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ARV-825

Catalog No. T5434   CAS 1818885-28-7

ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.

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ARV-825 Chemical Structure
ARV-825, CAS 1818885-28-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 60.00
2 mg In stock $ 86.00
5 mg In stock $ 147.00
10 mg In stock $ 178.00
25 mg In stock $ 278.00
50 mg In stock $ 372.00
100 mg In stock $ 556.00
1 mL * 10 mM (in DMSO) In stock $ 228.00
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Purity: 98%
Purity: 97.54%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ARV-825, a heterobifunctional PROTAC (Proteolysis Targeting Chimera) that recruits BRD4 to the E3 ubiquitin ligase cereblon leading to fast, efficient, and prolonged degradation of BRD4 in all BL cell lines tested.
Targets&IC50 Bromodomain 1 of BRD4:90 nM (Kd), Bromodomain 2 of BRD4:28 nM (Kd)
In vitro ARV-825 more effectively suppresses c-MYC levels and downstream signaling than small molecule BRD4 inhibitors resulting in more effective cell proliferation inhibition and apoptosis induction in BL.In Burkitt's lymphoma cells, ARV-825 reduces c-Myc levels, blocks cell proliferation, and induces apoptosis.
Cell Research Cells (50000/100ul) were seeded in 96-well tissue culture plates followed by addition of ARV-825?at indicated concentration.?After 72 hours, 100 μL per well of reconstituted CellTiter-Glo reagent was added and read on Cytation 3 imaging reader.?Relative cell growth was determined by comparing assay readings of treated cells with control DMSO treated cells.?For apoptosis induction, Caspase-Glo 3/7 Assay was used following manufacturer s instruction.
Molecular Weight 923.43
Formula C46H47ClN8O9S
CAS No. 1818885-28-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (54.15 mM)

TargetMolReferences and Literature

1. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

Related compound libraries

This product is contained In the following compound libraries:
Ubiquitination Compound Library Bioactive Compound Library PPI Inhibitor Library Bioactive Compounds Library Max Reprogramming Compound Library Histone Modification Compound Library Anti-Aging Compound Library Kinase Inhibitor Library HIF-1 Signaling Pathway Compound Library Epigenetics Compound Library

Related Products

Related compounds with same targets
dCBP-1 BY27 BRD4 degrader AT1 Molibresib HJB97 FL-411 BRD4-BD1-IN-2 KG-501

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Keywords

ARV-825 1818885-28-7 Chromatin/Epigenetic Epigenetic Reader Domain ARV 825 inhibit PROTACs Inhibitor ARV825 inhibitor

 

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