Chemical Structure : JNJ-64619178
CAS No.: 2086772-26-9
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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10 mg | $378 | In stock | |
25 mg | $598 | In stock | |
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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.
M.Wt | 483.37 | |
Formula | C22H23BrN6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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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 |
1. Brehmer D, et al. Mol Cancer Ther. 2021 Dec;20(12):2317-2328.
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