Date published: 2025-10-12

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Grap Activators

Chemicals that indirectly lead to the functional activation of the GRAP protein do so by modulating various signaling pathways and cellular processes that GRAP is known to be involved in. Lithium Chloride, for instance, inhibits glycogen synthase kinase 3 (GSK-3), a negative regulator of the Wnt signaling pathway. This inhibition can lead to the stabilization and accumulation of β-catenin, a component that can drive the transcription of various genes, potentially including GRAP, thereby increasing its expression and activity. Forskolin, Isoproterenol, and IBMX all act to increase the levels of cyclic AMP (cAMP) within cells, which activates protein kinase A (PKA). The activation of PKA can lead to a range of downstream effects including the phosphorylation of proteins that could enhance the activation state or expression of GRAP.

Similarly, ionomycin, by increasing intracellular calcium levels, can activate calcium-dependent signaling pathways, which might influence the activity of GRAP. TPA is a well-known activator of protein kinase C (PKC), which plays a significant role in intracellular signaling and can phosphorylate proteins within the Ras-MAPK pathway where GRAP functions. Dibutyryl-cAMP, as a cAMP analog, serves a similar function to Forskolin by activating PKA and potentially affecting GRAP activity. Anisomycin acts as a stress-activated protein kinase activator, which can lead to the activation of the MAPK pathway, possibly resulting in the activation of GRAP through its involvement in this pathway. Sodium Orthovanadate serves as a phosphatase inhibitor, which can lead to increased phosphorylation levels within the cell, affecting various signaling pathways including those that GRAP is part of. Okadaic Acid, by inhibiting protein phosphatases, can also result in enhanced phosphorylation signaling, potentially affecting GRAP's activation state. Piceatannol and LY294002 modulate kinase activity, thereby influencing signaling pathways and possibly leading to changes in the activation state of GRAP, as these kinases are part of the complex cellular signaling networks that GRAP is involved in.

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