BRD4780 | TMED9 inhibitor | Probechem Biochemicals

Chemical Structure : BRD4780

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BRD4780 (BRD 4780)

货号: PC-73087Not For Human Use, Lab Use Only.

BRD4780 is a small molecule that releases MUC1-fs from TMED9-enriched compartments and promotes its anterograde trafficking to the lysosome, directly binds to TMED9.

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生物&药学活性

BRD4780 is a small molecule that releases MUC1-fs from TMED9-enriched compartments and promotes its anterograde trafficking to the lysosome, directly binds to TMED9.
BRD4780 selectively reduces mutant (EC50=143 nM) but not wild-type MUC1.
BRD4780 phenocopied the effect of TMED9 deletion.
BRD4780 directly binds to TMED9, BRD4780 dose-dependently (EC50 = 143 nM) removes of mutant MUC1-fs without decreasing wild-type MUC1.
BRD4780 showed no effect on MUC1 transcriptional regulation.
BRD4780 rescued P cells from THP-induced cell death, and significantly reduced UPR activation.
BRD4780 removes mutant MUC1-fs from kidneys of heterozygous knockin mice and patient iPSC-derived kidney organoids.
BRD4780 is effective in removing other misfolded proteins (mutant C126R UMOD protein, rhodopsin mutation P23H), but not the mutant version of huntingtin (97 polyQ).

物理化学性质&存储条件

分子量	189.727
分子式	C10H20ClN
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	(1R,2R,3R,4S)-3-Isopropylbicyclo[2.2.1]heptan-2-amine hydrochloride

参考文献

1. Dvela-Levitt M, et al. Cell. 2019 Jul 25;178(3):521-535.e23.

BRD4780 (BRD 4780)

生物&药学活性

物理化学性质&存储条件

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BRD4780 (BRD 4780)

生物&药学活性

物理化学性质&存储条件

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