BRD73954 |
| Catalog No.GC12484 |
potent and selective HDAC inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1440209-96-0
Sample solution is provided at 25 µL, 10mM.
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BRD73954 is a potent and selective inhibitor of HDAC with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively [1].
Histone deacetylases (HADCs) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription [1].
BRD73954 is a potent and selective HDAC inhibitor with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively. Also, BRD73954 inhibited HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC7 and HDAC9 with IC50 values of 12, 9.0, 23, >33, >33, 13 and >33 μM, respectively. In HeLa cells, BRD73954 significantly increased α-tubulin acetylation, which was a substrate for HDAC6, while there was no change in the acetylation state of histone H3, which was a substrate for HDACs 1, 2 and 3 [1].
Reference:
[1]. Olson DE, Wagner FF, Kaya T, et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem, 2013, 56(11): 4816-4820.
| Cas No. | 1440209-96-0 | SDF | |
| Chemical Name | N1-hydroxy-N3-phenethylisophthalamide | ||
| Canonical SMILES | ONC(C1=CC=CC(C(NCCC2=CC=CC=C2)=O)=C1)=O | ||
| Formula | C16H16N2O3 | M.Wt | 284.31 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 1 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5173 mL | 17.5864 mL | 35.1729 mL |
| 5 mM | 0.7035 mL | 3.5173 mL | 7.0346 mL |
| 10 mM | 0.3517 mL | 1.7586 mL | 3.5173 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 12 reference(s) in Google Scholar.)
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