PBRM1-BD2-IN-1

Cat. No.: HY-151528: FAQs
Data Sheet Handling Instructions

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PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with K_d and IC₅₀ values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer.

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

PBRM1-BD2-IN-1 Chemical Structure

CAS No. : 1915012-21-3

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Description

IC₅₀ & Target

Kd: 0.7 μM (PBRM1-BD2), 0.35 μM (PBRM1-BD5), 8.1 μM (SMARCA2B), 5.0 μM (SMARCA4) ^[1].
IC50: 0.2 μM (PBRM1-BD2)^[1].

In Vitro

PBRM1-BD2-IN-1 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line^[1].
PBRM1-BD2-IN-1 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with K_d values of 0.7 μM, 0.35 μM, 8.1 μM and 5.0 μM, respectively^[1].
PBRM1-BD2-IN-1 has inhibitory activity for PBRM1-BD2 with IC₅₀ value of 0.2 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	Human prostate cell lines LNCaP, PC3, and RWPE-1
Concentration:	0, 0.1, 1, and 10 μM
Incubation Time:	5 days
Result:	Inhibited LNCaP growth at higher concentrations.

Molecular Weight

302.80

Formula

C₁₇H₁₉ClN₂O

CAS No.

1915012-21-3

SMILES

O=C1N=C(/C(CC2)=C/C(CC)CC)N2C3=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]. Shifali Shishodia, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13. [Content Brief]

PBRM1-BD2-IN-1 Related Classifications

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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-11915012-21-3Epigenetic Reader Domainpolybromo-1 (PBRM1)bromodomainbinding affinityinhibitorycancerInhibitorinhibitorinhibit

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