1. Epigenetics
    PROTAC
  2. Epigenetic Reader Domain
    PROTAC

ARV-825 

Cat. No.: HY-16954 Purity: 99.35% ee.: 100.00%
Data Sheet SDS Handling Instructions

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

For research use only. We do not sell to patients.
ARV-825 Chemical Structure

ARV-825 Chemical Structure

CAS No. : 1818885-28-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $234 In-stock
5 mg $150 In-stock
10 mg $230 In-stock
50 mg $700 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 shows affinity to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

IC50 & Target

Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)[1]

In Vitro

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 µM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors[1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.0829 mL 5.4146 mL 10.8292 mL
5 mM 0.2166 mL 1.0829 mL 2.1658 mL
10 mM 0.1083 mL 0.5415 mL 1.0829 mL
Kinase Assay
[1]

Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

923.43

Formula

C₄₆H₄₇ClN₈O₉S

CAS No.

1818885-28-7

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Inquiry Information

Product Name:
ARV-825
Cat. No.:
HY-16954
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