2. Epigenetics
  3. Epigenetic Reader Domain
  4. PBRM1-BD2-IN-5

PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer.

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

PBRM1-BD2-IN-5 Chemical Structure

PBRM1-BD2-IN-5 Chemical Structure

CAS No. : 2819989-61-0

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1 mg USD 110 In-stock
5 mg USD 240 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PBRM1-BD2-IN-5 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer[1].

IC50 & Target

Kd: 1.5 μM (PBRM1-BD2), 3.9 μM (PBRM1-BD5)[1]
IC50: 0.26 μM (PBRM1-BD2)[1]
In Vitro

PBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides[1].

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

PBRM1-BD2-IN-5 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP cells expressing lentiviral shPBRM1
Concentration: 0, 0.1, 1 and 10 μM
Incubation Time: 5 days
Result: Exhibited a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown.
Reduced the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.
Molecular Weight

272.73

Formula

C15H13ClN2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C2=CC=CC(C)=C2)NC3=C1C(Cl)=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (366.66 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 3.6666 mL 18.3331 mL 36.6663 mL
5 mM 0.7333 mL 3.6666 mL 7.3333 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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

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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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 4 mg/mL (14.67 mM); Clear solution

  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (9.17 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.
Purity & Documentation

Purity: 99.55%

COA (250 KB) HNMR (200 KB) RP-HPLC (118 KB)

Handling Instructions (2659 KB)
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. 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 3.6666 mL 18.3331 mL 36.6663 mL 91.6657 mL
5 mM 0.7333 mL 3.6666 mL 7.3333 mL 18.3331 mL
10 mM 0.3667 mL 1.8333 mL 3.6666 mL 9.1666 mL
15 mM 0.2444 mL 1.2222 mL 2.4444 mL 6.1110 mL
20 mM 0.1833 mL 0.9167 mL 1.8333 mL 4.5833 mL
25 mM 0.1467 mL 0.7333 mL 1.4667 mL 3.6666 mL
30 mM 0.1222 mL 0.6111 mL 1.2222 mL 3.0555 mL
40 mM 0.0917 mL 0.4583 mL 0.9167 mL 2.2916 mL
50 mM 0.0733 mL 0.3667 mL 0.7333 mL 1.8333 mL
60 mM 0.0611 mL 0.3056 mL 0.6111 mL 1.5278 mL
80 mM 0.0458 mL 0.2292 mL 0.4583 mL 1.1458 mL
100 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
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PBRM1-BD2-IN-5 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-52819989-61-0Epigenetic Reader DomainanticancerPBRM1BD2BD5LNCaPInhibitorinhibitorinhibit

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