DC-TEAD3in03 | TEAD3 inhibitor | Probechem Biochemicals

Chemical Structure : DC-TEAD3in03

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DC-TEAD3in03 (TEAD3 inhibitor)

货号: PC-73283Not For Human Use, Lab Use Only.

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

DC-TEAD3in03 is a potent, selective, covalent TEAD3 inhibitor with IC50 of 0.16 uM, 100-fold selectivity over other TEAD isoforms (IC50>20 uM) in ABPP assays.
DC-TEAD3in03 could significantly improve the thermal stability of TEAD3 protein, while it had minimal effect on widetype TEAD1, TEAD1 C359S and TEAD3 C371A mutants, demonstrated selective cellular engagement with Cys371 of TEAD3.
DC-TEAD3in03 showed selective inhibitory effect on TEAD3 in GAL4-TEAD (1–4) reporter assays with IC50 of 1.15 uM in cellular assays.
DC-TEAD3in03 reduced the growth rate of zebrafish caudal fins when administered to zebrafish juveniles.
In the Hippo signaling pathway, the transcription factor TEA domains (TEADs) family proteins (TEAD1‒4) are the most important terminal regulators, which play an important role in development, cell proliferation, cell differentiation, tissue homeostasis, and regeneration.

物理化学性质&存储条件

分子量	288.391
分子式	C17H24N2O2
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-(3-(3-(benzyloxy)propyl)tetrahydropyrimidin-1(2H)-yl)prop-2-en-1-one

参考文献

1. Tian Lu, et al. Acta Pharm Sin B. 2021 Oct;11(10):3206-3219.