[CAS NO. 926259-99-6] BG45
PRODUCTS SPECIFICATIONS [926259-99-6]
DESCRIPTION [926259-99-6]
Overview
| MDL | MFCD09046162 |
|---|---|
| Molecular Weight | 214.22 |
| Molecular Formula | C11H10N4O |
| SMILES | O=C(C1=NC=CN=C1)NC2=CC=CC=C2N |
2 Publications Citing Use of MCE
Summary
IC50 & Target
|
HDAC3 0.289 μM (IC 50 ) |
HDAC1 2.0 μM (IC 50 ) |
HDAC2 2.2 μM (IC 50 ) |
HDAC6 >20 μM (IC 50 ) |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | MM.1S, RPMI8226, U266, OPM1, and H929 cells |
| Concentration: | 1.875, 3.75, 7.5, 15, and 30 µM |
| Incubation Time: | 48 and 72 hours |
| Result: | Inhibited multiple myeloma (MM) cells growth in a dose-dependent manner. |
Western Blot Analysis [1]
| Cell Line: | MM.1S cells |
| Concentration: | 15 µM |
| Incubation Time: | 0, 6, 12, 24, and 48 hours |
| Result: | Induced caspase-dependent apoptosis in multiple myeloma (MM) cells. |
Western Blot Analysis [1]
| Cell Line: | MM.1S cells |
| Concentration: | 10 and 20 µM |
| Incubation Time: | 12 hours |
| Result: | Increased acetylation of histone in a dose-dependent manner. |
Western Blot Analysis [1]
| Cell Line: | MM.1S cells |
| Concentration: | 10 and 20 µM |
| Incubation Time: | 10 hours |
| Result: |
Downregulated p-STAT3 in a dose-dependent manner.
Increased acetylation of STAT3 in MM.1S cells. |
In Vivo
BG45 (15-50 mg/kg; i.p.; 5 days a week for 3 weeks; CB17 SCID mice with MM.1S xenograft model) inhibits human multiple myeloma (MM) cells growth and enhances bortezomib (HY-10227) induced cytotoxicity in vivo [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | CB17 SCID mice (48-54 days old) with MM.1S xenograft model [1] |
| Dosage: | 15 and 50 mg/kg |
| Administration: | Intraperitoneal injection; 5 days a week for 3 weeks |
| Result: |
Inhibited MM tumor growth in a dose-dependent fashion.
Enhanced either single agent activity in combination with bortezomib (HY-10227). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 48 mg/mL ( 224.07 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
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
References
- [1] Minami J, et, al. Histone deacetylase 3 as a novel therapeutic target in multiple myeloma. Leukemia. 2014 Mar;28(3):680-9.
- [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.