[CAS NO. 1431612-23-5] UNC1999

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PRODUCTS SPECIFICATIONS [1431612-23-5]

Catalog

SLK-S7165

Brand

Selleck

CAS

1431612-23-5

DESCRIPTION [1431612-23-5]

Overview

MDL	MFCD26960958
Molecular Weight	569.74
Molecular Formula	C33H43N7O2
SMILES	C(C)(C)N1C=2C(=C(C(NCC3=C(CCC)C=C(C)NC3=O)=O)C=C(C2)C=4C=CC(=NC4)N5CCN(C(C)C)CC5)C=N1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

UNC1999 is a potent, orally bioavailable and selective inhibitor of and with of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets. UNC1999 is a potent inducer. UNC1999 specifically suppresses H3K27me3/2 and induces a range of anti-leukemia effects including anti-proliferation, differentiation, and .

Features

The first orally bioavailable inhibitor against wild-type and mutant EZH2 as well as EZH1.

Targets

EZH2 ^[2] (Cell-free assay)	EZH1 ^[2] (Cell-free assay)
2 nM	45 nM

In vitro

UNC1999 is highly potent for both EZH2 Y641N and EZH2 Y641F mutants in vitro. UNC1999 causes concentration-dependent reductions of H3K27me3 in MCF10A cells with IC50 of 124 nM , while shows low cellular toxicity. UNC1999 displays potent, concentration-dependent inhibition of cell proliferation with EC50 of 633 nM in a DLBCL cell line harboring the EZH2Y641N mutant. In addition, biotinylated UNC1999 enriches EZH2 from HEK293T cell lysates, and thus may be used in chemoproteomics studies.

In vivo

Treatment of UNC1999 (150 and 50 mg/kg, i.p.) results in the plasma concentrations of UNC1999 above its cellular IC50 over 24 hours in vivo. In addition, UNC1999 is also orally bioavailable in mice, which makes chronic animal studies more practical and convenient.

References

[1] Konze KD, et al. ACS Chem. Biol. 2013, 8 (6), 1324–1334.
[2] Structural Genomics Consortium.

Synonyms

1H-Indazole-4-carboxamide, N-[(1,2-dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-

N-[(1,2-Dihydro-6-methyl-2-oxo-4-propyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-piperazinyl]-3-pyridinyl]-1H-indazole-4-carboxamide

UNC 1999

6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide