HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)

Targeting HDACS provides promising epigenetic therapies for many diseases including Alzheimer’s and spinal muscular atrophy.

Contributors

Inventor Institute
Andrew Riley ; Barry Potter University of Bath
Cat. #: 153334
Tool sub type: Fluorescent Probe
Research Fields: Cancer;Drug development;Stem cell biology
Application: 2-FAM-InsP5 [2-FAM-Ins(1,3,4,5,6)P5] is a fluorescent derivative of Ins(1,3,4,5,6)P5. 2-FAM-InsP5 activates the HDAC3:SMRT complex in a similar manner to the natural ligand, Ins(1,4,5,6)P4. The binding constant (Kd) for binding of 2-FAM-InsP5 to HDAC3:SMRT measured by a direct binding assay, 0.3 Âą 0.01 ÎźM, was approximately 10-fold lower than the Kdapp for activation of the catalytic activity of HDAC3:SMRT by Ins(…
Alternate name: HDACs; Histone deacetylases; SMRT; silencing mediator for retinoid or thyroid-hormone receptors; Nuclear receptor co-repressor 2; NCOR2; HDAC:SMRT3; 2-FAM-InsP5; T3 receptor-associating cofactor 1; TRAC-1
Product description: Class I histone deacetylase (HDAC) enzymes are involved in epigenetic gene regulation by controlling acetylation of lysine sidechains in histone tails They form a catalytic subunit for other large protein complexes that repress gene expression when targeted to genomic DNA. The Class I HDAC family includes HDACs 1, 2, 3 & 8, however only HDAC3 is recruited exclusively to the SMRT co-repressor complex. Functional and structural studies of HDACs when bound to their cognate corepressors has reve…
Molecular weight: 1436 g/mol
Primary target: HDAC3:SMRT Complex
Storage conditions: -20° C, protect from light
Shipping conditions: Dry Ice
References:

Watson et al. 2016. Nat Commun. 7:11262. PMID: 27109927.

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