计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存,充氩。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC 50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes
In Vitro
GNA002 (10 μM; 72 hours) clearly inhibits the proliferation of numerous cancer cell lines with IC 50 s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11. GNA002 (2 μM; 24 hours) demonstrates an elevated capacity to induce cell death in human cancer cells. GNA002 (0.1-4 μM; 48 hours) efficiently reduces EZH2-mediated H3K27 trimethylation in Cal-27 head and neck cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Numerous cancer cell lines Concentration: 10 μM Incubation Time: 72 hours Result: Inhibited the proliferation of numerous cancer cell lines with IC50s of 0.070 μM and 0.103 μM for MV4-11 and RS4-11. Apoptosis AnalysisCell Line: HN-4 and Cal-27 head and neck cancer cells Concentration: 2 μM Incubation Time: 24 hours Result: Induced cellular apoptosis in human cancer cells. Western Blot AnalysisCell Line: Cal-27 head and neck cancer cells Concentration: 0.1, 0.2, 0.5, 1, 2, 4 μM Incubation Time: 48 hours Result: Reduced H3K27Me3 levels.
In Vivo
GNA002 (oral administration; 100 mg/kg; daily) significantly decreases the volumes of Cal-27-derived tumors and reduces H3K27Me3 levels in tumor tissues. GNA002 also significantly suppresses the in vivo tumor growth derived from the xenografted A549 lung cancer cells, Daudi and Pfeiffer cells. GNA002 inhibits the aberrant oncogenic functions of EZH2, thus inhibiting tumor growth in vivo, at least in the xenograft experimental model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors Dosage: 100 mg/kg Administration: Oral administration; daily Result: Decreased the size and weight of tumors formed by Cal-27 cells.
Form:Oil
IC50& Target:EZH2 1.1 μM (IC 50 )
规格
规格或纯度
≥98%
英文名称
GNA002
生化机理
GNA002 是一种高效、特异性共价 EZH2（zeste 同源体增强子 2）抑制剂，IC 50 为 1.1 μM。GNA002 能特异性地与 EZH2-SET 结构域中的 Cys668 共价结合，通过 EZH2 的 COOH 末端 H
储存条件
-20°C储存,充氩
运输条件
超低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
IUPAC Name
(Z)-4-[(1S,2S,13S,15R)-7-[(2E)-3,7-dimethylocta-2,6-dienyl]-6,8-dihydroxy-17,17-dimethyl-5-(3-methylbut-2-enyl)-10,14-dioxo-3,16-dioxapentacyclo[11.4.1.02,11.02,15.04,9]octadeca-4,6,8,11-tetraen-15-yl]-N-(2-ethoxyethyl)-2-methylbut-2-enamide
INCHI
1S/C42H55NO8/c1-10-49-21-20-43-39(48)27(7)18-19-41-38(47)28-22-31-36(46)33-35(45)29(17-15-26(6)13-11-12-24(2)3)34(44)30(16-14-25(4)5)37(33)50-42(31,41)32(23-28)40(8,9)51-41/h12,14-15,18,22,28,32,44-45H,10-11,13,16-17,19-21,23H2,1-9H3,(H,43,48)/b26-15+,27-18-/t28-,32+,41+,42-/m1/s1
InChi Key
HJJVIXXMFVHPER-PTQVRNBOSA-N
Smiles
CCOCCNC(=O)C(=CCC12C(=O)C3CC(C14C(=C3)C(=O)C5=C(C(=C(C(=C5O4)CC=C(C)C)O)CC=C(C)CCC=C(C)C)O)C(O2)(C)C)C
PubChem CID
分子量
701.89
技术文档
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
DMSO : 25 mg/mL (35.62 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥98%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C、氩气保护条件下保存。本品在氩气保护下供应，每次取用后请在惰性气体下重新密封。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1385035-79-9，分子式为 C42H55NO8，分子量为 701.89 g/mol。InChIKey HJJVIXXMFVHPER-PTQVRNBOSA-N。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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