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Ro 31-8220 mesylate

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Chemical Structure| 138489-18-6 同义名 : Ro 31-8220 methanesulfonate;Bisindolylmaleimide IX mesylate;Ro 31-8220;BIM IX;Bisindolylmaleimide IX (mesylate);Bisindolylmaleimide IX
CAS号 : 138489-18-6
货号 : A350912
分子式 : C26H27N5O5S2
纯度 : 99%+
分子量 : 553.653
MDL号 : MFCD03788207
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(63.22 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
靶点

  • PKCβ

    PKCβ1, IC50:24 nM

    PKCβ2, IC50:14 nM

  • PKCγ

    PKCγ, IC50:27 nM

  • PKCε

    PKCε, IC50:24 nM

  • PKCα

    PKCα, IC50:5 nM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.03mL

1.81mL

0.90mL

18.06mL

3.61mL

1.81mL
参考文献

[1]Davies SP, Reddy H, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt1):95-105.

[2]Wilkinson SE, Parker PJ, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7.

[3]Koivunen J, Aaltonen V, Peltonen J. Protein kinase C (PKC) family in cancer progression. Cancer Lett. 2006; 235(1): 1-10

[4]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993; 294:335-337

[5]Wen HC, Huang WC, Ali A, Woodgett JR, Lin WW. Negative regulation of phosphatidylinositol 3-kinase and Akt signaling pathway by PKC. Cell Signal. 2003; 15(1): 37-45

[6]Beltman J, McCormick F, Cook SJ. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996;271(43):27018-27024

[7]Bailey TA, Luan H, Tom E, et al. A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells. J Biol Chem. 2014;289(44):30443-30458

[8]Choi B, Lee HW, Mo S, et al. Inositol 1,4,5-trisphosphate 3-kinase A overexpressed in mouse forebrain modulates synaptic transmission and mGluR-LTD of CA1 pyramidal neurons. PLoS One. 2018;13(4):e0193859

[9]Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993; 294:335-337