All Photos(1)
Synonym(s):
EBP1 Inhibitor, WS6, N-(6-(4-(2-(4-((4-Methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenylamino)-2-oxoethyl)phenoxy)pyrimidin-4-yl)cyclopropanecarboxamide, xHCl, Erb3 Binding Protein-1 Inhibitor, IKK Inhibitor XV, PA2G4 Inhibitor
Empirical Formula (Hill Notation):
C29H31F3N6O3 · xHCl
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
white
solubility
DMSO: 100 mg/mL
water: 100 mg/mL
storage temp.
−20°C
SMILES string
CN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)CC3=CC=C(C=C3)OC4=NC=NC(=C4)NC(=O)C5CC5)C(F)(F)F
General description
A cell-permeable phenoxypyrimidin-cyclopropanecarboxamide compound that effectively stimulates the growth of primary β cells in cultured primary rat and human islets in vitro (ECmax in 4 d = 200 and 400 nM, respectively) and in the murine type 1 diabetes (T1D) model RIP-DTA in 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 µM; 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 cultures in vitro (ECmax in 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-DTA in 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 µM) and transcription activity (1.4- and 1.5-fold of vehicle control, respectively, at 0.74 and 2.22 µM; 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 µM; Cat. Nos. 401486 & 505378) is shown to fully recapitulate the proliferating effect of WS6 in R7T1 cells.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EBP1/PA2G4/Erb3 binding protein-1
EBP1/PA2G4/Erb3 binding protein-1
Reversible: yes
Secondary Target
IKKε
IKKε
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Shen, W., et al. 2013. J. Am. Chem. Soc.135, 1669.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
新产品
Certificates of Analysis (COA)
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