(+)-JQ1

(+)-JQ1是一种BET bromodomain抑制剂,作用于BRD4(1/2),无细胞试验中IC50为77 nM/33 nM,结合到BET家族的所有溴结构域,而不结合到BET家族以外的溴结构域。(+)-JQ1可通过诱导自噬来抑制细胞增殖。(+)-JQ1 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表达。

(+)-JQ1 Chemical Structure

(+)-JQ1 Chemical Structure

CAS: 1268524-70-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
10mg RMB 1040.13 现货
25mg RMB 1941.03 现货
100mg RMB 4823.91 现货
1g RMB 7944.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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客户使用Selleck的(+)-JQ1发表文献383

产品质控

批次: 纯度: 99.99%
99.99

(+)-JQ1相关产品

Target Protein Ligand抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
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
点击查看更多细胞系数据

生物活性

产品描述 (+)-JQ1是一种BET bromodomain抑制剂,作用于BRD4(1/2),无细胞试验中IC50为77 nM/33 nM,结合到BET家族的所有溴结构域,而不结合到BET家族以外的溴结构域。(+)-JQ1可通过诱导自噬来抑制细胞增殖。(+)-JQ1 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表达。
特性 (+)-JQ1比(-)-JQ1更有效。
靶点
BRD4 (2) [1]
(Cell-free assay)
BRD4 (1) [1]
(Cell-free assay)
33 nM 77 nM
体外研究(In Vitro)
体外研究活性 (+)-JQ1对映体直接结合到BET bromodomain结构域的Kac结合位点。(+)-JQ1(500 nM)与染色质竞争性结合到BRD4,导致NMC细胞分化和生长停滞。通过Ki67染色减少,证明了(+)-JQ1(500 nM)减弱NMC 797和Per403细胞系的快速增殖。(+)-JQ1(500 nM)作用于NMC 797细胞,有效降低BRD4靶基因的表达。(+)-JQ1作用于NMC 11060细胞,抑制细胞活力, IC50为4 nM。[1](+)-JQ1作用于MM细胞系,强抑制MYC表达。(+)-JQ1抑制KMS-34和LR5增殖,IC50分别为 68 nM和98 nM。(+)-JQ1(500 nM)处理MM.1S细胞,导致S期细胞比例明显下降,随之细胞停滞在G0/G1期增多。(+)-JQ1(500 nM)通过β-半乳糖苷酶染色,导致明显的细胞衰老。(+)-JQ1(800 nM)处理CD138+病患衍生的MM样本,显著降低细胞活力。[2] (+)-JQ1抑制LP-1细胞生长,GI50 为98 nM。(+)-JQ1(625 nM)导致LP-1细胞在G0/G1期的百分数增高。(+)-JQ1(500 nM)作用于LP-1细胞,抑制MYC, BRD4 和CDK9表达。[3](+)-JQ1(1 μM)处理潜伏感染的Jurkat T细胞,激活HIV转录。(+)-JQ1(50 μM)作用于Jurkat和HeLa细胞,主要刺激Tat依赖性的HIV转录。(+)-JQ1(5 μM)作用于J-Lat A2细胞,诱导Brd4解离,从而使Tat招募SEC到HIV启动子上,诱导Pol II CTD磷酸化和病毒转录。[4]
细胞实验 细胞系 MC 11060细胞
浓度 ~500 nM
孵育时间 48小时
方法

细胞按每孔500个接种在白色, 384孔微孔板,孔中含总体为50 μL的培养基。797, TT和TE10细胞生长在含1% Penicillin/Streptomycin 和 10% FBS的DMEM培养基上。Per403细胞生长在含1 % Penicillin/Streptomycin和20% FBS的DMEM 培养基上。病患衍生的NMC 11060细胞生长在含10% FBS 和1% Penicillin/Streptomycin的RPMI培养基上。通过自动化针转移机将(+)-JQ1置于微量检测板上。使细胞裂解,通过增殖试验测评孔中的总ATP含量。根据剂量,重复测量分析,通过逻辑回归(GraphPad Prism)计算IC50。

实验图片 检测方法 检测指标 实验图片 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
体内研究(In Vivo)
体内研究活性 (+)-JQ1(50 mg/kg)处理携带NMC 797移植瘤的小鼠,抑制肿瘤生长。(+)-JQ1(50 mg/kg) 抹消掉携带NMC 797移植瘤的小鼠的NUT核斑点, 与竞争性结合到核染色质相一致。(+)-JQ1(50 mg/kg)处理NMC 797移植瘤, 显著诱导(31级)角蛋白表达。(+)-JQ1(50 mg/kg)处理携带NMC移植瘤的小鼠模型,促进分化,肿瘤衰退,延长寿命。[1](+)-JQ1(50 mg/kg)处理静脉注射MM.1S-luc+细胞,携带原位移植瘤的SCID米色小鼠,与对照组动物相比,显著延长小鼠的总生存期。[2](+)-JQ1(50 mg/kg,腹腔注射)处理携带Raji移植瘤的小鼠,显著提高小鼠寿命。[3]
动物实验 Animal Models 携带NMC 797移植瘤的小鼠
Dosages 50 mg/kg
Administration 腹腔注射

化学信息&溶解度

分子量 456.99 分子式

C23H25ClN4O2S

CAS号 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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 91 mg/mL ( (199.12 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 91 mg/mL (199.12 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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常见问题及建议解决方法

问题 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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