YAP PROTAC YZ-6 | YAP PROTAC | Probechem Biochemicals

Chemical Structure : YAP PROTAC YZ-6

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YAP PROTAC YZ-6 (YAP degrader YZ-6)

货号: PC-22970Not For Human Use, Lab Use Only.

YAP PROTAC YZ-6 is a selective Yes-associated protein (YAP) PROTAC degrader with DC50 of 8.2 uM in NCI-H226 cells, Dmax value of 97%.

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25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

YAP PROTAC YZ-6 is a selective Yes-associated protein (YAP) PROTAC degrader with DC50 of 4.3 uM and 8.2 uM in Huh7 and NCI-H226 cells respectively, Dmax value of 97%.
exhibits potent significant reduction in YAP levels-over 80% at 10 μM in NCI-H226 cell line.
YZ-6 inhibits the CTGF expression at a low concentration of 5 μM in NCI-H226 cells.
YZ-6 shows an IC50 of 2.9 uM for growth inhibition on Huh7 cells that overexpress YAP.
YZ-6 is able to induce the degradation of YAP with a DC50 value of 4.3 μM and effectively inhibits CTGF expression dose dependently in the Huh7 cell line.
YZ-6 also degrades TAZ protein like YAP protein in the Huh7 cell line.
YZ-6 can effectively reduce the total expression and concentration of YAP in the cell nucleus.
YZ-6 (35 mg/kg, i.p.) exhibits in vivo antitumor activity in Huh7 cell-derived xenograft, profoundly suppresses YAP expression, markedly reduces the levels of the YAP-TEAD target genes CTGF and CYR61.

物理化学性质&存储条件

分子量	995.21
分子式	C56H62N6O9S
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	(2S,4R)-4-Hydroxy-1-((S)-2-(3-(2-(2-(2-methoxy-4-(6-oxo-2-phenyl-6,7-dihydro-5H-benzo[b]pyrido[2,3-d]azepin-4-yl)phenoxy)ethoxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Chen Zhou, et al. J Med Chem. 2024 Aug 27. doi: 10.1021/acs.jmedchem.4c00815.

YAP PROTAC YZ-6 (YAP degrader YZ-6)

生物&药学活性

物理化学性质&存储条件

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YAP PROTAC YZ-6 (YAP degrader YZ-6)

生物&药学活性

物理化学性质&存储条件

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