ALDH1A1 inhibitor 974 | ALDH1A1 inhibitor | Probechem Biochemicals

Chemical Structure : ALDH1A1 inhibitor 974

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ALDH1A1 inhibitor 974 (ALDH1A1i 974)

货号: PC-49238Not For Human Use, Lab Use Only.

ALDH1A1 inhibitor 974 (Compound 974) is a first-in-class, highly potent and specific ALDH1A1 inhibitor with IC50 of 470 nM, suppresses chemotherapy-induced senescence as well as stemness.

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生物&药学活性

ALDH1A1 inhibitor 974 (Compound 974) is a first-in-class, highly potent and specific ALDH1A1 inhibitor with IC50 of 470 nM, suppresses chemotherapy-induced senescence as well as stemness.
Compound 974 (5 µM for 48 h) significantly reduces the percentage of ALDH-positive cells in OVCAR3 and OVCAR5 cells, does not affect the proliferation of normal ovarian cells.
Compound 974 significantly decreases the expression of the well-known stemness genes Bmi-1, Nanog, Oct4, and Sox2 in OVCAR3 and OVCAR5 cells.
Compound 974 significantly reduces cancer stem cells (CSC) frequency in mice, suppresses ovarian cancer stemness in vivo.
Compound 974 suppresses pathways involved in chemoresistance and stemness, significantly downregulates the senescence biomarkers p21(CDKN1A) and p15INK4b (CDKN2B) and genes associated with the senescence-associated secretory phenotype (SASP), including IL6, IL8, CXCL1, and CXCL3.
Compound 974 suppressed CDDP-induced senescence-associated beta galactosidase (SA-β gal) staining in OVCAR3 cells, also significantly reduces the basal and CDDP-induced expression of senescence marker p21 (CDKN1A) in OVCAR3 cells and SASP gene expression in OVCAR3 and OVCAR5 cells.

物理化学性质&存储条件

分子量	395.499
分子式	C24H29NO4
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	1'-methyl-2'-(piperidine-1-carbonyl)spiro[cycloheptane-1,7'-furo[3,2-f]chromen]-9'(8'H)-one

参考文献

1. Tang J., et al. Mol. Cancer Res. 2018;16:1226–1240.

2. Vaishnavi Muralikrishnan, et al. Cancers (Basel). 2022 Jul 15;14(14):3437.

ALDH1A1 inhibitor 974 (ALDH1A1i 974)

生物&药学活性

物理化学性质&存储条件

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ALDH1A1 inhibitor 974 (ALDH1A1i 974)

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物理化学性质&存储条件

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