Sar1 Inhibitors
Chemical inhibitors of Sar1 can disrupt its role in vesicle trafficking through various mechanisms. Brefeldin A, for instance, targets the ADP-ribosylation factor (ARF), a GTPase necessary for the formation of vesicles from the endoplasmic reticulum (ER), which is crucial for Sar1's function. By inhibiting ARF, Brefeldin A effectively disrupts the function of Sar1 by halting vesicle transport at an early stage. Similarly, Golgicide A and Exo1 focus on inhibiting the Golgi BFA resistance factor 1 (GBF1) and the Sec7 domain of GBF1, respectively. Both GBF1 and its Sec7 domain are essential for the activation of ARF, critical for COPI vesicle formation. This prevention of ARF activation indirectly affects Sar1, as its role is intertwined with ARF's function in vesicle transport.
Further, inhibitors such as H89 and SecinH3 act on upstream regulators that influence Sar1 activity. H89 impedes protein kinase A, known to phosphorylate proteins that regulate Sar1, thus indirectly decreasing Sar1's activity through reduced regulatory protein function. SecinH3 targets cytohesins, a family of ARF guanine nucleotide exchange factors (GEFs), leading to a reduction in Sar1-related trafficking by impeding ARF-related processes. Conversely, AG1478, MiTMAB, and Dynasore affect Sar1 function by altering processes peripheral to COPI vesicle formation. AG1478, a tyrosine kinase inhibitor, can alter cell signaling pathways that influence vesicle formation, thus indirectly affecting Sar1. MiTMAB and Dynasore disrupt the function of dynamin, a GTPase involved in vesicle scission, which is a step subsequent to the formation of vesicles where Sar1 operates. Finally, ML141, CASIN, Latrunculin B, and Cytochalasin D disrupt the actin cytoskeleton, which plays a role in vesicle transport. ML141 and CASIN inhibit Cdc42, a GTPase involved in actin filament formation, while Latrunculin B and Cytochalasin D prevent actin polymerization and promote depolymerization, respectively. These disruptions to the cytoskeleton can indirectly impact Sar1's role in the transport of vesicles.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $31.00 $53.00 $124.00 $374.00 | 25 | |
Brefeldin A inhibits the ADP-ribosylation factor (ARF), a small GTPase essential for vesicle formation from the ER, which is a process Sar1 is critically involved in. Inhibition of ARF disrupts Sar1 function by blocking vesicle transport. | ||||||
Golgicide A | 1005036-73-6 | sc-215103 sc-215103A | 5 mg 25 mg | $191.00 $683.00 | 11 | |
Golgicide A specifically inhibits Golgi BFA resistance factor 1 (GBF1), a GEF for ARF, which is necessary for COPI vesicle formation. As Sar1 is involved in vesicle transport, GBF1 inhibition indirectly impedes Sar1's function in this process. | ||||||
Exo1 | 461681-88-9 | sc-200752 sc-200752A | 10 mg 50 mg | $84.00 $297.00 | 4 | |
Exo1 is a selective inhibitor of the Sec7 domain of GBF1, leading to an indirect inhibition of Sar1's role in vesicle formation and trafficking by preventing the activation of ARF which is necessary for Sar1 function. | ||||||
H-89 dihydrochloride | 130964-39-5 | sc-3537 sc-3537A | 1 mg 10 mg | $94.00 $186.00 | 71 | |
H89 inhibits protein kinase A, which can phosphorylate proteins that regulate Sar1 activity. By inhibiting this kinase, H89 can lead to a reduction in Sar1 activity due to decreased regulation of its associated proteins. | ||||||
SecinH3 | 853625-60-2 | sc-203260 | 5 mg | $278.00 | 6 | |
SecinH3 inhibits cytohesins, which are another family of ARF-GEFs, thus indirectly reducing Sar1 function by impacting ARF-related trafficking processes in which Sar1 is involved. | ||||||
Tyrphostin AG 1478 | 175178-82-2 | sc-200613 sc-200613A | 5 mg 25 mg | $96.00 $421.00 | 16 | |
AG1478 is a tyrosine kinase inhibitor that can inhibit EGFR kinase, which could indirectly decrease Sar1 activity by altering signaling pathways that impact vesicle formation and Sar1's role in this process. | ||||||
Dynamin Inhibitor I, Dynasore | 304448-55-3 | sc-202592 | 10 mg | $89.00 | 44 | |
Dynasore also targets dynamin, blocking its GTPase activity. This disrupts the endocytosis and vesicle formation processes, thereby having an indirect effect on Sar1 function, which is critical for vesicle trafficking from the ER. | ||||||
ML 141 | 71203-35-5 | sc-362768 sc-362768A | 5 mg 25 mg | $137.00 $512.00 | 7 | |
ML141 is an inhibitor of Cdc42, a small GTPase involved in actin filament formation. Since the actin cytoskeleton can regulate vesicle transport where Sar1 operates, inhibiting Cdc42 can indirectly inhibit Sar1's role in trafficking. | ||||||
CASIN | 425399-05-9 | sc-397016 | 10 mg | $460.00 | 1 | |
CASIN inhibits Cdc42 activity, which can influence actin dynamics and vesicle transport that Sar1 is a part of. This leads to an indirect inhibition of Sar1's function in vesicle trafficking by impeding actin structure formation. | ||||||
Latrunculin B | 76343-94-7 | sc-203318 | 1 mg | $240.00 | 29 | |
Latrunculin B binds to actin monomers, preventing polymerization and leading to actin depolymerization. This disruption of the cytoskeleton can indirectly inhibit Sar1's function in vesicle transport linked to the actin network. | ||||||