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HDAC3 inhibitor LSQ-28

Chemical Structure : HDAC3 inhibitor LSQ-28

CAS No.:

HDAC3 inhibitor LSQ-28

Catalog No.: PC-23965Not For Human Use, Lab Use Only.

LSQ-28 is a potent, selective HDAC3 inhibitor with IC50 of 42 nM, >150-fold selective over HDAC1, HDAC2, and HDAC6.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

LSQ-28 is a potent, selective HDAC3 inhibitor with IC50 of 42 nM, >150-fold selective over HDAC1, HDAC2, and HDAC6.
LSQ-28 does not inhibit HDAC4, 5, 7–10 at concentrations up to 10 μM, but inhibits HDAC11 with an IC50 value of 8.87 μM.
LSQ-28 exhibits antiproliferative activities across HCT-116 (colorectal carcinoma), 4T1 (breast cancer), B16-F10 (melanoma), and SK-OV-3 (ovarian cancer) with IC50 of 5.558 to 12.49 μM.
LSQ-28 inhibits B16-F10 cell migration, markedly reduces the invasive capacity, possesses apoptotic potential.
LSQ-28 (5, 10, and 20 μM) induced a significant increase in Ac-H3 levels in B16-F10 and 4T1 cells.
LSQ-28 induces a dose-dependent degradation in PD-L1 levels in B16-F10 cells.
LSQ-28 enhancse the antitumor activity of PARP inhibitors through a synergistic enhancement of the DNA-damage response.
Combination treatment of LSQ-28 and olaparib significantly enhanced TGI, achieving a TGI of 91% in in 4T1 tumor xenograft models.

Physicochemical Properties

M.Wt 485.59
Formula C31H27N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N'-Propyl-4-((6-(pyridin-2-yl)-11H-indolo[3,2-c]quinolin-11-yl)methyl)benzohydrazide

References

1. Li S, et al. J Med Chem. 2025 Jan 28. doi: 10.1021/acs.jmedchem.4c02445.

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