SIRT1/2/3-IN-1

Names

[ CAS No. ]:
2413212-06-1

[ Name ]:
SIRT1/2/3-IN-1

Biological Activity

[Description]:

SIRT1/2/3-IN-1 (compound 10) is a highly potent, selective and cell permeable inhibitor of SIRT1, SIRT2 and SIRT3, with IC50s of 0.54, 0.253, and 0.72 μM respectively. SIRT1/2/3-IN-1 (compound 10) can be used for research of cancer[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Sirtuin
Signaling Pathways >> Cell Cycle/DNA Damage >> Sirtuin

[Target]

0.54 μM(SIRT1), 0.253 μM(SIRT2), and 0.72 μM(SIRT3) [1].


[In Vitro]

SIRT1/2/3-IN-1 (compound 10) possesses cell growth inhibition to cancer cells with time- and concentration-dependently[1]. Western Blot Analysis[1] Cell Line: HCT116 human colon cancer cells Concentration: 0, 0.5, 2, 10, 50, and 100 µM Incubation Time: 8 h Result: Inhibited deacetylation of the K382-acetylated tumor suppresser protein p53. Cell Proliferation Assay[1] Cell Line: Human MCF-7 breast cancer cells and human SK-MEL-2 melanoma cells Concentration: 0, 5, 12.5, 25, 50 or 100 µM Incubation Time: 24 h, 48 h or 72 h Result: Concentration-dependently inhibited cell growth

[References]

[1]. Li R , et al. A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring Nε-thioacetyl-lysine[J]. Bioorganic & Medicinal Chemistry, 2020, 28(7):115356.

Chemical & Physical Properties

[ Molecular Formula ]:
C46H63N9O8S2

[ Molecular Weight ]:
934.18


Related Compounds

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