138489-18-6|Ro 31-8220 mesylate|CsnPharm

CAS No.: 138489-18-6

Ro 31-8220 mesylate/Ro 31-8220 甲磺酸盐 Catalog No. CSN11854

Synonyms: Ro 31-8220 methanesulfonate;Bisindolylmaleimide IX mesylate;Bisindolylmaleimide IX (mesylate)

Ro 31-8220 mesylate is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.

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描述The protein kinase C (PKC) family consists of at least 12 serine-threonine kinases and can be classified into three major groups: classical, novel, and atypical. Under physiological conditions, activation PKC is a response to various growth factors^[3]. Ro 31-8220 Mesylate is a potent inhibitor with IC50 values of 5nM, 24nM, 14nM, 27nM and 24nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively^[4]. In vitro, treatment with 3 μM Ro 31-8220 Mesylate significantly increased Akt/PKB phosphorylation at Ser 473 within 60 mins in A549 cells^[5]. Ro 31-8220 Mesylate activated JNK1 with EC50 value of 2.3 nM. Ro 31-8220 Mesylate also inhibited growth factor-stimulated c-Fos expression and amplified c-Jun expression in Rat-1 fibroblasts^[6]. Ro 31-8220 Mesylate diminished the 17AAG-induced clearance ErbB2 from the cell surface at the concentration of 1 μM in SKBR-3 cells^[7]. Treatment of hippocampal slice prior to DHPG administration with Ro 31-8220 Mesylate at the concentration of 1 μM significantly reduced the baseline PPF ratio by approximately 7%, indicating that inhibiting basal PKC activity increased presynaptic release in WT mice^[8].
作用机制Ro 31-8220 Mesylate carries a straight-chain alkyl side-chain bearing the cationic substituent which inhibits the PKC-α, PKC-β, PKC-γ and PKC-ε^[9].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8062 mL
- 9.0309 mL
- 18.0619 mL
- 5 mM
- 0.3612 mL
- 1.8062 mL
- 3.6124 mL
- 10 mM
- 0.1806 mL
- 0.9031 mL
- 1.8062 mL

技术信息

CAS号

138489-18-6

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H27N5O5S2

运输

蓝冰

分子量

553.65

别名

Ro 31-8220 methanesulfonate;Bisindolylmaleimide IX mesylate;Bisindolylmaleimide IX (mesylate);BIM IX;Ro 31-8220;RO31-8220 mesylate;Bisindolylmaleimide IX

溶解度

DMSO	50.0 mg/mL (90.3 mM)
Water	insoluble

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Ro 31-8220 mesylate/Ro 31-8220 甲磺酸盐 Catalog No. CSN11854

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