| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg |
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| 1g | |||
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| Targets |
OF-1 specifically targets BRPF1B, BRPF2, and BRPF3 bromodomains. It binds to BRPF1B with a Kd of 100 nM (ITC), to BRPF2 with a Kd of 500 nM (ITC), and to BRPF3 with a Kd of 2.4 μM (ITC). It exhibits 39-fold selectivity for BRPF1B and BRPF2 over BRD4.
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| ln Vitro |
In vitro, OF-1 demonstrates potent binding to BRPF bromodomains, particularly BRPF1B (Kd = 100 nM) and BRPF2 (Kd = 500 nM). It shows excellent selectivity over other bromodomains including BRD4 (39-fold selectivity). At 20 μM, OF-1 shows 50% inhibition of TIF1α, indicating some off-target activity at high concentrations.
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| ln Vivo |
Cellular and in vivo activity of OF-1 has been characterized primarily through its use as a chemical probe. By inhibiting BRPF bromodomains, OF-1 disrupts the function of proteins that recognize and bind specific epigenetic marks, affecting the interpretation of epigenetic signals and chromatin-mediated gene regulation. It is utilized to explore the role of BRPF1 bromodomains in gene regulation.
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| Enzyme Assay |
The binding of OF-1 to BRPF bromodomains is typically measured using isothermal titration calorimetry (ITC). Recombinant BRPF bromodomain proteins are titrated with the compound, and the heat change upon binding is measured. Kd values are calculated from the binding isotherms. Fluorescence polarization (FP) or AlphaScreen assays can also be used for higher-throughput screening.
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| Cell Assay |
Cellular assays for OF-1 involve treating cells with the compound and assessing the effects on BRPF-dependent gene expression. Chromatin immunoprecipitation (ChIP) assays are used to evaluate the occupancy of BRPF proteins at target gene promoters. qRT-PCR is used to measure changes in the expression of BRPF-regulated genes. Cell viability and proliferation assays assess the functional consequences of BRPF inhibition.
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| Animal Protocol |
In vivo studies of OF-1 are typically conducted in animal models to investigate the role of BRPF bromodomains in disease. The compound is administered via intraperitoneal (i.p.) injection or oral gavage. Tissues are collected for analysis of BRPF target gene expression by qRT-PCR and histone modification status by Western blotting or ChIP. Pharmacodynamic markers are assessed to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of OF-1 are evaluated in rodents following administration. The compound is soluble in warmed DMSO but insoluble in water and ethanol. Formulation in appropriate vehicles (e.g., PEG-based solutions or cyclodextrin-containing formulations) is required for in vivo administration. Plasma concentrations are measured using LC-MS/MS.
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| Toxicity/Toxicokinetics |
OF-1 is intended for research use only and is not approved for clinical use. Standard toxicology assessments would include acute and repeat-dose toxicity studies in rodents. The compound's selectivity profile suggests a favorable off-target safety margin, though specific toxicity data is not available in the public domain.
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| References | |
| Additional Infomation |
OF-1 is a chemical probe for studying BRPF bromodomains in epigenetic research. BRPF1, BRPF2, and BRPF3 are scaffolding proteins that form complexes with histone acetyltransferases (HATs) such as MOZ and MORF, and play important roles in chromatin remodeling and gene regulation. OF-1 provides a valuable tool for dissecting the biological functions of BRPF bromodomains and evaluating them as therapeutic targets for cancer and other diseases.
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| Exact Mass |
439.02
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| Elemental Analysis |
C, 46.37; H, 4.12; Br, 18.15; N, 9.54; O, 14.53; S, 7.28
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| CAS # |
19973-83-4
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| Appearance |
White to off-white solid powder
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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-(2,3-dihydro-6-methoxy-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl)-2-methyl-benzenesulfonamide
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| Synonyms |
OF-1; OF1; OF 1.
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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 |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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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