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Purity: ≥98%
BG45 (BG-45) is a novel, potent and selective class I HDAC inhibitor with potential anticancer activity. In cell-free experiments, it suppresses HDAC3, HDAC1, HDAC2, and HDAC6 with IC50s of 289 nM, 2.0 μM, 2.2 μM, and >20 μM, respectively. When it comes to inhibiting HDAC3, BG45 is more selective than HDAC1, 2 (IC50 = 289 nM). At IC50 >20 μM, it did not inhibit HDAC6. In a multiple myeloma mouse model, BG45 significantly reduced tumor growth when used alone or in combination with bortezomib. In MM, HDAC3 is a viable target for therapy, and the novel HDAC3 inhibitor BG45 is validated as a prototype.
| Targets |
HDAC3 ( IC50 = 0.289 μM ); HDAC1 ( IC50 = 2.0 μM ); HDAC2 ( IC50 = 2.2 μM ); HDAC6 ( IC50 > 20 μM )
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| Cell Assay |
The method of measuring 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrasodium bromide (MTT) dye absorbance is used to evaluate the growth inhibitory effects of BG45 in MM cell lines. [3H]thymidine uptake is used to measure the rate of DNA synthesis and, consequently, the proliferation of MM cells.
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| Animal Protocol |
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| References |
| Molecular Formula |
C11H10N4O
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| Molecular Weight |
214.22
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| Exact Mass |
214.09
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| Elemental Analysis |
C, 61.67; H, 4.71; N, 26.15; O, 7.47
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| CAS # |
926259-99-6
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C(=C1)N)NC(=O)C2=NC=CN=C2
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| InChi Key |
LMWPVSNHKACEKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10N4O/c12-8-3-1-2-4-9(8)15-11(16)10-7-13-5-6-14-10/h1-7H,12H2,(H,15,16)
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| Chemical Name |
N-(2-aminophenyl)pyrazine-2-carboxamide
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| Synonyms |
BG 45; BG-45; BG45
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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 |
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| 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6681 mL | 23.3405 mL | 46.6810 mL | |
| 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL | |
| 10 mM | 0.4668 mL | 2.3340 mL | 4.6681 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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