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Identification of an Ire1alpha Endonuclease Specific Inhibitor With Cytotoxic Activity Against Human Multiple Myeloma

Identification of an Ire1alpha Endonuclease Specific Inhibitor With Cytotoxic Activity Against Human Multiple Myeloma

Ioanna Papandreou, Nicholas C Denko, Michael Olson, Heleen Van Melckebeke, Sofie Lust, Arvin Tam, David E Solow-Cordero, Donna M Bouley, Fritz Offner, Maho Niwa, Albert C Koong

Blood. 2011 Jan 27;117(4):1311-4.

PMID: 21081713

Abstract:

Activation of the adaptive Ire1-XBP1 pathway has been identified in many solid tumors and hematologic malignancies, including multiple myeloma (MM). Here, we report the identification of STF-083010, a novel small-molecule inhibitor of Ire1. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress both in vitro and in vivo. Treatment with STF-083010 showed significant antimyeloma activity in model human MM xenografts. Similarly, STF-083010 was preferentially toxic to freshly isolated human CD138(+) MM cells compared with other similarly isolated cell populations. The identification of this novel Ire1 inhibitor supports the hypothesis that the Ire1-XBP1 axis is a promising target for anticancer therapy, especially in the context of MM.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP307543711	STF-083010		307543-71-1	Price

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