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Merck

SML2683

Sigma-Aldrich

dBET6

≥98% (HPLC)

别名:

(6S)-4-(4-Chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

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About This Item

经验公式(希尔记法):
C42H45ClN8O7S
分子量:
841.37
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

ligand

thalidomide

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

生化/生理作用

dBET6 is a highly cell penetrant, potent and selective BET (bromodomain and extra-terminal domain) degrader that induces rapid (<4hrs) degradation of BRD2, BRD3 and BRD4 and complete down-regulation of c-MYC protein and induction of apoptosis. dBET6 exhibits potent anti-cancer activities.

相關產品

产品编号
说明
价格

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Liang Xu et al.
Proceedings of the National Academy of Sciences of the United States of America, 115(22), E5086-E5095 (2018-05-17)
Competitive BET bromodomain inhibitors (BBIs) targeting BET proteins (BRD2, BRD3, BRD4, and BRDT) show promising preclinical activities against brain cancers. However, the BET protein-dependent glioblastoma (GBM)-promoting transcriptional network remains elusive. Here, with mechanistic exploration of a next-generation chemical degrader of
Georg E Winter et al.
Molecular cell, 67(1), 5-18 (2017-07-05)
Processive elongation of RNA Polymerase II from a proximal promoter paused state is a rate-limiting event in human gene control. A small number of regulatory factors influence transcription elongation on a global scale. Prior research using small-molecule BET bromodomain inhibitors
Behnam Nabet et al.
Nature chemical biology, 14(5), 431-441 (2018-03-28)
Dissection of complex biological systems requires target-specific control of the function or abundance of proteins. Genetic perturbations are limited by off-target effects, multicomponent complexity, and irreversibility. Most limiting is the requisite delay between modulation to experimental measurement. To enable the

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