化学療法基盤支援活動及びユーザによる評価結果




アッセイの概要
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。
評価のクライテリア
toxicity: pGL-CONT 70%<control activity (solvent) non-specific: FOP 50%< control activity (solvent)
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


評価結果の詳細(評価のクライテリアに基づいて陽性と判断された化合物については背景色を黄色にしています.)
WellKIT 1KIT 2KIT 3
compound結果compound結果compound結果
1 - Anone (DMSO)  none (DMSO)  none (DMSO) 
1 - B5-FU  Pifithrin-a (cyclic)  ABT-702 
1 - CBestatin Hydrochloride  PRIMA-1  Akt Inhibitor IV 
1 - DBleomycin sulfate  Finasteride  Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 
1 - ECisplatin  Aminoglutethimide  Akt Inhibitor XI 
1 - FMethotrexate  Formestane  compound C 
1 - GMitomycin C  Mifepristone  ATM/ATR kinase inhibitor 
1 - HVinblastine sulfate  TOFA  ATM kinase inhibitor 
2 - APaclitaxelnon-specific  Amastatin  Aurora kinase/cdk inhibitor 
2 - BFlutamide  Actinonin  Aurora kinase inhibitor II 
2 - CDaunorubicin, HCltoxicity  Oligomycin  Aurora kinase inhibitor III 
2 - DDoxorubicin, HClnon-specific  Bafilomycin A1  AG957 
2 - ETamoxifen, citratenon-specific  HA 14-1  LFM-A13 
2 - FActinomycin Dnon-specific  BH3I-1toxicity  Terreic acid 
2 - GCamptothecin  LFM-A13  KN-93 
2 - HAclarubicin  Terreic acid  KN-62 
3 - AEtoposide (VP-16)toxicity  E-64d  Lavendustin C 
3 - BCytochalasin Dnon-specific  ALLN  Kenpaullone 
3 - C2',5'-dideoxyadenosine  CA-074  purvalanol A 
3 - DAKT inhibitor  Pepstatin A  Olomoucine 
3 - ENL-71-101  Z-GLF-CMK  Alsterpaullone, 2-cyanoethyl 
3 - FAG957  RS 102895  Cdk1/2 inhibitor III 
3 - GKN93  SB 328437  Cdk2/9 inhibitor 
3 - HZ-VAD-FMK  SB 225002  NU6102toxicity 
4 - AKenpaullonenon-specific  AMD3100 octahydrochloride  Cdk4 inhibitor 
4 - BPurvalanol Anon-specific  NSC95397  NSC625987non-specific 
4 - C3-ATA  SC-ααδ9  SB218078 
4 - DOlomoucine  Amiloride  isogranulatimide 
4 - ETBB  Lidocaine  Chk2 inhibitor 
4 - FSulindac sulfide  Monensin  Chk2 inhibitor II 
4 - GValeryl salicylate  Ouabaintoxicity  Ellagic acid (Dihydrate) 
4 - HNS-398  Sanguinarinetoxicity  TBB 
5 - ASodium salicylate toxicity  Glibenclamide  DMAT 
5 - BTheophylline  Dequaliniumtoxicity  D4476non-specific 
5 - CAzacytidine  Diazoxidetoxicity  TG003 
5 - DAphidicolin  Valinomycintoxicity  Diacylglycerol kinase inhibitor II 
5 - EAG1478  Nigericintoxicity  IC60211 
5 - FGenistein  Diltiazemtoxicity  TX-1918 
5 - GManumycin A  Nifedipinetoxicity  BPIQ-Ⅱ 
5 - HFTI-276  Verapamiltoxicity  AG1478 
6 - ASU1498  PGP-4008  AG490 
6 - BGGTI-286  Fumitremorgin Ctoxicity  SU4984 
6 - CDexamethasone  A23187toxicity  SU5402 
6 - DGSK-3 inhibitor II  Ionomycintoxicity  Flt-3 Inhibitor 
6 - EScriptaid  Thapsigargintoxicity  cFMS Receptor Tyrosine Kinase Inhibitor 
6 - FTrichostatin A  t-Butylhydroquinone (BHQ)  SU6656 
6 - GAG825  N-phenylanthranilic acidtoxicity  GSK-3 inhibitor IX 
6 - HCycloheximide  DIDStoxicity  1-Azakenpaullone 
7 - ALovastatin  SB 218078toxicity  Indirubin-3'-monoxime 
7 - BRadicicol  Debromohymenialdisine (DBH)toxicity  AG825non-specific 
7 - C17-AAG  Rotenonetoxicity  AG1024 
7 - DAG1024  Antimycin A1toxicity  AGL 2263 
7 - E1400W, HCl  Leptomycin B*  BMS-345541non-specific 
7 - FAMT, HCl  R59022  IKK-2 inhibitor VInon-specific 
7 - GAG490  Dioctanoylglycol  IRAK-1/4 inhibitornon-specific 
7 - HCucurbitacin Inon-specific  RHC80267toxicity  JAK Inhibitor I 
8 - ASP600125  Xanthohumol  JAK3 Inhibitor VI 
8 - BDamnacanthal  C75toxicity  SP600125 
8 - CPD 98059  Cerulenintoxicity  JNK inhibitor VIII 
8 - DU0126  Tunicamycin  Damnacanthal 
8 - EFumagillin  Deoxynojirimycin  PP2 
8 - FGM 6001  Swainsonine  ERK inhibitor II 
8 - GN-Acetyl-L-cysteine  LY 83583  PD98059 
8 - HAminoguanidine, HCl  ODQ  U-0126 
9 - AL-NMMAnon-specific  Anacardic acid  MEK inhibitor I 
9 - BPD169316toxicity  Chetomin  SU11274 
9 - CSB 203580non-specific  Dimethyloxalylglycine  ML-7 
9 - DRapamycin  HR22C16  SB202190 
9 - ENU1025  Monastrol  SB239063 
9 - FBenzamide  Nordihydroguaiaretic acid (NDGA)  AG1296 
9 - GD609  ETYA  SU11652 
9 - HIBMXnon-specific  Baicalein  PDGF receptor tyrosine kinase inhibitor V 
10 - ARo-20-1724  Nutlin-3toxicity  PDGF receptor tyrosine kinase inhibitor IV 
10 - BZaprinast  MDM2 inhibitor  LY-294002 
10 - CAG1296  Phenelzine  Wortmannin 
10 - DLY294002  Deprenyl  H-89 
10 - EWortmannin  Decylubiquinone  4-cyano-3-methylisoquinoline 
10 - FH-89, HCl  Ro 5-4864  Bisindolymaleimide I, HCl 
10 - GBisindolymaleimide I, HCl  Lonidamine  Go7874 
10 - HH-7non-specific  ML-7  Rp-8-CPT-cGMPS 
11 - AStaurosporine  Benzylguanine  KT5823 
11 - BcPLA2inhibitor  DFMO  PKR inhibitor 
11 - COBAA  KT 5823  RAF1 kinase inhibitor I 
11 - DCantharidin  Rp-8-CPT-cGMPS  ZM 336372 
11 - ECytostatin  MK 886  H-1152 
11 - FCyclosporin Anon-specific  Clofibrate  Y-27632 
11 - GFK-506non-specific  BADGE  radicicol 
11 - HMG-132non-specific  Troglitazone  PP1 analog 
12 - ALactacystin  AZT  Syk inhibitor 
12 - BHydroxyurea  Nalidixic acid  SB431542 
12 - CHA1077  a-Amanitin  TGF-b RI kinase inhibitor II 
12 - DY27632  MST-312  Tpl2 kinase inhibitornon-specific 
12 - EPP1 (analog)  b-Rubromycin  TrkA inhibitor 
12 - FPP-H  SB 431542  VEGFR receptor tyrosine kinase inhibitor II 
12 - GNocodazole  N1,N12-Diethylspermine (BESpm)  VEGF recptor 2 kinase inhibitor I 
12 - HDephostatin  Fumonisin B1  SU1498