S42481
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- 公司名稱 上海源葉生物科技有限公司
- 品牌
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- 產(chǎn)地
- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時(shí)間 2025/5/14 20:23:32
- 訪問次數(shù) 254
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- 產(chǎn)品描述：
EPZ005687 is a potent inhibitor of EZH2 (K(i) of 24 nM). EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against the closely related enzyme EZH1. The compound reduces H3K27 methylation in various lymphoma cells; this translates into apoptotic cell killing in heterozygous Tyr641 or Ala677 mutant cells, with minimal effects on the proliferation of wild-type cells.
- 靶點(diǎn)： EZH2
- 體外研究： EPZ005687 shows concentration-dependent inhibition of PRC2 enzymatic activity with an IC50 value of 54±5 nM. EPZ005687 specifically inhibits H3K27 methylation in lymphoma cells. EPZ005687 has a notable effect on proliferation of the EZH2Y641F-bearing cell line. EPZ005687 decreases proliferation in mutant but not wild-type EZH2 lymphoma cells. EPZ005687 (0.5, 1, 5 and 10 µM) induces an obvious apoptosis of U937 cells in a dose-dependent manner. EPZ005687 inhibits obviously the proliferation of U937 cells but has weak effect on the proliferation of NBMCD34+ cells. EPZ005687 induces G1 phase blocking and decreases the percentage of cells in S phase in U937 cells. In addition, EPZ005687 produces obviously depletion of H3K27 methylation in U937 cells, but hardly has effect on the H3K27 methylation of NBMCD34+ cells.
- 細(xì)胞實(shí)驗(yàn)： Plating densities are determined for each cell line on the basis of linear log-phase growth. Cells are counted and split back to the original plating density in fresh medium with EPZ005687 on days 4 and 7.(Only for Reference) Cell lines: OCI-LY19, WSU-DLCL2, Pfeiffer
- 參考文獻(xiàn)：
1. Knutson SK, et al. A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012;8(11):890-6.
2. Tang SH, et al. Effects of H3K27 methylation inhibitor EPZ005687 on apoptosis, proliferation and cell cycle of U937 cells and normal CD34 positive cells. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2014 Dec;22(6):1561-6.
- 溶解度： DMSO : 5 mg/mL (ultrasonic and warming)
母液保存：分裝凍存，避免反復(fù)凍融；-20℃，1個(gè)月；-80℃，6個(gè)月（稀釋后溶液溫度低保存可能會(huì)析出，盡量現(xiàn)用現(xiàn)配）
細(xì)胞實(shí)驗(yàn):先用DMSO溶解：再用培養(yǎng)基進(jìn)行稀釋，稀釋過程建議分段進(jìn)行，避免濃度變化過快導(dǎo)致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶。在稀釋時(shí)要確保工作液中 DMSO 的終濃度盡量在0.1%以下，不要超過0.5%，并設(shè)置相應(yīng)濃度的DMSO對(duì)照組。
動(dòng)物實(shí)驗(yàn)：先用DMSO溶解：再用水或者生理鹽水等去稀釋，稀釋過程建議分段進(jìn)行，避免濃度變化過快導(dǎo)致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況， 可采用超聲的方法使其復(fù)溶?？梢酝ㄟ^添加助溶劑來幫助溶解，比如植物油、Tween80、甘油、羧甲基纖維素鈉和PEG400等。具體方式請(qǐng)參考文獻(xiàn)。懸濁液可用于口服和腹腔注射，不會(huì)影響產(chǎn)品活性。
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 1.853 ml 9.265 ml 18.53 ml 5 mM 0.371 ml 1.853 ml 3.706 ml 10 mM 0.185 ml 0.926 ml 1.853 ml 50 mM 0.037 ml 0.185 ml 0.371 ml
- 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的性，僅供客戶參考交流研究之用。
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