Home Ubiquitin E3 Ligase inhibitor Homo-PROTAC cereblon degrader 1 For research use only.

Homo-PROTAC cereblon degrader 1

Synonyms: OUN20985

Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.

Homo-PROTAC cereblon degrader 1 Chemical Structure

Homo-PROTAC cereblon degrader 1 Chemical Structure

CAS No. 2244520-98-5

Purity & Quality Control

Batch: S288101 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.51%
99.51

Homo-PROTAC cereblon degrader 1 Related Products

Signaling Pathway

E3 Ligase Signaling Pathways

E3 Ligase Signaling Pathway

Biological Activity

Description Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
Targets
CRBN [1]
In vitro
In vitro

Homo-PROTAC cereblon degrader 1 (OUN20985), a highly potent and efficient Cereblon (CRBN) degrader with only minimal effects on pomalidomide neosubstrates IKZF1 and IKZF3, has no effects on proliferation of different cell lines, prevents pomalidomide-induced degradation of IKZF1 and IKZF3, and antagonizes the effects of pomalidomide on multiple myeloma cellslidomide resistance in different multiple myeloma cells.[1]
Cell Research Cell lines Multiple myeloma cell line NCI-H929, MM1S, HEK293T
Concentrations 0.1 µM
Incubation Time 3 h
Method

HEK293T cells were transfected with a FLAG-CRBN-expressing plasmid. Forty-eight hours after transfection, cells were treated with DMSO or compound 15a for 3 h. Cells were then washed twice with ice-cold phosphate-buffered saline (PBS), lysed under denaturing conditions using 2% sodium dodecyl sulfate  (SDS)-containing lysis buffer, and boiled for 10 min at 95 ℃. The SDS was diluted via the addition of 10×IP lysis buffer (Pierce) containing HALT Protease and Phosphatase Inhibitor Cocktail, MG132 (10 μM), and PR619 (50 nM) and incubated at 4 ℃ for 30 min. Immunoprecipitation was performed using anti-FLAG M2 Affinity Gel according to the manufacturer's protocol, and protein was eluted with FLAG peptide. CRBN was detected by a FLAG-specific antibody, and ubiquitinated CRBN by the FK2 antibody.

Chemical Information & Solubility

Molecular Weight 660.63 Formula

C32H32N6O10
CAS No. 2244520-98-5 SDF --
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (151.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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.

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