[CAS NO. 1550053-02-5] BRD3308
PRODUCTS SPECIFICATIONS [1550053-02-5]
DESCRIPTION [1550053-02-5]
Overview
| MDL | MFCD30187588 |
|---|---|
| Molecular Weight | 287.29 |
| Molecular Formula | C15H14FN3O2 |
| SMILES | O=C(C)NC1=CC=C(C(NC2=CC=C(F)C=C2N)=O)C=C1 |
Summary
BRD3308 is a highly selective HDAC3 inhibitor with an IC 50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 ( IC 50 of 1.26 μM) or HDAC2 ( IC 50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency [1] [2] [3] .
IC50 & Target
|
HDAC3 54 nM (IC 50 ) |
HDAC3 29 nM (Ki) |
HDAC1 1260 nM (IC 50 ) |
HDAC1 5100 nM (Ki) |
HDAC2 1340 nM (IC 50 ) |
HDAC2 6300 nM (Ki) |
HIV-1
|
In Vitro
BRD3308 (5-30 µM; 6-24 hours) treatment increases HIV-1 expression in the 2D10 cell line
[1]
.
BRD3308 (15 µM; overnight) is able to induce outgrowth of HIV-1 from latently infected cells ex vivo in resting CD4+ T cells
[1]
.
BRD3308 inhibits HDAC1, HDAC2 and HDAC3 with K
i
values of 5.1 μM, 6.3 μM and 29 nM, respectively
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
RT-PCR [1]
| Cell Line: | 2D10 cells |
| Concentration: | 5 µM, 10 µM, 15 µM, or 30 µM |
| Incubation Time: | 6 hours, 12 hours, 18 hours, or 24 hours |
| Result: | An increase in HIV-1 expression was observed. |
In Vivo
BRD3308 (5 mg/kg; intraperitoneal injection; every second day; male Zucker Diabetic Fatty rats) treatment reduces hyperglycaemia and increases insulin secretion in a rat model of type 2 diabetes. At the end of the hyperglycaemic clamp, circulating insulin levels are significantly higher in BRD3308-treated rats. Pancreatic insulin staining and contents are also significantly higher. BRD3308 preserves the functional β-cell mass against glucolipotoxicity in vivo [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Zucker Diabetic Fatty (Obese) rats (6-week-old) [2] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; every second day |
| Result: | Reduced hyperglycaemia and increased insulin secretion in a rat model of type 2 diabetes. |
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 : 250 mg/mL ( 870.20 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.4808 mL | 17.4040 mL | 34.8080 mL |
| 5 mM | 0.6962 mL | 3.4808 mL | 6.9616 mL |
| 10 mM | 0.3481 mL | 1.7404 mL | 3.4808 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (7.24 mM); Clear solution
References
- [1] Barton KM, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684.
- [2] Lundh M, et al. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7.
- [3] Wagner FF, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016 Feb 19;11(2):363-74.