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.

Physicochemical Properties

Molecular Formula	C17H18BRN3O4S
Molecular Weight	440.31
Exact Mass	439.02
CAS #	919973-83-4
Related CAS #	919973-83-4
PubChem CID	35397514
Appearance	White to off-white solid powder
Density	1.6±0.1 g/cm3
Boiling Point	573.8±60.0 °C at 760 mmHg
Flash Point	300.8±32.9 °C
Vapour Pressure	0.0±1.6 mmHg at 25°C
Index of Refraction	1.644
LogP	3.32
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	4
Heavy Atom Count	26
Complexity	640
Defined Atom Stereocenter Count	0
InChi Key	YUNQZQREIHWDQT-UHFFFAOYSA-N
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
Chemical Name	4-Bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzoimidazol-5-yl)-2-methyl-benzenesulfonamide
Synonyms	OF-1; SGC OF 1; SGC OF1; SGC OF-1; SGCOF1; SGC-OF-1;
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

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].
ln Vivo
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.
Animal Protocol
References	[1]. Selective Targeting of Bromodomains of the Bromodomain-PHD Fingers Family Impairs Osteoclast Differentiation. ACS Chem Biol. 2017 Oct 20;12(10):2619-2630. [2]. Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF. J Med Chem. 2016 Feb 25;59(4):1642-7.

Solubility Data

Solubility (In Vitro)

DMSO: 76 mg/mL (172.6 mM) Water:<1 mg/mL Ethanol:<1 mg/mL

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.