|(S)-2-(4-(4-氯苯基)-2,3,9-三甲基-6H-噻吩并[3,2-F][1,2,4]三唑并[4,3-A][1,4]二氮杂卓-6-基)乙酸叔丁酯|CsnPharm

CAS No.: 1268524-70-4

(S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Catalog No. CSN13058

Synonyms: JQ1;Bromodomain Inhibitor

(+)-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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bromodomain 4

IC50:77nM or 33 nM
描述BRDs (bromodomains) of human proteome can recognize the relaxed chromatin segments and bind to the acetylated nucleosomes, transcription factors and co-activators. (+)-JQ1 is a potent and selective bromodomain inhibitor with IC50 values of 77nM, 33nM and >10uM for BRD4(1), BRD4(2) and CREBBP, respectively^[1]. The (+)-JQ-1-specific inhibition of BRDs can affect the production of the targeted transcription factor-dependent protein, including NRF2-dependent HO-1, NADPH:quinone oxidoreductase-1 as well as GCLC, SOCS3, STAT5-mediated regulation of target genes, RUNX3, SIRT1, MYC and its downstream target genes, etc.^[2]. JQ1 can induce the differentiation and growth arrest in NUT midline carcinoma. Treatment with (+)-JQ-1, 250nM for 48h, potently decreased the expression of both BRD4 target genes, RAD21 and RAN, in NMC cells. Treatment with JQ1, i.p., 50mg/kg for 18 days, can regress the tumor growth and prolong overall survival of NMC797 xenografted mice. In addition, (-)-JQ-1 is the negative control compound of (+)-JQ-1^[1].
作用机制JQ1 can bind lysine acetylation binding site of BET bromodomains competitively with chromatin in a cellular environment.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
148I	-	Growth Inhibition Assay	72 h	IC50=0.284±0.035 μM	25944566
148I	0.25/0.5/1.0 μM	Apoptosis Assay	24 h	increases levels of cleaved caspase-3	25944566
148I	1 μM	Apoptosis Assay	48 h	induces cell apoptosis significantly	25944566

更多
动物研究
剂量
Mice^[1] (i.p.): 50 mg/kg

给药途径
i.p.
参考文献

动物研究
剂量	Mice^[1] (i.p.): 50 mg/kg
给药途径	i.p.

[1] Filippakopoulos P, Qi J, et al. Selective inhibition of BET bromodomains. Nature. 2010;468(7327):1067-73.
[2] Shin DG, Bayarsaihan D. A Novel Epi-drug Therapy Based on the Suppression of BET Family Epigenetic Readers. Yale J Biol Med. 2017;90(1):63-71.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1882 mL
- 10.9412 mL
- 21.8823 mL
- 5 mM
- 0.4376 mL
- 2.1882 mL
- 4.3765 mL
- 10 mM
- 0.2188 mL
- 1.0941 mL
- 2.1882 mL

技术信息

CAS号

1268524-70-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H25ClN4O2S

运输

蓝冰

分子量

456.99

别名

JQ1;Bromodomain Inhibitor

溶解度

DMSO	660.0 mg/mL (1444.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	6 mg/mL	clear
PO	0.5% CMC-Na	45 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

148I	-	Growth Inhibition Assay	72 h	IC50=0.284±0.035 μM	25944566
148I	0.25/0.5/1.0 μM	Apoptosis Assay	24 h	increases levels of cleaved caspase-3	25944566
148I	1 μM	Apoptosis Assay	48 h	induces cell apoptosis significantly	25944566
148L	-	Growth Inhibition Assay	72 h	IC50=0.146±0.017 μM	25944566
493H	-	Growth Inhibition Assay	72 h	IC50=0.047±0.009 μM	25944566
493L	-	Growth Inhibition Assay	72 h	IC50=0.050±0.011 μM	25944566
494H	-	Growth Inhibition Assay	72 h	IC50=0.122±0.004 μM	25944566
494H	0.25/0.5/1.0 μM	Apoptosis Assay	24 h	increases levels of cleaved caspase-3	25944566
494H	1 μM	Apoptosis Assay	48 h	induces cell apoptosis significantly	25944566
494L	-	Growth Inhibition Assay	72 h	IC50=0.317±0.012 μM	25944566
716H	-	Growth Inhibition Assay	72 h	IC50=0.212±0.034 μM	25944566
858	0-1 μM	Cell Viability Assay	5 d	decreases cell viability in a dose-dependent manner	26206333
89R	-	Growth Inhibition Assay	72 h	IC50=0.126±0.003 μM	25944566
92.1	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
92.1	500 nM	Apoptosis Assay	48 h	induces apoptosis	26397223
92.1	500 nM	Cell Cycle Assay	24/48/72 h	induces the cell accumulation at sub-G1	26397223
98L	-	Growth Inhibition Assay	72 h	IC50=0.309±0.029 μM	25944566
98Sc	-	Growth Inhibition Assay	72 h	IC50=0.115±0.004 μM	25944566
A549	0.1-10 μM	Growth Inhibition Assay	72 h	inhibits cell growth in a dose-dependent manner	26415225
A549	1/2.5/5 μM	Function Assay	12 h	weakly decreased Bcl-2 levels	26415225
A549	100/400/1000 nM	Function Assay	24 h	upregulates and activates SIRT1	26212199
BCPAP	250/500/1000 nM	Cell Viability Assay	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
BCPAP	250/500/1000 nM	Cell Cycle Assay	72 h	arrests cell cycle at G0/G1 phase	26707881
BE(2)-C	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
BE(2)-M17	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
BEL7402	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.47 μM	26575167
C8161	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
DDR2L63V	0-1 μM	Cell Viability Assay	5 d	decreases cell viability in a dose-dependent manner	26206333
H1299	0.1-10 μM	Growth Inhibition Assay	72 h	inhibits cell growth in a dose-dependent manner	26415225
H1299	1/2.5/5 μM	Function Assay	12 h	weakly decreased Bcl-2 levels	26415225
H1299	1/2.5/5 μM	Function Assay	12 h	decreased DR4 expression	26415225
H157	0.1-10 μM	Growth Inhibition Assay	72 h	inhibits cell growth in a dose-dependent manner	26415225
H157	1/2.5/5 μM	Function Assay	12 h	decreased DR4 expression	26415225
HBL-1	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
HCCLM3	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.14 μM	26575167
HCCLM3	0.1/0.5/2.5 μM	Cell Cycle Assay	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
HCCLM3	0.1/0.5/2.5 μM	Apoptosis Assay	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
HEK293	100/400/1000 nM	Function Assay	24 h	upregulates and activates SIRT1	26212199
Hela	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
Hep3B	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.08 μM	26575167
Hep3B	0.1/0.5/2.5 μM	Cell Cycle Assay	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
Hep3B	0.1/0.5/2.5 μM	Apoptosis Assay	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
HepG2	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.34 μM	26575167
HLY-1	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
HMC-1.1	5-5000 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.1	200-5000 nM	Apoptosis Assay	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HMC-1.2	5-5000 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.2	200-5000 nM	Apoptosis Assay	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HuH7	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.21 μM	26575167
IMR-32	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
JF	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
K1	250/500/1000 nM	Cell Viability Assay	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
K1	250/500/1000 nM	Cell Cycle Assay	72 h	arrests cell cycle at G0/G1 phase	26707881
MCF-7	100/400/1000 nM	Function Assay	24 h	upregulates and activates SIRT1	26212199
Mel202	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel270	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel285	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel290	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
MG63	-	Growth Inhibition Assay	72 h	IC50=0.114±0.025 μM	25944566
MHCC97H	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.41 μM	26575167
MOLM13	250 nM	Apoptosis Assay	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MOLM13	250 nM	Function Assay	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MOLM13	250 nM	Apoptosis Assay	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
MV4-11	250 nM	Apoptosis Assay	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MV4-11	250 nM	Function Assay	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MV4-11	250 nM	Apoptosis Assay	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
OCI-Ly10	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	172/250/500 nM	Growth Inhibition Assay	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly3	172/250 nM	Apoptosis Assay	7d	increases caspase-3/7 activity significantly	25009295
OCI-Ly8	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly8	172/250/500 nM	Growth Inhibition Assay	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly8	172/250 nM	Apoptosis Assay	7d	increases caspase-3/7 activity significantly	25009295
OCL-Ly18	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
Omm1	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
Omm1.3	0-2 μM	Cell Viability Assay	4 d	decreases cell viability in a dose-dependent manner	26397223
Omm1.3	500 nM	Apoptosis Assay	48 h	induces apoptosis	26397223
Omm1.3	500 nM	Cell Cycle Assay	24/48/72 h	induces the cell accumulation at sub-G1	26397223
OS17	-	Growth Inhibition Assay	72 h	IC50=0.079±0.003 μM	25944566
OS17	0.25/0.5/1.0 μM	Apoptosis Assay	24 h	increases levels of cleaved caspase-3	25944566
OS17	1 μM	Apoptosis Assay	48 h	induces cell apoptosis significantly	25944566
OS9	-	Growth Inhibition Assay	72 h	IC50=0.406±0.028 μM	25944566
RC-K8	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
ROSA KIT D816V	5-5000 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	26055303
ROSA KIT D816V	200-5000 nM	Apoptosis Assay	48 h	induces cell apoptosis in a dose-dependent manner	26055303
ROSA KIT WT	5-5000 nM	Growth Inhibition Assay	48 h	inhibits cell growth in a dose-dependent manner	26055303
ROSA KIT WT	200-5000 nM	Apoptosis Assay	48 h	induces cell apoptosis in a dose-dependent manner	26055303
SAOS2	-	Growth Inhibition Assay	72 h	IC50=0.217±0.003 μM	25944566
SJSA-1	-	Growth Inhibition Assay	72 h	IC50=0.100±0.010 μM	25944566
SK-N-DZ	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
SK-N-SH	1 μM	Cell Viability Assay	1-4 d	decreases cell viability significantly	26067464
SMMC7721	0-10 μM	Growth Inhibition Assay	5 d	IC50=0.41 μM	26575167
SU-DHL-10	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-10	172/250/500 nM	Growth Inhibition Assay	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-10	172/250 nM	Apoptosis Assay	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-4	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-4	172/250/500 nM	Growth Inhibition Assay	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-4	172/250 nM	Apoptosis Assay	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-5	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-6	0-500 nM	Cell Viability Assay	72 h	decreases cell viability in a dose-dependent manner	25009295
U2OS	-	Growth Inhibition Assay	72 h	IC50=0.198±0.008 μM	25944566

(S)-tert-Butyl 2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Catalog No. CSN13058

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