1665195-94-7
1665195-94-7 structure
- Name: BAZ2-ICR
- Chemical Name: 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile
- CAS Number: 1665195-94-7
- Molecular Formula: C20H19N7
- Molecular Weight: 357.412
- Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
- Create Date: 2016-03-07 04:44:27
- Modify Date: 2025-08-25 22:41:41
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BAZ2-ICR 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. BAZ2-ICR is an epigenetic chemical probe[1].
| Name | 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-benzonitrile |
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| Synonyms |
Benzonitrile, 4-[4-(1-methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl]-
4-{4-(1-Methyl-1H-pyrazol-4-yl)-1-[2-(1-methyl-1H-pyrazol-4-yl)ethyl]-1H-imidazol-5-yl}benzonitrile BAZ2-ICR |
| Description | BAZ2-ICR 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. BAZ2-ICR is an epigenetic chemical probe[1]. |
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| Related Catalog | |
| Target |
IC50: 130 nM (BAZ2A) and 180 nM (BAZ2B); Kd: 109 nM (BAZ2A) and 170 nM (BAZ2A)[1] |
| 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[1]. |
| In Vivo | 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[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
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| Boiling Point | 632.8±55.0 °C at 760 mmHg |
| Molecular Formula | C20H19N7 |
| Molecular Weight | 357.412 |
| Flash Point | 336.5±31.5 °C |
| Exact Mass | 357.170197 |
| LogP | 2.06 |
| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
| Index of Refraction | 1.685 |