C 21

Product Name:C 21

CAS No:1229236-78-5

Purity:95%

Molar Mass:2166.92

Chemical Formula:C90H161ClN36O24

Storage:Store at -20 degrees Celsius

Sequence:Ac-SG-[N5-(2-Chloro-1-iminoethyl)]-Orn-GKGGKGLGKGGAKRHRKV

Target:PRMT1

Application:C 21 is a selective inhibitor of PRMT1 (Protein Arginine Methyltransferase 1), an enzyme that catalyzes the methylation of arginine residues in proteins. PRMT1 plays a critical role in regulating gene expression, signal transduction, and other cellular processes by modifying histones and non-histone proteins. Inhibitors like C 21 are valuable tools in research exploring the functional roles of PRMT1, particularly in cancer and other diseases where abnormal methylation patterns contribute to disease progression. C 21 helps block PRMT1 activity, allowing researchers to study its biological implications and potential therapeutic applications.

Current Research:

C 21 (CAS: 1229236-78-5) is a synthetic peptide that functions as a potent, irreversible, and selective inhibitor of protein arginine methyltransferase 1 (PRMT1), an enzyme involved in the methylation of arginine residues on histones and other proteins. This post-translational modification plays a crucial role in regulating gene expression and various cellular processes.

Structural Characteristics

The peptide sequence of C 21 is Ac-Ser-Gly-[N5-(2-chloro-1-iminoethyl)]-Orn-Gly-Lys-Gly-Gly-Lys-Gly-Leu-Gly-Lys-Gly-Gly-Ala-Lys-Arg-His-Arg-Lys-Val, with a molecular formula of C₉₀H₁₆₁ClN₃₆O₂₄ and a molecular weight of 2166.92 g/mol. The incorporation of a chloroacetamidine group at the ornithine residue is critical for its inhibitory activity.

Mechanism of Action

C 21 inhibits PRMT1 by covalently modifying the enzyme's active site, leading to irreversible inactivation. It exhibits an IC₅₀ of 1.8 μM for PRMT1 and shows selectivity over other PRMT isoforms, with an IC₅₀ of 8.8 μM for PRMT6 and significantly higher IC₅₀ values for PRMT3 and CARM1, indicating over 250-fold selectivity for PRMT1.

Research Applications

Due to its specificity and potency, C 21 is utilized in research to study the biological functions of PRMT1, including its role in gene regulation, signal transduction, and the development of diseases such as cancer. By inhibiting PRMT1, researchers can investigate the effects of reduced arginine methylation on cellular processes and assess the therapeutic potential of targeting PRMT1 in various pathological conditions.

Conclusion

C 21 serves as a valuable tool in epigenetic research, enabling the exploration of PRMT1's functions and its implications in health and disease. Its high selectivity and irreversible inhibition make it particularly useful for dissecting the specific contributions of PRMT1-mediated arginine methylation in complex biological systems.

Reference:

Obianyo, O., Causey, C. P., Osborne, T., Jones, J. E., Lee, Y. H., Stallcup, M. R., & Thompson, P. R. (2010). A chloroacetamidine-based inactivator of protein arginine methyltransferase 1: design, synthesis, and in vitro and in vivo evaluation. Chembiochem: a European journal of chemical biology, 11(9), 1219.