KPZ560 | HDAC1/2 inhibitor | Probechem Biochemicals

Chemical Structure : KPZ560

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KPZ560 (KPZ-560)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	515.61
分子式	C26H21N5O3S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-[2-Amino-5-(thiophen-2-yl)phenyl]-4-[1-(phenylsulfonylmethyl)-1H-1,2,3-triazol-4-yl]benzamide

参考文献

1. Yukihiro Itoh, et al. J Med Chem. 2023 Oct 17. doi: 10.1021/acs.jmedchem.3c01095.

KPZ560 (KPZ-560)

生物&药学活性

物理化学性质&存储条件

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KPZ560 (KPZ-560)

生物&药学活性

物理化学性质&存储条件

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