A730069N07Rik Inhibitors
Chemical inhibitors of deleted in liver cancer 1 (DLC1) function by targeting various elements of the Rho GTPase signaling pathways, which are integral to the actin cytoskeleton organization and cellular dynamics that DLC1 influences. NSC 23766 operates by preventing the interaction between Rac1 GTPase and its guanine nucleotide exchange factors (GEFs) like Trio and Tiam1, effectively reducing Rac1 activity. Similarly, EHT 1864 binds directly to Rac1, inhibiting its action and, by extension, the actin cytoskeleton reorganization that DLC1 is involved in. Y-27632 takes a different approach by inhibiting ROCK, which is a downstream effector in the Rho pathway. Since DLC1 is a Rho-GTPase activating protein (RhoGAP), its function is indirectly reduced when ROCK activity is lowered. Furthermore, CCG-1423 disrupts RhoA-mediated gene transcription by inhibiting the MKL1/SRF pathway, which, under normal conditions, is influenced by DLC1's regulatory role on RhoA signaling.
Continuing the theme of Rho GTPase signaling inhibition, Rhosin and CASIN target the RhoA and Cdc42 GTPases, respectively. Rhosin selectively inhibits the binding of RhoA to Rho GEFs, leading to a decrease in RhoA signaling, while CASIN inhibits Cdc42, disrupting actin polymerization and cell motility processes that DLC1 affects. ZCL278 and Secramine A both act on Cdc42; ZCL278 inhibits the interaction between Cdc42 and its GEFs, while Secramine A traps Cdc42 in the Golgi apparatus, preventing its localization and function. ITX3 targets the GEF Trio, which is responsible for the activation of Rac1 and RhoG, hence affecting DLC1's role in cytoskeletal organization. ML141, as a potent inhibitor of Cdc42, disrupts its GTPase activity, leading to indirect inhibition of DLC1 since it modulates Rho GTPase-mediated processes. Lastly, CID-2950007 and Rho Inhibitor I specifically target RhoA signaling; CID-2950007 selectively inhibits the RhoA GEF, GEF-H1, while Rho Inhibitor I prevents the activation of RhoA itself, resulting in diminished stress fiber formation and focal adhesions, both of which are key areas where DLC1 exerts its regulatory effects.
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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 | |
Inhibits the Rac1 GTPase interaction with guanine nucleotide exchange factors Trio and Tiam1, leading to inhibition of Rac1 activity and its downstream signaling which is crucial for actin cytoskeleton reorganization; as deleted in liver cancer 1 (DLC1) is involved in actin cytoskeleton regulation, this would result in functional inhibition of DLC1. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Inhibits ROCK (Rho-associated protein kinase), a downstream effector in the Rho pathway; since DLC1 is a Rho-GTPase activating protein, inhibiting ROCK can decrease migration and cytoskeletal changes normally influenced by active Rho GTPases, thus functionally inhibiting DLC1. | ||||||
CCG-1423 | 285986-88-1 | sc-205241 sc-205241A | 1 mg 5 mg | $30.00 $90.00 | 8 | |
Inhibits RhoA-mediated gene transcription by blocking the MKL1/SRF pathway; DLC1, as a Rho-GTPase activating protein, would have reduced function due to the reduced RhoA-mediated signaling. | ||||||
Rhosin | 1173671-63-0 | sc-507401 | 25 mg | $555.00 | ||
Selectively inhibits RhoA subfamily binding to Rho guanine nucleotide exchange factors (GEFs), reducing RhoA signaling; this would lead to inhibition of downstream effects on the actin cytoskeleton, thereby inhibiting the functional role of DLC1 in this pathway. | ||||||
ITX 3 | 347323-96-0 | sc-295214 sc-295214A | 10 mg 50 mg | $145.00 $615.00 | ||
Inhibits Trio, a guanine nucleotide exchange factor (GEF) for Rac1 and RhoG; as DLC1 has GAP activity towards RhoGTPases, inhibiting Trio would reduce RhoGTPase signaling and thus inhibit DLC1's functional role in actin cytoskeletal organization. | ||||||
EHT 1864 | 754240-09-0 | sc-361175 sc-361175A | 10 mg 50 mg | $213.00 $889.00 | 12 | |
Directly binds to and inhibits Rac1, leading to inhibition of Rac1-mediated actin cytoskeleton organization; since DLC1 has a role in actin cytoskeleton regulation via its RhoGAP domain, inhibition of Rac1 would limit DLC1's functional impact on cell shape and migration. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
Inhibits Cdc42, another Rho GTPase, which indirectly reduces actin polymerization and cell motility; DLC1's functional role is related to the regulation of actin dynamics, and inhibiting Cdc42 would therefore inhibit DLC1's effects on the actin cytoskeleton. | ||||||
ZCL278 | 587841-73-4 | sc-507369 | 10 mg | $115.00 | ||
Inhibits the interaction between Cdc42 and its GEFs, specifically intersectin, thereby reducing Cdc42 activity; since DLC1 regulates cytoskeletal organization through its RhoGAP activity, decreasing Cdc42 activity would inhibit the functional role of DLC1 in cytoskeletal reorganization. | ||||||