PIG-M Inhibitors
Chemical inhibitors of PIG-M function primarily by disrupting the essential post-translational modification process known as farnesylation. Manumycin A, Tipifarnib, and Lonafarnib are inhibitors that directly target farnesyltransferase, the enzyme responsible for attaching a farnesyl group to PIG-M. The farnesyl group facilitates the association of PIG-M with cell membranes, which is crucial for its activity. The inhibition of farnesyltransferase by these chemicals prevents the farnesylation of PIG-M, resulting in its mislocalization and subsequent loss of function. In a similar but more indirect fashion, Zoledronic acid, Alendronate, Ibandronate, Risedronate, and Pamidronate inhibit farnesyl pyrophosphate synthase (FPPS). FPPS is an upstream enzyme in the farnesylation pathway that produces farnesyl pyrophosphate, the substrate for farnesylation reactions. The inhibition of FPPS leads to a depletion of farnesyl pyrophosphate, thereby reducing the farnesylation and functionality of PIG-M.
In a different approach, Neratinib, Dasatinib, Lenvatinib, and Sorafenib are kinase inhibitors that can impede the activity of PIG-M by inhibiting kinases involved in its downstream signaling pathways. Although these chemicals are not directly interfering with the farnesylation process, they can disrupt the signaling mechanisms that are necessary for PIG-M's role within the cell. By inhibiting these kinases, the chemicals affect the pathways that relay signals required for the proper functioning of PIG-M. This results in an overall inhibition of PIG-M activity, despite the exact molecular interactions between PIG-M and these kinases not being the direct target of these chemicals. The broad-spectrum activity of Dasatinib and the multi-targeted approach of Sorafenib, in particular, suggest that multiple kinases involved in PIG-M related pathways can be inhibited, leading to a reduction in PIG-M's functional activity.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Manumycin A | 52665-74-4 | sc-200857 sc-200857A | 1 mg 5 mg | $215.00 $622.00 | 5 | |
Manumycin A is a selective inhibitor of farnesyltransferase, an enzyme that is crucial for the post-translational modification of many proteins, including PIG-M. By inhibiting farnesyltransferase, Manumycin A prevents the farnesylation that PIG-M requires for proper localization and function, leading to its functional inhibition. | ||||||
Tipifarnib | 192185-72-1 | sc-364637 | 10 mg | $720.00 | ||
Tipifarnib is another farnesyltransferase inhibitor that would interfere with the farnesylation process necessary for the proper functioning of PIG-M. By blocking this post-translational modification, Tipifarnib disrupts the localization and activity of PIG-M. | ||||||
Lonafarnib | 193275-84-2 | sc-482730 sc-482730A | 5 mg 10 mg | $173.00 $234.00 | ||
Lonafarnib is a farnesyltransferase inhibitor that impedes the farnesylation of proteins like PIG-M. As a result, PIG-M is unable to undergo proper membrane association, thereby inhibiting its biological activity. | ||||||
Zoledronic acid, anhydrous | 118072-93-8 | sc-364663 sc-364663A | 25 mg 100 mg | $90.00 $251.00 | 5 | |
Zoledronic acid is a bisphosphonate that inhibits farnesyl pyrophosphate synthase (FPPS), an enzyme upstream of farnesyltransferase. By inhibiting FPPS, the production of farnesyl pyrophosphate is reduced, indirectly inhibiting the farnesylation of PIG-M and thus its function. | ||||||
Alendronate acid | 66376-36-1 | sc-337520 | 5 g | $135.00 | 2 | |
Alendronate is another bisphosphonate that targets farnesyl pyrophosphate synthase, leading to reduced availability of farnesyl groups necessary for the farnesylation and subsequent activity of proteins like PIG-M. | ||||||
Ibandronate Sodium Monohydrate | 138926-19-9 | sc-218589 | 100 mg | $290.00 | ||
Ibandronate belongs to the bisphosphonate class and operates by inhibiting farnesyl pyrophosphate synthase. The inhibition of this enzyme decreases the farnesylation and membrane association of PIG-M, thereby reducing its functional activity. | ||||||
Neratinib | 698387-09-6 | sc-364549 sc-364549A sc-364549B sc-364549C sc-364549D | 5 mg 25 mg 100 mg 500 mg 1 g | $90.00 $210.00 $375.00 $740.00 $1225.00 | 4 | |
Neratinib is a tyrosine kinase inhibitor that, while primarily used to target HER2, could theoretically inhibit PIG-M-associated kinases that participate in downstream signaling pathways necessary for PIG-M function, thus resulting in its inhibition. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Dasatinib is a broad-spectrum tyrosine kinase inhibitor that could inhibit kinases involved in the signaling pathways where PIG-M plays a role. By inhibiting these kinases, Dasatinib may impair the signaling required for PIG-M's function. | ||||||
Lenvatinib | 417716-92-8 | sc-488530 sc-488530A sc-488530B | 5 mg 25 mg 100 mg | $178.00 $648.00 $1657.00 | 3 | |
Lenvatinib is a multi-kinase inhibitor that targets vascular endothelial growth factor receptors (VEGFRs), which could be part of the signaling pathways involving PIG-M. Inhibition of these receptors may thus indirectly inhibit the function of PIG-M. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $56.00 $260.00 $416.00 | 129 | |
Sorafenib is a kinase inhibitor that targets multiple receptors, potentially including those involved in pathways with PIG-M. Inhibition of these pathways would likely disrupt PIG-M's functional role in the cell. | ||||||