Date published: 2025-12-7

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Cdk9 Inhibitors

Cyclin-dependent kinase 9 (Cdk9) is an integral enzyme in the family of cyclin-dependent kinases (Cdks), which are paramount for the regulation of the cell cycle and transcriptional elongation processes. Cdk9, in association with its cyclin partners (typically cyclin T1), constitutes a critical component of the positive transcription elongation factor b (P-TEFb). The primary role of P-TEFb is to facilitate the transition of RNA polymerase II (RNAPII) from initiation to elongation during transcription, primarily by phosphorylating the carboxy-terminal domain (CTD) of RNAPII. Given its vital role in transcriptional regulation, Cdk9 is a focus of interest in biochemical and molecular biology studies. Inhibitors targeting Cdk9 are chemicals that suppress the kinase activity of Cdk9, effectively hindering its ability to phosphorylate its substrates. These inhibitors can exhibit varied modes of action, including competitive and non-competitive inhibition. They might target the ATP-binding pocket of the kinase, preventing ATP from accessing the site, or they could bind to allosteric regions of the enzyme, inducing conformational alterations that diminish Cdk9's activity. The structural diversity of Cdk9 inhibitors spans from small synthetic molecules to intricate natural compounds.

Items 1 to 10 of 17 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Flavopiridol

146426-40-6sc-202157
sc-202157A
5 mg
25 mg
$78.00
$254.00
41
(3)

Flavopiridol acts as a potent inhibitor of Cdk9, exhibiting a unique mechanism of action through its ability to disrupt ATP binding. This compound forms specific hydrogen bonds and hydrophobic interactions with the kinase domain, leading to a conformational change that impairs enzyme activity. Its influence on transcriptional regulation is notable, as it modulates the phosphorylation of RNA polymerase II, thereby affecting gene expression dynamics and cellular processes.

Cdk9 Inhibitor II

140651-18-9sc-203326
5 mg
$172.00
1
(1)

Cdk9 Inhibitor II selectively targets the Cdk9 kinase, engaging in unique molecular interactions that stabilize the inactive conformation of the enzyme. By binding to the ATP pocket, it alters the enzyme's dynamics, effectively reducing its catalytic efficiency. This compound also influences downstream signaling pathways by modulating the phosphorylation state of key substrates, thereby impacting cellular proliferation and transcriptional control mechanisms. Its specificity for Cdk9 highlights its role in regulating cell cycle progression.

Flavopiridol Hydrochloride

131740-09-5sc-207687
10 mg
$311.00
(2)

Flavopiridol is a potent inhibitor of CDKs, including Cdk9. It binds to the ATP-binding pocket, thus preventing kinase activity and the phosphorylation of RNA polymerase II by Cdk9.

Purvalanol B

212844-54-7sc-361300
sc-361300A
10 mg
50 mg
$199.00
$846.00
(1)

Purvalanol B acts as a selective inhibitor of Cdk9, exhibiting a unique binding affinity that disrupts the enzyme's ATP-binding site. This interaction leads to a conformational shift, diminishing the kinase's activity and altering its interaction with cyclins. The compound's kinetic profile reveals a competitive inhibition mechanism, which effectively modulates the phosphorylation of target proteins, influencing transcriptional regulation and cellular signaling pathways. Its distinct selectivity underscores its potential in fine-tuning cellular processes.

DRB

53-85-0sc-200581
sc-200581A
sc-200581B
sc-200581C
10 mg
50 mg
100 mg
250 mg
$42.00
$185.00
$310.00
$650.00
6
(1)

DRB is a potent inhibitor of Cdk9, characterized by its ability to interfere with the enzyme's phosphorylation activity. It binds to the enzyme in a manner that stabilizes an inactive conformation, thereby preventing substrate access. This compound exhibits a unique interaction with the RNA polymerase II complex, impacting transcription elongation. Its kinetic behavior suggests a non-competitive inhibition, effectively altering the dynamics of gene expression and cellular response mechanisms.

PHA 767491 hydrochloride

942425-68-5sc-204187
sc-204187A
10 mg
50 mg
$194.00
$786.00
3
(2)

PHA 767491 hydrochloride is a selective inhibitor of Cdk9, demonstrating a unique binding affinity that disrupts the enzyme's catalytic cycle. It engages in specific interactions with the ATP-binding site, leading to a conformational shift that hinders substrate phosphorylation. This compound also influences the recruitment of transcription factors, modulating the transcriptional landscape. Its kinetic profile indicates a mixed inhibition pattern, affecting cellular signaling pathways and transcriptional regulation.

SNS-032

345627-80-7sc-364621
sc-364621A
5 mg
10 mg
$169.00
$262.00
(1)

SNS-032 is another CDK inhibitor with selectivity for Cdk9. It can inhibit transcription elongation by blocking Cdk9 activity.

AZD 5438

602306-29-6sc-361115
sc-361115A
10 mg
50 mg
$205.00
$865.00
(0)

AZD 5438 is a potent inhibitor of Cdk9, characterized by its ability to selectively target the enzyme's active site. It forms stable interactions with key residues, altering the enzyme's conformation and impeding its kinase activity. This compound exhibits a unique kinetic behavior, displaying competitive inhibition that affects the phosphorylation of RNA polymerase II. Additionally, AZD 5438 can modulate downstream signaling cascades, impacting gene expression dynamics.

Cdc7/Cdk9 Inhibitor

845714-00-3sc-311303
5 mg
$270.00
1
(1)

Cdc7/Cdk9 Inhibitor is a selective modulator of Cdk9, known for its unique ability to disrupt the enzyme's phosphorylation cascade. By binding to specific allosteric sites, it induces conformational changes that hinder substrate access. This inhibitor demonstrates a distinct kinetic profile, exhibiting non-competitive inhibition that influences transcriptional regulation. Its interactions with protein complexes can also alter chromatin dynamics, affecting cellular processes at a molecular level.

CR8, (R)-Isomer

294646-77-8sc-311306
5 mg
$174.00
(0)

CR8, (R)-Isomer, acts as a potent Cdk9 inhibitor, characterized by its ability to selectively engage with the enzyme's active site. This interaction stabilizes a unique conformation that prevents ATP binding, effectively halting kinase activity. The compound exhibits a remarkable affinity for Cdk9, leading to altered phosphorylation patterns in target proteins. Additionally, CR8 influences downstream signaling pathways, contributing to changes in gene expression and cellular response mechanisms.