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Chemical Structure : KPZ560
Catalog No.: PC-21309Not For Human Use, Lab Use Only.
KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively.
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KPZ560 is a potent, HDAC1/2-selective inhibitor with IC50 of 12/68 nM, respectively.
KPZ560 does not strongly inhibit other class I (HDAC3 and HDAC8) and class II HDACs (HDAC4-7 and 9).
KPZ560 inhibits HDAC2 through a two-step slow-binding mechanism.
KPZ560 shows high selectivity and potent cancer cell growth-inhibitory activity (MCF-7, GI50=43 nM) over normal HMEC cells (GI50=9850 nM).
KPZ560 increases the acetylation of histone H3 at lysine 9 (H3K9) and lysine 18 (H3K18) in a dose-dependent manner in MCF-7 cells, also upregulates acetylation of p53 in the presence of etoposide, which induces p53 expression.
KPZ560 induces up-regulation of genes associated with cell proliferation genes and DNA damage.
KPZ560 enhances neurite outgrowth of N2a cells and increases the dendritic spine density in mice.
| M.Wt | 515.61 | |
| Formula | C26H21N5O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yukihiro Itoh, et al. J Med Chem. 2023 Oct 17. doi: 10.1021/acs.jmedchem.3c01095.
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