Date published: 2025-10-30

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GFR-1 Activators

Chemical activators of the Glial cell line-derived neurotrophic factor receptor 1 (GFR-1) engage in various biochemical pathways to enhance receptor signaling. (S)-3,5-DHPG, a group I metabotropic glutamate receptor agonist, initiates a cascade that can result in increased intracellular calcium levels. This rise in calcium can positively influence the activity of the RET coreceptor that associates with GFR-1, amplifying the signal. Similarly, Mangiferin and IBMX elevate cAMP levels, which leads to the activation of protein kinase A (PKA). PKA, in turn, can phosphorylate RET, resulting in enhanced GFR-1-mediated signaling. Forskolin, like Mangiferin and IBMX, also increases cAMP and subsequently activates PKA, contributing to the phosphorylation and activation of RET. This series of events can amplify GFR-1 signaling.

Other chemicals like Anisomycin and Beta-Lapachone function through different mechanisms but converge on the same pathway. Anisomycin activates the JNK pathway, which can lead to the upregulation of RET phosphorylation and, consequently, GFR-1 activity. Beta-Lapachone operates through modulating cellular redox states and thus can indirectly influence the activity of tyrosine kinases such as RET, promoting GFR-1 signaling. Zinc pyrithione raises intracellular zinc levels, which can enhance kinase activity involved in RET phosphorylation and GFR-1 signaling. Sodium orthovanadate and Cantharidin inhibit protein phosphatases, leading to increased phosphorylation of RET, thereby facilitating GFR-1 activation. Genistein, while primarily known as a tyrosine kinase inhibitor, at certain concentrations can enhance RET phosphorylation and GFR-1 activity. Similarly, Quercetin modulates kinase signaling pathways, which can contribute to increased RET activity and subsequent GFR-1 signaling enhancement.

SEE ALSO...

Items 1 to 10 of 11 total

Display:

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

(S)-3,5-DHPG

162870-29-3sc-204256
sc-204256A
5 mg
10 mg
$206.00
$346.00
2
(1)

(S)-3,5-DHPG selectively activates group I metabotropic glutamate receptors, which could lead to an increase in intracellular calcium levels. Elevated calcium may enhance the activity of RET, the coreceptor associated with GFR-1, thereby potentiating GFR-1 signaling.

Mangiferin

4773-96-0sc-491041
10 mg
$140.00
(0)

Mangiferin increases cAMP levels, which can lead to the activation of PKA. PKA can phosphorylate and activate the RET receptor that complexes with GFR-1, leading to enhanced GFR-1-mediated signaling.

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 raises intracellular cAMP levels, leading to PKA activation. PKA can phosphorylate RET, which is part of the GFR-1 receptor complex, thereby enhancing GFR-1 signaling.

IBMX

28822-58-4sc-201188
sc-201188B
sc-201188A
200 mg
500 mg
1 g
$159.00
$315.00
$598.00
34
(1)

IBMX increases intracellular cAMP by inhibiting phosphodiesterases, which may lead to PKA activation. PKA can then phosphorylate and activate RET that associates with GFR-1, thus augmenting GFR-1 signaling.

Anisomycin

22862-76-6sc-3524
sc-3524A
5 mg
50 mg
$97.00
$254.00
36
(2)

Anisomycin activates the JNK pathway, which is known to interact with RET signaling. Activation of JNK could enhance RET phosphorylation and thus indirectly increase GFR-1 activity.

Sodium Orthovanadate

13721-39-6sc-3540
sc-3540B
sc-3540A
5 g
10 g
50 g
$45.00
$56.00
$183.00
142
(4)

Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases that can increase phosphorylation levels of tyrosine kinases like RET, which when associated with GFR-1, can lead to its activation.

β-Lapachone

4707-32-8sc-200875
sc-200875A
5 mg
25 mg
$110.00
$450.00
8
(1)

Beta-Lapachone activates NQO1, which modulates cellular redox states. Redox changes can activate tyrosine kinases such as RET that are associated with GFR-1, leading to GFR-1 signaling.

Zinc

7440-66-6sc-213177
100 g
$47.00
(0)

Zinc pyrithione can lead to increased intracellular zinc levels, which may enhance kinase activity involved in RET phosphorylation, thereby promoting GFR-1 activation.

Genistein

446-72-0sc-3515
sc-3515A
sc-3515B
sc-3515C
sc-3515D
sc-3515E
sc-3515F
100 mg
500 mg
1 g
5 g
10 g
25 g
100 g
$26.00
$92.00
$120.00
$310.00
$500.00
$908.00
$1821.00
46
(1)

Genistein is a tyrosine kinase inhibitor but at certain concentrations can paradoxically enhance tyrosine kinase activity. This could lead to increased RET activity and, as a result, GFR-1 activation.

Cantharidin

56-25-7sc-201321
sc-201321A
25 mg
100 mg
$81.00
$260.00
6
(1)

Cantharidin inhibits protein phosphatases, potentially leading to increased phosphorylation and activation of RET, which in turn would enhance GFR-1 signaling.