lat1

LAT1-IN-1 (BCH) is a selective and competitive inhibitor of L-type amino acid transporter protein 1 (LAT1). LAT1-IN-1 has antitumor activity, inducing apoptosis in tumor cells and inhibiting cell proliferation.

JPH203 (KYT-0353) is a potent and specific inhibitor of L-type amino acid transporter protein 1 (LAT-1). JPH203 inhibits cellular uptake of leucine, inhibits cell proliferation, induces apoptosis, and possesses anti-inflammatory and anti-tumor activities.

MALAT1-IN-1 modulated Malat1 downstream genes in a dose-dependent manner without affecting the expression of nuclear enriched abundant transcript 1 (Neat1). MALAT1-IN-1 is an effective and specific Malat1 inhibitor.

GPNA hydrochloride is specific glutamine (Gln) transporter ASCT2(SLC1A5) inhibitor. GPNA reversibly induces apoptosis in A549 cells. GPNA hydrochloride is a well-known substrate of the enzyme γ-glutamyltransferase (GGT). GPNA hydrochloride also inhibits

QBS10072S dihydrochloride is a bifunctional chemotherapeutic agent capable of penetrating the blood-brain barrier (BBB), featuring a LAT1-targeted domain and a cytotoxic domain. Its inhibitory potency on LAT1-mediated substrate uptake (IC50 = 21 μM) is approximately 50 times greater than on LAT2 (IC50 = 1100 μM). QBS10072S dihydrochloride enters tumor cells expressing LAT1 through LAT1-mediated active transport, resulting in DNA interstrand cross-linking, DNA damage, and cell death. This compound is applicable in research on glioblastoma and aggressive T-cell lymphoma.

Piezo1 agonist 2 (Compound PD2) is a Piezo1 activator capable of crossing the blood-brain barrier and serves as a Jedi2 conjugate utilizing LAT1. It releases Jedi2 in mice and can be used for research in neurodegenerative diseases.

AChE/BChE-IN-35, a tacrine derivative, is a dual inhibitor of AChE and BChE capable of crossing the blood-brain barrier. It exhibits an IC50 of 123.66 nM for electric eel AChE, 122.34 nM for human AChE, and 488.00 nM for equine BChE. The compound crosses cell membranes through LAT1-mediated active transport, showing increased brain exposure and a slower clearance rate from brain tissue. AChE/BChE-IN-35 is applicable in Alzheimer's disease research.

KMH-233 is a potent selective LAT1 inhibitor 1 that inhibits the uptake of LAT1 substrate, L-leucine, and cell growth. Even at low concentrations (25 μM), it significantly enhanced the efficacy of betastatin and cisplatin.

QBS10072S is a bifunctional chemotherapeutic agent that exerts its effects by combining a cytotoxin with a selective LAT1 transporter substrate. It demonstrates cytotoxicity in MDA-MB-231 cells and exhibits antitumor activity in mice. Additionally, QBS10072S possesses blood-brain barrier (BBB) permeability.

KHK-2898 represents a highly specialized humanized monoclonal antibody specifically engineered to target the CD98 heavy chain (CD98hc/SLC3A2) with exceptional binding affinity to the human and monkey LAT1/CD98hc complex. It effectively facilitates the measurable blockade of amino acid transport and the induction of potent antibody-dependent cellular cytotoxicity (ADCC) across various preclinical experimental models to evaluate the disruption of tumor nutrient uptake and metabolic homeostasis during strictly monitored laboratory observation periods and functional cell viability assays.

L-Citrulline (Standard) is available for quantitative analysis.) L-Citrulline is a non-essential amino acid involved in the nitric oxide cycle and the urea cycle, promotes vasodilatation, has antioxidant and anti-inflammatory properties, is orally available, and crosses the blood-brain barrier through LAT1. It is an agonist of eNOS (endothelial nitric oxide synthase), iNOS (inducible nitric oxide synthase), and mTORC1 (rapamycin targeting protein complex 1), and an inhibitor of SREBP-1 (sterol regulatory element binding protein 1).

(R)-KMH-233 is an isomer of KMH-233, which can serve as a reference compound in experiments. KMH-233 functions as a potent, reversible, and selective inhibitor of L-type amino acid transporter 1 (LAT1), effectively hindering the uptake of LAT1 substrate, l-leucine (IC50=18 μM), and also inhibiting cell growth. Even at a low concentration of 25 μM, KMH-233 significantly enhances the efficacy of Bestatin and cisplatin.