(+)-JQ1

製品コード：S7110 純度：99.99%

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

CAS No. 1268524-70-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 43000	国内在庫あり
10mg	JPY 40500	国内在庫あり
25mg	JPY 70500	国内在庫あり
100mg	JPY 145500	国内在庫なし(納期7~10日)
1g	JPY 295500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（393）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

(+)-JQ1関連製品

関連製品	Quizartinib (AC220)	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

Target Protein Ligand阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
ROSA KIT D816V	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
ROSA KIT WT	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HMC-1.2	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HMC-1.1	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
ROSA KIT D816V	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
ROSA KIT WT	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.2	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.1	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
SK-N-DZ	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
SK-N-SH	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
BE(2)-M17	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
JF	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
IMR-32	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
BE(2)-C	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
DDR2L63V	Cell Viability Assay	0-1 μM	5 d	decreases cell viability in a dose-dependent manner	26206333
858	Cell Viability Assay	0-1 μM	5 d	decreases cell viability in a dose-dependent manner	26206333
HEK293	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
MCF-7	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
A549	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
Omm1.3	Cell Cycle Assay	500 nM	24/48/72 h	induces the cell accumulation at sub-G1	26397223
92.1	Cell Cycle Assay	500 nM	24/48/72 h	induces the cell accumulation at sub-G1	26397223
Omm1.3	Apoptosis Assay	500 nM	48 h	induces apoptosis	26397223
92.1	Apoptosis Assay	500 nM	48 h	induces apoptosis	26397223
Omm1	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel270	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel202	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Omm1.3	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
92.1	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel290	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel285	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
C8161	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
H1299	Function Assay	1/2.5/5 μM	12 h	decreased DR4 expression	26415225
H157	Function Assay	1/2.5/5 μM	12 h	decreased DR4 expression	26415225
H1299	Function Assay	1/2.5/5 μM	12 h	weakly decreased Bcl-2 levels	26415225
A549	Function Assay	1/2.5/5 μM	12 h	weakly decreased Bcl-2 levels	26415225
H1299	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
H157	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
A549	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
HCCLM3	Apoptosis Assay	0.1/0.5/2.5 μM	48 h	activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria	26575167
Hep3B	Apoptosis Assay	0.1/0.5/2.5 μM	48 h	activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria	26575167
HCCLM3	Cell Cycle Assay	0.1/0.5/2.5 μM	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
Hep3B	Cell Cycle Assay	0.1/0.5/2.5 μM	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
MHCC97H	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.41 μM	26575167
BEL7402	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.47 μM	26575167
SMMC7721	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.41 μM	26575167
HepG2	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.34 μM	26575167
HuH7	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.21 μM	26575167
HCCLM3	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.14 μM	26575167
Hep3B	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.08 μM	26575167
BCPAP	Cell Cycle Assay	250/500/1000 nM	72 h	arrests cell cycle at G0/G1 phase	26707881
K1	Cell Cycle Assay	250/500/1000 nM	72 h	arrests cell cycle at G0/G1 phase	26707881
BCPAP	Cell Viability Assay	250/500/1000 nM	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
K1	Cell Viability Assay	250/500/1000 nM	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
494H	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
148I	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
OS17	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
494H	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
148I	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
OS17	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
MOLM13	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MV4-11	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MOLM13	Function Assay	250 nM	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MV4-11	Function Assay	250 nM	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MOLM13	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
MV4-11	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
Hela	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
HBL-1	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
HLY-1	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly10	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-4	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-5	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-6	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-10	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
RC-K8	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly8	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCL-Ly18	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly8	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-4	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-10	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly3	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
OCI-Ly8	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-4	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-10	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
494L	Growth Inhibition Assay		72 h	IC50=0.317±0.012 μM	25944566
89R	Growth Inhibition Assay		72 h	IC50=0.126±0.003 μM	25944566
98Sc	Growth Inhibition Assay		72 h	IC50=0.115±0.004 μM	25944566
148I	Growth Inhibition Assay		72 h	IC50=0.284±0.035 μM	25944566
716H	Growth Inhibition Assay		72 h	IC50=0.212±0.034 μM	25944566
493H	Growth Inhibition Assay		72 h	IC50=0.047±0.009 μM	25944566
494H	Growth Inhibition Assay		72 h	IC50=0.122±0.004 μM	25944566
493L	Growth Inhibition Assay		72 h	IC50=0.050±0.011 μM	25944566
148L	Growth Inhibition Assay		72 h	IC50=0.146±0.017 μM	25944566
98L	Growth Inhibition Assay		72 h	IC50=0.309±0.029 μM	25944566
OS17	Growth Inhibition Assay		72 h	IC50=0.079±0.003 μM	25944566
OS9	Growth Inhibition Assay		72 h	IC50=0.406±0.028 μM	25944566
MG63	Growth Inhibition Assay		72 h	IC50=0.114±0.025 μM	25944566
SAOS2	Growth Inhibition Assay		72 h	IC50=0.217±0.003 μM	25944566
U2OS	Growth Inhibition Assay		72 h	IC50=0.198±0.008 μM	25944566
SJSA-1	Growth Inhibition Assay		72 h	IC50=0.100±0.010 μM	25944566
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0066 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0076 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0089 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0107 μM	26080064
MV4-11	Antiproliferative activity assay		72 h	IC50 = 0.012 μM	26731490
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.012 μM	29758518
VCaP	Antiproliferative activity assay		12 h	IC50 = 0.012 μM	28463487
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0125 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0132 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0149 μM	28463487
TY82	Antiproliferative activity assay		72 h	IC50 = 0.018 μM	28586718
MM1S	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	28586718
MM1S	Cytotoxicity assay		72 h	IC50 = 0.02 μM	29758518
HT-29	Antiproliferative activity assay		12 h	IC50 = 0.02 μM	28535045
MV4-11	Growth inhibition assay		72 h	IC50 = 0.023 μM	25559428
MV4-11	Cytotoxicity assay		4 days	IC50 = 0.024 μM	28463487
MV4-11	Growth inhibition assay		4 days	IC50 = 0.024 μM	26080064
Rosetta2 DE3	Function assay		30 mins	IC50 = 0.0287 μM	26080064
NALM16	Cytotoxicity assay		5 days	EC50 = 0.03 μM	29170024
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.033 μM	28195723
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0357 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0422 μM	28463487
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0467 μM	28463487
MOLM13	Cytotoxicity assay		4 days	IC50 = 0.056 μM	28463487
MOLM13	Growth inhibition assay		4 days	IC50 = 0.056 μM	26080064
HL60	Antiproliferative activity assay		72 h	IC50 = 0.06 μM	29170024
HL60	Growth inhibition assay		3 days	GC50 = 0.06 μM	29657099
NALM6	Cytotoxicity assay		5 days	EC50 = 0.06 μM	28549889
Raji	Function assay		4 h	IC50 = 0.069 μM	24900758
MM1S	Antiproliferative activity assay		72 h	IC50 = 0.0691 μM	29525435
BL21 (DE3)-codon plus-RIL	Fluorescence polarization assay		by fluorescence anisotropy assay	IC50 = 0.07 μM	28586718
22Rv1	Antiproliferative activity assay		96 h	IC50 = 0.071 μM	29758518
22Rv1	Antiproliferative activity assay		12 h	IC50 = 0.071 μM	29541371
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	26731490
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	28195723
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	29776834
MV4-11	Cytotoxicity assay		24 h	GI50 = 0.08 μM	26191363
MV411	Antiproliferative activity assay		72 h	IC50 = 0.08 μM	28314513
TY82	Antiproliferative activity assay		72 h	IC50 = 0.0808 μM	29525435
HL60	Function assay		24 h	IC50 = 0.086 μM	28549889
697	Cytotoxicity assay		5 days	EC50 = 0.09 μM	29170024
Loucy	Cytotoxicity assay		5 days	EC50 = 0.09 μM	29170024
HT-29	Growth inhibition assay		72 h	IC50 = 0.104 μM	25559428
MM1S	Growth inhibition assay		72 h	IC50 = 0.109 μM	25559428
T cells	Function assay		24 h	IC50 = 0.11 μM	28314513
HL60	Antiproliferative activity assay		72 h	IC50 = 0.11 μM	26869194
BL21(DE3)	Function assay		2.5 h	IC50 = 0.12 μM	29541371
H1299	Function assay		24 h	EC50 = 0.153 μM	28949521
HD-MB03	Cytotoxicity assay		5 days	EC50 = 0.16 μM	29758518
LNCAP	Antiproliferative activity assay		96 h	IC50 = 0.16 μM	29758518
Hs578T	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29758518
MV4-11	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29170024
LNCAP	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29541371
C4-2B	Antiproliferative activity assay		96 h	IC50 = 0.19 μM	29758518
C4-2B	Antiproliferative activity assay		12 h	IC50 = 0.19 μM	29541371
Vero E6	Antiviral activity assay		48 h	IC50 = 0.19275 μM	32353859
MCF7	Antiproliferative activity assay		12 h	IC50 = 0.2 μM	29758518
MV4-11	Cytotoxicity assay		72 h	IC50 = 0.242 μM	23517011
MX1	Antiproliferative activity assay		72 h	EC50 = 0.254 μM	28949521
HT-29	Antiproliferative activity assay		72 h	IC50 = 0.28 μM	26731490
HFL1	Antiproliferative activity assay		12 h	IC50 = 0.29 μM	29758518
MDA-MB-231	Growth inhibition assay		3 days	GC50 = 0.3 μM	28549889
MV4-11	Antiproliferative activity assay		48 h	EC50 = 0.33113 μM	28595007
HL60	Antiproliferative activity assay		48 h	EC50 = 0.74131 μM	28595007
NCI-H1975	Antiproliferative activity assay		12 h	IC50 = 1.23 μM	29758518
SAE	Function assay		4 h	IC50 = 1.38 μM	29649741
SAE	Function assay		4 h	IC50 = 1.49 μM	29649741
SAE	Function assay		4 h	IC50 = 1.51 μM	29649741
U2OS	Antiproliferative activity assay		12 h	IC50 = 1.62 μM	29758518
SAE	Function assay		4 h	IC50 = 1.63 μM	29649741
A549	Antiproliferative activity assay		12 h	IC50 = 1.67 μM	29758518
MCF7	Growth inhibition assay		3 days	GC50 = 1.7 μM	28549889
DU145	Antiproliferative activity assay		96 h	IC50 = 2.52 μM	29758518
DU145	Antiproliferative activity assay		12 h	IC50 = 2.52 μM	29541371
T47D	Growth inhibition assay		3 days	GC50 = 2.8 μM	28549889
PC3	Antiproliferative activity assay		96 h	IC50 = 3.01 μM	29758518
PC3	Antiproliferative activity assay		12 h	IC50 = 3.01 μM	29541371
HeLa	Antiproliferative activity assay		12 h	IC50 = 3.76 μM	29758518
K562	Growth inhibition assay		3 days	GC50 = 3.8 μM	28549889
A2780	Growth inhibition assay		3 days	GC50 = 4 μM	28549889
HL60	Cytotoxicity assay		24 h	IC50 = 5.3 μM	27266999
MV4-11	Cytotoxicity assay		24 h	IC50 = 6.4 μM	27266999
K562	Antiproliferative activity assay		72 h	IC50 = 9.12 μM	28314513
OVCAR5	Growth inhibition assay		3 days	GC50 = 12 μM	28549889
Rosetta2 DE3	Function assay			Kd = 0.0062 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0067 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0117 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0128 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0136 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0147 μM	26080064
BL21(DE3)	Function assay			Kd = 0.034 μM	26731490
Raji	Function assay			IC50 = 0.06 μM	26731490
MV4-11	Antiproliferative activity assay			IC50 = 0.072 μM	28195723
BL21(DE3)	Function assay			Kd = 0.092 μM	29541371
BL21(DE3)-R3-pRARE2	Function assay			Kd = 0.1 μM	28595007
LNCAP cells	Antiproliferative activity assay			IC50 = 0.1096 μM	29758518
BL21(DE3)	Function assay			IC50 = 0.12 μM	26731490
MV4-11	Antiproliferative activity assay			IC50 = 0.24 μM	27142751
K562	Antiproliferative activity assay			IC50 = 0.64 μM	27142751
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生物活性

製品説明

特性

(+)-JQ1 is more effective than (-)-JQ1.

Targets

BRD4 (2) ^[1] (Cell-free assay)	BRD4 (1) ^[1] (Cell-free assay)
33 nM	77 nM

In Vitro
In vitro	(+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. ^[1] (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. ^[2] (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. ^[3] (+)-JQ1 (1 μM) activates HIV transcription in latently infected Jurkat T cells. (+)-JQ1 (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. (+)-JQ1 (5 μM) induces Brd4 dissociation enables Tat to recruit SEC to HIV promoter and induce Pol II CTD phosphorylation and viral transcription in J-Lat A2 cells. JQ1 enables Tat to increase CDK9 T-loop phosphorylation and partially dissociates P-TEFb from 7SK snRNP in Jurkat T cells. ^[4]
細胞実験	細胞株	MC 11060 cells
	濃度	~500 nM
	反応時間	48 hours
	実験の流れ	Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism).
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	pDNA-PKcs / γH2AX / Ub-γH2AX / p-c-Jun S63 / Bax c-Myc p27		26119999
	Growth inhibition assay	Cell viability		23792448
	Immunofluorescence	GM130 MHC / EdU		29074567

In Vivo
In Vivo	(+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. ^[1] (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. ^[2] (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. ^[3]
動物実験	動物モデル	Mice bearing NMC 797 xenografts
	投与量	50 mg/kg
	投与経路	intraperitoneal injection

参考
[1] Filippakopoulos P, et al. Nature, 2010, 468(7327), 1067-1073. [2] Delmore JE, et al. Cell, 2011, 146(6), 904-917. [3] Mertz JA, et al. Proc Natl Acad Sci U S A, 2011, 108(40), 16669-16674. [4] Li Z, et al. Nucleic Acids Res, 2013, 41(1), 277-287. + 展開

参考

[4] Li Z, et al. Nucleic Acids Res, 2013, 41(1), 277-287.

+ 展開

化学情報

分子量	456.99	化学式	C₂₃H₂₅ClN₄O₂S
CAS No.	1268524-70-4	SDF	Download (+)-JQ1 SDFをダウンロードする
Smiles	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 91 mg/mL ( (199.12 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 91 mg/mL

Water : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 95% Corn oil	0.625mg/ml (1.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/mL clarified DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml (10.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2% DMSO 1 30% PEG 300 2 5%Tween80 3 63%ddH2O	3.34mg/ml (7.31mM)	Taking the 1 mL working solution as an example, add 20 μL of 167 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 630 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

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よくある質問（FAQ）

質問1:
How can I reconstitute the compound for in vivo injection?

回答
JQ1 does not dissolve in water/PBS. The vehicle we recommend is 2% DMSO+30% PEG 300+5% Tween 80+ddH2O. The compound can be dissolved in the vehicle at 5mg/ml and you can use it for IV injection.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):