Chemical Structure : Tafbromin
CAS No.:
Tafbromin
(TAF1(2) inhibitor cis-5)
Catalog No.: PC-22395Not For Human Use, Lab Use Only.
Tafbromin is a selective inhibitor of TAF1 bromodomain by binding to the second bromodomain (TAF1(2)) with KD of 260 nM, inhibits Hh pathway-dependent osteoblast differentiation.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Tafbromin is a selective inhibitor of TAF1 bromodomain by binding to the second bromodomain (TAF1(2)) with KD of 260 nM, inhibits Hh pathway-dependent osteoblast differentiation.
Tafbromin displays no significant binding affinity to BRD7, BRD9, BRPF1 andTRIM24 (KD>10 uM).
Tafbromin inhibits Purmorphamine-induced osteoblast differentiation by modulating canonical Hh signaling and this activity is cell-type dependent and does not involve SMO binding.
Tafbromin does not inhibit Wnt and BMP-induced reporter geneexpression.
Tafbromin reduced the expression of Gli1 and Ptch1 in C3H10T1/2 cells by approximately 75% at a concentration of 5 uM.
Tafbromin is a better selective TAF1 bromodomain 2 ligand compared with CeMMEC1, BAY-299 and GNE-371.
Physicochemical Properties
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M.Wt
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393.46
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Formula
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C23H24FN3O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-((5R,7R)-1-acetyl-7-(4-fluorophenyl)-2,3,5,6,7,8-hexahydro-1H-pyrrolo[3,2-g]quinolin-5-yl)pyrrolidin-2-one
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References
1. Patil S, et al. Angew Chem Int Ed Engl. 2024 May 27:e202404645.
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