トポイソメラーゼ
阻害剤の選択性比較
カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
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水 | DMSO | アルコール | ||
S1208 | Doxorubicin (Adriamycin) HCl | 20 mg/mL | 100 mg/mL | <1 mg/mL |
S1225 | Etoposide | <1 mg/mL | 100 mg/mL | <1 mg/mL |
S1288 | Camptothecin | <1 mg/mL | 3 mg/mL | '<1 mg/mL |
S1231 | Topotecan HCl | 91 mg/mL | 91 mg/mL | <1 mg/mL |
S1198 | Irinotecan | <1 mg/mL | 7 mg/mL | <1 mg/mL |
S2653 | 9-amino-CPT (9-Aminocamptothecin) | <1 mg/mL | 25 mg/mL | <1 mg/mL |
S0093 | Genz-644282 | <1 mg/mL | <1 mg/mL | <1 mg/mL |
S2288 | Rubitecan | <1 mg/mL | 58 mg/mL | <1 mg/mL |
S1228 | Idarubicin HCl | 5 mg/mL | 100 mg/mL | <1 mg/mL |
S1223 | Epirubicin HCl | 100 mg/mL | 100 mg/mL | <1 mg/mL |
S2485 | Mitoxantrone 2HCl | 89 mg/mL | 89 mg/mL | <1 mg/mL |
S3035 | Daunorubicin HCl | 100 mg/mL | 100 mg/mL | <1 mg/mL |
S1465 | Moxifloxacin HCl | 60 mg/mL | 87 mg/mL | <1 mg/mL |
S2217 | Irinotecan HCl Trihydrate | 1 mg/mL | 100 mg/mL | 7 mg/mL |
S4908 | SN-38 | <1 mg/mL | 21 mg/mL | <1 mg/mL |
S1367 | Amonafide | <1 mg/mL | 57 mg/mL | 4 mg/mL |
S1787 | Teniposide | <1 mg/mL | 40 mg/mL | <1 mg/mL |
S1340 | Gatifloxacin | <1 mg/mL | 7 mg/mL | <1 mg/mL |
S1222 | Dexrazoxane HCl (ICRF-187) | 60 mg/mL | 60 mg/mL | <1 mg/mL |
S1342 | Genistein | <1 mg/mL | 54 mg/mL | 2 mg/mL |
S1940 | Levofloxacin | 11 mg/mL | 24 mg/mL | 9 mg/mL |
S1393 | Pirarubicin | <1 mg/mL | 7 mg/mL | <1 mg/mL |
S1464 | Marbofloxacin | <1 mg/mL | 3 mg/mL | <1 mg/mL |
S2027 | Ciprofloxacin | <1 mg/mL | <1 mg/mL | <1 mg/mL |
S2492 | Novobiocin Sodium | 100 mg/mL | 100 mg/mL | 100 mg/mL |
S1756 | Enoxacin | <1 mg/mL | 32 mg/mL | <1 mg/mL |
S1463 | Ofloxacin | <1 mg/mL | 0.4 mg/mL | <1 mg/mL |
S1509 | Norfloxacin | <1 mg/mL | 3 mg/mL | <1 mg/mL |
S1327 | Ellagic acid | <1 mg/mL | 3 mg/mL | <1 mg/mL |
S2328 | Nalidixic acid | <1 mg/mL | 6 mg/mL | <1 mg/mL |
S7261 | Beta-Lapachone | <1 mg/mL | 33 mg/mL | '10 mg/mL |
S4006 | Clinafloxacin | <1 mg/mL | 0.03 mg/mL | <1 mg/mL |
S6747 | SW-044248 | <1 mg/mL | 14 mg/mL | <1 mg/mL |
S4119 | Pefloxacin Mesylate Dihydrate | 67 mg/mL | 9 mg/mL | <1 mg/mL |
S2064 | Balofloxacin | <1 mg/mL | 5 mg/mL | <1 mg/mL |
S2271 | Berberine chloride | <1 mg/mL | 40 mg/mL | <1 mg/mL |
S4604 | Levofloxacin hydrate | 5 mg/mL | 74 mg/mL | 10 mg/mL |
S2423 | (S)-10-Hydroxycamptothecin | <1 mg/mL | 8 mg/mL | <1 mg/mL |
S9321 | Topotecan | -1 mg/mL | 84 mg/mL | -1 mg/mL |
S7518 | Voreloxin (SNS-595) hydrochloride | 1 mg/mL | 1 mg/mL | '<1 mg/mL |
S5059 | Pixantrone Maleate | 100 mg/mL | 100 mg/mL | 1 mg/mL |
S3603 | Betulinic acid | <1 mg/mL | 20 mg/mL | 10 mg/mL |
S5111 | 7-Ethylcamptothecin | -1 mg/mL | 20 mg/mL | -1 mg/mL |
S3898 | Hydroxy Camptothecine | -1 mg/mL | 29 mg/mL | '-1 mg/mL |
S6631 | Belotecan (CKD-602) hydrochloride | 4 mg/mL | 47 mg/mL | <1 mg/mL |
S3181 | Flumequine | <1 mg/mL | 3 mg/mL | <1 mg/mL |
S9634 | Phenoxodiol (Haginin E) | <1 mg/mL | 48 mg/mL | 48 mg/mL |
S6790 | Ellipticine hydrochloride | ˂1 mg/mL | 3 mg/mL | ˂1 mg/mL |
Topoisomerase製品
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX) 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. |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1225 |
EtoposideEtoposide (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. |
![]() ![]() Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
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S1288 |
CamptothecinCamptothecin (NSC-100880, CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2. |
![]() ![]() Growth suppression by UBE2M silencing is enhanced by DNA damaging agents. Growth sensitivity of HEY cells in the presence of Camptothecin(CPT) was monitored using clonogenic assay.
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S1231 |
Topotecan HClTopotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis. |
![]() ![]() Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.
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S1198新 |
IrinotecanIrinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
![]() ![]() In vitro cell uptake data showing the HA coating on HAC-PFP-DC nanoparticles significantly improves drug delivery into prostasphere and mammosphere cells enriched with CSCs. Fluorescence micrographs of mammosphere cells after incubated with the simple mixture of free DOX&CPT, PFP-DC nanoparticles, and HAC-PFPDC nanoparticles for 3 h at 37℃. |
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S2653新 |
9-amino-CPT (9-Aminocamptothecin)9-amino-CPT (9-Aminocamptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin. |
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S0093新 |
Genz-644282Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research. |
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S2288新 |
RubitecanRubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity. |
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S1228 |
Idarubicin HClIdarubicin 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. |
![]() ![]() Sensitivity of AML cells to conventional induction treatment and small-molecule p53 activators. Cell viability in OCI-AML3 cells treated for 24 hours with cytarabin/idarubicin (CI) and Nultin-3A (Nut; A), CI and Leptomycin-B (LMB; B), or Nut and LMB (D), respectively. CI was tested at 0, 100, 200, and 300 nmol/L CI; Nutlin-3A at 0, 2.5, 5, 7.5; and LMB at 0, 2, 8, 32 ng/mL in dosages 0, 1, 2, and 3, respectively. Cell viability in normal and AML bone marrow cells. |
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S1223 |
Epirubicin HClEpirubicin HCl (4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis. |
![]() ![]()
Growth inhibitory effects of Epirubicin human pancreatic cancer cells. MiaPaCa-2 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (0.5% FBS) containing DMSO (control) or indicated doses of Epirubicin (Selleckchem). Cell viability 48 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells. |
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S2485 |
Mitoxantrone 2HClMitoxantrone 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. |
![]() ![]() Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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S3035 |
Daunorubicin HClDaunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
![]() ![]() A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. *p<0.05, **p<0.01, ***p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown). |
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S1465 |
Moxifloxacin HClMoxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent. |
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S2217 |
Irinotecan HCl TrihydrateIrinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1. |
![]() ![]() Growth inhibitory effects of Irinotecan in human pancreatic cancer cells. Panc1 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Irinotecan (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells. |
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S4908 |
SN-38SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy. |
![]() ![]() HCT116 cells were pretreated with tested compounds for 1 hour and then cotreated with 1 μM SN-38 for 2 hours. Cell lysates were then subjected to Western blot analysis. Data shown are representative of three independent experiments. Con, concentration. |
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S1367 |
AmonafideAmonafide (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. |
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S1787 |
TeniposideTeniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL). |
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S1340 |
GatifloxacinGatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. |
![]() ![]() Cleavable complex formation with nuclear DNA in P. falciparum treated with topoisomerase poisons. Parasites were metabolically labeled with [3H]hypoxanthine, treated with etoposide (■), gatifloxacin (●), levofloxacin(▲), ciprofloxacin (□), fleroxacin (○), or nalidixic acid (△) at the indicated concentrations for 18-22 h, lysed with SDS and digested with RNases. SDS and protein-bound DNA were precipitated with potassium. The fold increase in nuclear DNA capture as compared to solvent controls (mean of triplicate determinations) was plotted against concentration. Coefficient of variation for each data point was 19%. |
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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 |
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S1342 |
GenisteinGenistein, 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. |
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S1940 |
LevofloxacinLevofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections. |
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S1393 |
PirarubicinPirarubicin 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. |
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S1464 |
MarbofloxacinMarbofloxacin is a potent antibiotic inhibiting bacterial DNA replication. |
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S2027 |
CiprofloxacinCiprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM. |
![]() ![]() Ciprofoxacin (Cipro) reduces cancer cell survival in combination with chemotherapy. A and B, colony formation was conducted with A549 and SW48 cells treated with the clinically relevant chemotherapeutics cisplatin or 5-FU in the presence or absence of 2 μmol/L cipro floxacin. C, cipro fl oxacin at 2 μmol/L decreased proliferation of KG-1 cells and slightly enhanced the effect of etoposide (Etop). *, P < 0.05; **, P < 0.01 ( t tests). |
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S2492 |
Novobiocin SodiumNovobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria. |
![]() ![]() Cell viability and caspase 3/7 activity in MDA-MB-231 cells co-treated with carbenoxolone, novobiocin, ibrutinib and bisphosphonates. Cell viability (A) and caspase 3/7 activity (B) was determined after treatment with ZA (zoledronic acid), RIS (risedronate), IBN (ibandronate), ALN (alendronate) in combination with carbenoxolone, novobiocin and ibrutinib. All data are expressed as means of three different measure points of three independent experiments ± SEM and were normalized to BP treatment alone. Significances were calculated with the Mann Whitney U test (*p < 0.05; **p < 0.005). |
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S1756 |
EnoxacinEnoxacin (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. |
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S1463 |
OfloxacinOfloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent. |
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S1509 |
NorfloxacinNorfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes. |
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S1327 |
Ellagic acidEllagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property. |
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S2328 |
Nalidixic acidNalidixic 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. |
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S7261 |
Beta-LapachoneBeta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. |
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S4006 |
ClinafloxacinClinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. |
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S6747 |
SW-044248SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. |
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S4119 |
Pefloxacin Mesylate DihydratePefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication. |
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S5627 |
Amsacrine hydrochlorideAmsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity. |
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S2064 |
BalofloxacinBalofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase. |
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S2271 |
Berberine chlorideBerberine chloride 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 of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
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S4604 |
Levofloxacin hydrateLevofloxacin (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). |
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S2423 |
(S)-10-Hydroxycamptothecin(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity. |
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S9321 |
TopotecanTopotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. |
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S7518 |
Voreloxin (SNS-595) hydrochlorideVoreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2. |
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S5059 |
Pixantrone MaleatePixantrone (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. |
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S3603 |
Betulinic acidBetulinic acid (ALS-357), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB. Phase 1/2. |
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S5111 |
7-Ethylcamptothecin7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. |
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S3898 |
Hydroxy CamptothecineHydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. |
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S6631 |
Belotecan (CKD-602) hydrochlorideBelotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. |
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S3181 |
FlumequineFlumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
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S9634新 |
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. |
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S6790新 |
Ellipticine hydrochlorideEllipticine Hydrochloride 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. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
---|---|---|---|
S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin, NSC 123127, DOX) 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. |
![]() ![]() Cell viabilities with increasing concentrations of cisplatin (CP) and doxorubicin (DOXO) under normoxic and hypoxic condition for 48 hours were determined by MTT assay. IC50 values are presented as the means ?SDs (n=4) and * denotes p<0.05. |
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S1225 |
EtoposideEtoposide (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. |
![]() ![]() Cellular biomarker responses in HT29 cells exposed to various cytotoxic chemotherapeutic agents in combination with the Chk1 inhibitor V158411. HT29 cells were exposed to the combination GI80 of gemcitabine (0.2 uM), camptothecin (0.44 uM), cisplatin (68 uM), oxaliplatin (131 uM), doxorubicin (1.2 uM) or etoposide (59 uM) for 18 hours followed by DMSO (-) or 400 nM V158411 (+) for a further 24 hours. Protein expression was characterized by immunoblotting.
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S1288 |
CamptothecinCamptothecin (NSC-100880, CPT) is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Camptothecin induces apoptosis in cancer cells via microRNA-125b-mediated mitochondrial pathways. Phase 2. |
![]() ![]() Growth suppression by UBE2M silencing is enhanced by DNA damaging agents. Growth sensitivity of HEY cells in the presence of Camptothecin(CPT) was monitored using clonogenic assay.
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S1231 |
Topotecan HClTopotecan HCl (NSC609699, Nogitecan, SKFS 104864A) is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis. |
![]() ![]() Pax3:Foxo1a knockdown increases select chemotherapy sensitivities. MTS assay was performed for Pax3:Foxo1a knockdown mouse aRMS tumor cells treated with DNA damaging agents and microtubule inhibitors. Pax3:Foxo1a knockdown reduced the concentration at which viability was impaired by 50% (IC50) of topotecan by 4.8 fold, respectively, yet did not affect the IC50 of mafosfamide.
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S1198新 |
IrinotecanIrinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively. |
![]() ![]() In vitro cell uptake data showing the HA coating on HAC-PFP-DC nanoparticles significantly improves drug delivery into prostasphere and mammosphere cells enriched with CSCs. Fluorescence micrographs of mammosphere cells after incubated with the simple mixture of free DOX&CPT, PFP-DC nanoparticles, and HAC-PFPDC nanoparticles for 3 h at 37℃. |
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S2653新 |
9-amino-CPT (9-Aminocamptothecin)9-amino-CPT (9-Aminocamptothecin) is a Topoisomerase I inhibitor with potent anticancer activities. 9-amino-CPT (9-Aminocamptothecin) is an active, water-insoluble derivative of camptothecin. |
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S0093新 |
Genz-644282Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research. |
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S2288新 |
RubitecanRubitecan (9-NC, 9-Nitro-camptothecin, Partaject Orathecin, Partaject rubitecan, RFS 2000) is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral camptothecin with antitumour activity. |
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S1228 |
Idarubicin HClIdarubicin 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. |
![]() ![]() Sensitivity of AML cells to conventional induction treatment and small-molecule p53 activators. Cell viability in OCI-AML3 cells treated for 24 hours with cytarabin/idarubicin (CI) and Nultin-3A (Nut; A), CI and Leptomycin-B (LMB; B), or Nut and LMB (D), respectively. CI was tested at 0, 100, 200, and 300 nmol/L CI; Nutlin-3A at 0, 2.5, 5, 7.5; and LMB at 0, 2, 8, 32 ng/mL in dosages 0, 1, 2, and 3, respectively. Cell viability in normal and AML bone marrow cells. |
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S1223 |
Epirubicin HClEpirubicin HCl (4'-epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. Epirubicin induces apoptosis. |
![]() ![]()
Growth inhibitory effects of Epirubicin human pancreatic cancer cells. MiaPaCa-2 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (0.5% FBS) containing DMSO (control) or indicated doses of Epirubicin (Selleckchem). Cell viability 48 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells. |
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S2485 |
Mitoxantrone 2HClMitoxantrone 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. |
![]() ![]() Immunohistochemistry and quantification of cleaved caspase 3 expression in DU145-DR tumor xenografts from (D). Scale bar, 100 mm. Data represent the mean ± SD. *p < 0.05.
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S3035 |
Daunorubicin HClDaunorubicin HCl (Daunomycin) inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. Daunorubicin is a topoisomerase II inhibitor that induces apoptosis. |
![]() ![]() A) MV411 or B) Kasumi 1 cells were incubated with YM155 (0.25 x IC50) in the presence or absence of i) 0.5 x IC50 or ii) 1 x IC50 of Daunorubicin or iii) 0.5 x IC50 or iv) 1 x IC50 of Cytarabine for 72h. Following 72h treatment, cells were subject to a resazurin reduction assay. Percentages were normalised to DMSO controls. Column, mean of 3 independent experiments; Bars, SEM. *p<0.05, **p<0.01, ***p<0.005. Students t-test. Similar trends were observed with 0.5 x and 1 x IC50 of YM155 in combination with Daunorubicin or Cytarabine (data not shown). |
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S1465 |
Moxifloxacin HClMoxifloxacin (BAY12-8039) is a fourth-generation synthetic fluoroquinolone antibacterial agent. |
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S2217 |
Irinotecan HCl TrihydrateIrinotecan (CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1. |
![]() ![]() Growth inhibitory effects of Irinotecan in human pancreatic cancer cells. Panc1 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Irinotecan (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells. |
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S4908 |
SN-38SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks. SN-38 induces autophagy. |
![]() ![]() HCT116 cells were pretreated with tested compounds for 1 hour and then cotreated with 1 μM SN-38 for 2 hours. Cell lysates were then subjected to Western blot analysis. Data shown are representative of three independent experiments. Con, concentration. |
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S1367 |
AmonafideAmonafide (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. |
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S1787 |
TeniposideTeniposide (NSC 122819, VM-26) is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL). |
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S1340 |
GatifloxacinGatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. |
![]() ![]() Cleavable complex formation with nuclear DNA in P. falciparum treated with topoisomerase poisons. Parasites were metabolically labeled with [3H]hypoxanthine, treated with etoposide (■), gatifloxacin (●), levofloxacin(▲), ciprofloxacin (□), fleroxacin (○), or nalidixic acid (△) at the indicated concentrations for 18-22 h, lysed with SDS and digested with RNases. SDS and protein-bound DNA were precipitated with potassium. The fold increase in nuclear DNA capture as compared to solvent controls (mean of triplicate determinations) was plotted against concentration. Coefficient of variation for each data point was 19%. |
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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 |
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S1342 |
GenisteinGenistein, 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. |
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S1940 |
LevofloxacinLevofloxacin (Fluoroquinolone) is a broad-spectrum antibiotic topoisomerase II and topoisomerase IV inhibitor, used to treat respiratory, urinary tract, gastrointestinal, and abdominal infections. |
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S1393 |
PirarubicinPirarubicin 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. |
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S1464 |
MarbofloxacinMarbofloxacin is a potent antibiotic inhibiting bacterial DNA replication. |
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S2027 |
CiprofloxacinCiprofloxacin (Bay o 9867) is a fluoroquinolone antibiotic, shows broad and potent antibacterial activity, with MIC90 of 0.024-6 μM. |
![]() ![]() Ciprofoxacin (Cipro) reduces cancer cell survival in combination with chemotherapy. A and B, colony formation was conducted with A549 and SW48 cells treated with the clinically relevant chemotherapeutics cisplatin or 5-FU in the presence or absence of 2 μmol/L cipro floxacin. C, cipro fl oxacin at 2 μmol/L decreased proliferation of KG-1 cells and slightly enhanced the effect of etoposide (Etop). *, P < 0.05; **, P < 0.01 ( t tests). |
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S2492 |
Novobiocin SodiumNovobiocin Sodium is an aminocoumarin antibiotic that targets bacterial DNA gyrase (TopoIV), used to treat susceptible gram positive bacteria. |
![]() ![]() Cell viability and caspase 3/7 activity in MDA-MB-231 cells co-treated with carbenoxolone, novobiocin, ibrutinib and bisphosphonates. Cell viability (A) and caspase 3/7 activity (B) was determined after treatment with ZA (zoledronic acid), RIS (risedronate), IBN (ibandronate), ALN (alendronate) in combination with carbenoxolone, novobiocin and ibrutinib. All data are expressed as means of three different measure points of three independent experiments ± SEM and were normalized to BP treatment alone. Significances were calculated with the Mann Whitney U test (*p < 0.05; **p < 0.005). |
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S1756 |
EnoxacinEnoxacin (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. |
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S1463 |
OfloxacinOfloxacin (DL8280) is a synthetic broad-spectrum antimicrobial agent. |
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S1509 |
NorfloxacinNorfloxacin (MK-0366) is a broad-spectrum antibiotic. Norfloxacin (MK-0366) targets bacterial gyrase and topoisomerase IV enzymes. |
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S1327 |
Ellagic acidEllagic acid (Elagostasine, Gallogen) has antiproliferative and antioxidant property. |
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S2328 |
Nalidixic acidNalidixic 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. |
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S7261 |
Beta-LapachoneBeta-Lapachone (β-Lapachone, ARQ-501) is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. |
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S4006 |
ClinafloxacinClinafloxacin (CI-960, PD127391, AM-1091) is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. |
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S6747 |
SW-044248SW-044248 is a non-canonical Top1 inhibitor with a pattern of selective toxicity for NSCLC cells. |
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S4119 |
Pefloxacin Mesylate DihydratePefloxacin Mesylate Dihydrate (1589 RB) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication. |
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S5627 |
Amsacrine hydrochlorideAmsacrine hydrochloride (m-AMSA, acridinyl anisidide) is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity. |
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S2064 |
BalofloxacinBalofloxacin (Q-35) is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase. |
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S2271 |
Berberine chlorideBerberine chloride 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 of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator. |
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S4604 |
Levofloxacin hydrateLevofloxacin (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). |
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S2423 |
(S)-10-Hydroxycamptothecin(S)-10-Hydroxycamptothecin (10-HCPT) is a DNA topoisomerase I inhibitor with potent anti-tumor activity. |
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S9321 |
TopotecanTopotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases. |
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S7518 |
Voreloxin (SNS-595) hydrochlorideVoreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2. |
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S5059 |
Pixantrone MaleatePixantrone (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. |
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S3603 |
Betulinic acidBetulinic acid (ALS-357), a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid acts as a new activator of NF-kB. Phase 1/2. |
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S5111 |
7-Ethylcamptothecin7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition. |
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S3898 |
Hydroxy CamptothecineHydroxy Camptothecine (10-Hydroxycamptothecin, Hydroxycamptothecine) is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones. |
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S6631 |
Belotecan (CKD-602) hydrochlorideBelotecan (CKD-602) is a potent DNA topoisomerase I inhibitor that exerts a clinical anticancer effect on various types of tumor. |
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S3181 |
FlumequineFlumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S9634新 |
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. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S6790新 |
Ellipticine hydrochlorideEllipticine Hydrochloride 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. |