GPR135 Inhibitors
GPR135 inhibitors operate through intricate cellular mechanisms to attenuate the protein's activity within its specific pathways. These inhibitors are diverse, yet they share the common result of disrupting the signaling cascades that GPR135 is a part of or influenced by. For example, the selective inhibition of kinases that are upstream in signaling pathways associated with GPR135, such as MAPK/ERK kinase and c-Raf, leads to a downstream reduction in GPR135 activity. This is achieved by preventing the necessary phosphorylation and activation steps that would typically propagate through the signaling pathway to GPR135. Similarly, inhibitors that target the RhoA/ROCK signaling, which GPR135's function is contingent upon, can lead to a decrease in its activity by preventing the cytoskeletal rearrangements necessary for its proper signaling.
Other inhibitors act on different aspects of cellular signaling that are crucial for GPR135 function. Compounds that inhibit protein kinase C or phospholipase C disrupt the generation and function of second messengers, which are instrumental in GPR135-mediated signal transduction. By blocking these signaling molecules, the protein's activity is indirectly decreased. Furthermore, inhibitors that impede pathways like BMP signaling via ALK receptors or PI3K/Akt signaling also contribute to a decrease in GPR135 activity, as these pathways can modulate the function of GPR135 under certain cellular conditions. Additionally, mTOR inhibitors and EGFR kinase inhibitors play a role in reducing GPR135 activity by hindering pathways that can upregulate or potentiate GPR135 signaling, hence leading to a dampened signaling output of the protein.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
LY 341495 | 201943-63-7 | sc-361244 sc-361244A | 1 mg 10 mg | $89.00 $223.00 | 1 | |
A selective group II metabotropic glutamate receptor antagonist. It inhibits GPR135 by attenuating the downstream signaling cascade initiated by glutamate, which could otherwise engage GPR135 activity through secondary messenger systems. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
A selective inhibitor of MAPK/ERK kinase. It indirectly inhibits GPR135 by blocking the phosphorylation and activation of the ERK pathway, which is implicated in GPR135-mediated cellular responses. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
A pyridinyl imidazole compound that inhibits p38 MAP Kinase. This inhibition disrupts cellular processes modulated by p38 MAPK that could activate GPR135, thereby reducing its functional activity. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
A selective inhibitor of the Rho-associated, coiled-coil containing protein kinase (ROCK). GPR135 activity is modulated via RhoA/ROCK signaling, and inhibiting this kinase leads to decreased activity of GPR135. | ||||||
GW 5074 | 220904-83-6 | sc-200639 sc-200639A | 5 mg 25 mg | $106.00 $417.00 | 10 | |
An inhibitor of c-Raf kinase, which is part of the Ras-Raf-MEK-ERK signaling pathway. By inhibiting c-Raf, GW 5074 indirectly reduces GPR135 signaling, since activation of this pathway can lead to GPR135 activation. | ||||||
ML-7 hydrochloride | 110448-33-4 | sc-200557 sc-200557A | 10 mg 50 mg | $91.00 $267.00 | 13 | |
An inhibitor of myosin light chain kinase (MLCK). Since MLCK is involved in cytoskeletal rearrangements that could influence GPR135 signaling, its inhibition by ML-7 decreases GPR135 activity. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $105.00 $299.00 $474.00 | 15 | |
A potent protein kinase C (PKC) inhibitor. PKC is implicated in the regulation of GPR135, and inhibition by Go 6983 reduces the functional activity of GPR135 by dampening PKC-mediated signal transduction. | ||||||
BML-275 | 866405-64-3 | sc-200689 sc-200689A | 5 mg 25 mg | $96.00 $355.00 | 69 | |
A selective inhibitor of BMP signaling via ALK2/3/6. By inhibiting this pathway, this compound indirectly reduces the functional activity of GPR135 which may be activated downstream of BMP-mediated cellular processes. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
A potent inhibitor of phosphoinositide 3-kinases (PI3K). PI3K inhibition by LY294002 leads to a reduction in Akt signaling, a pathway that can modulate GPR135 activity, thus indirectly inhibiting GPR135. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
An mTOR inhibitor that indirectly affects GPR135 activity by inhibiting the mTOR pathway, which plays a role in cellular processes that could upregulate GPR135 signaling. | ||||||