Lysine-specific Demethylase Inhibitor (1C)
(Synonyms: KDM1 Inhibitor I|LSD1 Inhibitor) 目录号 : GC13534
lysine-specific demethylase Inhibitor
Cas No.:927019-63-4
Sample solution is provided at 25 µL, 10mM.
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Lysine-specific Demethylase Inhibitor (1C) is a lysine-specific demethylase inhibitor.
Lysine-specific demethylase 1 (LSD1) is the first of several protein lysine demethylases identified. Through a FAD-dependent oxidative reaction, LSD1 could specifically remove histone H3K4me2 to H3K4me1 or H3K4me0. When forming a complex with androgen receptor, LSD1 alters its substrates to H3K9me2. The LSD1 complex regulates a coordinated histone modification switch via enzymatic activities and histone modification readers.
In vitro: Lysine-specific Demethylase Inhibitor (1C) was identified as a bisguanidine polyamine analogue exhibiting noncompetitive and specific LSD1 inhibition, with 14.1% in vitro LSD1 activity at 10 μM. Lysine-specific Demethylase Inhibitor (1C) at 0.25 μM to 10 μM could significantly and dose-dependently increase methylation at the histone 3 lysine 4 chromatin mark, H3K4me1 and H3K4me2, without affecting global H3K9me2 levels in HCT116 human colon carcinoma cells. Lysine-specific Demethylase Inhibitor (1C) could also induce expression of several epigenetically silenced genes, such as SFRP1, SFRP4, SFRP5, and GATA5, particularly in the case of SFRP4 and SFRP5 [1].
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Sharma SK, Wu Y, Steinbergs N, Crowley ML, Hanson AS, Casero RA, Woster PM. (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.J Med Chem. 2010 Jul 22;53(14):5197-212.
| Cas No. | 927019-63-4 | SDF | |
| 别名 | KDM1 Inhibitor I|LSD1 Inhibitor | ||
| 化学名 | N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide | ||
| Canonical SMILES | CN/C(NCCCNCCCNCCCN/C(NC)=N/C)=N\C | ||
| 分子式 | C15H36N8 | 分子量 | 328.5 |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0441 mL | 15.2207 mL | 30.4414 mL |
| 5 mM | 0.6088 mL | 3.0441 mL | 6.0883 mL |
| 10 mM | 0.3044 mL | 1.5221 mL | 3.0441 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet