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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 Chemical Structure

(+)-JQ1 Chemical Structure

CAS No. 1268524-70-4

Purity & Quality Control

(+)-JQ1 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K1  Cell Viability Assay 250/500/1000 nM 24/48/72 h DMSO inhibits cell viability in both dose- and time- dependent manner 26707881
BCPAP Cell Viability Assay 250/500/1000 nM 24/48/72 h DMSO inhibits cell viability in both dose- and time- dependent manner 26707881
K1  Cell Cycle Assay 250/500/1000 nM 72 h DMSO arrests cell cycle at G0/G1 phase 26707881
BCPAP Cell Cycle Assay 250/500/1000 nM 72 h DMSO arrests cell cycle at G0/G1 phase 26707881
Hep3B Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.08 μM 26575167
HCCLM3 Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.14 μM 26575167
HuH7 Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.21 μM 26575167
HepG2 Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.34 μM 26575167
SMMC7721 Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.41 μM 26575167
BEL7402 Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.47 μM 26575167
MHCC97H Growth Inhibition Assay 0-10 μM 5 d DMSO IC50=0.41 μM 26575167
Hep3B Cell Cycle Assay 0.1/0.5/2.5 μM 48 h DMSO leads to a substantial accumulation of HCC cells in sub-G1 phase  26575167
HCCLM3 Cell Cycle Assay 0.1/0.5/2.5 μM 48 h DMSO leads to a substantial accumulation of HCC cells in sub-G1 phase  26575167
Hep3B Apoptosis Assay 0.1/0.5/2.5 μM 48 h DMSO activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria 26575167
HCCLM3 Apoptosis Assay 0.1/0.5/2.5 μM 48 h DMSO activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria 26575167
A549 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
H1299 Growth Inhibition Assay 0.1-10 μM 72 h inhibits cell growth in a dose-dependent manner 26415225
A549 Function Assay 1/2.5/5 μM 12 h  weakly decreased Bcl-2 levels 26415225
H1299 Function Assay 1/2.5/5 μM 12 h  weakly decreased Bcl-2 levels 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 decreased DR4 expression 26415225
C8161 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Mel285 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Mel290 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
92.1 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Omm1.3 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Mel202 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Mel270 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
Omm1 Cell Viability Assay 0-2 μM 4 d DMSO decreases cell viability in a dose-dependent manner 26397223
92.1 Apoptosis Assay 500 nM 48 h DMSO induces apoptosis 26397223
Omm1.3 Apoptosis Assay 500 nM 48 h DMSO induces apoptosis 26397223
92.1 Cell Cycle Assay 500 nM 24/48/72 h DMSO induces the cell accumulation at sub-G1  26397223
Omm1.3 Cell Cycle Assay 500 nM 24/48/72 h DMSO induces the cell accumulation at sub-G1  26397223
A549 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
HEK293 Function Assay 100/400/1000 nM 24 h upregulates and activates SIRT1 26212199
858 Cell Viability Assay 0-1 μM 5 d DMSO decreases cell viability in a dose-dependent manner 26206333
DDR2L63V Cell Viability Assay 0-1 μM 5 d DMSO decreases cell viability in a dose-dependent manner 26206333
BE(2)-C 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
JF 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
SK-N-SH Cell Viability Assay 1 μM 1-4 d decreases cell viability significantly 26067464
SK-N-DZ  Cell Viability Assay 1 μM 1-4 d decreases cell viability significantly 26067464
HMC-1.1  Growth Inhibition Assay 5-5000 nM 48 h DMSO inhibits cell growth in a dose-dependent manner 26055303
HMC-1.2 Growth Inhibition Assay 5-5000 nM 48 h DMSO inhibits cell growth in a dose-dependent manner 26055303
ROSA KIT WT  Growth Inhibition Assay 5-5000 nM 48 h DMSO inhibits cell growth in a dose-dependent manner 26055303
ROSA KIT D816V Growth Inhibition Assay 5-5000 nM 48 h DMSO inhibits cell growth in a dose-dependent manner 26055303
HMC-1.1  Apoptosis Assay 200-5000 nM 48 h DMSO induces cell apoptosis in a dose-dependent manner 26055303
HMC-1.2 Apoptosis Assay 200-5000 nM 48 h DMSO induces cell apoptosis in a dose-dependent manner 26055303
ROSA KIT WT  Apoptosis Assay 200-5000 nM 48 h DMSO induces cell apoptosis in a dose-dependent manner 26055303
ROSA KIT D816V Apoptosis Assay 200-5000 nM 48 h DMSO induces cell apoptosis in a dose-dependent manner 26055303
494H Growth Inhibition Assay 72 h DMSO IC50=0.122±0.004 μM 25944566
493H Growth Inhibition Assay 72 h DMSO IC50=0.047±0.009 μM 25944566
716H Growth Inhibition Assay 72 h DMSO IC50=0.212±0.034 μM 25944566
148I Growth Inhibition Assay 72 h DMSO IC50=0.284±0.035 μM 25944566
98Sc Growth Inhibition Assay 72 h DMSO IC50=0.115±0.004 μM 25944566
89R Growth Inhibition Assay 72 h DMSO IC50=0.126±0.003 μM 25944566
494L Growth Inhibition Assay 72 h DMSO IC50=0.317±0.012 μM 25944566
493L Growth Inhibition Assay 72 h DMSO IC50=0.050±0.011 μM 25944566
148L Growth Inhibition Assay 72 h DMSO IC50=0.146±0.017 μM 25944566
98L Growth Inhibition Assay 72 h DMSO IC50=0.309±0.029 μM 25944566
OS17 Growth Inhibition Assay 72 h DMSO IC50=0.079±0.003 μM 25944566
OS9 Growth Inhibition Assay 72 h DMSO IC50=0.406±0.028 μM 25944566
MG63 Growth Inhibition Assay 72 h DMSO IC50=0.114±0.025 μM 25944566
SAOS2 Growth Inhibition Assay 72 h DMSO IC50=0.217±0.003 μM 25944566
U2OS Growth Inhibition Assay 72 h DMSO IC50=0.198±0.008 μM 25944566
SJSA-1 Growth Inhibition Assay 72 h DMSO IC50=0.100±0.010 μM 25944566
494H Apoptosis Assay 0.25/0.5/1.0 μM 24 h DMSO increases levels of cleaved caspase-3  25944566
148I Apoptosis Assay 0.25/0.5/1.0 μM 24 h DMSO increases levels of cleaved caspase-3  25944566
OS17 Apoptosis Assay 0.25/0.5/1.0 μM 24 h DMSO increases levels of cleaved caspase-3  25944566
494H Apoptosis Assay 1 μM 48 h DMSO induces cell apoptosis significantly 25944566
148I Apoptosis Assay 1 μM 48 h DMSO induces cell apoptosis significantly 25944566
OS17 Apoptosis Assay 1 μM 48 h DMSO induces cell apoptosis significantly 25944566
MOLM13 Apoptosis Assay 250 nM 48 h DMSO induces significantly apoptosis cotreatment with quizartinib 25053825
MV4-11  Apoptosis Assay 250 nM 48 h DMSO induces significantly apoptosis cotreatment with quizartinib 25053825
MOLM13 Function Assay 250 nM 24 h DMSO enhances quizartinib-induced more p21, BIM, and cleaved PARP 25053825
MV4-11  Function Assay 250 nM 24 h DMSO enhances quizartinib-induced more p21, BIM, and cleaved PARP 25053825
MOLM13 Apoptosis Assay 250 nM 48 h DMSO induces significantly apoptosis cotreatment with ponatinib 25053825
MV4-11  Apoptosis Assay 250 nM 48 h DMSO induces significantly apoptosis cotreatment with ponatinib 25053825
Hela Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
HBL-1 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
HLY-1 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
OCI-Ly3 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
OCI-Ly10 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
SU-DHL-4 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
SU-DHL-5 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
SU-DHL-6 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
SU-DHL-10 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
RC-K8 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
OCI-Ly8 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
OCL-Ly18 Cell Viability Assay 0-500 nM 72 h DMSO decreases cell viability in a dose-dependent manner 25009295
OCI-Ly3 Growth Inhibition Assay 172/250/500 nM 2/7 d DMSO induces cell-cycle arrest at sub-G1 with minimal cell death  25009295
OCI-Ly8 Growth Inhibition Assay 172/250/500 nM 2/7 d DMSO 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 DMSO 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 DMSO induces cell-cycle arrest at sub-G1 with minimal cell death  25009295
OCI-Ly3 Apoptosis Assay 172/250 nM 7d DMSO increases caspase-3/7 activity significantly 25009295
OCI-Ly8 Apoptosis Assay 172/250 nM 7d DMSO increases caspase-3/7 activity significantly 25009295
SU-DHL-4 Apoptosis Assay 172/250 nM 7d DMSO increases caspase-3/7 activity significantly 25009295
SU-DHL-10 Apoptosis Assay 172/250 nM 7d DMSO increases caspase-3/7 activity significantly 25009295
Rosetta2 DE3 Function assay Kd = 0.0062 μM 26080064
Rosetta2 DE3 Fluorescence polarization assay 30 mins Ki = 0.0066 μM 26080064
Rosetta2 DE3 Function assay Kd = 0.0067 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
Rosetta2 DE3 Function assay Kd = 0.0117 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 Function assay Kd = 0.0128 μM 26080064
Rosetta2 DE3 Fluorescence polarization assay 30 mins Ki = 0.0132 μM 26080064
Rosetta2 DE3 Function assay Kd = 0.0136 μM 26080064
Rosetta2 DE3 Function assay Kd = 0.0147 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
BL21(DE3) Function assay Kd = 0.034 μM 26731490
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 IC50 = 0.06 μM 26731490
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
MV4-11 Antiproliferative activity assay IC50 = 0.072 μM 28195723
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
BL21(DE3) Function assay Kd = 0.092 μM 29541371
BL21(DE3)-R3-pRARE2 Function assay Kd = 0.1 μM 28595007
HT-29 Growth inhibition assay 72 h IC50 = 0.104 μM 25559428
MM1S Growth inhibition assay 72 h IC50 = 0.109 μM 25559428
LNCAP cells Antiproliferative activity assay IC50 = 0.1096 μM 29758518
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 IC50 = 0.12 μM 26731490
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 Antiproliferative activity assay IC50 = 0.24 μM 27142751
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
K562 Antiproliferative activity assay IC50 = 0.64 μM 27142751
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
Click to View More Cell Line Experimental Data

Biological Activity

Description (+)-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.
Features (+)-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]
Cell Research Cell lines MC 11060 cells
Concentrations ~500 nM
Incubation Time 48 hours
Method

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).
Experimental Result Images Methods Biomarkers Images 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]
Animal Research Animal Models Mice bearing NMC 797 xenografts
Dosages 50 mg/kg
Administration intraperitoneal injection

Chemical Information & Solubility

Molecular Weight 456.99 Formula

C23H25ClN4O2S
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (199.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

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

Answer:
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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