LERK-3 Inhibitors
Chemical inhibitors of LERK-3 function by disrupting the protein's ability to engage in its normal cellular signaling processes. PD168393, for instance, irreversibly inhibits the activity of EGFR tyrosine kinase, which is known to phosphorylate and activate LERK-3, thereby preventing its usual role in cell adhesion and migration. Similarly, Erlotinib and Lapatinib target the EGFR, with Lapatinib also inhibiting HER2 tyrosine kinases, both of which are involved in the activation of LERK-3. Gefitinib acts in the same vein, focusing on EGFR to prevent its kinase activity, which is essential for LERK-3 activation. By blocking these kinases, these inhibitors effectively reduce the functional activity of LERK-3 within cellular signaling pathways.
Other inhibitors target a broader spectrum of tyrosine kinases that interact with or are part of the same pathways as LERK-3. Dasatinib, for example, inhibits Src family kinases responsible for phosphorylating LERK-3, thereby diminishing its activity. Bosutinib and Nilotinib also target Src family kinases, with the additional target of Abl kinase for Bosutinib and exclusive inhibition of Abl tyrosine kinase by Nilotinib, both resulting in reduced LERK-3 signaling. Sorafenib, Sunitinib, Pazopanib, Vandetanib, and Axitinib inhibit a variety of receptor tyrosine kinases like VEGFR, PDGFR, and c-Kit, or a combination of these along with EGFR and RET, as seen with Vandetanib. These inhibitors collectively decrease the signaling cascades that facilitate LERK-3 mediated functions, particularly in the context of angiogenesis and vascular remodeling, which are processes where LERK-3 is known to be involved. By curtailing the kinase activity of these receptors, the inhibitors obstruct the cross-talk and activation necessary for LERK-3 to fulfill its role in the cell.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PD 168393 | 194423-15-9 | sc-222138 | 1 mg | $162.00 | 4 | |
PD168393 irreversibly inhibits the tyrosine kinase activity of EGFR, which LERK-3 (Ephrin type-B receptor 3) can interact with, leading to reduced downstream signaling and functional inhibition of LERK-3 mediated cell adhesion and migration. | ||||||
Dasatinib | 302962-49-8 | sc-358114 sc-358114A | 25 mg 1 g | $47.00 $145.00 | 51 | |
Dasatinib is a Src family kinase inhibitor. Since Src family kinases can phosphorylate LERK-3 and modulate its signaling, inhibition by Dasatinib reduces LERK-3's kinase activity, resulting in its functional inhibition. | ||||||
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 targets and inhibits EGFR tyrosine kinase, which can phosphorylate LERK-3. This inhibition disrupts the EGFR-mediated activation of LERK-3, leading to functional inhibition. | ||||||
Lapatinib | 231277-92-2 | sc-353658 | 100 mg | $412.00 | 32 | |
Lapatinib is a dual inhibitor of EGFR and HER2 tyrosine kinases. By inhibiting EGFR, it prevents the activation and signaling of LERK-3, thereby functionally inhibiting its activity. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $56.00 $260.00 $416.00 | 129 | |
Sorafenib inhibits multiple receptor tyrosine kinases, including VEGFR and PDGFR, which are involved in the same pathways as LERK-3. Its inhibition reduces the signaling that contributes to LERK-3 activation and function. | ||||||
Sunitinib Malate | 341031-54-7 | sc-220177 sc-220177A sc-220177B | 10 mg 100 mg 3 g | $193.00 $510.00 $1072.00 | 4 | |
Sunitinib is a receptor tyrosine kinase inhibitor, including PDGFR and VEGFR, which are part of pathways LERK-3 is involved in. By inhibiting these kinases, Sunitinib decreases LERK-3-mediated signaling, leading to its functional inhibition. | ||||||
Pazopanib | 444731-52-6 | sc-396318 sc-396318A | 25 mg 50 mg | $127.00 $178.00 | 2 | |
Pazopanib targets VEGFR, PDGFR, and c-Kit, which are part of the angiogenesis and vascular remodeling pathways in which LERK-3 functions. Inhibiting these kinases disrupts the signaling and function of LERK-3. | ||||||
Vandetanib | 443913-73-3 | sc-220364 sc-220364A | 5 mg 50 mg | $167.00 $1353.00 | ||
Vandetanib inhibits VEGFR, EGFR, and RET tyrosine kinases. Inhibition of these kinases diminishes the cross-talk and activation of LERK-3, leading to its functional inhibition. | ||||||
Nilotinib | 641571-10-0 | sc-202245 sc-202245A | 10 mg 25 mg | $205.00 $405.00 | 9 | |
Nilotinib is a selective inhibitor of Abl tyrosine kinase. Since Abl can interact with and activate LERK-3, inhibition by Nilotinib reduces LERK-3's functional activity in cellular signaling. | ||||||
Gefitinib | 184475-35-2 | sc-202166 sc-202166A sc-202166B sc-202166C | 100 mg 250 mg 1 g 5 g | $62.00 $112.00 $214.00 $342.00 | 74 | |
Gefitinib is an EGFR inhibitor. It prevents the kinase activity of EGFR, which is necessary for the phosphorylation and activation of LERK-3, thus functionally inhibiting LERK-3 signaling in cells. | ||||||