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Merck
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Key Documents

5.00580

Sigma-Aldrich

Ezh2抑制剂III,GSK126

别名:

Ezh2抑制剂III,GSK126

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About This Item

经验公式(希尔记法):
C31H38N6O2
分子量:
526.67
分類程式碼代碼:
12352200
NACRES:
NA.77

化驗

≥98% (HPLC)

品質等級

形狀

semisolid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

brown

溶解度

DMSO: 10 mg/mL

儲存溫度

−20°C

一般說明

A cell-permeable EI1 (Cat. No. 500561) structural analog that acts as an equally potent, SAM-competitive, Ezh2/PRC2 inhibitor (Ki = 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2; [SAM] = 7.5 µM) with similar selectivity over Ezh1/PRC2 (Ki = 89 nM) and other HTMases as EI1. Among panels of 14 HDACs, 11 GPCRs, and 300 kinases, only serotonin 3 receptor, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50 ≥4 µM). Shown to inhibit the proliferation of DLBCL (IC50 28 nM to 5.5 µM; 6 d treatment) in vitro and completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo (50 mg/kg/d i.p.). In addition to DLBCL (diffuse large B cell lymphoma; IC50 ranges from 28 nM to 5.5 µM; 6 d treatment), GSK126 is also shown to inhibit the proliferation of other B-NHL (non-Hodgkin′s lymphoma) and Hodgkin′s lymphoma cell lines, being least active against MC116, HD-MY-Z, WSU-FSCCL, Toledo, NU-DUL-1, and WILL-2 (IC50 >10 µM; 6 d treatment). When administered at a daily i.p. dose of 50 mg/kg, GSK126 is reported to completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in mice in vivo, while complete tumor eradication can be achieved with higher dosing regimens (150 mg/kg/day or two 300 mg/kg dosages per week). It has been demonstrated to regulate the EZH2-PAX6-CXCL10 pathway, thereby suppressing myocardial fibrosis. Additionally, GSK126 has been observed to inhibit apoptosis and reduce H3K27me3 levels in the brains of rat models.

應用

GSK126, Ezh2 Inhibitor III has been used:
  • in testing the epigenetic interactions for the formation of single-cell domains.
  • to induce hyper histone methylation in IMR-90 cells.

包裝

用惰性气体包装

警告

毒性:标准处理(A)

重構

仅使用新鲜的DMSO进行溶解。
复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。

其他說明

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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