CBB1007
目录号 : GC14151CBB1007 是一种细胞可渗透的脒基胍化合物,可作为一种有效的、可逆的和底物竞争性 LSD1 选择性抑制剂(hLSD1 的 IC50 = 5.27 μM)。
Cas No.:1379573-92-8
Sample solution is provided at 25 µL, 10mM.
CBB1007 is an inhibitor of histone demethylase LSD1with IC50 values of 5.27μM [1].
LSD1 is a member of the FAD-dependent amine oxidase family. It converts di-methylated H3K4 to mono- and un-methylated H3K4 and suppresses gene expression. As an inhibitor of LSD1, CBB1007 is developed to understand the function of the enzyme. In the in vitro assay, CBB1007 shows highly potent inhibitory activity with IC50 value of 5.27μM. It is specific against LSD1 and has no effect on other histone demethylases including LSD2 and JARID1A. In the mouse F9 embryonic teratocarcinoma cells, CBB1007 cause a reproducible increase of mono- and di-methylated H3K4 with IC50 value of 1μM-5μM. It also activates the expression of CHRM4 and SCN3A which are the target genes of LSD1. The inhibition of LSD1 results in the growth inhibition of these cells. Furthermore, CBB1007 is found to inhibit the proliferation of other pluripotent cancer cells as well as the embryonic stem cells that express the stem cell markers Oct4 and Sox2 [1].
References:
[1] Wang J, Lu F, Ren Q, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer research, 2011, 71(23): 7238-7249.
Cas No. | 1379573-92-8 | SDF | |
化学名 | methyl 3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate | ||
Canonical SMILES | COC(C1=CC(CN2CCN(C(N)=N)CC2)=CC(C(N3CCN(C(C4=CC=C(C(N)=N)C=C4)=O)CC3)=O)=C1)=O | ||
分子式 | C27H34N8O4 | 分子量 | 534.61 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.8705 mL | 9.3526 mL | 18.7052 mL |
5 mM | 0.3741 mL | 1.8705 mL | 3.741 mL |
10 mM | 0.1871 mL | 0.9353 mL | 1.8705 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
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