UCPH-102

UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder[1][2][3][4].

Product Specifications

CAS Number

[1229591-56-3]

Product Name Alternative

SKQ1

UNSPSC

12352005

Target

EAAT

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ucph-102.html

Purity

99.20

Solubility

DMSO : 8 mg/mL (ultrasonic; warming)

Smiles

N#CC1=C(OC(CC(C2)C3=C4C=CC=CC4=CC=C3)=C(C1C)C2=O)N

Molecular Formula

C21H18N2O2

Molecular Weight

330.38

References & Citations

[1]Huynh TH, et al. Design, synthesis and pharmacological characterization of coumarin-based fluorescent analogs of excitatory amino acid transporter subtype 1 selective inhibitors, UCPH-101 and UCPH-102. Bioorg Med Chem. 2012 Dec 1;20 (23) :6831-9.|[2]Haym I, et al. Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102. ChemMedChem. 2016 Feb 17;11 (4) :403-19.|[3]Stanulović V S, et al. Proliferation and Survival of T-cell Acute Lymphoblastic Leukaemia Depends on mTOR-regulated Glutamine Uptake and EAAT1-dependent Conversion of Glutamine to Aspartate and Nucleotides. bioRxiv. 2020. |[4]Abrahamsen B, et al. Allosteric modulation of an excitatory amino acid transporter: the subtype-selective inhibitor UCPH-101 exerts sustained inhibition of EAAT1 through an intramonomeric site in the trimerization domain. J Neurosci. 2013 Jan 16;33 (3) :1068-87.