OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor (Kd value = 100nM and 500 nM, respectively; >100-fold selectivity over majority of other bromodomains).
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.
In cellular thermal shift assay (CETSA) of full length BRPF1B, OF-1 enhanced thermal stability at 1 µM. In BRPF2 FRAP assay, OF-1 showed accelerated FRAP recovery at 5µM. OF-1 exhibited modest general cytotoxicity.
References:
[1]. OF-1 - A chemical probe for BRPF bromodomains. (2010, October 13). SGC. Retrieved from http://www.thesgc.org/chemical-probes/OF-1
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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
919973-83-4
Chemical Name
4-bromo-N-(6-methoxy-1,3-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)-2-methylbenzenesulfonamide
SMILES
CN1C2=C(C=C(OC)C(NS(=O)(C3=C(C)C=C(Br)C=C3)=O)=C2)N(C)C1=O
Molecular Formula
C17H18BrN3O4S
Molecular Weight
440.31
Solubility
≥ 14.55mg/mL in DMSO
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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