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SMYD3 inhibitor 29

Chemical Structure : SMYD3 inhibitor 29

CAS No.: 2095160-79-3

SMYD3 inhibitor 29

Catalog No.: PC-72992Not For Human Use, Lab Use Only.

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 1.7 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SMYD3 inhibitor 29 is a highly potent, selective, covalent inhibitor of histone methyltransferase SMYD3 with IC50 of 11.7 nM.
SMYD3 inhibitor 29 exhibits high potency by inhibiting SMYD3's enzymatic activity and showing antiproliferative activity against HepG2 in 3D cell culture (GI50=1.04 uM).
SMYD3 inhibitor 29 inhibits cellular MAP3K2 methylation.
SMYD3 inhibitor 29 displayed high selectivity when tested against a panel of methyltransferases, namely, SMYD1-2, G9a, PRDM9, and PRMT5.

Physicochemical Properties

M.Wt 491.032
Formula C28H31ClN4O2
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

(R)-1-(4-(2-(4-(1-aminocyclopropyl)phenyl)-4-chloroquinoline-7-carbonyl)-2-methylpiperazin-1-yl)butan-1-one

References

1. Huang C, et al. ACS Med Chem Lett. 2019 May 23;10(6):978-984.

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