[CAS NO. 38937-66-5] Suberoyl bis-hydroxamic acid
PRODUCTS SPECIFICATIONS [38937-66-5]
DESCRIPTION [38937-66-5]
Overview
| MDL | MFCD00192455 |
|---|---|
| Molecular Weight | 204.22 |
| Molecular Formula | C8H16N2O4 |
| SMILES | O=C(NO)CCCCCCC(NO)=O |
Summary
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID 50 values of 0.25 μM and 0.30 μM, respectively [1] .Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways [2] .Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC) [3] .
IC50 & Target
|
HDAC1 0.25 μM (IC 50 ) |
HDAC3 0.30 μM (IC 50 ) |
In Vitro
Suberoyl bis-hydroxamic acid (10, 20 or 50 μM; 24 hours) combination with TRAIL improves apoptosis extent, and when TRAIL is combined with 20 μM SBHA (itself causing only 10–15% apoptosis), resulting in 45–50% cell death
[1]
.
Suberoyl bis-hydroxamic acid (20-50 μM; 10-20 hours) alone has little effect on the expression of the proteins Bcl-xL, Mcl-1, and has albeit mildeffect on Bax. When it combines with TRAIL,which increases the ratio of relative protein expression of Bcl-xL and Bax in early periods, while the change in the ratio of Mcl-1 and Bax increases later in MM-BI and Ist-Mes2 cells
[1]
.
Suberoyl bis-hydroxamic acid (30 μM; 6 hours) causes accumulation of acetylated histone H4 in MEL cells
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis [1]
| Cell Line: | MM-BI and Ist-Mes2 cells |
| Concentration: | 10 μM, 20 μM or 50 μM |
| Incubation Time: | 24 hours |
| Result: | Showed a cooperative effect in cell apoptosis. |
In Vivo
Suberoyl bis-hydroxamic acid (intraperitoneal injection; 200 mg/kg; every 2 days; 12 days) reveals a marked increase in the active form of Notch1 (NICD) with a concomitant decrease in ASCL1. It reduces the MTC tumor growth
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nude mice injected with human MTC cells [3] |
| Dosage: | 200 mg/kg |
| Administration: | Intraperitoneal injection; every 2 days; 12 days |
| Result: | Resulted in an average 55% inhibition of tumor growth in SBHA treatment group. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 244.83 mM ; Need ultrasonic)
H 2 O : 8.33 mg/mL ( 40.79 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.8967 mL | 24.4834 mL | 48.9668 mL |
| 5 mM | 0.9793 mL | 4.8967 mL | 9.7934 mL |
| 10 mM | 0.4897 mL | 2.4483 mL | 4.8967 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 5 mg/mL (24.48 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (12.24 mM); Clear solution
References
- [1] Jiri Neuzil, et al. Sensitization of Mesothelioma to TRAIL Apoptosis by Inhibition of Histone Deacetylase: Role of Bcl-xL Down-Regulation. Biochem Biophys Res Commun. 2004 Jan 30;314(1):186-91.
- [2] V M Richon, et al. A Class of Hybrid Polar Inducers of Transformed Cell Differentiation Inhibits Histone Deacetylases.Proc Natl Acad Sci U S A
- [3] Li Ning, et al. Suberoyl Bishydroxamic Acid Activates notch1 Signaling and Suppresses Tumor Progression in an Animal Model of Medullary Thyroid Carcinoma. Ann Surg Oncol. 2008 Sep;15(9):2600-5.