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(+)-JQ1

(+)-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.

(+)-JQ1化学構造

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
JPY 40500 国内在庫あり
JPY 70500 国内在庫あり
JPY 145500 国内在庫あり
JPY 295500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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(+)-JQ1関連製品

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 (+)-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.
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

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

In vitro
Batch:

DMSO : 91 mg/mL ( (199.12 mM)； Warmed with 50℃ water bath; 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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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）

mg/kg g μL 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

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Handling Instructions

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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.

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