3-[1-[3-(二甲基氨基)丙基]-1H-吲哚-3-基]-4-(1H-吲哚-3-基)-1H-吡咯-2,5-二酮单盐酸盐;二吲哚基顺丁烯二酰亚胺 I盐酸;双吲哚基马来酰亚胺 I .盐酸盐
英文名称
Bisindolylmaleimide I hydrochloride
英文别名
1H-Pyrrole-2,5-dione,3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-, hydrochloride(1:1);1H-Pyrrole-2,5-dione,3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-, hydroch...;3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione,hydrochloride;BISINDOLYLMALEIMIDE I, HYDROCHLORIDE SALT;2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)maleimide, HCl;3-[1-(Dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride;AC1O4WDA;BIM I;Bisindolylmaleimide;Bisindolylmaleimide I;Bisindolylmaleimide I hydrochloride;Bisindolylmaleimide I, HCl;Go-6850;BIM 1 hydrochloride;BisindolylMaleiMide I( Hydrochloride Salt);3-[1-[3-(Dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione monohydrochloride;BisindolylMaleiMide I . hydrochloride [GF-109203K;3-[1-(dimethylaminopropyl)indol-3-yl]-4-(indol-3-yl)maleimide hydrochloride
Cas No.
176504-36-2
分子式
C25H24N4O2.HCl
分子量
448.94
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Bisindolylmaleimide I (GF109203X) hydrochloride 是一种具有细胞渗透性和可逆性的 PKC 抑制剂 (对 PKCα, PKCβI, PKCβII, and PKCγ 的 IC50 分别为 20 nM、17 nM、16 nM 和 20 nM)。Bisindolylmaleimide I hydrochloride 也是一种 GSK-3 抑制剂。
生物活性
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC 50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.
性状
Solid
IC50 & Target[1][2]
Bovine brain PKC 10 nM (IC50) PKC-βII 16 n
体外研究(In Vitro)
Bisindolylmaleimide I hydrochloride (5 μM) 抑制 α-凝血酶诱导的 P47 磷酸化。Bisindolylmaleimide I hydrochloride (0-1 μM) 抑制静息态 swiss 3T3 细胞中的 DNA 合成。Bisindolylmaleimide I hydrochloride (5 μM) 可将脂肪细胞裂解物中的 GSK-3 活性降低至 25.1±4.3%。Bisindolylmaleimide I hydrochloride (10 μM,24 小时) 抑制 PC3 细胞释放外泌体和微泡 (EMV)。Bisindolylmaleimide I hydrochloride (10 μM,24 小时) 增强 5-fluorouracil (HY-90006) 的细胞毒性。 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Bisindolylmaleimide I hydrochloride (0.02 mg/kg,腹腔注射.) 降低小鼠机械通气 (MV) 组中升高的 NLRP3、P-PKCɑ 和 PKCɑ 水平。
Bisindolylmaleimide I hydrochloride (0-20 mg/kg,腹腔注射) 降低了鼩鼱中喹吡罗诱导的呕吐的平均频率。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Toullec D, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. [2]. Vetri F, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (139.22 mM; ultrasonic and warming and heat to 60°C)配制储备液