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SIRT6 inhibitor 10d

Chemical Structure : SIRT6 inhibitor 10d

CAS No.:

SIRT6 inhibitor 10d

Catalog No.: PC-23601Not For Human Use, Lab Use Only.

SIRT6 inhibitor 10d is a potent, selective competitive SIRT6 inhibitor, effectively inhibits the deacetylation activity of SIRT6 on fluorescent acetyl substrate Ac-RHKK(Ac)-AMC with IC50 of 5.8 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SIRT6 inhibitor 10d is a potent, selective competitive SIRT6 inhibitor, effectively inhibits the deacetylation activity of SIRT6 on fluorescent acetyl substrate Ac-RHKK(Ac)-AMC with IC50 of 5.8 uM.
SIRT6 inhibitor 10d displays >27-fold selective over other SIRTs.
SIRT6 inhibitor 10d inhibits the proliferation of MCF-7 cells in a dose-dependent manner, with an IC50 of 8.3 uM.
SIRT6 inhibitor 10d (20 uM) inhibits the deacetylation activity of SIRT6 in breast cancer MCF-7 cells.
SIRT6 inhibitor 10d (5-20 uM) inhibits the proliferation, migration, and invasion of breast cancer MCF-7 cells, blocks the DNA damage repair pathway in breast cancer and promotes apoptosis.
SIRT6 inhibitor 10d (10, 20, and 40 mg/kg) exhibits antibreast cancer activity in mice bearing 4T1 tumor graft.

Physicochemical Properties

M.Wt 451.91
Formula C26H18ClN5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-Chloro-9-(4-cyanobenzyl)-N-(pyridin-2-ylmethyl)-9H-pyrido[3,4-b]indole-3-carboxamide

References

1. Liang C, et al. J Med Chem. 2024 Dec 4. doi: 10.1021/acs.jmedchem.4c01921.

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