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PBRM1 inhibitor PB16

Chemical Structure : PBRM1 inhibitor PB16

CAS No.: 2819989-61-0

PBRM1 inhibitor PB16 (PBRM1-BD2 inhibitor 16)

Catalog No.: PC-25802Not For Human Use, Lab Use Only.

PBRM1 inhibitor PB16 is a selective, cell-active Polybromo-1 (PBRM1) bromodomain inhibitor with ITC KD of 2 uM for PBRM1-BD2, and IC50 of 0.26 uM in AlphaScreen assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PBRM1 inhibitor PB16 is a selective, cell-active Polybromo-1 (PBRM1) bromodomain inhibitor with ITC KD of 2 uM for PBRM1-BD2, and IC50 of 0.26 uM in AlphaScreen assays.
PB16 does not bind the SMARCA2 and SMARCA4 bromodomains.
PB16 shows promising inhibition toward PBRM1-dependent prostate cancer cell line LNCaP with IC50 of 9 uM.

Physicochemical Properties

M.Wt 272.73
Formula C15H13ClN2O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Chloro-2-(3-methylphenyl)-2,3-dihydroquinazolin-4(1H)-one

References

1. Nuñez R, et al. ACS Med Chem Lett. 2025 Sep 16;16(10):1955-1962.

2. Shishodia S, et al. J Med Chem. 2022 Oct 27;65(20):13714-13735.

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