OF-1 Chemical Properties

Boiling point:

573.8±60.0 °C(Predicted)

Density 

1.557±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble5mg/mL, clear (warmed)

pka

9.44±0.20(Predicted)

form 

powder

color 

white to beige

Safety Information

Hazard Codes 

T,Xi

Risk Statements 

25-36

Safety Statements 

26-45

RIDADR 

UN 2811 6.1 / PGIII

OF-1 Usage And Synthesis

Uses

4-Bromo-N-(2,3-dihydro-6-methoxy-1,3-dimethyl-2-oxo-1H-benzimidazol-5-yl)-2-methylbenzenesulfonamide is a selective BRPF2 bromodomain inhibitor.

Biological Activity

OF-1 is a chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1, BRPF2, BRPF3) th at assemble histone acetyltransferase (HAT) complexes of the MYST family members MOZ and MORF. The BRPF1 protein is the scaffold subunit of the MYST acetyltransferase complex, which plays a crucial roles in DNA repair, recombination and replication as well as transcription activation. OF-1 binds to BRPF1B with a Kd of 100 nM , to BRPF2 with a Kd of 500 nM and to BRPF3 with a Kd of 2.4 mM, and shows >100-fold selectivity against most other bromodomains. The closest off-target effects are against BRD4 (39-fold selectivity) and 50% inhibition of TIF1a at 20 μM. For full characterization details, please see OF-1 on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

storage

Store at +4°C

OF-1(919973-83-4)Related Product Information

• PFI-2
• PFI3
• Ribociclib
• Methotrexate
• EPZ015666
• Foretinib (GSK1363089)