MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 530970 | Name: STF-083010
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

STF-083010, also known as IRE1 Inhibitor I, is an inhibitor of the IRE1/XBP1 pathway. Pretreatment with STF-083010 partially attenuated CPO-induced apoptosis.

Chemical Structure

STF-083010
STF-083010
CAS#307543-71-1

Theoretical Analysis

MedKoo Cat#: 530970

Name: STF-083010

CAS#: 307543-71-1

Chemical Formula: C15H11NO3S2

Exact Mass: 317.0180

Molecular Weight: 317.38

Elemental Analysis: C, 56.77; H, 3.49; N, 4.41; O, 15.12; S, 20.20

Price and Availability

Size Price Availability Quantity
50mg USD 350.00 2 Weeks
100mg USD 650.00 2 Weeks
200mg USD 1,150.00 2 Weeks
500mg USD 2,350.00 2 Weeks
1g USD 3,650.00 2 Weeks
2g USD 6,250.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
STF-083010; STF 083010; STF083010, IRE1 Inhibitor I
IUPAC/Chemical Name
(E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide
InChi Key
TVIVJHZHPKNDAQ-MHWRWJLKSA-N
InChi Code
InChI=1S/C15H11NO3S2/c17-14-8-7-11-4-1-2-5-12(11)13(14)10-16-21(18,19)15-6-3-9-20-15/h1-10,17H/b16-10+
SMILES Code
O=S(C1=CC=CS1)(/N=C/C2=C3C=CC=CC3=CC=C2O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
STF-083010 reduces the splicing of XBP1 by IRE1 in the presence of thapsigargin. STF-083010 has cytotoxic effects against multiple myeloma cells and drives apoptosis in pancreatic cancer cells.
In vitro activity:
STF-083010 has potential as a therapy for multiple myeloma and other cancers. STF-083010 inhibited Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress. STF-083010 was preferentially toxic to freshly isolated human CD138(+) multiple myeloma cells compared with other similarly isolated cell populations. Reference: Blood. 2011 Jan 27;117(4):1311-4. https://pubmed.ncbi.nlm.nih.gov/21081713/
In vivo activity:
STF-083010 has potential to prevent thioacetamide (TAA)-induced acute liver injury. STF-083010 protected against TAA-induced liver injury, as evidenced by higher survival rates in response to a lethal dose of TAA and less severe liver injury in response to a toxic dose of TAA. STF-083010 triggered hepatocyte autophagy in response to TAA stimulation, leading to reduced ROS production and attenuated hepatic inflammation. Reference: Int Immunopharmacol. 2019 Aug;73:261-269. https://pubmed.ncbi.nlm.nih.gov/31121416/
Solvent mg/mL mM
Solubility
DMF 2.0 6.30
DMSO 1.0 3.15
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 317.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Chien W, Ding LW, Sun QY, Torres-Fernandez LA, Tan SZ, Xiao J, Lim SL, Garg M, Lee KL, Kitajima S, Takao S, Leong WZ, Sun H, Tokatly I, Poellinger L, Gery S, Koeffler PH. Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells. Oncotarget. 2014 Jul 15;5(13):4881-94. doi: 10.18632/oncotarget.2051. PMID: 24952679; PMCID: PMC4148107. 2. Papandreou I, Denko NC, Olson M, Van Melckebeke H, Lust S, Tam A, Solow-Cordero DE, Bouley DM, Offner F, Niwa M, Koong AC. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4. doi: 10.1182/blood-2010-08-303099. Epub 2010 Nov 16. PMID: 21081713; PMCID: PMC3056474. 3. Zhan F, Zhao G, Li X, Yang S, Yang W, Zhou S, Zhang F. Inositol-requiring enzyme 1 alpha endoribonuclease specific inhibitor STF-083010 protects the liver from thioacetamide-induced oxidative stress, inflammation and injury by triggering hepatocyte autophagy. Int Immunopharmacol. 2019 Aug;73:261-269. doi: 10.1016/j.intimp.2019.04.051. Epub 2019 May 21. PMID: 31121416. 4. Liu L, Xu L, Zhang S, Wang D, Dong G, Chen H, Li X, Shu C, Wang R. STF-083010, an inhibitor of XBP1 splicing, attenuates acute renal failure in rats by suppressing endoplasmic reticulum stress-induced apoptosis and inflammation. Exp Anim. 2018 Jul 30;67(3):373-382. doi: 10.1538/expanim.17-0131. Epub 2018 Apr 25. PMID: 29695649; PMCID: PMC6083033.
In vitro protocol:
1. Chien W, Ding LW, Sun QY, Torres-Fernandez LA, Tan SZ, Xiao J, Lim SL, Garg M, Lee KL, Kitajima S, Takao S, Leong WZ, Sun H, Tokatly I, Poellinger L, Gery S, Koeffler PH. Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells. Oncotarget. 2014 Jul 15;5(13):4881-94. doi: 10.18632/oncotarget.2051. PMID: 24952679; PMCID: PMC4148107. 2. Papandreou I, Denko NC, Olson M, Van Melckebeke H, Lust S, Tam A, Solow-Cordero DE, Bouley DM, Offner F, Niwa M, Koong AC. Identification of an Ire1alpha endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma. Blood. 2011 Jan 27;117(4):1311-4. doi: 10.1182/blood-2010-08-303099. Epub 2010 Nov 16. PMID: 21081713; PMCID: PMC3056474.
In vivo protocol:
1. Zhan F, Zhao G, Li X, Yang S, Yang W, Zhou S, Zhang F. Inositol-requiring enzyme 1 alpha endoribonuclease specific inhibitor STF-083010 protects the liver from thioacetamide-induced oxidative stress, inflammation and injury by triggering hepatocyte autophagy. Int Immunopharmacol. 2019 Aug;73:261-269. doi: 10.1016/j.intimp.2019.04.051. Epub 2019 May 21. PMID: 31121416. 2. Liu L, Xu L, Zhang S, Wang D, Dong G, Chen H, Li X, Shu C, Wang R. STF-083010, an inhibitor of XBP1 splicing, attenuates acute renal failure in rats by suppressing endoplasmic reticulum stress-induced apoptosis and inflammation. Exp Anim. 2018 Jul 30;67(3):373-382. doi: 10.1538/expanim.17-0131. Epub 2018 Apr 25. PMID: 29695649; PMCID: PMC6083033.
1: Feng B, Lu J, Jiang W, Xu N, Sun W. Chlorpyrifos-oxon induced neuronal cell death via endoplasmic reticulum stress-triggered apoptosis pathways. Toxicol In Vitro. 2024 Dec;101:105939. doi: 10.1016/j.tiv.2024.105939. Epub 2024 Sep 7. PMID: 39251113. 2: Sun DL, Guo ZY, Liu WY, Zhang L, Zhang ZY, Hu YL, Li SF, Zhang MY, Zhang G, Wang JJ, Fang JA. Astragaloside IV Alleviates Podocyte Injury in Diabetic Nephropathy through Regulating IRE-1α/NF-κ B/NLRP3 Pathway. Chin J Integr Med. 2024 Jul 23. doi: 10.1007/s11655-024-3568-0. Epub ahead of print. PMID: 39039342. 3: Blanc M, Habbouche L, Xiao P, Lebeaupin C, Janona M, Vaillant N, Irondelle M, Gilleron J, Murcy F, Rousseau D, Luci C, Barouillet T, Marchetti S, Lacas- Gervais S, Yvan-Charvet L, Gual P, Cardozo AK, Bailly-Maitre B. Bax Inhibitor-1 preserves pancreatic β-cell proteostasis by limiting proinsulin misfolding and programmed cell death. Cell Death Dis. 2024 May 14;15(5):334. doi: 10.1038/s41419-024-06701-x. PMID: 38744890; PMCID: PMC11094198. 4: Yuan S, Liu Y, Mu Y, Kuang Y, Chen S, Zhao YT, Liu Y. Peste des petits ruminants virus infection induces endoplasmic reticulum stress and apoptosis via IRE1-XBP1 and IRE1-JNK signaling pathways. J Vet Sci. 2024 Mar;25(2):e21. doi: 10.4142/jvs.23236. PMID: 38568823; PMCID: PMC10990917. 5: Zhang H, Li J, Wang X, Wang K, Xie J, Chen G, Li Y, Zhong K, Li J, Chen X. IRE1α/XBP-1 promotes β-catenin signaling activation of airway epithelium in lipopolysaccharide-induced acute lung injury. Pulm Pharmacol Ther. 2023 Dec;83:102263. doi: 10.1016/j.pupt.2023.102263. Epub 2023 Nov 5. PMID: 37935327. 6: Chou X, Li X, Ma K, Shen Y, Min Z, Xiao W, Zhang J, Wu Q, Sun D. N-methyl-d- aspartate receptor 1 activation mediates cadmium-induced epithelial-mesenchymal transition in proximal tubular cells. Sci Total Environ. 2023 Dec 15;904:166955. doi: 10.1016/j.scitotenv.2023.166955. Epub 2023 Sep 11. PMID: 37704144. 7: Park SB, Cho GH, Park YE, Chun HS. Emodin, an Emerging Mycotoxin, Induces Endoplasmic Reticulum Stress-Related Hepatotoxicity through IRE1α-XBP1 Axis in HepG2 Cells. Toxins (Basel). 2023 Jul 12;15(7):455. doi: 10.3390/toxins15070455. PMID: 37505724; PMCID: PMC10467057. 8: Hatokova Z, Evinova A, Racay P. STF-083010 an inhibitor of IRE1α endonuclease activity affects mitochondrial respiration and generation of mitochondrial membrane potential. Toxicol In Vitro. 2023 Oct;92:105652. doi: 10.1016/j.tiv.2023.105652. Epub 2023 Jul 21. PMID: 37482139. 9: Huang X, Bian C, Ji H, Ji S, Sun J. DHA induces adipocyte lipolysis through endoplasmic reticulum stress and the cAMP/PKA signaling pathway in grass carp (Ctenopharyngodon idella). Anim Nutr. 2022 Dec 31;13:185-196. doi: 10.1016/j.aninu.2022.10.010. PMID: 37123617; PMCID: PMC10131065. 10: Chen L, Huan X, Jia F, Zhang Z, Bi M, Fu L, Du X, Chen X, Yan C, Jiao Q, Jiang H. Deubiquitylase OTUD3 Mediates Endoplasmic Reticulum Stress through Regulating Fortilin Stability to Restrain Dopaminergic Neurons Apoptosis. Antioxidants (Basel). 2023 Mar 26;12(4):809. doi: 10.3390/antiox12040809. PMID: 37107185; PMCID: PMC10135230. 11: Liu S, Gao Q, Li Y, Lun J, Yu M, Zhang H, Fang J. XBP1s acts as a transcription factor of IRE1α and promotes proliferation of colon cancer cells. Arch Biochem Biophys. 2023 Mar 15;737:109552. doi: 10.1016/j.abb.2023.109552. Epub 2023 Feb 22. PMID: 36828260. 12: Jing G, Zuo J, Fang Q, Yuan M, Xia Y, Jin Q, Liu Y, Wang Y, Zhang Z, Liu W, Wu X, Song X. Erbin protects against sepsis-associated encephalopathy by attenuating microglia pyroptosis via IRE1α/Xbp1s-Ca2+ axis. J Neuroinflammation. 2022 Sep 28;19(1):237. doi: 10.1186/s12974-022-02598-5. PMID: 36171629; PMCID: PMC9520943. 13: Salimi A, Schroeder KM, Schemionek-Reinders M, Vieri M, Maletzke S, Gezer D, Masouleh BK, Appelmann I. Targeting autophagy increases the efficacy of proteasome inhibitor treatment in multiple myeloma by induction of apoptosis and activation of JNK. BMC Cancer. 2022 Jul 6;22(1):735. doi: 10.1186/s12885-022-09775-y. PMID: 35790913; PMCID: PMC9258169. 14: Ye H, Chen C, Wu H, Zheng K, Martín-Adrados B, Caparros E, Francés R, Nelson LJ, Gómez Del Moral M, Asensio I, Vaquero J, Bañares R, Ávila MA, Andrade RJ, Isabel Lucena M, Martínez-Chantar ML, Reeves HL, Masson S, Blumberg RS, Gracia- Sancho J, Nevzorova YA, Martínez-Naves E, Cubero FJ. Genetic and pharmacological inhibition of XBP1 protects against APAP hepatotoxicity through the activation of autophagy. Cell Death Dis. 2022 Feb 10;13(2):143. doi: 10.1038/s41419-022-04580-8. PMID: 35145060; PMCID: PMC8831621. 15: Evinova A, Hatokova Z, Tatarkova Z, Brodnanova M, Dibdiakova K, Racay P. Endoplasmic reticulum stress induces mitochondrial dysfunction but not mitochondrial unfolded protein response in SH-SY5Y cells. Mol Cell Biochem. 2022 Mar;477(3):965-975. doi: 10.1007/s11010-021-04344-6. Epub 2022 Jan 31. PMID: 35098438. 16: Niu J, Wu Z, Xue H, Zhang Y, Gao Q, Li C, Zhao P. Sevoflurane post- conditioning alleviated hypoxic-ischemic brain injury in neonatal rats by inhibiting endoplasmic reticulum stress-mediated autophagy via IRE1 signalings. Neurochem Int. 2021 Nov;150:105198. doi: 10.1016/j.neuint.2021.105198. Epub 2021 Sep 30. PMID: 34601014. 17: Li C, Liu Y, Li Y, Tai R, Sun Z, Wu Q, Liu Y, Sun C. Collagen XV Promotes ER Stress-Induced Inflammation through Activating Integrin β1/FAK Signaling Pathway and M1 Macrophage Polarization in Adipose Tissue. Int J Mol Sci. 2021 Sep 16;22(18):9997. doi: 10.3390/ijms22189997. PMID: 34576160; PMCID: PMC8465275. 18: Rezghi Barez S, Movahedian Attar A, Aghaei M. MicroRNA-30c-2-3p regulates ER stress and induces apoptosis in ovarian cancer cells underlying ER stress. EXCLI J. 2021 May 25;20:922-934. doi: 10.17179/excli2020-2970. PMID: 34121978; PMCID: PMC8192875. 19: Dong L, Tan CW, Feng PJ, Liu FB, Liu DX, Zhou JJ, Chen Y, Yang XX, Zhu YH, Zhu ZQ. Activation of TREM-1 induces endoplasmic reticulum stress through IRE-1α/XBP-1s pathway in murine macrophages. Mol Immunol. 2021 Jul;135:294-303. doi: 10.1016/j.molimm.2021.04.023. Epub 2021 May 3. PMID: 33957479. 20: Chou X, Ma K, Shen Y, Min Z, Wu Q, Sun D. Dual role of inositol-requiring enzyme 1α (IRE-1α) in Cd-induced apoptosis in human renal tubular epithelial cells: Endoplasmic reticulum stress and STAT3 signaling activation. Toxicology. 2021 May 30;456:152769. doi: 10.1016/j.tox.2021.152769. Epub 2021 Apr 1. PMID: 33813002.

View History

CP 461

CP 461