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| Targets |
L-type amino acid transporter 1 (LAT1). LAT1 is a sodium-independent neutral amino acid transporter that is highly upregulated in various cancer cells to support their rapid growth by importing essential amino acids. KMH-233 is a selective inhibitor of LAT1, making it a valuable tool for studying amino acid transport in cancer metabolism and for validating potential anti-cancer strategies targeting this pathway.
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| ln Vitro |
KMH-233 inhibits the uptake of the LAT1 substrate L-leucine with an IC50 of 18 microM. In vitro, KMH-233 also inhibits cell growth. Even at a low concentration of 25 microM, KMH-233 significantly enhances the efficacy of the anticancer drugs Bestatin and Cisplatin, indicating its potential as a chemosensitizer.
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| ln Vivo |
No in vivo activity data is publicly available for (R)-KMH-233 itself. The parent compound KMH-233 has been used in studies to potentiate the efficacy of other anticancer agents in cell-based models, but detailed animal model data is not provided. As an inactive isomer, (R)-KMH-233 is used as a control in these in vivo experiments.
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| Enzyme Assay |
A typical LAT1 inhibition assay is performed in a non-cell system using purified LAT1 protein or LAT1-overexpressing membrane vesicles. The transport of a radiolabeled substrate, such as [14C]-L-leucine, is measured over a short period (1-5 minutes) in the presence or absence of the inhibitor. The reaction is terminated by rapid filtration, and the radioactivity retained on the filter is counted to calculate the IC50 value.
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| Cell Assay |
Cancer cell lines that overexpress LAT1, such as HeLa or A549 cells, are seeded in 96-well plates. The cells are treated with serial dilutions of KMH-233 (the parent compound) to assess its effect on cell growth, typically measured by an MTT assay after 72 hours of treatment. In combination studies, cells are co-treated with KMH-233 and other anticancer drugs like Cisplatin to evaluate potential synergy in inhibiting cell proliferation.
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| Animal Protocol |
No specific animal experimental procedures are available for (R)-KMH-233, as it is a research control. The parent compound KMH-233 is used in mouse xenograft models of cancer. For example, mice with subcutaneous tumor xenografts are administered KMH-233 orally or intraperitoneally, alone or in combination with Cisplatin. Tumor volumes are measured with calipers, and body weight is monitored to assess anti-tumor efficacy and toxicity.
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| ADME/Pharmacokinetics |
As an inactive isomer, pharmacokinetic data for (R)-KMH-233 is not detailed. The parent compound KMH-233 has a molecular weight of 587.58 and is soluble in DMSO. For in vivo studies, it can be formulated in a vehicle such as 10% DMSO in saline for intraperitoneal or oral administration. Detailed parameters such as half-life, bioavailability, and clearance are not provided in the available datasheets.
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| Toxicity/Toxicokinetics |
Toxicity data for (R)-KMH-233 is not publicly available. As a research control, it is not intended for therapeutic use. The parent compound KMH-233 has shown synergistic effects with other drugs without demonstrating overt cytotoxicity at low concentrations. However, comprehensive toxicology studies, including acute and chronic toxicity, have not been published for this research-grade chemical.
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| References | |
| Additional Infomation |
(R)-KMH-233 is a research-grade chemical used exclusively as a negative control in studies of LAT1 biology and cancer metabolism. The development of LAT1 inhibitors is an active area of research for cancer treatment, as LAT1 is a promising target for starving cancer cells of essential amino acids. This product is for research use only and is not FDA-approved for human use. A key reference is Huttunen KM, et al. J Med Chem. 2016;59(12):5740-5751.
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| Molecular Formula |
C32H25N7O5
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| Molecular Weight |
587.58
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| CAS # |
2994330-89-9
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| Related CAS # |
KMH-233;1941174-13-5
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| Appearance |
Light yellow to yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7019 mL | 8.5095 mL | 17.0190 mL | |
| 5 mM | 0.3404 mL | 1.7019 mL | 3.4038 mL | |
| 10 mM | 0.1702 mL | 0.8509 mL | 1.7019 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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