LS-170
Based on 1 Customer Validation
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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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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.
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (65.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
Verweise
Complete Stock Solution Preparation Table
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3077 mL | 6.5385 mL | 13.0770 mL | 32.6926 mL |
| 5 mM | 0.2615 mL | 1.3077 mL | 2.6154 mL | 6.5385 mL | |
| 10 mM | 0.1308 mL | 0.6539 mL | 1.3077 mL | 3.2693 mL | |
| 15 mM | 0.0872 mL | 0.4359 mL | 0.8718 mL | 2.1795 mL | |
| 20 mM | 0.0654 mL | 0.3269 mL | 0.6539 mL | 1.6346 mL | |
| 25 mM | 0.0523 mL | 0.2615 mL | 0.5231 mL | 1.3077 mL | |
| 30 mM | 0.0436 mL | 0.2180 mL | 0.4359 mL | 1.0898 mL | |
| 40 mM | 0.0327 mL | 0.1635 mL | 0.3269 mL | 0.8173 mL | |
| 50 mM | 0.0262 mL | 0.1308 mL | 0.2615 mL | 0.6539 mL | |
| 60 mM | 0.0218 mL | 0.1090 mL | 0.2180 mL | 0.5449 mL |
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