OCRL1 Inhibitors
Chemical inhibitors of OCRL1 employ various mechanisms to impede its enzymatic activity. Genistein, as a tyrosine kinase inhibitor, targets the phosphorylation process by hindering proteins that are substrates or regulators for OCRL1, thereby diminishing its functional activity. Sodium orthovanadate, on the other hand, competes with the natural substrates of OCRL1 by mimicking phosphate groups and binding to the enzyme's active site. This competition effectively blocks OCRL1 from catalyzing its normal dephosphorylation reactions. Similarly, Deoxynojirimycin constrains OCRL1 by structurally imitating a transition-state intermediate, which in turn hinders the enzyme's glycosyltransferase activity. Phenylarsine oxide takes a different approach by binding to vicinal dithiols and important cysteine residues within OCRL1, leading to the disruption of its catalytic activity.
Other inhibitors interfere with OCRL1's function through additional cellular mechanisms. Suramin, for instance, obstructs the enzymatic activity of OCRL1 by binding to its substrate-binding sites, preventing the interaction with its natural substrates. Calyculin A, a potent inhibitor of protein phosphatases, binds to the phosphatase domain of OCRL1, thereby blocking substrate dephosphorylation. Bafilomycin A1 disrupts OCRL1's activity indirectly by altering endosomal pH, which is a precondition for OCRL1's optimal function. Dynasore inhibits OCRL1 by halting dynamin-dependent endocytosis, a pathway crucial for OCRL1 to reach its action sites within the cell. Tyrphostin AG 1478 and Roscovitine act indirectly; Tyrphostin AG 1478 inhibits the EGFR tyrosine kinase which may regulate OCRL1 activity, while Roscovitine targets cyclin-dependent kinases that could influence OCRL1 or its substrates. Lastly, Chlorpromazine creates inhibitory effects by altering membrane associations, which is essential for the enzyme's action.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
Genistein inhibits OCRL1 by directly targeting its phosphatase activity. As a tyrosine kinase inhibitor, Genistein can impede the phosphorylation state of proteins that might serve as substrates or regulatory elements for OCRL1, thereby reducing its functional activity. | ||||||
Sodium Orthovanadate | 13721-39-6 | sc-3540 sc-3540B sc-3540A | 5 g 10 g 50 g | $49.00 $57.00 $187.00 | 142 | |
Sodium orthovanadate is a phosphatase inhibitor that can inhibit OCRL1 by mimicking phosphate and binding to the active site of the protein. This competitive inhibition prevents the dephosphorylation of physiological substrates by OCRL1, leading to an inhibition of its enzymatic function. | ||||||
Deoxynojirimycin | 19130-96-2 | sc-201369 sc-201369A | 1 mg 5 mg | $73.00 $145.00 | ||
Deoxynojirimycin binds to OCRL1 and inhibits its function by mimicking the structure of a transition-state intermediate in the reaction that OCRL1 catalyzes. This structural mimicry inhibits the enzyme's glycosyltransferase activity. | ||||||
Phenylarsine oxide | 637-03-6 | sc-3521 | 250 mg | $41.00 | 4 | |
Phenylarsine oxide acts as an inhibitor of OCRL1 by binding to vicinal dithiols within the active site and other critical cysteine residues, leading to the functional inhibition of the protein by disrupting its catalytic activity. | ||||||
Suramin sodium | 129-46-4 | sc-507209 sc-507209F sc-507209A sc-507209B sc-507209C sc-507209D sc-507209E | 50 mg 100 mg 250 mg 1 g 10 g 25 g 50 g | $152.00 $214.00 $728.00 $2601.00 $10965.00 $21838.00 $41096.00 | 5 | |
Suramin inhibits OCRL1 by binding to the protein's substrate-binding sites, which prevents the interaction of OCRL1 with its natural substrates, inhibiting its enzymatic activity. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Calyculin A, a potent inhibitor of protein phosphatases, can inhibit OCRL1 by binding to its phosphatase domain and preventing the dephosphorylation of substrates, thereby inhibiting its activity. | ||||||
Bafilomycin A1 | 88899-55-2 | sc-201550 sc-201550A sc-201550B sc-201550C | 100 µg 1 mg 5 mg 10 mg | $98.00 $255.00 $765.00 $1457.00 | 280 | |
Bafilomycin A1 inhibits OCRL1 by disrupting endosomal acidification, which is necessary for OCRL1's activity. The alteration in pH can affect the binding of OCRL1 to phosphoinositides and its subsequent phosphatase activity. | ||||||
Dynamin Inhibitor I, Dynasore | 304448-55-3 | sc-202592 | 10 mg | $89.00 | 44 | |
Dynasore inhibits OCRL1 by blocking dynamin-dependent endocytosis, a cellular process that OCRL1 is involved in. Inhibiting this pathway can prevent OCRL1 from reaching its sites of action within the cell, thereby inhibiting its normal function. | ||||||
Tyrphostin AG 1478 | 175178-82-2 | sc-200613 sc-200613A | 5 mg 25 mg | $96.00 $421.00 | 16 | |
Tyrphostin AG 1478 inhibits OCRL1 indirectly by inhibiting the epidermal growth factor receptor (EGFR) tyrosine kinase which could downregulate signaling pathways that potentially regulate OCRL1 activity and localization. | ||||||
Chlorpromazine | 50-53-3 | sc-357313 sc-357313A | 5 g 25 g | $61.00 $110.00 | 21 | |
Chlorpromazine inhibits OCRL1 by intercalating in cellular membranes and potentially altering the localization and membrane association of OCRL1, which is necessary for its activity. | ||||||