Products
Online Inquiry
Our Products Cannot Be Used As Medicines Directly For Personal Use.
Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.
PF-4708671
Cat No.
CEI-0865
Description
PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity FOR S6K1than MSK1 and RSK1/2, respectively. First S6K1-specific inhibitor to be reported.
Alias
PF-04708671
CAS No.
1255517-76-0
Molecular Weight
390.41
Storage
2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.
Synonyms
PF-04708671
Targets
p70 S6K1
IC50
160 nM
Molecular Formula
C19H21F3N6
Chemical Name
1H-Benzimidazole, 2-[[4-(5-ethyl-4-pyrimidinyl)-1-piperazinyl]methyl]-6-(trifluoromethyl)-
Solubility
DMSO 30 mg/mL; Water <1 mg/mL; Ethanol 8 mg/mL
In vitro
PF-4708671 is a piperazinyl-pyrimidine analogue and the first S6K1-specific inhibitor. PF-4708671 does not significantly inhibit the activity of the closely related S6K2 isoform or a number of other AGC kinases (Akt1, Akt2, PKA, PKCα, PKCϵ, PRK2, ROCK2, RSK1, RSK2 or SGK1) . PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), while having no effect upon the PMA-induced phosphorylation of substrates of the highly related RSK (p90 ribosomal S6 kinase) and MSK (mitogen- and stress-activated kinase) kinases. PF-4708671 is also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1). PF-4708671 does not affect activity of mTORC1.
Download
Download Datasheet