cPKC βI Inhibitors
Chemical inhibitors of cPKC βI employ a variety of mechanisms to impede the enzyme's activity. Go 6983 and Bisindolylmaleimide I both target cPKC βI by competing with ATP at the kinase's catalytic site, effectively blocking the transfer of phosphate groups to substrate proteins. This competitive inhibition is also the strategy employed by Enzastaurin, Hispidin, Ruboxistaurin (also known by the identifier LY333531), K252a, Staurosporine, and Balanol, each binding to the ATP-binding pocket and thus preventing the kinase from phosphorylating its substrates. These compounds mimic ATP's structure to varying degrees, which allows them to fit into the ATP-binding site and obstruct the enzyme's function.
Ro 31-8220 differs slightly, functioning by mimicking the substrate rather than ATP and binding to the active site of cPKC βI. This action blocks the enzyme's natural substrates from accessing the active site, thereby inhibiting the kinase's function. Chelerythrine operates via an allosteric mechanism, where it intercalates into the catalytic domain and induces a conformational change that hinders the enzyme's activity. Similarly, C1-10 modulates the kinase domain allosterically but with a different binding mode that disrupts the catalytic activity of cPKC βI. These inhibitors collectively work to dampen the phosphorylation activity of cPKC βI by either direct competition with ATP or by altering the enzyme's structure so that it cannot interact effectively with its substrates.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $105.00 $299.00 $474.00 | 15 | |
Go 6983 is a potent protein kinase C inhibitor, which includes isoforms such as cPKC βI. It inhibits cPKC βI by competing with ATP for binding to the catalytic site of the enzyme, thereby preventing the phosphorylation of substrate proteins. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
Bisindolylmaleimide I, also known as GF 109203X, inhibits cPKC βI by acting as an ATP-competitive inhibitor, which directly blocks the kinase activity of cPKC βI, leading to a reduction in its catalytic function. | ||||||
Ro 31-8220 | 138489-18-6 | sc-200619 sc-200619A | 1 mg 5 mg | $92.00 $245.00 | 17 | |
Ro 31-8220 functions as a potent inhibitor of cPKC βI by mimicking the substrate and binding to the active site, which prevents the enzyme from interacting with its natural substrates, thus inhibiting its function. | ||||||
Chelerythrine | 34316-15-9 | sc-507380 | 100 mg | $540.00 | ||
Chelerythrine is a natural alkaloid that inhibits cPKC βI by intercalating into the catalytic domain of the kinase, inhibiting its activity through an allosteric mechanism that alters the enzyme's conformation. | ||||||
Enzastaurin | 170364-57-5 | sc-364488 sc-364488A sc-364488B | 10 mg 50 mg 200 mg | $259.00 $612.00 $1721.00 | 3 | |
Enzastaurin inhibits cPKC βI through competitive inhibition at the ATP-binding site of the kinase domain, leading to the reduction of its kinase activity and subsequent downstream signaling events. | ||||||
Hispidin | 555-55-5 | sc-203998 | 5 mg | $416.00 | ||
Hispidin is a natural compound that inhibits cPKC βI by binding to the ATP pocket of the enzyme, and it acts as a competitive inhibitor of ATP, leading to the suppression of cPKC βI activity. | ||||||
Ruboxistaurin | 169939-94-0 | sc-507364 | 25 mg | $1080.00 | ||
Ruboxistaurin, also known as LY333531, inhibits cPKC βI by selectively binding to the ATP-binding pocket, which prevents ATP from binding and hence inhibits the phosphorylation activity of the kinase. | ||||||
K-252a | 99533-80-9 | sc-200517 sc-200517B sc-200517A | 100 µg 500 µg 1 mg | $129.00 $214.00 $498.00 | 19 | |
K252a is a staurosporine-related compound that inhibits cPKC βI by binding to the ATP-binding site of the kinase, which prevents the phosphorylation of target proteins and inhibits the kinase's activity. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a potent kinase inhibitor that inhibits cPKC βI by binding to the ATP-binding pocket of the enzyme, thus blocking the ATP required for phosphorylation and inhibiting the kinase activity. | ||||||
Balanol | 63590-19-2 | sc-503251 | 10 mg | $13500.00 | ||
Balanol inhibits cPKC βI by mimicking the structure of ATP and competing for its binding site on the kinase, which inhibits the phosphorylation of downstream proteins and thereby the activity of cPKC βI. | ||||||