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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Keap1-Nrf2-VVD-065
VVD-065

Chemical Structure : VVD-065

CAS No.: 3034876-85-9

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VVD-065 (VVD065)

货号: PC-25485Not For Human Use, Lab Use Only.

VVD-065 is a first-in-class, allosteric molecular glue of Keap1-Cul3 E3-ligase complex and NRF2 inhibitor, specifically and covalently engages C151 on KEAP1 with engagement potency (TE50) of 9 nM in KYSE70 cells, promotes KEAP1-CUL3 complex formation, leading to enhancement of NRF2 degradation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

VVD-065 is a first-in-class, allosteric molecular glue of Keap1-Cul3 E3-ligase complex and NRF2 inhibitor, specifically and covalently engages C151 on KEAP1 with engagement potency (TE50) of 9 nM in KYSE70 cells, promotes KEAP1-CUL3 complex formation, leading to enhancement of NRF2 degradation.
VVD-065 covalently binds C151 of KEAP1, may increase KEAP1 activity by stabilizing a KEAP1 conformation that favors CUL3 binding.
VVD-065 induces robust degradation of NRF2 and decreases expression of NRF2 target genes.
VVD-065 (5-25 mg/kg) exhibits cancer cell growth inhibitory effects. VVD-065 exhibits anti-tumorigenic effects in KYSE70 tumor bearing animals
VVD-065 exhibits strong antitumor effects in syngeneic with cisplatin and nab-paclitaxel in various solid tumor types such as NSCLC, ESCC, HNSCC, and uterine cancers.

物理化学性质&存储条件

分子量 345.79
分子式 C16H16ClN5O2
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

(R)-1-(3-(3-(4-amino-1,3,5-triazin-2-yl)-5-chlorophenyl)morpholino)prop-2-en-1-one

参考文献

1. Nilotpal Roy, et al. Suppression of NRF2-dependent cancer growth by a covalent allosteric molecular glue. bioRxiv, 2024, preprint, 10.1101/2024.10.04.616592.

2. Nil Roy, et al. Mol Cancer Ther (2023) 22 (12_Supplement): PR011.

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