2. Epigenetics PI3K/Akt/mTOR JAK/STAT Signaling Stem Cell/Wnt Protein Tyrosine Kinase/RTK Cytoskeleton
  3. AMPK JAK Cadherin
  4. NUAK1-IN-3

NUAK1-IN-3 是一种强效且选择性的 NUAK1 抑制剂，其 IC50 为 0.49 nM。NUAK1-IN-3 还可抑制 NUAK2 和 JAK3，对应的 IC50 值分别为 265 nM 和 225 nM。NUAK1-IN-3 可结合 NUAK1 的 Glu139，其双环环氮原子与 Asp142 形成盐桥，并通过氟原子增强疏水结合相互作用。NUAK1-IN-3 可减弱 MYPT1 的磷酸化，抑制 NUAK1-MYPT1 信号轴，同时抑制三阴性乳腺癌细胞的增殖、迁移与侵袭。NUAK1-IN-3 可逆转 TGF-β1 诱导的上皮-间质转化 (EMT) 标志物改变，在肿瘤组织中下调 Snail 和 N-钙黏蛋白 (N-cadherin) 的表达，上调 E-钙黏蛋白 (E-cadherin) 的表达。NUAK1-IN-3 可抑制三阴性乳腺癌异种移植模型中的肿瘤生长。NUAK1-IN-3 可用于三阴性乳腺癌的相关研究。

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NUAK1-IN-3

NUAK1-IN-3 Chemical Structure

CAS No. : 3097515-05-1

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NUAK1-IN-3 相关抗体

Top Publications Citing Use of Products

查看 AMPK 亚型特异性产品:

查看所有亚型
NUAK1 NUAK2 AMPK AMPK α1β1γ1 AMPK α2β1γ1 AMPK α1β2γ1 AMPK α2β2γ1 BRSK1 BRSK2 HUNK AMPKα

查看 JAK 亚型特异性产品:

查看所有亚型
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NUAK1-IN-3 is a potent and selective NUAK1 inhibitor with an IC50 of 0.49 nM. NUAK1-IN-3 also inhibits NUAK2 and JAK3 with IC50 values of 265 and 225 nM. NUAK1-IN-3 engages Glu139 of NUAK1, forms a salt bridge between its bicyclic ring nitrogen and Asp142, and uses a fluorine atom to enhance hydrophobic binding interactions. NUAK1-IN-3 attenuates MYPT1 phosphorylation, suppresses the NUAK1-MYPT1 signaling axis, and inhibits proliferation, migration, and invasion of triple-negative breast cancer cells. NUAK1-IN-3 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) marker alterations, downregulates Snail and N-cadherin, and upregulates E-cadherin in tumor tissues. NUAK1-IN-3 suppresses tumor growth in triple-negative breast cancer xenograft models. NUAK1-IN-3 can be used for the research of triple-negative breast cancer[1].

IC50 & Target[1]

NUAK1

0.49 nM (IC50)

JAK3

225 nM (IC50)

NUAK2

265 nM (IC50)

体外研究
(In Vitro)

NUAK1-IN-3 (Compound 10i) 可强效抑制 NUAK1，其 IC50 为 0.49 nM；对 JAK3 (IC50 = 225 nM) 和 NUAK2 (IC50 = 265 nM) 的选择性分别达到 459 倍和 541 倍[1]。
NUAK1-IN-3 (0-50 μM; 96 h) 可抑制三阴性乳腺癌细胞 BT549 和 MDA-MB-231 的增殖，其 IC50 值分别为 2.8 μM 和 3.4 μM[1]。
NUAK1-IN-3 (1000-10000 nM; 16 h) 可浓度依赖性地抑制 BT549 和 MDA-MB-231 三阴性乳腺癌细胞中 MYPT1 的磷酸化[1]。
NUAK1-IN-3 (1-5 μM; 24 h) 呈剂量依赖性抑制 BT549 和 MDA-MB-231 三阴性乳腺癌细胞的迁移[1]。
NUAK1-IN-3 (3-10 μM; 24 h) 可剂量依赖性地抑制 BT549 和 MDA-MB-231 三阴性乳腺癌细胞的侵袭，其中 10 μM 浓度下的效力与 siRNA 介导的 NUAK1 敲低相当[1]。
NUAK1-IN-3 (1-10 μM; 24 h) 可在 TGF-β1 存在的情况下，通过下调 N-cadherin 和 Snail 的表达，以剂量依赖的方式抑制 BT549 和 MDA-MB-231 三阴性乳腺癌细胞中的 EMT 通路[1]。

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

NUAK1-IN-3 相关抗体:

Western Blot Analysis[1]

Cell Line: human triple-negative breast cancer BT549 cells, human triple-negative breast cancer MDA-MB-231 cells
Concentration: 1000, 3000, 5000, 10000 nM
Incubation Time: 16 h
Result: Dose-dependently reduced phosphorylation of MYPT1 (Ser668) in both BT549 and MDA-MB-231 cells.
Confirmed direct NUAK1 target engagement and inhibition of the NUAK1-MYPT1 signaling axis.

Western Blot Analysis[1]

Cell Line: human triple-negative breast cancer BT549 cells, human triple-negative breast cancer MDA-MB-231 cells
Concentration: 1, 5, 10 μM (in the presence of 20 ng/mL TGF-β1)
Incubation Time: 24 h
Result: Dose-dependently downregulated the expression of EMT markers N-cadherin and Snail in both BT549 and MDA-MB-231 cells.
Reversed TGF-β1-induced EMT alterations.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-∞ CL Vss F
Mice[1] 2 mg/kg i.v. 0.85 h 0.03 h 581 ng/mL 204 ng·h/mL 206 ng·h/mL 0.64 h 161 mL/min/kg 6.20 L/kg /
Mice[1] 6 mg/kg p.o. 1.69 h 0.08 h 45.6 ng/mL 96.6 ng·h/mL 103 ng·h/mL 2.37 h / / 16.6 %
Mice[1] 60 mg/kg p.o. 1.21 h 0.194 h 809 ng/mL 768 ng·h/mL 783 ng·h/mL 1.52 h / / 12.6 %
Mice[1] 60 mg/kg i.p. 0.773 h 0.194 h 7177 ng/mL 5947 ng·h/mL 5950 ng·h/mL 0.620 h / / 95.9 %
体内研究
(In Vivo)

NUAK1-IN-3 (Compound 10i) (60-100 mg/kg；腹腔注射；每日一次；连续 16 天) 可剂量依赖性地抑制 NCG 小鼠体内 MDA-MB-231 三阴性乳腺癌异种移植物的生长[1]。

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

Animal Model: NCG mice (female, 4 weeks old, triple-negative breast cancer subcutaneous xenograft model)[1]
Dosage: 60 mg/kg; 100 mg/kg
Administration: i.p.; daily; 16 days
Result: Achieved 70.93% tumor growth inhibition (TGI) at 60 mg/kg.
Achieved 83.55% TGI at 100 mg/kg.
Significantly reduced tumor volumes and weights relative to vehicle control at both doses.
Increased E-cadherin expression in tumor sections relative to vehicle control.
Reduced N-cadherin expression in tumor sections relative to vehicle control.
Caused no overt toxicity, significant body weight loss, or histopathological abnormalities in heart, liver, spleen, or kidneys.
分子量

644.09

Formula

C30H35ClFN7O6
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

NUAK1-IN-3 相关分类

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  • 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.

Keywords:

NUAK1-IN-33097515-05-1AMPKJAKCadherinAMP-activated protein kinaseJanus kinaseJAK3TGF-β1triple-negative breast cancer cellsNUAK2CD-1 miceNUAK1MYPT1MDA-MB-231epithelial-mesenchymal transitionBT549Inhibitorinhibitorinhibit

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