恩扎妥林|T6280|TargetMol

Enzastaurin
170364-57-5

￥198 1mg 起订

￥443 5mg 起订

￥732 10mg 起订

上海更新日期：2024-09-23

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

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邮箱：marketing@targetmol.com

产品详情:

中文名称：: 恩扎妥林

英文名称：: Enzastaurin

CAS号：: 170364-57-5

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.24%

产品类别：: 抑制剂

货号：: T6280

Product Introduction

Bioactivity

名称	Enzastaurin
描述	Enzastaurin (LY317615) (LY317615) is an effective PKCβ selective inhibitor (IC50: 6 nM), 6- to 20-fold selectivity against PKCα/γ/ε.
细胞实验	Induction of apoptosis by enzastaurin is measured by nucleosomal fragmentation and terminal deoxynucleotidyl transferase-mediated nick-end labeling (TUNEL) and staining in HCT116 and U87 mg cell lines. Briefly, 5 × 103 cells are plated per well in 96-well plates (1% FBS-supplemented media conditions), incubated with or without Enzastaurin for 48 to 72 hours. The absorbance values are normalized to those from control-treated cells to derive a nucleosomal enrichment factor at all concentrations as per the manufacturer's protocol. The concentrations studied ranges from 0.1 to 10 μM. In situ TUNEL staining is assayed with the In situ Cell Death Detection, Fluorescein kit. Cells (7.5 ×104) are plated per well in 6-well plates and incubated 72 hours in 1% FBS-supplemented media Enzastaurin. Fluorescein-labeled DNA strand breaks are detected with the BD epics flow cytometer. Ten thousand, single-cell, FITC-staining events are collected for each test. (Only for Reference)
激酶实验	Kinase inhibition assays: The inhibition of PKCβII, PKCα, PKCε, or PKCγ activity by enzastaurin is determined using a filter plate assay format measuring 33P incorporation into myelin basic protein substrate. Reactions are done in 100 μL reaction volumes in 96-well polystyrene plates with final conditions as follows: 90 mM HEPES (pH 7.5), 0.001% Triton X-100, 4% DMSO, 5 mM MgCl2, 100 μM CaCl2, 0.1 mg/mL phosphatidylserine, 5 μg/mL diacetyl glyerol, 30 μM ATP, 0.005 μCi/μL 33ATP, 0.25 mg/mL myelin basic protein, serial dilutions of enzastaurin (1-2,000 nM), and recombinant human PKCβII, PKCα, PKCε, or PKCγ enzymes (390, 169, 719, or 128 pM, respectively). Reactions are started by addition of the enzyme and incubated at room temperature for 60 minutes. They are then quenched with 10% H3PO4, transferred to multiscreen anionic phosphocellulose 96-well filter plates, incubated for 30 to 90 minutes, filtered and washed with 4 volumes of 0.5% H3PO4 on a vacuum manifold. Scintillation cocktail is added and plates are read on a Microbeta scintillation counter. IC50 values are determined by fitting a three-variable logistic equation to the 10-point dose-response data using ActivityBase 4.0.
体外活性	Enzastaurin 在所有研究的MM细胞系中，包括MM.1S、MM.1R、RPMI 8226 (RPMI)、RPMI-Dox40 (Dox40)、NCI-H929、KMS-11、OPM-2和U266，均显示出显著的剂量依赖性生长抑制作用，IC50范围为0.6-1.6 μM。Enzastaurin 直接作用于人类肿瘤细胞，诱导凋亡并抑制培养肿瘤细胞的增殖。Enzastaurin 还抑制了GSK3βser9、核糖体蛋白S6S240/244和AKTThr308的磷酸化，但对VEGFR磷酸化无直接影响。[1] Enzastaurin 提高了CTCL恶性淋巴细胞的凋亡率。与GSK3抑制剂联合使用时，enzastaurin 显示出提高的细胞毒性水平。使用enzastaurin与GSK3抑制剂AR-A014418的组合处理，增加了β-catenin总蛋白水平和β-catenin介导的转录。阻断β-catenin介导的转录或小发夹RNA (shRNA)敲减β-catenin产生了与enzastaurin加AR-A014418相同的细胞毒作用。此外，enzastaurin和AR-A014418的治疗降低了CD44的mRNA水平和表面表达。[2]
体内活性	将异种移植瘤用Enzastaurin和放射线联合处理，比单独使用任一治疗能更大幅度降低微血管密度。微血管密度的减少与肿瘤生长延迟相对应。[3]
存储条件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 10.3 mg/mL (20 mM)
关键字	Apoptosis \| LY-317615 \| Autophagy \| PKC \| Protein kinase C \| LY 317615 \| inhibit \| Enzastaurin \| Inhibitor
相关产品	Guanidine hydrochloride \| Naringin \| Gefitinib \| Hydroxychloroquine \| Stavudine \| L-Ascorbic acid \| Paeonol \| Sodium 4-phenylbutyrate
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 药物功能重定位化合物库 \| FDA 上市激酶抑制剂库 \| 抗癌临床化合物库 \| 抗癌药物库

恩扎妥林|||LY317615|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