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Purity: ≥98%
OF-1 (OF1; SGC-OF-1) is a potent and selective inhibitor of bromodomain and PHD finger containing protein 1 (BRPF1) with important biological activity. It inhibits BRPF1B and BRPF2 bromodomain with Kds of 100 nM and 500 nM, respectively. BRPF (BRomodomain and PHD Finger containing) protein family are scaffolding proteins that assembles MYST histone acetyltransferase complexes. MYST complexes play important role in DNA repair, recombination, replication and transcription activation.
| ln Vitro |
OF-1 (1 μM and 2 μM, 0, 1, 2, and 3 days) induces significant reductions in the number of multinucleated tartrate-resistant acid phosphatase (TRAP) positive cells[1]. OF-1 is the sole inhibitor to totally suppress the fusion into multinucleated “osteoclast-like” cells[1].
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| ln Vivo |
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Murine BMCs during differentiation with 10 ng/mL RANKL. Tested Concentrations: 1 μM and 2 μM. Incubation Duration: 0, 1, 2, and 3 days. Experimental Results: Particularly strong at day 2 after RANKL-induced differentiation. |
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| Animal Protocol |
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| References |
[1]. Julia C Meier, et al. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630.
[2]. James Bennett, et al. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J Med Chem. 2016 Feb 25;59(4):1642-7. |
| Molecular Formula |
C17H18BRN3O4S
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| Molecular Weight |
440.31
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| CAS # |
919973-83-4
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| Related CAS # |
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| SMILES |
O=S(C1=CC=C(Br)C=C1C)(NC2=C(OC)C=C(N3C)C(N(C)C3=O)=C2)=O
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| InChi Key |
YUNQZQREIHWDQT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18BrN3O4S/c1-10-7-11(18)5-6-16(10)26(23,24)19-12-8-13-14(9-15(12)25-4)21(3)17(22)20(13)2/h5-9,19H,1-4H3
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| Chemical Name |
4-Bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-2-methyl-benzenesulfonamide
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| Synonyms |
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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 (5.68 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 (5.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2711 mL | 11.3556 mL | 22.7113 mL | |
| 5 mM | 0.4542 mL | 2.2711 mL | 4.5423 mL | |
| 10 mM | 0.2271 mL | 1.1356 mL | 2.2711 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04591171 | Completed Has Results | Procedure: n-of-1 trial guided clinical decision making |
Hypertension Chronic Kidney Diseases |
The University of Texas Health Science Center, Houston |
January 25, 2021 | Not Applicable |
| NCT02744456 | Completed | Drug: Amlodipine Drug: Hydrochlorothiazide |
Hypertension High Blood Pressure |
Columbia University | August 1, 2014 | Early Phase 1 |
| NCT00299169 | Terminated | Behavioral: N of 1 Trials | Diabetes Cardiovascular Disease |
Lawson Health Research Institute | September 2006 | Phase 4 |
| NCT04757584 | Completed Has Results | Drug: Beta blockers | Heart Failure Heart Failure, Diastolic |
Weill Medical College of Cornell University |
April 1, 2021 | Phase 4 |
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