ARHGEF5L Inhibitors
ARHGEF5L Inhibitors are a unique class of chemical compounds that specifically target the signaling pathways and biological processes in which ARHGEF5L is directly involved, leading to its functional inhibition. The Rho Kinase Inhibitor Y-27632 works by inhibiting Rho kinase, an effector in the RhoA signaling pathway, causing a decrease in RhoA-mediated signaling and consequently reducing ARHGEF5L's activity. Similarly, NSC23766 and ITX3 specifically inhibit Rac1 by binding to Rac-specific GEFs and Trio, respectively, which decreases the substrate availability for ARHGEF5L and reduces its functional activity. PD98059, a MEK inhibitor, and LY294002, a PI3K inhibitor, indirectly affect ARHGEF5L by blocking pathways that would otherwise phosphorylate and activate molecules involved in ARHGEF5L-mediated signaling. SB203580, ML141, and SecinH3 each target different kinases and GTPases such as p38 MAPK, Cdc42, and cytohesins, which play a role in the pathways regulated by ARHGEF5L. By inhibiting these molecules, they contribute to the indirect reduction of ARHGEF5L signaling.
Further expanding on ARHGEF5L inhibition, Brefeldin A disrupts ARF GTPase's function, which interacts with pathways involving ARHGEF5L, leading to a decrease in its signaling capability. CCG-1423 approaches inhibition at the transcriptional level by inhibiting SRF, a downstream target of RhoA signaling, which affects ARHGEF5L. GSK269962A, another Rho kinase inhibitor, diminishes the downstream effects of RhoA activation, thereby reducing ARHGEF5L's output. Toxin B uniquely modifies Rho GTPases through glucosylation, disrupting their signaling and indirectly inhibiting ARHGEF5L. Each inhibitor, through its specific action on different molecules or pathways, contributes to a cumulative decrease in ARHGEF5L activity by either reducing the activation of its direct regulators or by altering the cellular environment in which ARHGEF5L operates. These well-characterized chemical interactions highlight the potential for precise modulation of ARHGEF5L function through targeted chemical inhibition.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $182.00 $693.00 | 88 | |
This chemical inhibits Rho kinase, which is an important downstream effector in the RhoA signaling pathway. ARHGEF5L acts as a guanine nucleotide exchange factor (GEF) for RhoA. Inhibition of Rho kinase leads to decreased RhoA-mediated signaling, reducing the functional activity of ARHGEF5L. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $148.00 $597.00 | 75 | |
NSC23766 is an inhibitor of Rac1, which interacts competitively with the binding site of Rac-specific GEFs. As ARHGEF5L has GEF activity, inhibiting Rac1 can indirectly decrease ARHGEF5L's functional activity by reducing its substrate availability. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
ITX3 selectively inhibits Trio, a GEF protein that activates Rac1. By inhibiting Trio, the pool of active Rac1 is reduced, which may indirectly lead to a decrease in ARHGEF5L activity due to reduced cross-talk between Rho family GTPases. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $39.00 $90.00 | 212 | |
PD98059 is a MEK inhibitor that blocks the MAPK/ERK pathway. ARHGEF5L can interact with components of the MAPK pathway. By inhibiting MEK, PD98059 can indirectly lead to decreased activation of ARHGEF5L through reduced phosphorylation and signaling cross-talk. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
A PI3K inhibitor that prevents the phosphorylation and activation of AKT. ARHGEF5L is involved in pathways that are regulated by PI3K signaling. Inhibition of PI3K can therefore lead to a reduction in ARHGEF5L-mediated signaling events. | ||||||
SB 203580 | 152121-47-6 | sc-3533 sc-3533A | 1 mg 5 mg | $88.00 $342.00 | 284 | |
SB203580 is a p38 MAPK inhibitor. Since p38 MAPK can influence the actin cytoskeleton and Rho GTPase activity, inhibiting this kinase could contribute to reduced ARHGEF5L signaling by diminishing the activation of pathways that involve actin remodeling and Rho GTPase regulation. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $134.00 $502.00 | 7 | |
ML141 is a Cdc42 inhibitor. It specifically inhibits the GTPase activity of Cdc42, which is a small Rho GTPase family member. Reduced Cdc42 activity can lead to the indirect inhibition of ARHGEF5L, as the function of ARHGEF5L is intertwined with the regulation of Rho family GTPases. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $273.00 | 6 | |
SecinH3 inhibits cytohesins, which are GEFs for ADP-ribosylation factor (ARF). ARF GTPases can regulate ARHGEF5L function indirectly through modulation of actin dynamics and vesicular trafficking, which are important for the signaling processes that ARHGEF5L is involved in. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A disrupts ARF function by inhibiting the exchange of GDP for GTP. As ARHGEF5L operates within the Rho family GTPase signaling pathways that can overlap with ARF-mediated pathways, Brefeldin A can indirectly inhibit ARHGEF5L function through disruption of these interacting pathways. | ||||||
CCG-1423 | 285986-88-1 | sc-205241 sc-205241A | 1 mg 5 mg | $30.00 $90.00 | 8 | |
CCG-1423 inhibits the transcriptional activity of serum response factor (SRF), which is downstream of RhoA signaling. By inhibiting SRF, CCG-1423 can indirectly reduce ARHGEF5L-mediated signaling by preventing the transcription of genes that are activated in response to RhoA signaling. | ||||||