UNC1999 | 2449

A potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC₅₀ = 2 nM). UNC1999 is >1000-fold selective for other HMTs except EZH1 (22-fold selectivity). It inhibits H3K27 methylation in MCF10A cells with an IC₅₀ of 124 nM as measured by immunofluorescence.

UNC1999 is a potent histone H3-lysine 27 (H3K27) methyltransferase EZH2 inhibitor (IC₅₀= 2 nM). UNC1999 is >1000-fold selective for other HMTs except EZH1 (22-fold selectivity).

2449 | UNC1999 DataSheet

Alternate Name/Synonyms: 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide

Appearance: White to off-white solid

Formulation: N/A

CAS Number: 1431612-23-5

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₃₃H₄₃N₇O₂

Molecular Weight: 569.74

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO (~15 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent EZH2 methyltransferase inhibitor

MDL Number: N/A

PubChem CID: N/A

SMILES: CC1=CC(CCC)=C(CNC(C2=C(C=NN3C(C)C)C3=CC(C4=CN=C(N5CCN(C(C)C)CC5)C=C4)=C2)=O)C(N1)=O

InChi: InChI=1S/C33H43N7O2/c1-7-8-24-15-23(6)37-33(42)28(24)19-35-32(41)27-16-26(17-30-29(27)20-36-40(30)22(4)5)25-9-10-31(34-18-25)39-13-11-38(12-14-39)21(2)3/h9-10,15-18,20-22H,7-8,11-14,19H2,1-6H3,(H,35,41)(H,37,42)

InChi Key: DPJNKUOXBZSZAI-UHFFFAOYSA-N