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Chemical Structure| 608512-97-6 Chemical Structure| 608512-97-6

Structure of PKR-IN-C16
CAS No.: 608512-97-6

Chemical Structure| 608512-97-6

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PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. It shows to effectively inhibit RNA-induced PKR autophosphorylation (IC50 = 210 nM) and rescue PKR-dependent translation block (IC50 = 100 nM).

Synonyms: PKR Inhibitor; imoxin; C16, PKR Inhibitor.

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Product Details of PKR-IN-C16

CAS No. :608512-97-6
Formula : C13H8N4OS
M.W : 268.29
SMILES Code : O=C1NC2=C(C(SC=N3)=C3C=C2)C1=CC4=CNC=N4
Synonyms :
PKR Inhibitor; imoxin; C16, PKR Inhibitor.
MDL No. :MFCD28046009
InChI Key :VFBGXTUGODTSPK-BAQGIRSFSA-N
Pubchem ID :6490494

Safety of PKR-IN-C16

GHS Pictogram:
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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 1μM 48 hours Inhibited RSK4 activation, resulting in decreased cellular cIAP1 and cIAP2 expression PMC7126238
Huh7 cells 500, 1000, 2000, 3000 nM 24 hours PMC7083831
HT29 cells 100, 500, 1000 nM 24 hours PMC11031597
HeLa cells 6 μM 2.5 hours To evaluate the ability of BSA–RuII(CO)2 complex to release CO in HeLa cells, results showed a significant increase in intracellular fluorescence indicating CO release. PMC10491595
Retinal endothelial cells 2 µM 16 hours To investigate whether PKR inhibition regulates the NLRP3 inflammasome pathway, results showed that PKR inhibition significantly reduced NLRP3, cleaved caspase 1, and IL-1β levels. PMC6580119
U-2 OS cells 1μM 48 hours C16 attenuates phosphorylation of p53 on Ser46 and Ser392 and prevents or attenuates upregulation of innate immunity genes. PMC7126238
HCT116 cells 100, 500, 1000 nM 24 hours To evaluate the effect of terbinafine on CRC cell viability, results showed that terbinafine significantly reduced the viability of HCT116 cells. PMC11031597

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Tg26 transgenic mouse model Intraperitoneal injection 10 µg/kg body weight Three times weekly from 6 to 12 weeks of age PKR inhibition by compound C16 ameliorates the HIV-associated nephropathy (HIVAN) kidney phenotype in the Tg26 transgenic mouse model, with reversal of mitochondrial dysfunction. PMC11361708
Nude mice Xenograft model Intraperitoneal injection 300 μg/kg Once daily for 4 weeks To evaluate the effect of C16 on HCC tumor growth. C16 significantly suppressed tumor growth and decreased angiogenesis in HCC tissue. PMC7083831

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

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10 mM

3.73mL

0.75mL

0.37mL

18.64mL

3.73mL

1.86mL

37.27mL

7.45mL

3.73mL

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