GSK-LSD1 (hydrochloride)
目录号 : GC18012
An LSD1 inhibitor
Cas No.:2102933-95-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK-LSD1 (hydrochloride) is a potent, irreversible and mechanism-based inhibitor of LSD1 [1].
Lysine specific demethylase 1 (LSD1) is a histone H3K4me1/2 demethylase existed in many transcriptional co-repressor complexes. LSD1 mediates H3K4 demethylation, causes a repressive chromatin environment which results in gene expression silence and has been shown to play a role in hematopoietic differentiation. It has been demonstrated that LSD1 is overexpressed in multiple tumor types [2].
In vitro: GSK-LSD1 inhibited the activity of LSD1 with an IC50 of 16 nM that is >1,000-fold selective over the closely related FAD-utilizing enzymes, such as LSD2, MAO-A, and MAO-B. GSK-LSD1 inhibited cell proliferation by inducing gene expression changes in various cancer cell lines, the EC50s were < 5 nM [1].
In vivo: In mice bearing LX44 or LX48, daily treatment with 1.5 mg/kg GSK-LSD1 showed 69% and 74% TGI, respectively [3].
References:
[1] Epigenetics probes collection. (2014).
[2] Smitheman K, Cusan M, Liu Y, et al. Inhibition of LSD1 for the treatment of cancer[J]. 2015.
[3] Mohammad H P, Smitheman K N, Kamat C D, et al. A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC[J]. Cancer Cell, 2015, 28(1): 57-69.
| Cas No. | 2102933-95-7 | SDF | |
| 化学名 | N-[(1R,2S)-2-phenylcyclopropyl]-4-piperidinamine, dihydrochloride | ||
| Canonical SMILES | [C@H]1(C2=CC=CC=C2)[C@H](NC3CCNCC3)C1.Cl.Cl | ||
| 分子式 | C14H20N2 • 2HCl | 分子量 | 289.2 |
| 溶解度 | ≤0.1mg/ml in ethanol;25mg/ml in DMSO;1mg/ml in dimethyl formamide | 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 | 3.4578 mL | 17.2891 mL | 34.5781 mL |
| 5 mM | 0.6916 mL | 3.4578 mL | 6.9156 mL |
| 10 mM | 0.3458 mL | 1.7289 mL | 3.4578 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。