Imidazolo-oxindole PKR inhibitor C16

Name: Imidazolo-oxindole PKR inhibitor C16
Brand: MM

≥90% (HPLC), solid, PKR inhibitor, Calbiochem^®

別名:

PKR Inhibitor, Double-stranded RNA-dependent Protein Kinase Inhibitor, C16, Double-stranded RNA-activated Protein Kinase Inhibitor I, EIF2AK2 Inhibitor I

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この商品について

実験式（ヒル表記法）:

C₁₃H₈N₄OS

CAS番号:

608512-97-6

分子量:

268.29

UNSPSC Code:

12352200

NACRES:

NA.77

MDL number:

MFCD06735404

主要文書

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製品名

PKR Inhibitor, The PKR Inhibitor, also referenced under CAS 608512-97-6, controls the biological activity of PKR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

[s]1c2c(nc1)ccc3c2\C(=C\c4nc[nH]c4)\C(=O)N3

InChI

1S/C13H8N4OS/c18-13-8(3-7-4-14-5-15-7)11-9(17-13)1-2-10-12(11)19-6-16-10/h1-6H,(H,14,15)(H,17,18)/b8-3-

InChI key

VFBGXTUGODTSPK-BAQGIRSFSA-N

assay

≥90% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze
protect from light

color

orange to orange-brown

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

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当該品目	527451	527455	406170
Sigma-Aldrich 527450 PKR Inhibitor	Sigma-Aldrich 527451 PKR Inhibitor	Sigma-Aldrich 527455 PKR Inhibitor, Negative Control	Sigma-Aldrich 406170 IP6K Inhibitor
assay ≥90% (HPLC)	assay ≥90% (HPLC)	assay ≥95% (sum of two isomers, HPLC)	assay ≥95% (HPLC)
form solid	form liquid	form solid	form solid
manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®	manufacturer/tradename Calbiochem^®
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. −20°C	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 5 mg/mL	solubility -	solubility DMSO: 10 mg/mL, ethanol: 10 mg/mL	solubility DMSO: 10 mg/mL, methanol: 5 mg/mL

Biochem/physiol Actions

Cell permeable: no

Primary Target
PKR

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 210 nM inhibiting RNA-induced PKR autophosphorylation and 100 nM in rescuing PKR-dependent translation block

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

General description

An imidazolo-oxindole compound that acts as a potent, ATP-binding site directed inhibitor of PKR. Shown to effectively inhibit RNA-induced PKR autophosphorylation (IC₅₀ = 210 nM) and rescue PKR-dependent translation block (IC₅₀ = 100 nM). Inactive control is also available. Shown to increase the late phase of long-lasting synaptic potentiation, and enhance long-term memory in mice. Also available as a 50 mM solution in DMSO (Cat. No. 527451).

Other Notes

Zhu, P.J., et al. 2011. Cell147, 1384.
Jammi, N.V., et al. 2003. Biochem. Biophys. Res. Commun.308, 50.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

試験成績書（COA）

製品のロット番号・バッチ番号を入力して、試験成績書（COA）を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。

以前この製品を購入いただいたことがある場合

文書ライブラリで、最近購入した製品の文書を検索できます。

文書ライブラリにアクセスする

PKR kinase directly regulates tau expression and Alzheimer's disease-related tau phosphorylation.

Lasse Reimer et al.

Brain pathology (Zurich, Switzerland), 31(1), 103-119 (2020-07-28)

Deposition of extensively hyperphosphorylated tau in specific brain cells is a clear pathological hallmark in Alzheimer's disease and a number of other neurodegenerative disorders, collectively termed the tauopathies. Furthermore, hyperphosphorylation of tau prevents it from fulfilling its physiological role as

PACT-mediated PKR activation acts as a hyperosmotic stress intensity sensor weakening osmoadaptation and enhancing inflammation.

Kenneth T Farabaugh et al.

eLife, 9 (2020-03-17)

The inability of cells to adapt to increased environmental tonicity can lead to inflammatory gene expression and pathogenesis. The Rel family of transcription factors TonEBP and NF-κB p65 play critical roles in the switch from osmoadaptive homeostasis to inflammation, respectively.

Progressive Rotavirus Infection Downregulates Redox-Sensitive Transcription Factor Nrf2 and Nrf2-Driven Transcription Units.

Upayan Patra et al.

Oxidative medicine and cellular longevity, 2020, 7289120-7289120 (2020-04-24)

Eukaryotic cells adopt highly tuned stress response physiology under threats of exogenous stressors including viruses to maintain cellular homeostasis. Not surprisingly, avoidance of cellular stress response pathways is an essential facet of virus-induced obligatory host reprogramming to invoke a cellular

Mitophagy antagonism by ZIKV reveals Ajuba as a regulator of PINK1 signaling, PKR-dependent inflammation, and viral invasion of tissues.

Sanket S Ponia et al.

Cell reports, 37(4), 109888-109888 (2021-10-28)

Dysregulated inflammation dominated by chemokine expression is a key feature of disease following infection with the globally important human pathogens Zika virus (ZIKV) and dengue virus, but a mechanistic understanding of how pro-inflammatory responses are initiated is lacking. Mitophagy is

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