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MC4171

Chemical Structure : MC4171

CAS No.:

MC4171 (KAT8 inhibitor 34, MC 4171)

Catalog No.: PC-20777Not For Human Use, Lab Use Only.

MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM.

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Biological Activity

MC4171 (KAT8 inhibitor 34) is a first-in-class, selective and reversible lysine acetyltransferase KAT8 inhibitor with IC50 of 8.1 uM and SPR Kd of 2.04 uM.
MC4171 displays high selectivity against a panel of KATs (KAT2A and the MYST family members KAT5, KAT6A, KAT6B, and KAT7), KDACs (KDAC1–3, 6, and 8).
MC4171 exhibits target engagement as stabilizing KAT8 against thermal-induced aggregation in cells.
MC4171 (50 uM) reduces more than 50% reduction of H4K16Ac in HT29 CRC cell line, with no influence on KAT8 expression levels or on H3K27 acetylation (acetylated by KAT3A/B).
MC4171 displayed antiproliferative activity in A549 cells (65% cell proliferation inhibition at 50 uM; 80% cell proliferation inhibition at 100 uM).
MC4171 is cancer-selective, exhibits mid-micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, without impacting the viability of nontransformed cells.
MC4171 is valuable chemical tool for elucidating KAT8 biology.

Physicochemical Properties

M.Wt 357.37
Formula C21H15N3O3
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

(Z)-4-(4-((1H-pyrrol-2-yl)methylene)-5-oxo-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid

References

1. Francesco Fiorentino, et al. Journal of Medicinal Chemistry. May 8, 2023

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