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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-PIKfyve-Apilimod
Apilimod

Chemical Structure : Apilimod

CAS No.: 541550-19-0

Apilimod (STA-5326, STA5326)

货号: PC-60412Not For Human Use, Lab Use Only.

Apilimod (STA5326) is a potent IL-12/IL-23 inhibitor that down-regulates both IL-12 p35 and IL-12/IL-23 p40 at the transcriptional level, and inhibits the production of both IL-12 and IL-23 cytokines (IC50=2 nM), inhibits PIKfyve phosphotransferase activity (IC50=14 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Apilimod (STA5326) is a potent IL-12/IL-23 inhibitor that down-regulates both IL-12 p35 and IL-12/IL-23 p40 at the transcriptional level, and inhibits the production of both IL-12 and IL-23 cytokines (IC50=2 nM), inhibits PIKfyve phosphotransferase activity (IC50=14 nM).
Apilimod (STA5326) suppresses Th1 but not Th2 immune response in mice.
Apilimod (STA5326) binds to PIKfyve and blocks its phosphotransferase activity (IC50=14 nM), has no activity on PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms.
Apilimod (STA5326) also potently blocks infections by EBOV and MARV in Huh 7, Vero E6 and primary human macrophage cells with IC50 of 10 nM.

物理化学性质&存储条件

分子量 418.49
分子式 C23H26N6O2
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

Benzaldehyde, 3-methyl-, [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone (9CI)

参考文献

1. Wada Y, et al. Blood. 2007 Feb 1;109(3):1156-64.

2. Cai X, et al. Chem Biol. 2013 Jul 25;20(7):912-21.

3. Nelson EA, et al. PLoS Negl Trop Dis. 2017 Apr 12;11(4):e0005540.

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