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topo IIα/βnhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Cytotoxin (2) Antibiotic (3) Apoptosis (18) Bacterial (8) Biochemical Assay Reagents (1) Cathepsin (1) CDK (2) COX (1) DNA/RNA Synthesis (1) Drug-Linker Conjugates for ADC (1) EGFR (2) Fungal (2) HDAC (2) Influenza Virus (2) MicroRNA (2) PI3K (1) Prostaglandin Receptor (1) Reactive Oxygen Species (3) Topoisomerase (38) VEGFR (1)
By Research Areas:	Cancer (34) Cardiovascular Disease (1) Infection (9) Inflammation/Immunology (2)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-149239

Topo II/HDAC-IN-2	Topoisomerase HDAC Apoptosis	Cancer
Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis .

HY-149238

Topo II/HDAC-IN-1	Topoisomerase HDAC Apoptosis	Cancer
Topo II/HDAC-IN-1 (7d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-1 (8d) induces apoptosis .

HY-150685

Topo I/COX-2-IN-1	Topoisomerase Prostaglandin Receptor Apoptosis	Inflammation/Immunology Cancer
Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC₅₀ value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity .

HY-145859

Topo I-IN-1	Topoisomerase Apoptosis Reactive Oxygen Species	Cancer
Topo I-IN-1 (Compound 14d) is a potent Topo I inhibitor with antitumor activity and DNA intercalative capability. Topo I-IN-1 induces cell apoptosis .

HY-150755

Topo I/COX-2-IN-2	Topoisomerase COX Apoptosis Reactive Oxygen Species	Cancer
Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC₅₀ values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway .

HY-143279

Topoisomerase II inhibitor 3	Topoisomerase Apoptosis	Cancer
Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC₅₀ is 0.17 μM for topo IIα and the value of IC₅₀ is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential .

HY-152187

*Topoisomerase IIα-IN-5*	Topoisomerase Apoptosis	Others
Topoisomerase IIα-IN-5 is a *topoisomerase II (topo* II) α** catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629) .

HY-162091

Topoisomerase I inhibitor 13	Topoisomerase	Cancer
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-100777

DACA
DACA inhibits two essential nuclear enzymes in vitro, DNA topoisomerase I and *DNA topoisomerase (topo) II. DACA stabilises topo* I, topo II alpha, and topo II beta cleavable complexes in human leukaemia CCRF-CEM cells .

HY-125424

AM8191 hydrochloride	Bacterial	Inflammation/Immunology
AM8191 is an orally active bactericidal and selectively inhibits DNA synthesis and Staphylococcus aureus gyrase (IC₅₀=1.02 μM) and topo IV (IC₅₀=10.4 μM). AM8191 inhibits S. aureus MSSA (MIC=0.02 μg/mL) and S. aureus MRSA (MIC=0.06 μg/mL) .

HY-146020

*Topoisomerase IIα-IN-1*	Topoisomerase	Cancer
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .

HY-146021

*Topoisomerase IIα-IN-2*	Topoisomerase	Cancer
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .

HY-147801

*Topoisomerase IIα-IN-3*	Topoisomerase Apoptosis	Cancer
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .

HY-151453

*Topoisomerase IIα-IN-4*	Topoisomerase Apoptosis	Cancer
Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC₅₀ value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .

HY-152473

*Topoisomerase IIα-IN-6*	Topoisomerase	Cancer
Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC₅₀ values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism .

HY-152479

*Topoisomerase IIα-IN-7*	Topoisomerase	Cancer
Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC₅₀ value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .

HY-W031307

Topoisomerase IIα-IN-8

Topoisomerase Cancer

Topoisomerase IIα-IN-8 (compound 15) is a weak human DNA topoisomerase IIa (htIIa) inhibitor, with an IC₅₀ of 462 ± 38.0 μM .

*Topoisomerase IIα-IN-8*	Topoisomerase	Cancer
Topoisomerase IIα-IN-8 (compound 15) is a weak human DNA topoisomerase IIa (htIIa) inhibitor, with an IC₅₀ of 462 ± 38.0 μM .

HY-149002

Topoisomerase I/II inhibitor 4	Topoisomerase Apoptosis	Cancer
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research .

HY-10982

Amonafide 3 Publications Verification AS1413	Topoisomerase	Cancer
Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA.

HY-B0902A

Rufloxacin hydrochloride MF-934 hydrochloride	Bacterial Antibiotic	Infection
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.

HY-149271

Anti-MRSA agent 7	Bacterial DNA/RNA Synthesis Topoisomerase	Infection
Anti-MRSA agent 7 (Compound 12) is a potent antibacterial agent. Anti-MRSA agent 7 inhibits S. aureus DNA gyrase, E. coli DNA gyrase, S. aureus topo IV and E. coli topo IV with IC₅₀s of 0.185, 0.365, 0.341 and 0.059 μM, respectively .

HY-N12747

Dichlorogelignate

Topoisomerase Others

Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

Dichlorogelignate	Topoisomerase	Others
Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

HY-137466

ARN-21934	Topoisomerase	Cancer
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC₅₀ of 2 μM as compared to the anticancer agent Etoposide (IC₅₀=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .

HY-145867

EGFR-IN-45	Topoisomerase EGFR CDK Apoptosis	Cancer
EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC₅₀s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis .

HY-146504

Topoisomerase I/II inhibitor 3	Topoisomerase PI3K Apoptosis Reactive Oxygen Species	Cancer
Topoisomerase I/II inhibitor 3 (compound 7) is a potent *topoisomerase I (Topo* I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K**/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research .

HY-115990

Topoisomerase IV inhibitor 1	Topoisomerase Bacterial	Infection
Topoisomerase IV inhibitor 2 (compound 7d) is a potent *DNA topoisomerase IV (TOPO* IV) inhibitor with IC₅₀*s of 0.23 μM and 0.43 μM for TOPO* IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 0.972 μM and 0.608 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively .

HY-115991

Topoisomerase IV inhibitor 2	Topoisomerase Bacterial	Infection
Topoisomerase IV inhibitor 2 (compound 5d) is a potent *DNA topoisomerase IV (TOPO* IV) inhibitor with IC₅₀*s of 0.35 μM and 0.55 μM for TOPO* IV and DNA gyrase, respectively. Topoisomerase IV inhibitor 2 has anti-bacterial activity, with MICs of 1.985 μM and 0.744 μM in Staphylococcus aureus Newman and Escherichia coli ATCC8739, respectively .

HY-N2063

12-Ethyl-9-hydroxycamptothecin	Topoisomerase	Others
12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM .

HY-147877

Topoisomerase II inhibitor 12	Topoisomerase	Cancer
Topoisomerase II inhibitor 12 (Compound 8c) is a *topoisomerase II (topo* II)** inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity .

HY-49556

(S)-Benzyl 2-cyclopropyl-2-hydroxyacetate	Others	Cancer
(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 .

HY-153401

Topoisomerase II inhibitor 13	Topoisomerase	Cancer
Topoisomerase II inhibitor 13 is a topoisomerase II (Topo II) inhibitor. Topoisomerase II inhibitor 13 shows antiproliferative activity against several cancer cells. Topoisomerase II inhibitor 13 induces cancer cells apoptosis .

HY-19024

Merbarone NSC 336628
Merbarone (NSC 336628) is an orally active inhibitor of topoisomerase II. Merbarone acts primarily by blocking topoisomerase II-mediated DNA cleavage without stabilizing topo II-DNA covalent complexes. Merbarone is an anticancer agent .

HY-17460B

Garenoxacin mesylate BMS 284756 mesylate	Bacterial Topoisomerase	Infection
Garenoxacin (BMS 284756) mesylate is an orally active quinolone antibiotic and Garenoxacin mesylate has a broad spectrum of activity against a wide array of gram-positive and gram-negative bacteria, anaerobes. Garenoxacin mesylate also inhibits Gyrase and TOPO IV .

HY-163104

Antibacterial agent 169	Bacterial	Infection
Antibacterial agent 169 (Compound 28) is a pyrrolamide-type GyrB/ParE inhibitor with antibacterial activity. Antibacterial agent 169 has an inhibitory effect on Gyrase and Topo IV of Staphylococcus aureus, with IC₅₀ values of 49 nmol/L and 1.513 μmol/L respectively .

HY-N12129

6,6′-Dihydroxythiobinupharidine	Cathepsin	Others
6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively .

HY-146094

Antitumor agent-63	Topoisomerase	Cancer
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct *topoisomerase I (Topo* I)** inhibition .

HY-156723

9-Chloromethyl-10-hydroxy-11-F-Camptothecin	Topoisomerase	Cancer
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 .

HY-141436

Sucrosofate potassium Sucrose octasulfate potassium	Biochemical Assay Reagents	Cancer
Sucrosofate (Sucrose octasulfate) potassium is a sucrose acid that can be used to prepare liposomes to deliver Irinotecan (HY-16562). Irinotecan is an inhibitor of topoisomerase Topo I and is commonly used in colon and rectal cancer research. Sucrosofate nanoliposome preparation loaded with Irinotecan, also known as PEP02 or MM-398 .

HY-101775A

9-Hydroxyellipticine hydrochloride	Topoisomerase	Cardiovascular Disease Cancer
9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC₅₀ values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively .

HY-137005

CS1	Topoisomerase Apoptosis	Cancer
CS1 is a potent *DNA Topo* II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis** .

HY-147698

ZLHQ-5f	CDK Topoisomerase Apoptosis	Cancer
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC₅₀ of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .

HY-157324

EGFR-IN-94	EGFR Apoptosis VEGFR	Cancer
EGFR-IN-94 (compound 5a) is a EGFR inhibitor with IC₅₀ of 0.086?μM, and also has IC₅₀ of 0.107μM and 2.52 μM for VEGFR-2 and Topo II, respectively. EGFR-IN-94 induces cell apoptosis and arrests cell cycle at the S phase in HepG-2 cells .

HY-146189

Topoisomerase II inhibitor 9	Topoisomerase Apoptosis	Cancer
Topoisomerase II inhibitor 9 (Compound 19b) is a Topo II inhibitor with an IC₅₀ of 0.97 μM. Topoisomerase II inhibitor 9 is also a classical DNA-intercalator with an IC₅₀ of 43.51 μM. Topoisomerase II inhibitor 9 arrests the cell cycle at the G2/M phase and induces apoptosis in Hep G‐2 cells .

HY-150045

TP0480066	Topoisomerase Bacterial	Infection
TP0480066 is a selective topoisomerase II inhibitor with IC₅₀s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea .

HY-16560

Camptothecin 35+ Cited Publications Campathecin; (S)-(+)-Camptothecin; CPT	Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic	Infection Cancer
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-128979

Deruxtecan analog 2	Drug-Linker Conjugates for ADC	Cancer
Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a agent-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC .

HY-16560S

Camptothecin-d5 Campathecin-d₅; (S)-(+)-Camptothecin-d₅; CPT-d₅	Topoisomerase ADC Cytotoxin 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[1]. 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[2][3].

HY-143280

Topoisomerase II inhibitor 4	Topoisomerase	Cancer
Topoisomerase II inhibitor 4 (compound E17) is a potent Topoisomerase II inhibitor. Topoisomerase II inhibitor 4 triggers G2/M cell cycle arrest and shows anti-tumor activity with strong cytotoxic and anti-proliferative effect .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2063

12-Ethyl-9-hydroxycamptothecin	Alkaloids Structural Classification Monophenols other families Pyrrole Alkaloids Classification of Application Fields Source classification Other Diseases Phenols Quinoline Alkaloids Plants Disease Research Fields	Topoisomerase
12-Ethyl-9-hydroxycamptothecin is a derivative of Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC₅₀ of 679 nM .

HY-16560

Camptothecin 35+ Cited Publications Campathecin; (S)-(+)-Camptothecin; CPT	Infection Alkaloids Structural Classification Classification of Application Fields Source classification Quinoline Alkaloids Camptotheca acuminata Decne. Plants Nyssaceae Disease Research Fields	Topoisomerase ADC Cytotoxin MicroRNA Influenza Virus Apoptosis Fungal Antibiotic
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-N12747

Dichlorogelignate	Structural Classification Source classification Phenols Polyphenols Plants Boraginaceae Arnebia euchroma (Royle) Johnst.	Topoisomerase
Dichlorogelignate (compound 4) is a selective inhibitor of topoisomerase II (Topo II). Dichlorogelignate has 100% inhibition at 50 μM .

HY-N12129

6,6′-Dihydroxythiobinupharidine	Structural Classification Alkaloids Terpenoids Other Alkaloids Sesquiterpenes Source classification Plants Nuphar pumila (Timm) de Candolle Nymphaeaceae	Cathepsin
6,6′-Dihydroxythiobinupharidine is a cysteine proteases inhibitor. 6,6′-Dihydroxythiobinupharidine can enhance DNA cleavage mediated by human topoisomerase IIα and IIβ ~8-fold and ~3-fold, respectively .

HY-101775A

9-Hydroxyellipticine hydrochloride	Structural Classification Alkaloids Carbazole Alkaloids	Topoisomerase
9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. 9-Hydroxyellipticine hydrochloride exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride exhibits IC₅₀ values of 1.6 μM and 1.2μM in Hela S-3 and 293T cells, respectively .

Cat. No.	Product Name	Chemical Structure

HY-16560S

Camptothecin-d5

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[1]. 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[2][3].

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