STF-083010

• CAT Number: I003089
• CAS Number: 307543-71-1
• Molecular Formula: C15H11NO3S2
• Molecular Weight: 317.4
• Purity: ≥95%
• Target: AChE
• Solubility: DMSO 5 mg/ml
• Storage: Store at -20C
• InChIKey: TVIVJHZHPKNDAQ-MHWRWJLKSA-N

STF-083010 is a novel small-molecule inhibitor of Ire1α; inhibits Ire1 endonuclease activity, without affecting its kinase activity after endoplasmic reticulum stress both in vitro and in vivo.IC50 value:Target: Ire1 inhibitorin 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 [1].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 [1].

Reference

[1]. Papandreou I, et al. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4.
[2]. Chien W, et al. Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells. Oncotarget. 2014 Jul 15;5(13):4881-94.
[3]. Tam AB, et al. Ire1 has distinct catalytic mechanisms for XBP1/HAC1 splicing and RIDD. Cell Rep. 2014 Nov 6;9(3):850-8.