Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and <100-fold selectivity over all other bromodomains.
Description | BAZ2-ICR is an epigenetic chemical probe and it also is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. |
Targets&IC50 | BAZ2B:180 nM, BAZ2A:170 nM(kd), BAZ2A:130 nM, BAZ2A:(kd)109 nM |
In vitro | The study aims to determine if BAZ2-ICR (Compound 13) is capable of displacing BAZ2 bromodomains from chromatin within live cells. A fluorescence recovery after photobleaching (FRAP) assay, employing a GFP-tagged full-length BAZ2A protein transfected into human osteosarcoma (U2OS) cells, was conducted. The results show that 1 μM BAZ2-ICR significantly shortens the recovery time of the wild-type (wt) construct to a level comparable to that of the dominant negative mutant. This indicates that BAZ2-ICR effectively inhibits BAZ2A's function in cells[1]. |
In vivo | BAZ2-ICR, administered at a dose of 5 mg/kg, demonstrates a 70% bioavailability with moderate clearance—approximately 50% of mouse liver blood flow—and an adequate volume of distribution[1]. As Compound 13, it exhibits exceptional solubility (25 mM in D2O) and a log D value of 1.05, indicating favorable distribution between lipophilic and aqueous phases. Furthermore, it shows high stability in mouse microsomes and effective permeation in the CaCo-2 model, presenting a profile appropriate for both oral and intravenous administration. |
Molecular Weight | 357.41 |
Formula | C20H19N7 |
CAS No. | 1665195-94-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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BAZ2-ICR 1665195-94-7 Chromatin/Epigenetic Epigenetic Reader Domain BAZ2ICR BAZ-2-ICR BAZ2 ICR inhibitor inhibit