Kap95 Activators
Kap95 activators are a specialized class of chemical compounds that target the cellular machinery responsible for nuclear import, specifically by enhancing the function of the karyopherin beta protein Kap95. Kap95, a crucial component of the nuclear pore complex, functions as an import receptor that facilitates the transport of proteins from the cytoplasm into the nucleus. Its activity is pivotal in maintaining cellular homeostasis and regulating gene expression by ensuring a timely and efficient translocation of proteins carrying nuclear localization signals (NLS). Activators of Kap95 work by binding to its recognition domains, thereby stabilizing the receptor-protein complex, which results in a more efficient translocation process. Some activators may also enhance Kap95's affinity for the RanGTPase system, a vital player in the disassembly of the Kap95-protein complex once it reaches the nuclear side, thereby resetting the receptor for further rounds of transport.
The mechanism by which Kap95 activators function can be multifaceted. Certain molecules may directly bind to Kap95, inducing a conformational change that promotes a higher affinity for its cargo. Others may work indirectly, by modulating the RanGTPase system to favor the formation of the Kap95-protein complex in the cytoplasm and its subsequent disassembly in the nucleus. This precise modulation is crucial as it dictates the directionality of transport and ensures that proteins are only imported into the nucleus, preventing their accidental export. By enhancing the function of Kap95, these activators play a significant role in cellular processes that demand rapid and increased import of nuclear proteins, such as during the cell cycle, or in response to stress signals requiring a prompt nuclear accumulation of transcription factors, DNA repair enzymes, or other regulatory proteins. The result is a finely tuned orchestration of protein localization, which is essential for the cell's response to internal and external cues, maintaining cellular functionality and integrity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin is a diterpene that directly stimulates adenylyl cyclase, leading to increased levels of cyclic AMP (cAMP) in cells. Elevated cAMP can enhance the nuclear import function of Kap95 by promoting the assembly of Kap95 with importin-α and the cargo protein. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
Isobutylmethylxanthine (IBMX) is a non-selective inhibitor of phosphodiesterases, which increases intracellular cAMP by preventing its breakdown. This indirectly promotes Kap95's role in nuclear transport by sustaining the cAMP-mediated signaling pathways. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $285.00 $520.00 $1300.00 | 78 | |
Okadaic acid is a potent inhibitor of protein phosphatases 1 and 2A, altering phosphorylation states within the cell. This can modulate the phosphorylation status of Kap95, thereby influencing its interaction with transport substrates. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A sc-24000B sc-24000C | 10 µg 100 µg 500 µg 1 mg | $160.00 $750.00 $1400.00 $3000.00 | 59 | |
Calyculin A, like okadaic acid, is an inhibitor of protein phosphatases 1 and 2A. It may enhance the activity of Kap95 by maintaining its phosphorylation state, which is crucial for its interaction with RanGTP and importin-β. | ||||||
(−)-Epigallocatechin Gallate | 989-51-5 | sc-200802 sc-200802A sc-200802B sc-200802C sc-200802D sc-200802E | 10 mg 50 mg 100 mg 500 mg 1 g 10 g | $42.00 $72.00 $124.00 $238.00 $520.00 $1234.00 | 11 | |
Epigallocatechin Gallate (EGCG) is a polyphenol that can inhibit various kinases, potentially altering the phosphorylation landscape in the cell. This could enhance Kap95-mediated nuclear transport by affecting the accessory proteins that regulate Kap95's activity. | ||||||
(±)-S-Nitroso-N-acetylpenicillamine | 79032-48-7 | sc-200319B sc-200319 sc-200319A | 10 mg 20 mg 100 mg | $73.00 $112.00 $367.00 | 18 | |
S-Nitroso-N-Acetylpenicillamine (SNAP) releases nitric oxide, which can lead to the S-nitrosylation of proteins and affect their function. S-nitrosylation of components in the nuclear import pathway may enhance Kap95's ability to transport cargo proteins. | ||||||
Zaprinast (M&B 22948) | 37762-06-4 | sc-201206 sc-201206A | 25 mg 100 mg | $103.00 $245.00 | 8 | |
Zaprinast is another phosphodiesterase inhibitor, increasing cAMP levels. It can indirectly enhance the activity of Kap95 by similar mechanisms as Forskolin and IBMX, promoting nuclear import processes. | ||||||
Taxol | 33069-62-4 | sc-201439D sc-201439 sc-201439A sc-201439E sc-201439B sc-201439C | 1 mg 5 mg 25 mg 100 mg 250 mg 1 g | $40.00 $73.00 $217.00 $242.00 $724.00 $1196.00 | 39 | |
Paclitaxel stabilizes microtubules and can indirectly influence the spatial distribution and trafficking of nuclear transport receptors including Kap95, potentially enhancing its ability to import proteins into the nucleus. | ||||||
Vinblastine | 865-21-4 | sc-491749 sc-491749A sc-491749B sc-491749C sc-491749D | 10 mg 50 mg 100 mg 500 mg 1 g | $100.00 $230.00 $450.00 $1715.00 $2900.00 | 4 | |
Vinblastine disrupts microtubules and can alter the cellular transport processes. This disruption could enhance Kap95 activity by affecting the distribution and localization of Kap95 and its cargo. | ||||||
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 is an ionophore that increases intracellular calcium levels, which can modulate various signaling pathways. Elevated calcium may enhance Kap95's interactions with its import substrates due to changes in phosphorylation states of regulatory proteins. | ||||||