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Bisindolylmaleimide X HCl

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Chemical Structure| 145317-11-9 同义名 : BIM-X hydrochloride;Ro31-8425 hydrochloride;Ro 31-8425;BIM X;Bisindolylmaleimide X (hydrochloride);Bisindolylmaleimide X hydrochloride
CAS号 : 145317-11-9
货号 : A1159144
分子式 : C26H25ClN4O2
纯度 : 99%+
分子量 : 460.955
MDL号 : MFCD04972010
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 20 mg/mL(43.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.85mL

2.17mL

1.08mL

21.69mL

4.34mL

2.17mL
参考文献

[1]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt2)(Pt2):335-7.

[2]Brehmer D, Godl K, Zech B, Wissing J, Daub H. Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors. Mol Cell Proteomics. 2004 May;3(5):490-500.

[3]Xu F, Satoh E, Iijima T. Protein kinase C-mediated Ca2+ entry in HEK 293 cells transiently expressing human TRPV4. Br J Pharmacol. 2003 Sep;140(2):413-21.

[4]Role of PKC and ERK Signaling in Epidermal Blistering and Desmosome Regulation in Pemphigus

[5]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt2)(Pt2):335-7.