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Topoisomerase I inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Topoisomerase (241) ADC Antibody (1) ADC Payload (46) AMPK (3) Androgen Receptor (3) Antibiotic (24) Antibody-Drug Conjugates (ADCs) (10) Apoptosis (49) ATM/ATR (1) Autophagy (27) Bacterial (17) Bcl-2 Family (3) Biochemical Assay Reagents (2) Btk (1) Caspase (5) CCR (1) Cholinesterase (ChE) (3) Cuproptosis (1) Cytochrome P450 (2) DNA Alkylator/Crosslinker (1) DNA-PK (1) DNA/RNA Synthesis (24) Drug Derivative (5) Drug Intermediate (4) Drug Metabolite (5) Drug-Linker Conjugates for ADC (54) EGFR (4) Elastase (1) Endogenous Metabolite (6) Estrogen Receptor/ERR (3) Fatty Acid Synthase (FASN) (1) Fluorescent Dye (3) Fungal (6) GLUT (2) Glutathione Peroxidase (1) HBV (3) Histone Methyltransferase (1) HIV (6) HSV (1) IAP (1) Indoleamine 2,3-Dioxygenase (IDO) (2) Influenza Virus (5) Integrin (1) Isotope-Labeled Compounds (15) Liposome (1) MDM-2/p53 (3) MicroRNA (3) Microtubule/Tubulin (14) Mitochondrial Metabolism (2) Mitophagy (6) Mixed Lineage Kinase (1) Mucin (1) Necroptosis (1) NF-κB (6) NO Synthase (1) Orthopoxvirus (2) Parasite (13) PARP (1) Peptide-Drug Conjugates (PDCs) (1) PI3K (1) Proteasome (3) Reactive Oxygen Species (ROS) (5) Reference Standards (22) RIP kinase (1) Sodium Channel (1) Survivin (1) TROP2 (1) α-synuclein (1)
By Research Areas:	Cancer (260) Cardiovascular Disease (1) Infection (37) Inflammation/Immunology (18) Metabolic Disease (2) Neurological Disease (2)
Click Chemistry:	ADC Synthesis (1) DBCO (3) Alkynes (2)

284

Inhibitors & Agonists

Fluorescent Dye

Biochemical Assay Reagents

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: Topoisomerase Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N3488

Isodiospyrin	Topoisomerase Bacterial Fungal	Infection Cancer
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 .

HY-148058

Topoisomerase I inhibitor 8	Topoisomerase	Cancer
Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells .

HY-162587

Fagopyrine	Topoisomerase	Cancer
Fagopyrine is a DNA topoisomerase I (Topo I) inhibitor. Fagopyrine is a photosensitizer that can be used in the study of tumors .

HY-178373

Topoisomerase I-IN-18	Topoisomerase DNA/RNA Synthesis Reactive Oxygen Species (ROS) MDM-2/p53 Caspase	Cancer
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 .

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-156969

Topoisomerase I inhibitor 11	Topoisomerase Btk	Cancer
Topoisomerase I inhibitor 11 is a potent inhibitor of *Topoisomerase* I. Topoisomerase I inhibitor 11 can bind to BTK .

HY-144774

Topoisomerase I inhibitor 5	Topoisomerase DNA/RNA Synthesis Apoptosis	Cancer
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 .

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-162341

Topoisomerase I inhibitor 15	Topoisomerase	Cancer
Topoisomerase I inhibitor 15 (compound 4b) is an inhibitor of topoisomerase I with anticancer activity. Topoisomerase I inhibitor 15 inhibits A549 cells with an IC₅₀ of 7.34 μM .

HY-143266

Topoisomerase I inhibitor 3	Topoisomerase Apoptosis	Cancer
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 .

HY-161082

Topoisomerase I inhibitor 12	Topoisomerase	Cancer
Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity .

HY-146437

Topoisomerase I inhibitor 6	Topoisomerase	Cancer
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 .

HY-169628

Topoisomerase I/II inhibitor 7	Topoisomerase	Cancer
Topoisomerase I/II inhibitor 7 (Compound 5h) is a **Topoisomerase I/II** inhibitor .

HY-143265

Topoisomerase I inhibitor 2	Topoisomerase Apoptosis Caspase	Cancer
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 .

HY-168739

Topoisomerase I inhibitor 17	Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis	Cancer
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 .

HY-146504

Topoisomerase I/II inhibitor 3	Topoisomerase PI3K Apoptosis Reactive Oxygen Species (ROS)	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-146497

Topoisomerase I inhibitor 7	Topoisomerase	Cancer
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-143301

Topoisomerase I inhibitor 4	Topoisomerase	Cancer
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC₅₀s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer .

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-156464

Topoisomerase I inhibitor 10	Topoisomerase	Infection
Topoisomerase I inhibitor 10 (compound 13) is a *leishmanial topoisomerase* IB** inhibitor. Topoisomerase I inhibitor 10 has antileishmanial activity against L. donovani promastigotes, with the IC₅₀ of 27.91 μM .

HY-143402

Topoisomerase I/II inhibitor 2	Topoisomerase	Cancer
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 .

HY-161385

Topoisomerase I inhibitor 16	Topoisomerase	Cancer
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 .

HY-16562

Irinotecan 60+ Cited Publications (+)-Irinotecan; CPT-11; VAL-413(free base)	Topoisomerase Autophagy	Cancer
Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex .

HY-156462

Topoisomerase I inhibitor 9	Topoisomerase	Infection
Topoisomerase I inhibitor 9 (compound 3d) is a *leishmanial topoisomerase* IB** inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC₅₀ of 34.81μM .

HY-159783

Mal-Exatecan	ADC Payload Topoisomerase	Cancer
Mal-Exatecan is a Mal (Maleimide) modified Exatecan (HY-13631), a DNA topoisomerase I (topoisomerase I) inhibitor .

HY-122014

S 39625	Topoisomerase	Others
39625 is a camptothecin ketone analogue, a stable, potent and selective topoisomerase I inhibitor, active against purified topoisomerase I and cytotoxic to cancer cells.

HY-168632

Topoisomerase I/II inhibitor 6	Topoisomerase Apoptosis	Cancer
Topoisomerase I/II inhibitor 6 (compound 3i) is a potent inhibitor of topoisomerase I and II with IC₅₀s of 4.77 and 15 µM, respectively. Topoisomerase I/II inhibitor 6 shows antiproliferative activities against human melanoma LOX IMVI cancer cell line with IC₅₀ values of 26.7 and 25.4 µM, respectively. Topoisomerase I/II inhibitor 6 provokes substantial levels of early, late apoptosis and increases the expression level of active caspase-3 .

HY-19825

Rebeccamycin	Topoisomerase ADC Payload Antibiotic	Cancer
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 .

HY-162342

Topoisomerase I inhibitor 14	Topoisomerase	Cancer
Topoisomerase I inhibitor 14 (Compound 4h) is an inhibitor for Topoisomerase I. Topoisomerase I inhibitor 14 inhibits proliferation of A549 and C6 with IC₅₀s of 4.56 μM and 13.17 μM, without significant toxicity in healthy cells NIH3T3 (IC₅₀ is 74.44 μM), which exhibits anticancer potency .

HY-16562S1

Irinotecan-d10 hydrochloride	Isotope-Labeled Compounds Topoisomerase Autophagy	Cancer
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-16562S

Irinotecan-d10 (+)-Irinotecan-d₁₀; CPT-11-d₁₀; VAL-413-d₁₀	Topoisomerase Autophagy	Cancer
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-125930A

T-2513 hydrochloride	Topoisomerase DNA/RNA Synthesis	Cancer
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 .

HY-125930

T-2513	Topoisomerase DNA/RNA Synthesis	Cancer
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 .

HY-N15319

Eupolauridine Canangine	Topoisomerase Fungal	Infection
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-14821

Namitecan ST-1968	Topoisomerase	Cancer
Namitecan is a potent topoisomerase I inhibitor, with antitumor property.

HY-16562R

Irinotecan (Standard) (+)-Irinotecan (Standard); CPT-11 (Standard); VAL-413(free base) (Standard)	Reference Standards Topoisomerase Autophagy	Cancer
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 .

HY-13768A

Topotecan hydrochloride 30+ Cited Publications SKF 104864A hydrochloride; NSC 609669 hydrochloride	Topoisomerase Autophagy Apoptosis	Cancer
Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

HY-14812

Karenitecin 1 Publications Verification Cositecan; BNP 1350	Topoisomerase	Cancer
Karenitecin (Cositecan) is a topoisomerase I inhibitor, with potent anti-cancer activity.

HY-N10115

Huanglongmycin N	Topoisomerase	Cancer
Huanglongmycin N is a *DNA topoisomerase* I** inhibitor (EC₅₀ = 14 μM).

HY-18350A

Indimitecan hydrochloride LMP776 hydrochloride	Topoisomerase	Cancer
Indimitecan hydrochloride is a topoisomerase I (Top1) inhibitor with anticancer activities .

HY-175034

Topoisomerase I/II-IN-1	Topoisomerase Apoptosis MDM-2/p53 Bcl-2 Family Caspase	Cancer
Topoisomerase I/II-IN-1 is a dual inhibitor of **topoisomerase I/II*. Topoisomerase* I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer .

HY-13566A

Belotecan hydrochloride 2 Publications Verification CKD-602	Topoisomerase	Cancer
Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative.

HY-16568

Irinotecan hydrochloride trihydrate 60+ Cited Publications (+)-Irinotecan hydrochloride trihydrate; CPT-11 hydrochloride trihydrate	Topoisomerase Autophagy	Cancer
Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity .

HY-169509

Topoisomerase I/II inhibitor 8	PARP Necroptosis Topoisomerase RIP kinase Mixed Lineage Kinase	Cancer
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 .

HY-119892

Batracylin NSC 320846; BAY-H 2049	Topoisomerase	Cancer
Batracylin (NSC320846) is a potent *DNA Topoisomerases* I and DNA Topoisomerases II** inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .

HY-16228

Genz-644282 2 Publications Verification	Topoisomerase	Cancer
Genz-644282 is a non-camptothecin topoisomerase I inhibitor, used for cancer research.

HY-18350

Indimitecan LMP776	Topoisomerase	Cancer
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities .

HY-N4329

Nidulalin A	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-13758

TAS-103 BMS-247615	Topoisomerase	Cancer
TAS-103 is a dual inhibitor of DNA **topoisomerase I/II**, used for cancer research.

HY-13758A

TAS-103 dihydrochloride 1 Publications Verification BMS-247615 dihydrochloride	Topoisomerase	Cancer
TAS-103 dihydrochloride is a dual inhibitor of DNA **topoisomerase I/II**, used for cancer research.

Cat. No.	Product Name	Type

HY-164152

ADC Control Human IgG1-Deruxtecan (DAR 4)	Fluorescent Dye
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

ADC Control Human IgG1-Deruxtecan (DAR 8)	Fluorescent Dye
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-164762

Trastuzumab rezetecan SHR-A1811	Fluorescent Dye
Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .

HY-138298A

Trastuzumab deruxtecan

2 Publications Verification

DS-8201; DS-8201a

Fluorescent Dye

Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd), and the drug-linker conjugate for ADC is Deruxtecan (HY-13631E). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .

HY-13631AG

Exatecan (mesylate) (GMP) DX8951f (GMP)	Fluorescent Dye
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-N2306R

Aclacinomycin A (Standard)

Aclarubicin (Standard)

Fluorescent Dye

Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-177442

DS-3939a

DS-3939

Fluorescent Dye

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-143692

SQDG	Biochemical Assay Reagents
SQDG inhibits topoisomerase I and P-selectin receptor, exhibits anti-inflammatory, antiviral and antitumor activities. SQDG is a glycolipid that possesses sugar moieties in their head groups. SQDG is a membrane lipid that can be used to investigate the effects of structural lipid in LNP formulations .

HY-13631AG

Exatecan (mesylate) (GMP) DX8951f (GMP)	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

HY-P10765

DTS-108	Peptide-Drug Conjugates (PDCs) Topoisomerase	Cancer
DTS-108 is a prodrug of SN38 (HY-13704) (a Topoisomerase I inhibitor). DTS-108 is a conjugate generated by linking SN38 to a human oligopeptide via an esterase sensitive cross-linker. DTS-108 exhibits anti-tumor activity against colorectal, lung, and mammary cancer .

Cat. No.	Product Name	Target	Research Area

HY-P99813

Patritumab deruxtecan HER3-DXd; U3-1402	Antibody-Drug Conjugates (ADCs)	Cancer
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .

HY-P99843

Datopotamab 1 Publications Verification	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-164152

ADC Control Human IgG1-Deruxtecan (DAR 4)	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) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N3488

Isodiospyrin	Quinones other families Diospyros virginiana L. Source classification Benzene Quinones Plants	Topoisomerase Bacterial Fungal
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 .

HY-13768A

Topotecan hydrochloride 30+ Cited Publications SKF 104864A hydrochloride; NSC 609669 hydrochloride	Alkaloids Monophenols Classification of Application Fields Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Plants Nyssaceae Disease Research Fields Cancer	Topoisomerase Autophagy Apoptosis
Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

HY-16562A

Irinotecan hydrochloride 60+ Cited Publications (+)-Irinotecan hydrochloride; CPT-11 hydrochloride; VAL-413	Alkaloids Classification of Application Fields Source classification Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields Cancer	Topoisomerase Autophagy
Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .

HY-100309

9-Aminocamptothecin 1 Publications Verification 9-Amino-20(S)-camptothecin; 9-Amino-CPT	Alkaloids Classification of Application Fields Source classification Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields Indole Alkaloids Cancer	Topoisomerase
9-Aminocamptothecin (9-Amino-CPT) is a topoisomerase I inhibitor with potent anticancer activity .

HY-N0275

(±)-10-Hydroxycamptothecin (±)-10-HCPT	Alkaloids Monophenols Pyrrole Alkaloids Classification of Application Fields Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields Cancer	Topoisomerase
(±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.

HY-N2063

12-Ethyl-9-hydroxycamptothecin	Alkaloids 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-19825

Rebeccamycin	Microorganisms Classification of Application Fields Antibiotics Source classification Disease Research Anticancer Disease Research Fields Other Antibiotics Cancer	Topoisomerase ADC Payload Antibiotic
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 .

HY-N15319

Eupolauridine Canangine	Alkaloids Other Alkaloids Cananga odorata Source classification Plants Annonaceae	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

Huanglongmycin N	Quinones Microorganisms Classification of Application Fields Anthraquinones Source classification Phenols Polyphenols Disease Research Fields Cancer	Topoisomerase
Huanglongmycin N is a *DNA topoisomerase* I** inhibitor (EC₅₀ = 14 μM).

HY-N4329

Nidulalin A	Microorganisms Ketones, Aldehydes, Acids Source classification	Topoisomerase
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-W897655

20-O-Acetylcamptothecin O-Acetylcamptothecin	Alkaloids Source classification Camptotheca acuminata Decne. Nyssaceae Plants Isoquinoline Alkaloids	Topoisomerase
20-O-Acetylcamptothecin (O-Acetylcamptothecin) is a derivative of Camptothecin (HY-16560) and an inhibitor of *Topoisomerase* I .

HY-N6800

Netropsin	Natural Products Microorganisms Source classification	Antibiotic DNA/RNA Synthesis Bacterial Influenza Virus Orthopoxvirus
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder) and antibiotic, inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei. Netropsin dihydrochloride has antibacterial and antiviral activity .

HY-N6800A

Netropsin dihydrochloride	Classification of Application Fields Inflammation/Immunology Disease Research Fields	Antibiotic DNA/RNA Synthesis Bacterial Influenza Virus Orthopoxvirus
Netropsin dihydrochloride is a small-molecule MGB (minor-groove binder) and antibiotic, inhibits the catalytic activity of isolated topoisomerase and interferes with the stabilization of the cleavable complexes of topoisomerase II and I in nuclei. Netropsin dihydrochloride has antibacterial and antiviral activity .

HY-W713570

Nectandrin B	Monophenols Saururaceae Saururus chinensis (Lour.) Baill. Source classification Phenols Plants	Topoisomerase
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 .

HY-N10367

Corydamine	Alkaloids Corydalis bulleyana Diels Classification of Application Fields Source classification Plants Isoquinoline Alkaloids Disease Research Fields Papaveraceae Cancer	Topoisomerase
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity .

HY-N6714

Alternariol	Infection Microorganisms Classification of Application Fields Source classification Phenols Polyphenols Disease Research Fields	Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis
Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-121309

Doxorubicinone 2 Publications Verification Adriamycin aglycone; Adriamycinone	Quinones Classification of Application Fields Anthraquinones Source classification Endogenous metabolite Disease Research Fields Cancer	Endogenous Metabolite
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human *DNA topoisomerase* I and topoisomerase II inhibitor with IC₅₀**s of 0.8 μM and 2.67 μM, respectively.

HY-13768AR

Topotecan hydrochloride (Standard) SKF 104864A hydrochloride (Standard); NSC 609669 hydrochloride (Standard)	Alkaloids Monophenols Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants	Reference Standards Topoisomerase Autophagy Apoptosis
Topotecan (hydrochloride) (Standard) is the analytical standard of Topotecan (hydrochloride). This product is intended for research and analytical applications. Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

HY-N6714R

Alternariol (Standard)	Microorganisms Source classification Phenols Polyphenols	Reference Standards Topoisomerase Androgen Receptor Estrogen Receptor/ERR Apoptosis
Alternariol (Standard) is the analytical standard of Alternariol. This product is intended for research and analytical applications. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-13555

β-Lapachone 10+ Cited Publications ARQ-501; NSC-26326	Quinones other families Classification of Application Fields Source classification Plants Naphthalene Quinones Disease Research Fields Cancer	Indoleamine 2,3-Dioxygenase (IDO) Topoisomerase Autophagy Apoptosis
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

HY-N2198

Podocarpusflavone A	Flavonoids Classification of Application Fields Guttiferae Source classification Phenols Polyphenols Plants Garcinia subelliptica Biflavones Disease Research Fields Cancer	Topoisomerase Apoptosis
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .

HY-16562AR

Irinotecan hydrochloride (Standard) (+)-Irinotecan hydrochloride (Standard); CPT-11 hydrochloride (Standard); VAL-413 (Standard)	Alkaloids Source classification Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants	Reference Standards Topoisomerase Autophagy
Irinotecan (hydrochloride) (Standard) is the analytical standard of Irinotecan (hydrochloride). This product is intended for research and analytical applications. Irinotecan hydrochloride ((+)-Irinotecan hydrochloride) is a topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer .

HY-121309R

Doxorubicinone (Standard) Adriamycin aglycone (Standard); Adriamycinone (Standard)	Quinones Anthraquinones Source classification Endogenous metabolite	Reference Standards Endogenous Metabolite
Doxorubicinone (Standard) is the analytical standard of Doxorubicinone. This product is intended for research and analytical applications. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin . Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.

HY-10529

Betulinic acid 25+ Cited Publications Lupatic acid; Betulic acid	Infection Triterpenes other families Classification of Application Fields Terpenoids Source classification Plants Endogenous metabolite Inflammation/Immunology Disease Research Fields	Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite Parasite
Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties .

HY-N0275R

(±)-10-Hydroxycamptothecin (Standard)	Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants	Topoisomerase
(±)-10-Hydroxycamptothecin (Standard) is the analytical standard of (±)-10-Hydroxycamptothecin. This product is intended for research and analytical applications. (±)-10-Hydroxycamptothecin is an indole alkaloid that inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity.

HY-15142

Doxorubicin hydrochloride Maximum Cited Publications 581 Publications Verification Hydroxydaunorubicin hydrochloride; ADR	Infection Quinones Structural Classification Microorganisms Classification of Application Fields Anthraquinones Source classification Disease Research Fields	Topoisomerase ADC Payload AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Fluorescent Dye
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 .

HY-N2306A

Aclacinomycin A hydrochloride Aclarubicin hydrochloride	Quinones Microorganisms Classification of Application Fields Anthraquinones Source classification Phenols Polyphenols Disease Research Fields Cancer	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Aclarubicin) hydrochloride is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A hydrochloride is an inhibitor of topoisomerase I and II. Aclacinomycin A hydrochloride inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A hydrochloride might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-N2306

Aclacinomycin A 5 Publications Verification Aclarubicin	Quinones Microorganisms Anthraquinones	Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-13744

Rubitecan RFS 2000; 9-Nitrocamptothecin	Alkaloids Classification of Application Fields Source classification Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields Cancer	Topoisomerase
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 .

HY-A0210

Cerulenin 5+ Cited Publications	Microorganisms Antifungal Classification of Application Fields Antibiotics Source classification Metabolic Disease Mammalian Cell Culture Disease Research Anticancer Disease Research Fields Other Antibiotics	Fatty Acid Synthase (FASN) Fungal Apoptosis Antibiotic
Cerulenin, a potent, natural inhibitor of fatty acid synthase (FASN), is an epoxide produced by the fungus Cephalosporium caeruleus. Cerulenin inhibits topoisomerase I catalytic activity and augments SN-38-induced apoptosis. Cerulenin has antifungal and antitumor activies .

HY-15142A

Doxorubicin Hydroxydaunorubicin	Infection Quinones Structural Classification Microorganisms Classification of Application Fields Anthraquinones Source classification Phenols Polyphenols Disease Research Fields	ADC Payload Antibiotic Bacterial Topoisomerase AMPK HIV Autophagy Mitophagy Apoptosis HBV Fluorescent Dye
Doxorubicin (Hydroxydaunorubicin), a broad-spectrum anthracycline antibiotic with cytotoxic properties, is an anti-cancer chemotherapy agent. Doxorubicin has fluorescence properties. Doxorubicin inhibits topoisomerase II with an IC₅₀ of 2.67 μM, thus stopping DNA replication. Doxorubicin reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin induces apoptosis and autophagy . Doxorubicin inhibits human *DNA topoisomerase* I with an IC₅₀** of 0.8 μM .

HY-N10495

Seconeolitsine	Infection Microorganisms Classification of Application Fields Antibiotics Source classification Disease Research Fields	Antibiotic Bacterial Topoisomerase
Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC₅₀ value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics .

HY-N11536

erythro-Austrobailignan-6	Saururaceae Saururus chinensis (Lour.) Baill. Source classification Lignans Phenylpropanoids Plants	Topoisomerase Apoptosis
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-13704

SN-38 65+ Cited Publications 7-Ethyl-10-hydroxycamptothecin	Alkaloids Classification of Application Fields Labiatae Samanea saman (Jacq.) Merr. Source classification Quinoline Alkaloids Plants Disease Research Fields Cancer	Drug Metabolite Topoisomerase ADC Payload Autophagy
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-16560

Camptothecin 55+ Cited Publications Campathecin; (S)-(+)-Camptothecin; CPT	Infection Alkaloids Classification of Application Fields Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields	Topoisomerase ADC Payload 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-13555R

β-Lapachone (Standard)	Quinones other families Source classification Plants Naphthalene Quinones	Indoleamine 2,3-Dioxygenase (IDO) Topoisomerase Autophagy Apoptosis
β-Lapachone (Standard) is the analytical standard of β-Lapachone. This product is intended for research and analytical applications. β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.

HY-15142R

Doxorubicin hydrochloride (Standard) 3 Publications Verification Hydroxydaunorubicin hydrochloride (Standard); ADR (Standard)	Quinones Structural Classification Microorganisms Anthraquinones Source classification	Reference Standards Topoisomerase ADC Payload AMPK Autophagy Apoptosis HIV HBV Mitophagy Antibiotic Bacterial Fluorescent Dye
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-10529R

Betulinic acid (Standard) Lupatic acid (Standard); Betulic acid (Standard)	Triterpenes other families Terpenoids Source classification Plants Endogenous metabolite	Reference Standards Apoptosis Topoisomerase HIV Autophagy Mitophagy NF-κB Endogenous Metabolite Parasite
Betulinic acid (Standard) is the analytical standard of Betulinic acid. This product is intended for research and analytical applications. Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties .

HY-N2306R

Aclacinomycin A (Standard) Aclarubicin (Standard)	Quinones Microorganisms Anthraquinones	Reference Standards Topoisomerase DNA/RNA Synthesis Proteasome Antibiotic
Aclacinomycin A (Standard) is the analytical standard of Aclacinomycin A. This product is intended for research and analytical applications. Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis .

HY-N5038

Mauritianin	Flavonols Classification of Application Fields Source classification Erythrina stricta Roxb. Plants Compositae Acalypha indica Linn. Flavonoids Phenols Polyphenols Euphorbiaceae Disease Research Fields Cancer	Topoisomerase
Mauritianin is an orally active kaempferol glycoside. Mauritianin can be isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor. Mauritianin has hepatoprotective, neuroprotective, and renoprotective activities. Mauritianin increases vascular tone when used in combination with Alcesefoliside (HY-N5049) .

HY-16560R

Camptothecin (Standard) Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)	Alkaloids Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants	Reference Standards Topoisomerase ADC Payload MicroRNA Influenza Virus Apoptosis Fungal Antibiotic
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-W046353

2-Methoxycinnamaldehyde o-Methoxycinnamaldehyde	Cinnamomum cassia (L.) D. Don Classification of Application Fields Simple Phenylpropanols Source classification Phenylpropanoids Plants Lauraceae Disease Research Fields Cancer	Apoptosis NF-κB Topoisomerase Mitochondrial Metabolism Caspase
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-13704R

SN-38 (Standard) 7-Ethyl-10-hydroxycamptothecin (Standard)	Alkaloids Labiatae Samanea saman (Jacq.) Merr. Source classification Quinoline Alkaloids Plants	Drug Metabolite Reference Standards Topoisomerase ADC Payload Autophagy
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-N0095

(S)-10-Hydroxycamptothecin 1 Publications Verification 10-HCPT; 10-Hydroxycamptothecin	Alkaloids Monophenols Pyrrole Alkaloids Classification of Application Fields Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants Disease Research Fields Cancer	Topoisomerase Apoptosis
(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-W046353R

2-Methoxycinnamaldehyde (Standard) o-Methoxycinnamaldehyde (Standard)	Cinnamomum cassia (L.) D. Don Simple Phenylpropanols Source classification Phenylpropanoids Plants Lauraceae	Reference Standards Apoptosis NF-κB Mitochondrial Metabolism Caspase Topoisomerase
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-B0147

Pefloxacin 2 Publications Verification 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-N0095R

(S)-10-Hydroxycamptothecin (Standard) 10-HCPT (Standard); 10-Hydroxycamptothecin (Standard)	Alkaloids Monophenols Pyrrole Alkaloids Source classification Phenols Quinoline Alkaloids Camptotheca acuminata Decne. Nyssaceae Plants	Reference Standards Topoisomerase Apoptosis
(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-Y0790R

Cuminaldehyde (Standard) p-Isopropylbenzaldehyde (Standard)	Ketones, Aldehydes, Acids Rudbeckia laciniata L. Source classification Umbelliferae Plants Endogenous metabolite	α-synuclein Reference Standards
Cuminaldehyde Standard is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC₅₀= 0.00085 mg/mL) and α-glucosidase (IC₅₀=0.5 mg/mL). Cuminaldehyde also inhibits the fibrillation of α-synuclein and prevents its aggregation Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases .

Cat. No.	Product Name	Chemical Structure

HY-16562S1

Irinotecan-d10 hydrochloride
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-16562S

Irinotecan-d10
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-13566AS

Belotecan-d7 hydrochloride
Belotecan-d₇ (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative .

HY-13631DS

Dxd-d5
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-13631AS

Exatecan-d5 mesylate
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-13704S

SN-38-d3
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-W653896

Alternariol-d2

Alternariol-d₂ is deuterium labeled Alternariol. Alternariol is an orally ingested mycotoxin produced by Alternaria, capable of inhibiting the activity of topoisomerase I and II (topoisomerase I, topoisomerase II). Alternariol has weak estrogenic (Estrogen Receptor/ERR) and androgen/antiandrogen (Androgen Receptor) effects. Alternariol can induce apoptosis, trigger cell cycle arrest, suppress innate immune responses, and exhibit anti-tumor activity. Alternariol has genotoxic, mutagenic, and endocrine-disrupting effects .

HY-16562AS

Irinotecan-d5 hydrochloride
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-13631AS1

Exatecan-d3 mesylate
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-126373S1

SN-38 glucuronide-13C6
SN-38 glucuronide- ¹³C₆ is the ¹³C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .

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 . 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-W744739

Betulinic acid-d3
Betulinic acid-d₃ (Lupatic acid-d₃) is a deuterium labeled Betulinic acid (HY-10529). Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties .

HY-132561S

RPR121056-d3
RPR121056-d₃ is the deuterium labeled RPR121056. RPR121056 is a metabolite of Irinotecan (HY-16562), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE .

HY-W653919

SN-38 glucuronide-d3
SN-38 glucuronide-d₃ is deuterium labeled SN-38 glucuronide. SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .

HY-13768S1

Topotecan-d6
Topotecan-d₆ is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC₅₀ values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95 μM of GSCs-U87 .

HY-13768S

Topotecan-d5
Topotecan-d₅ is the deuterium labeled Topotecan. Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC₅₀ values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87 .

HY-N0095S

(S)-10-Hydroxycamptothecin-d5
(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-B0147S1

Pefloxacin-d3

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

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 .

Cat. No.	Product Name		Classification

HY-160788

DBCO-β-Glu-PEG12-Exatecan		DBCO
DBCO-β-Glu-PEG12-Exatecan (Compound 107) is an inhibitor for topoisomerase I. DBCO-β-Glu-PEG12-Exatecan can be used as a Drug-Linker Conjugate for ADC molecule .

HY-164792

DBCO-PEG3-VC-Exatecan		DBCO
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) .

HY-134723

DBCO-PEG4-GGFG-Dxd		DBCO ADC Synthesis
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-163099

P5(PEG24)-VC-PAB-Exatecan		Alkynes
P5(PEG24)-VC-PAB-Exatecan (LP5) 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(PEG24)-VC-PAB-Exatecan can be used for the research of tumor .

HY-173625

P5(PEG12)-VC-PAB-Exatecan		Alkynes
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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