HL435 | BRD4 degrader | Probechem Biochemicals

Chemical Structure : HL435

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HL435 (HL-435, HL 435)

货号: PC-22411Not For Human Use, Lab Use Only.

HL435 is a potent, alkenyl oxindole-based heterobifunctional BRD4 degrader PROTAC with DC50 values of 11.9 and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively.

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生物&药学活性

HL435 is a potent, alkenyl oxindole-based heterobifunctional BRD4 degrader PROTAC with DC50 values of 11.9 and 21.9 nM in MDA-MB-231 and MCF-7 cells, respectively.
HL435 is demonstrated to efficiently degrade BRD4 in a concentration-dependent manner in multiple cell lines, the Dmax all >95%.
CRL4 DCAF11 complex is potentially responsible for HL435-induced proteasomal degradation activity.
HL435 recruits CRL4DCAF11 complex to induce proteasomal degradation of BRD4.
HL435 potently inhibits proliferation and induces apoptosis of tumor cells in vitro (22RV1 prostate cancer cell, IC50 of 8.6 nM), significantly superior to JQ1 (IC50 = 157 nM).
HL435 not only exhibits excellent antiproliferative capacity against multiple tumor cell lines but also effectively arrests the cell cycle and induces apoptosis in breast cancer cells (MCF-7, MDA-MB-231, IC50=0.38 and 0.21 uM, respectively).
HL435 (20 mg/kg, daily, i.p.) exhibits potent antitumor ability in mouse xenograft tumor model of MDA-MB-231 xenograft.

物理化学性质&存储条件

分子量	1027.35
分子式	C47H48BrClF3N7O7S
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	(S,Z)-2-(4-bromo-2-((2-oxo-6-(trifluoromethyl)indolin-3-ylidene)methyl)phenoxy)-N-(1-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-2-oxo-7,10,13-trioxa-3-azahexadecan-16-yl)acetamide

参考文献

1. Wang Y, et al. PLoS Biol. 2024 May 20;22(5):e3002550.

HL435 (HL-435, HL 435)

生物&药学活性

物理化学性质&存储条件

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HL435 (HL-435, HL 435)

生物&药学活性

物理化学性质&存储条件

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