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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
49 Results for "
TOP1
" in MedChemExpress (MCE) Product Catalog:
Products (49)
49 Results for "TOP1" in MCE Product Catalog:
Cat. No.: HY-107133A
CAS No.: 951290-31-6
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Simmitecan is a potent topoisomerase I (TOP1) inhibitor, which is a 9-substituted lipophilic camptothecin (Camptothecin (HY-16560)) derivative. Simmitecan blocks DNA replication and transcription, thereby inducing tumor cell apoptosis by inhibiting the activity of TOP1. Simmitecan can be used in the research of cancers such as liver cancer [1] .
Cat. No.: HY-W1063697
CAS No.: 19506-19-5
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5,8-Dimethoxyquinoxaline is a drug intermediate that can be used in studies related to organic synthesis. The derived cyclization product of 5,8-Dimethoxyquinoxaline specifically blocks TOP1-mediated DNA cleavage reactions [1] .
Cat. No.: HY-184984
CAS No.: 3110372-70-5
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SN-38-A2 is a topoisomerase I (TOP1) degrader with an IC50 of 6.2 nM in MIA PaCa-2 pancreatic cancer cells. SN-38-A2 mimics protein misfolding via an adamantane hydrophobic tag, hijacks the HSP90 chaperone system, and mediates TOP1 degradation through the ubiquitin-proteasome system. SN-38-A2 assembles with poly β-cyclodextrin to form pH-responsive nanoparticles, enabling site-specific release under the acidic conditions of the tumor microenvironment, and exhibits tumor growth inhibitory effects in MIA PaCa-2 pancreatic cancer and HCT116 colorectal cancer xenograft models. SN-38-A2 can be used in research related to pancreatic cancer, colorectal cancer, and breast cancer [1].
Cat. No.: HY-184245
CAS No.: 3117528-53-4
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Hsp90-IN-48 is an orally active Hsp90 inhibitor with an IC50 of 19.4 nM. Hsp90-IN-48 improves tumor-cell uptake and intracellular active-component release, and suppresses tumor metastasis. Hsp90-IN-48 induces G2/M phase cell cycle arrest and tumor cell apoptosis whlie simultaneously inhibits Top1/Top2 activity. Hsp90-IN-48 inhibits tumor growth and can be used for colon cancer research [1].
Cat. No.: HY-188120
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AZD5335 is an ADC targeting FRα, with an IC50 of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research [1].
Cat. No.: HY-180555
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SN38-(PEG)2-Pom-α is a selective PROTAC RPL15 degrader. SN38-(PEG)2-Pom-α induces ubiquitin-mediated degradation of RPL15 without affecting TOP1. SN38-(PEG)2-Pom-α induces damage-associated molecular pattern (DAMP) secretion from cancer cells, which activated cGAS-STING signaling in dendritic cells. SN38-(PEG)2-Pom-α enhances anti-PD-1 immunotherapy in a murine melanoma tumor model expressing human CRBN. SN38-(PEG)2-Pom-α can be used for melanoma research [1].
Cat. No.: HY-W654323
CAS No.: 2468637-62-7
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PNU-142586 sodiu) is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
