Date published: 2025-9-14

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Sp5 Activators

The chemical class referred to as Sp5 Activators comprises a group of small molecules that play a crucial role in modulating the activity of the Sp5 transcription factor. Sp5 is a member of the Sp/KLF (Specificity Protein/Krüppel-Like Factor) family of transcription factors, and it is involved in regulating gene expression by binding to specific DNA sequences known as Sp1 sites. Sp5 has been linked to various cellular processes, including embryonic development, cell proliferation, and differentiation.

One group of chemicals that can activate Sp5 indirectly includes retinoids, such as All-Trans Retinoic Acid (ATRA) and 9-Cis-Retinoic Acid (Isotretinoin). These compounds modulate retinoic acid signaling pathways, which have crosstalk with Sp5 activity. Another set of chemicals includes SB431542 and A83-01, which inhibit the TGF-β signaling pathway. TGF-β has been implicated in the regulation of Sp5 expression, and inhibiting this pathway can alter Sp5-mediated gene expression. Additionally, chemicals like XAV939 and CHIR99021 impact the Wnt signaling pathway, which is intricately linked to Sp5. These compounds indirectly influence Sp5 activity by modulating the signaling cascades that converge on Sp5-regulated gene expression. Furthermore, epigenetic modifiers like Trichostatin A (TSA) and SAHA (Vorinostat) indirectly activate Sp5 by inhibiting histone deacetylases (HDACs), leading to altered chromatin structure and gene expression patterns. Proteasome inhibitors like Bortezomib and MG-132 indirectly affect Sp5 by inhibiting proteasome-mediated protein degradation pathways, stabilizing Sp5 protein levels. Finally, modulators of the Hedgehog signaling pathway, such as Cyclopamine and SANT-1, indirectly impact Sp5 activity by altering the signaling events upstream of Sp5-regulated genes.

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