KN-92 phosphate 是 KN-93 的非活性衍生物,不能抑制 CaM 激酶活性。它可作为阐明 KN-93 的拮抗活性的对照化合物。KN-93 能够渗透细胞,是一种可逆的 CaMKII 竞争性抑制剂。
产品描述
KN-92 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).
体外活性
KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 inhibits histamine-induced aminopyrine uptake in parietal cells (IC50 = 300 nM). KN-93 has been used to implicate roles for CaMKII in Ca2+-induced Ca2+ release in cardiac myocytes, constitutive phosphorylation of 5-lipoxygenase in 3T3 cells, and Ca2+-dependent activation of HIF-1α in colon cancer cell.
Cas No.
1135280-28-2
分子式
C24H28ClN2O7PS
分子量
554.98
别名
KN-92 磷酸盐;KN92-H3PO4
储存和溶解度
DMSO:5.6 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years