GPR139 Inhibitors
The landscape of GPR139 inhibitors is a blend of general GPCR modulators and a few specific chemicals like ML221 that act on GPR139 directly. GPR139, being an orphan GPCR, has potential avenues of regulation via modulating its G-protein-mediated signaling. Pertussis toxin, for instance, is a potent inhibitor of certain G-protein subtypes and can impact GPR139's actions as it couples through those specific subtypes. Likewise, YM-254890 and NF023, which target Gq/11 proteins and Gαi/o proteins respectively, offer similar regulatory avenues if GPR139 operates through these pathways.
Additionally, many GPCRs signal through downstream effectors such as phospholipase C (PLC) and protein kinase C (PKC). Thus, compounds like U73122, a PLC inhibitor, and both chelerythrine chloride and Go6983, which are PKC inhibitors, can indirectly influence GPR139. Another integral aspect of GPCR signaling is the cAMP pathway. SQ 22536 and H89, which inhibit adenylate cyclase and protein kinase A (PKA) respectively, offer ways to modulate this pathway, potentially influencing GPR139 function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Pertussis Toxin (islet-activating protein) | 70323-44-3 | sc-200837 | 50 µg | $442.00 | 3 | |
This chemical can inhibit certain G-protein signaling and could thus potentially modulate GPR139. | ||||||
YM 254890 | 568580-02-9 | sc-507356 | 1 mg | $500.00 | ||
Specific Gq/11 protein inhibitor that may influence GPR139 signaling if it couples via this pathway. | ||||||
NF 023 | 104869-31-0 | sc-204124 sc-204124A | 10 mg 50 mg | $158.00 $617.00 | 1 | |
Gαi/o protein inhibitor that might modulate GPR139 if it couples via this pathway. | ||||||
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 | $149.00 $210.00 $714.00 $2550.00 $10750.00 $21410.00 $40290.00 | 5 | |
A general GPCR antagonist which might influence GPR139. | ||||||
Chelerythrine chloride | 3895-92-9 | sc-3547 sc-3547A | 5 mg 25 mg | $88.00 $311.00 | 17 | |
PKC inhibitor which may influence downstream GPCR signaling. | ||||||
SQ 22536 | 17318-31-9 | sc-201572 sc-201572A | 5 mg 25 mg | $93.00 $356.00 | 13 | |
An adenylate cyclase inhibitor that could indirectly affect cAMP levels related to GPR139 signaling. | ||||||
H-89 dihydrochloride | 130964-39-5 | sc-3537 sc-3537A | 1 mg 10 mg | $92.00 $182.00 | 71 | |
PKA inhibitor that can modulate cAMP-mediated GPCR signaling. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $103.00 $293.00 $465.00 | 15 | |
A broad-spectrum PKC inhibitor affecting GPCR downstream signaling. | ||||||