PPP1R4 Inhibitors
Chemical inhibitors of PPP1R4 target the protein by disrupting its regulatory influence on protein phosphatase 1 (PP1). Okadaic Acid and Calyculin A, for instance, are potent inhibitors of PP1 and by extension inhibit PPP1R4, as the regulatory subunit's primary function is to modulate PP1 activity. These compounds bind to PP1 and prevent PPP1R4 from exerting its effects, which include dephosphorylation of key cellular proteins. Similarly, Tautomycin and Cantharidin inhibit PP1, and therefore PPP1R4's role is also inhibited since it cannot regulate an inactive PP1. Microcystin-LR and Endothall function in a comparable manner, binding to PP1, leading to the functional inhibition of PPP1R4 by disallowing any regulatory action on the now inactive PP1. Rubratoxin B, though less commonly referenced, also inhibits PP1 and, by association, prevents PPP1R4 from fulfilling its regulatory functions.
In another approach, Cyclosporin A and FK506 inhibit calcineurin, a protein phosphatase whose activity can influence the signaling pathways that PPP1R4 is a part of. The inhibition of these pathways impedes PPP1R4's ability to regulate PP1, thereby indirectly inhibiting its function. Rapamycin, which targets mTOR, disrupts downstream signaling that can include pathways regulated by PPP1R4. The inhibition of mTOR by Rapamycin ultimately leads to an indirect inhibition of PPP1R4 by altering the cellular processes it influences. Sanglifehrin A, akin to Cyclosporin A and FK506, binds to cyclophilins and inhibits calcineurin, affecting the same pathways as PPP1R4 and thereby hindering its functional activity. Lastly, Zoledronic Acid inhibits farnesyl pyrophosphate synthase, a key enzyme in protein prenylation. By interfering with this process, Zoledronic Acid can inhibit the localization and function of proteins such as PPP1R4, which rely on proper prenylation for their activity within the cell.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $285.00 $520.00 $1300.00 | 78 | |
Okadaic Acid is a potent inhibitor of protein phosphatase 1 (PP1) and PP2A. Since PPP1R4 is a regulatory subunit of PP1, inhibition of PP1's phosphatase activity by Okadaic Acid will lead to the functional inhibition of PPP1R4, preventing it from mediating its regulatory effects on PP1. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A sc-24000B sc-24000C | 10 µg 100 µg 500 µg 1 mg | $160.00 $750.00 $1400.00 $3000.00 | 59 | |
Calyculin A, similar to Okadaic Acid, is a strong inhibitor of PP1 and PP2A. By inhibiting PP1, Calyculin A consequently inhibits the function of PPP1R4 by preventing it from exerting its regulatory role on the phosphatase activity of PP1. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $169.00 $299.00 | 66 | |
Tautomycin selectively inhibits protein phosphatases PP1 and PP2A. By binding to and inhibiting PP1, Tautomycin will inhibit the functional role of PPP1R4 by disallowing it from regulating PP1 activity. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $81.00 $260.00 | 6 | |
Cantharidin is an inhibitor of serine/threonine protein phosphatases including PP1. By inhibiting PP1, Cantharidin will impair the functional capacity of PPP1R4, since PPP1R4 is known to bind to and regulate PP1. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $48.00 $199.00 | 1 | |
Endothall acts as an inhibitor of PP1 and PP2A. Thus, the inhibition of PP1 by Endothall will functionally inhibit PPP1R4 by preventing its interaction with and regulation of PP1's activity. | ||||||
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $62.00 $90.00 $299.00 $475.00 $1015.00 $2099.00 | 69 | |
Cyclosporin A is primarily known as an immunosuppressant, but it also inhibits calcineurin, a protein phosphatase. Through inhibition of downstream pathways of calcineurin, Cyclosporin A can lead to the functional inhibition of PPP1R4, which relies on regulated phosphatase activity for its function. | ||||||
FK-506 | 104987-11-3 | sc-24649 sc-24649A | 5 mg 10 mg | $76.00 $148.00 | 9 | |
FK506, also known as Tacrolimus, inhibits calcineurin. The inhibition of calcineurin indirectly leads to the functional inhibition of PPP1R4 by altering the phosphatase signaling pathways that PPP1R4 is a part of. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
Sirolimus inhibits mTOR, which is a key kinase in the regulation of cell growth and metabolism. By inhibiting mTOR, Sirolimus can indirectly inhibit PPP1R4 by disrupting signaling pathways that regulate cellular processes involving PPP1R4. | ||||||
Zoledronic acid, anhydrous | 118072-93-8 | sc-364663 sc-364663A | 25 mg 100 mg | $90.00 $251.00 | 5 | |
Zoledronic Acid inhibits farnesyl pyrophosphate synthase, leading to disruption of prenylation. This disruption can inhibit PPP1R4 by interfering with signaling pathways that regulate protein prenylation, which affects the localization and function of proteins like PPP1R4. | ||||||