821794-92-7 Usage
Description
1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone, also known as FMK, is a potent and irreversible RSK1/2 inhibitor with an IC50 of 15 nM. It inactivates the C-terminal auto-kinase domain activity and suppresses RSK2 kinase activity in RSK2-expressing HNSCC cell lines. FMK reduces HNSCC cell invasive ability and displays no effect on EGF-stimulated phosphorylation of ERK1 or ERK2.
Uses
Used in Cancer Research:
FMK is used as a research tool for studying the role of RSK1/2 in cancer progression, particularly in head and neck squamous cell carcinoma (HNSCC). Its ability to suppress RSK2 kinase activity and reduce HNSCC cell invasive ability makes it a valuable compound for investigating the underlying mechanisms of cancer development and progression.
Used in Drug Development:
FMK is used as a starting point for the development of potential therapeutic agents targeting RSK1/2 in cancer treatment. Its potent inhibitory activity and selectivity for RSK1/2 make it a promising candidate for further optimization and evaluation in preclinical and clinical studies.
Used in Drug Screening:
FMK is used as a reference compound in high-throughput screening assays to identify novel RSK1/2 inhibitors with potential therapeutic applications in cancer treatment. Its well-defined inhibitory profile and selectivity for RSK1/2 enable the development of robust screening assays to discover new and more effective cancer therapeutics.
Used in Molecular Biology:
FMK is used as a molecular probe to study the regulation of RSK1/2 activity and its downstream signaling pathways in various cellular processes. Its ability to irreversibly inhibit RSK1/2 allows researchers to investigate the specific roles of these kinases in cellular signaling and their potential as therapeutic targets in cancer and other diseases.
Check Digit Verification of cas no
The CAS Registry Mumber 821794-92-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,2,1,7,9 and 4 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 821794-92:
(8*8)+(7*2)+(6*1)+(5*7)+(4*9)+(3*4)+(2*9)+(1*2)=187
187 % 10 = 7
So 821794-92-7 is a valid CAS Registry Number.
InChI:InChI=1/C18H19FN4O2/c1-11-3-5-12(6-4-11)14-15-17(20)21-10-22-18(15)23(7-2-8-24)16(14)13(25)9-19/h3-6,10,24H,2,7-9H2,1H3,(H2,20,21,22)
821794-92-7Relevant articles and documents
SELECTIVE SERINE/THREONINE KINASE INHIBITORS
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Page/Page column 33, (2008/06/13)
Inhibition of protein kinases having one or more cysteine residues within the ATP binding site is effected by contacting the kinase, per se or in a cell or subject, with an inhibitory-effective amount of a compound having a heterocyclic core structure comprised of two or more fused rings containing at least one nitrogen ring atom, and an electrophilic substituent that is capable of reacting with a cysteine residue within the ATP binding site of a kinase. Preferred compounds include certain pyrrolopyrimidines and oxindoles having such an electrophilic substituent and optionally an aromatic or heteroaromatic substituent that is capable of interacting with a threonine or smaller residue located in the gatekeeper position of the kinase. Kinases lacking such cysteine residues may be engineered or modified so that they are capable of being inhibited by such compounds by replacing a valine or other amino acid residue within the ATP binding site by a cysteine residue.
