RASGEF1A Inhibitors
In the context of RASGEF1A inhibition, a series of small molecule inhibitors exert their effects by targeting specific proteins that are either upstream activators or part of the signaling cascade in which RASGEF1A operates. Key targets include various growth factor receptors whose inhibition leads to a reduction in RAS signaling, effectively decreasing the functional activity of RASGEF1A. These inhibitors are particularly focused on the epidermal growth factor receptor (EGFR) and other receptor tyrosine kinases, whose downstream signaling is crucial for RASGEF1A activation. By attenuating the upstream EGFR tyrosine kinase activity, the subsequent intracellular RAS-RAF-MEK-ERK pathway is dampened, thereby reducing the engagement of RASGEF1A. Additionally, several compounds specifically inhibit MEK, a kinase within the ERK signaling pathway, which further ensures a decrease in RASGEF1A activation due to its reliance on this pathway for its function.
Further indirect inhibition of RASGEF1A is achieved through the use of inhibitors that prevent the post-translational modification of RAS proteins, a necessary step for their proper function. By obstructing farnesyltransferase, which facilitates the farnesylation of RAS proteins, the inhibitors thwart the localization and subsequent activation of RAS proteins, indirectly precluding the activation of RASGEF1A. Some multi-targeted inhibitors also contribute to the reduction of RASGEF1A activity by simultaneously inhibiting various receptor tyrosine kinases, thereby broadly suppressing the signaling pathways leading to RAS activation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 | |
Inhibits epidermal growth factor receptor (EGFR) tyrosine kinase, which indirectly downregulates RAS signaling as EGFR is upstream of RAS in the signaling cascade. This reduction in RAS signaling decreases the activation of RASGEF1A. | ||||||
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 | |
Targets and inhibits EGFR tyrosine kinase, leading to reduced RAS-RAF-MEK-ERK signaling, which consequently diminishes the functional activation of RASGEF1A. | ||||||
Lapatinib | 231277-92-2 | sc-353658 | 100 mg | $412.00 | 32 | |
Dual inhibitor of EGFR and HER2 tyrosine kinases, attenuating the RAS-RAF-MEK-ERK pathway upstream, thus decreasing the functional activity of RASGEF1A. | ||||||
Trametinib | 871700-17-3 | sc-364639 sc-364639A sc-364639B | 5 mg 10 mg 1 g | $112.00 $163.00 $928.00 | 19 | |
A MEK inhibitor that interrupts the MEK-ERK signaling pathway. With the pathway inhibited, the activity of RASGEF1A is also reduced due to its functional position within this cascade. | ||||||
Cobimetinib | 934660-93-2 | sc-507421 | 5 mg | $270.00 | ||
MEK inhibitor that disrupts the downstream signaling of RAS, leading to reduced activation of RASGEF1A, which relies on RAS signaling for 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 | |
RAF kinase inhibitor that blocks the RAS-RAF-MEK-ERK signaling pathway, subsequently inhibiting the downstream activation of RASGEF1A. | ||||||
Sunitinib, Free Base | 557795-19-4 | sc-396319 sc-396319A | 500 mg 5 g | $150.00 $920.00 | 5 | |
A receptor tyrosine kinase inhibitor that indirectly affects RAS signaling by inhibiting growth factor receptors upstream of RASGEF1A, leading to its decreased activity. | ||||||
Pazopanib | 444731-52-6 | sc-396318 sc-396318A | 25 mg 50 mg | $127.00 $178.00 | 2 | |
Inhibits multiple receptor tyrosine kinases, reducing RAS signaling upstream and thereby indirectly diminishing the functional activity of RASGEF1A. | ||||||
Selumetinib | 606143-52-6 | sc-364613 sc-364613A sc-364613B sc-364613C sc-364613D | 5 mg 10 mg 100 mg 500 mg 1 g | $28.00 $80.00 $412.00 $1860.00 $2962.00 | 5 | |
A selective MEK1/2 inhibitor that impairs the MEK-ERK pathway, leading to a reduction in RASGEF1A functional activity as part of this signaling cascade. | ||||||
Tipifarnib | 192185-72-1 | sc-364637 | 10 mg | $720.00 | ||
A farnesyltransferase inhibitor that prevents the farnesylation and subsequent activation of RAS proteins, thereby indirectly inhibiting RASGEF1A activation. | ||||||