Date published: 2025-10-21

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Mnk1 Inhibitors

The class of Mnk1 inhibitors comprises a diverse repertoire of small molecules that intricately modulate the activity of Mnk1, a kinase involved in the regulation of translation initiation. One notable member of this class is CGP57380, a direct inhibitor that targets the ATP-binding site in the kinase domain of Mnk1. Through its binding, CGP57380 disrupts ATP binding, thereby inhibiting the catalytic activity of Mnk1. This direct interference highlights the potential of small molecules to specifically and selectively inhibit Mnk1, offering a precise strategy to modulate cellular processes governed by Mnk1. Another representative, Eukaryotic elongation factor 2 kinase (eEF2K) Inhibitor, exemplifies an indirect approach to inhibit Mnk1. By targeting eEF2K, this compound indirectly suppresses Mnk1 activity. eEF2K negatively regulates Mnk1 by promoting the dephosphorylation of eukaryotic initiation factor 4E (eIF4E), a downstream substrate of Mnk1. This intricate interplay showcases the regulatory network between kinases and how inhibiting an upstream regulator can impact Mnk1 function indirectly. The class also includes compounds like LY2584702, A-443654, PF-4708671, and others, all acting as direct inhibitors of Mnk1 by targeting its ATP-binding site. This targeted approach emphasizes the potential of small molecules to interfere specifically with Mnk1 function, underscoring the importance of understanding the structural and catalytic aspects of the kinase for effective inhibition. Additionally, compounds such as Halofuginone showcase the diversity of mechanisms employed for Mnk1 inhibition. Halofuginone indirectly inhibits Mnk1 by inducing endoplasmic reticulum (ER) stress and activating the unfolded protein response (UPR) pathway. This indirect modulation reveals the intricate connection between cellular stress responses and the regulation of Mnk1 function. This diversity in mechanisms highlights the potential for developing a range of Mnk1 inhibitors with varied modes of action. In conclusion, the chemical class of Mnk1 inhibitors offers a nuanced understanding of how small molecules can modulate Mnk1 activity, providing a toolkit for targeted interventions in cellular processes regulated by Mnk1.
Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

CGP 57380

522629-08-9sc-202993
5 mg
$172.00
6
(1)

CGP 57380 acts as a selective inhibitor of Mnk1, showcasing unique binding dynamics that alter the enzyme's phosphorylation activity. Its interaction with the Mnk1 active site induces specific conformational shifts, impacting downstream signaling cascades. The compound's kinetic behavior reveals a competitive inhibition pattern, which modulates the translation of stress-responsive proteins. This nuanced regulation highlights its role in fine-tuning cellular responses to environmental stimuli.

Cercosporamide

131436-22-1sc-202095
sc-202095A
500 µg
2.5 mg
$300.00
$1200.00
2
(1)

Cercosporamide functions as a selective modulator of Mnk1, exhibiting distinct molecular interactions that disrupt the enzyme's catalytic efficiency. Its binding affinity leads to unique allosteric changes, influencing the phosphorylation of target substrates. The compound's reaction kinetics suggest a non-competitive inhibition mechanism, which alters the dynamics of protein synthesis pathways. This intricate modulation underscores its potential to affect cellular homeostasis and stress adaptation processes.

Homoharringtonine

26833-87-4sc-202652
sc-202652A
sc-202652B
1 mg
5 mg
10 mg
$51.00
$123.00
$178.00
11
(1)

HHT acts as an indirect inhibitor of Mnk1 by modulating eukaryotic initiation factor 4E (eIF4E) phosphorylation. It inhibits protein synthesis by interfering with the interaction between eIF4E and the mRNA cap, indirectly suppressing Mnk1 activity.

eIF4E/eIF4G Interaction Inhibitor, 4EGI-1

315706-13-9sc-202597
10 mg
$260.00
14
(1)

4EGI-1 serves as an indirect inhibitor of Mnk1 by disrupting the eIF4E-eIF4G interaction, preventing the assembly of the eIF4F complex. By inhibiting the formation of this complex, 4EGI-1 indirectly suppresses Mnk1 activity, as Mnk1 phosphorylates eIF4E, a component of the eIF4F complex.

Ro-32-0432

145333-02-4sc-3549
sc-3549A
1 mg
5 mg
$103.00
$388.00
13
(1)

Ro 32-0432 serves as an indirect inhibitor of Mnk1 by targeting protein kinase C (PKC). Activation of PKC by Ro 32-0432 leads to the inhibition of eIF4E phosphorylation by Mnk1, providing an indirect mechanism to suppress Mnk1 activity.

A-443654

552325-16-3sc-507339
1 mg
$140.00
(0)

A-443654 serves as a direct inhibitor of Mnk1 by targeting its ATP-binding site. By binding to the kinase domain, this compound disrupts ATP binding, leading to the inhibition of Mnk1 catalytic activity.

PF 4708671

1255517-76-0sc-361288
sc-361288A
10 mg
50 mg
$175.00
$700.00
9
(1)

PF-4708671 acts as a direct inhibitor of Mnk1 by targeting its ATP-binding site. Through binding to the kinase domain, this compound disrupts ATP binding, leading to the inhibition of Mnk1 catalytic activity.

Halofuginone

55837-20-2sc-507290
100 mg
$1740.00
(0)

Halofuginone indirectly inhibits Mnk1 by modulating the unfolded protein response (UPR) pathway. By inducing endoplasmic reticulum (ER) stress, halofuginone triggers the PERK-eIF2α-ATF4 pathway, leading to the suppression of Mnk1 activity.