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BRD3308

Catalog No. T8233   CAS 1550053-02-5

BRD3308 is a highly selective inhibitor of HDAC3(IC50 of 54 nM), attenuating PE-mediated phosphorylation of ERK but not JNK.

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BRD3308 Chemical Structure
BRD3308, CAS 1550053-02-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 38.00
2 mg In stock $ 54.00
5 mg In stock $ 87.00
10 mg In stock $ 128.00
25 mg In stock $ 233.00
50 mg In stock $ 352.00
100 mg In stock $ 528.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 97.12%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BRD3308 is a highly selective inhibitor of HDAC3(IC50 of 54 nM), attenuating PE-mediated phosphorylation of ERK but not JNK.
Targets&IC50 HDAC1:1260 nM , HDAC1:5100 nM (Ki) , HDAC3:29 nM (Ki) , HDAC3:54 nM , HDAC2:1340 nM , HDAC2:6300 nM (Ki)
In vivo BRD3308 is a selective HDAC3 inhibitor,to reduce hyperglycaemia and increase insulin secretion in a rat model of type 2 diabetes.?At diabetes onset, an ambulatory hyperglycaemic clamp was performed.?HDAC3 inhibition improved hyperglycaemia over the study period without affecting weight gain.?At the end of the hyperglycaemic clamp, circulating insulin levels were significantly higher in BRD3308-treated rats.?Pancreatic insulin staining and contents were also significantly higher.?These findings highlight HDAC3 as a key therapeutic target for β-cell protection in type 2 diabetes[1].
Animal Research Male Zucker Diabetic Fatty (Obese) rats (6-week-old); 5 mg/kg; Intraperitoneal injection; every second day
Molecular Weight 287.29
Formula C15H14FN3O2
CAS No. 1550053-02-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 52 mg/ml(181 mM)

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Apoptosis Compound Library Bioactive Compound Library Inhibitor Library Histone Modification Compound Library Anti-Cancer Compound Library NF-κB Signaling Compound Library Anti-Breast Cancer Compound Library Epigenetics Compound Library NO PAINS Compound Library

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Keywords

BRD3308 1550053-02-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Proteases/Proteasome HIV Protease HDAC β-cells glucolipotoxicity inflammatory Human immunodeficiency virus Histone deacetylases HDAC3 diabetes HIV-1 Inhibitor latency BRD 3308 cytokines hyperglycaemia HIV inhibit insulin BRD-3308 inhibitor

 

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