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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-JNJ-64619178
JNJ-64619178

Chemical Structure : JNJ-64619178

CAS No.: 2086772-26-9

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JNJ-64619178 (Onametostat, JNJ64619178)

货号: 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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5 mg ￥2380 In stock
10 mg ￥3780 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 483.37
分子式 C22H23BrN6O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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

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