BAZ2-ICR

Research use only, not for human use.

BAZ2-ICR is a potent, selective and cell-active inhibitor of BAZ2A and BAZ2B bromodomains.

BAZ2-ICR is a potent, selective and cell-active inhibitor of BAZ2A (Kd=109 nM; IC50=130 nM) and BAZ2B (Kd=170 nM; IC50=180 nM) bromodomains; demonstrates 15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains.

To investigate whether BAZ2-ICR (Compound 13) can displace BAZ2 bromodomains from chromatin in living cells, a fluorescence recovery after photobleaching (FRAP) assay utilizing GFP-tagged BAZ2A full length protein transfected into human osteosarcoma cells (U2OS) are tested. 1 μM BAZ2-ICR reduces the recovery time of the wild-type (wt) construct to a level similar to the dominant negative mutant, confirming that BAZ2-ICR inhibits BAZ2A in cells.

BAZ2-ICR (Compound 13) shows very high solubility (25 mM in D2O), a measured log D of 1.05, high stability in mouse microsomes, and permeation in the CaCo-2 model and thus a suitable profile for oral and intravenous gavage. BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (～50% of mouse liver blood flow) and volume of distribution.

BAZ2 ICR

Chromatin/Epigenetic

Bromodomain

Bromodomain

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1665195-94-7

357.421

C20H19N7

>98% (HPLC)

In Vitro:?DMF : 20 mg/mL (55.96 mM)

CN(N=C1)C=C1C2=C(C3=CC=C(C#N)C=C3)N(CCC4=CN(C)N=C4)C=N2

4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile

(-20℃)

With Ice Pack

≥ 2 years