A 366 |
| カタログ番号GC16015 |
A 366 は、G9a および GLP (EHMT1) に対してそれぞれ 3.3 および 38 nM の IC50 を持つ、強力で高度に選択的なペプチド競合性ヒストン メチルトランスフェラーゼ G9a 阻害剤です。 A 366 は、他の 21 のメチルトランスフェラーゼよりも 1000 倍以上の選択性を示します。 A 366 は、Spindlin1-H3K4me3 相互作用の強力なナノモル阻害剤でもあります (IC50 = 182.6 nM)。 A 366 は、ヒト ヒスタミン H3 受容体に対して高い親和性を示し (Ki = 17 nM)、ヒスタミン作動性およびドーパミン作動性受容体ファミリーのサブセット間でサブタイプ選択性を示します。
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Cas No.: 1527503-11-2
Sample solution is provided at 25 µL, 10mM.
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A-366 is a potent histone methyltransferase G9a inhibitor with an IC50 of 3.3 nM.
References:
[1]. Pappano WN, et al. The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.PLoS One. 2015 Jul 6;10(7):e0131716.
| Cas No. | 1527503-11-2 | SDF | |
| Chemical Name | 5'-methoxy-6'-(3-(pyrrolidin-1-yl)propoxy)spiro[cyclobutane-1,3'-indol]-2'-amine | ||
| Canonical SMILES | NC1=NC2=CC(OCCCN3CCCC3)=C(OC)C=C2C14CCC4 | ||
| Formula | C19H27N3O2 | M.Wt | 329.44 |
| 溶解度 | ≥ 11.9mg/mL 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 | 3.0355 mL | 15.1773 mL | 30.3545 mL |
| 5 mM | 0.6071 mL | 3.0355 mL | 6.0709 mL |
| 10 mM | 0.3035 mL | 1.5177 mL | 3.0355 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
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- Purity: >97.00%
- 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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