Lysine-specific Demethylase Inhibitor (1C) (Synonyms: KDM1 Inhibitor I|LSD1 Inhibitor) |
| Catalog No.GC13534 |
lysine-specific demethylase Inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | KDM1 Inhibitor I|LSD1 Inhibitor | ||
| Chemical Name | N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide | ||
| Canonical SMILES | CN/C(NCCCNCCCNCCCN/C(NC)=N/C)=N\C | ||
| Formula | C15H36N8 | M.Wt | 328.5 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)
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