Topoisomerase Inhibitors | Inhibitors | 여러 강력하고, 높은 선택성을 가지며, 잘 인용된

Topoisomerases can manage DNA's topological state in the nuclear to facilitate the replication, recombination, transcription and repair of DNA by separating the two strands of the helix temporarily. There are 2 types of DNA topoisomerases which are type I topoisomerase and type II topoisomerase.

기타 DNA Damage/DNA Repair 억제제

HDAC PARP WRN Sirtuin Telomerase DNA/RNA Synthesis MTH1 DNA alkylator High-mobility Group CRISPR/Cas9

아이소폼 선택적 제품

Topo I Topo II Topo IV

Cat.No.	제품명	정보	제품 사용 인용
E2516	Doxorubicin	Adriamycin(Doxorubicin, Hydroxydaunorubicin)은 세포독성 안트라사이클린 항생제이자 항암 화학요법제로, 2.67 μM의 IC50으로 Topoisomerase II를 억제하여 DNA 복제를 중단시키고 apoptosis를 유도합니다.	Cell Death Differ, 2026, 10.1038/s41418-026-01679-9 Int J Biol Sci, 2026, 22(4):1793-1806 Biomed Pharmacother, 2026, 196:119090
S1198	Irinotecan (CPT-11)	Irinotecan (CPT-11)은 LoVo 세포와 HT-29 세포에 대해 각각 15.8 μM과 5.17 μM의 IC50 값을 가지는 Topoisomerase I 억제제입니다.	Br J Cancer, 2026, 135(2):290-302 N Biotechnol, 2026, 93:341-350 Oncol Rep, 2026, 55(1)9
S1288	Camptothecin (CPT)	Camptothecin (CPT)은 세포 무함유 분석(cell-free assay)에서 0.68 μM의 IC50을 가지는 DNA Topoisomerase I (Topo I)의 특이적 억제제입니다. Camptothecin은 MicroRNA-125b 매개 미토콘드리아 경로를 통해 암세포에서 Apoptosis related 세포 사멸을 유도합니다. 임상 2상.	Nucleic Acids Res, 2026, 54(5)gkag188 Br J Cancer, 2026, 135(2):290-302 bioRxiv, 2026, 2026.06.05.730358
S1208	Doxorubicin (Adriamycin) Hydrochloride	Doxorubicin (DOX) HCl은 IC50 2.67 μM으로 인간 Topoisomerase II를 억제하는 항생제입니다. Doxorubicin은 AMPK의 기저 인산화를 감소시킵니다. Doxorubicin은 HIV 감염 환자의 병용 치료에 사용되지만 HBV 재활성화 위험이 높은 것으로 밝혀졌습니다.본 제품은 PBS 용액에 용해될 때 침전될 수 있습니다. 스톡 용액은 순수한 물로 준비하고, 순수한 물이나 식염수로 희석하여 작업 용액을 얻는 것이 좋습니다.Doxorubicin (Adriamycin) Hydrochloride는 신장 질환의 동물 모델을 유도하는 데 사용할 수 있습니다.	American Journal of Physiology-Gastrointestinal and Liver Physiology, May 1, 2025, G594-G609 Translational Oncology, January 2025, 102204 Research Square, February 21, 2024, nan
S1225	Etoposide	Etoposide는 podophyllotoxin의 반합성 유도체로, Topoisomerase II 억제 활성을 통해 DNA 합성을 저해하며, 이는 DNA의 이중 가닥 및 단일 가닥 절단을 촉진하고 Topoisomerase II 결합에 의한 복구를 가역적으로 억제합니다. Etoposide는 Autophagy, Mitophagy 및 Apoptosis를 유도합니다.	Nature Communications, October 15, 2025, 9160 Oncology Letters, March 2018, 3895-3903 Journal for ImmunoTherapy of Cancer, December 21, 2025, e012591
S2492	Novobiocin Sodium (Cathomycin, Albamycin)	Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin)은 감수성 그람 양성균을 치료하는 데 사용되는 박테리아 DNA gyrase (TopoIV)를 표적으로 하는 아미노쿠마린계 항생제입니다.	Cancer Science, May 2023, 1943-1957 Cell Rep Med, 2026, 7(3):102687 Redox Biol, 2025, 85:103672
S4908	SN-38	SN-38 (NK012)은 CPT-11의 활성 대사산물로, DNA topoisomerase I과 DNA 합성을 억제하며 빈번한 DNA 단일 가닥 절단을 유발합니다. SN-38은 Autophagy를 유도합니다.	Cancer Res, 2026, 10.1158/0008-5472.CAN-25-4114. International Journal of Nanomedicine, 2026, 555824 Commun Biol, 2026, 9(1)552
S2217	Irinotecan Hydrochloride Trihydrate	Irinotecan Hydrochloride Trihydrate는 Topoisomerase I 억제제인 irinotecan(Camptosar, Campto, CPT-11)의 염산염 삼수화물이며, LoVo 세포와 HT-29 세포에 대해 각각 15.8 μM과 5.17 μM의 IC50 값을 나타냅니다.	Int J Biol Macromol, 2026, 345:150612 Commun Biol, 2026, 9(1)552 Sci Adv, 2026, 12(9):eaea6453
S3035	Daunorubicin Hydrochloride (Daunomycin)	Daunorubicin HCl은 DNA 및 RNA 합성을 모두 억제하며, 무세포 분석에서 0.02 μM의 K_i로 DNA 합성을 억제합니다. Daunorubicin은 apoptosis를 유도하는 topoisomerase II 억제제입니다.Daunorubicin (RP 13057) HCl은 신장 질환의 동물 모델을 유도하는 데 사용할 수 있습니다.	Blood Advances, 2025 Mar 11, 1078-1091 Nat Commun, 2025, 16(1):617 Cell Rep Med, 2025, 6(4):102053
S1231	Topotecan HCl	Topotecan HCl은 세포 무세포 분석(cell-free assays)에서 MCF-7 Luc 세포 및 DU-145 Luc 세포에 대해 각각 13 nM 및 2 nM의 IC50을 나타내는 Topoisomerase I 억제제입니다. 이 화합물은 Autophagy 및 Apoptosis related를 유도합니다.	NPJ Precis Oncol, 2025, 9(1):306 Int J Mol Sci, 2025, 26(17)8494 Pharmaceuticals (Basel), 2025, 18(2)181
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DNA topoisomerases are nuclear enzymes that play a critical role in DNA transcription and replication events for the efficient creation and compaction of two identical genomes in two daughter cells. There are at least five different topoisomerase that have been found in higher eukaryotes that can be grouped into two categories: (1) type I family, includes topoisomerases I, IIIα, IIIβ, and (2) type II family, includes topoisomerases IIα and IIβ.^[1][2]

Type I enzymes, which do not require ATP, cleave one DNA strand at a time to achieve DNA strand relaxation. More specifically, among type I family constituents, topoisomerase I-mediated DNA strand scission involves a nucleophilic attack by the active site tyrosine OH group on the DNA phosphodiester bond at the site of cleavage. Such an attack results in the breakage of the DNA phosphodiester backbone and the creation of a phosphotyrosine bond between the enzyme and DNA. This covalent binary complex DNA-topoisomerase I, the so-called cleavable complex, is typically only an intermediate. Relaxation via passage (swivel movement) of the broken DNA strand around the unbroken strand is followed by reformation of the phosphodiester backbone as a result of relegation, with concomitant release of topoisomerase I and enzyme turnover.^[1][2]

In contrast, type II enzymes which are typically ATP-dependent are able to perform double strand cuts that relieve superhelical twists, intramolecular DNA knots, and intermolecular tangles for chromosomal segregation to produce a DNA-linked protein gate through which another intact duplex can pass. It should be emphasized that the enzyme shows strong preference for supercoiled DNA versus relaxed molecules. More specifically, with topoisomerase II enzymes it is observed that DNA cleavage occurs at preferred sequences within its recognition/binding sites, but there is not clear specificity.^[1][2]

In either case, both types of topoisomerases cleave DNA at the phosphodiester backbone by nucleophilic attack from a catalytic tyrosine residue which becomes linked to the phosphate end (P-Y) of the DNA break. The reactions of both types of topoisomerases are highly reversible and leave the DNA sequence unchanged following topoisomerization.^[1][2]

While both topoisomerases can relax supercoiled DNA, only topoisomerase II can decatenate DNA molecules. Interestingly, throughout the cell cycle topoisomerase I and topoisomerase IIβ do not change in concentration, meanwhile topoisomerase IIα protein level are noted to fluctuate in relation to the proliferative stage and cell cycle position. In particular, topoisomerase IIα mRNA peak in late S and G2/M several-fold over (typically more than 10 times) the amount observed in G1 cells. The high levels of topoisomerase IIα during the final stages of DNA replication is intended to assist with chromosome untangling, condensation and mitotic segregation events. Consequently, cancerous cells are noted to have high topoisomerase IIα activity, and these findings have prompted researchers to develop new anti-cancer agents that specifically target to poisomerase II.^[1][2]

In general, topoisomerase I or topoisomerase II-directed anti-cancer agents are able to interfere with at least one step of the catalytic cycle of the enzyme. Among the topoisomerase I inhibitor class of compounds, Camptothecin (CPT) and its derivatives – a pentacyclic alkaloid formerly isolated as a natural extract from the Chinese tree Camptoteca acuminate – are effective at selectively targeting topoisomerase I by trapping its catalytic intermediate during the topoisomerase I-DNA reaction. Agents that effectively target topoisomerase II include the Anthracyclines (i.e. Adriamycin and Daunorubicin, 9 and 10), Epipodophyllotoxins (i.e. Etoposide and Teniposide 11 and 12), Antracendedione (i.e. Mitoxantrone, 13) and Aminoacrideines (i.e. m-AMSA). The compounds are successful at stabilizing the short-lived covalent complexes between topoisomerase II and DNA. The anti-cancer agents convert the topoisomerase II enzymes into DNA-cleaving toxins which are currently are area of research interest.^[2]