Home Epigenetics Target Protein Ligand 화학물질 (+)-JQ1

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(+)-JQ1 BET 억제제

제품 번호S7110

(+)-JQ1은 BET bromodomain 억제제로, 세포 없는 분석에서 BRD4(1/2)에 대해 77nM/33nM의 IC50을 가지며, BET 계열의 모든 브로모도메인에 결합하지만 BET 계열 외부의 브로모도메인에는 결합하지 않습니다. (+)-JQ1은 autophagy 유도를 통해 세포 증식을 억제합니다. (+)-JQ1은 Nuclear receptor binding SET domain protein 3 (NSD3) 표적 유전자의 발현을 억제합니다.
(+)-JQ1 Target Protein Ligand 화학물질 Chemical Structure

화학 구조

분자량: 456.99

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품질 관리

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 456.99 화학식

C23H25ClN4O2S

 보관 (수령일로부터)
CAS 번호 1268524-70-4 SDF 다운로드 원액 보관

동의어 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

용해도

In vitro
배치:

DMSO : 91 mg/mL (199.12 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 91 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징
(+)-JQ1 is more effective than (-)-JQ1.
Targets/IC50/Ki
BRD4 (2)
(Cell-free assay)
33 nM
BRD4 (1)
(Cell-free assay)
77 nM
시험관 내(In vitro)
(+)-JQ1 이성질체는 BET 브로모도메인의 Kac 결합 부위에 직접 결합합니다. 이 화합물(500 nM)은 BRD4와 크로마틴에 경쟁적으로 결합하여 NMC 세포의 분화 및 성장 정지를 유도합니다. 이 화학물질(500 nM)은 Ki67 염색 감소로 입증된 바와 같이 NMC 797 및 Per403 세포주의 빠른 증식을 약화시킵니다. 이 화합물(500 nM)은 NMC 797 세포에서 두 BRD4 표적 유전자의 발현을 강력하게 감소시킵니다. NMC 11060 세포에서 IC50이 4 nM인 세포 생존력을 억제합니다. 이는 MM 세포주에서 MYC 발현을 강력하게 억제합니다. 이 화합물은 KMS-34 및 LR5의 증식을 각각 68 nM 및 98 nM의 IC50으로 억제합니다. 이 화학물질(500 nM)로 처리된 MM.1S 세포는 S-단계 세포의 비율이 현저하게 감소하고, G0/G1 단계에 정지된 세포의 수가 동시에 증가합니다. 이는 (500 nM) 베타-갈락토시다아제 염색에 의해 현저한 세포 노화를 유도합니다. 이 화합물(800 nM) 노출은 테스트된 CD138+ 환자 유래 MM 샘플의 대부분에서 세포 생존력을 유의하게 감소시킵니다. 이는 LP-1 세포의 성장을 98 nM의 GI50으로 억제합니다. 이 화학물질(625 nM)은 G0/G1 단계에 있는 LP-1 세포의 비율을 증가시킵니다. 이는 (500 nM) LP-1 세포에서 MYC, BRD4 및 CDK9의 발현을 억제합니다. 이 화합물(1 μM)은 잠복 감염된 Jurkat T 세포에서 HIV 전사를 활성화합니다. 이는 (50 μM) Jurkat 및 HeLa 세포 모두에서 Tat-의존성 HIV 전사를 주로 자극합니다. 이 화학물질(5 μM)은 Brd4 해리를 유도하여 Tat이 SEC를 HIV 프로모터로 모집하고 J-Lat A2 세포에서 Pol II CTD 인산화 및 바이러스 전사를 유도할 수 있도록 합니다. 이는 Tat이 CDK9 T-루프 인산화를 증가시키고 Jurkat T 세포에서 P-TEFb를 7SK snRNP로부터 부분적으로 해리시킬 수 있도록 합니다.
생체 내(In vivo)
(+)-JQ1 (50 mg/kg)은 NMC 797 이종이식을 받은 쥐에서 종양 성장을 억제합니다. 이 화합물은 NMC 797 이종이식을 받은 쥐에서 NUT 핵 반점의 소실을 초래하며, 이는 핵 염색질에 대한 경쟁적 결합과 일치합니다. 이는 NMC 797 이종이식에서 강력한 (31등급) 케라틴 발현을 유도합니다. 이 화학 물질은 NMC 이종이식 쥐 모델에서 분화, 종양 퇴행 및 생존 기간 연장을 촉진합니다. 이는 MM.1S-luc+ 세포를 정맥 주사한 후 정위적으로 이종이식된 SCID-베이지 쥐의 전체 생존 기간을 차량 처리 동물에 비해 유의하게 연장시킵니다. 이 화합물은 Raji 이종이식을 가진 쥐의 생존 기간을 매우 유의하게 증가시킵니다.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/23087374/

적용 분야

방법 바이오마커 이미지 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

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자주 묻는 질문

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

답변:
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.