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：　U017	報告日：　2011/03/02	所属：　三重大学医学部	アッセイ者名：　広川佳史	アッセイ名：　RhoB過剰発現細胞の運動能に与える影響
概要前立腺がんDU145細胞にRhoBを過剰発現させると細胞の運動能が亢進する。運動能亢進を抑制する阻害剤を同定し、RhoBとの関連を調べるのが目的。細胞をDilにて蛍光標識し、Boyden chamberの底部に阻害剤を入れる。一晩培養し、chamberの裏側に移動した細胞をプレートリーダーで測定する。GSK-3 inhibitorの３種、GSK-3 inhibitor IX ,1-Azakenpaullone, Indirubin-3'-monoxime-5-sulphonic Acidが細胞移動を抑制した。
評価のクライテリアプレートリーダーによる蛍光測定値が103以下
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．）

Well	KIT 1		KIT 2		KIT 3
Well	compound	結果	compound	結果	compound	結果
1 - A	none (DMSO)	150	none (DMSO)	177	none (DMSO)	151
1 - B	5-FU	141	Pifithrin-a (cyclic)	171	ABT-702	217
1 - C	Bestatin Hydrochloride	136	PRIMA-1	133	Akt Inhibitor IV	137
1 - D	Bleomycin sulfate	151	Finasteride	186	Akt Inhibitor VIII, Isozyme-Selective, Akti-1/2	140
1 - E	Cisplatin	156	Aminoglutethimide	172	Akt Inhibitor XI	194
1 - F	Methotrexate	167	Formestane	156	compound C	155
1 - G	Mitomycin C	132	Mifepristone	224	ATM/ATR kinase inhibitor	307
1 - H	Vinblastine sulfate	162	TOFA	185	ATM kinase inhibitor	167
2 - A	Paclitaxel	118	Amastatin	197	Aurora kinase/cdk inhibitor	108
2 - B	Flutamide	128	Actinonin	213	Aurora kinase inhibitor II	163
2 - C	Daunorubicin, HCl	165	Oligomycin	144	Aurora kinase inhibitor III	236
2 - D	Doxorubicin, HCl	158	Bafilomycin A1	107	AG957	269
2 - E	Tamoxifen, citrate	165	HA 14-1	219	LFM-A13	285
2 - F	Actinomycin D	134	BH3I-1	225	Terreic acid	293
2 - G	Camptothecin	159	LFM-A13	160	KN-93	203
2 - H	Aclarubicin	141	Terreic acid	191	KN-62	365
3 - A	Etoposide (VP-16)	152	E-64d	186	Lavendustin C	300
3 - B	Cytochalasin D	124	ALLN	149	Kenpaullone	140
3 - C	2',5'-dideoxyadenosine	128	CA-074	170	purvalanol A	129
3 - D	AKT inhibitor	161	Pepstatin A	136	Olomoucine	433
3 - E	NL-71-101	133	Z-GLF-CMK	135	Alsterpaullone, 2-cyanoethyl	239
3 - F	AG957	141	RS 102895	170	Cdk1/2 inhibitor III	201
3 - G	KN93	149	SB 328437	145	Cdk2/9 inhibitor	155
3 - H	Z-VAD-FMK	137	SB 225002	81	NU6102	145
4 - A	Kenpaullone	92	AMD3100 octahydrochloride	186	Cdk4 inhibitor	226
4 - B	Purvalanol A	113	NSC95397	203	NSC625987	271
4 - C	3-ATA	122	SC-ααδ9	148	SB218078	173
4 - D	Olomoucine	133	Amiloride	165	isogranulatimide	217
4 - E	TBB	137	Lidocaine	190	Chk2 inhibitor	146
4 - F	Sulindac sulfide	123	Monensin	108	Chk2 inhibitor II	150
4 - G	Valeryl salicylate	137	Ouabain	82	Ellagic acid　(Dihydrate)	243
4 - H	NS-398	127	Sanguinarine	66	TBB	239
5 - A	Sodium salicylate	143	Glibenclamide	169	DMAT	373
5 - B	Theophylline	127	Dequalinium	116	D4476	248
5 - C	Azacytidine	127	Diazoxide	147	TG003	234
5 - D	Aphidicolin	148	Valinomycin	93	Diacylglycerol kinase inhibitor II	239
5 - E	AG1478	152	Nigericin	131	IC60211	248
5 - F	Genistein	123	Diltiazem	236	TX-1918	277
5 - G	Manumycin A	161	Nifedipine	178	BPIQ-Ⅱ	194
5 - H	FTI-276	176	Verapamil	170	AG1478	224
6 - A	SU1498	150	PGP-4008	132	AG490	295
6 - B	GGTI-286	171	Fumitremorgin C	144	SU4984
6 - C	Dexamethasone	150	A23187	111	SU5402	211
6 - D	GSK-3 inhibitor II	164	Ionomycin	99	Flt-3 Inhibitor	193
6 - E	Scriptaid	145	Thapsigargin	87	cFMS Receptor Tyrosine Kinase Inhibitor	267
6 - F	Trichostatin A	143	t-Butylhydroquinone (BHQ)	138	SU6656	238
6 - G	AG825	177	N-phenylanthranilic acid	182	GSK-3 inhibitor IX	103
6 - H	Cycloheximide	153	DIDS	106	1-Azakenpaullone	105
7 - A	Lovastatin	201	SB 218078	169	Indirubin-3'-monoxime	46
7 - B	Radicicol	125	Debromohymenialdisine (DBH)	167	AG825	134
7 - C	17-AAG	114	Rotenone	119	AG1024	209
7 - D	AG1024	194	Antimycin A1	94	AGL 2263	155
7 - E	1400W, HCl	172	Leptomycin B*	162	BMS-345541	428
7 - F	AMT, HCl	166	R59022	166	IKK-2 inhibitor VI	123
7 - G	AG490	164	Dioctanoylglycol	151	IRAK-1/4 inhibitor	314
7 - H	Cucurbitacin I	155	RHC80267	130	JAK Inhibitor I	244
8 - A	SP600125	140	Xanthohumol	110	JAK3 Inhibitor VI	120
8 - B	Damnacanthal	152	C75	169	SP600125	223
8 - C	PD 98059	172	Cerulenin	122	JNK inhibitor VIII	269
8 - D	U0126	149	Tunicamycin	85	Damnacanthal	155
8 - E	Fumagillin	182	Deoxynojirimycin	188	PP2	119
8 - F	GM 6001	168	Swainsonine	185	ERK inhibitor II	235
8 - G	N-Acetyl-L-cysteine	181	LY 83583	113	PD98059	209
8 - H	Aminoguanidine, HCl	195	ODQ	229	U-0126	110
9 - A	L-NMMA	165	Anacardic acid	126	MEK inhibitor I	178
9 - B	PD169316	136	Chetomin	66	SU11274	130
9 - C	SB 203580	176	Dimethyloxalylglycine	192	ML-7	189
9 - D	Rapamycin	178	HR22C16	104	SB202190	87
9 - E	NU1025	185	Monastrol	150	SB239063	145
9 - F	Benzamide	168	Nordihydroguaiaretic acid (NDGA)	130	AG1296	132
9 - G	D609	164	ETYA	192	SU11652	90
9 - H	IBMX	165	Baicalein	147	PDGF receptor tyrosine kinase inhibitor V	97
10 - A	Ro-20-1724	159	Nutlin-3	179	PDGF receptor tyrosine kinase inhibitor IV	102
10 - B	Zaprinast	170	MDM2 inhibitor	179	LY-294002	162
10 - C	AG1296	170	Phenelzine	166	Wortmannin	78
10 - D	LY294002	168	Deprenyl	182	H-89	464
10 - E	Wortmannin	148	Decylubiquinone	189	4-cyano-3-methylisoquinoline	243
10 - F	H-89, HCl	160	Ro 5-4864	264	Bisindolymaleimide I, HCl	92
10 - G	Bisindolymaleimide I, HCl	128	Lonidamine	210	Go7874	134
10 - H	H-7	166	ML-7	137	Rp-8-CPT-cGMPS	376
11 - A	Staurosporine	135	Benzylguanine	211	KT5823	244
11 - B	cPLA2inhibitor	144	DFMO	203	PKR inhibitor	67
11 - C	OBAA	141	KT 5823	176	RAF1 kinase inhibitor I	244
11 - D	Cantharidin	169	Rp-8-CPT-cGMPS	269	ZM 336372	239
11 - E	Cytostatin	185	MK 886	184	H-1152	269
11 - F	Cyclosporin A	149	Clofibrate	230	Y-27632	303
11 - G	FK-506	155	BADGE	167	radicicol	95
11 - H	MG-132	157	Troglitazone	170	PP1 analog	167
12 - A	Lactacystin	144	AZT	337	Syk inhibitor	169
12 - B	Hydroxyurea	150	Nalidixic acid	174	SB431542	190
12 - C	HA1077	137	a-Amanitin	66	TGF-b RI kinase inhibitor II	267
12 - D	Y27632	143	MST-312	207	Tpl2 kinase inhibitor	203
12 - E	PP1 (analog)	165	b-Rubromycin	111	TrkA inhibitor	123
12 - F	PP-H	146	SB 431542	170	VEGFR receptor tyrosine kinase inhibitor II	167
12 - G	Nocodazole	143	N1,N12-Diethylspermine (BESpm)	126	VEGF recptor 2 kinase inhibitor I	254
12 - H	Dephostatin	155	Fumonisin B1	268	SU1498	193