PBRM1-BD2-IN-4

Cat. No.: HY-151531: Data Sheet Handling Instructions
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PBRM1-BD2-IN-4 is a PBRM1-BD2 inhibitor with an IC₅₀ of 0.2 μM, and its K_d values for PBRM1-BD2 and PBRM1-BD5 are 5.5 μM and 11.1 μM, respectively. PBRM1-BD2-IN-4 selectively inhibits the proliferation of PBRM1-dependent prostate cancer cells. PBRM1-BD2-IN-4 can be used in studies related to prostate cancer.

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

PBRM1-BD2-IN-4 Chemical Structure

CAS No. : 2819989-60-9

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•Related Small Molecules:

•Related Proteins:

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
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BD2

0.2 μM (IC₅₀)

In Vitro

PBRM1-BD2-IN-4 (Compound 12) (0.1-10 μM; 5 days) inhibits the proliferation of LNCaP cells in a dose-dependent manner, while exerts no significant effect on PC3 and PWPE-1 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:	LNCaP, PC3 and PWPE-1 cell
Concentration:	0.1, 1 and 10 μM
Incubation Time:	5 days
Result:	Inhibited the proliferation of LNCaP cells in a dose-dependent manner, while exerts no significant effect on PC3 and PWPE-1 cells.

Molecular Weight

272.73

Formula

C₁₅H₁₃ClN₂O

CAS No.

2819989-60-9

SMILES

O=C1NC(C2=CC=CC=C2C)NC3=C1C(Cl)=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Shishodia S, Nuñez R, Strohmier BP, et al.. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. Journal of medicinal chemistry. 2022 Oct 27;65(20):13714-13735. [Content Brief]

PBRM1-BD2-IN-4 Related Classifications

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

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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.

Keywords:

PBRM1-BD2-IN-42819989-60-9Epigenetic Reader DomainPBRM1 bromodomainshistone H3K14acetyl peptideprostate cancer cellsPBAF complexPBRM1-BD2SMARCA2B bromodomainsSMARCA4 bromodomainsPBRM1-BD5acetylated histone peptidesfull-length PBRM1Inhibitorinhibitorinhibit

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