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(+)-JQ1

(+)-JQ1是一種BET bromodomain抑制劑，作用于BRD4(1/2)，無(wú)細(xì)胞試驗(yàn)中IC50為77 nM/33 nM，結(jié)合到BET家族的所有溴結(jié)構(gòu)域，而不結(jié)合到BET家族以外的溴結(jié)構(gòu)域。(+)-JQ1可通過誘導(dǎo)自噬來抑制細(xì)胞增殖。(+)-JQ1 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表達(dá)。

(+)-JQ1 Chemical Structure

(+)-JQ1 Chemical Structure

CAS: 1268524-70-4

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
10mg 1040.13 現(xiàn)貨
25mg 1941.03 現(xiàn)貨
100mg 4823.91 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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(+)-JQ1相關(guān)產(chǎn)品

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
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

產(chǎn)品描述 (+)-JQ1是一種BET bromodomain抑制劑，作用于BRD4(1/2)，無(wú)細(xì)胞試驗(yàn)中IC50為77 nM/33 nM，結(jié)合到BET家族的所有溴結(jié)構(gòu)域，而不結(jié)合到BET家族以外的溴結(jié)構(gòu)域。(+)-JQ1可通過誘導(dǎo)自噬來抑制細(xì)胞增殖。(+)-JQ1 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表達(dá)。
特性 (+)-JQ1比(-)-JQ1更有效。
靶點(diǎn)
BRD4 (2) [1]
(Cell-free assay)		 BRD4 (1) [1]
(Cell-free assay)
33 nM 77 nM
體外研究(In Vitro)
體外研究活性 (+)-JQ1對(duì)映體直接結(jié)合到BET bromodomain結(jié)構(gòu)域的Kac結(jié)合位點(diǎn)。(+)-JQ1(500 nM)與染色質(zhì)競(jìng)爭(zhēng)性結(jié)合到BRD4，導(dǎo)致NMC細(xì)胞分化和生長(zhǎng)停滯。通過Ki67染色減少，證明了(+)-JQ1(500 nM)減弱NMC 797和Per403細(xì)胞系的快速增殖。(+)-JQ1(500 nM)作用于NMC 797細(xì)胞，有效降低BRD4靶基因的表達(dá)。(+)-JQ1作用于NMC 11060細(xì)胞，抑制細(xì)胞活力， IC50為4 nM。[1](+)-JQ1作用于MM細(xì)胞系，強(qiáng)抑制MYC表達(dá)。(+)-JQ1抑制KMS-34和LR5增殖，IC50分別為 68 nM和98 nM。(+)-JQ1(500 nM)處理MM.1S細(xì)胞，導(dǎo)致S期細(xì)胞比例明顯下降，隨之細(xì)胞停滯在G0/G1期增多。(+)-JQ1(500 nM)通過β-半乳糖苷酶染色，導(dǎo)致明顯的細(xì)胞衰老。(+)-JQ1(800 nM)處理CD138+病患衍生的MM樣本，顯著降低細(xì)胞活力。[2] (+)-JQ1抑制LP-1細(xì)胞生長(zhǎng)，GI50 為98 nM。(+)-JQ1(625 nM)導(dǎo)致LP-1細(xì)胞在G0/G1期的百分?jǐn)?shù)增高。(+)-JQ1(500 nM)作用于LP-1細(xì)胞，抑制MYC, BRD4 和CDK9表達(dá)。[3](+)-JQ1(1 μM)處理潛伏感染的Jurkat T細(xì)胞，激活HIV轉(zhuǎn)錄。(+)-JQ1(50 μM)作用于Jurkat和HeLa細(xì)胞，主要刺激Tat依賴性的HIV轉(zhuǎn)錄。(+)-JQ1(5 μM)作用于J-Lat A2細(xì)胞，誘導(dǎo)Brd4解離，從而使Tat招募SEC到HIV啟動(dòng)子上，誘導(dǎo)Pol II CTD磷酸化和病毒轉(zhuǎn)錄。[4]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MC 11060細(xì)胞
濃度 ~500 nM
孵育時(shí)間 48小時(shí)
方法

細(xì)胞按每孔500個(gè)接種在白色, 384孔微孔板，孔中含總體為50 μL的培養(yǎng)基。797, TT和TE10細(xì)胞生長(zhǎng)在含1% Penicillin/Streptomycin 和 10% FBS的DMEM培養(yǎng)基上。Per403細(xì)胞生長(zhǎng)在含1 % Penicillin/Streptomycin和20% FBS的DMEM 培養(yǎng)基上。病患衍生的NMC 11060細(xì)胞生長(zhǎng)在含10% FBS 和1% Penicillin/Streptomycin的RPMI培養(yǎng)基上。通過自動(dòng)化針轉(zhuǎn)移機(jī)將(+)-JQ1置于微量檢測(cè)板上。使細(xì)胞裂解，通過增殖試驗(yàn)測(cè)評(píng)孔中的總ATP含量。根據(jù)劑量，重復(fù)測(cè)量分析，通過邏輯回歸（GraphPad Prism）計(jì)算IC50。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 (+)-JQ1(50 mg/kg)處理攜帶NMC 797移植瘤的小鼠，抑制腫瘤生長(zhǎng)。(+)-JQ1(50 mg/kg) 抹消掉攜帶NMC 797移植瘤的小鼠的NUT核斑點(diǎn), 與競(jìng)爭(zhēng)性結(jié)合到核染色質(zhì)相一致。(+)-JQ1(50 mg/kg)處理NMC 797移植瘤， 顯著誘導(dǎo)（31級(jí)）角蛋白表達(dá)。(+)-JQ1(50 mg/kg)處理攜帶NMC移植瘤的小鼠模型，促進(jìn)分化，腫瘤衰退，延長(zhǎng)壽命。[1](+)-JQ1(50 mg/kg)處理靜脈注射MM.1S-luc+細(xì)胞，攜帶原位移植瘤的SCID米色小鼠，與對(duì)照組動(dòng)物相比，顯著延長(zhǎng)小鼠的總生存期。[2](+)-JQ1(50 mg/kg，腹腔注射)處理攜帶Raji移植瘤的小鼠，顯著提高小鼠壽命。[3]
動(dòng)物實(shí)驗(yàn) Animal Models 攜帶NMC 797移植瘤的小鼠
Dosages 50 mg/kg
Administration 腹腔注射

化學(xué)信息&溶解度

分子量 456.99 分子式

C23H25ClN4O2S
CAS號(hào) 1268524-70-4 SDF Download (+)-JQ1 SDF
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 91 mg/mL ( (199.12 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 91 mg/mL (199.12 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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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