Date published: 2026-5-30

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Gα i-2 Activators

The term Gαi-2 activators refers to a class of chemicals that modulate the activity of the Gαi-2 subunit of heterotrimeric G proteins, thereby influencing downstream signaling pathways. While direct activators of Gαi-2 are not explicitly identified, these chemicals target pathways and cellular processes associated with Gαi-2 activation. Pertussis Toxin is a potent inhibitor of Gαi-2 signaling. It catalyzes the ADP-ribosylation of the Gαi subunit, preventing its interaction with receptors and downstream signaling. Mastoparan, on the other hand, directly activates Gαi by interacting with the Gα subunit, leading to the inhibition of adenylyl cyclase and downstream cascades. The exchange of GDP for GTP is a crucial step in Gαi-2 activation. GDP, when bound to Gαi-2, keeps it in an inactive state. In contrast, GTP, or its non-hydrolyzable analog GTPγS, maintains the active conformation of Gαi-2, facilitating sustained signaling through inhibition of adenylyl cyclase and other effectors.

Lysophosphatidic Acid (LPA) and Sphingosine-1-Phosphate (S1P) are extracellular lipids that activate Gαi-2-coupled receptors, leading to the inhibition of adenylyl cyclase and modulating cellular responses. Clonidine, Somatostatin, CXCL12 (SDF-1α), Carbachol, N-Arachidonyl-Glycine, and Fingolimod (FTY720) are compounds that activate Gαi-2-coupled receptors, inhibiting adenylyl cyclase and regulating various cellular processes.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Mastoparan

72093-21-1sc-200831
1 mg
$99.00
(1)

A wasp venom peptide that activates Gαi by interacting directly with the Gα subunit, leading to the inhibition of adenylyl cyclase and downstream signaling cascades.

Guanosine 5′-diphosphate sodium salt hydrate (GDP)

146-91-8 non-saltsc-507402
10 mg
$645.00
(0)

Guanosine diphosphate, which, when bound to Gαi, keeps it in an inactive state. Activation involves the exchange of GDP for GTP, leading to a conformational change in Gαi and subsequent downstream signaling.

Lysophosphatidic Acid

325465-93-8sc-201053
sc-201053A
5 mg
25 mg
$98.00
$341.00
50
(3)

An extracellular lipid that activates Gαi-coupled receptors, leading to the inhibition of adenylyl cyclase and downstream signaling events.

D-erythro-Sphingosine-1-phosphate

26993-30-6sc-201383
sc-201383D
sc-201383A
sc-201383B
sc-201383C
1 mg
2 mg
5 mg
10 mg
25 mg
$165.00
$322.00
$570.00
$907.00
$1727.00
7
(1)

A bioactive lipid that activates Gαi-coupled receptors, inhibiting adenylyl cyclase and modulating cellular responses.

Clonidine

4205-90-7sc-501519
100 mg
$240.00
1
(0)

An alpha-2 adrenergic agonist that activates Gαi-coupled receptors, inhibiting adenylyl cyclase and reducing cAMP levels.

Somatostatin Acetate

38916-34-6sc-220124
10 mg
$320.00
(0)

A peptide hormone that activates Gαi-coupled somatostatin receptors, leading to the inhibition of adenylyl cyclase and downstream signaling.

Carbachol

51-83-2sc-202092
sc-202092A
sc-202092C
sc-202092D
sc-202092B
sc-202092E
1 g
10 g
25 g
50 g
100 g
250 g
$122.00
$281.00
$388.00
$683.00
$1428.00
$3060.00
12
(2)

A cholinergic agonist that activates Gαi-coupled muscarinic receptors, inhibiting adenylyl cyclase and regulating cellular responses.

N-Arachidonoyl glycine

179113-91-8sc-362169
sc-362169A
5 mg
25 mg
$114.00
$191.00
2
(1)

An endocannabinoid that activates Gαi-coupled cannabinoid receptors, inhibiting adenylyl cyclase and modulating neurotransmitter release and other cellular processes.

Fingolimod

162359-55-9sc-507334
10 mg
$160.00
(0)

A sphingosine analog that activates Gαi-coupled receptors, leading to the internalization and degradation of these receptors, modulating immune cell trafficking and other responses.