496864-16-5 Usage
Description
RP107 is a cell-permeable pyrrolo-pyrazine compound that exerts anti-proliferative effects. It acts as a potent, selective, reversible, and ATP-competitive inhibitor of cyclin-dependent kinases (Cdks), glycogen synthase kinase-3 (GSK-3), and c-Jun N-terminal kinase (JNK). RP107 has shown to arrest cells in both G1 and G2 phases and selectively stimulates CFTR-dependent iodide efflux in certain cell lines. It is a yellow solid.
Uses
Used in Pharmaceutical Industry:
RP107 is used as an inhibitor for cyclin-dependent kinases (Cdks), glycogen synthase kinase-3 (GSK-3), and c-Jun N-terminal kinase (JNK) for its anti-proliferative properties and potential applications in cancer treatment.
Used in Research Applications:
RP107 is used as a research tool to study the effects of inhibiting Cdks, GSK-3, and JNK on cell cycle arrest and other cellular processes. It can be employed in various experimental setups to investigate the roles of these enzymes in different cellular pathways.
Used in Drug Development:
RP107 can be utilized in the development of new drugs targeting cyclin-dependent kinases, glycogen synthase kinase-3, and c-Jun N-terminal kinase, which are involved in various diseases, including cancer and other proliferative disorders.
Used in Cell Biology Studies:
RP107 is used as a compound to induce cell cycle arrest in both G1 and G2 phases, allowing researchers to study the effects of cell cycle inhibition on cellular processes and the potential therapeutic applications of such inhibition.
Used in Cystic Fibrosis Research:
RP107 is used to selectively stimulate CFTR-dependent iodide efflux in certain cell lines, making it a valuable tool for studying the function of the CFTR protein and the development of treatments for cystic fibrosis.
Biochem/physiol Actions
EC50 = 150 nM, 140 nM and 111 nM, in stimulating CFTR-dependent iodide efflux in wtCFTR-CHO, Calu-3 and F508del-CFTR-CF15 cells in the presence of 1 μM Forskolin, respectively
Check Digit Verification of cas no
The CAS Registry Mumber 496864-16-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,9,6,8,6 and 4 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 496864-16:
(8*4)+(7*9)+(6*6)+(5*8)+(4*6)+(3*4)+(2*1)+(1*6)=215
215 % 10 = 5
So 496864-16-5 is a valid CAS Registry Number.
InChI:InChI=1/C16H17N3O/c1-2-3-4-13-14(11-5-7-12(20)8-6-11)19-16-15(13)17-9-10-18-16/h5-10,20H,2-4H2,1H3,(H,18,19)
496864-16-5Relevant articles and documents
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects
Mettey, Yvette,Gompel, Marie,Thomas, Virginie,Garnier, Matthieu,Leost, Maryse,Ceballos-Picot, Irène,Noble, Martin,Endicott, Jane,Vierfond, Jean-Michel,Meijer, Laurent
, p. 222 - 236 (2007/10/03)
Cyclin-dependent kinases (CDKs) regulate the cell cycle, apoptosis, neuronal functions, transcription, and exocytosis. The observation of CDK deregulations in various pathological situations suggests that CDK inhibitors may have a therapeutic value. In th
