CEP152 Inhibitors
Chemical inhibitors of CEP152 include a range of compounds that target various aspects of the cell cycle, particularly mitosis, where CEP152 plays a critical role in centrosome duplication and spindle formation. Monastrol, an inhibitor of the mitotic kinesin Eg5, leads to the formation of monopolar spindles, disrupting the functions of CEP152 in centrosome and spindle dynamics. Similarly, S-Trityl-L-cysteine and Dimethylenastron also target Eg5, affecting spindle pole separation and indirectly inhibiting CEP152's role in the centrosome and spindle assembly. Ispinesib, by selectively inhibiting the kinesin spindle protein (KSP), destabilizes spindle microtubules, which can impede the proper function of CEP152 in microtubule nucleation.
Furthermore, a group of Aurora kinase inhibitors, including VX-680, ZM447439, Hesperadin, MLN8054, MLN8237, Barasertib, and PHA-680632, disrupt the phosphorylation state of proteins associated with centrosome maturation and function. CEP152's interaction with Aurora A kinase is essential for its role in centrosome duplication, and thus, inhibitors like VX-680, MLN8054, and MLN8237 can impair CEP152 activity by inhibiting Aurora A. Barasertib and Hesperadin, targeting Aurora B, could compromise the mitotic processes that CEP152 supports, given Aurora B's role in chromosome segregation and cytokinesis. PHA-680632, with its broader range of inhibition, affects both Aurora A and B kinases, altering the phosphorylation of substrates necessary for processes involving CEP152. Additionally, Maribavir, though an outlier as it is primarily known for targeting viral kinases, can have off-target effects on human kinases, which may indirectly affect kinase interactions with CEP152, thereby impeding its role in centrosome cycling and the proper function of the mitotic spindle.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Monastrol | 254753-54-3 | sc-202710 sc-202710A | 1 mg 5 mg | $120.00 $233.00 | 10 | |
Monastrol is a cell-permeable small molecule inhibitor of the mitotic kinesin Eg5. CEP152 is essential for centrosome duplication and maturation, which is a process closely linked to the mitotic spindle assembly. By inhibiting Eg5, Monastrol causes the formation of monopolar spindles, which could disrupt the functions of CEP152 in centrosome and spindle dynamics. | ||||||
S-Trityl-L-cysteine | 2799-07-7 | sc-202799 sc-202799A | 1 g 5 g | $31.00 $65.00 | 6 | |
S-Trityl-L-cysteine is a selective inhibitor of Eg5, a kinesin associated with spindle formation. By disrupting the function of Eg5, this compound indirectly affects spindle pole separation and thus can inhibit CEP152's role in centrosome duplication and spindle formation. | ||||||
Eg5 Inhibitor III, Dimethylenastron | 863774-58-7 | sc-221576 sc-221576A sc-221576B sc-221576C | 1 mg 5 mg 10 mg 25 mg | $38.00 $132.00 $244.00 $516.00 | 1 | |
Dimethylenastron is a potent inhibitor of the mitotic motor protein Eg5, leading to the formation of monoastral spindles. This disruption of the spindle assembly process can functionally inhibit CEP152's involvement in organizing and maintaining the spindle poles. | ||||||
Ispinesib | 336113-53-2 | sc-364747 | 10 mg | $495.00 | ||
Ispinesib selectively inhibits the kinesin spindle protein (KSP), which is implicated in microtubule function. As CEP152 has a role in microtubule nucleation at the centrosome, the inhibition of KSP by Ispinesib can impede the proper function of CEP152 by destabilizing spindle microtubules. | ||||||
Tozasertib | 639089-54-6 | sc-358750 sc-358750A | 25 mg 50 mg | $61.00 $85.00 | 4 | |
VX-680 (also known as MK-0457) is an Aurora kinase inhibitor. CEP152 interacts with Aurora A kinase for proper centrosome maturation. By inhibiting Aurora kinases, VX-680 can impede centrosome function and spindle assembly, indirectly inhibiting CEP152 activity. | ||||||
ZM-447439 | 331771-20-1 | sc-200696 sc-200696A | 1 mg 10 mg | $150.00 $349.00 | 15 | |
ZM447439 is an Aurora kinase inhibitor that may disrupt the phosphorylation state of proteins associated with centrosome maturation and function, a process in which CEP152 is involved. This can lead to aberrant spindle formation and functionally inhibit CEP152. | ||||||
Hesperadin | 422513-13-1 | sc-490384 | 10 mg | $304.00 | ||
Hesperadin is an inhibitor of Aurora B kinase, which is involved in chromosome alignment and segregation. By inhibiting Aurora B, Hesperadin can affect centrosome-associated functions, indirectly inhibiting CEP152's role in mitosis. | ||||||
MLN 8054 | 869363-13-3 | sc-484828 | 5 mg | $398.00 | ||
MLN8054 is a selective inhibitor of Aurora A kinase. Since CEP152 requires interaction with Aurora A for its role in centrosome duplication, inhibiting Aurora A with MLN8054 can functionally inhibit the activity of CEP152. | ||||||
MLN8237 | 1028486-01-2 | sc-394162 | 5 mg | $220.00 | ||
MLN8237, also known as Alisertib, is an Aurora A kinase inhibitor. By specifically targeting Aurora A, MLN8237 can inhibit centrosome maturation and spindle assembly where CEP152 is critical, thus indirectly inhibiting CEP152 function. | ||||||