Date published: 2026-1-22

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ENT1 Inhibitors

ENT1 inhibitors belong to a chemical class of compounds designed to selectively modulate Equilibrative Nucleoside Transporter 1 (ENT1) activity. ENT1 is a membrane-associated protein found in various cell types, including neurons and vascular cells, and it plays a pivotal role in mediating the transmembrane transport of nucleosides like adenosine and uridine. These nucleosides are fundamental for essential cellular processes, including DNA and RNA synthesis, and also serve as key signaling molecules within the nervous system. The core mechanism of action for ENT1 inhibitors revolves around their ability to obstruct ENT1 function, setting off a cascade of effects that significantly impact cellular activities and intricate signaling pathways. When ENT1 is inhibited by this class of compounds, it triggers a range of physiological consequences. By impeding the reuptake of adenosine, ENT1 inhibitors lead to an increase in extracellular adenosine concentrations. This, in turn, can contribute to neuroprotective and anti-inflammatory responses. Moreover, the inhibition of ENT1 can disrupt the availability of nucleosides necessary for DNA and RNA synthesis, thereby influencing cell proliferation and differentiation. Additionally, altering nucleoside transport through ENT1 can have broader implications for purinergic signaling, a multifaceted system governing various physiological processes such as neurotransmission, immune responses, and vascular regulation. Therefore, ENT1 inhibitors stand as invaluable tools for researchers seeking to unravel the intricacies of these cellular mechanisms, with applications extending beyond their primary purpose into various scientific disciplines.

Items 1 to 10 of 14 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Dipyridamole

58-32-2sc-200717
sc-200717A
1 g
5 g
$31.00
$102.00
1
(1)

Dipyridamole is a unique compound that functions as an inhibitor of adenosine uptake, engaging in specific interactions with nucleoside transporters. Its dual-ring structure allows for effective π-π stacking with aromatic residues, enhancing binding affinity. The compound exhibits complex reaction kinetics, characterized by a slow dissociation rate, which prolongs its effects on cellular signaling pathways. Additionally, its hydrophilic nature influences solubility and distribution in biological systems.

S-(4-Nitrobenzyl)-6-thioinosine (NBTI, NBMPR)

38048-32-7sc-200117
50 mg
$163.00
1
(1)

S-(4-Nitrobenzyl)-6-thioinosine (NBTI) is a selective inhibitor of nucleoside transporters, characterized by its unique thioinosine moiety that enhances binding through sulfur interactions. The nitrobenzyl group facilitates strong π-π interactions with aromatic amino acids, promoting specificity. NBTI exhibits distinct reaction kinetics, with a notable affinity for the transporter, leading to prolonged inhibition. Its lipophilic properties influence membrane permeability, affecting cellular uptake dynamics.

Imatinib

152459-95-5sc-267106
sc-267106A
sc-267106B
10 mg
100 mg
1 g
$26.00
$119.00
$213.00
27
(1)

Imatinib is a tyrosine kinase inhibitor that specifically targets the BCR-ABL fusion protein, inhibiting aberrant signaling pathways in chronic myeloid leukemia (CML) cells.

MDV3100

915087-33-1sc-364354
sc-364354A
5 mg
50 mg
$245.00
$1051.00
7
(1)

Enzalutamide inhibits the androgen receptor (AR) by binding to it and preventing its activation, suppressing AR-mediated transcription and growth of prostate cancer cells.

Gefitinib

184475-35-2sc-202166
sc-202166A
sc-202166B
sc-202166C
100 mg
250 mg
1 g
5 g
$63.00
$114.00
$218.00
$349.00
74
(2)

Gefitinib is an epidermal growth factor receptor (EGFR) inhibitor, blocking EGFR tyrosine kinase activity to halt signaling in lung cancer cells with EGFR mutations.

Sorafenib

284461-73-0sc-220125
sc-220125A
sc-220125B
5 mg
50 mg
500 mg
$57.00
$100.00
$250.00
129
(3)

Sorafenib is a multi-kinase inhibitor that inhibits the RAF/MEK/ERK pathway, reducing cell proliferation and angiogenesis in liver and kidney cancers.

Vemurafenib

918504-65-1sc-364643
sc-364643A
10 mg
50 mg
$117.00
$423.00
11
(1)

Vemurafenib selectively targets mutated BRAF kinases in melanomas, inhibiting their activity and preventing downstream signaling in cancer cells.

Lapatinib

231277-92-2sc-353658
100 mg
$420.00
32
(1)

Lapatinib is a dual tyrosine kinase inhibitor targeting EGFR and HER2, inhibiting their phosphorylation and blocking signaling in breast and gastric cancers.

Ibrutinib

936563-96-1sc-483194
10 mg
$156.00
5
(0)

Ibrutinib is a Bruton's tyrosine kinase (BTK) inhibitor that disrupts B-cell receptor signaling, leading to apoptosis and reducing the growth of B-cell malignancies.

Bortezomib

179324-69-7sc-217785
sc-217785A
2.5 mg
25 mg
$135.00
$1085.00
115
(2)

Bortezomib inhibits the proteasome, preventing protein degradation and causing apoptosis in multiple myeloma cells and some lymphomas.