| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
BAZ2-ICR targets BAZ2A and BAZ2B bromodomains. Bromodomains are protein interaction modules that recognize acetylated lysine residues on histones and other proteins, playing a key role in epigenetic regulation. BAZ2A and BAZ2B are bromodomain-containing proteins involved in chromatin remodeling and gene transcription. BAZ2-ICR is a potent and selective inhibitor of these bromodomains. By inhibiting BAZ2A/B, BAZ2-ICR modulates gene expression and is used as a chemical probe to study the function of these proteins.
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| ln Vitro |
Using GFP-tagged BAZ2A full-length protein transfected into human osteosarcoma cells (U2OS), the fluorescence recovery after photobleaching (FRAP) test was used to examine whether BAZ2-ICR (compound 13) may substitute the BAZ2 bromodomain in the chromatin of living cells. ..It was confirmed that BAZ2-ICR inhibits BAZ2A in cells when 1 μM BAZ2-ICR reduced the recovery time of the wild-type (wt) construct to a level comparable to that of the dominant-negative mutant [1].
In vitro, BAZ2-ICR is a potent inhibitor of BAZ2A and BAZ2B bromodomains. It has IC50 values of 130 nM for BAZ2A and 180 nM for BAZ2B, and Kd values of 109 nM and 170 nM, respectively. It exhibits 15-fold selectivity for the BAZ2 bromodomain over the CERC2 bromodomain and >100-fold selectivity over a range of other bromodomains. These in vitro studies confirm BAZ2-ICR's potency and selectivity as a BAZ2 bromodomain inhibitor. |
| ln Vivo |
BAZ2-ICR (chemical 13) exhibits both oral and intravenous delivery due to its very high solubility (25 mM in DO), observed log D of 1.05, great stability in mouse microsomes, and permeability in the CaCo-2 model. BAZ2-ICR (5 mg/kg) has a volume of distribution of 70% and a modest clearance (about 50% of mouse liver blood flow) [1].
In vivo activity data for BAZ2-ICR is limited, as the compound is primarily used as a research tool in in vitro studies. However, it is reported to be orally active, suggesting potential for in vivo studies. BAZ2-ICR could be used in animal models to study the role of BAZ2 bromodomains in epigenetic regulation and disease. However, specific in vivo protocols and results are not detailed in standard product descriptions. |
| Enzyme Assay |
In vitro assays for BAZ2-ICR measure its binding to BAZ2A and BAZ2B bromodomains. Binding assays are performed using recombinant bromodomain proteins and a labeled probe (e.g., a fluorescent or biotinylated acetyl-lysine peptide). BAZ2-ICR is added at increasing concentrations to compete with the labeled probe. The IC50 and Kd are determined from binding curves. Selectivity is assessed by testing the compound against a panel of other bromodomains.
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| Cell Assay |
In vitro cell-based assays for BAZ2-ICR are used to study its effects on epigenetic regulation and gene expression. Cells are treated with BAZ2-ICR, and the expression of BAZ2 target genes is measured by quantitative PCR. The compound's effects on chromatin remodeling can be assessed using ChIP-seq or ATAC-seq. Cell proliferation and viability can also be assessed. These assays confirm the compound's cellular activity as a BAZ2 bromodomain inhibitor.
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| Animal Protocol |
In vivo animal experiments for BAZ2-ICR are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a bromodomain inhibitor would involve its administration to animal models of cancer or other diseases. However, specific protocols for BAZ2-ICR are not detailed.
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| ADME/Pharmacokinetics |
BAZ2-ICR has a molecular weight not specified in standard product descriptions. It is a solid compound. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. The compound is reported to be orally active.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for BAZ2-ICR is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. BAZ2-ICR is a bromodomain inhibitor, and its toxicity would be related to its effects on epigenetic regulation in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed.
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| References | |
| Additional Infomation |
BAZ2-ICR is a research compound and is not approved for any clinical or therapeutic use. It is a potent, selective, cell-active, and orally active BAZ2A/B bromodomain inhibitor. BAZ2-ICR inhibits BAZ2A with an IC50 of 130 nM and a Kd of 109 nM, and BAZ2B with an IC50 of 180 nM and a Kd of 170 nM. It exhibits 15-fold selectivity for BAZ2 over CERC2 and >100-fold selectivity over other bromodomains. BAZ2-ICR is an epigenetic chemical probe used to study BAZ2 bromodomain function.
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| Molecular Formula |
C20H19N7
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| Molecular Weight |
357.41
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| Exact Mass |
357.17
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| CAS # |
1665195-94-7
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| PubChem CID |
91654625
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
632.8±55.0 °C at 760 mmHg
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| Flash Point |
336.5±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.685
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| LogP |
2.06
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
538
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RRZVGDGTWNQAPW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19N7/c1-25-12-16(10-23-25)7-8-27-14-22-19(18-11-24-26(2)13-18)20(27)17-5-3-15(9-21)4-6-17/h3-6,10-14H,7-8H2,1-2H3
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| Chemical Name |
4-[5-(1-methylpyrazol-4-yl)-3-[2-(1-methylpyrazol-4-yl)ethyl]imidazol-4-yl]benzonitrile
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| Synonyms |
BAZ2-ICR BAZ2 ICR BAZ2ICR
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMF : 20 mg/mL (~55.96 mM)
DMSO : ~10 mg/mL (~27.98 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7979 mL | 13.9895 mL | 27.9791 mL | |
| 5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL | |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7979 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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