CDK9-IN-1

• CAT Number: I001585
• CAS Number: 1415559-43-1
• Molecular Formula: C26H21N5O4S
• Molecular Weight: 499.54
• Purity: ≥95%
• Synonyms: N-[5-[[6-[3-(1,3-dioxoisoindol-2-yl)phenyl]pyrimidin-4-yl]amino]-2-methylphenyl]methanesulfonamide
• Target: Cyclin-Dependent Kinases
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C
• InChI: InChI=1S/C26H21N5O4S/c1-16-10-11-18(13-22(16)30-36(2,34)35)29-24-14-23(27-15-28-24)17-6-5-7-19(12-17)31-25(32)20-8-3-4-9-21(20)26(31)33/h3-15,30H,1-2H3,(H,27,28,29)
• InChIKey: CKUFOBCNTCLXJP-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=C1)NC2=NC=NC(=C2)C3=CC(=CC=C3)N4C(=O)C5=CC=CC=C5C4=O)NS(=O)(=O)C

CDK9-IN-1（Cat No.:I001585）is a selective and potent inhibitor of cyclin-dependent kinase 9 (CDK9), a key regulator of transcription and RNA polymerase II-mediated gene expression. By inhibiting CDK9, this compound disrupts transcriptional elongation, leading to reduced expression of anti-apoptotic proteins and promoting apoptosis in cancer cells. CDK9-IN-1 is an important tool for studying transcriptional regulation and exploring its therapeutic potential in oncology, particularly in targeting cancers with dysregulated transcriptional programs. Its selectivity and efficacy make it a valuable asset in cancer research and drug discovery.

Reference

[1]. Németh G, Varga Z, Greff Z, Bencze G, Sipos A, Szántai-Kis C, Baska F, Gyuris A, Kelemenics K, Szathmáry Z, Minárovits J, Kéri G, Orfi L.Novel, selective CDK9 inhibitors for the treatment of HIV infection.Curr Med Chem. 2011;18(3):342-58.

Abstract
Cyclin Dependent Kinases (CDKs) are important regulators of cell cycle and gene expression. Since an up-to-date review about the pharmacological inhibitors of CDK family (CDK1-10) is not available; therefore in the present paper we briefly summarize the most relevant inhibitors and point out the low number of selective inhibitors. 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 (IC(50)