1. PROTAC Epigenetics
  2. PROTACs Epigenetic Reader Domain
  3. PROTAC BRD9 Degrader-1

PROTAC BRD9 Degrader-1 est un dégradeur chimique au plomb PROTAC BRD9 (IC50=13,5 nM), qui peut être utilisé comme sonde sélective utile pour l'étude de la biologie complexe du FBA.

PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.

For research use only. We do not sell to patients.

PROTAC BRD9 Degrader-1 Chemical Structure

PROTAC BRD9 Degrader-1 Chemical Structure

CAS No. : 2097971-01-0

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Description

PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology[1].

IC50 & Target[1]

BRD9

13.5 nM (IC50)

BRD4

3.78 μM (IC50)

CRBN-DDB1

48.9 nM (IC50)

In Vitro

PROTAC BRD9 Degrader-1 (Compound 1) inhibits BRD9, BRD4, and CRBN-DDB1 with IC50s of 13.5 nM, 3.78 μM, and 48.9 nM, respectively[1].

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

Molecular Weight

903.98

Formula

C42H45N7O12S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(C=C(C(NC(CC2)CCS2(=O)=O)=N)S3)=C3C(C4=CC(OC)=C(OCC(NCCCCNC(COC5=C(C(N6C(CCC7=O)C(N7)=O)=O)C(C6=O)=CC=C5)=O)=O)C=C4)=CN1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (165.93 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 1.1062 mL 5.5311 mL 11.0622 mL
5 mM 0.2212 mL 1.1062 mL 2.2124 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.

  • Molarity Calculator

  • Dilution Calculator

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: ≥ 2.5 mg/mL (2.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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 1.1062 mL 5.5311 mL 11.0622 mL 27.6555 mL
5 mM 0.2212 mL 1.1062 mL 2.2124 mL 5.5311 mL
10 mM 0.1106 mL 0.5531 mL 1.1062 mL 2.7655 mL
15 mM 0.0737 mL 0.3687 mL 0.7375 mL 1.8437 mL
20 mM 0.0553 mL 0.2766 mL 0.5531 mL 1.3828 mL
25 mM 0.0442 mL 0.2212 mL 0.4425 mL 1.1062 mL
30 mM 0.0369 mL 0.1844 mL 0.3687 mL 0.9218 mL
40 mM 0.0277 mL 0.1383 mL 0.2766 mL 0.6914 mL
50 mM 0.0221 mL 0.1106 mL 0.2212 mL 0.5531 mL
60 mM 0.0184 mL 0.0922 mL 0.1844 mL 0.4609 mL
80 mM 0.0138 mL 0.0691 mL 0.1383 mL 0.3457 mL
100 mM 0.0111 mL 0.0553 mL 0.1106 mL 0.2766 mL
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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.

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Product Name:
PROTAC BRD9 Degrader-1
Cat. No.:
HY-103632
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