Topoisomerases are enzymes that regulate the overwinding or underwinding of DNA. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. Topoisomerases are isomerase enzymes that act on the topology of DNA. Type I topoisomerase cuts one strand of a DNA double helix, relaxation occurs, and then the cut strand is reannealed. Type I topoisomerases are subdivided into two subclasses: type IA topoisomerases, which share many structural and mechanistic features with the type II topoisomerases, and type IB topoisomerases, which utilize a controlled rotary mechanism. Type II topoisomerase cuts both strands of one DNA double helix, pass another unbroken DNA helix through it, and then reanneal the cut strands. This class is also split into two subclasses: type IIA and type IIB topoisomerases, which possess similar structure and mechanisms.


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DHAQ DIACETATE

Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity[1][2][3][4]. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively[5].

  • CAS Number: 70711-41-0
  • MF: C24H32N4O8
  • MW: 504.53300
  • Catalog: Apoptosis
  • Density: 1.45g/cm3
  • Boiling Point: 805.7ºC at 760 mmHg
  • Melting Point: 203-5ºC
  • Flash Point: 441.1ºC

Niranthin

Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis treatment[1].

  • CAS Number: 50656-77-4
  • MF: C24H32O7
  • MW: 432.507
  • Catalog: Topoisomerase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 559.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 221.8±30.0 °C

NHC-triphosphate

NHC-triphosphate is an intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate is a weak alternative substrate for the viral polymerase and changes the mobility of the product in polyacrylamide electrophoresis gels[1].

  • CAS Number: 34973-27-8
  • MF: C9H16N3O15P3
  • MW: 499.15600
  • Catalog: HCV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aldoxorubicin•HCl

Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.

  • CAS Number: 1361563-03-2
  • MF: C37H43ClN4O13
  • MW: 787.21
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topoisomerase I inhibitor 4

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[1].

  • CAS Number: 2485135-31-5
  • MF: C23H19FN4O
  • MW: 386.42
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Etoposide

Etoposide is a chemotherapy medication used for the treatments of a number of types of cancer. Etoposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA.

  • CAS Number: 33419-42-0
  • MF: C29H32O13
  • MW: 588.557
  • Catalog: Autophagy
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 798.1±60.0 °C at 760 mmHg
  • Melting Point: 236-251ºC
  • Flash Point: 263.6±26.4 °C

Topoisomerase I inhibitor 9

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[1].

  • CAS Number: 1228150-86-4
  • MF: C23H15Br2FN2
  • MW: 498.19
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pyrazoloacridine

Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment[1][2].

  • CAS Number: 99009-20-8
  • MF: C19H21N5O3
  • MW: 367.40200
  • Catalog: Apoptosis
  • Density: 1.314g/cm3
  • Boiling Point: 595.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 314ºC

6,9-bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione,hydrochloride

Pixantrone (BBR 2778 (free base)) hydrochloride, a mitoxantrone analog, is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity[1][2].

  • CAS Number: 175989-38-5
  • MF: C17H19N5O2
  • MW: 325.36500
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Doxorubicin Hydrochloride

Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair.

  • CAS Number: 25316-40-9
  • MF: C27H30ClNO11
  • MW: 579.980
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 810.3ºC at 760 mmHg
  • Melting Point: 216ºC
  • Flash Point: 443.8ºC

N-(3-Fluoro-4-methyl-8-oxo-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide

Exatecan Intermediate 6 is the intermediate of Exatecan (HY-13631) And Exatecan (DX-8951) is a DNA topoisomerase I inhibitor with an IC50 value of 2.2 μM (0.975 μg/mL) that can be used in cancer research. Exatecan Intermediate 6 can be used to synthesize Antibody-Drug Conjugates (ADCs).

  • CAS Number: 143655-58-7
  • MF: C13H14FNO2
  • MW: 235.25
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anticancer agent 75

Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial[1].

  • CAS Number: 2414491-13-5
  • MF: C22H24N2O
  • MW: 332.44
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

coralyne chloride hydrate

Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage[2]. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes[3].

  • CAS Number: 38989-38-7
  • MF: C22H22ClNO4
  • MW: 399.86700
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 215ºC
  • Flash Point: N/A

Simmitecan hydrochloride

Simmitecan hydrochloride, a 9-substituted lipophilic Camptothecin (HY-16560) derivative, is a potent topoisomerase I inhibitor. Simmitecan hydrochloride is an anticancer agent[1][2].

  • CAS Number: 1247847-78-4
  • MF: C34H39ClN4O6
  • MW: 635.150
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mitoxantrone-d8

Mitoxantrone-d8 (mitozantrone-d8) is the deuterium labeled Mitoxantrone. Mitoxantrone is a topoisomerase II inhibitor and also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM[1][2].

  • CAS Number: 1189974-82-0
  • MF: C22H20D8N4O6
  • MW: 452.53000
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 145 °C
  • Flash Point: N/A

Rebeccamycin

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[1][2].

  • CAS Number: 93908-02-2
  • MF: C27H21Cl2N3O7
  • MW: 570.37800
  • Catalog: ADC Cytotoxin
  • Density: 1.87g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Daunorubicin HCl

Daunorubicin hydrochloride is a topoisomerase II inhibitor with potent antineoplastic activities.

  • CAS Number: 23541-50-6
  • MF: C27H30ClNO10
  • MW: 563.981
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: 770ºC at 760 mmHg
  • Melting Point: 188 - 190ºC
  • Flash Point: 419.5ºC

Topoisomerase I inhibitor 3

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[1].

  • CAS Number: 2588211-50-9
  • MF: C18H14FNO3
  • MW: 311.31
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

7-Ethyl-10-hydroxycamptothecin

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.

  • CAS Number: 86639-52-3
  • MF: C22H20N2O5
  • MW: 392.405
  • Catalog: Autophagy
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 810.3±65.0 °C at 760 mmHg
  • Melting Point: 217 °C
  • Flash Point: 443.8±34.3 °C

Mitoxantrone

Mitoxantrone is a topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.

  • CAS Number: 65271-80-9
  • MF: C22H28N4O6
  • MW: 444.481
  • Catalog: Topoisomerase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 805.7±65.0 °C at 760 mmHg
  • Melting Point: 170-174ºC
  • Flash Point: 441.1±34.3 °C

Trovafloxacin-d4 mesylate

Trovafloxacin-d4 mesylate is the deuterium labeled Trovafloxacin mesylate. Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].

  • CAS Number: 1346601-60-2
  • MF: C21H15D4F3N4O6S
  • MW: 516.48
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topoisomerase II inhibitor 16

Topoisomerase II inhibitor 16 (compound CT3) is a selective, orally active, brain-penetrant and irreversible trypanosomal topoisomerase II inhibitor by stabilizing double-stranded DNA:enzyme cleavage complexes. Topoisomerase II inhibitor 16 has the potential for Chagas disease research[1].

  • CAS Number: 2403729-27-9
  • MF: C19H12F4N6O
  • MW: 416.33
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

erythro-Austrobailignan-6

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[1][2].

  • CAS Number: 114127-24-1
  • MF: C20H24O4
  • MW: 328.4
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topoisomerase II inhibitor 9

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[1].

  • CAS Number: 2413901-61-6
  • MF: C22H17N7O3S2
  • MW: 491.55
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Topoisomerase II inhibitor 7

Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis[1].

  • CAS Number: 2697171-03-0
  • MF: C32H28BrN5O5S
  • MW: 674.56
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Irinotecan hydrochloride

Irinotecan hydrochloride is a water soluble topoisomerase I inhibitor mainly used to treat colon cancer and rectal cancer.

  • CAS Number: 100286-90-6
  • MF: C33H39ClN4O6
  • MW: 623.139
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: 257 °C
  • Melting Point: 250-256°C (dec.)
  • Flash Point: 482ºC

CS-1

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[1].

  • CAS Number: 1448009-94-6
  • MF: C16H12O3
  • MW: 252.265
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 508.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 251.3±23.3 °C

MC-GGFG-AM-(10Me-11F-Camptothecin)

MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells[1].

  • CAS Number: 2873460-70-7
  • MF: C51H56FN9O14
  • MW: 1038.04
  • Catalog: Topoisomerase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+/-)-Evodiamine

(±)-Evodiamine, a quinazolinocarboline alkaloid, is a Top1 inhibitor. Evodiamine exhibits anti-inflammatory, antiobesity, and antitumor effects. (±)-Evodiamine inhibits the proliferation of a wide variety of tumor cells by inducing their apoptosis[1].

  • CAS Number: 518-18-3
  • MF: C19H17N3O
  • MW: 303.358
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 575.1±50.0 °C at 760 mmHg
  • Melting Point: 272 °C
  • Flash Point: 301.6±30.1 °C

NH2-methylpropanamide-Exatecan TFA

NH2-methylpropanamide-Exatecan TFA is a methylpropanamide-modified Exatecan (HY-13631), which is the common ADC Cytotoxin used in the synthesis of ADC. Exatecan is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research[1].

  • CAS Number: 1817857-35-4
  • MF: C30H30F4N4O7
  • MW: 634.58
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A