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

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.

For research use only. We do not sell to patients.

NUAK1-IN-3

NUAK1-IN-3 Chemical Structure

CAS No. : 3097515-05-1

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NUAK1-IN-3 Related Antibodies

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JAK1 JAK2 JAK3 Tyk2 JAK

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Description

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)

In Vitro

NUAK1-IN-3 (Compound 10i) potently inhibits NUAK1 with an IC50 of 0.49 nM, and exhibits 459-fold and 541-fold selectivity over JAK3 (IC50 = 225 nM) and NUAK2 (IC50 = 265 nM) , respectively[1].
NUAK1-IN-3 (0-50 μM; 96 h) inhibits proliferation of BT549 and MDA-MB-231 triple-negative breast cancer cells with IC50 values of 2.8 μM and 3.4 μM, respectively[1].
NUAK1-IN-3 (1000-10000 nM; 16 h) dose-dependently attenuates MYPT1 phosphorylation in BT549 and MDA-MB-231 triple-negative breast cancer cells[1].
NUAK1-IN-3 (1-5 μM; 24 h) dose-dependently inhibits migration of BT549 and MDA-MB-231 triple-negative breast cancer cells[1].
NUAK1-IN-3 (3-10 μM; 24 h) dose-dependently inhibits invasion of BT549 and MDA-MB-231 triple-negative breast cancer cells, with 10 μM showing efficacy comparable to siRNA-mediated NUAK1 knockdown[1].
NUAK1-IN-3 (1-10 μM; 24 h) dose-dependently inhibits the EMT pathway in BT549 and MDA-MB-231 triple-negative breast cancer cells by downregulating N-cadherin and Snail expression in the presence of TGF-β1[1].

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

NUAK1-IN-3 Related Antibodies

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.
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 %
In Vivo

NUAK1-IN-3 (Compound 10i) (60-100 mg/kg; i.p.; daily; 16 days) dose-dependently inhibits MDA-MB-231 triple-negative breast cancer xenograft growth in NCG mice[1].

MedChemExpress (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.
Molecular Weight

644.09

Formula

C30H35ClFN7O6
CAS No.
SMILES

[H][C@@]12[C@@H](CO[C@@]1([C@@H](CO2)OC3=NC(NC4=CC=C(C(NC(C5=CN(N=C5)C)=O)=C4)OC[C@@]67CCCN6C[C@@H](C7)F)=NC=C3Cl)[H])OC
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Purity & Documentation
References
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NUAK1-IN-3 Related Classifications

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    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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