化學信息：
| 化學名 | (3aR)-2-(2-hydroxyphenyl)-3a-methyl-1-[3-(trifluoromethyl)benzoyl]-3,4,6,6a-tetrahydro-2H-pyrrolo[2,3-b]pyrrol-5-one |
|
| 簡稱 | A-366 | |
| 別名 |
MS-2629, HMS2312E03, AKOS005107865, SMR000126755 |
|
| 中文名 | N/A | |
| 化學式 | C19H27N3O2 | |
| 分子量 | 329.44 | |
| CAS號 | 1527503-11-2 | |
| 純度 | 98% | |
| 溶劑/溶解度 |
Water<1mg/ml; DMSO65mg/ml; Ethanol65mg/ml |
|
| 溶液配制 | 5mg加入1.52ml DMSO，或者每3.29mg加入1ml DMSO，配制成10mM溶液。SD1092-10mM用DMSO配制。 |
生物信息：
| 產(chǎn)品描述 | A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor with IC50 of 3.3nM, exhibiting >1000-fold selectivity for G9a/GLP over 21 other methyltransferases. | ||||
| 信號通路 | Epigenetics | ||||
| 靶點 | G9a/GLP | － | － | － | － |
| IC50 | 3.3nM | － | － | － | － |
| 體外研究 | A-366 has significantly less cytotoxic effects on the growth of tumor cell lines compared to other known G9a/GLP small molecule inhibitors despite equivalent cellular activity on methylation of H3K9me2. Treatment of various leukemia cell lines in vitro results in marked differentiation and morphological changes of these tumor cell lines. | ||||
| 體內(nèi)研究 | Treatment of a flank xenograft leukemia model with A-366 results in growth inhibition consistent with the profile of H3K9me2 reduction observed. | ||||
| 臨床實驗 | N/A | ||||
| 特征 | N/A | ||||
相關實驗數(shù)據(jù)(此數(shù)據(jù)來自于公開文獻，碧云天并不保證其有效性)：
| 酶活性檢測實驗 | |
| 方法 | N/A |
| 細胞實驗 | |
| 細胞系 | PC-3 prostate adenocarcinoma cells |
| 濃度 | 0, 0.01, 0.03, 0.1, 0.3, 1, 3, 10μM |
| 處理時間 | 72h |
| 方法 | PC-3 prostate adenocarcinoma cells are incubated in triplicate with DMSO or the indicated concentrations of A-366 or UNC0638 for 72 hours. H3K9me2 levels are assessed by In-Cell Western assay. |
| 動物實驗 | |
| 動物模型 | SCID-beige female mice (Aml flank xenograft model) |
| 配制 | 98% PEG-400 and 2% Tween-80 |
| 劑量 | 30mg/kg/day |
| 給藥方式 | by osmotic mini-pump |
參考文獻：
包裝清單：
1. Pappano WN, et al. PLoS One. 2015, 10(7):e0131716.
2. Sweis RF, et al. ACS Med Chem Lett. 2014, 5(2):205-209.
| 產(chǎn)品編號 | 產(chǎn)品名稱 | 包裝 |
| SD1092-10mM | A-366 (Histone Methyltransferase抑制劑) | 10mM×0.2ml |
| SD1092-5mg | A-366 (Histone Methyltransferase抑制劑) | 5mg |
| SD1092-25mg | A-366 (Histone Methyltransferase抑制劑) | 25mg |
| — | 說明書 | 1份 |
保存條件：
-20℃保存，至少一年有效。5mg和25mg包裝也可室溫保存，至少6個月有效。如果溶于非DMSO溶劑，建議分裝后-80℃保存，預計6個月內(nèi)有效。
注意事項：
本產(chǎn)品對人體有害，操作時請小心，并注意有效防護以避免直接接觸人體或吸入體內(nèi)。
本產(chǎn)品僅限于專業(yè)人員的科學研究用，不得用于臨床診斷或治療，不得用于食品或藥品，不得存放于普通住宅內(nèi)。
為了您的安全和健康，請穿實驗服并戴一次性手套操作。
黨沛 
