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JNJ-64619178

Chemical Structure : JNJ-64619178

CAS No.: 2086772-26-9

JNJ-64619178 (Onametostat, JNJ64619178)

Catalog No.: PC-72444Not For Human Use, Lab Use Only.

JNJ-64619178 (Onametostat, JNJ 64619178) is a selective, and potent PRMT5 inhibitor with Kiapp of 0.77 nM, inhibits the PRMT5/MEP50 complex impairing cancer cell proliferation.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

JNJ-64619178 (Onametostat, JNJ 64619178) is a selective, and potent PRMT5 inhibitor with Kiapp of 0.77 nM, inhibits the PRMT5/MEP50 complex impairing cancer cell proliferation.
JNJ-64619178 displays high selectivity gainst 37 purified recombinant human arginine (Arg) and lysine (Lys) methyltransferases, including 4 DNA methyltransferases, with exception of MEP50 (Kd <0.1 nM) and RIOK1 (Kd<0.1 nM).
JNJ-64619178 inhibited general nuclear arginine dimethylation by IHC assay on A549 cells (IC50=0.2 nM), JNJ-64619178 inhibited dimethylation of SmD1/3 (reduction of SmD1/3-Me2 levels) by >50% and 80% at 1 and 10 nmol/L concentrations, respectively.
JNJ-64619178 inhibited cell proliferation in a panel of lung cancer cell lines with IC50 of 0.4-1.9 nM.
JNJ-64619178 demonstrates sustained target engagement associated with potent antitumor activity in tumor-xenograft mouse models.

Physicochemical Properties

M.Wt 483.37
Formula C22H23BrN6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1S,2R,3S,5R)-3-(2-(2-amino-3-bromoquinolin-7-yl)ethyl)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol

References

1. Brehmer D, et al. Mol Cancer Ther. 2021 Dec;20(12):2317-2328.

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