Home Epigenetics Target Protein Ligand chemisch (+)-JQ1

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(+)-JQ1 BET-remmer

Cat.Nr.S7110

(+)-JQ1 is een BET-bromodomein-remmer, met een IC50 van 77 nM/33 nM voor BRD4(1/2) in celvrije assays, die bindt aan alle bromodomeinen van de BET-familie, maar niet aan bromodomeinen buiten de BET-familie. (+)-JQ1 onderdrukt celproliferatie door autophagy te induceren. (+)-JQ1 remt de expressie van Nuclear receptor binding SET domain protein 3 (NSD3) doelgenen.
(+)-JQ1 Target Protein Ligand chemisch Chemical Structure

Chemische structuur

Moleculair gewicht: 456.99

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%
99.99

Celkweek, behandeling & werkconcentratie

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving 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
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht 456.99 Formule

C23H25ClN4O2S

 Opslag (Vanaf de ontvangstdatum)
CAS-nr. 1268524-70-4 SDF downloaden Opslag van stamoplossingen

Synoniemen N/A Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C

Oplosbaarheid

In vitro
Batch:

DMSO : 91 mg/mL (199.12 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble

Molariteitscalculator

Massa Concentratie Volume Moleculair gewicht
Verdunningscalculator Moleculair gewicht calculator

In vivo
Batch:

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Kenmerken
(+)-JQ1 is more effective than (-)-JQ1.
Targets/IC50/Ki
BRD4 (2)
(Cell-free assay)
33 nM
BRD4 (1)
(Cell-free assay)
77 nM
In vitro
Het (+)-JQ1-enantiomeer bindt direct in de Kac-bindingsplaats van BET-bromodomeinen. Deze verbinding (500 nM) bindt BRD4 competitief met chromatine, wat resulteert in differentiatie en groeistilstand van NMC-cellen. Deze chemische stof (500 nM) vermindert de snelle proliferatie van NMC 797- en Per403-cellijnen, zoals aangetoond door verminderde Ki67-kleuring. Deze verbinding (500 nM) vermindert krachtig de expressie van beide BRD4-doelgenen in NMC 797-cellen. Het remt de cellulaire vitaliteit met een IC50 van 4 nM in NMC 11060-cellen. Het resulteert in robuuste remming van MYC-expressie in MM-cellijnen. Deze verbinding remt de proliferatie van KMS-34 en LR5 met een IC50 van respectievelijk 68 nM en 98 nM. Deze chemische stof (500 nM) behandelde MM.1S-cellen resulteert in een uitgesproken afname van het aandeel cellen in de S-fase, met een gelijktijdige toename van cellen die in G0/G1 zijn gearresteerd. Het (500 nM) resulteert in uitgesproken cellulaire senescentie door beta-galactosidase-kleuring. Blootstelling aan deze verbinding (800 nM) leidt tot een significante vermindering van de cellevensvatbaarheid onder de meerderheid van de geteste CD138+ patiënt-afgeleide MM-monsters. Het remt de groei van LP-1-cellen met een GI50 van 98 nM. Deze chemische stof (625 nM) resulteert in een toename van het percentage LP-1-cellen in G0/G1. Het (500 nM) onderdrukt de expressie van MYC, BRD4 en CDK9 in LP-1-cellen. Deze verbinding (1 μM) activeert HIV-transcriptie in latent geïnfecteerde Jurkat T-cellen. Het (50 μM) stimuleert voornamelijk Tat-afhankelijke HIV-transcriptie in zowel Jurkat- als HeLa-cellen. Deze chemische stof (5 μM) induceert Brd4-dissociatie, waardoor Tat SEC kan rekruteren naar de HIV-promotor en Pol II CTD-fosforylering en virale transcriptie kan induceren in J-Lat A2-cellen. Het stelt Tat in staat om CDK9 T-loop-fosforylering te verhogen en P-TEFb gedeeltelijk te dissociëren van 7SK snRNP in Jurkat T-cellen.
In vivo
(+)-JQ1 (50 mg/kg) remt tumorgroei bij muizen met NMC 797-xenografts. Deze verbinding resulteert in verdwijning van NUT-kernspikkels bij muizen met NMC 797-xenografts, in overeenstemming met competitieve binding aan nucleair chromatine. Het induceert een sterke (graad 31) keratine-expressie in NMC 797-xenografts. Deze chemische stof bevordert differentiatie, tumorregressie en een langere overleving in muismodellen van NMC-xenografts. Het resulteert in een significante verlenging van de algehele overleving van SCID-beige muizen die orthotopisch zijn getransplanteerd na intraveneuze injectie met MM.1S-luc+-cellen, vergeleken met voertuigbehandelde dieren. Deze verbinding leidt tot een zeer significante toename van de overleving van muizen met Raji-xenografts.
Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/23087374/

Toepassingen

Methoden Biomarkers Afbeeldingen PMID
Western blot pDNA-PKcs / γH2AX / Ub-γH2AX / p-c-Jun S63 / Bax c-Myc p27
S7110-WB1
26119999
Growth inhibition assay Cell viability
S7110-viability1
23792448
Immunofluorescence GM130 MHC / EdU
S7110-IF1
29074567

Technische ondersteuning

Gebruiksaanwijzing

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Veelgestelde vragen

Vraag 1:
How can I reconstitute it for in vivo injection?

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