Search Result
Results for "
DNA topoisomerase I inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15142
-
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Hydroxydaunorubicin hydrochloride; ADR
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Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
Fluorescent Dye
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Infection
Cancer
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Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride; ADR), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
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- HY-13631D
-
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Exatecan derivative for ADC
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Topoisomerase
ADC Payload
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Cancer
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DXd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
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-
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- HY-16562
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-
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- HY-13631
-
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DX-8951
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ADC Payload
Topoisomerase
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Cancer
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Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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-
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- HY-13631A
-
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DX8951f
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ADC Payload
Topoisomerase
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Cancer
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Exatecan mesylate (DX8951f) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research.
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- HY-16560
-
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Campathecin; (S)-(+)-Camptothecin; CPT
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Topoisomerase
ADC Payload
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
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Infection
Cancer
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Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
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-
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- HY-13631AS
-
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DX8951f-d5; Deuterated labeled Exatecan mesylate
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Isotope-Labeled Compounds
ADC Payload
Topoisomerase
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Cancer
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Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
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-
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- HY-42487
-
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ADC Payload
Topoisomerase
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Cancer
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Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects .
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-
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- HY-148668
-
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SHR-A1811 Drug-linker
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
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MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan (SHR-A1811 Drug-linker) is a agent-linker conjugates for ADC, consisting Exatecan (HY-13631). Exatecan is a DNA Topoisomerase I inhibitor (IC50=2.2 μM) .
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- HY-13566
-
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CKD-602 free base
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Topoisomerase
Apoptosis
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Cancer
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Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
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-
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- HY-13631R
-
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DX-8951 (Standard)
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ADC Payload
Reference Standards
Topoisomerase
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Cancer
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Exatecan (Standard) is the analytical standard of Exatecan. This product is intended for research and analytical applications. Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
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- HY-13631DS
-
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Exatecan-d5 derivative for ADC
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Topoisomerase
ADC Payload
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Cancer
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DXd-d5 is a deuterium labeled DXd. DXd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
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- HY-131057
-
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Drug-Linker Conjugates for ADC
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Cancer
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Mc-VC-PAB-SN38 consists a cleavable ADC linker (Mc-VC-PAB) and a DNA topoisomerase I inhibitor (SN38). Mc-VC-PAB-SN38 can be used in the synthesis of antibody-drug conjugates (ADCs) .
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- HY-15142A
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- HY-156617A
-
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SHR169265
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ADC Payload
Topoisomerase
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Cancer
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(αR)-Cyclopropaneacetamide-Exatecan (SHR169265) is a DNA Topoisomerase I inhibitor with enhanced membrane permeability (with an IC50 of 1.34 μM against the human DNA Topoisomerase I). (αR)-Cyclopropaneacetamide-Exatecan exerts cytotoxic effects by inhibiting the enzymatic activity of Topoisomerase I, and this anticancer effect is independent of the expression level of HER2. (αR)-Cyclopropaneacetamide-Exatecan is an ADC Cytotoxin derived from Exatecan (HY-13631), which can be used in research related to advanced cancers such as breast cancer, gastric cancer, colorectal cancer and non-small cell lung cancer .
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- HY-B1099
-
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DNA/RNA Synthesis
Topoisomerase
Parasite
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Infection
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Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
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- HY-13631AG
-
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DX8951f
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ADC Payload
Topoisomerase
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Cancer
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
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- HY-156755
-
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Drug-Linker Conjugates for ADC
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Cancer
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Propargyl-PEG4-GGFG-DXd is a drug-linker conjugate for ADC. Propargyl-PEG4-GGFG-DXd contains a ADC linker and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
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- HY-13744
-
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RFS 2000; 9-Nitrocamptothecin
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Topoisomerase
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Cancer
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Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells .
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- HY-156848
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Drug-Linker Conjugates for ADC
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Cancer
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Fmoc-GGFG-DXd is a drug-linker conjugate for ADC. Fmoc-GGFG-DXd contains a ADC linker Fmoc-GGFG and a DNA topoisomerase I inhibitor DXd (HY-13631D) .
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- HY-153013
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Drug-Linker Conjugates for ADC
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Cancer
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SN38-COOH is used for the synthesis of antibody-drug conjugates (ADCs). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis .
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- HY-164835
-
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SMP-54418
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Drug-Linker Conjugates for ADC
Microtubule/Tubulin
Topoisomerase
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Cancer
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VcMMAE-Deruxtecan (SMP-54418) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule MMAE (HY-15162) (Microtubule inhibitor) and Exatecan (HY-13631) (DNA topoisomerase I inhibitor). VcMMAE-Deruxtecan can be used for ADC synthesis.
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- HY-N3488
-
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Topoisomerase
Bacterial
Fungal
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Infection
Cancer
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Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities .
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- HY-13758A
-
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BMS-247615 dihydrochloride
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Topoisomerase
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Cancer
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TAS-103 dihydrochloride is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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- HY-U00248A
-
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MJ-III65 hydrochloride; NSC706744 hydrochloride
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Topoisomerase
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Cancer
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LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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- HY-175203
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- HY-136170
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MC-SN38
2 Publications Verification
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Drug-Linker Conjugates for ADC
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Cancer
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MC-SN38 is a agent-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody agent conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks .
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- HY-43565
-
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ADC Payload
Topoisomerase
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Cancer
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Exatecan intermediate 9 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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- HY-U00248
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MJ-III65; NSC706744
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Topoisomerase
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Cancer
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LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity .
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- HY-148668A
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- HY-158137
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Drug-Linker Conjugates for ADC
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Cancer
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Val-Cit-PAB-DEA-Dxd (compound 81) is a Drug-Linker Conjugates for ADC, which is composed of a linker and a toxic molecule Dxd (DNA topoisomerase I inhibitor). Val-Cit-PAB-DEA-Dxd can be used for ADC synthesis .
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- HY-177546
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- HY-13618
-
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J 107088; PF 804950
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Topoisomerase
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Cancer
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Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
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- HY-101647
-
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RP 60475
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Topoisomerase
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Cancer
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Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
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- HY-159783
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- HY-16562S1
-
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Isotope-Labeled Compounds
Topoisomerase
Autophagy
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Cancer
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Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-160774
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Drug-Linker Conjugates for ADC
Topoisomerase
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Cancer
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Val-Cit-PABC-DOX (compound 10109), an epsilon-poly-L-lysine-based drug conjugate, is an agent-linker conjugate for ADC by using a DNA topoisomerase I and topoisomerase II inhibitor, Doxorubicin (HY-15142), linked via the linker, Val-Cit-PABC .
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- HY-145078
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Drug-Linker Conjugates for ADC
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Cancer
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PNU-EDA-Gly5 is an oligo-glycine linker-payload for ADC synthesis, composed of a DNA topoisomerase I inhibitor PNU-159682 and a linker EDA-Gly5 .
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- HY-125331
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Topoisomerase
ADC Payload
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Cancer
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DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype .
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- HY-13758
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TAS-103
1 Publications Verification
BMS-247615
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Topoisomerase
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Cancer
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TAS-103 is a dual inhibitor of DNA topoisomerase I/II, used for cancer research.
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- HY-13631P
-
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DX-8951 mesylate dihydrate
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ADC Payload
Topoisomerase
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Cancer
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Exatecan (DX-8951) mesylate dihydrate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
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- HY-49556
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Topoisomerase
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Cancer
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(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate is an intermediate reactant in the synthesis of Camptothecin (HY-16560). Camptothecin is an inhibitor of the DNA topoisomerase Topo I, withIC50=679 nM .
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- HY-164836
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- HY-18351A
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LMP-400 hydrochloride; NSC-724998 hydrochloride
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Topoisomerase
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Infection
Cancer
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Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
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- HY-19825
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Topoisomerase
ADC Payload
Antibiotic
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Cancer
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Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II .
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- HY-162587
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Topoisomerase
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Cancer
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Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors .
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- HY-128994
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Drug Intermediate
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Cancer
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GGFG-Exatecan is a synthetic intermediate for drug-linker conjugates used in antibody-drug conjugates (ADCs). GGFG-Exatecan consists of a glycyl-glycyl-phenylalanyl-glycine (GGFG) tetrapeptide linker and a DNA topoisomerase I inhibitor Exatecan (HY-13631). GGFG-Exatecan can be used for the study of cancer .
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- HY-179520
-
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Topoisomerase
DNA/RNA Synthesis
MDM-2/p53
Bcl-2 Family
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Cancer
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XSJ151 is a topoisomerase I inhibitor, stabilizing the DNA-Topo I covalent complex and inducing DNA double-strand breaks. XSJ151-induces DNA damage activates the p53-p21 signaling pathway, specifically regulating the expression of cyclins, leading to G2/M phase cell cycle arrest and disrupting the dynamic homeostasis of Bcl-2 family proteins, thereby triggering apoptosis in gastric cancer cells. XSJ151 can be used for the study of gastric cancer .
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- HY-143265
-
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Topoisomerase
Apoptosis
Caspase
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Cancer
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Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect .
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- HY-144774
-
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Topoisomerase
DNA/RNA Synthesis
Apoptosis
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Cancer
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Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
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- HY-125930
-
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Topoisomerase
DNA/RNA Synthesis
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Cancer
|
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T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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- HY-178373
-
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Topoisomerase
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
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Cancer
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Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer .
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- HY-W713570
-
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Topoisomerase
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Cancer
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Nectandrin B is an inhibitor of DNA topoisomerases I and II, which is found in Saururus chinensis. Nectandrin B is promising for research of cancers .
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- HY-13631AS1
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- HY-101647A
-
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RP 60475 dimesylate
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Topoisomerase
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Cancer
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Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA .
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- HY-48878
-
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ADC Payload
Topoisomerase
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Cancer
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Exatecan analog 36 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
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- HY-42487R
-
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ADC Payload
Reference Standards
Topoisomerase
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Cancer
|
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Exatecan Intermediate 1 (Standard) is the analytical standard of Exatecan Intermediate 1. This product is intended for research and analytical applications. Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects .
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- HY-156723
-
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Topoisomerase
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Cancer
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9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a novel camptothecin derivatives. 9-Chloromethyl-10-hydroxy-11-F-Camptothecin is a DNA topoisomerase I (Topo I) inhibitor, can be used in anticancer research .
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- HY-143266
-
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase .
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- HY-16562S
-
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(+)-Irinotecan-d10; CPT-11-d10; VAL-413-d10free base
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Topoisomerase
Autophagy
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Cancer
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Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-146437
-
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases .
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- HY-N15319
-
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Canangine
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Topoisomerase
Fungal
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Infection
|
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Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases .
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- HY-125930A
-
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Topoisomerase
DNA/RNA Synthesis
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Cancer
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T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death .
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- HY-16562R
-
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(+)-Irinotecan (Standard); CPT-11 (Standard); VAL-413free base (Standard)
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Reference Standards
Topoisomerase
Autophagy
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Cancer
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Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
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- HY-119892
-
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NSC 320846; BAY-H 2049
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Topoisomerase
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Cancer
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Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .
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- HY-161385
-
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Topoisomerase
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Cancer
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Topoisomerase I inhibitor 21 (Compound 3e) is an inhibitor for Topoisomerase I through stabilization of enzyme-DNA complex. Topoisomerase I inhibitor 21 exhibits antiproliferative activity in 39 human cancer cells (JFCR39) with mean GI50 39 nM .
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- HY-N10115
-
-
- HY-143402
-
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Topoisomerase
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Cancer
|
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Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
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- HY-120185
-
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UCT-1003
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Topoisomerase
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Infection
Cancer
|
|
Saintopin is an antitumor antibiotic. Saintopin is also an inhibitor of DNA topoisomerases I and II. Saintopin induces DNA cleavage .
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- HY-168739
-
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Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
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Cancer
|
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Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
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- HY-13565
-
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NSC 655649; BMS 181176; BMY 27557
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Topoisomerase
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Cancer
|
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Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
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- HY-N10367
-
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Topoisomerase
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Cancer
|
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Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity .
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- HY-169509
-
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PARP
Necroptosis
Topoisomerase
RIP kinase
Mixed Lineage Kinase
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Cancer
|
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Topoisomerase I/II Inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of Topoisomerase I/II, capable of inducing DNA damage and PARP-1 activation, which subsequently leads to the activation of RIPK1, RIPK3, and MLKL, ultimately triggering necroptosis. Topoisomerase I/II Inhibitor 8 demonstrates remarkable anticancer activity by effectively targeting the nuclei of cancer cells and inducing cell death through necroptosis, showing great clinical potential in circumventing drug resistance in cancer treatment .
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- HY-158230
-
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Topoisomerase
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Cancer
|
|
SN-398 is a derivative of Camptothecin (HY-158230), which is an antitumor drug. Acting by inhibiting mammalian DNA topoisomerase I (Topo I), stabilizing the Topo I-DNA complex prevents DNA rewiring to induce Topo I mediated DNA breaks. In Hela cell tests, SN-398 shows stronger antitumor activity than SN-38 (HY-13704) (IC50=1.562 μM). SN-398 can be used to study the anti-proliferation and growth inhibition of Topo I in cancer cells .
|
-
- HY-161970
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
|
-
- HY-174151
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
|
-
- HY-177548
-
-
- HY-164647
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Val-Ala-PABC-N(Mesylpropane)-Exatecan is an agent-linker conjugate for ADC. Val-Ala-PABC-N(Mesylpropane)-Exatecan is a Exatecan (a DNA topoisomerase I inhibitor) d with cleavable Val-Ala-PABC-N(Mesylpropane) linker .
|
-
- HY-43565B
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan intermediate 10 is an intermediate in the synthesis of Exatecan (HY-13631).Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 of 2 .2 μM (0 .975 μg/mL) for use in cancer research .
|
-
- HY-49861
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan intermediate 11 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-400316
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan intermediate 8 is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-N11536
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK .
|
-
- HY-B1099R
-
|
|
DNA/RNA Synthesis
Topoisomerase
Parasite
Reference Standards
|
Infection
|
|
Hycanthone (Standard) is the analytical standard of Hycanthone. This product is intended for research and analytical applications. Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
|
-
- HY-156686
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-164380
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid (example 13) is a drug-linker conjugate that consists of a DNA topoisomerase I inhibitor Exatecan (HY-13631) and a linker (HY-180841). MC-Val-Cit-Gly-exatecan-β-D-glucopyranosiduronic acid can be used in synthesis of ADC .
|
-
- HY-182816
-
|
|
Topoisomerase
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Topoisomerase I-IN-22 is an inhibitor of MRSA DNA Topoisomerase I with an IC50 of 0.85 μg/mL. Topoisomerase I-IN-22 can specifically disrupt the cell membrane structure of MRSA, enter the interior of bacteria and inhibit the activity of DNA Topoisomerase I, thereby interfering with the processes of DNA replication and transcription. Topoisomerase I-IN-22 can be used for the research of MRSA infection .
|
-
- HY-182926
-
|
|
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer .
|
-
- HY-N4329
-
|
|
Topoisomerase
|
Others
|
|
Nidulalin A is a DNA topoisomerase II inhibitor with an IC50 of 2.2 μM. Nidulalin A has an IC50 of 172 μM for DNA topoisomerase I. Nidulalin A has certain cytotoxicity .
|
-
- HY-16562S2
-
-
- HY-181725
-
|
|
Topoisomerase
Apoptosis
MDM-2/p53
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Topoisomerase I-IN-20 is a Topoisomerase I inhibitor. Topoisomerase I-IN-20 disrupts DNA synthesis and transcription, thereby inhibiting the proliferation and migration of cancer cells. Topoisomerase I-IN-20 induces S-phase cell cycle arrest and mitochondria-mediated Apoptosis in cancer cells, which is characterized by upregulated expression of p53, Bax, caspase-3 and caspase-9, along with downregulated expression of Bcl-2. Topoisomerase I-IN-20 increases intracellular ROS levels. Topoisomerase I-IN-20 is applicable to lung cancer-related research .
|
-
- HY-182748
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
NL-26 is a Topoisomerase I inhibitor. NL-26 stabilizes the covalent Topoisomerase I (Topo I)-DNA complex, prevents DNA religation and triggers the DNA damage response. NL-26 induces G2/M cell cycle arrest and apoptosis in cancer cells. NL-26 can be used for the research of colorectal cancer .
|
-
- HY-13631U
-
|
DX-8951 hydrochloride
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan (DX-8951) hydrochloride is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-185370
-
|
Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposome
|
Liposome
Topoisomerase
Antibiotic
|
Cancer
|
|
Doxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
|
-
- HY-13631G
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan analog 13 is a analog of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM) .
|
-
- HY-N15249
-
|
Isovalerylspiramycin I; Shengjimycin E
|
Topoisomerase
DNA/RNA Synthesis
Checkpoint Kinase (Chk)
Apoptosis
Bacterial
|
Infection
Cancer
|
|
4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection .
|
-
- HY-N8250
-
|
|
Topoisomerase
PEPCK
|
Metabolic Disease
|
|
cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus .
|
-
- HY-42487S1
-
|
|
Isotope-Labeled Compounds
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 1-d2 is the deuterium labeled Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
|
-
- HY-183330
-
|
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
MDM-2/p53
Caspase
Bcl-2 Family
|
Cancer
|
|
Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC50 of 8.99 μM against Topo I and an IC50 of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of γ-H2AX, p53, activated caspase-9, Bax and activated caspase-3, while downregulating the expression of Bcl-2. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer .
|
-
- HY-101647R
-
|
RP 60475 (Standard)
|
Topoisomerase
Reference Standards
|
Cancer
|
|
Intoplicine (Standard) is the analytical standard of Intoplicine (HY-101647). This product is intended for research and analytical applications. Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA .
|
-
- HY-43565C
-
|
|
Drug Intermediate
|
Cancer
|
|
(1S,9R)-Ac-Exatecan is an intermediate for the synthesis of Exatecan (HY-13631). Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50=2.2 μM) .
|
-
- HY-131438
-
|
|
Topoisomerase
|
Cancer
|
|
GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts) .
|
-
- HY-13631F
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Gly-Gly-Phe-Gly-NH-O-CO-Exatecan, as a drug-linker conjugate composed of linker Gly-Gly-Phe-Gly-NH-O-CO and Exatecan, can be used to prepare antibody conjugate drugs. Exatecan is a DNA topoisomerase I inhibitor that can be used in cancer research .
|
-
- HY-13566R
-
|
CKD-602 free base (Standard)
|
Topoisomerase
Apoptosis
Reference Standards
|
Cancer
|
|
Belotecan (Standard) is the analytical standard of Belotecan. This product is intended for research and analytical applications. Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer .
|
-
- HY-46081
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 3 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 3 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-43564
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 5 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 5 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-13631N
-
|
(9R)-DX8951f
|
Drug Derivative
ADC Payload
Topoisomerase
|
Cancer
|
|
(9R)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
|
-
- HY-44369
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-107096
-
|
TP3076
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-18351
-
|
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-164792
-
-
- HY-147270
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity .
|
-
- HY-45157
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan Intermediate 7 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 7 can be used to synthesize Antibody-Drug Conjugates (ADCs).
|
-
- HY-101647AR
-
|
RP 60475 dimesylate (Standard)
|
Topoisomerase
Reference Standards
|
Cancer
|
|
Intoplicine (dimesylate) (Standard) is the analytical standard of Intoplicine (dimesylate) (HY-101647A). This product is intended for research and analytical applications. Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA .
|
-
- HY-15142R
-
|
Hydroxydaunorubicin hydrochloride (Standard); ADR (Standard)
|
Reference Standards
Topoisomerase
ADC Payload
AMPK
Autophagy
Apoptosis
HIV
HBV
Mitophagy
Antibiotic
Bacterial
Fluorescent Dye
|
Infection
Cancer
|
|
Doxorubicin hydrochloride (Standard) is the analytical standard of Doxorubicin hydrochloride. This product is intended for research and analytical applications. Doxorubicin (Hydroxydaunorubicin) hydrochloride, a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy .
|
-
- HY-168285
-
-
- HY-128994A
-
|
|
Drug Intermediate
|
Cancer
|
|
GGFG-Exatecan TFA is a synthetic intermediate for drug-linker conjugates used in antibody-drug conjugates (ADCs). GGFG-Exatecan TFA consists of a glycyl-glycyl-phenylalanyl-glycine (GGFG) tetrapeptide linker and a DNA topoisomerase I inhibitor Exatecan (HY-13631). GGFG-Exatecan TFA can be used for the study of cancer .
|
-
- HY-107096B
-
|
TP3076 TFA
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-13704S
-
|
NK012-d3
|
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
|
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
|
-
- HY-13704
-
|
7-Ethyl-10-hydroxycamptothecin
|
Drug Metabolite
Topoisomerase
ADC Payload
Autophagy
|
Infection
Cancer
|
|
SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-156376
-
|
|
Cuproptosis
Apoptosis
Topoisomerase
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
Cu(II)-Elesclomol is a complex formed by Elesclomol (HY-12040) and Cu 2+ (copper ions). Cu(II)-Elesclomol is also a weak inhibitor of DNA topoisomerase I. Cu(II)-Elesclomol exerts anticancer effects by inducing oxidative stress and DNA damage through copper chelation. Cu(II)-Elesclomol can inhibit tumor cell proliferation and induce cell cycle arrest and apoptosis. Cu(II)-Elesclomol can be used in the study of cancer .
|
-
- HY-147307
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan is a agent-linker conjugate for ADC, contains the ADC linker (MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic acid) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-Gly-Gly-Phe-Gly-Cyclobutanecarboxylic-Exatecan synthesized ADC can be used in study of cancer .
|
-
- HY-114233
-
|
MC-GGFG-DX8951
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC) .
|
-
- HY-13631T
-
|
(1R,9S)-DX8951f
|
Drug Derivative
ADC Payload
Topoisomerase
|
Cancer
|
|
(1R,9S)-Exatecan (DX8951f) is the (1R,9S) stereoisomer of Exatecan (HY-13631). Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-122532
-
|
|
Histone Methyltransferase
|
Cancer
|
|
Fagaronine chloride is an alkaloid with inhibitory activity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection .
|
-
- HY-171580
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mc-PEG4-Val-Ala-PAB-Exatecan is a Drug-linker conjugate for ADC. Mc-PEG4-Val-Ala-PAB-Exatecan contains the ADC linker (Mc-PEG4-Val-Ala-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
|
-
- HY-16560S
-
|
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Isotope-Labeled Compounds
Topoisomerase
ADC Payload
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
|
-
- HY-79490
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Ac-Exatecan is acetylation-modified Exatecan (HY-13631). Exatecan is a common toxin component in ADC preparation (ADC cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM). Exatecan has antitumor activity. Exatecan can be used as a payload for ADC. Exatecan is effective against P-glycoprotein mediated multi-drug resistant cells .
|
-
- HY-W046353
-
|
o-Methoxycinnamaldehyde
|
Apoptosis
NF-κB
Topoisomerase
Mitochondrial Metabolism
Caspase
|
Cancer
|
|
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-116926
-
|
|
Antibiotic
Bacterial
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Infection
Cancer
|
|
Deoxynybomycin is an antibiotic, that can be isolated from Streptomyces, and antibacterial activity against Staphylococcus aureus. Deoxynybomycin is the inhibitor for DNA gyrase and Topoisomerase I. Deoxynybomycin induces expression of p21/WAF1, exhibits cytotoxicity and induces apoptosis in cancer cells Saos-2, TMK-1, and THP-1 .
|
-
- HY-B0147A
-
|
Pefloxacinium mesylate
|
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies .
|
-
- HY-B0147
-
|
Pefloxacinium
|
Antibiotic
Bacterial
Parasite
DNA/RNA Synthesis
Topoisomerase
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-P99843
-
|
|
TROP2
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
- HY-148696A
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Gly-Cyclopropane-Exatecan involves in the synthesis of anti-B7-H4 ADC, containing Exatecan (HY-13631), a DNA Topoisomerase I inhibitor. Gly-Cyclopropane-Exatecan participated in the formation of the ADC hu2F7-Exatecan (compound 34), which showed antitumor activity in vivo and in vitro .
|
-
- HY-13704R
-
|
7-Ethyl-10-hydroxycamptothecin (Standard)
|
Drug Metabolite
Reference Standards
Topoisomerase
ADC Payload
Autophagy
|
Cancer
|
|
SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-16560R
-
|
Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)
|
Reference Standards
Topoisomerase
ADC Payload
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
|
-
- HY-175269
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia .
|
-
- HY-N2108
-
|
|
Drug Derivative
Drug Intermediate
Topoisomerase
|
Cancer
|
|
7-Ethylcamptothecin is a derivative of Camptothecin (HY-16560) and a DNA topoisomerase I inhibitor that exhibits significant antitumor activity against tumor cells. 7-Ethylcamptothecin serves as a key precursor for the synthesis of 20 (S)-O-substituted benzoyl-7-ethylcamptothecin compounds. 7-Ethylcamptothecin is widely used in various tumor-related scientific studies .
|
-
- HY-181836
-
|
|
IKK
Topoisomerase
Apoptosis
NF-κB
Reactive Oxygen Species (ROS)
Bcl-2 Family
|
Cancer
|
|
IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer .
|
-
- HY-B0147B
-
|
Pefloxacinium mesylate dihydrate
|
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies .
|
-
- HY-N0095
-
|
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
|
-
- HY-164152
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-164152A
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-153067
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan (Compound 11) is a bioactive compound-linker conjugate for ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can conjugate with antibodies to form ADC (C-11) with anti-tumor activity. Exatecan is a DNA Topoisomerase I inhibitor. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can be used in the research of squamous cell carcinoma, pancreatic adenocarcinoma and colorectal cancer .
|
-
- HY-B0147R
-
|
Pefloxacinium (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Standard) (Pefloxacinium (Standard)) is the analytical standard of Pefloxacin (HY-B0147). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-B0147AR
-
|
Pefloxacinium mesylate (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin mesylate (Standard) (Pefloxacinium mesylate (Standard)) is the analytical standard of Pefloxacin mesylate (HY-B0147A). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) mesylate is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate can be used for infection studies .
|
-
- HY-B0147S1
-
|
Pefloxacinium-d3
|
Isotope-Labeled Compounds
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-B0147S
-
|
Pefloxacinium-d5
|
Isotope-Labeled Compounds
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
- HY-162472
-
|
|
ATM/ATR
DNA-PK
|
Cancer
|
|
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-175700
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved
caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .
|
-
- HY-134723
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
|
-
- HY-153795
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is a bioactive drug-linker conjugate for ADC (Drug-Linker Conjugates for ADC). Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan consists of Exatecan (HY-13631) and a linker. Mal-PEG2-Gly-Gly-Phe-Gly-Exatecan is applicable to ADC synthesis and cancer research. Exatecan acts as a DNA Topoisomerase I inhibitor .
|
-
- HY-160005
-
|
NSC 781517
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer .
|
-
- HY-W046353R
-
|
o-Methoxycinnamaldehyde (Standard)
|
Reference Standards
Apoptosis
NF-κB
Mitochondrial Metabolism
Caspase
Topoisomerase
|
Cancer
|
|
2-Methoxycinnamaldehyde (Standard) is the analytical standard of 2-Methoxycinnamaldehyde. This product is intended for research and analytical applications. 2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects .
|
-
- HY-128943
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouse plasma .
|
-
- HY-173625
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
|
-
- HY-156513
-
|
7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)
|
ADC Payload
|
Cancer
|
|
ZD06519 (7-Hydroxyethyl carbamate-(10Me-11F-Camptothecin)) is a camptothecin (HY-16560) analogue and a topoisomerase I inhibitor. ZD06519 is an ADC cytotoxin with a strong bystander effect, inhibiting a variety of malignancies such as HER2-positive and FRα-overexpressing tumors. ZD06519 inhibits DNA cleavage, relaxation, and reconnection processes, inducing tumor cell death. ZD06519 can be used for ADC synthesis and cancer research .
|
-
- HY-173703
-
|
|
Topoisomerase
Drug Intermediate
|
Cancer
|
|
β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers .
|
-
- HY-B0147BR
-
|
Pefloxacinium mesylate dihydrate (Standard)
|
Reference Standards
Topoisomerase
DNA/RNA Synthesis
Antibiotic
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Pefloxacin (Pefloxacinium) mesylate dihydrate (Standard) is the analytical standard of Pefloxacin mesylate dihydrate (HY-B0147B). This product is intended for research and analytical applications. Pefloxacin (Pefloxacinium) mesylate dihydrate is a broad spectrum antibiotic. Pefloxacin mesylate dihydrate blocks DNA replication by inhibiting DNA gyrase. Pefloxacin mesylate dihydrate inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin mesylate dihydrate exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin mesylate dihydrate has anti-Plasmodium yoelii infection activity. Pefloxacin mesylate dihydrate increase UVA-induced edema and immunesuppression. Pefloxacin mesylate dihydrate can be used for infection studies .
|
-
- HY-16055
-
|
AR-67; DB 67
|
Topoisomerase
Drug Derivative
MDM-2/p53
|
Cancer
|
|
Silatecan (AR-67) is a blood-brain barrier-permeable derivative of Camptothecin (HY-16560), DNA topoisomerase I inhibitor, an anticancer agent, and a radiosensitizer. Silatecan potently radiosensitizes wild-type p53 gliomas. Silatecan can be used in research related to glioma, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer, breast cancer, cervical cancer, gastric cancer, nasopharyngeal cancer, and uterine cancer .
|
-
- HY-N0095S
-
|
10-HCPT-d5; 10-Hydroxycamptothecin-d5
|
Isotope-Labeled Compounds
Apoptosis
Topoisomerase
|
Cancer
|
|
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
|
-
- HY-13704S2
-
|
7-Ethyl-10-hydroxycamptothecin-13C6
|
Isotope-Labeled Compounds
Autophagy
ADC Payload
Topoisomerase
Drug Metabolite
|
Infection
Cancer
|
|
SN-38- 13C6 (7-Ethyl-10-hydroxycamptothecin- 13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
- HY-128946
-
|
|
Drug-Linker Conjugates for ADC
|
Inflammation/Immunology
Cancer
|
|
CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects .
|
-
- HY-162805
-
|
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
|
-
- HY-177681
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal)-N-(PEG8-Val-Cit-PAB-MMAE)-N-(PEG8-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-185101
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-AcLys-GDEVD-PABC-Exatecan (MC-AcLys-GDEVD-PABC-DX8951) is a agent-linker conjugate for ADC. MC-AcLys-GDEVD-PABC-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with a novel caspase-3 cleavable peptide linker MC-AcLys-GDEVD-PABC linker. MC-AcLys-GDEVD-PABC-Exatecan can be used to prepare DX8951 antibody conjugate (ADC), and it exhibites significant bystander effect mediated by the caspase-3-triggered extracellular cleavage of the linker, enhancing payload release into the tumor microenvironment.
|
-
- HY-N0095R
-
|
10-HCPT (Standard); 10-Hydroxycamptothecin (Standard)
|
Reference Standards
Topoisomerase
Apoptosis
|
Cancer
|
|
(S)-10-Hydroxycamptothecin (Standard) is the analytical standard of (S)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment .
|
-
- HY-171124
-
|
AZD9592
|
Antibody-Drug Conjugates (ADCs)
EGFR
c-Met/HGFR
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research .
|
-
- HY-118899
-
|
|
Endogenous Metabolite
|
Cancer
|
|
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 .
|
-
- HY-178738
-
|
|
Antibiotic
Bacterial
Topoisomerase
DNA/RNA Synthesis
|
Infection
|
|
GC-072 is an orally active, 4-oxoquinolizine antibiotic that selectively inhibits bacterial DNA gyrase and Topo IV enzymes. GC-072 does not inhibit human topoisomerases I and II. GC-072 demonstrates strong antimicrobial activity against various bacterial strains, including Gram-positive, Gram-negative, and resistant bacteria. GC-072 also exhibits bactericidal activity against Burkholderia pseudomallei both extracellularly and intracellularly, leading to dose-dependent survival in mice exposed to lethal inhalational models of B. pseudomallei infection. GC-072 can be used for the research of melioidosis .
|
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
TROP2
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-177683
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(DBCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177678
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177686
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Azido-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177685
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(TCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(TCO-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177679
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Amino-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177687
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177682
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177684
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(endo-BCN-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177688
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Cancer
|
|
N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-177680
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
Microtubule/Tubulin
|
Others
|
|
N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) is a drug-linker conjugate for ADC (Drug-Linker Conjugate for ADC), consisting of a tubulin polymerization inhibitor MMAE (HY-15162) and a DNA topoisomerase I inhibitor Exatecan (HY-13631), and an ADC linker composition. N-(Mal-PEG4)-N-(PEG4-Val-Cit-PAB-MMAE)-N-(PEG4-Val-Cit-PAB-Exatecan) can be used for synthesis of ADCs and for cancer research.
|
-
- HY-178145
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan (compound 12) is a Drug-Linker Conjugate for ADC. Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan contains the ADC linker (Mc-Lys(PEG12)-Cap-Ala-Ala-PABC) (HY-178146) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). Mc-Lys(PEG12)-Cap-Ala-Ala-PABC-exatecan can be used for the development of ADC targeting HER2-positive breast cancer .
|
-
- HY-13631J
-
|
(1R,9R)-DX8951f
|
Drug Derivative
Topoisomerase
Apoptosis
|
Cancer
|
(1R,9R)-Exatecan mesylate ((1R,9R)-DX8951f) is a non-prodrug camptothecin derivative and a potent topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1R,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1R,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1R,9R)-Exatecan mesylate is widely used in preclinical studies of multiple cancers including pancreatic cancer, lung cancer, breast cancer, and leukemia . The low-activity isomer of (1R,9R)-Exatecan mesylate is (1S,9R)-Exatecan mesylate (HY-13631I).
|
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-183594
-
|
|
Drug-Linker Conjugates for ADC
|
Others
|
|
Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal is a linker-payload conjugate. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal contains the linker D-2,4-DHB-NH2-AA(bPEG8)-Mal (HY-183595) and the cytotoxic agent Exatecan (HY-13631), a potent DNA topoisomerase I inhibitor. Exatecan-(D-2,4-DHB)-NH2-AA (bPEG8)-Mal can be utilized for the development of antibody-drug conjugates (ADCs) .
|
-
- HY-177442
-
|
DS-3939
|
Antibody-Drug Conjugates (ADCs)
Mucin
Topoisomerase
Apoptosis
|
Cancer
|
|
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers .
|
-
- HY-173634
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB-Exatecan (LP1) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker Mal((3S,3aR,6S,6aR)-Hexahydrofuro[3,2-b]furan-3,6-diamine-PEG12)-β-Glu-PAB (HY-173635) to make antibody agent conjugate (ADC), AZD0516 (HY-173639) .
|
-
- HY-13631I
-
|
(1S,9R)-DX8951f
|
Drug Derivative
Topoisomerase
Apoptosis
|
Cancer
|
(1S,9R)-Exatecan mesylate ((1S,9R)-DX8951f) is a non-prodrug camptothecin derivative and a topoisomerase I inhibitor (IC50=0.975 μg/mL in mice and 0.82 μg/mL in humans). (1S,9R)-Exatecan mesylate blocks enzyme activity and induces apoptosis by stabilizing the enzyme-DNA cleavable complex. (1S,9R)-Exatecan mesylate not only effectively inhibits the proliferation of various malignant tumor cells and tumor growth, but also circumvents P-glycoprotein-mediated multidrug resistance. (1S,9R)-Exatecan mesylate is widely used in preclinical studies of various cancers such as pancreatic cancer, lung cancer, breast cancer, and leukemia . The chiral isomer of (1S,9R)-Exatecan mesylate is (1R,9R)-Exatecan mesylate (HY-13631J).
|
-
- HY-182759
-
|
|
DNA Alkylator/Crosslinker
Topoisomerase
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-141598
-
|
DS-1062 (solution); Dato-DXd (solution)
|
Fluorescent Dyes
|
|
Datopotamab deruxtecan (DS-1062) solution is a TROP2-targeted antibody-drug conjugate (ADC) with human TROP2 Kd of 0.74 nmol/L. Datopotamab deruxtecan solution consists of the antibody Datopotamab (HY-P99843) and the toxic molecule-linker conjugate Deruxtecan (HY-13631E). Datopotamab deruxtecan solution binds TROP2, triggers internalization and lysosomal trafficking and releases DXd topoisomerase I inhibitor payload. Datopotamab deruxtecan solution disrupts DNA function, induces DNA damage, apoptosis, and bystander killing of tumor microenvironment cells. Datopotamab deruxtecan solution can be used in research related to triple-negative breast cancer, gastric cancer, and non-small cell lung cancer .
|
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Fluorescent Dyes
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
- HY-164152A
-
|
|
Fluorescent Dyes
|
|
ADC Control Human IgG1-Deruxtecan (DAR 8) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-164152
-
|
|
Fluorescent Dyes
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
- HY-13631AG
-
|
DX8951f
|
Fluorescent Dyes
|
|
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
-
- HY-177442
-
|
DS-3939
|
Fluorescent Dyes
|
|
DS-3939a (DS-3939) is an anti-TA-MUC1 (tumor-associated mucin-1) antibody-drug conjugate (ADC). DS-3939a consists of a humanized anti-TA-MUC1 IgG1 monoclonal antibody Gatipotuzumab ( HY-P99634), a stable and cleavable tetrapeptide-based linker (Gly-Gly-Phe-Gly), and a DNA topoisomerase I inhibitor payload (DXd) (HY-13631D), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). DS-3939a inhibits the growth of TA-MUC1-positive cancer cells (CFPAC-1, NCI-H2110) by inducing DNA damage and apoptosis. DS-3939a exhibits significant antitumor activity in a variety of TA-MUC1-expressing advanced solid tumors. DS-3939a can be used for the study of TA-MUC1-expressing advanced cancers .
|
| Cat. No. |
Product Name |
Type |
-
- HY-13631AG
-
|
DX8951f
|
Biochemical Assay Reagents
|
|
Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99843
-
|
|
TROP2
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
(5)
-
- HY-P3371
-
|
DS-7300a; MABX-9001a; I-DXd
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
Apoptosis
|
Cancer
|
|
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
|
-
(5)
-
- HY-164152
-
|
|
Antibody-Drug Conjugates (ADCs)
Topoisomerase
|
Cancer
|
|
ADC Control Human IgG1-Deruxtecan (DAR 4) is a humanized monoclonal antibody that is an isotype control of ADC human IgG1-Deruxtecan and can inhibit DNA topoisomerase I. The antibody portion is Human IgG1 kappa, Isotype Control (HY-P99001), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E) .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-15142
-
-
-
- HY-13704
-
-
-
- HY-16560
-
-
-
- HY-15142R
-
-
-
- HY-15142A
-
-
-
- HY-B0147
-
|
Pefloxacinium
|
Infection
Classification of Application Fields
Disease Research Fields
|
Antibiotic
Bacterial
Parasite
DNA/RNA Synthesis
Topoisomerase
|
|
Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-N0095
-
-
-
- HY-13744
-
-
-
- HY-N3488
-
-
-
- HY-N2108
-
-
-
- HY-W046353
-
-
-
- HY-13704R
-
-
-
- HY-19825
-
-
-
- HY-W713570
-
-
-
- HY-16560R
-
-
-
- HY-N15319
-
|
Canangine
|
Alkaloids
Other Alkaloids
Cananga odorata
Plants
Annonaceae
Source Classification
|
Topoisomerase
Fungal
|
|
Eupolauridine (Canangine) is a selective DNA topoisomerase II inhibitor with IC50 values of 20 μM for fungal topoisomerase I and 33 μM for human topoisomerase I. Eupolauridine exerts antifungal activity by inhibiting the catalytic activity of topoisomerase II and stabilizing its cleavage complex with DNA, leading to DNA damage. Eupolauridine is promising for research of fungal infectious diseases .
|
-
-
- HY-N10115
-
-
-
- HY-N10367
-
-
-
- HY-N11536
-
-
-
- HY-W046353R
-
-
-
- HY-N0095R
-
-
-
- HY-N4329
-
-
-
- HY-N15249
-
|
Isovalerylspiramycin I; Shengjimycin E
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
Topoisomerase
DNA/RNA Synthesis
Checkpoint Kinase (Chk)
Apoptosis
Bacterial
|
|
4"-Isovalerylspiramycin I (Isovalerylspiramycin I) is a topoisomerase 1 (TOP1) inhibitor and an antitumor agent. 4"-Isovalerylspiramycin I directly binds to TOP1, suppresses DNA replication, and induces DNA damage. 4"-Isovalerylspiramycin I downregulates phosphorylated CHEK1 and the ATR/CHEK1 DNA damage repair pathway, blocks DNA repair, and augments DNA damage. 4"-Isovalerylspiramycin I suppresses proliferation, migration, and invasion of osteosarcoma cells. 4"-Isovalerylspiramycin I induces apoptosis and cell cycle arrest in osteosarcoma cells. 4"-Isovalerylspiramycin I exerts antibacterial activity against methicillin-resistant Staphylococcus aureus. 4"-Isovalerylspiramycin I can be used for the research of osteosarcoma, upper respiratory bacterial infections, and methicillin-resistant Staphylococcus aureus infection .
|
-
-
- HY-N8250
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13631AS
-
|
|
|
Exatecan-d5 (DX8951f-d5) mesylate is deuterium labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL). Exatecan mesylate can be used in cancer research .
|
-
-
- HY-13631DS
-
|
|
|
DXd-d5 is a deuterium labeled DXd. DXd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) .
|
-
-
- HY-13704S
-
|
|
|
SN-38-d3 is the deuterium labeled SN-38. SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively .
|
-
-
- HY-16562S1
-
|
|
|
Irinotecan-d10 (hydrochloride) is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
|
-
-
- HY-16560S
-
|
|
|
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
|
-
-
- HY-13631AS1
-
|
|
|
Exatecan-d3 (DX8951f-d3) mesylate is deuterium-labeled Exatecan mesylate (HY-13631A). Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL .
|
-
-
- HY-16562S
-
|
|
|
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
|
-
-
- HY-B0147S1
-
|
|
|
Pefloxacin-d3 (Pefloxacinium-d3) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-B0147S
-
|
|
|
Pefloxacin-d5 (Pefloxacinium-d5) is the deuterium labeled Pefloxacin (HY-B0147). Pefloxacin (Pefloxacinium) is a broad spectrum antibiotic. Pefloxacin blocks DNA replication by inhibiting DNA gyrase. Pefloxacin inhibits DNA relaxation catalyzed by topoisomerase I with an IC50 of 45 μg/mL. Pefloxacin exhibits antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, and Bacteroides fragilis with MIC90s of 0.12, 4, and 16 mg/L, respectively. Pefloxacin has anti-Plasmodium yoelii infection activity. Pefloxacin increase UVA-induced edema and immunesuppression. Pefloxacin can be used for infection studies .
|
-
-
- HY-N0095S
-
|
|
|
(S)-10-Hydroxycamptothecin-d5 (10-HCPT-d5) is the deuterium labeled (S)-10-Hydroxycamptothecin. (S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia research .
|
-
-
- HY-16562S2
-
|
|
|
Irinotecan- 13C6 ((+)-Irinotecan- 13C6) is the 13C-labeled Irinotecan (HY-16562). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .
|
-
-
- HY-42487S1
-
|
|
|
Exatecan Intermediate 1-d2 is the deuterium labeled Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor with anticancer effects.
|
-
-
- HY-13704S2
-
|
|
|
SN-38- 13C6 (7-Ethyl-10-hydroxycamptothecin- 13C6) is the 13C-labeled SN-38 (HY-13704). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 can bind to RPL15. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254) .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-134723
-
|
|
|
DBCO
ADC Synthesis
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DBCO-PEG4-GGFG-Dxd is a agent-linker conjugate for ADC with potent antitumor activity by using Dxd (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG . DBCO-PEG4-GGFG-Dxd is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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- HY-164792
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DBCO
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DBCO-PEG3-VC-Exatecan (compound 25) is a Drug-Linker Conjugate for ADC. DBCO-PEG3-VC-Exatecan contains the ADC linker (DBCO-PEG3-VC) and a DNA topoisomerase I inhibitor Exatecan (HY-13631) .
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- HY-173625
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Alkynes
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P5(PEG12)-VC-PAB-Exatecan (LP3) is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor Exatecan (HY-13631) and a linker P5(PEG24)-VC-PAB to make antibody agent conjugate (ADC). P5(PEG12)-VC-PAB-Exatecan can be used for the research of tumor .
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| Cat. No. |
Product Name |
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Classification |
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- HY-185370
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Pegylated liposomal doxorubicin; Liposomal doxorubicin; Doxorubicin hydrochloride liposome
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Liposome
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Doxorubicin liposome is a liposome-encapsulated form of doxorubicin hydrochloride (HY-15142). Doxorubicin hydrochloride, a cytotoxic anthracycline antibiotic, is a potent human DNA topoisomerase I and topoisomerase II inhibitor. Compared to traditional doxorubicin, liposome encapsulation reduces its cardiotoxicity and prolongs its circulation time, thus enabling it to effectively target tumor tissue.
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13631AG
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DX8951f
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ADC Payload
Topoisomerase
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Cancer
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Exatecan mesylate (DX8951f ) GMP is a GMP-class Exatecan (HY-13631). Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research .
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