2. Epigenetics Cell Cycle/DNA Damage
  3. Epigenetic Reader Domain SWI/SNF Complex
  4. PBRM1-BD2-IN-8

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity.

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PBRM1-BD2-IN-8

PBRM1-BD2-IN-8 Estructura química

No. CAS : 2819989-75-6

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
1 mg En stock
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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PBRM1-BD2-IN-8 Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Epigenetic Reader Domain:

Ver todas las isoformas
Brd BRPF1 BRPF2 BRPF3 BRD2 BRD3 BRD4 BRDT CECR2 BD1 BD2 BRD7 BRD9 BET BAZ

Ver todos los productos específicos de isoformas SWI/SNF Complex:

Ver todas las isoformas
SMARCA2 SMARCA4 Protein Polybromo-1

  • Actividad biológica

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Descripciòn

PBRM1-BD2-IN-8 (compound 34) is a potent PBRM1 Bromodomain inhibitor (PBRM1-BD2 Kd=4.4 μM, PBRM1-BD2 IC50=0.16 μM; PBRM1-BD5 Kd=25 μM). PBRM1-BD2-IN-8 shows anti-cancer activity[1].

IC50 & Target

IC50: 0.16 μM (PBRM1-BD2)[1]
Cellular Effect
Cell Line Type Value Description References
LNCaP IC50
9.3 μM
Compound: 34
Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
Cytotoxicity against human LNCaP cells assessed as inhibition of cell growth measured after 7 days with compound replacement for every 48 hrs by celltiter-glo assay
[PMID: 36227159]
In Vitro

PBRM1-BD2-IN-8 (0-100 μM; 48 h) inhibits the growth of PBRM1-dependent prostate cancer cells[1].

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

PBRM1-BD2-IN-8 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP cells
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Inhibited the growth of LNCaP cells with IC50 value of about 9 μM.
Peso molecular

317.18

Fòrmula

C15H13BrN2O
No. CAS
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1NC(C2=CC=CC(C)=C2)NC3=C1C(Br)=CC=C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (315.28 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 3.1528 mL 15.7639 mL 31.5278 mL
5 mM 0.6306 mL 3.1528 mL 6.3056 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Calculadora de molaridad

  • Calculadora de dilución

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 (7.88 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.
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).
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.
Pureza y Documentación
Referencias

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. 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 3.1528 mL 15.7639 mL 31.5278 mL 78.8196 mL
5 mM 0.6306 mL 3.1528 mL 6.3056 mL 15.7639 mL
10 mM 0.3153 mL 1.5764 mL 3.1528 mL 7.8820 mL
15 mM 0.2102 mL 1.0509 mL 2.1019 mL 5.2546 mL
20 mM 0.1576 mL 0.7882 mL 1.5764 mL 3.9410 mL
25 mM 0.1261 mL 0.6306 mL 1.2611 mL 3.1528 mL
30 mM 0.1051 mL 0.5255 mL 1.0509 mL 2.6273 mL
40 mM 0.0788 mL 0.3941 mL 0.7882 mL 1.9705 mL
50 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5764 mL
60 mM 0.0525 mL 0.2627 mL 0.5255 mL 1.3137 mL
80 mM 0.0394 mL 0.1970 mL 0.3941 mL 0.9852 mL
100 mM 0.0315 mL 0.1576 mL 0.3153 mL 0.7882 mL
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PBRM1-BD2-IN-8 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:

PBRM1-BD2-IN-82819989-75-6Epigenetic Reader DomainSWI/SNF ComplexSWI/SNF Family of Chromatin-Remodelling ComplexesBD2BD5anticancer activityLNCaPInhibitorinhibitorinhibit

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Nombre del producto:
PBRM1-BD2-IN-8
Cat. No.:
HY-151538
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