UNC2399

Names

[ Name ]:
UNC2399

Biological Activity

[Description]:

UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM[1][2].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[Target]

EZH2:17 nM (IC50)

[In Vitro]

UNC2399 (1-1000 nM) displays high in vitro potency (IC50=17±2 nM) in the EZH2 radioactive biochemical assay[1]. UNC2399 (100 μM) enriches EZH2 from HEK293T cell lysates[1].

[References]

[1]. Konze KD, et, al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013; 8(6): 1324-34.

[2]. Ma A, et, al. Discovery of a first-in-class EZH2 selective degrader. Nat Chem Biol. 2020 Feb;16(2):214-222.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₈H₆₆N₁₀O₇S

[ Molecular Weight ]:
927.17

Related Compounds

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