STF 083010

Chemical Properties

CAS No.	307543-71-1	Cat. No.	BCP16458
Name	STF 083010
Synonyms	STF-083010;STF083010;
Formula	C15H11NO3S2	M. Wt	317.38

Biological Activity

Description	IC50 value: Target: Ire1 inhibitor in vitro: With the addition of STF-083010, splicing was almost completely blocked. STF-083010 also inhibited XBP1 splicing activated by other types of ER stress, including tunicamycin treatment, glucose deprivation, or severe hypoxia. in vivo: Treatment of these reporter mice with bortezomib induced ER stress and a commensurate increase in XBP1-luciferase bioluminescent activity. However, when STF-083010 was injected with bortezomib, there was no increase in bioluminescent signal. This inhibition was not the result of cellular toxicity in the animals, as we did not find any histologic effects of STF-083010 after treatment at doses used in these studies (60 mg/kg one time and 30 mg/kg 2 times.

Description

IC50 value: Target: Ire1 inhibitor in vitro: With the addition of STF-083010, splicing was almost completely blocked. STF-083010 also inhibited XBP1 splicing activated by other types of ER stress, including tunicamycin treatment, glucose deprivation, or severe hypoxia. in vivo: Treatment of these reporter mice with bortezomib induced ER stress and a commensurate increase in XBP1-luciferase bioluminescent activity. However, when STF-083010 was injected with bortezomib, there was no increase in bioluminescent signal. This inhibition was not the result of cellular toxicity in the animals, as we did not find any histologic effects of STF-083010 after treatment at doses used in these studies (60 mg/kg one time and 30 mg/kg 2 times.

Structure

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