OR1S2 Inhibitors
OR1S2 inhibitors encompass a range of compounds that target various aspects of GPCR signaling, either by direct interaction with the receptors or by altering the receptor signaling environment. Staurosporine, for example, is a pan-kinase inhibitor that can attenuate the phosphorylation level of OR1S2, leading to a decrease in its functional activity. Pertussis toxin, by ADP-ribosylating the alpha subunit of Gi/o type G-proteins, can disrupt the coupling of OR1S2 to its associated G-protein, thereby hindering the receptor's ability to regulate downstream effectors such as adenylate cyclase.
Other compounds like LY294002 and U73122 target specific enzymes within the GPCR signaling cascade. LY294002 inhibits PI3K, which is involved in the recruitment and activation of downstream signaling components essential for OR1S2 function. This can result in reduced OR1S2 activity due to impaired signal propagation. U73122, by inhibiting phospholipase C, can disrupt the generation of second messengers from PIP2, impeding OR1S2-mediated signal transduction through the Gq protein pathway. Such inhibitors demonstrate the intricate network of interactions and feedback mechanisms that regulate OR1S2 activity, where altering one component of the signaling pathway can have a cascade effect on the receptor's function.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a non-specific protein kinase inhibitor. By inhibiting protein kinases, it can reduce the phosphorylation of G-protein coupled receptors (GPCRs), including OR1S2, preventing their activation and subsequent signaling. | ||||||
Pertussis Toxin (islet-activating protein) | 70323-44-3 | sc-200837 | 50 µg | $451.00 | 3 | |
Pertussis Toxin irreversibly ADP-ribosylates the alpha subunit of the Gi/o type G-proteins, which could prevent OR1S2 from inhibiting adenylate cyclase, thus maintaining high cAMP levels and keeping the receptor in an inactive state. | ||||||
Haloperidol | 52-86-8 | sc-507512 | 5 g | $190.00 | ||
Haloperidol acts as an antagonist at dopamine receptors, another type of GPCR. By altering the dopamine pathway, it could indirectly affect the signaling environment and desensitize GPCRs like OR1S2 through cross-regulation mechanisms. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor. PI3K is involved in the activation of AKT, which can phosphorylate and regulate GPCR trafficking. Inhibition of PI3K might reduce the trafficking of OR1S2 to the membrane, reducing its activity. | ||||||
Propranolol | 525-66-6 | sc-507425 | 100 mg | $180.00 | ||
Propranolol is a beta-adrenergic antagonist that can affect beta-adrenergic receptor GPCRs. As these receptors often have cross-talk with other GPCRs, the inhibition could lead to downstream effects that reduce OR1S2 activity. | ||||||
Ritonavir | 155213-67-5 | sc-208310 | 10 mg | $124.00 | 7 | |
Ritonavir is known to inhibit the activity of cytochrome P450 3A4. This enzyme metabolizes certain GPCR ligands, and its inhibition may lead to altered ligand availability for OR1S2, possibly reducing its activation. | ||||||
Chlorpromazine | 50-53-3 | sc-357313 sc-357313A | 5 g 25 g | $61.00 $110.00 | 21 | |
Chlorpromazine is a dopamine receptor antagonist and can block GPCR signaling. Altered dopamine signaling could indirectly decrease OR1S2 activity through changes in receptor desensitization or internalization. | ||||||
Gallein | 2103-64-2 | sc-202631 | 50 mg | $85.00 | 20 | |
Gallein is a Gβγ subunit signaling inhibitor. By inhibiting the function of Gβγ, it can indirectly inhibit the signaling of GPCRs like OR1S2 that rely on these subunits for their signaling cascade. | ||||||
Suramin sodium | 129-46-4 | sc-507209 sc-507209F sc-507209A sc-507209B sc-507209C sc-507209D sc-507209E | 50 mg 100 mg 250 mg 1 g 10 g 25 g 50 g | $152.00 $214.00 $728.00 $2601.00 $10965.00 $21838.00 $41096.00 | 5 | |
Suramin is a non-specific antagonist of various GPCRs. By binding to these receptors, it might prevent the activation of OR1S2 by either steric hindrance or through the alteration of the lipid rafts where GPCRs reside. | ||||||
Ketoconazole | 65277-42-1 | sc-200496 sc-200496A | 50 mg 500 mg | $63.00 $265.00 | 21 | |
Ketoconazole inhibits cytochrome P450 enzymes, affecting the synthesis and metabolism of various GPCR ligands. This could lead to decreased activation of OR1S2 due to altered ligand concentrations. | ||||||