1. PI3K/Akt/mTOR NF-κB
  2. NF-κB PIKfyve IKK
  3. DC-SX029

DC-SX029 是一种口服有效的 SNX10 蛋白质-蛋白质相互作用 (PPI) 抑制剂,通过表面等离子共振 (SPR) 实验获得 KD 约为 0.935 μM。DC-SX029 阻断 SNX10-PIKfyve 相互作用,从而减少 TBK1/c-Rel 信号传导激活。DC-SX029 不影响SNX10的蛋白水平。DC-SX029 具有用于炎症性肠病 (IBD) 研究的潜力。

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DC-SX029 Chemical Structure

DC-SX029 Chemical Structure

CAS No. : 300713-88-6

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  • 生物活性

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生物活性

DC-SX029 is a potent SNX10 protein-protein interaction (PPI) inhibitor with oral activity with an estimated KD constant of ~0.935 μM by surface plasmon resonance (SPR). DC-SX029 blocks the SNX10-PIKfyve interaction, thereby decreased the TBK1/c-Rel signaling activation. DC-SX029 does not affect the protein level of SNX10. DC-SX029 has the potential for inflammatory bowel disease (IBD) research[1][2].

体外研究
(In Vitro)

DC-SX029 (50 μM,6 h) 在 BMDMs 中抑制 PIKfyve 介导的 TBK1/c-Rel 信号激活,降低炎症反应[1]
DC-SX029 (10-50 μM,2 h) 显著降低了 LPS (HY-D1056) 诱导的 c-Rel 的核定位和 TBK1 的磷酸化[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: BMDMs
Concentration: 50 μM
Incubation Time: 6 h
Result: Inhibited IL-12/23, IL-1β, IL-6 and TNF-α mRNA.

Western Blot Analysis[1]

Cell Line: BMDMs
Concentration: 10, 50 μM
Incubation Time: 2 h
Result: Reduced phosphorylation of TBK1.
体内研究
(In Vivo)

DC-SX029 (1-6 mg/kg,口服,每日一次,10 天) 可减轻 DSS 诱导的小鼠结肠炎[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mouse colitis model[1]
Dosage: 1, 2, 6 mg/kg; daily; 10 days
Administration: Oral
Result: Restored the body weight of mice, reduced DAI during the recovery period, reduced the shortening of colon length, reduced the production of pro-inflammatory cytokines, and had a significant alleviation effect on erosion, inflammatory cell infiltration and crypt loss.
分子量

398.35

Formula

C14H17F3N2O6S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DC-SX029
目录号:
HY-160477
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