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Chemical Structure : SIRT6 inhibitor 11e
Catalog No.: PC-21990Not For Human Use, Lab Use Only.
SIRT6 inhibitor 11e (Compound 11e) is a potent, selective and allosteric SIRT6 inhibitor with IC50 of 0.98 uM, directly binds to SIRT6 with Kd of 9.46 uM, inhibits pancreatic cancer metastasis in vitro and vivo.
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SIRT6 inhibitor 11e (Compound 11e) is a potent, selective and allosteric SIRT6 inhibitor with IC50 of 0.98 uM, directly binds to SIRT6 with Kd of 9.46 uM, inhibits pancreatic cancer metastasis in vitro and vivo.
SIRT6 inhibitor 11e deos not affect the enzymatic activity of SIRT1, SIRT2, SIRT3, and HDAC1-11 at 100 uM.
SIRT6 inhibitor 11e (0-20 uM) upregulates the acetylation levels of H3K9, H3K18, and H3K56 in a concentration-dependent manner in human-derived cell line BxPC-3 and the murine-derived cell line PANC-02.
SIRT6 inhibitor 11e (20 uM) completely blocks the migration of BxPC-3 or PANC-02 cells, which is more potent than JYQ-42 (Cat#PC-49248, 40 uM reached).
SIRT6 inhibitor 11e moderate dose (10 mg/kg, i.p.) displaysmarked inhibition of liver metastases, the high dose of 30 mg/kg shows no obvious weight loss or hepatotoxicity or renal toxicity in mouse-derived pancreatic cancer cells PANC-02, inhibits the metastasis of mouse-derived pancreatic cancer.
| M.Wt | 480.89 | |
| Formula | C22H16ClF3N2O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Xinyuan Xu, et al. Acta Pharm Sin B. 2024 Mar;14(3):1302-1316.
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