價格 | ¥395 | ¥828 | ¥1490 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2025-02-28 |
中文名稱:化合物 A196 | 英文名稱:A-196 |
CAS:1982372-88-2 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.93% | 產(chǎn)品類別: 抑制劑 |
貨號: T4343 |
名稱 | A-196 |
描述 | A-196 is a potent and selective inhibitor of SUV420 h1 and SUV420 h2 with IC50 values of 0.025 and 0.144 μM, respectively; more than 100-fold selective over other histone methyltransferases and non-epigenetic targets. |
細(xì)胞實(shí)驗(yàn) | U2OS cells are seeded on 6-well plates with 3 μM A-196 or DMSO as a control, and incubated for 48 h. The cells are washed once in 1 X PBS and then lysis buffer (20 mM Tris-HCl pH 7.5, 0.5% Triton X-100, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, PMSF, protease inhibitors, benzonase) is added to half the cells to create whole cell extract (WCE). The remaining cells are subjected to sequential cellular fractionation. First the cell pellet is resuspended in hypotonic buffer A (10 mM HEPES pH 7.5, 10 mM KCl, 1.5 mM MgCl2, 0.3 M sucrose, 1 mM DTT and protease inhibitors) and then 0.1% triton X-100 is added. The cells are incubated for 15 min on ice and pelleted by centrifugation at 1,500 g. The supernatant is clarified by centrifugation at max speed and saved as the cytoplasmic fraction. The pellet is resuspended in buffer B (3 mM EDTA, 3 mM EGTA, 1 mM DTT and protease inhibitors) and incubated on ice for 40 min and then centrifuged at 1,500 g for 5 min. The supernatant is clarified and saved as the nucleoplasmic fraction. The pellet is resuspended in lysis buffer and incubated for 5 min at room temperature before being resuspended in 4× loading dye. The final lysate contains the solubilized chromatin fraction. |
激酶實(shí)驗(yàn) | Briefly, Hsp90 from porcine spleen extract is isolated by affinity capture on a purine-affinity media. The Hsp90 loaded media is then challenged with test compound (PF-04929113) at a given concentration, ranging from 0.8 to 500 μM, and the amount of Hsp90 liberated at each concentration is determined. The resulting IC50 values are corrected for the ATP ligand concentration and presented as apparent Kd values. |
體外活性 | A-196 在1和10μM濃度下強(qiáng)效抑制SUV420 h1和SUV420 h2,但對其它PKMTs(包括另一種H4K20修飾酶PR-SET7以及以H3K4、H3K9、H3K27和H3K79為底物的酶)無活性。在細(xì)胞內(nèi),A-196引起全局性H4K20me2和H4K20me3的下降,同時使H4K20me1上升,但對其它組蛋白修飾無影響。A-196抑制電離輻射后53BP1焦點(diǎn)的形成,并減少NHEJ介導(dǎo)的DNA斷裂修復(fù),但不影響同源指導(dǎo)修復(fù)。 |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 7.2 mg/mL (20.04 mM), Sonication is recommended. |
關(guān)鍵字 | SUV420H2 | SUV420H1 | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | A-196 | A196 |
相關(guān)產(chǎn)品 | XY1 | MRTX-1719 | MAK683 | Tazemetostat | iso-Azalansta | EPZ015666 | ORIC-944 | UNC 0631 | AMI-1 free acid | MS37452 | MAK-683 hydrochloride | Piribedil |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 染色質(zhì)修飾分子庫 | 組蛋白修飾化合物庫 | 高選擇性抑制劑庫 | 抗衰老化合物庫 | 表觀遺傳庫 | 干細(xì)胞分化化合物庫 | 膜蛋白靶向化合物庫 | 甲基化化合物庫 | 細(xì)胞重編程化合物庫 |
成立日期 | 2013-04-18 (13年) | 注冊資本 | 566.265100萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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