Date published: 2025-9-16

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Cyp21a1 Activators

Cyp21a1 encodes a protein predicted to have 17-hydroxyprogesterone 21-hydroxylase, heme binding, and progesterone 21-hydroxylase activities, and is involved in progesterone metabolic and steroid biosynthetic processes. It is located in the endoplasmic reticulum and membrane and is expressed in various tissues, including the adrenal gland, lung, metanephros, spleen, and testis. The human ortholog, CYP21A2, is implicated in congenital adrenal hyperplasia.

Activation of Cyp21a1 involves complex regulation through direct and indirect mechanisms. Direct activators may include compounds that directly impact the enzymatic activity of Cyp21a1 or its heme-binding capabilities. For example, the steroidogenesis inhibitor Ketoconazole targets cytochrome P450 enzymes, potentially suppressing Cyp21a1 activity by interfering with steroid biosynthetic pathways. On the other hand, indirect activators may modulate signaling pathways involved in steroidogenesis, affecting Cyp21a1 expression and function. The adenylate cyclase activator Forskolin, for instance, influences cAMP levels, potentially activating Cyp21a1 by impacting progesterone metabolic processes and steroid biosynthetic pathways. Overall, the regulation of Cyp21a1 is intricately linked to steroid hormone synthesis, and its activation or suppression involves a network of signaling cascades and cellular processes. Understanding these activation mechanisms provides insights into the intricate regulatory networks governing steroidogenesis and the role of Cyp21a1 in these processes.

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