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Purity: ≥98%
BRD73954 (BRD-73954) is a novel, potent and dual inhibitor of histone deacetylase 6 (HDAC6) and HDAC8 with potential anticancer activity. Its IC50 values for HDAC6 and HDAC8 inhibition are 36 and 120 nM, respectively.
| Targets |
HDAC6 ( IC50 = 0.036 μM ); HDAC8 ( IC50 = 0.12 μM ); HDAC2 ( IC50 = 9 μM )
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| Enzyme Assay |
RD73954 ia a novel inhibitor of HDAC with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
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| Cell Assay |
The first small molecule inhibitor of histone deacetylase (HDAC), BRD73954 can potently and selectively inhibit both HDAC6 and HDAC8, even though these isoforms are related to different phylogenetic classes of the HDAC family of enzymes. Our findings reveal that phenyl hydroxamic acid meta substituents are easily incorporated into HDAC6 binding sites and are also required for the strong inhibition of HDAC8. When HeLa cells are treated with BRD73954, there is a noticeable rise in the acetylation of α-tubulin, which is a known substrate for HDAC6, but not of histone H3, which is a substrate for HDAC1, 2, and 3.
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| References |
| Molecular Formula |
C16H16N2O3
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| Molecular Weight |
284.31
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| Exact Mass |
284.12
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| Elemental Analysis |
C, 67.59; H, 5.67; N, 9.85; O, 16.88
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| CAS # |
1440209-96-0
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C=C1)CCNC(=O)C2=CC(=CC=C2)C(=O)NO
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| InChi Key |
FIHKWEQJEDRIFS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16N2O3/c19-15(17-10-9-12-5-2-1-3-6-12)13-7-4-8-14(11-13)16(20)18-21/h1-8,11,21H,9-10H2,(H,17,19)(H,18,20)
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| Chemical Name |
3-N-hydroxy-1-N-(2-phenylethyl)benzene-1,3-dicarboxamide
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| Synonyms |
BRD-73954; BRD73954; BRD 73954
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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