transportin 2 Activators
Chemical activators of transportin 2 employ a diverse array of mechanisms to modulate its activity. Phorbol 12-myristate 13-acetate (PMA) and 1,2-Dioctanoyl-sn-glycerol (DiC8), both functionally related due to their ability to activate protein kinase C (PKC), can enhance the nuclear import function of transportin 2. PKC achieves this by phosphorylating substrates that include components of the nuclear import machinery, thereby potentially increasing transportin 2's binding affinity for its cargo proteins. Forskolin, through the activation of adenylyl cyclase and subsequent increase in cAMP levels, activates protein kinase A (PKA). The activation of PKA can lead to the phosphorylation of proteins involved in nuclear transport, which in turn can affect transportin 2's efficiency or alter its substrate specificity.
Additional compounds such as ionomycin and thapsigargin act by increasing intracellular calcium levels, which can activate calmodulin-dependent kinases like CaMK. CaMK can phosphorylate various proteins, including those associated with nuclear transport, which can enhance transportin 2's activity. Conversely, okadaic acid and calyculin A inhibit protein phosphatases 1 and 2A, which prevents dephosphorylation, resulting in a hyperphosphorylated state of cellular proteins and potentially enhancing the function of transportin 2. Similarly, epidermal growth factor (EGF) and insulin trigger signaling cascades, specifically the MAPK/ERK and PI3K/Akt pathways, respectively. These pathways can lead to the phosphorylation of nuclear transport machinery components, which could enhance the activity of transportin 2. Bisindolylmaleimide I, though primarily a PKC inhibitor, can result in compensatory activation of other kinases that may affect transportin 2's activity. Lastly, 8-Br-cAMP, a cAMP analog, activates PKA, which then can phosphorylate nuclear transport components, potentially enhancing transportin 2's capacity for nuclear import. Staurosporine, while known as a kinase inhibitor, can also indirectly activate kinases that phosphorylate proteins involved in nuclear transport, thereby affecting transportin 2's function.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA activates protein kinase C (PKC), which can phosphorylate substrates that include elements of the nuclear import machinery, of which transportin 2 is a component. This phosphorylation can enhance the nuclear import function of transportin 2 by increasing its binding affinity to cargo proteins. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin is a calcium ionophore increasing intracellular calcium levels, which can activate calmodulin-dependent kinase (CaMK). CaMK can then phosphorylate components of the nuclear transport process, thereby possibly enhancing the activity of transportin 2 for nuclear import. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Okadaic acid is a potent inhibitor of protein phosphatases 1 and 2A, which leads to increased phosphorylation levels of cellular proteins. Inhibition of these phosphatases can lead to the hyperphosphorylation of factors involved in nuclear transport, potentially enhancing the function of transportin 2. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Similar to okadaic acid, calyculin A is an inhibitor of protein phosphatases 1 and 2A, leading to increased phosphorylation within the cell. By preventing dephosphorylation, it may increase the phosphorylation state of elements within the nuclear import pathway, potentially enhancing transportin 2 activity. | ||||||
Insulin | 11061-68-0 | sc-29062 sc-29062A sc-29062B | 100 mg 1 g 10 g | $156.00 $1248.00 $12508.00 | 82 | |
Insulin can activate the PI3K/Akt pathway, which is known to phosphorylate a wide range of substrates, including those involved in nucleocytoplasmic transport. Activation of this pathway may lead to phosphorylation events that enhance the activity of transportin 2. | ||||||
1,2-Dioctanoyl-sn-glycerol | 60514-48-9 | sc-202397 sc-202397A | 10 mg 50 mg | $47.00 $254.00 | 2 | |
DiC8 is a synthetic analog of diacylglycerol (DAG) and can activate PKC. Activated PKC may phosphorylate nuclear transport machinery components, potentially leading to enhanced activity of transportin 2. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin is an inhibitor of the sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pumps, leading to increased cytosolic calcium levels. Elevated calcium can activate calcium-dependent kinases, which might target and phosphorylate proteins associated with transportin 2, potentially enhancing its transport activity. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $105.00 $242.00 | 36 | |
Although primarily a PKC inhibitor, bisindolylmaleimide I can lead to compensatory mechanisms in cells that upregulate other kinases or phosphatases that impact phosphorylation states. This might incidentally increase phosphorylation of components that interact with or regulate transportin 2, leading to its increased activity. | ||||||
8-Bromo-cAMP | 76939-46-3 | sc-201564 sc-201564A | 10 mg 50 mg | $126.00 $328.00 | 30 | |
8-Br-cAMP is a cAMP analog that activates PKA. PKA then phosphorylates various proteins, potentially including those within the nuclear transport machinery. Enhanced phosphorylation of these components could result in increased functional activity of transportin 2. | ||||||
Staurosporine | 62996-74-1 | sc-3510 sc-3510A sc-3510B | 100 µg 1 mg 5 mg | $82.00 $153.00 $396.00 | 113 | |
Staurosporine is a known kinase inhibitor, but it can have complex effects on cellular signaling pathways leading to an indirect activation of other kinases. Such off-target effects may upregulate kinases that phosphorylate nuclear transport-related proteins, potentially increasing the activity of transportin 2 in transporting cargo into the nucleus. | ||||||