8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE
- CAS No.
- 608512-97-6
- Chemical Name:
- 8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE
- Synonyms
- GW 506033X;PKR INHIBITOR;C16 (PKR Inhibitor);InSolution? PKR Inhibitor;GW-506033X(PKR Inhibitor C16);Imidazolo-oxindole PKR inhibitor C16;PKR Inhibitor - CAS 608512-97-6 - Calbiochem;InSolution PKR Inhibitor - CAS 608512-97-6 - Calbiochem;8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE;(Z)-8-((1H-Imidazol-4-yl)methylene)-6H-thiazolo[5,4-e]indol-7(8H)-one
- CBNumber:
- CB3160831
- Molecular Formula:
- C13H8N4OS
- Molecular Weight:
- 268.29
- MDL Number:
- MFCD06735404
- MOL File:
- 608512-97-6.mol
- MSDS File:
- SDS
Boiling point | 674.6±55.0 °C(Predicted) |
---|---|
Density | 1.604±0.06 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | DMSO: soluble12mg/mL |
pka | 10.20±0.20(Predicted) |
form | Orange to orange brown solid |
color | yellow to orange-brown |
Stability | Stable for 2 years from date of purchsae as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
FDA UNII | C9Q75QZK84 |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS07 |
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Signal word | Warning | |||||||||
Hazard statements | H302-H315-H319-H335 | |||||||||
Precautionary statements | P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501 | |||||||||
Hazard Codes | Xi | |||||||||
Risk Statements | 36/37/38 | |||||||||
Safety Statements | 26 | |||||||||
WGK Germany | 3 | |||||||||
NFPA 704 |
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8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE price More Price(23)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich | 527451 | InSolution? PKR Inhibitor | 608512-97-6 | 5mg | $187 | 2024-03-01 | Buy |
Sigma-Aldrich | 527450 | PKR Inhibitor | 608512-97-6 | 5mg | $172 | 2024-03-01 | Buy |
Cayman Chemical | 15323 | PKR Inhibitor ≥95% | 608512-97-6 | 1mg | $32 | 2024-03-01 | Buy |
Cayman Chemical | 15323 | PKR Inhibitor ≥95% | 608512-97-6 | 5mg | $78 | 2024-03-01 | Buy |
Sigma-Aldrich | I9785 | Imidazolo-oxindole PKR inhibitor C16 ≥98% (HPLC) | 608512-97-6 | 5mg | $106 | 2024-03-01 | Buy |
8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE Chemical Properties,Uses,Production
Description
The activity of double-
Uses
PKR Inhibitor is a drug which acts as a selective inhibitor of the enzyme double-stranded RNA-dependent protein kinase (PKR). It has been shown to effectively inhibit PKR function in vivo and has neuroprotective and nootropic effects in animal studies.
Biochem/physiol Actions
Imidazolo-oxindole PKR inhibitor C16 is a selective inhibitor of RNA-dependent protein kinases (PKR, Eif2ak2). C16 is a first reported, potent and selective PKR inhibitor. Its inhibition effect on PKR is ATP-binding site directed. C16 specifically inhibits the apoptotic PKR/eIF2a signaling pathway without stimulating the proliferative mTOR/p70S6K signaling mechanism.
in vitro
pkr inhibitor was identified as a small molecule able to inhibit the autophosphorylation of pkr and to rescue the translation blockade induced by pkr. it was found that pkr inhibitor prevented not only pkr phosphorylation but also the activation of caspase 3 induced by ab in sh-sy5y cells. in addition, the protective effect of pkr inhibitor on the neuronal cell death induced by endoplasmic reticulum-stress in sh-sy5y cells has been reported [1].
in vivo
a previous animal study used an in-vivo model of 7-day-old rat exhibiting a high activation of brain pkr to investigate the effects of pkr inhibitor. results showed for the first time that acute systemic injection of pkr inhibitor could specifically inhibit the apoptotic pkr/eif2a signaling pathway without stimulating the proliferative mtor/p70s6k signaling mechanism [1].
IC 50
186-210 nm
storage
Store at -20°C
References
1) Jammi et al. (2003), Small molecule inhibitors of the RNA-dependent protein kinase; Biochem. Biophys. Res. Commun., 308 50 2) Shimazawa et al. (2007), Involvement of double-stranded RNA-dependent protein kinase in ER stress-induced retinal neuron damage; Ophthalmol. Vis. Sci., 48 3729 3) Ingrand et al. (2007), The oxindole/imidazole derivative C16 reduces in vivo brain PKR activation; FEBS Lett. 581 4473 4) Tronel et al. (2014), The specific PKR inhibitor C16 prevents apoptosis and IL-1β production in an acute excitotoxic rat model with a neuroinflammatory component; Neurochem. Int. 64 73 5) Couturier et al. (2011) Prevention of the β-amyloid peptide-induced inflammatory process by inhibition of double-stranded RNA-dependent protein kinase in primary murine mixed co-cultures; Neuroinflammation, 8 72
8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE Preparation Products And Raw materials
Raw materials
Preparation Products
8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29825 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
Shanghai Acmec Biochemical Technology Co., Ltd. | +undefined18621343501 | product@acmec-e.com | China | 33350 | 58 |
Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Watson Biotechnology Co.,Ltd | +86-18186686046 +86-18186686046 | sales01@watsonbiotech.cn | China | 5853 | 58 |
J & K SCIENTIFIC LTD. | 010-82848833 400-666-7788 | jkinfo@jkchemical.com | China | 94658 | 76 |
Shanghai XR Chemical Technology Co., Ltd. | 021-31007982 18019432809 | info@xrpharma.com | China | 764 | 55 |
Sigma-Aldrich | 021-61415566 800-8193336 | orderCN@merckgroup.com | China | 51471 | 80 |
View Lastest Price from 8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE manufacturers
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2019-12-24 | 8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE
608512-97-6
|
US $1.00 / g | 1g | 99% | 20kg | Career Henan Chemical Co |
-
- 8-(1H-IMIDAZOL-4-YLMETHYLENE)-6,8-DIHYDRO-THIAZOLO[5,4-E]INDOL-7-ONE
608512-97-6
- US $1.00 / g
- 99%
- Career Henan Chemical Co