Date published: 2025-12-24

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GPR82 Inhibitors

Inhibitors of GPR82 operate through various molecular mechanisms, each targeting different aspects of the signaling pathways to diminish the functional activity of this G-protein-coupled receptor (GPCR). One class of inhibitors targets key kinases involved in the phosphorylation of GPCRs, thereby altering the phosphorylation status of GPR82 and reducing its signaling capability. Another set of inhibitors perturbs the regulatory role of G proteins themselves; for example, certain toxins enzymatically modify G protein subunits leading to altered GPR82 activity. Some inhibitors exert their effects by affecting the intracellular second messengers that are critical for GPR82 signaling. This includes compounds that prevent the interaction of GPR82 with its associated G proteins, thus shutting down the signaling cascade it would normally initiate. Other inhibitors act by disrupting the lipid kinase pathways or phospholipase C activity, both essential for the generation of secondary messengers in GPCR-mediated signaling, hence impacting GPR82 activity. Further refining the modulation of GPR82 activity, inhibitors can target downstream effectors, such as protein kinase C or Rho-associated protein kinase, which are involved in the phosphorylation and activity regulation of GPCRs. Additionally, compounds that selectively inhibit ion channels that modulate cellular excitability and downstream signaling of GPCRs provide an indirect approach to restraining GPR82 function. The cytoskeletal dynamics also play a crucial role in the trafficking and signaling of GPCRs, and inhibitors that impede small GTPase functions can lead to impaired receptor trafficking, thereby attenuating GPR82 signaling. Finally, antagonists of other GPCR subtypes contribute to the nuanced modulation of GPCR networks, potentially leading to a decrease in GPR82 signaling due to the intricate interplay of GPCR regulatory mechanisms.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Staurosporine

62996-74-1sc-3510
sc-3510A
sc-3510B
100 µg
1 mg
5 mg
$82.00
$150.00
$388.00
113
(4)

A potent kinase inhibitor that targets a wide range of kinases involved in various signaling pathways. Inhibition of these kinases disrupts downstream signaling which could inhibit GPR82 activation or reduce its expression due to altered cellular signaling dynamics.

GW 5074

220904-83-6sc-200639
sc-200639A
5 mg
25 mg
$106.00
$417.00
10
(1)

C-Raf kinase inhibitor that impedes the MAPK/ERK pathway. As kinase cascades are essential for various receptor functions, GPR82 activity or signaling could be indirectly attenuated due to impaired phosphorylation events within the cascade.

LY 294002

154447-36-6sc-201426
sc-201426A
5 mg
25 mg
$121.00
$392.00
148
(1)

A PI3K inhibitor that disrupts the PI3K/Akt pathway, which is integral to many GPCR-mediated functions. This could lead to a decrease in GPR82-mediated signaling through reduced downstream Akt activation, inhibiting its functional activity.

Pertussis Toxin (islet-activating protein)

70323-44-3sc-200837
50 µg
$442.00
3
(1)

An inhibitor of G(i/o) protein coupling, which can prevent GPR82 from exerting its effects via this G protein subfamily, thereby inhibiting its signaling capabilities.

Y-27632, free base

146986-50-7sc-3536
sc-3536A
5 mg
50 mg
$182.00
$693.00
88
(1)

A ROCK inhibitor that could hinder Rho-associated kinase pathways. As these are linked to GPCR function, GPR82 signaling could be indirectly inhibited due to downstream effects on cytoskeletal reorganization and cell motility.

Gö 6983

133053-19-7sc-203432
sc-203432A
sc-203432B
1 mg
5 mg
10 mg
$103.00
$293.00
$465.00
15
(1)

A broad-spectrum protein kinase C inhibitor which could attenuate signaling pathways that are activated downstream of GPR82, indirectly leading to its inhibition by altering the receptor's ability to initiate intracellular responses.

Chelerythrine

34316-15-9sc-507380
100 mg
$540.00
(0)

Another protein kinase C inhibitor that could indirectly inhibit GPR82 by disrupting its associated signaling pathways, preventing normal receptor function and downstream signaling events.

PD 98059

167869-21-8sc-3532
sc-3532A
1 mg
5 mg
$39.00
$90.00
212
(2)

MEK inhibitor that disrupts the MAPK/ERK pathway downstream of various GPCRs, leading to decreased GPR82 signaling through reduced ERK1/2 phosphorylation and activity.

Clozapine

5786-21-0sc-200402
sc-200402A
50 mg
500 mg
$68.00
$357.00
11
(1)

Known to bind to various GPCRs and could antagonize GPR82, leading to decreased receptor activation and signaling capacity.

Gabazine

105538-73-6sc-211552
10 mg
$714.00
3
(0)

A GABA receptor antagonist that, while its primary action is on GABA receptors, may also exhibit off-target effects on other GPCRs, inhibiting GPR82 activity through altered neurotransmission and receptor crosstalk.