Topo II Selective Inhibitors | Activators

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1228 Idarubicin HCl

Idarubicin HCl (4-demethoxydaunorubicin, NSC256439, 4-DMDR) is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay. Idarubicin induces mTOR-dependent cytotoxic autophagy.

Selective Topo II (MCF-7 cells), IC50: 3.3 ng/mL
S3181 Flumequine

Flumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM.

Selective Topo II, IC50: 15 μM
S1367 Amonafide

Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.

Selective
S1393 Pirarubicin (NSC-333054)

Pirarubicin (NSC-333054) is an anthracycline antibiotic, and also a DNA/RNA synthesis inhibitor by intercalating into DNA and interacts with topoisomerase II, used as an antineoplastic agent.

Selective
S5627 Amsacrine hydrochloride

Amsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.

Selective
S1208 Doxorubicin (Adriamycin) HCl

Doxorubicin (Adriamycin, NSC 123127, DOX, Hydroxydaunorubicin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage, mitophagy and apoptosis in tumor cells. Doxorubicin reduces basal phosphorylation of AMPK. Doxorubicin is used in the concomitant treatment of HIV-infected patients but is found to be at high risk of HBV reactivation.

Selective
S1342 Genistein (NPI 031L)

Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.

Selective
S6790 Ellipticine hydrochloride

Ellipticine Hydrochloride (NSC 71795, PZE) is a potent inhibitor of DNA topoisomerase II and forms covalent DNA adducts mediated by its oxidation with cytochromes P450 (CYP) and peroxidases. Ellipticine Hydrochloride is a natural product isolated from the Australian evergreen tree of the Apocynaceae family with antineoplastic activity.

Selective
S4119 Pefloxacin Mesylate Dihydrate

Pefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.

Selective
S5059 Pixantrone Maleate

Pixantrone (BBR-2778) is a novel aza-anthracenedione compound with antitumor activity. It is a weak topoisomerase II inhibitor and forms stable DNA adducts through alkylation with specificity for DNA hypermethylated sites.

Selective
S5008 Ciprofloxacin hydrochloride

Ciprofloxacin (CPX, Cetraxal, Ciloxan, Cipro, Bay-09867) hydrochloride, a fluorinated quinolone, is a β-diketone antibiotic with a broad spectrum antibacterial activity. Ciprofloxacin is an inhibitor of bacterial DNA gyrase (a subclass of Type II topoisomerases).

Selective
S9634 Phenoxodiol (Haginin E)

Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.

Selective
S1222 Dexrazoxane HCl (ICRF-187)

Dexrazoxane HCl (ICRF-187, ADR-529) is an intracellular iron chelator, which decreases the formation of superoxide radicals, used as a cardioprotective agent; also an inhibitor of topoisomerase II

Selective
S2064 Balofloxacin

Balofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase.

Selective
S1225 Etoposide (VP-16)

Etoposide (VP-16, VP-16213) is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. Etoposide induces autophagy, mitophagy and apoptosis.

Selective
S7518 Voreloxin (SNS-595) hydrochloride

Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

Selective
s4604 Levofloxacin hydrate

Levofloxacin (Levaquin, Tavanic, Quixin, Iquix, Cravit) is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active L-isomer of ofloxacin with antibacterial activity. It acts by inhibiting DNA gyrase (bacterial topoisomerase II).

Selective
S1787 Teniposide

Teniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL).

Selective
S2485 Mitoxantrone (NSC-301739) 2HCl

Mitoxantrone 2HCl (NSC-301739) is a dihydrochloride salt of Mitoxantrone. Mitoxantrone is an inhibitor of type II topoisomerase and protein kinase C (PKC) with IC50 of 8.5 μM for PKC. Mitoxantrone inhibits cell proliferative growth of MCF-7/wt cells with IC50 of 0.42 μM. Mitoxantrone also induces apoptosis.

Selective
S2492 Novobiocin Sodium (NSC 2382)

Novobiocin Sodium (NSC 2382, Albamycin, Cathomycin) is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria.

Pan
S5964 Gatifloxacin hydrochloride

Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively.

Pan
S4006 Clinafloxacin

Clinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae.

Pan
S1464 Marbofloxacin

Marbofloxacin is a potent antibiotic inhibiting bacterial DNA replication.

Pan
S1465 Moxifloxacin (BAY12-8039) HCl

Moxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent.

Pan
S2271 Berberine chloride (NSC 646666)

Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation

Pan
S1463 Ofloxacin

Ofloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent.

Pan
S1340 Gatifloxacin

Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.

Pan
S1756 Enoxacin

Enoxacin (AT-2266, CI919, Pd107779, NSC 629661) is an oral broad-spectrum fluoroquinolone antibacterial agent by inhibiting bacterial DNA gyrase and topoisomerase IV, used to treat a wide variety of infections.

Pan
S1940 Levofloxacin

Levofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections.

Pan
S1327 Ellagic acid

Ellagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property.

Pan
S2328 Nalidixic acid

Nalidixic acid (NSC-82174) is a synthetic 1,8-naphthyridine antimicrobial agent with a limited bacteriocidal spectrum. It is an inhibitor of the A subunit of bacterial DNA gyrase.

Pan