JNJ-64619178

A PRMT5 inhibitor

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库存: 现货

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1mg

￥1100.00

880.00

- +
5mg

￥3162.00

2530.00

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10mg

￥5287.00

4230.00

- +
50mg

￥12825.00

10260.00

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已选 0 种 0 瓶

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Background

JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (PRMT5-MEP-50, IC50=0.14 nM), good pharmacokinetic properties and safety.

JNJ-64619178 can be combined with a SAM binding pocket to inhibit the function of PRMT/MEP50 in a time-dependent manner. Various cell lines exhibited different degrees of sensitivity to JNJ-64619178, indicating that JNJ-64619178 inhibits PRMT5 mainly by genomic rather than general targeted cytotoxicity [1].

The methylation of SMD1/3 protein can be selectively and effectively prevented by oral administration of 10 mg/kg JNJ-64619178 per day. SMD1/3 is a key component of the splice and a substrate for PRMT5/MEP50. In the biomarker-driven human small cell lung cancer xenograft model (NCI-H1048), JNJ-64619178 can cause tumor regression and prolong tumor growth inhibition after termination of administration [1].

Reference:

[1] Dirk Brehmer, et al. 108th Annu Meet Am Assoc Cancer Research