化合物 Ro 31-8220 Mesylate|T6643|TargetMol

Ro 31-8220 Mesylate
138489-18-6

￥269 1mg 起订

￥662 5mg 起订

￥987 10mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Ro 31-8220 Mesylate

英文名称：: Ro 31-8220 Mesylate

CAS号：: 138489-18-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.18%

产品类别：: 抑制剂

货号：: T6643

Product Introduction

Bioactivity

名称	Ro 31-8220 Mesylate
描述	Ro 31-8220 Mesylate (Bisindolylmaleimide IX mesylate) is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.
细胞实验	Human A549 lung and MCF-7 breast carcinoma cells are obtained from the European Collection of Animal Cell Cultures. Cells (passage number 10-30) are cultured in an atmosphere of 5% carbon dioxide, the former in Ham's F-12 medium with penicillin/streptomycin, the latter in minimum essential medium (Eagle's modification) with additional pyruvate (1 mM) and non-essential amino acids. Both media are supplemented with 10% FCS and glutamine (2 mM). Cells are subcultured routinely twice weekly to maintain logarithmic growth. For cell proliferation studies cells are seeded and incubated with 3 ml of medium including agents, which is replenished at intervals of 48 h (A549) or 72 h (MCF-7). Following incubation for 4 days (A549) or 6 days (MCF-7) with drugs, cell number is assessed using a Coulter Counter Model ZM. In order to achieve PKC depletion, cells are incubated for 24 h with bryostatin 1 (1 μM). Under these conditions growth inhibition caused by bryostatin 1 is negligible. Bryostatin is removed by extensive washing of the cells followed by a 2 h recovery period. In previous work using the A549 cell line this washing procedure has been shown to eliminate bryostatin-mediated effects. The cells are then incubated for a further 24 h with staurosporine, RO 31-8220, UCN-01 or H-7. In some experiments cells are incubated with inhibitor for 48 rather than 24 h, in this case bryostation was not removed and left in the incubate. After removal of agents inhibition of DNA synthesis is evaluated by measurement of [3H]Tdr incorporation into cell. Radioactivity is counted using a Packard 1500 Tricarb scintillation counter. (Only for Reference)
激酶实验	Assay of PKC Activity : Assay mixtures contain 0.2 mg/mL peptide-gamma, 10 μM MgCl2, 0.6 mM CaCl2, 10 μM [γ-32P]ATP, 1.25 mg/mL phosphatidylserine and 1.25 ng/mL phorbol 12-myristate 13-acetate in 20 mM Hepes (pH 7.5), 2 mM EDTA, 1 mM dithiothreitol and 0.02% (w/v) Triton X-100. Peptide-γ is a synthetic peptide, GPRPLFCRKGSLRQKW, resembling the PKC-γ pseudosubstrate site, except that a serine residue replaces the pseudosubstrate alanine, converting the peptide from an inhibitor into a substrat. The assays are started by the addition of 2.5 m-units of enzyme, incubated at 30 °C for 10 min and terminated by spotting on to P81 paper, followed by extensive washing in 75 mM orthophosphoric acid. The papers are then washed in ethanol, dried, and incorporated radioactivity is determined by liquidscintillation spectroscopy.
体外活性	在MLP?/?小鼠体内,Ro 31-8220 (6 mg/kg/d,s.c.)可明显增加心肌收缩力.
体内活性	RO31-8220可有效抑制A549细胞（IC50：0.78 μM）和MCF-7细胞（IC50：0.897 μM）的生长。在儿茶酚胺低反应血小板中,RO31-8220可增强Akt的磷酸化从而使肾上腺素诱导的血小板聚集作用增强。通过抑制apoE基因的囊泡运输到质膜,RO31-8220对载脂蛋白E从原代人巨噬细胞的分泌有显著降低效果,对ApoE的mRNA水平或蛋白水平无显著影响。RO31-8220抑制大鼠脑蛋白激酶C活性（IC50：23 nM）,对PKC-α/β/γ/ε无选择性。此外,RO31-8220对电压依赖性钠离子通道有抑制作用。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 2.8 mg/mL (5 mM) DMSO : 55.4 mg/mL (100 mM)
关键字	inhibit \| Inhibitor \| Ro 318220 Mesylate \| Protein kinase C \| PKC \| Ro 31 8220 Mesylate \| Ro 31-8220 Mesylate \| Bisindolylmaleimide IX Mesylate \| Ro 31-8220
相关产品	Myricitrin \| Midostaurin \| Mitoxantrone dihydrochloride \| DCPLA-ME \| Methyl-Hesperidin \| Darovasertib \| Staurosporine \| R59949 \| α-Vitamin E \| Ro-3306 \| Daphnetin \| N-Desmethyltamoxifen hydrochloride
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 氧化还原化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 细胞骨架化合物库 \| NO PAINS 化合物库 \| TGF-β/Smad靶点化合物库 \| 细胞重编程化合物库

Ro 31-8220 methanesulfonate|||Bisindolylmaleimide IX|||Bisindolylmaleimide IX mesylate|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子