Date published: 2025-12-5

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MEK-1 Inhibitors

MEK-1, also known as MAP2K1 or mitogen-activated protein kinase kinase 1, is a pivotal component within the MAP kinase signaling pathway, which is a fundamental intracellular signaling cascade involved in various cellular processes such as proliferation, differentiation, and apoptosis. MEK-1 functions as a dual-specificity protein kinase, primarily responsible for phosphorylating and activating extracellular signal-regulated kinases 1 and 2 (ERK1/2), which subsequently phosphorylate numerous downstream substrates, thereby orchestrating diverse cellular responses. Specifically, MEK-1 catalyzes the phosphorylation of threonine and tyrosine residues within the activation loop of ERK1/2, thereby inducing their activation and subsequent translocation to the nucleus where they modulate gene expression and cellular behavior. Inhibition of MEK-1 activity serves as a potent strategy for perturbing aberrant MAP kinase signaling implicated in various pathological conditions, particularly cancer. Mechanistically, MEK-1 inhibition typically involves the competitive binding of small molecule inhibitors to the ATP-binding pocket of the enzyme, thereby preventing ATP binding and subsequent phosphorylation of downstream targets. Additionally, allosteric inhibitors may also hinder MEK-1 activity by inducing conformational changes that impair substrate recognition and catalytic activity. Moreover, certain compounds act as MEK-1 inhibitors by disrupting upstream signaling events or scaffolding proteins essential for MEK-1 activation, thereby indirectly suppressing its activity. Overall, elucidating the precise mechanisms of MEK-1 inhibition offers valuable insights into the development of strategies targeting dysregulated MAP kinase signaling in various disease contexts.

Items 1 to 10 of 24 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

PD 98059

167869-21-8sc-3532
sc-3532A
1 mg
5 mg
$39.00
$90.00
212
(2)

PD 98059 functions as a MEK-1 inhibitor, characterized by its ability to selectively disrupt the phosphorylation of ERK1/2. This compound exhibits unique binding dynamics, engaging in hydrophobic interactions with the enzyme's active site, which alters the conformational landscape of MEK-1. Its kinetic behavior reveals a competitive inhibition mechanism, where it effectively competes with ATP, leading to a pronounced decrease in downstream signaling. The compound's structural features also enhance its stability in various environments, making it a subject of interest in biochemical research.

Arctigenin

7770-78-7sc-202957
25 mg
$81.00
14
(1)

Arctigenin acts as a MEK-1 inhibitor, showcasing a distinctive ability to modulate the MAPK signaling pathway. Its interaction with MEK-1 involves specific hydrogen bonding and van der Waals forces, which stabilize the enzyme's inactive conformation. This compound exhibits allosteric inhibition, altering the enzyme's activity without directly competing with ATP. Additionally, its lipophilic nature enhances membrane permeability, influencing cellular uptake and distribution.

U-0126

109511-58-2sc-222395
sc-222395A
1 mg
5 mg
$63.00
$241.00
136
(2)

U-0126 functions as a selective MEK-1 inhibitor, characterized by its unique ability to disrupt the phosphorylation cascade within the MAPK pathway. It engages in specific hydrophobic interactions with the enzyme, effectively altering its conformation and inhibiting downstream signaling. The compound's kinetic profile reveals a rapid onset of action, while its structural features promote strong binding affinity, ensuring prolonged inhibition. Its distinct physicochemical properties facilitate effective cellular localization and interaction dynamics.

Selumetinib

606143-52-6sc-364613
sc-364613A
sc-364613B
sc-364613C
sc-364613D
5 mg
10 mg
100 mg
500 mg
1 g
$28.00
$80.00
$412.00
$1860.00
$2962.00
5
(1)

Selumetinib acts as a selective inhibitor of MEK-1, showcasing a unique mechanism of action through its ability to interfere with the RAS-RAF-MEK-ERK signaling axis. It exhibits a high degree of specificity, engaging in critical electrostatic interactions that stabilize the inactive conformation of MEK-1. The compound's unique structural attributes enhance its solubility and permeability, allowing for efficient cellular uptake and modulation of intracellular signaling pathways.

Trametinib

871700-17-3sc-364639
sc-364639A
sc-364639B
5 mg
10 mg
1 g
$112.00
$163.00
$928.00
19
(1)

Trametinib is a selective MEK-1 inhibitor that disrupts the RAS-RAF-MEK-ERK signaling cascade. Its unique binding affinity is characterized by specific hydrophobic interactions and hydrogen bonding, which stabilize the inactive form of MEK-1. This compound demonstrates distinct kinetic properties, exhibiting a slow dissociation rate from its target, which prolongs its inhibitory effect. Additionally, Trametinib's molecular structure contributes to its favorable pharmacokinetic profile, enhancing its interaction with cellular membranes.

Myricetin

529-44-2sc-203147
sc-203147A
sc-203147B
sc-203147C
sc-203147D
25 mg
100 mg
1 g
25 g
100 g
$95.00
$184.00
$255.00
$500.00
$1002.00
3
(1)

Myricetin acts as a MEK-1 modulator, influencing the RAS-RAF-MEK-ERK pathway through unique molecular interactions. Its structure allows for specific π-π stacking and hydrogen bonding with MEK-1, promoting conformational changes that inhibit its activity. The compound exhibits notable reaction kinetics, with a rapid association rate leading to effective modulation of downstream signaling. Myricetin's distinct physical properties, including its solubility profile, further enhance its interaction dynamics within cellular environments.

10Z-Hymenialdisine

82005-12-7sc-360987
500 µg
$210.00
(1)

10Z-Hymenialdisine functions as a MEK-1 inhibitor by engaging in selective binding interactions that disrupt the RAS-RAF-MEK-ERK signaling cascade. Its unique structural features facilitate strong van der Waals forces and hydrophobic interactions with MEK-1, leading to altered enzyme conformation and reduced catalytic activity. The compound's stability and reactivity profile contribute to its effective modulation of cellular signaling pathways, showcasing its distinct role in biochemical processes.

BAY 869766

923032-37-5sc-364427
sc-364427A
5 mg
10 mg
$240.00
$420.00
1
(1)

BAY 869766 acts as a MEK-1 inhibitor through its ability to form specific hydrogen bonds and electrostatic interactions with the enzyme's active site. This compound exhibits a unique conformational flexibility that allows it to adapt to the binding pocket of MEK-1, enhancing its inhibitory potency. Additionally, its kinetic properties reveal a slow dissociation rate from the target, ensuring prolonged engagement and sustained modulation of downstream signaling pathways.

Cobimetinib

934660-93-2sc-507421
5 mg
$270.00
(0)

MEK-1 inhibitor that hinders the MAPK pathway by selectively targeting MEK-1, disrupting the phosphorylation cascade crucial for proper cellular responses.

Debromohymenialdisine

75593-17-8sc-202127
100 µg
$100.00
2
(1)

Debromohymenialdisine functions as a MEK-1 inhibitor by engaging in selective hydrophobic interactions and π-π stacking with key residues in the enzyme's active site. Its unique structural features facilitate a stable binding conformation, which enhances its affinity for MEK-1. The compound also demonstrates distinct reaction kinetics, characterized by a moderate rate of inhibition that allows for effective modulation of cellular signaling cascades over time.