アッセイID: U065 | 報告日: 2010/07/23 | 所属: 東京大学医科学研究所 | アッセイ者名: 古川 洋一 | アッセイ名: Tcf4活性阻害剤スクリーニング |
概要 大腸癌や肝癌においては、APCやβ-catenin、Axin1などの遺伝子異常により、転写因子TCF4の転写活性化が認められている。しかもこの活性化が大腸癌細胞の増殖およびstemnessの維持に重要である。そこでキナーゼインヒビターを含む既知の阻害薬が、TCF4転写活性を制御するかどうかを検討した。TCF4結合配列を持つTOP-Flash ルシフェラーゼレポータープラスミドまたはそのコントロールプラスミドを大腸癌細胞株などに導入し、レポーターアッセイを行った。この実験結果を通じて、既知の阻害薬の新しい作用の発見や、新しいWNTシグナル経路を調節するシグナルの発見など、有益な情報が得られるものと思われる。 |
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評価のクライテリア toxicity: pGL-CONT 70%<control activity (solvent) non-specific: FOP 50%< control activity (solvent) |
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発表論文 | レポート提出者によるレポート内容の最終確認日: 2013/11/15 |
Well | KIT 1 | KIT 2 | KIT 3 | |||
compound | 結果 | compound | 結果 | compound | 結果 | |
1 - A | none (DMSO) | none (DMSO) | none (DMSO) | |||
1 - B | 5-FU | Pifithrin-a (cyclic) | ABT-702 | |||
1 - C | Bestatin Hydrochloride | PRIMA-1 | Akt Inhibitor IV | |||
1 - D | Bleomycin sulfate | Finasteride | Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 | |||
1 - E | Cisplatin | Aminoglutethimide | Akt Inhibitor XI | |||
1 - F | Methotrexate | Formestane | compound C | |||
1 - G | Mitomycin C | Mifepristone | ATM/ATR kinase inhibitor | |||
1 - H | Vinblastine sulfate | TOFA | ATM kinase inhibitor | |||
2 - A | Paclitaxel | non-specific | Amastatin | Aurora kinase/cdk inhibitor | ||
2 - B | Flutamide | Actinonin | Aurora kinase inhibitor II | |||
2 - C | Daunorubicin, HCl | toxicity | Oligomycin | Aurora kinase inhibitor III | ||
2 - D | Doxorubicin, HCl | non-specific | Bafilomycin A1 | AG957 | ||
2 - E | Tamoxifen, citrate | non-specific | HA 14-1 | LFM-A13 | ||
2 - F | Actinomycin D | non-specific | BH3I-1 | toxicity | Terreic acid | |
2 - G | Camptothecin | LFM-A13 | KN-93 | |||
2 - H | Aclarubicin | Terreic acid | KN-62 | |||
3 - A | Etoposide (VP-16) | toxicity | E-64d | Lavendustin C | ||
3 - B | Cytochalasin D | non-specific | ALLN | Kenpaullone | ||
3 - C | 2',5'-dideoxyadenosine | CA-074 | purvalanol A | |||
3 - D | AKT inhibitor | Pepstatin A | Olomoucine | |||
3 - E | NL-71-101 | Z-GLF-CMK | Alsterpaullone, 2-cyanoethyl | |||
3 - F | AG957 | RS 102895 | Cdk1/2 inhibitor III | |||
3 - G | KN93 | SB 328437 | Cdk2/9 inhibitor | |||
3 - H | Z-VAD-FMK | SB 225002 | NU6102 | toxicity | ||
4 - A | Kenpaullone | non-specific | AMD3100 octahydrochloride | Cdk4 inhibitor | ||
4 - B | Purvalanol A | non-specific | NSC95397 | NSC625987 | non-specific | |
4 - C | 3-ATA | SC-ααδ9 | SB218078 | |||
4 - D | Olomoucine | Amiloride | isogranulatimide | |||
4 - E | TBB | Lidocaine | Chk2 inhibitor | |||
4 - F | Sulindac sulfide | Monensin | Chk2 inhibitor II | |||
4 - G | Valeryl salicylate | Ouabain | toxicity | Ellagic acid (Dihydrate) | ||
4 - H | NS-398 | Sanguinarine | toxicity | TBB | ||
5 - A | Sodium salicylate | toxicity | Glibenclamide | DMAT | ||
5 - B | Theophylline | Dequalinium | toxicity | D4476 | non-specific | |
5 - C | Azacytidine | Diazoxide | toxicity | TG003 | ||
5 - D | Aphidicolin | Valinomycin | toxicity | Diacylglycerol kinase inhibitor II | ||
5 - E | AG1478 | Nigericin | toxicity | IC60211 | ||
5 - F | Genistein | Diltiazem | toxicity | TX-1918 | ||
5 - G | Manumycin A | Nifedipine | toxicity | BPIQ-Ⅱ | ||
5 - H | FTI-276 | Verapamil | toxicity | AG1478 | ||
6 - A | SU1498 | PGP-4008 | AG490 | |||
6 - B | GGTI-286 | Fumitremorgin C | toxicity | SU4984 | ||
6 - C | Dexamethasone | A23187 | toxicity | SU5402 | ||
6 - D | GSK-3 inhibitor II | Ionomycin | toxicity | Flt-3 Inhibitor | ||
6 - E | Scriptaid | Thapsigargin | toxicity | cFMS Receptor Tyrosine Kinase Inhibitor | ||
6 - F | Trichostatin A | t-Butylhydroquinone (BHQ) | SU6656 | |||
6 - G | AG825 | N-phenylanthranilic acid | toxicity | GSK-3 inhibitor IX | ||
6 - H | Cycloheximide | DIDS | toxicity | 1-Azakenpaullone | ||
7 - A | Lovastatin | SB 218078 | toxicity | Indirubin-3'-monoxime | ||
7 - B | Radicicol | Debromohymenialdisine (DBH) | toxicity | AG825 | non-specific | |
7 - C | 17-AAG | Rotenone | toxicity | AG1024 | ||
7 - D | AG1024 | Antimycin A1 | toxicity | AGL 2263 | ||
7 - E | 1400W, HCl | Leptomycin B* | BMS-345541 | non-specific | ||
7 - F | AMT, HCl | R59022 | IKK-2 inhibitor VI | non-specific | ||
7 - G | AG490 | Dioctanoylglycol | IRAK-1/4 inhibitor | non-specific | ||
7 - H | Cucurbitacin I | non-specific | RHC80267 | toxicity | JAK Inhibitor I | |
8 - A | SP600125 | Xanthohumol | JAK3 Inhibitor VI | |||
8 - B | Damnacanthal | C75 | toxicity | SP600125 | ||
8 - C | PD 98059 | Cerulenin | toxicity | JNK inhibitor VIII | ||
8 - D | U0126 | Tunicamycin | Damnacanthal | |||
8 - E | Fumagillin | Deoxynojirimycin | PP2 | |||
8 - F | GM 6001 | Swainsonine | ERK inhibitor II | |||
8 - G | N-Acetyl-L-cysteine | LY 83583 | PD98059 | |||
8 - H | Aminoguanidine, HCl | ODQ | U-0126 | |||
9 - A | L-NMMA | non-specific | Anacardic acid | MEK inhibitor I | ||
9 - B | PD169316 | toxicity | Chetomin | SU11274 | ||
9 - C | SB 203580 | non-specific | Dimethyloxalylglycine | ML-7 | ||
9 - D | Rapamycin | HR22C16 | SB202190 | |||
9 - E | NU1025 | Monastrol | SB239063 | |||
9 - F | Benzamide | Nordihydroguaiaretic acid (NDGA) | AG1296 | |||
9 - G | D609 | ETYA | SU11652 | |||
9 - H | IBMX | non-specific | Baicalein | PDGF receptor tyrosine kinase inhibitor V | ||
10 - A | Ro-20-1724 | Nutlin-3 | toxicity | PDGF receptor tyrosine kinase inhibitor IV | ||
10 - B | Zaprinast | MDM2 inhibitor | LY-294002 | |||
10 - C | AG1296 | Phenelzine | Wortmannin | |||
10 - D | LY294002 | Deprenyl | H-89 | |||
10 - E | Wortmannin | Decylubiquinone | 4-cyano-3-methylisoquinoline | |||
10 - F | H-89, HCl | Ro 5-4864 | Bisindolymaleimide I, HCl | |||
10 - G | Bisindolymaleimide I, HCl | Lonidamine | Go7874 | |||
10 - H | H-7 | non-specific | ML-7 | Rp-8-CPT-cGMPS | ||
11 - A | Staurosporine | Benzylguanine | KT5823 | |||
11 - B | cPLA2inhibitor | DFMO | PKR inhibitor | |||
11 - C | OBAA | KT 5823 | RAF1 kinase inhibitor I | |||
11 - D | Cantharidin | Rp-8-CPT-cGMPS | ZM 336372 | |||
11 - E | Cytostatin | MK 886 | H-1152 | |||
11 - F | Cyclosporin A | non-specific | Clofibrate | Y-27632 | ||
11 - G | FK-506 | non-specific | BADGE | radicicol | ||
11 - H | MG-132 | non-specific | Troglitazone | PP1 analog | ||
12 - A | Lactacystin | AZT | Syk inhibitor | |||
12 - B | Hydroxyurea | Nalidixic acid | SB431542 | |||
12 - C | HA1077 | a-Amanitin | TGF-b RI kinase inhibitor II | |||
12 - D | Y27632 | MST-312 | Tpl2 kinase inhibitor | non-specific | ||
12 - E | PP1 (analog) | b-Rubromycin | TrkA inhibitor | |||
12 - F | PP-H | SB 431542 | VEGFR receptor tyrosine kinase inhibitor II | |||
12 - G | Nocodazole | N1,N12-Diethylspermine (BESpm) | VEGF recptor 2 kinase inhibitor I | |||
12 - H | Dephostatin | Fumonisin B1 | SU1498 |