Chemical Structure : PLAGL2 inhibitor Compound C8
CAS No.:
3099026-16-8
PLAGL2 inhibitor Compound C8
货号: PC-26151Not For Human Use, Lab Use Only.
PLAGL2 inhibitor Compound C8 is a small-molecule inhibitor targeting PLAGL2 (Pleiomorphic adenoma-like protein 2) with SPR KD of 2.23 uM, inhibits PLAGL2 transcriptional activity and HCC cell viability (MHCC-97H, IC50=3.69 uM).
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纯度 & COA & 质检文件 纯度:
>98% (HPLC)
生物&药学活性
PLAGL2 inhibitor Compound C8 is a small-molecule inhibitor targeting PLAGL2 (Pleiomorphic adenoma-like protein 2) with SPR KD of 2.23 uM, inhibits PLAGL2 transcriptional activity and HCC cell viability (MHCC-97H, IC50=3.69 uM).
Compound C8 shows potent cell viability inhibition against PLAGL2 high-expressed cells ( lung cancer (IC50=0.96-1.35 μM) and breast cancer (IC50=1.64 -2.21 uM)).
Compound C8 remarkably inhibits colony formation of HCC cells (MHCC-97H, IC50=0.02 uM), reduces division of HCC cells, inhibits migration and invasion ability of HCC cells.
Compound C8 interferes with the extracellular matrix organization pathway in HCC.
Compound C8 significantly inhibits PLAGL2-dependent AKT phosphorylation at both Thr308 and Ser473, indicating its ability to suppress both the EGFR-PI3K-PDK1 and EGFR-PI3K-mTORC2 axes to exert anti-tumor effects.
Compound C8 (15 mg/kg/day, i.p.) effectively inhibited tumor growth in HCCLM3-derived subcutaneous xenograft tumor models.
物理化学性质&存储条件
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分子量
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632.60
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分子式
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C30H35Cl2N5O4S
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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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N-(5-(4-(2,2-dichloroacetyl)piperazine-1-carbonyl)-2-(4-isopropylpiperazin-1-yl)phenyl)naphthalene-2-sulfonamide
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参考文献
1. Yushi Ding, et al. Eur J Med Chem. 2026 Feb 5:303:118471.
