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.
PHA-767491
Cat No.
CEI-0286
Description
PHA-767491
CAS No.
845714-00-3
Molecular Weight
213.24
Purity
>99%
Storage
2 years at -20 centigrade
Targets
Cdc7
Molecular Formula
C12H11N3O
Solubility
No
In vitro
PHA-767491 is a potent Cdc7 inhibitor. PHA-767491 is the first molecule that directly affects the mechanisms controlling initiation as opposed to elongation in DNA replication. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. PHA-767491 prevents the activation of replication origins but does not impede replication fork progression, and it does not trigger a sustained DNA damage response. PHA-767491 induced apoptosis in all CLL samples tested with an average EC50 of 0.6 uM. PHA-767491 activates the intrinsic apoptotic pathway in resting CLL cells. Exposure of CLL cells to 1 uM PHA-767491 induced Bax activation occurs upstream of caspase activation. PHA-767491 induces downregulation of Mcl-1 protein in a caspase-independent manner. And DNA synthesis and Cdc7 activity of IL-4 and CD154-stimulated CLL cells can be inhibited by PHA-767491.
Download
Download Datasheet