| 货号 | 10599-1mg |
| 描述 | Cl-amidine is an inhibitor of protein arginine deiminases (PAD; IC50s = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4 in vitro, respectively).1,2 It irreversibly inactivates all four PAD subtypes (kinact/KI = 37,000, 1,200, 2,000, and 13,000 M-1min-1 for PAD1-4, respectively) by covalently modifying an active site cysteine that is important for its catalytic activity.1,3 Cl-amidine is cytotoxic to HL-60, MCF7, and HT-29 cancer cell lines (IC50s = 0.25, 0.05 and 1 μM, respectively).4 In a collagen-induced mouse model of inflammatory arthritis, Cl-amidine dose-dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Luo, Y.,Arita, K.,Bhatia, M., et al. Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterization. Biochemistry 45(39), 11727-11736 (2006). 2.Knuckley, B.,Causey, C.P.,Jones, J.E., et al. Substrate specificity and kinetic studies of PADs 1, 3, and 4 identify potent and selective inhibitors of protein arginine deiminase 3. Biochem. 49(23), 1-28 (2010). 3.Muth, A.,Subramanian, V.,Beaumont, E., et al. Development of a Selective Inhibitor of Protein Arginine Deiminase 2.. J. Med. Chem. 60(7), 3198-3211 (2017). 4.Slack, J.L.,Causey, C.P., and Thompson, P.R. Protein arginine deiminase 4: A target for an epigenetic cancer therapy. Cell Mol. Life Sci. 68(4), 709-720 (2011). 5.Willis, V.C.,Gizinski, A.M.,Banda, N.K., et al. N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-orninthine amide, a protein arginine deiminase inhibitor, reduces the severity of murine collagen-induced arthritis. Journal of Immunology 186, 4396-4404 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 424.8 |
| 分子式 | C14H19ClN4O2 • CF3CO2H |
| CAS号 | 1043444-18-3 |
| 稳定性 | ≥ 1 year |
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