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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-CDYL inhibitor Compound D03
CDYL inhibitor Compound D03

Chemical Structure : CDYL inhibitor Compound D03

CAS No.: 2378625-66-0

CDYL inhibitor Compound D03 (D03)

货号: PC-22846Not For Human Use, Lab Use Only.

Compound D03 is a potent and selective small-molecule inhibitor of histone methyllysine reader protein chromodomain Y-like (CDYL) with SPR KD of 0.5 uM, disrupts the recruitment of CDYL onto chromatin.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Compound D03 is a potent and selective small-molecule inhibitor of histone methyllysine reader protein chromodomain Y-like (CDYL) with SPR KD of 0.5 uM, disrupts the recruitment of CDYL onto chromatin.
Compound D03 shows excellent selectivity among other chromodomain proteins, including CDYL2 (>140 folds), CDY1 (no observed binding) and CBX7 (>32 folds).
Compound D03 engages with endogenous CDYL, and perturbs the recruitment of CDYL onto chromatin, subsequently resulting in transcriptional derepression of its target genes.
Compound D03 promotes dendritic maturation in primary cultured neurons, consistent with the known ability of CDYL overexpression to restrict dendritic arborization.
Compound D03 (2.5 mg·kg-1·d-1, i.p.) effectively attenuated the kidney dysfunction, pathological damages and tubular pyroptosis without side effects on liver or kidney function and other tissue injuries in cisplatin-induced acute kidney injury mice.

物理化学性质&存储条件

分子量 329.40
分子式 C18H23N3O3
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

3-(2-oxo-2-(4-(pyrrolidin-1-yl)piperidin-1-yl)ethyl)benzo[d]oxazol-2(3H)-one

参考文献

1. Xiang T, et al. Acta Pharmacol Sin. 2024 Jul 23. doi: 10.1038/s41401-024-01345-1.

2. Yang L, et al. Eur J Med Chem. 2019 Nov 15;182:111656.

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