CCT020312 is a potent and selective EIF2AK3 Activator. CCT020312 modulates the biological activity of EIF2AK3. CCT020312 sensitizes cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. CCT020312 is a novel small molecule chemical tool for the selective activation of EIF2A-mediated translation control with utility for proof-of-concept applications in EIF2A-centered therapeutic approaches, and as a chemical starting point for pathway selective agent development. CCT020312 is potent, and EIF2AK3 selective agent and can act as a sensitizer to chemotherapy-associated stresses as elicited by taxanes.
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名称 | CCT020312 |
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Iupac 化学名称 | 6-Bromo-3-[5-(4-bromo-phenyl)-1-(3-diethylamino-propionyl)-4,5-dihydro-1H-pyrazol-3-yl]-4-phenyl-1H-quinolin-2-one |
同义词 | CCT020312; CCT-020312; CCT 020312. |
英文同义词 | CCT020312; CCT-020312; CCT 020312. |
分子式 | C31H30Br2N4O2 |
分子量 | 650.40 |
Smile | O=C1NC2=C(C=C(Br)C=C2)C(C3=CC=CC=C3)=C1C4=NN(C(CCN(CC)CC)=O)C(C5=CC=C(Br)C=C5)C4 |
InChiKey | OAXDKXMGESZLKV-UHFFFAOYSA-N |
InChi | InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39) |
Cas号 | 324759-76-4 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
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Blagg J, Workman P, Garrett MD, Mittnacht S. Mechanism-based screen for G1/S
checkpoint activators identifies a selective activator of EIF2AK3/PERK
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T, Winklhofer KF, Müller U, Höglinger GU. PERK activation mitigates tau pathology
in vitro and in vivo. EMBO Mol Med. 2017 Feb 1. pii: e201606664. doi:
10.15252/emmm.201606664. [Epub ahead of print] PubMed PMID: 28148553.