Date published: 2025-12-13

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Pygopus 1 Activators

Pygopus 1 activators encompass a diverse array of chemical compounds that specifically enhance the functional activity of Pygopus 1, a co-activator involved in the Wnt signaling pathway crucial for cell proliferation, differentiation, and migration. These molecules are fine-tuned to modulate the pathway by ensuring that Pygopus 1 can effectively interact with its nuclear partners, such as the TCF/LEF family of transcription factors, to induce the transcription of Wnt-responsive genes. For example, certain small molecule stabilizers directly amplify Pygopus 1's ability to maintain its necessary conformation for protein-protein interactions. This enhancement is critical because Pygopus 1 does not bind DNA directly but influences transcription through its role as a transcriptional co-activator. By strengthening this interaction, these activators ensure that the transcriptional machinery is more robustly assembled, leading to an upregulation of target gene expression integral to Wnt signaling.

Additionally, some activators work by shielding Pygopus 1 from negative regulatory influences, thereby preserving its functional state within the nucleus. This might involve the inhibition of enzymes that would otherwise modify Pygopus 1 in a manner that reduces its co-activator efficacy. By preventing such modifications, these activators maintain Pygopus 1 in an active form conducive to the propagation of Wnt signaling. The exact mechanisms of these chemicals can vary widely; some may increase the local concentration of Pygopus 1 within the nucleus, while others could enhance its stability, or influence the cellular localization of its antagonists. Collectively, these Pygopus 1 activators contribute to the precise regulation of gene expression patterns that are essential for the proper functioning of the Wnt pathway, thereby ensuring that cellular outcomes such as growth and development proceed correctly.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Lithium

7439-93-2sc-252954
50 g
$214.00
(0)

Lithium Chloride acts as a GSK-3 inhibitor. By inhibiting GSK-3, Wnt/β-catenin signaling is enhanced. Pygopus 1, being a co-activator in the Wnt signaling pathway, has increased functional activity due to the stabilization of β-catenin and the subsequent nuclear accumulation which forms a complex with TCF/LEF transcription factors where Pygopus 1 is essential.

GSK-3 Inhibitor IX

667463-62-9sc-202634
sc-202634A
sc-202634B
1 mg
10 mg
50 mg
$57.00
$184.00
$867.00
10
(1)

BIO is a specific inhibitor of GSK-3. It mimics Wnt signaling activation, where GSK-3 inhibition results in the stabilization and accumulation of β-catenin in the nucleus. This stabilization allows β-catenin to form a transcriptional complex with TCF/LEF and Pygopus 1, enhancing the transcription of Wnt target genes.

Valproic Acid

99-66-1sc-213144
10 g
$85.00
9
(1)

Valproic Acid is a histone deacetylase (HDAC) inhibitor. By inhibiting HDACs, it results in a more relaxed chromatin structure, which facilitates transcription factor access. Pygopus 1, as part of the transcriptional activation complex with β-catenin, benefits from increased chromatin accessibility, thus potentially enhancing its functional role in gene transcription.

SB-216763

280744-09-4sc-200646
sc-200646A
1 mg
5 mg
$70.00
$198.00
18
(1)

SB-216763 is another GSK-3 inhibitor. It enhances the Wnt/β-catenin signaling pathway by preventing β-catenin degradation. The accumulation of β-catenin in the nucleus and its association with TCF/LEF transcription factors is facilitated, which indirectly increases the functional activity of Pygopus 1 in the transcription of Wnt-responsive genes.

GSK-3 Inhibitor XVI

252917-06-9sc-221691
sc-221691A
5 mg
25 mg
$153.00
$520.00
4
(1)

CHIR99021 is a potent GSK-3 inhibitor. It leads to the nuclear accumulation of β-catenin by inhibiting GSK-3 mediated phosphorylation. The enhanced level of β-catenin in the nucleus promotes the formation of a transcriptional complex including TCF/LEF and Pygopus 1, which is crucial for the transcriptional activation of Wnt target genes.

Wnt Synergist, QS11

944328-88-5sc-222417
sc-222417A
5 mg
25 mg
$138.00
$595.00
(1)

QS11 is an inhibitor of ARFGAP with SH3 domain, an antagonist of Wnt/β-catenin signaling. By inhibiting this ARFGAP, QS11 can indirectly promote the activity of β-catenin, thus boosting the formation of the transcriptional complex that includes Pygopus 1, enhancing the transcription of Wnt target genes.