Derived from HTS for compounds that increase the SIRT1-mediated deacetylation of a SIRT1-specific substrate; dose-dependently suppresses the NF-κB-dependent induction of TNF-α by LPS in THP-1 cells

CAY10602 – 100 mg

Brand:
Cayman
CAS:
374922-43-7
Storage:
-20
UN-No:
Non-Hazardous - /

Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate.{14683} Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity.{14683} CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.  

 

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SKU: 10009796 - 100 mg Category:

Description

Derived from HTS for compounds that increase the SIRT1-mediated deacetylation of a SIRT1-specific substrate; dose-dependently suppresses the NF-κB-dependent induction of TNF-α by LPS in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity

Formal name: 1-(4-fluorophenyl)-3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]quinoxalin-2-amine

Synonyms: 

Molecular weight: 418.4

CAS: 374922-43-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Activators|Deacetylases||Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation||Research Area|Immunology & Inflammation|Innate Immunity

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