UF 010Novel and selective class I HDAC inhibitor CAS# 537672-41-6 |
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Quality Control & MSDS
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| Cas No. | 537672-41-6 | SDF | Download SDF |
| PubChem ID | 4596836 | Appearance | Powder |
| Formula | C11H15BrN2O | M.Wt | 271.15 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (368.80 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-bromo-N'-butylbenzohydrazide | ||
| SMILES | CCCCNNC(=O)C1=CC=C(C=C1)Br | ||
| Standard InChIKey | BVQCFCYPFJOOAV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C11H15BrN2O/c1-2-3-8-13-14-11(15)9-4-6-10(12)7-5-9/h4-7,13H,2-3,8H2,1H3,(H,14,15) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Class I HDAC inhibitor (IC50 values are 0.06, 0.1, 0.5 and 1.5 μM for HDACs 3, 2, 1 and 8, respectively). Exhibits >6-fold selectivity over other HDACs. Induces accumulation of acetylated histones in HCT116 cells in vitro. Inhibits proliferation of a range of cancer cell lines. Arrests cells at G1/S transition. |
UF 010 Dilution Calculator
UF 010 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.688 mL | 18.44 mL | 36.88 mL | 73.7599 mL | 92.1999 mL |
| 5 mM | 0.7376 mL | 3.688 mL | 7.376 mL | 14.752 mL | 18.44 mL |
| 10 mM | 0.3688 mL | 1.844 mL | 3.688 mL | 7.376 mL | 9.22 mL |
| 50 mM | 0.0738 mL | 0.3688 mL | 0.7376 mL | 1.4752 mL | 1.844 mL |
| 100 mM | 0.0369 mL | 0.1844 mL | 0.3688 mL | 0.7376 mL | 0.922 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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UF 010 is a novel and selective class I HDAC inhibitor with IC50 values of 0.5, 0.1, 0.06, 1.5, 9.1, 15.3 and 44.5 μM for HDAC1, 2, 3, 8, 6, 10 and 11 [1].
Histone deacetylases (HDACs) are a class of enzymes that remove acetyl groups from ε-N-acetyl lysines on histones, allowing the histones to wrap the DNA more tightly. DNA expression is regulated by de-acetylation and acetylation.
UF 010 is a novel and selective class I HDAC inhibitor, and is a fast-on but slow-off inhibitor. In fluorescence assays, UF 010 (5 nM to 100 μM) exhibited inhibitory potency with IC50 values of 0.5, 0.1, 0.06, 1.5, 9.1, 15.3 and 44.5 μM for HDAC1, 2, 3, 8, 6, 10 and 11, and exhibited IC50 values of >100 μM for HDAC4, 5, 7 and 9. In HCT116 cells, UF 010 induced the accumulation of acetylated histones at all sites examined and significantly inhibited cellular HDACs. In HCT116 cell cultures, UF 010 inhibited HDAC with IC50 value of 1.8 μM. UF 010 also exhibited IC50 value of 11.2 μM for killing cells. In HepG2 liver cancer cell line, UF 010 inhibited cell survival with IC50 value of 4.6 μM. In MDA-MB-231 cells, UF 010 induced G1/S arrest with increased cells in G1 phase and reduced cells in S phase in a dose-dependent way. UF010 at 1 μM also significantly slowed migration [1].
Reference:
[1]. Wang Y, Stowe RL, Pinello CE, et al. Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases. Chem Biol, 2015, 22(2): 273-284.
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Identification of histone deacetylase inhibitors with benzoylhydrazide scaffold that selectively inhibit class I histone deacetylases.[Pubmed:25699604]
Chem Biol. 2015 Feb 19;22(2):273-84.
Inhibitors of histone deacetylases (HDACi) hold considerable therapeutic promise as clinical anticancer therapies. However, currently known HDACi exhibit limited isoform specificity, off-target activity, and undesirable pharmaceutical properties. Thus, HDACi with new chemotypes are needed to overcome these limitations. Here, we identify a class of HDACi with a previously undescribed benzoylhydrazide scaffold that is selective for the class I HDACs. These compounds are competitive inhibitors with a fast-on/slow-off HDAC-binding mechanism. We show that the lead compound, UF010, inhibits cancer cell proliferation via class I HDAC inhibition. This causes global changes in protein acetylation and gene expression, resulting in activation of tumor suppressor pathways and concurrent inhibition of several oncogenic pathways. The isotype selectivity coupled with interesting biological activities in suppressing tumor cell proliferation support further preclinical development of the UF010 class of compounds for potential therapeutic applications.
