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首页-小分子抑制剂&激动剂-NF-κB Pathway-IκB kinase (IKK)-Shikonin
Shikonin

Chemical Structure : Shikonin

CAS No.: 517-89-5

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Shikonin (Isoarnebin 4)

货号: PC-21476Not For Human Use, Lab Use Only.

Shikonin is a specific inhibitor of the IKKβ/NEMO complex PPI with IC50 of 170 nM, also a potent TMEM16A chloride channel inhibitor (IC50=6.5 uM) and specific pyruvate kinase M2 (PKM2) inhibitor.

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50 mg ￥1280 In stock
100 mg ￥2180 In stock
250 mg ￥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Shikonin is a specific inhibitor of the IKKβ/NEMO complex PPI with IC50 of 170 nM, also a potent TMEM16A chloride channel inhibitor (IC50=6.5 uM) and specific pyruvate kinase M2 (PKM2) inhibitor.
Shikonin possesses various physiological and pharmacological properties, including anti-inflammatory, wound healing, and anti-cancer effects.
Shikonin suppresses the malignant phenotypes of colorectal cancer cells in vitro and in vivo, decreases the protein levels Cyclin E1/D1, CDK4 and MMP2/9, while increasing the levels of cleaved caspases 3 and 9, cleaved PARP, and TIMP.
Shikonin shows no effects on the upstream regulators of IKKβ/NEMO complex.
Shikonin effectively impairs NEMO/IKKβ interaction with IC50 of 231.03 nM in fluorescence resonance energy transfer (FRET) assays.
Shikonin is a natural product and is a bioactive constituent of Lithospermum erythrorhizon, which has a long history of more than 2000 years of use as a Chinese medicinal herb known as zicao.

物理化学性质&存储条件

分子量 288.3
分子式 C16H16O5
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)-5,8-Dihydroxy-2-(1-hydroxy-4-methylpent-3-en-1-yl)naphthalene-1,4-dione

参考文献

1. Zhenlong Yu, et al. Signal Transduction and Targeted Therapy volume 7, Article number: 71 (2022)

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