| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
UF010 (UF-010; UF 010) is a novel, potent and selective class I HDAC inhibitor with potential anticancer activities. HDAC isoforms (HDAC1, HDAC2, HDAC3, HDAC8, HDAC6, and HDAC10) are inhibited with IC50 values of 0.5 nM, 0.1 nM, 0.06 nM, 1.5 nM, 9.1 nM, and 15.3 nM, in that order. The use of histone deacetylase inhibitors (HDACi) as clinical anticancer therapies has great therapeutic promise. Yet, the HDACi that are currently on the market have unfavorable pharmacological characteristics, poor isoform selectivity, and off-target activity. For HDACi to get around these restrictions, new chemotypes are required. UF010 is a competitive inhibitor that binds to HDAC in a fast-on, slow-off manner. UF010 inhibits class I HDAC to prevent the growth of cancer cells. Global alterations in gene expression and protein acetylation result from this, which simultaneously inhibits multiple oncogenic pathways and activates tumor suppressor pathways. The UF010 class of compounds is supported in its preclinical development for potential therapeutic applications by its isotype selectivity and intriguing biological activities in suppressing tumor cell proliferation.
| Targets |
HDAC3 (IC50 = 0.06 μM); HDAC2 (IC50 = 0.1 μM); HDAC1 (IC50 = 0.5 μM); HDAC8 (IC50 = 9.1 μM); HDAC10 (IC50 = 15.3 μM); HDAC11 (IC50 = 44.5 μM)
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| ln Vitro |
UF010 primarily inhibits the G1/S transition with an increased G1 cell population and a decreased cell population in the S phase in a dose-dependent manner in cell-cycle analysis using MDA-MB-231 cells. In cell culture medium containing 10% fetal bovine serum, UF010 has a half-life of 15.8 hours[1].
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| Cell Assay |
For six hours, HCT116 and A549 cells are exposed to either DMSO or etoposide (10 μM). One hour prior to cell lysis, TSA (0.2 μM), MS-275, and UF010 (2 μM) are added. Western blotting is performed on the whole cell lysates using antibodies to the specified proteins. It is found that PCNA is a loading control.
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| References |
| Molecular Formula |
C11H15BRN2O
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| Molecular Weight |
271.16
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| Exact Mass |
270.036
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| Elemental Analysis |
C, 48.72; H, 5.58; Br, 29.47; N, 10.33; O, 5.90
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| CAS # |
537672-41-6
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| Related CAS # |
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| PubChem CID |
4596836
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| Appearance |
White to off-white crystalline solid
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
326.7±34.0 °C at 760 mmHg
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| Flash Point |
151.4±25.7 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.550
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| LogP |
3.46
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
15
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| Complexity |
191
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC1C([H])=C([H])C(=C([H])C=1[H])C(N([H])N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O
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| InChi Key |
BVQCFCYPFJOOAV-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
4-bromo-N'-butylbenzohydrazide
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| Synonyms |
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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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6879 mL | 18.4393 mL | 36.8786 mL | |
| 5 mM | 0.7376 mL | 3.6879 mL | 7.3757 mL | |
| 10 mM | 0.3688 mL | 1.8439 mL | 3.6879 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.
UF010 Induces the Accumulation of Protein Acetylation. |
Fig. 4. Antiproliferation Effects of UF010. |
Fig. 5. Global Effects of UF010 on Gene Expression.Chem Biol.2015 Feb 19;22(2):273-84. |
Mechanisms of HDAC Inhibition by UF010.Chem Biol.2015 Feb 19;22(2):273-84. |
Suppression of Cancer Cell Viability by UF010 Analogs Correlates with Their HDAC Inhibition Potencies.Chem Biol.2015 Feb 19;22(2):273-84. |
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