BG45
Based on 4 publication(s) in Google Scholar
BG45 is a potent HDAC3 inhibitor with IC50 values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependent apoptosis.
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- Pureté: 99.95%
- CAS No.: 926259-99-6
- Formule: C11H10N4O
- Masse moléculaire:214.22
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) BG45
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Customer Validation & Images
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Activité biologique
Description
IC50 & Target
[2]|
HDAC3 0.289 μM (IC50) |
HDAC1 2.0 μM (IC50) |
HDAC2 2.2 μM (IC50) |
HDAC6 >20 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
29.14 μM
Compound: BG45
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Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay
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[PMID: 31420269] |
| B16-F10 | IC50 |
34.59 μM
Compound: BG45
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Antiproliferative activity against mouse B16F10 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against mouse B16F10 cells incubated for 48 hrs by MTT assay
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[PMID: 31420269] |
| HeLa | IC50 |
28.28 μM
Compound: BG45
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Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
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[PMID: 31420269] |
| Sf9 | IC50 |
2200 nM
Compound: 26; BG45
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Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence ass
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence ass
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[PMID: 30735902] |
| Sf9 | IC50 |
>20000 nM
Compound: 26; BG45
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Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence assa
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence assa
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[PMID: 30735902] |
| Sf9 | IC50 |
2 μM
Compound: 26; BG45
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Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using (S)-6-acetamido-2-(2-((S)-2-acetamido-4-methylpentanamido)acetamido)-N-(4-methyl-2-oxo-2H-chromen-7-yl)hexanamide as substrate by fluorescence
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[PMID: 30735902] |
In Vitro
BG45 (1.875-30 µM; 48 and 72 h) targets multiple myeloma (MM) cells and inhibits cell growth in a dose-dependent manner[1].
BG45 (15 µM; 0-48 h; MM.1S cells) induces apoptosis via caspase-3/PARP cleavage[1].
BG45 (10 and 20 µM; 12 h; MM.1S cells) induces acetylation of histone H2A, H3, and H4 in a dose-dependent manner[1].
BG45 (10 and 20 µM; 10 h; MM.1S cells) induces multiple myeloma (MM) cells toxicity is associated with hyperacetylation of histones and STAT3 and downregulation of p-STAT3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S, RPMI8226, U266, OPM1, and H929 cells
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Concentration:1.875, 3.75, 7.5, 15, and 30 µM
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Incubation Time:48 and 72 hours
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Result:Inhibited multiple myeloma (MM) cells growth in a dose-dependent manner.
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Cell Line:MM.1S cells
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Concentration:15 µM
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Incubation Time:0, 6, 12, 24, and 48 hours
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Result:Induced caspase-dependent apoptosis in multiple myeloma (MM) cells.
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Cell Line:MM.1S cells
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Concentration:10 and 20 µM
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Incubation Time:12 hours
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Result:Increased acetylation of histone in a dose-dependent manner.
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Cell Line:MM.1S cells
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Concentration:10 and 20 µM
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Incubation Time:10 hours
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Result:Downregulated p-STAT3 in a dose-dependent manner.
Increased acetylation of STAT3 in MM.1S cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID mice (48-54 days old) with MM.1S xenograft model[1]
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Dosage:15 and 50 mg/kg
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Administration:Intraperitoneal injection; 5 days a week for 3 weeks
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Result:Inhibited MM tumor growth in a dose-dependent fashion.
Enhanced either single agent activity in combination with bortezomib (HY-10227).
Chemical Information
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CAS No. 926259-99-6
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Appearance Solid
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Masse moléculaire 214.22
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Formule C11H10N4O
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Color Light yellow to yellow
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SMILES
O=C(C1=NC=CN=C1)NC2=CC=CC=C2N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Alternative splicing of BAZ1A in colorectal cancer disrupts the DNA damage response and increases chemosensitization. [Abstract]2024 Aug 7;15(8):570. PMID: 39112459 -
EMBO J
Acetylation of TIR domains in the TLR4-Mal-MyD88 complex regulates immune responses in sepsis. [Abstract]2024 Nov;43(21):4954-4983. PMID: 39294473 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
Oncol Rep
Metformin facilitates BG45‑induced apoptosis via an anti‑Warburg effect in cholangiocarcinoma cells. [Abstract]2018 Apr;39(4):1957-1965. PMID: 29484415
BG45 purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Apr;39(4):1957-1965. [Abstract]
Cells are treated with 10 mM Metformin, 10 μM BG45, or the combination of both drugs for 48 h, and then lysates are collected and apoptosis-associated markers are examined via western blot analysis.
Solvant et solubilité
In Vitro:
DMSO : ≥ 48 mg/mL (224.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (11.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (11.67 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Minami J, et, al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9. [Content Brief]
[2]. Iaconelli J, et, al. HDAC6 inhibitors modulate Lys49 acetylation and membrane localization of β-catenin in human iPSC-derived neuronal cells. ACS Chem Biol. 2015 Mar 20;10(3):883-90. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 4.6681 mL | 23.3405 mL | 46.6810 mL | 116.7025 mL |
| 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL | 23.3405 mL | |
| 10 mM | 0.4668 mL | 2.3340 mL | 4.6681 mL | 11.6702 mL | |
| 15 mM | 0.3112 mL | 1.5560 mL | 3.1121 mL | 7.7802 mL | |
| 20 mM | 0.2334 mL | 1.1670 mL | 2.3340 mL | 5.8351 mL | |
| 25 mM | 0.1867 mL | 0.9336 mL | 1.8672 mL | 4.6681 mL | |
| 30 mM | 0.1556 mL | 0.7780 mL | 1.5560 mL | 3.8901 mL | |
| 40 mM | 0.1167 mL | 0.5835 mL | 1.1670 mL | 2.9176 mL | |
| 50 mM | 0.0934 mL | 0.4668 mL | 0.9336 mL | 2.3340 mL | |
| 60 mM | 0.0778 mL | 0.3890 mL | 0.7780 mL | 1.9450 mL | |
| 80 mM | 0.0584 mL | 0.2918 mL | 0.5835 mL | 1.4588 mL | |
| 100 mM | 0.0467 mL | 0.2334 mL | 0.4668 mL | 1.1670 mL |
BG45 Related Classifications
HY-18712 Related Classifications
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