Date published: 2026-3-17

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TLE1 Inhibitors

TLE1 inhibitors are a class of chemical compounds specifically designed to target and inhibit the function of Transducin-Like Enhancer of Split 1 (TLE1), a transcriptional corepressor that plays a significant role in regulating gene expression during various developmental processes and cellular differentiation. TLE1 is a member of the Groucho/TLE family of proteins, which are known for their ability to interact with DNA-bound transcription factors and repress the transcription of target genes. This repression is typically achieved through the recruitment of histone deacetylases (HDACs) and other chromatin remodeling factors, leading to the condensation of chromatin and the subsequent inhibition of gene transcription. TLE1 is involved in numerous signaling pathways, including Wnt, Notch, and Hedgehog, which are critical for embryonic development, cell fate determination, and tissue homeostasis. By inhibiting TLE1, researchers can disrupt these repressive activities, providing a tool to study the specific contributions of TLE1 to gene regulation and cellular function.

In research, TLE1 inhibitors are valuable tools for exploring the mechanisms by which TLE1 mediates transcriptional repression and how this regulation influences developmental processes and cellular differentiation. By blocking TLE1 activity, scientists can investigate the downstream effects on gene expression profiles, particularly focusing on how the loss of TLE1-mediated repression affects the activation of specific genes and the resulting cellular outcomes. This inhibition allows researchers to study the role of TLE1 in various signaling pathways and its interactions with other transcriptional regulators, providing insights into the complex networks of protein-protein interactions that govern gene expression and cellular identity. Additionally, TLE1 inhibitors can be used to examine the broader implications of transcriptional repression in maintaining tissue homeostasis and preventing aberrant gene expression. Through these studies, the use of TLE1 inhibitors enhances our understanding of the molecular mechanisms underlying transcriptional regulation, the role of corepressors in gene expression, and the broader impact of these processes on cellular development and function.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

XAV939

284028-89-3sc-296704
sc-296704A
sc-296704B
1 mg
5 mg
50 mg
$36.00
$117.00
$525.00
26
(1)

XAV939 is a tankyrase inhibitor that indirectly modulates TLE1 by stabilizing Axin1. By inhibiting tankyrase, XAV939 prevents Axin1 degradation, enhancing the destruction complex's activity and reducing TLE1 association with β-catenin. This indirect modulation can impact Wnt signaling and potentially affect TLE1 expression or function.

DAPT

208255-80-5sc-201315
sc-201315A
sc-201315B
sc-201315C
5 mg
25 mg
100 mg
1 g
$40.00
$120.00
$480.00
$2141.00
47
(3)

GSI-IX (DAPT) is a gamma-secretase inhibitor that directly modulates TLE1 by inhibiting Notch signaling. By blocking gamma-secretase activity, GSI-IX prevents the cleavage of Notch, reducing the release of the Notch intracellular domain (NICD). This inhibits Notch-mediated transcriptional activation and can influence TLE1 expression or function.

β-Catenin/Tcf Inhibitor, FH535

108409-83-2sc-221398
sc-221398A
10 mg
50 mg
$182.00
$374.00
7
(1)

FH535 is a dual inhibitor that indirectly modulates TLE1 by targeting the Wnt/β-catenin and PPARγ signaling pathways. By inhibiting β-catenin and PPARγ, FH535 can disrupt TLE1's association with β-catenin and alter its transcriptional activity. This dual impact provides an alternative approach to influence TLE1 expression or function by modulating multiple signaling pathways simultaneously.

KY02111

1118807-13-8sc-397043
sc-397043A
5 mg
25 mg
$79.00
$336.00
(0)

KY02111 is a Wnt/β-catenin signaling inhibitor that directly modulates TLE1 by disrupting the interaction between β-catenin and TLE1. By inhibiting Wnt/β-catenin signaling, KY02111 prevents the nuclear translocation of β-catenin and reduces its association with TLE1. This direct modulation can impact TLE1's transcriptional activity and expression by disrupting its interaction with β-catenin in the nucleus.

PRI-724

1422253-38-0sc-507535
25 mg
$260.00
(0)

PRI-724 is a CBP/β-catenin antagonist that indirectly modulates TLE1 by disrupting the interaction between CBP and β-catenin. By inhibiting this interaction, PRI-724 interferes with β-catenin-mediated transcription, potentially affecting TLE1 expression or function. This indirect modulation provides an avenue to influence TLE1 through specific disruption of the CBP/β-catenin complex.

Wnt-C59

1243243-89-1sc-475634
sc-475634A
sc-475634B
5 mg
10 mg
50 mg
$214.00
$326.00
$1275.00
1
(0)

C59 is a tankyrase inhibitor that indirectly modulates TLE1 by stabilizing Axin1. By inhibiting tankyrase, C59 prevents Axin1 degradation, enhancing the destruction complex's activity and reducing TLE1 association with β-catenin. This indirect modulation can impact Wnt signaling and potentially affect TLE1 expression or function.