BRD4770 (Synonyms: HMTase Inhibitor VI) |
カタログ番号GC10259
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BRD4770 は、ヒストンメチルトランスフェラーゼ G9a 阻害剤です。 BRD4770 は、ヒストン H3 (H3K9) 上のリジン 9 のジメチル化およびトリメチル化を 5 μM の EC50 で減少させ、H3K27me3、H3K36me3、H3K4me3、および H3K79me3 に対してほとんどまたはほとんど影響を与えません。 BRD4770 は毛細血管拡張性運動失調症変異 (ATM) 経路を活性化し、細胞老化を誘導することができます。
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Cas No.: 1374601-40-7
Sample solution is provided at 25 µL, 10mM.
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BRD4770 is a novel G9a(EHMT2) inhibitor with EC50 of 5 uM (trimethylated H3K9 in PANC-1 cell).IC50 value: 5 uM (PANC-1 cell) [1]Target: G9a inhibitorBRD4770 activates the ATM pathway without inducing DNA damage, while the ATR pathway is not affected. BRD4770 is a novel probe for studying G9a and its role in cellular senescence.Treatment of 5 μM BRD4770 for 24 h decreased H3K9 trimethylation level by 23% in PANC-1 cells. BRD9539 also inhibits PRC2 activity.
References:
[1]. Yuan Y, et al. A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma. ACS Chem Biol. 2012 Jul 20;7(7):1152-7.
| Cas No. | 1374601-40-7 | SDF | |
| 同義語 | HMTase Inhibitor VI | ||
| Chemical Name | methyl 2-benzamido-1-(3-phenylpropyl)benzimidazole-5-carboxylate | ||
| Canonical SMILES | COC(=O)C1=CC2=C(C=C1)N(C(=N2)NC(=O)C3=CC=CC=C3)CCCC4=CC=CC=C4 | ||
| Formula | C25H23N3O3 | M.Wt | 413.47 |
| 溶解度 | DMF: 20 mg/ml,DMF:PBS(pH7.2) (1:2): 0.25 mg/ml,DMSO: 10 mg/ml | 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 | 2.4186 mL | 12.0928 mL | 24.1856 mL |
| 5 mM | 483.7 μL | 2.4186 mL | 4.8371 mL |
| 10 mM | 241.9 μL | 1.2093 mL | 2.4186 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)