MZ 1 | Tocris Bioscience 6154 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

MZ 1

catalog :

6154

quantity :

5 mg

price :

388 USD

more info or order :

Tocris Bioscience product webpage

citations: 5

Reference
Kaji T, Koga H, Kuroha M, Akimoto T, Hayata K. Characterization of cereblon-dependent targeted protein degrader by visualizing the spatiotemporal ternary complex formation in cells. Sci Rep. 2020;10:3088 pubmed publisher
Otto C, Schmidt S, Kastner C, Denk S, Kettler J, Muller N, et al. Targeting bromodomain-containing protein 4 (BRD4) inhibits MYC expression in colorectal cancer cells. Neoplasia. 2019;21:1110-1120 pubmed publisher
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
Tsujikawa L, Fu L, Das S, Halliday C, Rakai B, Stotz S, et al. Apabetalone (RVX-208) reduces vascular inflammation in vitro and in CVD patients by a BET-dependent epigenetic mechanism. Clin Epigenetics. 2019;11:102 pubmed publisher

product information

brand :

Tocris

master code :

6154

SKU :

6154/5

product name :

MZ 1

description :

(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells

target :

Active Degraders

category :

Small Molecules

unit size :

5 mg

purity :

98%

observed molecular weight :

1002.64

url print :

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

details of functionality :

Cell penetrant Proteolysis Targeting Chimera (PROTAC ) compound based on (+)-JQ1 (Cat.No. 4499) conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and antiproliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells). Negative control cis MZ 1 also available. . PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license.

catalog number base :

6154

product keywords :

MZ1 PROTAC PROTACs Proteolysis targeted chimeras Bromodomain BRD2 BRD3 BRD4 BET proteins JQ1 VHL E3 ubiquitin ligase HIF-alpha HIF-a HIF- active degraders degrades targeted protein degradation tpd Ubiquitin E3 Ligases Bromodomains Active Degraders 6154, target protein knockdown, PROTAC, SNIPER

extended description :

(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells

chemical name text :

(2S,4R)-1-((S)-2-(tert-butyl)-17-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-4,16-dioxo-6,9,12-trioxa-3,15-diazaheptadecanoyl)- 4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

formula :

C 49 H 60 ClN 9 O 8 S 2

formula text :

C49H60ClN9O8S2

cas num :

1797406-69-9

2020 USD :

373

2021 USD :

388 USD

storage :

Store at -20°C

more info or order :

Tocris Bioscience product webpage