Smt3 Inhibitors
The chemical class known as Smt3 inhibitors encompasses a variety of compounds that influence the SUMOylation pathway at different points, from the initial activation of Smt3 by E1 enzyme to its final conjugation to target proteins by E2 and E3 ligases. These compounds often exhibit their inhibitory effects by interfering with the enzymatic machinery directly involved in Smt3's conjugation to substrates or by altering cellular pathways that indirectly affect the SUMOylation process.
Most Smt3 inhibitors function by disrupting the activity of SUMO-specific enzymes. For instance, ginkgolic acid and anacardic acid can inhibit the E1 activating enzyme, a key regulator of Smt3's attachment to target proteins. NEM chemically modifies the cysteines in SUMO-conjugating enzymes, which blocks their activity. Similarly, ML-792 acts as a potent inhibitor of the SUMO-activating enzyme SAE, directly preventing the initiation of the SUMOylation process. Other compounds like 2-D08 interfere with the SUMO E2 conjugating enzyme, stopping the transfer of Smt3 to substrates. Apart from direct enzyme inhibition, some Smt3 inhibitors act by modifying the intracellular environment. Compounds like arsenic trioxide and chloroquine induce stress responses or alter intracellular pH levels, respectively, which can lead to a decrease in the overall SUMOylation activity. This indirect inhibition can be a result of either downregulation of the SUMOylation machinery components or impairment of their function due to cellular stress.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Anacardic Acid | 16611-84-0 | sc-202463 sc-202463A | 5 mg 25 mg | $102.00 $204.00 | 13 | |
Similar to ginkgolic acid, anacardic acid can inhibit the E1 activating enzyme and thus has a dual role. It can impede the initial step of the SUMOylation pathway, effectively reducing SMT3 conjugation to target proteins. | ||||||
Gallotannin | 1401-55-4 | sc-202619 sc-202619A sc-202619B sc-202619C sc-202619D sc-202619E sc-202619F | 1 g 10 g 100 g 250 g 1 kg 2.5 kg 5 kg | $26.00 $37.00 $67.00 $78.00 $234.00 $536.00 $983.00 | 12 | |
Tannic acid has been reported to inhibit the SUMO-specific protease SENP, which could lead to reduced deSUMOylation and therefore potentially result in a negative feedback loop inhibiting SMT3 activation. | ||||||
Arsenic(III) oxide | 1327-53-3 | sc-210837 sc-210837A | 250 g 1 kg | $89.00 $228.00 | ||
Arsenic trioxide is known to induce oxidative stress, which can interfere with various cellular processes, including SUMOylation. The stress response might down-regulate the SUMOylation pathway, thereby inhibiting SMT3 activity. | ||||||
N-Ethylmaleimide | 128-53-0 | sc-202719A sc-202719 sc-202719B sc-202719C sc-202719D | 1 g 5 g 25 g 100 g 250 g | $22.00 $69.00 $214.00 $796.00 $1918.00 | 19 | |
NEM is an alkylating agent that can modify cysteines within the SUMO conjugation enzymes E1 and E2, inhibiting their activity and consequently SMT3's function in the SUMOylation process. | ||||||
ML-792 | 1644342-14-2 | sc-507423 | 10 mg | $398.00 | ||
ML-792 is a selective inhibitor of the SUMO-activating enzyme SAE, which is essential for SMT3 activation. By inhibiting SAE, this compound effectively blocks the SUMOylation process. | ||||||
FCM Lysing solution (1x) | sc-3621 | 150 ml | $62.00 | 8 | ||
Ammonium chloride acts to alkalinize intracellular compartments such as lysosomes, potentially disrupting cellular processes that depend on acidic environments, which could affect the SUMOylation process and indirectly inhibit SMT3. | ||||||
BAY 11-7082 | 19542-67-7 | sc-200615B sc-200615 sc-200615A | 5 mg 10 mg 50 mg | $62.00 $85.00 $356.00 | 155 | |
Bay 11-7082 inhibits the NF-kB pathway by blocking the phosphorylation of IkBα. Since NF-kB can regulate the expression of proteins involved in SUMOylation, this compound could indirectly reduce SMT3 activity. | ||||||
Camptothecin | 7689-03-4 | sc-200871 sc-200871A sc-200871B | 50 mg 250 mg 100 mg | $58.00 $186.00 $94.00 | 21 | |
As a topoisomerase I inhibitor, camptothecin can induce DNA damage responses which might paradoxically downregulate the SUMOylation machinery due to excessive DNA damage, thus indirectly inhibiting SMT3. | ||||||