Potent, cell-permeable JMJD2 inhibitor (IC 50 = 920 nM). Shows antiviral effects (IC 50 = 10 μM), HSV-1 immediate early gene expression). Reversibly blocks human cytomegalovirus infection in vivo.
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of lysine demethylase 4A;Inhibitor of lysine demethylase 4E
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
1.Whetstine JR, Nottke A, Lan F, Huarte M, Smolikov S, Chen Z, Spooner E, Li E, Zhang G, Colaiacovo M et al.. (2006) Reversal of histone lysine trimethylation by the JMJD2 family of histone demethylases.. Cell, 125 (3):(467-81). [PMID:16603238][10.1021/op500134e]
2.Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON et al.. (2010) Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. Probe Reports from the NIH Molecular Libraries Program, 71 (13):(1755-70). [PMID:24260783][10.1021/op500134e]
3.Reader J, van der Watt ME, Taylor D, Le Manach C, Mittal N, Ottilie S, Theron A, Moyo P, Erlank E, Nardini L et al.. (2021) Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box.. Nat Commun, 12 (1):(269). [PMID:33431834][10.1021/op500134e]
4.Matthews KA, Senagbe KM, Nötzel C, Gonzales CA, Tong X, Rijo-Ferreira F, Bhanu NV, Miguel-Blanco C, Lafuente-Monasterio MJ, Garcia BA et al.. (2020) Disruption of the Plasmodium falciparum Life Cycle through Transcriptional Reprogramming by Inhibitors of Jumonji Demethylases.. ACS Infect Dis, 6 (5):(1058-1075). [PMID:32272012][10.1021/op500134e]
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J2128037