HDAC4 PROTAC TP1

Chemical Structure : HDAC4 PROTAC TP1

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货号: PC-28642Not For Human Use, Lab Use Only.

HDAC4 PROTAC TP1 is a potent, selective Tasquinimod-based PROTAC degrader of HDAC4, exhibits radiosensitizing effectsby enhancing ferroptosis in lung cancer.

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生物&药学活性

HDAC4 PROTAC TP1 is a potent, selective Tasquinimod-based PROTAC degrader of HDAC4, exhibits radiosensitizing effectsby enhancing ferroptosis in lung cancer.
TP1 decreases the protein levels of HDAC4 and MBD1 in in lung cancer LCO-1 and LCO-4 organoids.
TP1 functions by binding to HDAC4, which leads to the CRBN-dependent proteasomal degradation of HDAC4.
TP1 upregulates ferroptosis regulator p53 in lung cancer cells.
TP1 inhibits the growth of A549 and H460 cells, with IC50 values of 1.27 μM and 0.86 μM respectively.
TP1 (10 mg/kg) markedly inhibited tumor growth in the xenograft, induced the degradation of HDAC4 in vivo, within similar effect as that of HDAC4 knockdown.
TP1 promotes the radiosensitivity of patient-derived organoids of lung adenocarcinoma.

物理化学性质&存储条件

分子量	886.93
分子式	C46H49F3N6O9
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	4-((9-(4-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)-9-oxononyl)oxy)-5-methoxy-N,1-dimethyl-2-oxo-N-(4-(trifluoromethyl)phenyl)-1,2-dihydroquinoline-3-carboxamide

参考文献

1. Cheng C, et al. Nat Commun. 2026 May 25;17(1):6832.

HDAC4 PROTAC TP1

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HDAC4 PROTAC TP1

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