2. Metabolic Enzyme/Protease
  3. SGK
  4. SGK1-IN-8

SGK1-IN-8 (compound 55) 是一种 SGK1 和 GSK3β 抑制剂，对人源 SGK1 的 IC50 为 0.11 μM，对人源 GSK3β 的 IC50 为 3.39 μM。SGK1-IN-8 可抑制 SGK1 和 GSK3β 的催化活性，降低 TAU 蛋白在 Ser214 位点的磷酸化水平。SGK1-IN-8 可用于阿尔茨海默病的研究。

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SGK1-IN-8

SGK1-IN-8 Chemical Structure

CAS No. : 3109982-48-8

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SGK1-IN-8 相关抗体

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查看 SGK 亚型特异性产品:

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SGK1 SGK3 SGK2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SGK1-IN-8 (compound 55) is a SGK1 and GSK3β inhibitor, with an IC50 of 0.11 μM against human SGK1 and an IC50 of 3.39 μM against human GSK3β. SGK1-IN-8 inhibits the catalytic activities of SGK1 and GSK3β, and reduces the phosphorylation level of TAU protein at the Ser214 site. SGK1-IN-8 is available for the research of Alzheimer's disease[1].

体外研究
(In Vitro)

SGK1-IN-8 (不同浓度；1 h) 可强效抑制人重组 SGK1，其 IC50 为 0.11 μM[1]。
SGK1-IN-8 (1 μM; 1 h pre-incubation, 24 h total with OA) 对 SH-SY5Y 细胞无毒性，且对冈田酸诱导的毒性具有统计学意义的神经保护作用[1]。
SGK1-IN-8 (1 μM) 不改变总 TAU 水平，但可显著降低 SH-SY5Y 细胞中 Ser396 和 Ser214 位点的 TAU 磷酸化水平[1]。
SGK1-IN-8 (10 μM; 120 min) 是一种 P-糖蛋白底物，在转染 MDR1 的 MDCKII 细胞中其外排率为 2.90，且该外排作用可被 P-gp 抑制剂 Zosuquidar (HY-15255) 逆转[1]。
SGK1-IN-8 (不同浓度；30 min) 可微弱抑制人重组 GSK3β，其 IC50 为 3.39 μM[1]。

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

SGK1-IN-8 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y human neuroblastoma cells (okadaic acid-induced AD model)
Concentration: 1 μM (compound 55)
Incubation Time: 1 h pre-incubation; 24 h total incubation with OA
Result: Showed no significant reduction in cell viability at 1 μM, and statistically significantly restored cell viability in OA-treated SH-SY5Y cells, indicating neuroprotective activity.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax (Plasma) Cmax AUC0-∞ T1/2 Tmax (Brain)
Mice[1] 5 mg/kg i.p. 0.25 h 568.84 ng/mL 591.58 / 0.25 h
Mice[1] 10 mg/kg p.o. 0.25 h 777.40 ng/mL 599.08 0.33 h /
体内研究
(In Vivo)

SGK1-IN-8 (compound 55)(5-10 mg/kg；腹腔注射、口服；单次给药) 在雄性 BALB/c 小鼠中单次腹腔注射或口服给药后表现出快速吸收，但其脑穿透性较低，两种给药途径对应的脑- Kp (AUClast) 均为 0.04[1]。

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

336.78

Formula

C18H13ClN4O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SGK1-IN-8 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

SGK1-IN-83109982-48-8SGKSerum-glucocorticoid regulated kinaseSerum and glucocorticoid-regulated kinaseSH-SY5Y cellsalzheimer's diseasezosuquidarGSK3βSGK1TAU proteinP-glycoproteinMDR1-transfected MDCKII cellsokadaic acidBALB/c miceInhibitorinhibitorinhibit

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产品名称：
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目录号：
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