NUAK1-IN-3

SKU: orb3211397

Description

NUAK1-IN-3 is a potent and selective inhibitor of NUAK1, with an IC50 of 0.49 nM. It also inhibits NUAK2 and JAK3, exhibiting IC50 values of 265 nM and 225 nM respectively. The compound interacts with NUAK1 at Glu139, forming a salt bridge with its bicyclic nitrogen atom and Asp142, and enhances hydrophobic interactions through a fluorine atom. NUAK1-IN-3 reduces the phosphorylation of MYPT1, thereby inhibiting the NUAK1-MYPT1 signaling axis while suppressing the proliferation, migration, and invasion of triple-negative breast cancer cells. It can reverse TGF-β1-induced epithelial-mesenchymal transition (EMT) marker changes, downregulating Snail and N-cadherin expression, while upregulating E-cadherin expression in tumor tissues. Additionally, NUAK1-IN-3 inhibits tumor growth in triple-negative breast cancer xenograft models, making it a useful tool for research related to this cancer.

Key Properties

• CAS Number: 3097515-05-1
• MW: 644.09
• Formula: C₃₀H₃₅ClFN₇O₆
• SMILES: C(OC1=C(NC(=O)C2=CN(C)N=C2)C=C(NC=3N=C(O[C@H]4[C@@]5([C@](OC4)([C@H](OC)CO5)[H])[H])C(Cl)=CN3)C=C1)[C@@]67N(C[C@H](F)C6)CCC7
• Target: Cadherin,JAK,AMPK

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Cadherin,JAK,AMPK