Home Epigenetics Epigenetic Reader Domain inhibitor OF-1

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OF-1 Epigenetic Reader Domain inhibitor

Cat.No.S7681

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

Chemical Structure

Molecular Weight: 440.31

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 440.31 Formula

C17H18BrN3O4S

 Storage (From the date of receipt)
CAS No. 919973-83-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=CC(=C1)Br)S(=O)(=O)NC2=CC3=C(C=C2OC)N(C(=O)N3C)C

Solubility

In vitro
Batch:

DMSO : 76 mg/mL (172.6 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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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.

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Mechanism of Action

Targets/IC50/Ki
BRPF1B [1]
100 nM(Kd)
BRPF2 [1]
500 nM(Kd)
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, this compound shows modest general cytotoxicity. [1]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06406816 Not yet recruiting
Intrahepatic Cholangiocarcinoma
Yongyi Zeng|Meng Chao Hepatobiliary Hospital of Fujian Medical University
 May 2024 Early Phase 1
NCT06407518 Not yet recruiting
Preoperative|Sleep Disturbance|Anxiety|Midazolam|Pain Postoperative
Sixth Affiliated Hospital Sun Yat-sen University
 May 2024 Not Applicable
NCT06402110 Recruiting
Femoral Triangle Block|Adductor Canal Block|Anterior Cruciate Ligament Reconstruction
Tanta University
 May 7 2024 Not Applicable

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