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Chemical Structure : MC4171
CAS No.:
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $248 | In stock | |
| 25 mg | $438 | In stock | |
| 50 mg | $758 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 357.37 | |
| Formula | C21H15N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(Z)-4-(4-((1H-pyrrol-2-yl)methylene)-5-oxo-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid |
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1. Francesco Fiorentino, et al. Journal of Medicinal Chemistry. May 8, 2023
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