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: B401報告日: -所属: 化学療法基盤支援活動アッセイ者名: 掛谷秀昭アッセイ名: 低酸素誘導因子(HIF)阻害活性の評価
概要
固形腫瘍内などの低酸素環境下に曝されている細胞の生存には、Hypoxia-inducible factor(HIF)が重要な役割を果たしている。そこで、HIFをターゲットとした分子標的治療には大きな期待が寄せられている。本測定系ではHIF-1/HIF-2のDNA結合配列(HRE; hypoxia response element)をルシフェラーゼ遺伝子の上流に挿入したプラスミドをレポーターとして用いたCell-based assayにより、提供化合物のHIFシグナル系に対する阻害効果を評価する。
評価のクライテリア
10 μMで50%以上の阻害活性が認められたものを有効とする.
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: -


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)Negative  none (DMSO)Negative  none (DMSO)Negative 
1 - B5-FUNegative  Pifithrin-a (cyclic)Positive  ABT-702Positive 
1 - CBestatin HydrochlorideNegative  PRIMA-1Negative  Akt Inhibitor IVPositive 
1 - DBleomycin sulfateNegative  FinasterideNegative  Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2Negative 
1 - ECisplatinNegative  AminoglutethimideNegative  Akt Inhibitor XINegative 
1 - FMethotrexatePositive  FormestaneNegative  compound CPositive 
1 - GMitomycin CPositive  MifepristoneNegative  ATM/ATR kinase inhibitorNegative 
1 - HVinblastine sulfatePositive  TOFANegative  ATM kinase inhibitorPositive 
2 - APaclitaxelNegative  AmastatinNegative  Aurora kinase/cdk inhibitorPositive 
2 - BFlutamideNegative  ActinoninNegative  Aurora kinase inhibitor IINegative 
2 - CDaunorubicin, HClPositive  OligomycinNegative  Aurora kinase inhibitor IIINegative 
2 - DDoxorubicin, HClPositive  Bafilomycin A1Negative  AG957Negative 
2 - ETamoxifen, citrateNegative  HA 14-1Negative  LFM-A13Negative 
2 - FActinomycin DPositive  BH3I-1Negative  Terreic acidNegative 
2 - GCamptothecinPositive  LFM-A13Negative  KN-93Negative 
2 - HAclarubicinNegative  Terreic acidNegative  KN-62Negative 
3 - AEtoposide (VP-16)Positive  E-64dNegative  Lavendustin CNegative 
3 - BCytochalasin DNegative  ALLNNegative  KenpaulloneNegative 
3 - C2',5'-dideoxyadenosineNegative  CA-074Negative  purvalanol ANegative 
3 - DAKT inhibitorNegative  Pepstatin ANegative  OlomoucineNegative 
3 - ENL-71-101Negative  Z-GLF-CMKPositive  Alsterpaullone, 2-cyanoethylPositive 
3 - FAG957Negative  RS 102895Negative  Cdk1/2 inhibitor IIIPositive 
3 - GKN93Negative  SB 328437Negative  Cdk2/9 inhibitorPositive 
3 - HZ-VAD-FMKNegative  SB 225002Negative  NU6102Positive 
4 - AKenpaulloneNegative  AMD3100 octahydrochlorideNegative  Cdk4 inhibitorNegative 
4 - BPurvalanol ANegative  NSC95397Negative  NSC625987Negative 
4 - C3-ATANegative  SC-ααδ9Positive  SB218078Negative 
4 - DOlomoucineNegative  AmilorideNegative  isogranulatimideNegative 
4 - ETBBNegative  LidocaineNegative  Chk2 inhibitorPositive 
4 - FSulindac sulfideNegative  MonensinNegative  Chk2 inhibitor IINegative 
4 - GValeryl salicylateNegative  OuabainPositive  Ellagic acid (Dihydrate)Negative 
4 - HNS-398Negative  SanguinarineNegative  TBBNegative 
5 - ASodium salicylate Negative  GlibenclamideNegative  DMATNegative 
5 - BTheophyllineNegative  DequaliniumPositive  D4476Negative 
5 - CAzacytidineNegative  DiazoxideNegative  TG003Negative 
5 - DAphidicolinNegative  ValinomycinNegative  Diacylglycerol kinase inhibitor IINegative 
5 - EAG1478Negative  NigericinNegative  IC60211Negative 
5 - FGenisteinNegative  DiltiazemNegative  TX-1918Negative 
5 - GManumycin ANegative  NifedipineNegative  BPIQ-ⅡNegative 
5 - HFTI-276Negative  VerapamilNegative  AG1478Positive 
6 - ASU1498Negative  PGP-4008Negative  AG490Negative 
6 - BGGTI-286Negative  Fumitremorgin CNegative  SU4984Negative 
6 - CDexamethasoneNegative  A23187Negative  SU5402Negative 
6 - DGSK-3 inhibitor IINegative  IonomycinNegative  Flt-3 InhibitorNegative 
6 - EScriptaidNegative  ThapsigarginNegative  cFMS Receptor Tyrosine Kinase InhibitorNegative 
6 - FTrichostatin ANegative  t-Butylhydroquinone (BHQ)Negative  SU6656Negative 
6 - GAG825Negative  N-phenylanthranilic acidNegative  GSK-3 inhibitor IXPositive 
6 - HCycloheximidePositive  DIDSNegative  1-AzakenpaulloneNegative 
7 - ALovastatinNegative  SB 218078Negative  Indirubin-3'-monoximeNegative 
7 - BRadicicolPositive  Debromohymenialdisine (DBH)Negative  AG825Negative 
7 - C17-AAGPositive  RotenoneNegative  AG1024Negative 
7 - DAG1024Negative  Antimycin A1Negative  AGL 2263Negative 
7 - E1400W, HClNegative  Leptomycin B*Negative  BMS-345541Negative 
7 - FAMT, HClNegative  R59022Negative  IKK-2 inhibitor VIPositive 
7 - GAG490Negative  DioctanoylglycolNegative  IRAK-1/4 inhibitorPositive 
7 - HCucurbitacin IPositive  RHC80267Negative  JAK Inhibitor IPositive 
8 - ASP600125Negative  XanthohumolNegative  JAK3 Inhibitor VIPositive 
8 - BDamnacanthalNegative  C75Negative  SP600125Negative 
8 - CPD 98059Negative  CeruleninNegative  JNK inhibitor VIIINegative 
8 - DU0126Negative  TunicamycinNegative  DamnacanthalNegative 
8 - EFumagillinNegative  DeoxynojirimycinNegative  PP2Positive 
8 - FGM 6001Negative  SwainsonineNegative  ERK inhibitor IINegative 
8 - GN-Acetyl-L-cysteineNegative  LY 83583Negative  PD98059Negative 
8 - HAminoguanidine, HClNegative  ODQNegative  U-0126Negative 
9 - AL-NMMANegative  Anacardic acidNegative  MEK inhibitor INegative 
9 - BPD169316Negative  ChetominNegative  SU11274Positive 
9 - CSB 203580Negative  DimethyloxalylglycineNegative  ML-7Negative 
9 - DRapamycinNegative  HR22C16Negative  SB202190Negative 
9 - ENU1025Negative  MonastrolNegative  SB239063Positive 
9 - FBenzamideNegative  Nordihydroguaiaretic acid (NDGA)Negative  AG1296Negative 
9 - GD609Negative  ETYANegative  SU11652Negative 
9 - HIBMXNegative  BaicaleinNegative  PDGF receptor tyrosine kinase inhibitor VPositive 
10 - ARo-20-1724Negative  Nutlin-3Negative  PDGF receptor tyrosine kinase inhibitor IVPositive 
10 - BZaprinastNegative  MDM2 inhibitorNegative  LY-294002Negative 
10 - CAG1296Negative  PhenelzineNegative  WortmanninNegative 
10 - DLY294002Negative  DeprenylNegative  H-89Negative 
10 - EWortmanninNegative  DecylubiquinoneNegative  4-cyano-3-methylisoquinolineNegative 
10 - FH-89, HClNegative  Ro 5-4864Negative  Bisindolymaleimide I, HClNegative 
10 - GBisindolymaleimide I, HClNegative  LonidamineNegative  Go7874Positive 
10 - HH-7Negative  ML-7Negative  Rp-8-CPT-cGMPSNegative 
11 - AStaurosporinePositive  BenzylguanineNegative  KT5823Negative 
11 - BcPLA2inhibitorNegative  DFMONegative  PKR inhibitorPositive 
11 - COBAANegative  KT 5823Negative  RAF1 kinase inhibitor INegative 
11 - DCantharidinNegative  Rp-8-CPT-cGMPSNegative  ZM 336372Negative 
11 - ECytostatinNegative  MK 886Negative  H-1152Negative 
11 - FCyclosporin ANegative  ClofibrateNegative  Y-27632Negative 
11 - GFK-506Negative  BADGENegative  radicicolPositive 
11 - HMG-132Positive  TroglitazoneNegative  PP1 analogPositive 
12 - ALactacystinPositive  AZTNegative  Syk inhibitorPositive 
12 - BHydroxyureaNegative  Nalidixic acidNegative  SB431542Negative 
12 - CHA1077Negative  a-AmanitinPositive  TGF-b RI kinase inhibitor IIPositive 
12 - DY27632Negative  MST-312Negative  Tpl2 kinase inhibitorPositive 
12 - EPP1 (analog)Positive  b-RubromycinNegative  TrkA inhibitorNegative 
12 - FPP-HNegative  SB 431542Positive  VEGFR receptor tyrosine kinase inhibitor IINegative 
12 - GNocodazoleNegative  N1,N12-Diethylspermine (BESpm)Negative  VEGF recptor 2 kinase inhibitor INegative 
12 - HDephostatinNegative  Fumonisin B1Negative  SU1498Negative