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。 |
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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. |
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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: - |
Well | KIT 1 | KIT 2 | KIT 3 | |||
compound | 結果 | compound | 結果 | compound | 結果 | |
1 - A | none (DMSO) | Negative | none (DMSO) | Negative | none (DMSO) | Negative |
1 - B | 5-FU | Negative | Pifithrin-a (cyclic) | Positive | ABT-702 | Positive |
1 - C | Bestatin Hydrochloride | Negative | PRIMA-1 | Negative | Akt Inhibitor IV | Positive |
1 - D | Bleomycin sulfate | Negative | Finasteride | Negative | Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2 | Negative |
1 - E | Cisplatin | Negative | Aminoglutethimide | Negative | Akt Inhibitor XI | Negative |
1 - F | Methotrexate | Positive | Formestane | Negative | compound C | Positive |
1 - G | Mitomycin C | Positive | Mifepristone | Negative | ATM/ATR kinase inhibitor | Negative |
1 - H | Vinblastine sulfate | Positive | TOFA | Negative | ATM kinase inhibitor | Positive |
2 - A | Paclitaxel | Negative | Amastatin | Negative | Aurora kinase/cdk inhibitor | Positive |
2 - B | Flutamide | Negative | Actinonin | Negative | Aurora kinase inhibitor II | Negative |
2 - C | Daunorubicin, HCl | Positive | Oligomycin | Negative | Aurora kinase inhibitor III | Negative |
2 - D | Doxorubicin, HCl | Positive | Bafilomycin A1 | Negative | AG957 | Negative |
2 - E | Tamoxifen, citrate | Negative | HA 14-1 | Negative | LFM-A13 | Negative |
2 - F | Actinomycin D | Positive | BH3I-1 | Negative | Terreic acid | Negative |
2 - G | Camptothecin | Positive | LFM-A13 | Negative | KN-93 | Negative |
2 - H | Aclarubicin | Negative | Terreic acid | Negative | KN-62 | Negative |
3 - A | Etoposide (VP-16) | Positive | E-64d | Negative | Lavendustin C | Negative |
3 - B | Cytochalasin D | Negative | ALLN | Negative | Kenpaullone | Negative |
3 - C | 2',5'-dideoxyadenosine | Negative | CA-074 | Negative | purvalanol A | Negative |
3 - D | AKT inhibitor | Negative | Pepstatin A | Negative | Olomoucine | Negative |
3 - E | NL-71-101 | Negative | Z-GLF-CMK | Positive | Alsterpaullone, 2-cyanoethyl | Positive |
3 - F | AG957 | Negative | RS 102895 | Negative | Cdk1/2 inhibitor III | Positive |
3 - G | KN93 | Negative | SB 328437 | Negative | Cdk2/9 inhibitor | Positive |
3 - H | Z-VAD-FMK | Negative | SB 225002 | Negative | NU6102 | Positive |
4 - A | Kenpaullone | Negative | AMD3100 octahydrochloride | Negative | Cdk4 inhibitor | Negative |
4 - B | Purvalanol A | Negative | NSC95397 | Negative | NSC625987 | Negative |
4 - C | 3-ATA | Negative | SC-ααδ9 | Positive | SB218078 | Negative |
4 - D | Olomoucine | Negative | Amiloride | Negative | isogranulatimide | Negative |
4 - E | TBB | Negative | Lidocaine | Negative | Chk2 inhibitor | Positive |
4 - F | Sulindac sulfide | Negative | Monensin | Negative | Chk2 inhibitor II | Negative |
4 - G | Valeryl salicylate | Negative | Ouabain | Positive | Ellagic acid (Dihydrate) | Negative |
4 - H | NS-398 | Negative | Sanguinarine | Negative | TBB | Negative |
5 - A | Sodium salicylate | Negative | Glibenclamide | Negative | DMAT | Negative |
5 - B | Theophylline | Negative | Dequalinium | Positive | D4476 | Negative |
5 - C | Azacytidine | Negative | Diazoxide | Negative | TG003 | Negative |
5 - D | Aphidicolin | Negative | Valinomycin | Negative | Diacylglycerol kinase inhibitor II | Negative |
5 - E | AG1478 | Negative | Nigericin | Negative | IC60211 | Negative |
5 - F | Genistein | Negative | Diltiazem | Negative | TX-1918 | Negative |
5 - G | Manumycin A | Negative | Nifedipine | Negative | BPIQ-Ⅱ | Negative |
5 - H | FTI-276 | Negative | Verapamil | Negative | AG1478 | Positive |
6 - A | SU1498 | Negative | PGP-4008 | Negative | AG490 | Negative |
6 - B | GGTI-286 | Negative | Fumitremorgin C | Negative | SU4984 | Negative |
6 - C | Dexamethasone | Negative | A23187 | Negative | SU5402 | Negative |
6 - D | GSK-3 inhibitor II | Negative | Ionomycin | Negative | Flt-3 Inhibitor | Negative |
6 - E | Scriptaid | Negative | Thapsigargin | Negative | cFMS Receptor Tyrosine Kinase Inhibitor | Negative |
6 - F | Trichostatin A | Negative | t-Butylhydroquinone (BHQ) | Negative | SU6656 | Negative |
6 - G | AG825 | Negative | N-phenylanthranilic acid | Negative | GSK-3 inhibitor IX | Positive |
6 - H | Cycloheximide | Positive | DIDS | Negative | 1-Azakenpaullone | Negative |
7 - A | Lovastatin | Negative | SB 218078 | Negative | Indirubin-3'-monoxime | Negative |
7 - B | Radicicol | Positive | Debromohymenialdisine (DBH) | Negative | AG825 | Negative |
7 - C | 17-AAG | Positive | Rotenone | Negative | AG1024 | Negative |
7 - D | AG1024 | Negative | Antimycin A1 | Negative | AGL 2263 | Negative |
7 - E | 1400W, HCl | Negative | Leptomycin B* | Negative | BMS-345541 | Negative |
7 - F | AMT, HCl | Negative | R59022 | Negative | IKK-2 inhibitor VI | Positive |
7 - G | AG490 | Negative | Dioctanoylglycol | Negative | IRAK-1/4 inhibitor | Positive |
7 - H | Cucurbitacin I | Positive | RHC80267 | Negative | JAK Inhibitor I | Positive |
8 - A | SP600125 | Negative | Xanthohumol | Negative | JAK3 Inhibitor VI | Positive |
8 - B | Damnacanthal | Negative | C75 | Negative | SP600125 | Negative |
8 - C | PD 98059 | Negative | Cerulenin | Negative | JNK inhibitor VIII | Negative |
8 - D | U0126 | Negative | Tunicamycin | Negative | Damnacanthal | Negative |
8 - E | Fumagillin | Negative | Deoxynojirimycin | Negative | PP2 | Positive |
8 - F | GM 6001 | Negative | Swainsonine | Negative | ERK inhibitor II | Negative |
8 - G | N-Acetyl-L-cysteine | Negative | LY 83583 | Negative | PD98059 | Negative |
8 - H | Aminoguanidine, HCl | Negative | ODQ | Negative | U-0126 | Negative |
9 - A | L-NMMA | Negative | Anacardic acid | Negative | MEK inhibitor I | Negative |
9 - B | PD169316 | Negative | Chetomin | Negative | SU11274 | Positive |
9 - C | SB 203580 | Negative | Dimethyloxalylglycine | Negative | ML-7 | Negative |
9 - D | Rapamycin | Negative | HR22C16 | Negative | SB202190 | Negative |
9 - E | NU1025 | Negative | Monastrol | Negative | SB239063 | Positive |
9 - F | Benzamide | Negative | Nordihydroguaiaretic acid (NDGA) | Negative | AG1296 | Negative |
9 - G | D609 | Negative | ETYA | Negative | SU11652 | Negative |
9 - H | IBMX | Negative | Baicalein | Negative | PDGF receptor tyrosine kinase inhibitor V | Positive |
10 - A | Ro-20-1724 | Negative | Nutlin-3 | Negative | PDGF receptor tyrosine kinase inhibitor IV | Positive |
10 - B | Zaprinast | Negative | MDM2 inhibitor | Negative | LY-294002 | Negative |
10 - C | AG1296 | Negative | Phenelzine | Negative | Wortmannin | Negative |
10 - D | LY294002 | Negative | Deprenyl | Negative | H-89 | Negative |
10 - E | Wortmannin | Negative | Decylubiquinone | Negative | 4-cyano-3-methylisoquinoline | Negative |
10 - F | H-89, HCl | Negative | Ro 5-4864 | Negative | Bisindolymaleimide I, HCl | Negative |
10 - G | Bisindolymaleimide I, HCl | Negative | Lonidamine | Negative | Go7874 | Positive |
10 - H | H-7 | Negative | ML-7 | Negative | Rp-8-CPT-cGMPS | Negative |
11 - A | Staurosporine | Positive | Benzylguanine | Negative | KT5823 | Negative |
11 - B | cPLA2inhibitor | Negative | DFMO | Negative | PKR inhibitor | Positive |
11 - C | OBAA | Negative | KT 5823 | Negative | RAF1 kinase inhibitor I | Negative |
11 - D | Cantharidin | Negative | Rp-8-CPT-cGMPS | Negative | ZM 336372 | Negative |
11 - E | Cytostatin | Negative | MK 886 | Negative | H-1152 | Negative |
11 - F | Cyclosporin A | Negative | Clofibrate | Negative | Y-27632 | Negative |
11 - G | FK-506 | Negative | BADGE | Negative | radicicol | Positive |
11 - H | MG-132 | Positive | Troglitazone | Negative | PP1 analog | Positive |
12 - A | Lactacystin | Positive | AZT | Negative | Syk inhibitor | Positive |
12 - B | Hydroxyurea | Negative | Nalidixic acid | Negative | SB431542 | Negative |
12 - C | HA1077 | Negative | a-Amanitin | Positive | TGF-b RI kinase inhibitor II | Positive |
12 - D | Y27632 | Negative | MST-312 | Negative | Tpl2 kinase inhibitor | Positive |
12 - E | PP1 (analog) | Positive | b-Rubromycin | Negative | TrkA inhibitor | Negative |
12 - F | PP-H | Negative | SB 431542 | Positive | VEGFR receptor tyrosine kinase inhibitor II | Negative |
12 - G | Nocodazole | Negative | N1,N12-Diethylspermine (BESpm) | Negative | VEGF recptor 2 kinase inhibitor I | Negative |
12 - H | Dephostatin | Negative | Fumonisin B1 | Negative | SU1498 | Negative |