Date published: 2025-12-6

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GLI-1 Activators

The chemical class known as GLI-1 activators comprises compounds that modulate the activity of GLI-1, a key transcription factor in the Hedgehog signaling pathway. These activators can directly impact GLI-1 or indirectly influence its transcriptional activity by targeting various signaling pathways and cellular processes. SAG (Smoothened Agonist) directly activates GLI-1 by binding to Smoothened, bypassing upstream negative regulators and promoting GLI-1 transcriptional activity within the Hedgehog pathway. In contrast, GANT61, TAK-441, and LDE225 indirectly activate GLI-1 by inhibiting negative regulatory mechanisms, preventing its processing and activation.

Arsenic Trioxide, Curcumin, Forskolin, 20α-Hydroxy Cholesterol, Vitamin D3, and All-trans Retinoic Acid indirectly activate GLI-1 by influencing the Hedgehog signaling pathway components. They impact the expression or function of negative regulators, promoting GLI-1 transcriptional activity and modulating cellular processes such as tissue development and regeneration. Verteporfin and Arsenic Trisulfide indirectly activate GLI-1 by targeting cross-talk with other signaling pathways. Verteporfin inhibits YAP/TAZ, preventing their negative regulation of GLI-1, while Arsenic Trisulfide influences negative regulators within the Hedgehog pathway.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

GANT61

500579-04-4sc-202630
sc-202630A
sc-202630B
1 mg
5 mg
10 mg
$63.00
$128.00
$200.00
6
(1)

GANT61 is a small molecule inhibitor of GLI-1 processing and transcriptional activity. By blocking the function of GLI-1, GANT61 indirectly activates GLI-1 by preventing its negative regulatory mechanisms. This indirect activation contributes to the modulation of the Hedgehog signaling pathway and the regulation of downstream target genes involved in cell differentiation and proliferation.

Forskolin

66575-29-9sc-3562
sc-3562A
sc-3562B
sc-3562C
sc-3562D
5 mg
50 mg
1 g
2 g
5 g
$76.00
$150.00
$725.00
$1385.00
$2050.00
73
(3)

Forskolin indirectly activates GLI-1 by modulating cAMP levels. Elevated cAMP levels activate protein kinase A (PKA), which, in turn, inhibits GSK-3β, leading to the stabilization and activation of GLI-1. This indirect activation influences the Hedgehog signaling pathway, impacting cell proliferation and differentiation processes regulated by GLI-1.

Verteporfin

129497-78-5sc-475698
sc-475698A
10 mg
100 mg
$347.00
$2710.00
5
(0)

Verteporfin is a small molecule inhibitor of YAP/TAZ, indirectly activating GLI-1 by preventing YAP/TAZ-mediated GLI-1 inhibition. This indirect activation influences the cross-talk between Hedgehog and Hippo signaling pathways, modulating cellular processes such as proliferation and stem cell maintenance.

SAG

912545-86-9sc-212905
sc-212905A
1 mg
5 mg
$163.00
$413.00
27
(1)

SAG is a Smoothened agonist that directly activates the Hedgehog signaling pathway, leading to the activation of GLI-1. By binding to Smoothened, SAG bypasses upstream negative regulators and promotes GLI-1 transcriptional activity. This direct activation influences Hedgehog signaling-mediated cellular processes, including embryonic development and tissue homeostasis.

20α-Hydroxy Cholesterol

516-72-3sc-209393
10 mg
$300.00
(0)

20α-Hydroxy Cholesterol indirectly activates GLI-1 by inhibiting Hedgehog signaling pathway negative regulators. This compound influences the modulation of GLI-1 transcriptional activity, contributing to Hedgehog pathway-mediated cellular processes such as tissue development and regeneration.

Cholecalciferol

67-97-0sc-205630
sc-205630A
sc-205630B
1 g
5 g
10 g
$70.00
$160.00
$290.00
2
(1)

Vitamin D3 indirectly activates GLI-1 by modulating Hedgehog pathway components. It impacts the expression of Hedgehog signaling regulators, promoting GLI-1 transcriptional activity. This indirect activation influences Hedgehog pathway-mediated cellular processes, including tissue development and maintenance.

Retinoic Acid, all trans

302-79-4sc-200898
sc-200898A
sc-200898B
sc-200898C
500 mg
5 g
10 g
100 g
$65.00
$319.00
$575.00
$998.00
28
(1)

All-trans Retinoic Acid (ATO) indirectly activates GLI-1 by influencing Hedgehog pathway components. ATO has been shown to modulate the expression of Hedgehog signaling regulators, leading to increased GLI-1 transcriptional activity. This indirect activation impacts cellular processes such as embryonic development and tissue homeostasis.

Erismodegib

956697-53-3sc-396280
sc-396280A
10 mg
100 mg
$255.00
$918.00
(0)

LDE225 is a small molecule inhibitor of Smoothened, indirectly activating GLI-1 by preventing Smoothened-mediated inhibition. This indirect activation contributes to the modulation of the Hedgehog signaling pathway, influencing cellular processes such as cell proliferation and differentiation regulated by GLI-1.