トポイソメラーゼ
シグナル伝達経路
研究分野
- 阻害剤の選択性比較
- 溶解度
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 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 |
| S1228 | Idarubicin HCl | 5 mg/mL | 100 mg/mL | <1 mg/mL |
| S5059 | Pixantrone Maleate | 100 mg/mL | 100 mg/mL | 1 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 |
| 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, ADR-529) | 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 |
| S4119 | Pefloxacin Mesylate Dihydrate | 67 mg/mL | 9 mg/mL | <1 mg/mL |
| S2064 | Balofloxacin | <1 mg/mL | 5 mg/mL | <1 mg/mL |
| S4591 | Nitroxoline | <1 mg/mL | 38 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 |
| S7518 | Voreloxin (SNS-595) hydrochloride | 1 mg/mL | 1 mg/mL | <1 mg/mL |
| S3603 | Betulinic acid | <1 mg/mL | 20 mg/mL | 10 mg/mL |
| S3181 | Flumequine | <1 mg/mL | 3 mg/mL | <1 mg/mL |
- Topoisomerase阻害剤(39)
- 新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 |
|---|---|---|---|
| S1208 |
Doxorubicin (Adriamycin) HClDoxorubicin (Adriamycin) HCl is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells. |
Enhancement of apoptotic response by addition of targeted agents lapatinib and sunitinib to doxorubicin in the same device reservoir at 24 hours. P values were determined using Student’s t test for all graphs.
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| S1225 |
EtoposideEtoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity. |
ABT-199 synergizes strongly with lymphoma chemotherapy agents that affect MCL1 levels. Viability and CI vs Fa after 24-h exposure to etoposide alone or in combination with ABT-199 in Riva, U2932 and VavP-Bcl2/c-MYC murine tumor cells. Viability shown at 500 nM.
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| S1288 |
CamptothecinCamptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2. |
CtIP and exonuclease 1 protect cells from chromosomal damage. (A) At 72 h after transfection with the indicated siRNA oligonucleotides, U2OS cells were treated with either DMSO or camptothecin (1 h, 1 μM; acute treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of five independent experiments. (B) Cell survival at low doses of camptothecin from the data shown in (A). Data represent the mean±s.e.m. of five independent experiments. (C) Cells transfected as in (A) were treated with either DMSO or camptothecin for 24 h (chronic treatment) and survival was determined by colony formation. Data represent the mean±s.e.m. of three independent experiments. (D) Metaphase spreads from cells transfected and treated as described in (A) were analysed for chromosomal aberrations. A total of 50 metaphase spreads was analysed for each sample. The percentages of metaphase spreads displaying the indicated numbers of radial chromosomes are shown. CNTL, control; DMSO, dimethyl sulphoxide; EXO1, exonuclease 1; siRNA, small interfering RNA. |
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| S1231 |
Topotecan HClTopotecan HCl 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. |
Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.
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| S1228 |
Idarubicin HClIdarubicin HCl 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. |
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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| S5059新 |
Pixantrone MaleatePixantrone 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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| S5111新 |
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新 |
Hydroxy Camptothecine10-Hydroxycamptothecin 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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| S1223 |
Epirubicin HClEpirubicin HCl, a semisynthetic L-arabino derivative of doxorubicin, is an antineoplastic agent by inhibiting Topoisomerase. |
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 is a type II topoisomerase inhibitor with IC50 of 2.0 μM, 0.42 mM for HepG2 and MCF-7/wt cells, respectively. |
C18SH: C18NH2 mixed monolayer. Panel A: Cyclic voltammograms of MTX at various scan rates (1) 9 mV/s, (2) 36 mV/s, (3) 64 mV/s, (4) 100 mV/s. Panel B: Bode plots (circles) with fit (solid line) and corresponding electrical equivalent circuit (inset); 1×10-5 M MTX(Mitoxantrone) in aqueous 0.1 M LiClO4, pH = 5.6, E = 0.4 V.
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| S3035 |
Daunorubicin HClDaunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay. |
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 is a fourth-generation synthetic fluoroquinolone antibacterial agent. |
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| S2217 |
Irinotecan HCl TrihydrateIrinotecan 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. |
(B) HCT116 cells were treated with increasing doses of SN-38 and treated with 4 nM SN-38 for different time. Cell extracts were prepared and analyzed by Western blotting with indicated antibody. These experiments were repeated thrice. (C) HCT116 cells were transfected with 2 μg of EGFP-LC3 construct. At 8 h post-transfection, cells were treated with 4 nM of SN-38 for 48 h. And then cells were examined by confocal microscopy (magnification × 400). The percentage of cells showing accumulation of EGFP-LC3 in puncta (EGFP-LC3vac) was quantified. (D) LOVO and HCT116 cells were treated with 2 nM and 4 nM of SN-38 combined with 10 mM of 3-Methyladenine (3-MA) for 48 h respectively. Cell extracts were prepared and analyzed by Western blotting with indicated antibody. These experiments were repeated thrice. (E) Cells were treated with indicated concentrations of 3-MA and SN-38 for 48 h. Cell apoptosis was assessed by Annexin V-FITC/PI staining assay by flow cytometry. Columns, means of three determinations; bars, SD. (F) and (G) LOVO and HCT116 cells were transfected with 50 nM of NC siRNA, ATG5 siRNA respectively, and then were treated with increasing doses of SN-38 for 48 h, the knockdown effects on ATG5 were confirmed by Western blot analysis (upper panel). Cell viability was measured using CCK8 assay. Columns, means of three determinations; bars, SD.
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| S1367 |
AmonafideAmonafide 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 is a chemotherapeutic medication mainly used in the treatment of childhood acute lymphocytic leukemia (ALL). |
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| S1340 |
GatifloxacinGatifloxacin 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, ADR-529)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 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 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 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 is a synthetic broad-spectrum antimicrobial agent. |
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| S1509 |
NorfloxacinNorfloxacin is a broad-spectrum antibiotic. |
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| S1327 |
Ellagic acidEllagic acid has antiproliferative and antioxidant property. |
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| S2328 |
Nalidixic acidNalidixic acid 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 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 is a fluoroquinolone that inhibits both DNA gyrase and topoisomerase IV dually in Streptococcus pneumoniae. |
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| S4119 |
Pefloxacin Mesylate DihydratePefloxacin Mesylate Dihydrate is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication. |
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| S2064 |
BalofloxacinBalofloxacin is a quinolone antibiotic, inhibiting the synthesis of bacterial DNA by interference with the enqyme DNA gyrase. |
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| S4591 |
NitroxolineNitroxoline is a urinary antibacterial agent active against susceptible gram-positive and gram-negative organisms commonly found in urinary tract infections. It is a fluorquinolone that is active against bacterial gyrases. |
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| S4604 |
Levofloxacin hydrateLevofloxacin 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-Hydroxycamptothecin10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor with potent anti-tumor activity. |
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| S7518 |
Voreloxin (SNS-595) hydrochlorideVoreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2. |
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| S3603 |
Betulinic acidBetulinic acid, a pentacyclic triterpenoid from Syzigium claviflorum, is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Phase 1/2. |
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| S3181 |
FlumequineFlumequine is a synthetic chemotherapeutic antibiotic, inhibiting topoisomerase II with IC50 of 15 μM. |
-10-Hydroxycamptothecin-J-Pharmacol-Exp-Ther-20161110.gif)
