Purdue Bioscience - SpeciPure

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.

Pack Size	Availability	Price/USD
2 mg	2-3 weeks	$ 86
4 mg	2-3 weeks	$ 163
8 mg	2-3 weeks	$ 246
20 mg	2-3 weeks	$ 468
40 mg	2-3 weeks	$ 702

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	BAZ2A:（kd）109 nM, BAZ2A:130 nM, BAZ2A:170 nM（kd）, BAZ2B:180 nM
In vitro	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.
In vivo	BAZ2-ICR (5 mg/kg) shows 70% bioavailability and moderate clearance (～50% of mouse liver blood flow) and volume of distribution. 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.
CAS No.	1665195-94-7
Chemical Formula	C20H19N7
Molecular Weight	357.421
Storage	Powder: -20°C for 2 years In solvent: -80°C for 1 year

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