PEF Inhibitors
Chemical inhibitors of PEF can interfere with its activity through various mechanisms, primarily by targeting the kinases that phosphorylate PEF or the signaling pathways that regulate its function. Staurosporine is a broad-spectrum kinase inhibitor that can inhibit the activity of kinases responsible for the phosphorylation of PEF, thus preventing its activation. Similarly, Bisindolylmaleimide I specifically inhibits protein kinase C, which is known to phosphorylate a wide array of proteins, including PEF. Consequently, the inhibition of PKC results in a decrease in PEF activity. LY294002 and Wortmannin are both inhibitors of PI3K, a kinase that activates the Akt signaling pathway, which may be responsible for the phosphorylation and subsequent activation of PEF. Therefore, by inhibiting PI3K, these chemicals lead to a reduction in PEF activity by preventing its phosphorylation. SB203580 targets p38 MAPK, and by impeding this kinase, it inhibits the MAPK pathway signaling, reducing the downstream effects on PEF activity.
Furthermore, PD98059 and U0126 are selective inhibitors of MEK, which operates upstream of the MAPK/ERK pathway. By inhibiting MEK, these chemicals impede the MAPK/ERK pathway, leading to a downstream reduction in PEF activity. SP600125 inhibits JNK, which is part of the MAPK pathway as well, and its inhibition also results in decreased PEF activity. In the realm of tyrosine kinase inhibitors, Lapatinib and Erlotinib inhibit the EGFR and HER2/neu, which are upstream of various signaling pathways that can lead to PEF activation. Therefore, the inhibition of these receptors by Lapatinib and Erlotinib results in diminished PEF activity. Sorafenib, a multi-kinase inhibitor, targets RAF kinases within the MAPK pathway. By inhibiting RAF, Sorafenib reduces signaling through MAPK, which translates into decreased PEF activity. Lastly, Sunitinib, as a receptor tyrosine kinase inhibitor, can also reduce PEF activity by inhibiting various receptors that are part of the signaling pathways contributing to PEF activation.
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. PEF is known to be regulated by phosphorylation; staurosporine inhibits kinases that phosphorylate PEF, thus preventing its activation. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I specifically inhibits protein kinase C (PKC). As PKC is responsible for phosphorylating a wide range of proteins, including PEF, its inhibition would lead to reduced PEF activity due to lack of necessary phosphorylation. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a PI3K inhibitor. By inhibiting PI3K, the downstream Akt signaling pathway, which may be responsible for activating PEF through phosphorylation, is inhibited, leading to decreased PEF activity. | ||||||
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 another PI3K inhibitor that works similarly to LY294002. It blocks PI3K activity, thereby inhibiting the Akt pathway and subsequent PEF phosphorylation and activation. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a specific inhibitor of p38 MAPK. PEF is a downstream effector in the MAPK pathway, and its activity is contingent upon signaling through this pathway. Inhibition of p38 MAPK results in decreased PEF activity. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 selectively inhibits MEK, which is upstream of the MAPK/ERK pathway. By blocking MEK, the activation of MAPK/ERK is prevented, leading to reduced PEF activity. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 is an inhibitor of JNK, another kinase within the MAPK pathway. Inhibition of JNK leads to decreased activation of downstream proteins, including PEF. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $63.00 $241.00 | 136 | |
U0126 is a specific inhibitor of MEK1/2, which are kinases upstream of ERK in the MAPK pathway. By inhibiting these kinases, PEF activity is decreased due to reduced ERK signaling. | ||||||
Lapatinib | 231277-92-2 | sc-353658 | 100 mg | $412.00 | 32 | |
Lapatinib inhibits the tyrosine kinase domains of EGFR and HER2/neu, which can lead to the activation of several downstream pathways, including ones involving PEF. Inhibition of EGFR and HER2/neu leads to decreased PEF activity. | ||||||
Erlotinib, Free Base | 183321-74-6 | sc-396113 sc-396113A sc-396113B sc-396113C sc-396113D | 500 mg 1 g 5 g 10 g 100 g | $85.00 $132.00 $287.00 $495.00 $3752.00 | 42 | |
Erlotinib is an EGFR inhibitor that prevents the activation of EGFR tyrosine kinase and subsequent downstream signaling pathways that could lead to PEF activation. With EGFR signaling inhibited, PEF activity is reduced. | ||||||