| CAS NO: | 138489-18-6 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 553.65 |
| Cas No. | 138489-18-6 |
| Formula | C25H23N5O2S·CH4O3S |
| Solubility | ≥27.7 mg/mL in DMSO; insoluble in EtOH; ≥22.6 mg/mL in H2O |
| Chemical Name | methanesulfonic acid;3-[3-[4-(1-methylindol-3-yl)-2,5-dioxopyrrol-3-yl]indol-1-yl]propyl carbamimidothioate |
| Canonical SMILES | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N.CS(=O)(=O)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Ro 31-8220 Mesylate是一种蛋白激酶C(PKC)的选择性抑制剂,对PKC α\PKC βI\PKC βII\PKC γ和PKC ε的IC50值分别为5\24\14\27和24 nM[1].
PKC是一种单体的Ca2+和磷脂依赖的Ser/Thr蛋白激酶,在生长因子激活的信号通路和恶性转化中扮演重要角色[1].
Ro 31-8220 Mesylate是一种PKC的选择性抑制剂.另外,Ro 31-8220可提高生长因子刺激的c-Jun表达,但抑制MKP-1和c-Fos表达.Ro-31-8220可以PKC依赖的方式强力地刺激应力活化的蛋白激酶JNK1[2].在外周血单核细胞中,Ro 31-8220可抑制有丝分裂原诱导的白细胞介素(IL)-2生成和IL-2依赖的T淋巴母细胞增殖,IC50值分别为80和350 nM.另外,Ro 31-8220(400 nM)可抑制27%的IL-2Rα(CD25)表达,表明Ro 31-8220可抑制早期和晚期T细胞活化[3].
在大鼠脂肪细胞和L6肌小管中,RO 31-8220可活化c-Jun N端激酶(JNK)和糖原合酶(GS),并可刺激葡萄糖并入糖原.RO 31-8220可以PKC依赖的方式抑制胞外响应激酶1和2(ERK1/2)活性[4].
参考文献：
[1]. Wilkinson SE, Parker PJ, Nixon JS. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J, 1993, 294 ( Pt 2): 335-337.
[2]. 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.
[3]. Geiselhart L, Conti DJ, Freed BM. RO 31-8220, a novel protein kinase C inhibitor, inhibits early and late T cell activation events. Transplantation, 1996, 61(11): 1637-1642.
[4]. Standaert ML, Bandyopadhyay G, Antwi EK, et al. RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin.
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