hRpn13 inhibitor XL44

Chemical Structure : hRpn13 inhibitor XL44

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	388.40
Formula	C23H17FN2O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(Z)-N-(3-((5-fluoro-2-oxoindolin-3-ylidene)methyl)phenyl)-4-methoxybenzamide

References

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