UPIIIb Inhibitors
Chemical inhibitors of Uroplakin IIIb (UPIIIb) function through diverse biochemical mechanisms to disrupt the protein's activity. Phloretin impacts UPIIIb by targeting its glycosylation process, which is pivotal for UPIIIb's proper folding and function. When glycosylation is hindered, UPIIIb cannot maintain its structure or its role within the cell membrane. Similarly, monensin, an ionophore, disrupts sodium ion gradients, which are integral for cellular processes, including the trafficking and localization of UPIIIb. By altering ion concentrations, monensin can impede the transport mechanisms essential for UPIIIb's functionality. Filipin, on the other hand, binds to membrane cholesterol, a key component in the maintenance of lipid rafts where UPIIIb is localized. By interacting with cholesterol, filipin can disrupt these microdomains and thus UPIIIb's activity.
Furthermore, okadaic acid inhibits protein phosphatases such as PP1 and PP2A, which are responsible for dephosphorylating proteins, a critical step for the functional regulation of UPIIIb. Inhibition of these enzymes can, therefore, result in a reduction of UPIIIb activity. Calphostin C and bisindolylmaleimide I specifically inhibit protein kinase C (PKC), essential for the phosphorylation events regulating UPIIIb's signaling pathways. The inhibition of PKC by these compounds leads to a decrease in UPIIIb activity. Similarly, W-7 hydrochloride inhibits calmodulin, which is involved in calcium signaling pathways that regulate UPIIIb function. KT5720, a protein kinase A (PKA) inhibitor, and Gö 6983, a pan-PKC inhibitor, disrupt the phosphorylation of proteins within UPIIIb's signaling pathways, thus impairing UPIIIb's activity. Lastly, PD 98059 and LY294002 target specific kinases such as MEK and PI3K, respectively, which are upstream regulators of pathways that UPIIIb may be involved in. By inhibiting these kinases, the compounds can lead to the downregulation of UPIIIb's activity within the cell.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Phloretin | 60-82-2 | sc-3548 sc-3548A | 200 mg 1 g | $64.00 $255.00 | 13 | |
Phloretin inhibits UPIIIb by interfering with its glycosylation process. Glycosylation is essential for the proper folding and functionality of membrane proteins like UPIIIb, and phloretin disrupts this enzymatic activity, leading to a functional inhibition of UPIIIb. | ||||||
Monensin A | 17090-79-8 | sc-362032 sc-362032A | 5 mg 25 mg | $155.00 $525.00 | ||
Monensin acts as an ionophore that disrupts sodium ion gradients across membranes. By altering intracellular ion concentrations, it can disrupt membrane trafficking pathways that are essential for the transport and proper localization of UPIIIb, thus inhibiting its function. | ||||||
Filipin III | 480-49-9 | sc-205323 sc-205323A | 500 µg 1 mg | $118.00 $148.00 | 26 | |
Filipin is a polyene macrolide that binds to cholesterol in the cell membrane. Since cholesterol is crucial for the proper organization and functioning of lipid rafts, and UPIIIb is associated with these microdomains, filipin can disrupt lipid rafts, leading to the inhibition of UPIIIb's activity. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Okadaic Acid is an inhibitor of protein phosphatases PP1 and PP2A. These phosphatases are involved in dephosphorylating proteins, a process essential for the function of many proteins including UPIIIb. Inhibition of these phosphatases leads to the functional inhibition of UPIIIb. | ||||||
Calphostin C | 121263-19-2 | sc-3545 sc-3545A | 100 µg 1 mg | $343.00 $1642.00 | 20 | |
Calphostin C inhibits protein kinase C (PKC), which plays a role in the phosphorylation of proteins involved in signaling pathways that include UPIIIb. Inhibition of PKC leads to decreased activity of UPIIIb due to the lack of necessary phosphorylation events. | ||||||
W-7 | 61714-27-0 | sc-201501 sc-201501A sc-201501B | 50 mg 100 mg 1 g | $166.00 $306.00 $1675.00 | 18 | |
W-7 Hydrochloride is an inhibitor of calmodulin, a calcium-binding messenger protein. Since calmodulin is involved in calcium signaling pathways that can regulate the activity of UPIIIb, its inhibition can lead to reduced UPIIIb activity. | ||||||
KT 5720 | 108068-98-0 | sc-3538 sc-3538A sc-3538B | 50 µg 100 µg 500 µg | $138.00 $220.00 $972.00 | 47 | |
KT5720 is an inhibitor of protein kinase A (PKA). PKA is involved in the phosphorylation of many proteins, a post-translational modification that can affect the function of UPIIIb. By inhibiting PKA, KT5720 can indirectly lead to the functional inhibition of UPIIIb. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
Bisindolylmaleimide I is a specific inhibitor of PKC. By inhibiting PKC, it prevents the phosphorylation of proteins that are part of the signaling pathways regulating UPIIIb, leading to the inhibition of UPIIIb's functional 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 | |
Gö 6983 is a pan-PKC inhibitor, which inhibits multiple isoforms of PKC. This broad-spectrum inhibition disrupts signaling pathways crucial for the function of UPIIIb, thus functionally inhibiting the protein. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD 98059 inhibits MEK, which is upstream of the extracellular signal-regulated kinase (ERK) pathway. ERK is potentially involved in the signaling pathways of UPIIIb, and by inhibiting this pathway, PD 98059 can result in the inhibition of UPIIIb. | ||||||