CBB1007 |
| Catalog No.GC14151 |
CBB1007 est un composé d'amidino-guanidinium perméable aux cellules qui agit comme un inhibiteur sélectif de LSD1 puissant, réversible et compétitif pour le substrat (IC50 = 5,27 μM pour hLSD1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1379573-92-8
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 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 | ||
| Formula | C27H34N8O4 | M.Wt | 534.61 |
| 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 | |||
|
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 |
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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 24 reference(s) in Google Scholar.)
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