-Myc
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 76 (Compound CT2-3) is an anticancer agent. Anticancer agent 76 significantly inhibits the proliferation of human NSCLC cells, induces cell cycle arrest, causes ROS generation and induces cell apoptosis .
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-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
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-
- HY-168210
-
|
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Fungal
Cytochrome P450
|
Infection
|
|
Antifungal agent 122 (compound 201) is a potent and broad-spectrum antifungal agent. Antifungal agent 122 prevents fungal phase transition and the formation of fungal biofilm. Antifungal agent 122 inhibits CYP3A4-M and CYP3A4-T enzyme activity with IC50 values of 2.11, 4.53 µM. Antifungal agent 122 shows no cytotoxicity .
|
-
- HY-155040
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Antitumor agent-106 (compound 42) is an anticancer agent that exhibits good inhibitory activity (IC50=4.2-6.6 µM) against both lung cancer and colon cancer cell lines .
|
-
- HY-150719
-
-
- HY-168267
-
|
|
Deubiquitinase
|
Infection
Cancer
|
|
XH161-180 is a potent and orally active ubiquitin carboxyl-terminal hydrolase 2 (USP2) inhibitor. XH161-180 decreases the protein of cyclin D and ACE2. XH161-180 shows antiproliferative activity. XH161-180 has the potential for the research of cancer and virus infection depending on ACE2 .
|
-
- HY-180562
-
|
|
Ras
|
Cancer
|
|
KARS-IN-1 (152) is a AKR1C3 dependent KARS inhibitor with an AC50 of 9.1 nM for human KARS. KARS-IN-1 shows anti-proliferative activity in H460 (NRF2 pathway mutant cell line with high AKR1C3 expression) and Hara (NRF2 pathway wild type cell line with low AKR1C3 expression), with AC50 values ??of 21 nM and 16 nM, respectively. KARS-IN-1 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-180853
-
|
|
PI3K
Akt
mTOR
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
PI3K/Akt/mTOR-IN-6 (Compound JW4) is an orally active PI3K/Akt/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-6 induces Apoptosis in cells via the mitochondrial pathway. PI3K/Akt/mTOR-IN-6 shows potent anti-NSCLC activity .
|
-
- HY-101089R
-
|
|
Telomerase
Reference Standards
Apoptosis
|
Cancer
|
|
RHPS4 (Standard) is the analytical standard of RHPS4 (HY-101089). This product is intended for research and analytical applications. RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer .
|
-
- HY-102066R
-
|
AZD-7451 (Standard)
|
Reference Standards
Trk Receptor
|
Cancer
|
|
Utatrectinib (Standard) is the analytical standard of Utatrectinib (HY-102066). This product is intended for research and analytical applications. Utatrectinib (AZD-7451) is a potent, selective and orally active Trk inhibitor. Utatrectinib blocks TrkC activation and associated tumorigenic behaviors .
|
-
- HY-158969
-
|
|
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
|
EGFR-IN-113 (compound II-1) is an EGFR kinase inhibitor with an IC50 of 14.79 μM. EGFR-IN-113 can induce apoptosis and inhibit cell proliferation by downregulating Akt and Erk1/2 signaling. EGFR-IN-113 can be used for research in EGFR-driven cancers, such as lung cancer, pancreatic cancer, and breast cancer .
|
-
- HY-N11060A
-
|
(±)-PBI 344
|
Others
|
Cancer
|
|
(±)-Dehydrovomifoliol ((±)-PBI 344) is a norisoprenoid found in the rhizomes of Sinomenium acutum. (±)-Dehydrovomifoliolshows no significant cytotoxic activity against cancer cells .
|
-
- HY-P11198
-
|
|
Apoptosis
VEGFR
ERK
Akt
Caspase
Bcl-2 Family
|
Cancer
|
|
AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research .
|
-
- HY-146276
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
|
-
- HY-111033
-
|
|
MEK
ERK
Apoptosis
p38 MAPK
CDK
PARP
|
Inflammation/Immunology
Cancer
|
|
RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research .
|
-
- HY-170954
-
|
|
Apoptosis
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity .
|
-
- HY-179614
-
|
|
PARP
DNA/RNA Synthesis
Apoptosis
CDK
Bcl-2 Family
|
Cancer
|
|
PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer .
|
-
- HY-181890
-
|
|
Glutaminase
|
Cancer
|
|
TRG-192 is a potent and selective glutaminase (GLS) inhibitor with an IC50 of 68 nM. TRG-192 inhibits intracellular glutamate levels. TRG-192 is applicable to related research on non-small cell lung cancer .
|
-
- HY-10226R
-
|
R306465 (Standard)
|
Reference Standards
Apoptosis
HDAC
|
Cancer
|
|
JNJ-16241199 (Standard) is the analytical standard of JNJ-16241199 (HY-10226). This product is intended for research and analytical applications. JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases
the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-10226
-
|
R306465
|
Apoptosis
HDAC
|
Cancer
|
|
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC50of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases
the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-110374
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
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 . NVS-CECR2-1 is a chemical probe.
|
-
- HY-124084
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Cancer
|
|
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
|
-
- HY-15957
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
FASN-IN-7 is a potent and orally active inhibitor of human Fatty Acid Synthase (FASN). FASN-IN-7 shows enzyme inhibition on full length FASN and the FASN KR domain with IC50 values of 28 and 54 nM. FASN-IN-7 effectively inhibits proliferation of multiple cancer cell types. FASN-IN-7 increases malonyl-CoA levels and decreases palmitate levels in tumor tissues .
|
-
- HY-183592
-
|
|
Orthopoxvirus
Drug Derivative
|
Infection
|
|
Anti-virus agent 2 is an orally active and selective anti-orthopoxvirus (poxvirus) agent, with EC50 values of 6.1 μM and 47.1 μM against VTT-Fluc and MPXV clade IIb, respectively. Anti-virus agent 2 covalently binds to viral A17L protein and mRNA methyltransferase, blocks viral membrane fusion and intracellular biosynthesis, and acts on multiple stages of the viral replication cycle. Anti-virus agent 2 achieves viral inhibition in nude mouse models. Anti-virus agent 2 can be used for the research of orthopoxvirus infections such as monkeypox and smallpox .
|
-
- HY-106381
-
|
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Aurothiomalate sodium is a potent and selective oncogenic PKCι signaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cell apoptosis. Aurothiomalate sodium is a potent thioredoxin reductase (TrxR) inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity .
|
-
- HY-134911
-
|
|
IRAK
CDK
|
Inflammation/Immunology
Cancer
|
|
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity .
|
-
- HY-147409
-
|
|
CDK
|
Cancer
|
|
Ulecaciclib is an orally activitive inhibitor of cyclin-dependent kinase (CDK), with Ki values of 0.62 μM (CDK2/Cyclin A), 0.2 nM (CDK4/Cyclin D1), 3 nM (CDK6/Cyclin D3), and 0.63 μM (CDK7/Cyclin H), respectively. Ulecaciclib can cross blood brain barrier and has good pharmacokinetic characteristics .
|
-
- HY-P11143A
-
|
|
Interleukin Related
Liposome
|
Cancer
|
|
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
|
-
- HY-162753
-
|
|
P-glycoprotein
|
Cancer
|
|
ZW-1226 is a dual Tyrosyl DNA phosphodiesterase 2 (TDP2) and Multidrug resistance-associated protein 1 (MRP1) inhibitor with IC50 values of 0.2 and 0.5 μM, respectively. ZW-1226 exhibits selectivity over other ABC transporters. ZW-1226 elevates intracellular GSH levels, and reverses MRP1-mediated drug resistance. ZW-1226 can be used for the research of leukemia, non-small-cell lung cancer, and multidrug resistant small-cell lung cancer .
|
-
- HY-17026A
-
|
dFdCTP
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
- HY-172364
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research .
|
-
- HY-N10549
-
|
|
Ferroptosis
c-Myc
Glutathione Peroxidase
JNK
Reactive Oxygen Species (ROS)
GSK-3
|
Infection
Metabolic Disease
Cancer
|
|
Gigantol is an orally active bibenzyl compound. Gigantol targets MYC to promote its ubiquitin-proteasomal degradation and inhibit the growth of lung cancer cells. Gigantol exerts anti-lung cancer activity by inducing ferroptosis (Ferroptosis) via the SLC7A11-GPX4 axis. Gigantol restores the sensitivity of mcr-harboring multidrug-resistant bacteria to colistin. Gigantol ameliorates carbon tetrachloride-induced liver injury by inhibiting the activation of the JNK/cPLA2/12-LOX inflammatory pathway. Gigantol promotes cholesterol metabolism and progesterone biosynthesis in Leydig cells. Gigantol can be used in studies related to diseases such as lung cancer, multidrug-resistant Gram-negative bacterial infections, and acute liver injury .
|
-
- HY-183327
-
|
|
PI3K
mTOR
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Bcl-2 Family
Caspase
|
Cancer
|
|
PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models .
|
-
- HY-121811
-
|
Lanceolatin C
|
Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Pongamol is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
|
-
- HY-171171
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NERx 329 is a replication protein A (RPA) inhibitor with an IC50 of 4.9 μM. NERx 329 blocks the interaction between RPA and single-stranded DNA, and induces functional RPA depletion, loss of single-stranded DNA gap protection, chromosome fragmentation and cell death. NERx 329 inhibits the DNA damage response signaling pathway, exhibits broad single-agent anticancer activity, and enhances the activity of DNA-damaging agents. NERx 329 can be used in research related to brca1-deficient breast cancer, non-small cell lung cancer, and brca1-deficient ovarian cancer .
|
-
- HY-N0660
-
|
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-164388
-
|
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
|
-
- HY-P11115
-
|
|
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
CIGB-552 is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 can increase the level of protein COMMD1. CIGB-552 significantly inhibits the NF-κB signaling pathway. CIGB-552 can promote apoptosis of the tumor cells. CIGB-552 can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 has anti-inflammatory and anti-angiogenic effects. CIGB-552 can be used for the research of the lung cancer and colon cancer.
|
-
- HY-P3139
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-113638
-
|
GS-456332
|
Stearoyl-CoA Desaturase (SCD)
Apoptosis
|
Cancer
|
|
CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer .
|
-
- HY-P10988
-
|
|
Apoptosis
MDM-2/p53
Integrin
|
Cancer
|
|
LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model .
|
-
- HY-P11115A
-
|
|
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
|
Cancer
|
|
CIGB-552 TFA is a cell-penetrating peptide with anti-tumor properties with the IC50 of 23 μM in H460 cells. CIGB-552 TFA can increase the level of protein COMMD1. CIGB-552 TFA significantly inhibits the NF-κB signaling pathway. CIGB-552 TFA can promote apoptosis of the tumor cells. CIGB-552 TFA can induce the accumulation of reactive oxygen species (ROS) in tumor cells. CIGB-552 TFA has anti-inflammatory and anti-angiogenic effects. CIGB-552 TFA can be used for the research of the lung cancer and colon cancer.
|
-
- HY-P11102
-
|
|
Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
|
|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
|
-
- HY-P3139A
-
|
|
PD-1/PD-L1
|
Cancer
|
|
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a high affinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
|
-
- HY-P11198
-
|
|
Apoptosis
VEGFR
ERK
Akt
Caspase
Bcl-2 Family
|
Cancer
|
|
AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research .
|
-
- HY-P11143A
-
|
|
Interleukin Related
Liposome
|
Cancer
|
|
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99197
-
|
CP-751871
|
IGF-1R
|
Cancer
|
|
Figitumumab (CP-751871) is a potent and fully human monoclonal anti–insulin-like growth factor 1 receptor (IGF1R) antibody. Figitumumab prevents IGF1 from binding to IGF1R with an IC50 of 1.8 nM .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N10503
-
|
|
Flavonoids
Flavones
Plants
Moraceae
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
-
- HY-N0660
-
|
|
Cardiovascular Disease
Triterpenes
Structural Classification
other families
Classification of Application Fields
Terpenoids
Plants
Disease Research Fields
Source Classification
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
-
- HY-116038
-
-
-
- HY-17026A
-
|
dFdCTP
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
-
- HY-N10549
-
-
-
- HY-121811
-
|
Lanceolatin C
|
Structural Classification
Pongamia pinnata (L.) Pierre
Leguminosae
Ketones, Aldehydes, Acids
Derris trifoliata Lour.
Plants
Source Classification
|
Glycosidase
Phosphatase
Interleukin Related
TNF Receptor
COX
Beclin1
GLUT
FAK
Akt
mTOR
p38 MAPK
Keap1-Nrf2
Apoptosis
Amyloid-β
Tau Protein
Autophagy
|
|
Pongamol is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia .
|
-
-
- HY-123298
-
-
-
- HY-N0867
-
-
-
- HY-N15267
-
|
|
Natural Products
Millettia peguensis Ali
Leguminosae
Plants
Source Classification
|
FAK
Akt
mTOR
|
|
Ovalitenone is a flavonoid compound that can be isolated from the plant Millettia peguensis. It shows no cytotoxic effects on lung cancer H460 and A549 cells, but it significantly inhibits anchorage-independent growth, CSC-like phenotypes, colony formation, and the migration and invasion capabilities of cancer cells. Ovalitenone can significantly reduce the levels of N-cadherin, snail, and slug, while increasing E-cadherin, thus inhibiting the EMT pathway. Additionally, Ovalitenone suppresses the signaling pathways regulated by focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42) .
|
-
-
- HY-N12821
-
-
-
- HY-122552
-
-
-
- HY-126803
-
-
-
- HY-N10877
-
-
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Fungal
|
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
-
- HY-N10876
-
-
-
- HY-138098
-
-
-
- HY-N10949
-
-
-
- HY-N9489
-
-
-
- HY-N11060A
-
-
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