Cat. #153334

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

Cat. #: 153334

Sub-type: Fluorescent Probe

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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 Kd_app for activation of the catalytic activity of HDAC3:SMRT by Ins(...

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Contributor

Inventor: Andrew Riley ; Barry Potter

Institute: University of Bath

Tool Details

Handling

Target Details

Application Details

References

Tool Details

*FOR RESEARCH USE ONLY

Tool name: HDAC3:SMRT Fluorescent Probe 2-FAM-InsP5 Small Molecule (Tool Compound)
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
Molecular formula: C29H32NO27P5.4.5Et3N
Tool sub type: Fluorescent Probe
Primary target: HDAC3:SMRT Complex
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...
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 Kd_app for activation of the catalytic activity of HDAC3:SMRT by Ins(...
Iupac: 2-O-(2-(5-fluoresceinylcarboxy)-aminoethyl)-myo-inositol 1,3,4,5,6-pentakisphosphate triethylammonium salt
Molecular weight: 1436 g/mol

Handling

Purity: 1436 g/mol
Storage conditions: -20° C, protect from light
Shipping conditions: Dry Ice

Target Details

Primary target: HDAC3:SMRT Complex

Application Details

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 Kd_app for activation of the catalytic activity of HDAC3:SMRT by Ins(...

References

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