125313-65-7 Usage
Description
RO-31-7549 is a cell-permeable, reversible, and selective protein kinase C (PKC) inhibitor. It acts at the ATP binding site of PKC and exhibits a certain degree of PKC isozyme specificity. With an IC50 of 158 nM for rat brain PKC, it does not inhibit tyrosine phosphorylation or the activation of phospholipase Cγ1. RO-31-7549 is effective in inhibiting carbachol-evoked noradrenaline release, with an IC50 of 600 nM.
Uses
Used in Pharmaceutical Research:
RO-31-7549 is used as a potent inhibitor of protein kinase C (PKC) activity for various research applications. Its specificity and cell permeability make it a valuable tool in studying the role of PKC in cellular processes and the development of potential therapeutic strategies.
Used in Cellular Signaling Studies:
RO-31-7549 is used as a research tool to investigate the role of PKC in cellular signaling pathways. Its ability to selectively inhibit different PKC isozymes allows researchers to explore the specific functions and interactions of these enzymes in various cellular processes.
Used in Neurochemical Research:
RO-31-7549 is used as an inhibitor to study the release of neurotransmitters, such as noradrenaline, in response to carbachol stimulation. This helps researchers understand the underlying mechanisms of neurotransmitter release and the role of PKC in these processes.
Used in Drug Development:
RO-31-7549 is used as a lead compound in the development of new drugs targeting PKC-related diseases. Its potent inhibitory activity and selectivity make it a promising candidate for the development of therapeutic agents for conditions where PKC plays a significant role, such as cancer, inflammation, and neurodegenerative diseases.
Used in Toxicology and Safety Assessment:
RO-31-7549 is used as a tool in toxicology and safety assessment to evaluate the potential effects of PKC inhibition on various physiological processes. This helps in understanding the safety profile of PKC inhibitors and their potential side effects in clinical applications.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 125313-65-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,2,5,3,1 and 3 respectively; the second part has 2 digits, 6 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 125313-65:
(8*1)+(7*2)+(6*5)+(5*3)+(4*1)+(3*3)+(2*6)+(1*5)=97
97 % 10 = 7
So 125313-65-7 is a valid CAS Registry Number.
InChI:InChI=1/C24H22N4O2/c1-27-13-17(15-7-2-4-9-19(15)27)21-22(24(30)26-23(21)29)18-14-28(12-6-11-25)20-10-5-3-8-16(18)20/h2-5,7-10,13-14H,6,11-12,25H2,1H3,(H,26,29,30)
125313-65-7Relevant articles and documents
Methods and materials for identifying agents which modulate bone remodeling and agents identified thereby
-
, (2008/06/13)
The invention discloses compositions, compounds, apparatuses and methods of using them to study bone mineralization and identify agents that regulate bone mineralization. Methods of using bone mineralization gene profiles and signatures for compound screening and research are also disclosed. Reagents for modulating bone mineralization are provided for both therapeutic and research usage.
Inhibitors of Protein Kinase C. 2. Substituted Bisindolylmaleimides with Improved Potency and Selectivity
Davis, Peter D.,Elliot, Lucy H.,Harris, William,Hill, Christopher H.,Hurst, Steven A.,et al.
, p. 994 - 1001 (2007/10/02)
A hypothetical mode of inhibition of protein kinase C (PKC) by the natural product staurosporine has been used as a basis for the design of substituted bisindolylmaleimides with improved potency over the parent compound.Structure-activity relationships were consistent with the interaction of a cationic group in the inhibitor with a carboxylate group in the enzyme, and the most potent compound had a Ki of 3 nM.The inhibitors were competitive with ATP but inhibited cAMP-dependent protein kinase (PKA) only at much higher concentrations despite the extensive sequence homology between ATP-binding regions of PKA and PKC.There compounds were evaluated further and found to inhibit a human allogeneic mixed lymphocyte reaction pointing to the potential utility of PKC inhibitors in immunosuppressive therapy.One of these compounds was orally absorbed in the rat and represents an attractive lead in the development of PKC inhibitors as drugs.
