LS-170
LS-170 is a YEATS2 YEATS domain inhibitor with an IC50 of 0.14 μM. LS-170 displays selectivity for the YEATS2 YEATS domain over other YEATS domain family members and other epigenetic 'reader' and 'eraser' proteins. LS-170 reduces chromatin occupancy of the Ada-two-A-containing (ATAC) complex, decreases ATAC-dependent histone acetylation levels, and downregulates expression of ATAC-governed genes. LS-170 suppresses tumor growth in a lung cancer mouse model. LS-170 can be used for the research of non-small cell lung cancer.
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- CAS. Nr.: 3099617-79-2
- Formel: C34H43BrFN5O7S
- Molecular Weight:764.70
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Biologische Aktivität
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YEATS2 YEATS 0.14 μM (IC50) |
LS-170 (0.14 μM) selectively inhibits the YEATS2 YEATS domain with an IC50 of 0.14 μM without affecting other YEATS domains or epigenetic reader/eraser proteins[1].
LS-170 (20 μM; 24 h) selectively dissociates YEATS2 from chromatin in U2OS cells without affecting other YEATS domain proteins[1].
LS-170 (20 μM) selectively targets the ATAC complex (YEATS2 and MBIP subunits) in H1299 cells[1].
LS-170 (20 μM; 24 h) displaces YEATS2 from chromatin at ATAC-bound gene promoters in H1299 cells[1].
LS-170 reduces ATAC-dependent histone acetylation marks (H3K9ac, H3K14ac, H3K27ac) in H1299 cells without altering YEATS2 expression[1].
LS-170 (20 μM; 24 h) downregulates ATAC-governed genes involved in DNA replication and cell cycle in H1299 cells[1].
LS-170 (72 h) inhibits the growth of NSCLC cell lines with GI50 values ranging from 6.8 μM (H157) to 29.0 μM (A549)[1].
LS-170 (20 μM; 14 days) inhibits colony formation in H1299, A549, and PC9 NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male, 4-6 weeks) bearing H1299 cells[1]
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Dosage:6 mg/kg
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Administration:i.v.; every 4 days; 14 days
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Result:Significantly suppressed tumor growth, reduced tumor volume, decreased Ki67 staining, decreased H3K9ac levels, and caused moderate reductions in H3K14ac, H3K27ac, and H4K16ac in tumor tissues. Observed no reduction in body weight or hepatotoxicity (unchanged AST/ALT levels).
Chemical Information
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CAS. Nr. 3099617-79-2
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Molecular Weight 764.70
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Formel C34H43BrFN5O7S
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SMILES
O=C(NCCCC[C@@H](C(N[C@@H](CC1=CC=C(F)C=C1)C(N(C)[C@@H](C)C(N2CCCCC2)=O)=O)=O)NS(=O)(C)=O)C3=CC4=C(O3)C=C(Br)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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