2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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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LS-170

LS-170 Chemical Structure

CAS No. : 3099617-79-2

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Description

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[1].

IC50 & Target

YEATS2 YEATS

0.14 μM (IC50)

In Vitro

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.

LS-170 Related Antibodies
In Vivo

Nanoparticles loaded with LS-170 (6 mg/kg; intravenous injection; once every 4 days; for 14 days) significantly inhibit tumor growth of non-small cell lung cancer in mice by suppressing the ATAC complex[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice (male, 4-6 weeks) bearing H1299 cells[1]
Dosage: 6 mg/kg
Administration: i.v.; every 4 days; 14 days
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).
Molecular Weight

764.70

Formula

C34H43BrFN5O7S
CAS No.
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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LS-170 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LS-1703099617-79-2LS170LS 170Epigenetic Reader Domainepigenetic eraser proteinsepigenetic reader proteinsH1299 cellslung cancer mouse modelYEATS2 YEATS domainYEATS domain familyU2OS cellsnon-small cell lung cancerATAC complexhistone acetylationInhibitorinhibitorinhibit

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