WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406266
CAS#: 1431612-23-5
Description: UNC1999, the first orally bioavailable inhibitor that has high in vitro potency for wildtype and mutant EZH2 as well as EZH1. UNC1999 was highly selective for EZH2 and EZH1 over a broad range of epigenetic and non-epigenetic targets, competitive with the cofactor SAM and non-competitive with the peptide substrate. UNC1999 was orally bioavailable in mice, making this inhibitor a valuable tool for investigating the role of EZH2 and EZH1 in chronic animal studies. UNC-1999 represents a useful tools for the biomedical community to investigate the role of EZH2 and EZH1 in health and disease.
MedKoo Cat#: 406266
Name: UNC-1999
CAS#: 1431612-23-5
Chemical Formula: C33H43N7O2
Exact Mass: 569.34782
Molecular Weight: 569.74022
Elemental Analysis: C, 69.57; H, 7.61; N, 17.21; O, 5.62
Synonym: UNC1999; UNC 1999; UNC-1999;
IUPAC/Chemical Name: 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
InChi Key: DPJNKUOXBZSZAI-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=C(NCC1=C(CCC)C=C(C)NC1=O)C2=C3C(N(C(C)C)N=C3)=CC(C4=CC=C(N5CCN(C(C)C)CC5)N=C4)=C2
1: Zhang P, de Gooijer MC, Buil LC, Beijnen JH, Li G, van Tellingen O. ABCB1 and ABCG2 restrict the brain penetration of a panel of novel EZH2-Inhibitors. Int J Cancer. 2015 Oct 15;137(8):2007-18. doi: 10.1002/ijc.29566. Epub 2015 Apr 24. PubMed PMID: 25868794.
2: Katona BW, Liu Y, Ma A, Jin J, Hua X. EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells. Cancer Biol Ther. 2014;15(12):1677-87. doi: 10.4161/15384047.2014.972776. PubMed PMID: 25535899.
3: Xu B, On DM, Ma A, Parton T, Konze KD, Pattenden SG, Allison DF, Cai L, Rockowitz S, Liu S, Liu Y, Li F, Vedadi M, Frye SV, Garcia BA, Zheng D, Jin J, Wang GG. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57. doi: 10.1182/blood-2014-06-581082. Epub 2014 Nov 13. PubMed PMID: 25395428; PubMed Central PMCID: PMC4287641.
4: Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24. PubMed PMID: 23614352; PubMed Central PMCID: PMC3773059.
