OF-1 is a chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) family of scaffolding proteins (BRPF1, BRPF2, BRPF3) that 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
Molecular Weight | 440.31 |
Formula | C17H18BrN3O4S |
CAS Number | 919973-83-4 |
Solubility (25°C) | DMSO: 5 mg/mL (warmed) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Won-Gune Jeong, et al. Removal of 1,2-dichloroethane in groundwater using Fenton oxidation
[2] Bas C Stunnenberg, et al. N-of-1 Trials in Neurology: A Systematic Review
[3] Wanying He, et al. Status of N-of-1 Trials in Chronic Pain Management: A Narrative Review
[4] Suzanne McDonald, et al. N-of-1 Trials in Healthcare
[5] E Mordijck, et al. N-of-1 trials in child and adolescent psychiatry: a closer look at stimulants
Related Products |
---|
DiosMetin 7-O-β-D-Glucuronide
DiosMetin 7-O-β-D-Glucuronide is an antioxidant constituent in the fruits of Luffa cylindrical. |
Bendazac L-Lysine
Bendazac L-Lysine is an aldose reductase (AR) inhibitor, which can be used to inhibit the activity of AR in the eye to prevent cataracts. |
Ro5-3335
Ro5-3335 acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation. |
Bendazac
Bendazac is an oxyacetic acid with anti-inflammatory, antinecrotic, choleretic and antilipidaemic properties. Bendazac acts by preventing protein denaturation. |
Dexamethasone palmitate
Dexamethasone palmitate (DXP) is a proagent of Dexamethasone. Dexamethasone palmitate can be used for the research of inflammation. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.