WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406819
Description: ZLD1039 is a potent, highly selective, and orally bioavailable small molecule inhibitor of EZH2, which inhibited breast tumor growth and metastasis. ZLD1039 considerably inhibited EZH2 methyltransferase activity with nanomolar potency, decreased global histone-3 lysine-27 (H3K27) methylation, and reactivated silenced tumor suppressors connected to increased survival of patients with breast cancer. Comparable to conditional silencing of EZH2, its inhibition by ZLD1039 decreased cell proliferation, cell cycle arrest, and induced apoptosis. ZLD1039 is a promising treatment for breast cancer.
MedKoo Cat#: 406819
Chemical Formula: C36H48N6O3
Exact Mass: 612.3788
Molecular Weight: 612.819
Elemental Analysis: C, 70.56; H, 7.90; N, 13.71; O, 7.83
Synonym: ZLD1039; ZLD-1039; ZLD 1039.
IUPAC/Chemical Name: 3-[Ethyl(tetrahydro-2H-pyran-4-yl)amino]-N-[(2,3,5,6,7,8-hexahydro-1-methyl-3-oxo-4-isoquinolinyl)methyl]-2-methyl-5-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-benzamide
InChi Key: SZAYCVHJDOWSNY-UHFFFAOYSA-N
InChi Code: InChI=1S/C36H48N6O3/c1-5-42(28-12-18-45-19-13-28)33-21-27(26-10-11-34(37-22-26)41-16-14-40(4)15-17-41)20-31(24(33)2)35(43)38-23-32-30-9-7-6-8-29(30)25(3)39-36(32)44/h10-11,20-22,28H,5-9,12-19,23H2,1-4H3,(H,38,43)(H,39,44)
SMILES Code: O=C(NCC1=C2CCCCC2=C(C)NC1=O)C3=CC(C4=CC=C(N5CCN(C)CC5)N=C4)=CC(N(CC)C6CCOCC6)=C3C
1: Song X, Gao T, Wang N, Feng Q, You X, Ye T, Lei Q, Zhu Y, Xiong M, Xia Y, Yang
F, Shi Y, Wei Y, Zhang L, Yu L. Corrigendum: Selective inhibition of EZH2 by
ZLD1039 blocks H3K27methylation and leads to potent anti-tumor activity in breast
cancer. Sci Rep. 2016 Apr 29;6:24893. doi: 10.1038/srep24893. PubMed PMID:
27128979; PubMed Central PMCID: PMC4850860.
2: Song X, Gao T, Wang N, Feng Q, You X, Ye T, Lei Q, Zhu Y, Xiong M, Xia Y, Yang
F, Shi Y, Wei Y, Zhang L, Yu L. Selective inhibition of EZH2 by ZLD1039 blocks
H3K27 methylation and leads to potent anti-tumor activity in breast cancer. Sci
Rep. 2016 Feb 12;6:20864. doi: 10.1038/srep20864. PubMed PMID: 26868841; PubMed
Central PMCID: PMC4751454.