2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. ZXH-3-26

ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM.

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CAS No. : 2243076-67-5

사이즈 가격 재고 수량
5 mg 해외재고보유
10 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

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고객리뷰

Based on 2 publication(s) in Google Scholar

ZXH-3-26 Related Antibodies

Top Publications Citing Use of Products

    ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47.  [Abstract]

    ZXH-3-26 (0.001, 0.005, 0.01, 0.025, 0.05, 0.1, 0.3, 1, 10 μM; 6 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.

    ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47.  [Abstract]

    ZXH-3-26 (100 nM; 0.5, 1, 2, 4, 6, 8, 12, 24 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.

    ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47.  [Abstract]

    ZXH-3-26 (0.01, 0.05, 0.1, 0.3, 1, 0.3, 10 μM; 6 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.

    ZXH-3-26 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2023 May 9;9(1):47.  [Abstract]

    ZXH-3-26 (100 nM; 0.5, 2, 4, 6, 12, 24 h) inhibits the expression of the long (BRD4 l) and the short (BRD4 s) isoform in HeLa cells.

    View All PROTACs Isoform Specific Products:

    View All Isoforms
    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    View All Epigenetic Reader Domain Isoform Specific Products:

    View All Isoforms
    Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    ZXH-3-26 is a PROTAC connected by ligands for Cereblon and BRD4 with a DC50/5h of 5 nM. The DC50/5h refers to half-maximal degradation after 5 hours of treatment of ~ 5 nM[1].

    IC50 & Target[1]

    BRD4

    5 nM (DC50, 5 hours of treatment)

    Cereblon

     

    In Vitro

    ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2/3[1].
    ZXH-3-26 shows activity exclusively on the first bromodomain of BRD4, and spares degradation of BRD2/3 at concentrations 10 μM. Immunoblot analysis confirms that ZXH-3-26 degrades endogenous BRD4 with comparable efficacy compared to the best pan-BET degrader dBET6, while being inactive on BRD2/3[1].
    ZXH-3-26 engages CRBN in a conformation distinct[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    ZXH-3-26 Related Antibodies
    분자량

    785.27

    화학식

    C38H37ClN8O7S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C(NCCCCCNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=O)S3)C(C7=CC=C(Cl)C=C7)=N1
    선적

    Room temperature in continental US; may vary elsewhere.
    보관

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    용액&용해도
    In Vitro: 

    DMSO : 50 mg/mL (63.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2734 mL 6.3672 mL 12.7345 mL
    5 mM 0.2547 mL 1.2734 mL 2.5469 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • 몰농도 계산기

    • 농도 희석 계산기

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (6.37 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    순도&문서
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.2734 mL 6.3672 mL 12.7345 mL 31.8362 mL
    5 mM 0.2547 mL 1.2734 mL 2.5469 mL 6.3672 mL
    10 mM 0.1273 mL 0.6367 mL 1.2734 mL 3.1836 mL
    15 mM 0.0849 mL 0.4245 mL 0.8490 mL 2.1224 mL
    20 mM 0.0637 mL 0.3184 mL 0.6367 mL 1.5918 mL
    25 mM 0.0509 mL 0.2547 mL 0.5094 mL 1.2734 mL
    30 mM 0.0424 mL 0.2122 mL 0.4245 mL 1.0612 mL
    40 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7959 mL
    50 mM 0.0255 mL 0.1273 mL 0.2547 mL 0.6367 mL
    60 mM 0.0212 mL 0.1061 mL 0.2122 mL 0.5306 mL
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    ZXH-3-26 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ZXH-3-262243076-67-5PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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    상품명:
    ZXH-3-26
    Cat. No.:
    HY-122826
    수량:
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