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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-STR-V-53
STR-V-53

Chemical Structure : STR-V-53

CAS No.: 2798954-66-0

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STR-V-53

货号: PC-22104Not For Human Use, Lab Use Only.

STR-V-53 is a novel glycosylated, liver cancer-selective histone deacetylase (HDAC) inhibitor with IC50 of 24.3/60.1/213.43 nM for HDAC1/2/3/6, demonstrates exquisite selective cytotoxicity against human HCC cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

STR-V-53 is a novel glycosylated, liver cancer-selective histone deacetylase (HDAC) inhibitor with IC50 of 24.3/60.1/213.43 nM for HDAC1/2/3/6, demonstrates exquisite selective cytotoxicity against human HCC cells.
STR-V-53 exhibits anti-proliferation effect against Hep-G2 and Huh7 cells with IC50 of 10.4 and 6.25 uM respectively, but lack of
growth inhibition effect against other cancer cells in the NCI-60 panel.
STR-V-53 shows weak inhibition of HDAC 8 and no inhibition of HDAC 11 at the maximum tested concentration of 10 uM.
STR-V-53 is uptaked by GLUT-2 and blockage of GLUT-2 attenuates the cytotoxicity of STR-V-53 against Hep-G2 HCC
cells.
STR-V-53 upregulates PD-L1 and downregulates PD-1 expression, upregulates CD54 (ICAM-1) in HCC cells.
STR-V-53 selectively induces apoptosis in HCC cells, causes cell cycle arrest at the S stage.
STR-V-53 (25, 50 mg/kg, i.p.) effectively suppresses HCC growth in xenograft and murine models of HCC.
STR-V-53 reprogrammed the T cell responses and prolonged median overall survival in an orthotopic HCC model in immunocompetent mice, when combined with anti-PD1 therapy.

物理化学性质&存储条件

分子量 466.49
分子式 C21H30N4O8
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-hydroxy-7-(4-(4-(((2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-1H-1,2,3-triazol-1-yl)heptanamide

参考文献

1. Bocheng Wu, et al. bioRxiv. 2024 Mar 28:2024.03.27.587062.

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