Date published: 2026-4-2

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CGBP Inhibitors

CGBP inhibitors, also known as cyclic GMP-AMP synthase (cGAS) stimulator inhibitors, are a chemical class of small molecules that specifically target the cyclic GMP-AMP synthase enzyme. Cyclic GMP-AMP synthase is a key component of the innate immune system, playing a crucial role in detecting cytosolic DNA, which can indicate the presence of pathogens or cellular damage. Upon activation, cGAS catalyzes the production of cyclic GMP-AMP (cGAMP), a second messenger molecule that initiates a downstream signaling cascade leading to the activation of interferon and other proinflammatory cytokines. CGBP inhibitors are designed to modulate the cGAS pathway by blocking its enzymatic activity, thereby preventing the production of cGAMP and subsequent immune responses. These inhibitors are often small molecules that can penetrate cells and effectively interact with the cGAS active site, competitively inhibiting its function. By controlling the cGAS pathway, CGBP inhibitors have the potential to impact various immune-related processes, such as inflammation and immune responses to infections or cellular stress. Their mechanism of action provides a means to understand and manipulate the innate immune system's response to DNA damage or pathogens. As our understanding of the cGAS pathway continues to evolve, CGBP inhibitors may hold promise as valuable tools for basic research and potential future applications in the context of immunomodulation.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Cilostazol

73963-72-1sc-201182
sc-201182A
10 mg
50 mg
$109.00
$322.00
3
(1)

Originally developed as a vasodilator and antiplatelet agent for peripheral vascular disease, cilostazol was found to inhibit cGMP phosphodiesterase, leading to increased levels of cGMP and subsequent vasodilation.

Tadalafil

171596-29-5sc-208412
50 mg
$180.00
13
(2)

Tadalafil is a phosphodiesterase 5 inhibitor

Vardenafil

224785-90-4sc-362054
sc-362054A
sc-362054B
100 mg
1 g
50 g
$526.00
$735.00
$16653.00
7
(1)

Vardenafil is a selective inhibitor of cGMP-specific phosphodiesterase type 5 (PDE5)

Riociguat

625115-55-1sc-476845
5 mg
$300.00
(0)

Unlike other PDE5 inhibitors, riociguat is a soluble guanylate cyclase (sGC) stimulator. It enhances the synthesis of cGMP by binding to sGC and has been investigated for pulmonary hypertension and chronic thromboembolic pulmonary hypertension (CTEPH).

BAY 73-6691

794568-92-6sc-252407
5 mg
$247.00
2
(0)

A potent and selective inhibitor of PDE9A, similar to PF-00489791, and also explored for its potential in neurodegenerative diseases.