参考文献 Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306 Janek Szychowski*, Robert Papp, Evelyne Dietrich,et al. Repare Therapeutics(加拿大) Publication Date:July 26, 2022 https://doi.org/10.1021/acs.jmedchem...
药学权威期刊Journal of Medicinal Chemistry在线发表题为“Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor,RP-6306”。研究人员运用药物化学方法对筛选得到的先导结构进行优化,得到了第一个有选择性且可口服的PKMYT1抑制剂—RP-6306,...
https://molecular-cancer.biomedcentral.com/articles/10.1186/s12943-021-01469-6#Abs1 本研究中使用到的lncRNA动物用ASO产品、miRNA mimic/inhibitor及其NC、FISH探针&试剂盒产品由锐博生物提供!
参考文献：[1]. Janek Szychowski, et al. Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 2022 Aug 11;65(15):10251-10284. [2]. David Gallo, et al. CCNE1 amplification is synthetic lethal with PKMYT1 kinase inhibition. Nature. 2022 Apr;604(...
The aim of the current study was to evaluate the impact of RP-6306, a novel and selective PKMYT1 inhibitor, on the CCNE1 amplified human breast cancer cell line, HCC1569. RP-6306 is a highly potent PKMYT1 inhibitor that displays single digit nM potency in an in vitro enzyme assay. ...
ACR-2316, a novel, selective dual WEE1 and PKMYT1 inhibitor development candidate, designed using AP3 to achieve superior single agent activity, demonstrates potent preclinical activity across studies ACR-2316 是一种新型的选择性双重 WEE1 和 PKMYT1 抑制剂开发候选药物,使用 AP3 设计,可实现卓越的...
RP-6306((S)-RP-6306)是一种有效的、选择性的、具有口服活性的PKMYT1抑制剂,IC50为14 nM。RP-6306在细胞结合测定中表现出比其他激酶更高的选择性。RP-6306具有抗癌活性。 MCE的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务 ...
Notably, PKHD-5 has been identified as a potent inhibitor that selectively targets both PKMYT1 and HDAC2 with nanomolar affinity. Molecular dynamics have confirmed the strong binding stability of PKHD-5 with PKMYT1 and HDAC2. Importantly, it displayed a notably lower ...
Background: Lunresertib (RP-6306) is a first-in-class membrane-associated tyrosine- and threonine-specific Cdc2-inhibitory kinase (PKMYT1) inhibitor that disrupts the G2/M checkpoint leading to premature mitosis and catastrophic DNA damage in cells harboring synthetic lethal genomic alterations. ...
将处于对数生长期的A549细胞(细胞密度为1×106/mL)接种至6孔板上,按照LipofectamineTM2000说明书将inhibitor NC、miR-93-5p inhibitor、pcDNA和pc-PKMYT1质粒分别转染至A549细胞中,定义为inhibitor NC组、miR-93-5p inhibitor组、pc...