ChemicalBook > CAS DataBase List > STF 083010

STF 083010

Product Name
STF 083010
CAS No.
307543-71-1
Chemical Name
STF 083010
Synonyms
CS-2901;CS-2595;STF 083010;STF-083010;STF083010;STF 083010;N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide;N-((2-Hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide;2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]-;(E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide;STF 083010,STF-083010,Inositol requiring enzyme 1,Inhibitor,inhibit,IRE1
CBNumber
CB22701433
Molecular Formula
C15H11NO3S2
Formula Weight
317.38
MOL File
307543-71-1.mol
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STF 083010 Property

Melting point:
199-201°C
Boiling point:
548.4±56.0 °C(Predicted)
Density 
1.40±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
DMSO: soluble5mg/mL (clear solution)
form 
powder
pka
7.31±0.50(Predicted)
color 
light yellow to yellow-green
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
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Safety

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0409
Product name
STF-083010
Purity
≥98% (HPLC)
Packaging
5mg
Price
$127
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0409
Product name
STF-083010
Purity
≥98% (HPLC)
Packaging
25mg
Price
$505
Updated
2024/03/01
Cayman Chemical
Product number
17370
Product name
STF-083010
Purity
≥98%
Packaging
5mg
Price
$47
Updated
2024/03/01
Cayman Chemical
Product number
17370
Product name
STF-083010
Purity
≥98%
Packaging
10mg
Price
$85
Updated
2024/03/01
Cayman Chemical
Product number
17370
Product name
STF-083010
Purity
≥98%
Packaging
25mg
Price
$165
Updated
2024/03/01
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STF 083010 Chemical Properties,Usage,Production

Description

STF-083010 (307543-71-1) is a novel small molecule inhibitor of IRE1. It inhibits IRE1 endonuclease activity but not its kinase activity after endoplasmic reticulum stress.1-3 It displays significant antimyeloma activity in model human MM xenografts.1?STF-083010 induces apoptosis in pancreatic cancer cells and displays growth inhibition in a clonogenic growth assay in soft agar as well as in a xenograft?in vivo model of pancreatic cancer.4?Active?in vivo.

Uses

STF 083010 is an inhibitor of Ire1 endonuclease.

Uses

STF-083010 has been used:

  • in a study to investigate the?potential?anti-lipotoxic effect of nicotinamide and to elucidate underlying mechanism(s)
  • as IRE1a inhibitor to study its effect on NOS 2 expression and investigate the underlying mechanisms in proinflammatory gene expression in astrocytes
  • to block endogenous XBP1 cleavage for one hour prior to palmitate exposure in order to examine whether inositol?requiring enzyme 1α (IRE1α ) activation is implicated in palmitate cytotoxicity

Biochem/physiol Actions

STF-083010 is a potent inhibitor of the ER transmembrane protein IRE1, which mediates the unfolded protein response. STF-083010 inhibits IRE1 endonuclease and mRNA splicing activity in response to endopasmic reticulum (ER) stress, but has no affect on the kinase activity of IRE1.

in vitro

after endoplasmic reticulum stress both in vitro and in vivo, stf-083010 prevented ire1 endonuclease activity without affecting its kinase activity. treatment with stf-083010 exhibited significant antimyeloma activity in model human mm xenografts. similarly, compared with other similarly isolated cell populations, stf-083010 was preferentially toxic to freshly isolated human cd138 mm cells. on basis of the identification of this novel ire1 inhibitor, propose that the ire1-xbp1 axis is a promising target for anticancer therapy (especially in the context of mm) [1].

in vivo

the small molecule stf083010, identified by a high-throughput screen of compounds affecting ire1 activity, was capable of directly inhibiting the endonuclease function of ire1 without affecting its kinase activity. after treatment of mice harboring subcutaneous xenografts led to tumor shrinkage and multiple myeloma cells harvested from cancer patients died following exposure to stf083010, the antimyeloma therapeutic potential of stf083010 was convincingly demonstrated [2].

storage

Store at -20°C

References

1) Papandreou?et al. (2011),?Identification of an Ire1α endonuclease specific inhibitor with cytotoxic activity against human multiple myeloma; Blood,?117?1311 2) Wang?et al. (2012),?Divergent allosteric control of the IRE1α endoribonuclease using kinase inhibitors; Nature Chem. Biol.,?8?982 3) Tam?et al. (2014),?Ire1 has distinct catalytic mechanisms for XBP/HAC1 splicing and RIDD; Cell Rep.,?9?850 4) Chien?et al. (2014),?Selective inhibition of unfolded protein response induces apoptosis in pancreatic cancer cells; Oncotarget,?5?4881

STF 083010 Preparation Products And Raw materials

Raw materials

Preparation Products

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STF 083010 Suppliers

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View Lastest Price from STF 083010 manufacturers

Career Henan Chemical Co
Product
STF 083010 307543-71-1
Price
US $1.00/g
Min. Order
100g
Purity
>98%
Supply Ability
g/kg/Ton
Release date
2020-01-14

307543-71-1, STF 083010Related Search:


  • STF-083010;STF083010;STF 083010
  • CS-2595
  • CS-2901
  • STF 083010
  • (E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide
  • N-[(2-Hydroxy-1-naphthalenyl)methylene]-2-thiophenesulfonamide
  • 2-Thiophenesulfonamide, N-[(2-hydroxy-1-naphthalenyl)methylene]-
  • N-((2-Hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide
  • STF 083010,STF-083010,Inositol requiring enzyme 1,Inhibitor,inhibit,IRE1
  • 307543-71-1
  • Inhibitors