138489-18-6 Usage
Description
RO-31-8220, also known as Ro 31-8220 mesylate, is a bisindolylmaleimide derivative of staurosporine. It is a potent protein kinase C (PKC) inhibitor, effectively blocking the activity of various PKC isoforms such as PKCα, PKCβI, PKCβII, PKCγ, and PKCε. Additionally, it inhibits other kinases like MAPKAP-K1b, MSK1, S6K1, and GSK3β. RO-31-8220 also has immunosuppressive properties and is known to block MAP kinase phosphatase-1 (MKP-1) expression, induce c-Jun expression, and stimulate Jun N-terminal Kinase (JNK1).
Uses
Used in Pharmaceutical Industry:
RO-31-8220 is used as a PKC inhibitor for its ability to inhibit various PKC isoforms, which play a role in cellular signaling and are involved in several diseases. Its inhibition of these kinases makes it a potential candidate for the development of therapeutic agents targeting conditions related to PKC dysregulation.
Used in Research Applications:
In the field of research, RO-31-8220 is used as a tool compound to study the role of PKC and other kinases in cellular processes. Its potent inhibition of these targets allows researchers to investigate the effects of modulating their activity on various cellular pathways and functions.
Used in Immunosuppressive Therapy:
Due to its immunosuppressive properties, RO-31-8220 can be used in the development of therapies aimed at suppressing the immune system, which may be beneficial in treating autoimmune diseases or preventing transplant rejection.
Used in Cancer Research and Treatment:
RO-31-8220's ability to inhibit PKC and other kinases involved in cellular signaling pathways makes it a potential candidate for cancer research and treatment. Its effects on JNK1 and MKP-1 expression may also contribute to its potential use in targeting cancer cells and understanding the underlying mechanisms of tumor growth and progression.
Biochem/physiol Actions
Inhibitor of GRK-5 (G protein-coupled receptor kinase); PKC (protein kinase C); MAPKAP kinase 1β and p70 S6 kinase.
Check Digit Verification of cas no
The CAS Registry Mumber 138489-18-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,8,4,8 and 9 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 138489-18:
(8*1)+(7*3)+(6*8)+(5*4)+(4*8)+(3*9)+(2*1)+(1*8)=166
166 % 10 = 6
So 138489-18-6 is a valid CAS Registry Number.
138489-18-6Relevant articles and documents
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.
