CDK9-IN-1

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 10mM/1mL
ArtNr HY-13231-10mM
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS No.
1415559-43-1
Purity
>98%
MW
499541
Formula
C26H21N5O4S
Solubility
10 mM in DMSO
Biological Description
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection.
IC50 value:
Target: CDK9; anti HIV
Among CDKs, CDK9 is a validated pathological target in HIV infection, inflammation and cardiac hypertrophy; however selective CDK9 inhibitors are still not available. We present a selective inhibitor family of CDK9 based on the 4-phenylamino-6- phenylpyrimidine nucleus. We show a convenient synthetic method to prepare a useful intermediate and its derivatisation resulting in novel compounds. The CDK9 inhibitory activity of the derivatives was measured in specific kinase assay and the CDK inhibitory profile of the best ones (IC50 > 100nM) was determined. The most selective compounds had high selectivity over CDK1, 2, 3, 5, 6, 7 and showed at least one order of magnitude higher inhibitory activity over CDK4 inhibition. The most selective molecules were examined in cytotoxicity assays and their ability to inhibit HIV-1 replication was determined in cellular assays.

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Menge: 10mM/1mL
Lieferbar: In stock
Listenpreis: 155,00 €
Preis: 155,00 €
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