| Description | KN-92 phosphate (KN92-H3PO4) is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM). |
| In vitro | KN-92旨在用作对照化合物，以揭示KN-93的拮抗活性。KN-93抑制了幽门细胞中由组胺诱导的氨基比林摄取(IC50 = 300 nM)。此外，KN-93还被用于指示CaMKII在心肌细胞的Ca2+-诱导Ca2+释放、3T3细胞中5-脂氧合酶的构成性磷酸化、以及结肠癌细胞中Ca2+-依赖性HIF-1α激活中的作用。 |
| Target activity | CaMK II:370 nM(ki) |
| Synonyms | KN-92 磷酸盐, KN92-H3PO4 |
| molecular weight | 554.98 |
| Molecular formula | C24H28ClN2O7PS |
| CAS | 1135280-28-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (99.1 mM) |
| References | 1. Rokhlin OW, Guseva NV, Taghiyev AF et al. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. Cancer Biol Ther. 2010 Feb;9(3):224-35. 2. An P, Zhu JY, Yang Y et al. KN-93, a specific inhibitor of CaMKII inhibits human hepatic stellate cell proliferation in vitro. World J Gastroenterol. 2007 Mar 7;13(9):1445-8. 3. Gao L, Blair LA, Marshall J. et al. CaMKII-independent effects of KN93 and its inactive analog KN92: reversible inhibition of L-type calcium channels. Biochem Biophys Res Commun. 2006 Jul 14;345(4):1606-10. |