(+)-JQ1 | Tocris Bioscience 4499 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

(+)-JQ1

catalog :

4499

quantity :

10 mg

price :

353 USD

more info or order :

Tocris Bioscience product webpage

citations: 12

Reference
Andrieu G, Shafran J, Smith C, Belkina A, Casey A, Jafari N, et al. BET protein targeting suppresses the PD-1/PD-L1 pathway in triple-negative breast cancer and elicits anti-tumor immune response. Cancer Lett. 2019;465:45-58 pubmed publisher
Noblejas López M, Nieto Jiménez C, Burgos M, Gómez Juárez M, Montero J, Esparís Ogando A, et al. Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer. J Exp Clin Cancer Res. 2019;38:383 pubmed publisher
Lin X, Spindler T, de Souza Fonseca M, Corona R, Seo J, Dezem F, et al. Super-Enhancer-Associated LncRNA UCA1 Interacts Directly with AMOT to Activate YAP Target Genes in Epithelial Ovarian Cancer. iScience. 2019;17:242-255 pubmed publisher
Georgilis A, Klotz S, Hanley C, Herranz N, Weirich B, Morancho B, et al. PTBP1-Mediated Alternative Splicing Regulates the Inflammatory Secretome and the Pro-tumorigenic Effects of Senescent Cells. Cancer Cell. 2018;34:85-102.e9 pubmed publisher
Sakaguchi T, Yoshino H, Sugita S, Miyamoto K, Yonemori M, Osako Y, et al. Bromodomain protein BRD4 inhibitor JQ1 regulates potential prognostic molecules in advanced renal cell carcinoma. Oncotarget. 2018;9:23003-23017 pubmed publisher
Xie H, Tang C, Song J, Mancuso A, Del Valle J, Cao J, et al. IRE1α RNase-dependent lipid homeostasis promotes survival in Myc-transformed cancers. J Clin Invest. 2018;128:1300-1316 pubmed publisher
Chen J, Fu Y, Day D, Sun Y, Wang S, Liang X, et al. VEGF amplifies transcription through ETS1 acetylation to enable angiogenesis. Nat Commun. 2017;8:383 pubmed publisher
Jang J, Eom J, Jeung H, Cheong J, Lee J, Kim J, et al. AMPK-ULK1-Mediated Autophagy Confers Resistance to BET Inhibitor JQ1 in Acute Myeloid Leukemia Stem Cells. Clin Cancer Res. 2017;23:2781-2794 pubmed publisher
Kato F, Fiorentino F, AlibÃ©s A, Perucho M, SÃ¡nchez CÃ©spedes M, Kohno T, et al. MYCL is a target of a BET bromodomain inhibitor, JQ1, on growth suppression efficacy in small cell lung cancer cells. Oncotarget. 2016;7:77378-77388 pubmed publisher
Shao Z, Yao C, Khodadadi Jamayran A, Xu W, Townes T, Crowley M, et al. Reprogramming by De-bookmarking the Somatic Transcriptional Program through Targeting of BET Bromodomains. Cell Rep. 2016;16:3138-3145 pubmed publisher
Sartor G, Powell S, Brothers S, Wahlestedt C. Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity. J Neurosci. 2015;35:15062-72 pubmed publisher
Perry M, Durham A, Austin P, Adcock I, Chung K. BET bromodomains regulate transforming growth factor-Î²-induced proliferation and cytokine release in asthmatic airway smooth muscle. J Biol Chem. 2015;290:9111-21 pubmed publisher

product information

brand :

Tocris

master code :

4499

SKU :

4499/10

product name :

(+)-JQ1

description :

Potent and selective BET bromodomain inhibitor; cell permeable

target :

Bromodomain Inhibitors

category :

Small Molecules

unit size :

10 mg

purity :

98%

observed molecular weight :

456.99

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

Potent, high affinity, selective BET bromodomain inhibitor (IC50 values are 17.7, 32.6, 76.9 and 12942 nM for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively; Kd values are 49, 59.5, 82, 90.1, 128 and 190 nM for BRD4 (N), BRD3 (N), BRD3 (C), BRD4 (C), BRD2 (N) and BRDT (N) respectively). Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models in vivo . Exhibits reversible contraceptive effects in germ cells from male mice. . Inactive Analog also available. . Carboxylic acid-functionalized (Cat. No. 6588) and click-activated (alkyne) (Cat. No. 6589) versions for PROTAC development also available.

catalog number base :

4499

product keywords :

BET bromodomains inhibitors inhibits potent selective high affinity NUT midline carcinomas antitumor male contraceptive BRD2 BRD3 BRD4 BRDT sgc Bromodomains 4499,

extended description :

Potent and selective BET bromodomain inhibitor; cell permeable

chemical name text :

(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetic acid 1,1-dimethylethyl ester

formula :

C 23 H 25 ClN 4 O 2 S

formula text :

C23H25ClN4O2S

cas num :

1268524-70-4

2020 USD :

346

2021 USD :

353 USD

storage :

Store at -20°C

more info or order :

Tocris Bioscience product webpage