1. Cell Cycle/DNA Damage
    Epigenetics
    Anti-infection
  2. HDAC
    HIV
  3. BRD3308

BRD3308 

Cat. No.: HY-19618
Handling Instructions

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.

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BRD3308 Chemical Structure

BRD3308 Chemical Structure

CAS No. : 1550053-02-5

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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[1][2][3].

IC50 & Target[1][3]

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

 

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].

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].

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.
Molecular Weight

287.29

Formula

C₁₅H₁₄FN₃O₂

CAS No.

1550053-02-5

SMILES

O=C(C)NC1=CC=C(C(NC2=CC=C(F)C=C2N)=O)C=C1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BRD3308BRD 3308BRD-3308HDACHIVHistone deacetylasesHuman immunodeficiency virusHDAC3HIV-1latencyinsulinhyperglycaemiaβ-cellsglucolipotoxicityinflammatorycytokinesdiabetesInhibitorinhibitorinhibit

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BRD3308
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HY-19618
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