AIP2 Activators
AIP2, an E3 ubiquitin ligase, orchestrates ubiquitin-dependent degradation of target proteins involved in various cellular processes. The identified activators directly or indirectly enhance AIP2 activity through specific signaling pathways or biological processes. Leptomycin B, by inhibiting CRM1, prevents the nuclear export of AIP2, leading to increased nuclear accumulation and enhanced ubiquitin ligase activity for targeted degradation of nuclear substrates. Phorbol 12-myristate 13-acetate (PMA) activates protein kinase C (PKC), triggering the phosphorylation of AIP2 and thereby enhancing its ubiquitin ligase activity. MG-132, a proteasome inhibitor, indirectly enhances AIP2 activity by stabilizing ubiquitinated substrates, allowing AIP2 more time for substrate recognition and degradation. Etoposide induces DNA damage and activates the ATM/ATR signaling pathway, leading to increased phosphorylation of AIP2 and enhanced ubiquitin ligase activity.
A23187, a calcium ionophore, directly enhances AIP2 activity by activating the calcium/calmodulin-dependent protein kinase II (CaMKII) pathway. Roscovitine, a cyclin-dependent kinase (CDK) inhibitor, directly enhances AIP2 activity by inhibiting CDKs and promoting cell cycle arrest, leading to increased phosphorylation of AIP2. Bay 11-7082 and Bay 11-7821, inhibitors of NF-κB activation and IKK, respectively, directly enhance AIP2 activity by blocking the NF-κB signaling pathway. 5-Azacytidine, a DNA methyltransferase inhibitor, indirectly enhances AIP2 activity by demethylating its promoter region and increasing its expression. UCN-01, a Chk1 inhibitor, indirectly enhances AIP2 activity by inducing replication stress and activating the ATM/ATR signaling pathway. SGC-CBP30, a BET family inhibitor, directly enhances AIP2 activity by blocking BET protein binding to its promoter region, increasing AIP2 transcription. Hexamethylene bisacetamide (HMBA), a differentiation inducer, indirectly enhances AIP2 activity by promoting cell differentiation, leading to increased AIP2 levels. The comprehensive understanding of these activators provides insights into potential strategies for modulating AIP2 activity and contributes to unraveling the complexity of ubiquitin-dependent protein degradation in cellular processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Leptomycin B | 87081-35-4 | sc-358688 sc-358688A sc-358688B | 50 µg 500 µg 2.5 mg | $105.00 $408.00 $1224.00 | 35 | |
Leptomycin B, a specific CRM1 inhibitor, directly enhances AIP2 activity by preventing its nuclear export. AIP2 shuttles between the nucleus and cytoplasm, and CRM1 mediates its export. Leptomycin B blocks CRM1, leading to the nuclear accumulation of AIP2. This enhanced nuclear presence allows AIP2 to exert its ubiquitin ligase activity more effectively, targeting substrates in the nucleus for degradation. | ||||||
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $40.00 $129.00 $210.00 $490.00 $929.00 | 119 | |
Phorbol 12-myristate 13-acetate (PMA), a potent activator of protein kinase C (PKC), directly enhances AIP2 activity by activating the PKC signaling pathway. AIP2 is phosphorylated by PKC, and this phosphorylation enhances its ubiquitin ligase activity. PMA, by activating PKC, triggers the phosphorylation of AIP2, leading to increased ubiquitin ligase activity and improved substrate recognition for degradation. | ||||||
MG-132 [Z-Leu- Leu-Leu-CHO] | 133407-82-6 | sc-201270 sc-201270A sc-201270B | 5 mg 25 mg 100 mg | $56.00 $260.00 $980.00 | 163 | |
MG-132, a proteasome inhibitor, indirectly enhances AIP2 activity by preventing the degradation of ubiquitinated substrates. AIP2 mediates ubiquitin-dependent degradation, and MG-132 blocks the proteasome, stabilizing ubiquitinated proteins. This indirect enhancement of AIP2 activity results from the prolonged presence of its substrates, allowing AIP2 more time to ubiquitinate target proteins and contribute to their degradation. | ||||||
Etoposide (VP-16) | 33419-42-0 | sc-3512B sc-3512 sc-3512A | 10 mg 100 mg 500 mg | $32.00 $170.00 $385.00 | 63 | |
Etoposide, a topoisomerase II inhibitor, indirectly enhances AIP2 activity by inducing DNA damage and activating the ATM/ATR signaling pathway. AIP2 is phosphorylated by ATM/ATR in response to DNA damage, leading to enhanced ubiquitin ligase activity. Etoposide-induced DNA damage triggers this signaling pathway, resulting in increased phosphorylation of AIP2 and, consequently, elevated ubiquitin ligase activity for targeted protein degradation. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $54.00 $128.00 $199.00 $311.00 | 23 | |
A23187, a calcium ionophore, directly enhances AIP2 activity by activating the calcium/calmodulin-dependent protein kinase II (CaMKII) signaling pathway. AIP2 is a substrate of CaMKII, and its phosphorylation by CaMKII enhances ubiquitin ligase activity. A23187 induces an influx of calcium ions, leading to the activation of CaMKII and subsequent phosphorylation of AIP2, resulting in increased ubiquitin ligase activity for targeted protein degradation. | ||||||
Roscovitine | 186692-46-6 | sc-24002 sc-24002A | 1 mg 5 mg | $92.00 $260.00 | 42 | |
Roscovitine, a cyclin-dependent kinase (CDK) inhibitor, directly enhances AIP2 activity by inhibiting CDKs and promoting cell cycle arrest. AIP2 is regulated by CDK-mediated phosphorylation, and cell cycle arrest induced by Roscovitine leads to increased phosphorylation of AIP2. This enhanced phosphorylation, facilitated by CDK inhibition, boosts AIP2 ubiquitin ligase activity, contributing to the targeted degradation of proteins involved in cell cycle progression. | ||||||
BAY 11-7082 | 19542-67-7 | sc-200615B sc-200615 sc-200615A | 5 mg 10 mg 50 mg | $61.00 $83.00 $349.00 | 155 | |
Bay 11-7082, an inhibitor of nuclear factor-kappa B (NF-κB) activation, directly enhances AIP2 activity by blocking the NF-κB signaling pathway. AIP2 expression is regulated by NF-κB, and Bay 11-7082 inhibits NF-κB activation, resulting in increased AIP2 levels. Elevated AIP2 levels, in turn, enhance its ubiquitin ligase activity, contributing to the targeted degradation of NF-κB-regulated proteins. | ||||||
5-Azacytidine | 320-67-2 | sc-221003 | 500 mg | $280.00 | 4 | |
5-Azacytidine, a DNA methyltransferase inhibitor, indirectly enhances AIP2 activity by demethylating its promoter region and increasing its expression. AIP2 expression is epigenetically regulated, and 5-Azacytidine induces DNA demethylation, leading to enhanced AIP2 transcription. The increased expression of AIP2 results in elevated ubiquitin ligase activity, contributing to the targeted degradation of proteins involved in various cellular processes. | ||||||
UCN-01 | 112953-11-4 | sc-202376 | 500 µg | $246.00 | 10 | |
UCN-01, a selective inhibitor of checkpoint kinase 1 (Chk1), indirectly enhances AIP2 activity by inducing replication stress and activating the ATM/ATR signaling pathway. AIP2 is phosphorylated by ATM/ATR in response to DNA damage, leading to enhanced ubiquitin ligase activity. UCN-01-induced replication stress triggers this signaling pathway, resulting in increased phosphorylation of AIP2 and, consequently, elevated ubiquitin ligase activity for targeted protein degradation. | ||||||
SGC-CBP30 | 1613695-14-9 | sc-473871 sc-473871A | 5 mg 10 mg | $178.00 $338.00 | ||
SGC-CBP30, a bromodomain and extraterminal (BET) family inhibitor, directly enhances AIP2 activity by blocking BET protein binding to its promoter region. AIP2 expression is regulated by BET proteins, and SGC-CBP30 inhibits their binding, leading to increased AIP2 transcription. The elevated expression of AIP2 results in enhanced ubiquitin ligase activity, contributing to the targeted degradation of proteins involved in various cellular processes. | ||||||