Topoisomerase

Topoisomerases regulate DNA topology by resolving supercoils, knots, and catenanes generated during replication, transcription, chromatin remodeling, and other nucleic acid metabolic processes^[1]. Mechanistically, these enzymes cleave one DNA strand through TOP1/TOP3 enzymes or both strands through TOP2 enzymes, forming transient cleavage complexes that permit DNA relaxation, decatenation, or strand passage before religation^[1]^[2]. Human topoisomerases include TOP1, TOP1MT, TOP2A, TOP2B, TOP3A, and TOP3B, and these isoforms support genome stability, transcription, DNA replication, chromatin remodeling, and higher-order genome organization^[3]. Compared with type I enzymes that cleave one DNA strand, type II topoisomerases generate temporary double-strand breaks and therefore play central roles in chromosome segregation, replication stress resolution, and transcription-linked chromatin topology^[2]^[4]. Disease relevance arises when irreversible topoisomerase cleavage complexes become DNA-protein crosslinks coupled with DNA breaks, creating genomic damage associated with cancer and neurological disease^[3]^[5]. In cancer research, TOP2A is linked to proliferation and drug response, whereas TOP2B contributes to DNA rearrangements and double-strand break formation after TOP2 poison exposure^[6]. For experimental and therapeutic applications, topoisomerase inhibitors such as topotecan, irinotecan, etoposide, doxorubicin, and mitoxantrone stabilize cleavage complexes, induce DNA damage, and support studies of chemotherapy response, resistance, and genome repair pathways^[1]^[5]^[7].

References:

[1]. Sun Y, et al. Excision repair of topoisomerase DNA-protein crosslinks (TOP-DPC). DNA Repair (Amst). 2020 May;89:102837. [Content Brief]

[2]. Maxwell T, et al. Topo2008: DNA topoisomerases in biology and medicine. Nucleic Acids Res. 2009 Feb;37(3):659-60. [Content Brief]

[3]. Pommier Y, et al. Human topoisomerases and their roles in genome stability and organization. Nat Rev Mol Cell Biol. 2022 Jun;23(6):407-427. [Content Brief]

[4]. Uusküla-Reimand L, et al. Untangling the roles of TOP2A and TOP2B in transcription and cancer. Sci Adv. 2022 Nov 4;8(44):eadd4920. [Content Brief]

[5]. Swan RL, et al. Mechanisms to Repair Stalled Topoisomerase II-DNA Covalent Complexes. Mol Pharmacol. 2022 Jan;101(1):24-32. [Content Brief]

[6]. Ma Y, et al. Regulation of topoisomerase II stability and activity by ubiquitination and SUMOylation: clinical implications for cancer chemotherapy. Mol Biol Rep. 2021 Sep;48(9):6589-6601. [Content Brief]

[7]. Hevener K, et al. Recent developments in topoisomerase-targeted cancer chemotherapy. Acta Pharm Sin B. 2018 Oct;8(6):844-861. [Content Brief]

Topoisomerase 관련 제품 (432):

By Type:	Pan (16) Selective (3)
By Effects:	Inhibitors (378) Agonist (1) Controls (4) Ligand (1)

Cat. No.	상품명	효과	Purity

HY-162091

Topoisomerase I inhibitor 13	Inhibitor
Topoisomerase I inhibitor 13 (Compound G11) is a Topo I inhibitor that inhibits cancer cell proliferation. Topoisomerase I inhibitor 13 significantly inhibits tumor growth in vivo.

HY-185683

Elfetabart drozuntecan	Inhibitor
Elfetabart drozuntecan (DB-1311; BNT324) is an antibody-drug conjugate (ADC) targeting B7H3. Elfetabart drozuntecan conjugates a humanized anti-B7H3 IgG1 monoclonal antibody with a topoisomerase I inhibitor via a cleavable linker. Elfetabart drozuntecan exerts antitumor activity in solid tumors. Elfetabart drozuntecan can be used for the research of advanced/metastatic solid tumors.

HY-16742R

Gepotidacin (Standard)	Inhibitor
Gepotidacin (Standard) is the analytical standard of Gepotidacin. This product is intended for research and analytical applications. Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.

HY-172395

TopoII/tubulin-IN-1	Inhibitor
TopoII/tubulin-IN-1 (Compound 1B8) is a TopoII/tubulin inhibitor. TopoII/tubulin-IN-1 can inhibit the proliferation and the level of ROS of tumor cells, induce apoptosis and cell cycle arrest of tumor cells, but has no significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 has antitumor activity.

HY-178036

ZM484	Inhibitor
ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.

HY-RS14892

Top1 Rat Pre-designed siRNA Set A	Inhibitor
Top1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Top1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-149925

DNA Gyrase-IN-6	Inhibitor
Antibacterial agent 138 is a benzothiazole inhibitor of bacterial DNA gyrase and topoisomerase IV. Antibacterial agent 138 exhibits favorable solubility and plasma protein binding. Antibacterial agent 138 has antibacterial activity against Gram-positive and Gram-negative strains. Antibacterial agent 138 is a dual GyrB and ParE inhibitor.

HY-16562AS

Irinotecan-d₅ hydrochloride	Inhibitor
Irinotecan-d₅ hydrochloride is deuterated labeled Irinotecan hydrochloride (HY-16562A). Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.

HY-177688

N-(NHS-PEG4)-N-(PEG4-Val-Cit-PAB-MMAF)-N-(PEG4-Val-Cit-PAB-Exatecan)
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-156517

7Ethanol-10NH2-11F-Camptothecin	Inhibitor
7Ethanol-10NH2-11F-Camptothecin is a Camptothecin (HY-16560) analogue that serves as an ADC cytotoxin for the synthesis of antibody-drug conjugates (ADCs). 7Ethanol-10NH2-11F-Camptothecin can inhibit tumor growth and is used in cancer research.

HY-158391

Anticancer agent 218	Inhibitor
Anticancer agent 218 (P136) is a Camptothecin compound, with anticancer activity.

HY-N4329

Nidulalin A	Inhibitor
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-10919

C-1311	Inhibitor
C-1311 shows to inhibit the catalytic activity of DNA topoisomerase II in vitro and in tumour cells. C-1311 prolongs G2 arrest followed by G2 to M transit and cell death during mitosis in the process of mitotic catastrophe.

HY-158230

SN-398	Inhibitor
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-13551B

Amsacrine (gluconate)	Inhibitor
Amsacrine gluconate is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.

HY-146497

Topoisomerase I inhibitor 7	Inhibitor
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.

HY-B0147S1

Pefloxacin-d₃		99.35%
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-159483

SelB-1	Inhibitor
SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH.

HY-19943

TLC388	Inhibitor
TLC388 is a novel camptothecin analog with limited antitumor activity in metastatic NEC.

HY-145290

CPT-Se3	Inhibitor
CPT-Se3, a selenoproagent of Camptothecin (CPT), shows improved potency in killing cancer cells and inhibiting tumor growth. CPT–Se3 decreases the GSH/GSSG ratio and total thiols, elevates the ROS level in Hep G2 cells, and eventually induces apoptosis of cancer cells. CPT-Se3 shows cytotoxicity against HeLa, Hep G2, A549, and SMMC-7721 cells (IC₅₀= 2.19-4.7 μM).

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