PRB4 Inhibitors
Chemical inhibitors of PRB4 act through various molecular pathways to impede its functional activity. Staurosporine and Bisindolylmaleimide I target protein kinase C (PKC), a critical enzyme in the phosphorylation process of PRB4. By inhibiting PKC, these chemicals restrict the phosphorylation and subsequent activation of PRB4, effectively reducing its activity within the cell. Similar inhibitory effects are achieved by Gö6976, which specifically suppresses PKC alpha and beta isoforms, leading to a decrease in PRB4 activity through PKC-mediated pathways. In contrast, LY294002 and Wortmannin exert their inhibitory effects by targeting PI3K. The PI3K signaling pathway is integral for multiple cellular functions, including the activation of AKT, which is believed to play a role in PRB4 activation. By impeding PI3K, these inhibitors contribute to the downregulation of AKT signaling, culminating in the functional inhibition of PRB4.
In addition to these, PD98059 and U0126 are inhibitors of MEK, a component of the MAPK/ERK pathway, which is known to phosphorylate various substrates within the cell, including PRB4. By obstructing MEK, PD98059 and U0126 prevent the phosphorylation and the contingent activation of PRB4. SB203580 operates through a similar mechanism by selectively inhibiting p38 MAP kinase, thereby averting the activation of PRB4 associated with p38 MAP kinase signaling. JNK signaling, implicated in influencing PRB4 activity, is inhibited by SP600125, which hinders the phosphorylation and activation of PRB4 mediated by JNK pathways. Rapamycin, an mTOR inhibitor, reduces the signaling within the PI3K/AKT/mTOR pathway, which can be vital for PRB4's activity. As a result, Rapamycin indirectly restricts PRB4 function by inhibiting mTOR. Lastly, Alsterpaullone and ZM-447439 target cell division-related kinases. Alsterpaullone inhibits cyclin-dependent kinases, which may regulate PRB4 activity, while ZM-447439 suppresses Aurora kinases, also preventing the phosphorylation and activation of PRB4 during mitosis.
Items 1 to 10 of 12 total
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $150.00 $388.00 | 113 | |
Staurosporine is a potent inhibitor of protein kinases. By inhibiting protein kinase C, which is known to phosphorylate PRB4, staurosporine can inhibit the phosphorylation process necessary for PRB4's functional activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a specific inhibitor of PI3K. PI3K signaling is crucial for many cellular functions, including the activation of AKT, which may be necessary for the full activation of PRB4. Inhibition of PI3K leads to downregulation of AKT signaling, thereby functionally inhibiting PRB4 downstream of AKT. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 specifically inhibits MEK, which is part of the MAPK/ERK pathway. The MAPK/ERK pathway can phosphorylate various substrates, including proteins similar to PRB4. By inhibiting MEK, PD98059 prevents the phosphorylation and subsequent activation of proteins in this pathway, including PRB4. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a selective inhibitor of p38 MAP kinase. PRB4 can be a downstream effector of p38 MAP kinase signaling. By inhibiting p38 MAP kinase, SB203580 can prevent the activation of PRB4 that would normally result from p38 MAP kinase activity. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an inhibitor of c-Jun N-terminal kinase (JNK). JNK can influence the activity of various cellular proteins, including PRB4. By inhibiting JNK, SP600125 can prevent the phosphorylation and activation of PRB4 that is mediated via JNK signaling pathways. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is an inhibitor of MEK1/2, which are upstream of ERK in the MAPK/ERK pathway. As the MAPK/ERK pathway can regulate the activity of proteins such as PRB4, inhibition by U0126 can lead to a reduction in PRB4 activity due to lack of required phosphorylation by ERK. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a potent inhibitor of PI3K. Similar to LY294002, by inhibiting PI3K, Wortmannin indirectly leads to a decrease in AKT activation, which is potentially necessary for PRB4 activation. Therefore, Wortmannin can functionally inhibit PRB4 by reducing AKT-mediated phosphorylation that is essential for PRB4 activity. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $62.00 $155.00 $320.00 | 233 | |
Rapamycin is an mTOR inhibitor. By inhibiting mTOR, which is a central component of the PI3K/AKT/mTOR pathway, Rapamycin can reduce the signaling necessary for the full functionality of PRB4. This leads to a functional inhibition of PRB4 by preventing its activity within this pathway. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a selective inhibitor of protein kinase C (PKC). Since PKC is involved in phosphorylating and activating proteins such as PRB4, its inhibition can lead to decreased PRB4 activity. | ||||||
Alsterpaullone | 237430-03-4 | sc-202453 sc-202453A | 1 mg 5 mg | $67.00 $306.00 | 2 | |
Alsterpaullone is a cyclin-dependent kinase inhibitor. By inhibiting CDKs, Alsterpaullone can prevent the phosphorylation and activation of proteins that are regulated by the cell cycle, including PRB4. | ||||||