3077714-09-8
Chemical Structure
SY-589
- CAS No.: 3077714-09-8
- Formula:C24H18ClFN8O3S
- Molecular Weight:552.97
InChIKey: IMASFXJJSIIIAS-UHFFFAOYSA-N
SMILES: COC1=C(C=C(Cl)N=C1)C2=CC(N3C(C(F)=CC=C3)=O)=NC=C2C(NC4=NC(C5=C(C=NN5C)C)=NS4)=O
Biological Activity: SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC50=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC50=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors[1].
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SY-589 | 98.50% | SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC50=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC50=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing γ-H2AX levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors. | ||||||||||||||||||||
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