N-[2-[N-(4-氯肉桂)-N-甲基氨基]苯基]-N-(2-羟乙基)-4-甲氧苯磺酰胺磷酸酯盐
中文名称:
N-[2-[N-(4-氯肉桂)-N-甲基氨基]苯基]-N-(2-羟乙基)-4-甲氧苯磺酰胺磷酸酯盐
中文同义词:
N-[2-[N-(4-氯肉桂)-N-甲基氨基]苯基]-N-(2-羟乙基)-4-甲氧苯磺酰胺磷酸酯盐 100MG;N-[2-[[[3-(4-氯苯基)-2-丙烯-1-基]甲基氨基]甲基]苯基]-N-(2-羟基乙基)-4-甲氧基苯磺酰胺;N-[2-[N-(4-氯肉桂)-N-甲基氨基]苯基]-N-(2-羟乙基)-4-甲氧苯磺酰胺磷酸酯盐;CA2+/钙调蛋白依赖性激酶Ⅱ(CA2+/CAM PKⅡ)竞争性抑制剂KN-3;N-[2-[[[3-(4-氯苯基)烯丙基](甲基)氨基]甲基]苯基]-N-(2-羟乙基)-4-甲氧基苯磺酰胺;神经元CAMK-II抑制剂(KN-93);(E)-N-(2-(((3-(4-氯苯基)烯丙基)(甲基)氨基)甲基)苯基)-N-(2-羟乙基)-4-甲氧基苯磺酰胺
英文名称:
KN-93
英文同义词:
2-[N-(2-HYDROXYETHYL)-N-(4-METHOXYBENZENESULFONYL)]AMINO-N-(4-CHLOROCINNAMYL)-N-METHYLBENZYLAMINE;METHOXYBENZENE-SULFONAMIDE;KN-93;KN-93, WATER-SOLUBLE;N-[2-[[[3-(4-CHLOROPHENYL)-2-PROPENYL]METHYLAMINO]METHYL]PHENYL]-N-(2-HYDROXYETHYL)-4-METHOXY-BENZENESULFONAMIDE PHOSPHATE;N-[2-[[[3-(4-CHLOROPHENYL)-2-PROPENYL]METHYLAMINO]METHYL]PHENYL]-N-(2-HYDROXYETHYL)-4-METHOXYBENZENESULPHONAMIDE;N-[2-N-4-CHLOROCINNAMYL-N-METHYLAMINOMETHYLPHENYL]-N-[2-HYDROXYETHYL]-4-METHOXYBENZENESULFONAMIDE;KN-93,98%
CAS号:
139298-40-1
分子式:
C26H29ClN2O4S
分子量:
501.04
EINECS号:
相关类别:
细胞生物学试剂;小分子抑制剂，天然产物;小分子抑制剂;Inhibitors;Aromatics;Intermediates Fine Chemicals;Pharmaceuticals;Protein Kinase;Sulfur Selenium Compounds
Mol文件:
139298-40-1.mol
密度
1.288
储存条件
2-8°C
溶解度
DMSO: 1 mg/mL
形态
Off-white solid
颜色
white
InChIKey
LLLQTDSSHZREGW-AATRIKPKSA-N
CAS 数据库
139298-40-1(CAS DataBase Reference)
生物活性
KN-93 是一种具有细胞渗透性和竞争性的 Ca2+/calmodulin-dependent protein kinase II (CaMK-II) 的可逆抑制剂，对于兔心肌 CaM 激酶活性的Ki值为2.58 μM。
靶点
Target Value
CaMKII
(Cell-free assay) 2.58 μM(Ki)
Target
Value
CaMKII
(Cell-free assay)
2.58 μM(Ki)
体外研究
After 2 days of KN-93 treatment, 95% of cells are arrested in G1. G1 arrest is reversible; 1 day after KN-93 release, a peak of cells had progressed into S and G2-M. KN-93 also blocks cell growth stimulated by basic fibroblast growth factor, platelet-derived growth factor-BB, and epidermal growth factor in NIH 3T3 fibroblasts. KN-93 inhibits the H + , K + -ATPase activity but strongly dissipates the proton gradient formed in the gastric membrane vesicles and reduces the volume of luminal space. KN-93 (0.5 μM) prevents increased LV developed pressure during action potential prolongation and early afterdepolarizations. Ca 2+ -independent CaM kinase activity is increased during early afterdepolarizations and this increase is prevented by KN-93. KN-93 (10 μM )significantly inhibits the activation of CaMKII/NF-κB signaling induced by elevated glucose, and subsequently decreases the expression of VEGF, iNOS and ICAM-1 in Müller cells.
体内研究
KN-93 (1 mg/kg/day, i.p.) inhibits retinal vascular leakage induced by diabetes, and suppresses phosphorylation of CaMKII and NF-κB in diabetic retina.
危险品标志
Xn
危险类别码
20/21/22
安全说明
22-24/25-36/37
WGK Germany
3
海关编码
29299000
