EBP1 Inhibitor, WS6-Calbiochem

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一般描述

A cell-permeable phenoxypyrimidin-cyclopropanecarboxamide compound that effectively stimulates the growth of primary β cells in cultured primary rat and human isletsin vitro(EC_maxin 4 d = 200 and 400 nM, respectively) and in the murine type 1 diabetes (T1D) model RIP-DTAin vivo(170% of control pancreas Ki-67-positive β cells in 1 wk; 5 mg/kg i.p. q.o.d.) by interacting with IKKε and EBP1/PA2G4/Erb3 binding protein-1 and blocking the known suppressor function of EBP1 toward E2F-mediated transcription. Likewise, dual inhibition of EBP1 (with shRNA) and IKK (1 ?M; Cat. Nos. 401486 & 505378) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells.
A cell-permeable phenoxypyrimidin-cyclopropanecarboxamide compound that effectively stimulates the growth of primary β cells in culturesin vitro(EC_maxin 4 d = 200 and 400 nM, respectively, for increasing Ki-67-positive β cell population in primary rat and human islets) and in the murine type 1 diabetes (T1D) model RIP-DTAin vivo(170% of control pancreas Ki-67-positive β cells in 1 wk and 150% of control pancreas β cell mass in 6 wks; 5 mg/kg i.p. q.o.d.) with significant blood glucose reducing efficacy (200 vs. 425 mg/dL on d45 with or without treatment). WS6 is shown to interact with IKKε and EBP1/PA2G4/Erb3 binding protein-1 as well as upregulate cellular E2F mRNA (2.8- and 4.8-fold of vehicle control, respectively, with 8 h and 12 h treatment; 1 ?M) and transcription activity (1.4- and 1.5-fold of vehicle control, respectively, at 0.74 and 2.22 ?M; 24 h treatment) in murine β cell line R7T1, consistent with blocking the known suppressor function of EBP1 toward E2F-mediated transcription. Likewise, dual inhibition of EBP1 (with shRNA) and IKK (1 ?M; Cat. Nos. 401486 & 505378) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
EBP1/PA2G4/Erb3 binding protein-1
Secondary Target
IKKε

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Shen, W., et al. 2013.J. Am. Chem. Soc.135,1669.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

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安全信息