A cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM); less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a SIRT1-dependent hypoxic response in vivo

SIRT1/2 Inhibitor IV – 5 mg

Brand:
Cayman
CAS:
14513-15-6
Storage:
-20
UN-No:
Non-Hazardous - /

SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner.{22839} It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases.{22839} By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest.{22839} It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1α protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice.{22840}  

 

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Description

A cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM); less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a SIRT1-dependent hypoxic response in vivo

Formal name: 2,3-dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone

Synonyms:  Cambinol|NSC 112546|SIRT1 Inhibitor II|SIRT2 Inhibitor VI

Molecular weight: 360.4

CAS: 14513-15-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Deacetylases||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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