GAP-assoc p62 Inhibitors
Chemical inhibitors of GAP-assoc p62 can disrupt its activity through a variety of molecular mechanisms, primarily by targeting pathways that are upstream of GAP-assoc p62. For instance, Wortmannin and LY294002 are compounds that inhibit phosphoinositide 3-kinases (PI3Ks), a group of enzymes involved in the initiation of the Akt signaling pathway. Since GAP-assoc p62 operates downstream of this pathway, the inhibition of PI3K by these compounds results in a reduction of Akt phosphorylation, which in turn diminishes the activation of GAP-assoc p62. Similarly, Spautin-1, which induces the degradation of PI3K, leads to reduced PI3K activity and thus less activation of the downstream components including GAP-assoc p62. Perifosine and Miltefosine, both alkylphospholipids, inhibit the activation of Akt, thereby preventing the phosphorylation and subsequent activation of GAP-assoc p62.
In addition to the PI3K/Akt pathway inhibitors, compounds that target mTOR, a key part of the same pathway, also play a role in regulating the activity of GAP-assoc p62. Rapamycin and its analogs, such as PP242 and Palomid 529, inhibit mTOR by different mechanisms; Rapamycin binds to mTOR complex 1 (mTORC1), while PP242 and Palomid 529 target the ATP-binding site of mTOR or both mTORC1 and mTORC2, respectively. This inhibition leads to reduced downstream signaling, which includes the activity of GAP-assoc p62. Other Akt-specific inhibitors, such as Triciribine, MK-2206, GSK690693, and AZD5363, directly prevent Akt phosphorylation and activation. By selectively inhibiting Akt, these compounds ensure that the phosphorylation-dependent activation of GAP-assoc p62 does not occur, effectively reducing its functional activity within the cell. Each of these inhibitors operates by impeding the signaling required for GAP-assoc p62 activation, although by different molecular targets and mechanisms.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin inhibits phosphoinositide 3-kinases (PI3Ks), which are upstream of Akt signaling pathway, a pathway that GAP-assoc p62 is known to interact with. Inhibition of PI3K activity can lead to reduced Akt phosphorylation and subsequent decreased activation of GAP-assoc p62. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is another PI3K inhibitor that can reduce Akt pathway activity. Since GAP-assoc p62 functions downstream of PI3K/Akt pathway, LY294002's inhibition of PI3K can result in the functional inhibition of GAP-assoc p62 by limiting its activation through the pathway. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
Rapamycin specifically inhibits mTOR (mammalian target of rapamycin), which is a part of the PI3K/Akt pathway. Through inhibiting mTOR, Rapamycin can diminish the downstream signaling that would otherwise contribute to the functional activity of GAP-assoc p62. | ||||||
PP242 | 1092351-67-1 | sc-301606A sc-301606 | 1 mg 5 mg | $56.00 $169.00 | 8 | |
PP242 is an inhibitor of mTOR that works differently from Rapamycin, as it targets the ATP-binding site of mTOR. By inhibiting mTOR's kinase activity, PP242 can suppress the mTOR signaling cascade, indirectly leading to the functional inhibition of GAP-assoc p62. | ||||||
Spautin-1 | 1262888-28-7 | sc-507306 | 10 mg | $165.00 | ||
Spautin-1 promotes the degradation of PI3K, which indirectly inhibits the PI3K/Akt signaling pathway. With reduced PI3K levels, the downstream activation of GAP-assoc p62 would be functionally inhibited due to less PI3K activity to propagate the signaling. | ||||||
Perifosine | 157716-52-4 | sc-364571 sc-364571A | 5 mg 10 mg | $184.00 $321.00 | 1 | |
Perifosine is an alkylphospholipid that inhibits Akt activation. By preventing phosphorylation and activation of Akt, perifosine can functionally inhibit the activity of GAP-assoc p62, which is regulated by the PI3K/Akt signaling pathway. | ||||||
Triciribine | 35943-35-2 | sc-200661 sc-200661A | 1 mg 5 mg | $102.00 $138.00 | 14 | |
Triciribine specifically targets the Akt pathway by preventing Akt phosphorylation and activation. This inhibition of Akt directly leads to a functional inhibition of GAP-assoc p62, as its activity is dependent on the Akt signaling. | ||||||
MK-2206 dihydrochloride | 1032350-13-2 | sc-364537 sc-364537A | 5 mg 10 mg | $178.00 $325.00 | 67 | |
MK-2206 is a highly selective inhibitor of Akt. By inhibiting Akt, MK-2206 can effectively reduce the functional activity of GAP-assoc p62, which operates downstream of the Akt signaling pathway. | ||||||
GSK 690693 | 937174-76-0 | sc-363280 sc-363280A | 10 mg 50 mg | $255.00 $1071.00 | 4 | |
GSK690693 is an ATP-competitive inhibitor of Akt. By inhibiting Akt kinase activity, GSK690693 can functionally inhibit GAP-assoc p62 since its activity is modulated through the Akt pathway. | ||||||
Miltefosine | 58066-85-6 | sc-203135 | 50 mg | $79.00 | 8 | |
Miltefosine is an alkylphosphocholine that interferes with PI3K/Akt signaling. The functional activity of GAP-assoc p62 would be inhibited by miltefosine due to the disruption of the pathway essential for its activation. | ||||||