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MedChemExpress - Model BRD3308 - ...

MedChemExpress - Model BRD3308 - 1550053-02-5

BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 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].

BRD3308

MCE China：BRD3308

Brand：MedChemExpress (MCE)

Cat. No.HY-19618

CAS：1550053-02-5

Purity：98.82%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 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.

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 Ki values of 5.1 μM, 6.3 μM and 29 nM, respectively[3].

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].

IC50 & Target：HDAC3 54 nM (IC50) HDAC3 29 nM (Ki) HDAC1 1260 nM (IC50) HDAC1 5100 nM (Ki) HDAC2 1340 nM (IC50) HDAC2 6300 nM (Ki) HIV-1

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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