S83783 |
I-CBP 112 |
源葉(MedMol) | ≥98%(HPLC) |
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- 產(chǎn)品描述: I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP/p300 bromodomains.
- 靶點(diǎn): Epigenetic Reader Domain;Histone Acetyltransferase;EpigeneticReaderDomain;?HistoneAcetyltransferase
- 體內(nèi)研究:
I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9+ AML cells in a dose-dependent manner in vitro and in vivo.
- 細(xì)胞實(shí)驗(yàn): I-CBP112 is dissolved in DMSO and diluted with appropriate medium before use. Cells (6000 KG1a and 13000 LNCaP cells/well) are plated in 96-well flat-bottom plates approximately 24 h prior to drug treatment. After 24 h, 10–20% fetal bovine serum-containing medium is replaced with 2.5% serum medium, and cells are treated with I-CBP112 in 0.18% DMSO; 0.18% DMSO is shown to have negligible cell growth effects under the conditions used in our experiments. After being exposed to I-CBP112 for 66 h, cells are subjected to a final concentration of 0.476% [3H]thymidine per well and allowed to proliferate for an additional 6 h (exposure to I-CBP112 for a total of 72 h). Cells are harvested, and the counts of 3H in each well are taken relative to those treated with vehicle alone to quantify the effect of the ligand on proliferation
- 參考文獻(xiàn):
1. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19. 2. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃;干燥
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 2.134 ml 10.67 ml 21.341 ml 5 mM 0.427 ml 2.134 ml 4.268 ml 10 mM 0.213 ml 1.067 ml 2.134 ml 50 mM 0.043 ml 0.213 ml 0.427 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)