Chemical Structure : HPV E7-ZER1 inhibitor Compound 4
CAS No.:
3108114-67-3
HPV E7-ZER1 inhibitor Compound 4
货号: PC-27386Not For Human Use, Lab Use Only.
HPV E7-ZER1 inhibitor Compound 4 (ZER1-IN-1) is a first-in-class small-molecule inhibitor of ZER1 ARM-repeat domain, selectively blocks the ZER1-E7 interaction, leading to retinoblastoma (Rb) stabilization, inhibition of HPV-positive cervical cancer cell proliferation.
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
HPV E7-ZER1 inhibitor Compound 4 (ZER1-IN-1) is a first-in-class small-molecule inhibitor of ZER1 ARM-repeat domain, selectively blocks the ZER1-E7 interaction, leading to retinoblastoma (Rb) stabilization, inhibition of HPV-positive cervical cancer cell proliferation.
Compound 4 inhibitsHeLa cell growth with an IC50 of 23.05 μM, but with no sensitivity in ZER1 knockout HeLa cells, has minimal effects on the proliferation of HPV-negative C33A cells.
Compound 4 treatment effectively inhibited cell growth of the HPV18-positive SUNE2 cell line but not the HPV-negative SCC-9 cells.
Compound 4 significantly reduced tumor volume and weight in mice bearing subcutaneous xenografts of either HPV18-positive HeLa.
HPV E7 is the recruitment of the CRL2ZER1 ubiquitin ligase complex to target Rb for proteasomal degradation.
ZER1 functions as the substrate receptor within the Cullin-2-RING E3 ligase (CRL2), and this E7-ZER1-dependent inactivation of Rb is essential for HPV-driven transformation.
物理化学性质&存储条件
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分子量
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288.31
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分子式
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C14H16N4O3
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外观性状
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Solid
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CAS No.
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储存条件
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- 固体粉末
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-20°C 12 个月; 4°C 6 个月
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- 配置液
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-80°C 6 个月; -20°C 6 个月
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-2-amino-3-hydroxy-N-(2-oxo-1-(pyridin-2-ylmethyl)-1,2-dihydropyridin-3-yl)propanamide
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参考文献
1. Wang X, et al. Cell Rep. 2026 Jul 28;45(8):117740.
