Home Epigenetics Epigenetic Reader Domain inhibitor OF-1 For research use only.

OF-1

OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.

OF-1 Chemical Structure

OF-1 Chemical Structure

CAS: 919973-83-4

Selleck's OF-1 has been cited by 3 publications

Purity & Quality Control

Batch: S768101 DMSO] 76 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.19%
99.19

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Biological Activity

Description OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
Targets
BRPF1B [1] BRPF2 [1]
100 nM(Kd) 500 nM(Kd)
In vitro
In vitro As a chemical probe for BRPF bromodomains, OF-1 increases thermal stability in the cellular thermal shift assay of full length BRPF1B at 1 μM and also demonstrates accelerated FRAP recovery at 5 μM in the BRPF2 FRAP assay. In addition, OF-1 shows modest general cytotoxicity. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05576974 Not yet recruiting
Head and Neck Cancer|Unknown Primary Cancer|Head and Neck Squamous Cell Carcinoma
University of Texas Southwestern Medical Center|National Cancer Institute (NCI)
 July 1 2024 Phase 2
NCT05979493 Not yet recruiting
Postoperative Pain|Fibroid Uterus
Joseph Findley MD|University Hospitals Cleveland Medical Center
 January 1 2024 Phase 4
NCT05585125 Recruiting
Heart Failure|Heart Failure Diastolic|Heart Failure With Preserved Ejection Fraction|Cardiac Failure|Heart Diseases
Weill Medical College of Cornell University|National Institute on Aging (NIA)
 December 2023 Phase 4

Chemical Information & Solubility

Molecular Weight 440.31 Formula

C17H18BrN3O4S
CAS No. 919973-83-4 SDF Download OF-1 SDF
Smiles CC1=C(C=CC(=C1)Br)S(=O)(=O)NC2=CC3=C(C=C2OC)N(C(=O)N3C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (172.6 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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