Rad GTPase Inhibitors
Rad GTPase inhibitors are specialized chemical agents devised to selectively impede the activity of the Rad GTPase enzyme, a member of the Ras superfamily of monomeric G proteins. Rad GTPases are involved in the intricate regulation of intracellular signaling networks that govern a variety of cellular functions such as cell growth, cytoskeletal organization, and the cell cycle. These proteins function as molecular switches cycling between an active GTP-bound state and an inactive GDP-bound state. The transition between these states is an essential process for the control of downstream signaling pathways. Rad GTPase inhibitors work by either stabilizing the inactive GDP-bound form or by preventing the exchange of GDP for GTP, thus maintaining Rad GTPase in a persistent inactive state. This inhibition can affect the conformational state of Rad GTPase and, consequently, its ability to interact with downstream effectors, effectively modulating the signaling cascades in which it is involved.
The discovery and development of Rad GTPase inhibitors involve a deep understanding of the molecular mechanisms that underpin the function of Rad GTPases, including knowledge of the nucleotide binding domain and the conformational changes associated with activation and inactivation. Inhibitors are often designed to mimic the structure of the nucleotides or to bind to specific regions of the GTPase, such as the switch I or switch II regions, which are critical for the conformational dynamics of the enzyme. Advanced techniques such as high-throughput screening, rational drug design, and computational modeling are employed to identify molecules that can effectively interact with Rad GTPase. Once potential inhibitors are identified, they are typically optimized through a series of chemical modifications to enhance their potency, selectivity, and ability to interact with the target enzyme. These compounds are then subjected to a battery of biochemical assays to assess their inhibitory activity, binding affinity, and specificity for Rad GTPase.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
NSC23766 disrupts the interaction between Rac1 GTPase and its specific guanine nucleotide exchange factors (GEFs), Trio and Tiam1, which can indirectly influence Rad GTPase signaling by modulating related GTPases within the Rho family, potentially altering the cellular effects mediated by Rad. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a potent inhibitor of phosphoinositide 3-kinases (PI3Ks), which can indirectly affect Rad GTPase activity by altering the PI3K/AKT pathway, a signaling cascade that can modulate various GTPases through downstream effects on cellular proliferation and survival signals. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Y-27632 is an inhibitor of Rho-associated protein kinase (ROCK), which can modulate the actin cytoskeleton and cellular motility, indirectly affecting Rad GTPase by influencing the downstream signaling pathways that Rad GTPase is a part of. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD98059 is an inhibitor of mitogen-activated protein kinase kinase (MEK), which is involved in the MAPK/ERK pathway. Inhibition of MEK can indirectly affect Rad GTPase function by altering the signaling dynamics of the MAPK/ERK pathway that regulates cell growth and differentiation. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $90.00 $349.00 | 284 | |
SB203580 is a p38 MAPK inhibitor, which can indirectly influence Rad GTPase signaling by modulating the cellular response to stress and cytokines, as p38 MAPK is involved in signaling pathways that can intersect with GTPase-mediated signaling networks. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin is a potent inhibitor of PI3K, which can affect Rad GTPase indirectly by modulating the PI3K/AKT signaling pathway, thus influencing various cellular processes including growth and survival that may be associated with Rad GTPase activity. | ||||||
Gö 6976 | 136194-77-9 | sc-221684 | 500 µg | $227.00 | 8 | |
Gö6976 is a potent inhibitor of protein kinase C (PKC), which can indirectly impact Rad GTPase by affecting PKC-mediated signaling pathways, potentially altering the phosphorylation states and activity of proteins within the same pathways as Rad GTPase. | ||||||
XAV939 | 284028-89-3 | sc-296704 sc-296704A sc-296704B | 1 mg 5 mg 50 mg | $36.00 $117.00 $525.00 | 26 | |
ZCL278 is a Cdc42 GTPase inhibitor that blocks the binding of Cdc42 to its GEFs, obstructing the activation of Cdc42. As part of the Rho family of GTPases, this can indirectly affect the signaling balance within the cell, potentially impacting Rad GTPase signaling pathways. | ||||||
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), which can indirectly influence Rad GTPase activity by affecting JNK signaling pathways involved in stress responses, apoptosis, and cytokine production that may intersect with Rad GTPase-regulated pathways. | ||||||