SY-589 | DNA Polθ inhibitor | Probechem Biochemicals

Chemical Structure : SY-589

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SY-589 (SY589)

货号: PC-26252Not For Human Use, Lab Use Only.

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生物&药学活性

SY-589 is a highly potent, selective and orally bioavailable DNA polymerase theta (Polθ) helicase inhibitor with ATPase inhibitory IC50 of 2.29 nM in ADP-Glo assays, inhibits microhomology-mediated end joining (MMEJ) pathway.
SY-589 exhibits cellular antiproliferative activity with IC50 of 2.71 nM against DLD1 BRCA2–/– cells.
SY-589 exhibits highly potent microhomology-mediated end joining (MMEJ) inhibition with IC50 of 0.85 nM in nanoluciferase-based MMEJ reporter assay.
SY-589 (0.05-12.8 nM) induces pronounced cell cycle arrest at the S phase in BRCA2-deficient DLD1 cells.
SY-589 shows snergistic antitumor activity with Olaparib in BRCA2-deficient DLD1 cells, significantly enhances Olaparib-induced apoptosis, increasing the apoptotic cell population to 44.2% compared to the blank group (9.13%) and Olaparib monotherapy (17.47%).
SY-589 (0.5, 2.5, or 12.5 mg/kg) demonstrated in vivo synergistic antitumor efficacy.

物理化学性质&存储条件

分子量	552.97
分子式	C24H18ClFN8O3S
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	2''-chloro-N-(3-(1,4-dimethyl-1H-pyrazol-5-yl)-1,2,4-thiadiazol-5-yl)-3-fluoro-5''-methoxy-2-oxo-2H-[1,2':4',4''-terpyridine]-5'-carboxamide

参考文献

1. Chongxun Ge, et al. J Med Chem. 2026 Feb 12;69(3):2789-2813.

SY-589 (SY589)

生物&药学活性

物理化学性质&存储条件

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SY-589 (SY589)

生物&药学活性

物理化学性质&存储条件

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