PBRM1-BD2-IN-5

Name: PBRM1-BD2-IN-5
Brand: MedChemExpress
SKU: HY-151532
Rating: 4.5 (1 reviews)

Cat. No.: HY-151532 Purity: 99.55%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with K_d 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

CAS No. : 2819989-61-0

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 790	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

K_d: 1.5 μM (PBRM1-BD2), 3.9 μM (PBRM1-BD5)^[1]
IC₅₀: 0.26 μM (PBRM1-BD2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	IC₅₀	8.8 μM Compound: 16	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-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.

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.

2819989-61-0

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
10 mM	0.3667 mL	1.8333 mL	3.6666 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.17 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

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

Handling Instructions (2659 KB)

References

[1]. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13. [Content Brief]

Complete Stock Solution Preparation Table

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

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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PBRM1-BD2-IN-5

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Dilution Calculator

Complete Stock Solution Preparation Table

PBRM1-BD2-IN-5 Related Classifications

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