hRpn13 inhibitor XL44

Chemical Structure : hRpn13 inhibitor XL44

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货号: PC-22061Not For Human Use, Lab Use Only.

XL44 is a potent, specific hRpn13 (proteasome subunit hRpn13)-binding compound, binds to hRpn13 Pru domain, induces loss of hRpn13 Pru and hRpn13-dependent apoptosis.

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生物&药学活性

XL44 is a potent, specific hRpn13 (proteasome subunit hRpn13)-binding compound, binds to hRpn13 Pru domain, induces loss of hRpn13 Pru and hRpn13-dependent apoptosis.
XL44 cannot compete with hRpn2.
XL44 induces the production of cleaved caspase-3 in these hRpn13-expressing trRpn13-MM2 cells, induces apoptosis in RPMI 8226 WT or trRpn13-MM2 with IC50 of 6.2 and 4.5 uM, respectively.
XL44 restricts the viability of multiple cancer cell lines, including breast cancer cell line MCF7, multidrug-resistant ovarian cancer cell line OVCAR-4, and metastatic carcinoma model cell line OVCAR-5, with IC50 values of 2.3 μM, 3.9 μM and 7.1 uM,, respectively.
XL44 reduces protein levels of PCLAF, its downstream target PTTG1 and RRM2 in RPMI 8226 cells.
XL44 dually targets hRpn13 and PCLAF, XL44-induced depletion of PCLAF and RRM2 requires proteasomes.

物理化学性质&存储条件

分子量	388.40
分子式	C23H17FN2O3
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	(Z)-N-(3-((5-fluoro-2-oxoindolin-3-ylidene)methyl)phenyl)-4-methoxybenzamide

参考文献

1. Xiuxiu Lu, et al. Nat Commun. 2024 Mar 20;15(1):2485.