1. Epigenetics
    PROTAC
  2. Epigenetic Reader Domain
    PROTAC

ARV-825 

Cat. No.: HY-16954 Purity: 99.37% ee.: 100.00%
Handling Instructions

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds 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 USD 280 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 276 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

    ARV-825 purchased from MCE. Usage Cited in: Sci Rep. 2018 Sep 5;8(1):13225.

    ARV-825 decreases IFN-γ-induced PD-L1 mRNA and protein expression in primary PSCs and in the stellate cell line.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds 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].

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    References
    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

    SMILES

    CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[[email protected]]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

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

    ARV-825

    Cat. No.: HY-16954