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Toyocamycin | Unfolded protein response (UPR) inhibitor

Toyocamycin (606-58-6) is an adenosine analog which inhibits ribozyme self cleavage in mammalian cells, EC50 = 0.4 μM (for expression of a luciferase reporter).1 A potent inhibitor of ER stress-induced XBP1 mRNA splicing.2 It suppresses thapsigargin-, tunicamycin- and 2-deoxyglucose-induced XBP1 mRNA splicing in HeLa cells without affecting ATF6 and PERK activation. Although unable to inhibit IRE1α phosphorylation, toyocamycin prevented IRE1α-induced XBP1 mRNA cleavage in vitro. It inhibits not only ER stress-induced but also constitutive activation of XBP1 expression in multiple myeloma cell lines as well as in primary patient samples.2 Displays synergistic effects with bortezomib. Toyocamycin inhibits unfolded protein response and induces apoptosis in pancreatic cancer cells.3

References/Citations

1) Yen et al. (2006), Identification of inhibitors of ribozyme self-cleavage in mammalian cells via high-throughput screening of chemical libraries; RNA, 12 797
2) Ri et al. (2012), Identification of Toyocamycin, an agent cytotoxic for multiple myeloma cells, as a potent inhibitor of ER stress-induced XBP1 mRNA splicing; Blood Cancer J., 2 e79
3) Chien et al. (2014), Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells; Oncotarget, 5 4881

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Catalog#  10-2750-0005

$70.00
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CAS:
606-58-6
Catalog Number:
10-2750
Activity:
Unfolded protein response (UPR) inhibitor
Chemical Name:
4-Amino-7-β-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Alternate Names:
7-Deaza-7-cyanoadenosine; NSC 63701; NSC 99843; Neuro 000027; Unamycin B; Vengicide
Molecular Weight:
291.26
Molecular Formula:
C12H13N5O4
Solubility:
Soluble in DMSO (up to 25 mg/ml)
Physical Properties:
White or off-white solid
Purity:
97% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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