CAS:145317-11-9Bisindolylmaleimide X HCl

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Bisindolylmaleimide xHCl is a potent protein kinase C (PKC) inhibitor.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

145317-11-9

储存条件

分子式

C26H25ClN4O2

运输

蓝冰

分子量

460.96

别名

溶解度

DMSO	65.0 mg/mL (141.0 mM)
Water	insoluble

动物实验配方

生物活性

描述The protein kinase C (PKC) family of isozymes are involved in various cellular physiological processes, including cell proliferation, differentiation, apoptosis, glycogenolysis, and ion channel regulation. Bisindolylmaleimide X HCl (BisX) is a PKC inhibitor with an IC50 value of 15nM against rat brain PKC. It also inhibits PKCα, βI, βII, γ, and ε with IC50 values of 8, 8, 14, 13, and 39nM, respectively^[1]. Moreover, BisX was shown as a potent antagonist of cyclin-dependent kinase 2 with an IC50 value of 200nM^[2]. In HEK 293 cells, a 60-min pre-incubation with BisX (60nM) inhibited PMA-induced Ca²⁺ entry without affecting the basal calcium level. The pre-exposure of BisX also significantly prolonged the mean time-to-peak effect of 4α-PDD (314.3±63.5s) in comparison to non-BisX-treated cells (157.9±16.1s)^[3]. In human skin biopsies received transdermal injection of pemphigus vulgaris-IgG, treatment with BisX (1μM) one hour before the injection significantly reduced the number of desmosomes as compared to normal control samples (0.33 ± 0.05/μm vs. 0.69 ± 0.02/μm)^[4].
作用机制Bisindolylmaleimide X HCl competes with ATP for binding to PKC^[5].
动物研究
剂量
Rat: 10 mg/kg - 50 mg/kg^[1] (p.o., BID); 10 mg/kg^[1] (i.v.)

给药途径
p.o., i.v.