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Tafbromin

Chemical Structure : Tafbromin

CAS No.:

Tafbromin (TAF1(2) inhibitor cis-5)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 393.46
分子式 C23H24FN3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

参考文献

1. Patil S, et al. Angew Chem Int Ed Engl. 2024 May 27:e202404645.

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