Date published: 2026-1-28

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Cdk8 Inhibitors

Cdk8 inhibitors belong to a specific chemical class of compounds meticulously designed to modulate the activity of the cyclin-dependent kinase 8 (Cdk8) protein. Cdk8 is a member of the cyclin-dependent kinase family that functions as a transcriptional regulator by phosphorylating transcription factors and co-regulators. These inhibitors are thoughtfully crafted molecules engineered to interact with the Cdk8 protein, influencing its normal function. Through these interactions, they might impact various cellular processes associated with transcriptional regulation, gene expression, and cellular responses, without directly altering its catalytic domains or its involvement in transcriptional complexes. The design of Cdk8 inhibitors is grounded in a comprehensive understanding of the structural and functional attributes of the Cdk8 protein. Typically developed using advanced chemical synthesis methods and informed by insights from molecular biology and transcriptional control mechanisms, these inhibitors are characterized by their ability to selectively bind to Cdk8. This selectivity enables focused modulation of cellular pathways that rely on the activity of this specific protein. Unraveling the intricacies of gene expression, transcriptional control, and cellular responses often employ Cdk8 inhibitors as valuable tools. The development and utilization of Cdk8 inhibitors contribute to advancing our knowledge of the complex interplay between cellular components and transcriptional dynamics, offering insights into the fundamental molecular mechanisms that govern gene regulation and contribute to cellular responses to changes in transcriptional programs.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Flavopiridol

146426-40-6sc-202157
sc-202157A
5 mg
25 mg
$78.00
$259.00
41
(3)

Flavopiridol functions as a selective inhibitor of Cdk8, exhibiting unique binding characteristics through a combination of hydrophobic and electrostatic interactions. Its structural conformation allows for effective competition with ATP, thereby modulating kinase activity. This compound influences transcriptional regulation by altering the phosphorylation state of target proteins, impacting downstream signaling pathways. Additionally, its kinetic profile reveals a distinct mechanism of action that can fine-tune cellular responses.

DRB

53-85-0sc-200581
sc-200581A
sc-200581B
sc-200581C
10 mg
50 mg
100 mg
250 mg
$43.00
$189.00
$316.00
$663.00
6
(1)

DRB acts as a potent inhibitor of Cdk8, characterized by its ability to disrupt the kinase's interaction with cyclin partners. This compound selectively alters the phosphorylation dynamics of transcription factors, leading to significant changes in gene expression. Its unique binding affinity is attributed to specific hydrogen bonding and hydrophobic interactions, which stabilize the inhibitor-kinase complex. Furthermore, DRB's influence on transcriptional elongation highlights its role in modulating RNA polymerase II activity, showcasing its impact on cellular transcriptional landscapes.

H-8 • 2HCL

113276-94-1sc-200526
sc-200526A
10 mg
50 mg
$60.00
$250.00
3
(0)

H-8 • 2HCl serves as a selective inhibitor of Cdk8, effectively modulating its kinase activity through unique molecular interactions. This compound engages in specific electrostatic and van der Waals forces, enhancing its binding affinity to the enzyme. By altering the phosphorylation state of target proteins, it influences critical signaling pathways. Additionally, H-8 • 2HCl's role in regulating transcriptional machinery underscores its potential to reshape cellular responses to various stimuli.

Roscovitine

186692-46-6sc-24002
sc-24002A
1 mg
5 mg
$94.00
$265.00
42
(2)

Roscovitine is a broad-spectrum CDK inhibitor that targets CDK8, among others, and blocks cell cycle progression by inhibiting CDK-mediated phosphorylation of cell cycle proteins.

THZ1

1604810-83-4sc-507542
1 mg
$95.00
(0)

THZ1 is a covalent CDK7/CDK12/CDK13 inhibitor that indirectly impacts CDK8 by inhibiting its transcription-regulating partners CDK7/CDK12/CDK13 in the Mediator complex.

LGK 974

1243244-14-5sc-489380
sc-489380A
5 mg
50 mg
$359.00
$1295.00
2
(0)

LGK 974 is a potent and specific inhibitor of the Wnt/β-catenin pathway by targeting CDK8-mediated phosphorylation of β-catenin, thereby impacting transcriptional activity.

RGB-286638

784210-88-4sc-507523
250 mg
$285.00
(0)

RGB-286638 is a selective CDK8 inhibitor that attenuates Wnt/β-catenin signaling by inhibiting CDK8-mediated phosphorylation of β-catenin, thereby modulating transcriptional output.