| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
LAT1 (L-type amino acid transporter 1, SLC7A5). LAT1 is a transmembrane protein that transports large neutral amino acids (e.g., leucine, isoleucine, valine, phenylalanine, tyrosine) across cell membranes. LAT1 is upregulated in many cancers and is a target for anti-cancer therapy.
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|---|---|
| ln Vitro |
By blocking the binding and transport of necessary neutral amino acids, KMH-233 can stop cancer cells from growing [1]. KMH-233 exhibits a noteworthy decrease in cell proliferation, with an IC50 of 124 µM[1]. KMH-233 inhibits cell growth by 53% and 50%, respectively, and is an effective supplement that can boost the anti-proliferative activity of Bestatin (100 µM) and cisplatin (100 µM) at a lower dose of 25 µM[1].
KMH-233 inhibits LAT1-mediated L-leucine uptake with an IC50 of 18 µM. It shows a significant reduction of cell growth in cancer cells with an IC50 of 124 µM. KMH-233 inhibits binding and transport of essential neutral amino acids. |
| ln Vivo |
No detailed in vivo activity data has been published in the available literature. KMH-233 shows reduction of cell growth in cancer cells in vitro. Further in vivo studies in xenograft tumor models would be needed to evaluate its anti-tumor efficacy and pharmacokinetics.
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| Enzyme Assay |
LAT1 substrate uptake assay: Cells expressing LAT1 (e.g., cancer cell lines or LAT1-transfected cells) are incubated with varying concentrations of KMH-233 and radiolabeled L-leucine ([³H]-leucine) in uptake buffer (HBSS, pH 7.4) at 37°C for 5-10 min. Cells are washed, lysed, and radioactivity is measured by liquid scintillation counting. IC50 values for inhibition of leucine uptake are calculated.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MCF-7 Cell Tested Concentrations: 0.5-1000 μM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated significant reduction in cell growth with IC50 of 124 μM. Cell growth assay: Cancer cell lines (e.g., those with high LAT1 expression) are seeded in 96-well plates and treated with KMH-233 at varying concentrations (1-500 µM) for 48-72 hours. Cell viability is measured using MTT, CellTiter-Glo, or counting of viable cells. IC50 values for inhibition of cell growth are calculated from dose-response curves. |
| Animal Protocol |
No in vivo animal experimental protocols have been published for KMH-233 in the available literature. In vivo studies would typically involve xenograft tumor models in immunocompromised mice, where KMH-233 would be administered via oral or intraperitoneal routes, followed by tumor volume measurement, amino acid uptake analysis, and histopathological evaluation.
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| ADME/Pharmacokinetics |
No pharmacokinetic data has been published in the available literature. KMH-233 has a molecular formula C₃₂H₂₅N₇O₅ and is soluble in DMSO at 100 mg/mL (170.19 mM). Comprehensive PK parameters such as bioavailability, half-life, and plasma protein binding remain to be characterized.
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| Toxicity/Toxicokinetics |
No toxicity data has been published in the available literature. KMH-233 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As a LAT1 inhibitor, potential effects on amino acid homeostasis in normal tissues should be considered.
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| References | |
| Additional Infomation |
KMH-233 is a selective, reversible inhibitor of LAT1 (SLC7A5). It inhibits L-leucine uptake with an IC50 of 18 µM and reduces cancer cell growth with an IC50 of 124 µM. The compound is a valuable research tool for studying amino acid transport in cancer metabolism. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C32H25N7O5
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|---|---|
| Molecular Weight |
587.584806203842
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| Exact Mass |
587.191
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| CAS # |
1941174-13-5
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| Related CAS # |
(R)-KMH-233
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| PubChem CID |
154730690
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| Appearance |
White to yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
44
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| Complexity |
1160
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CNC(=O)COC1=CC=C(C=C1)C2=C(C3=NC4=CC=CC=C4N3C(=C2C#N)NC(=O)C5=CC=CC(=C5)C[C@@H](C(=O)O)N)C#N
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| InChi Key |
MLNOOVGSMCJSCE-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C32H25N7O5/c1-36-27(40)17-44-21-11-9-19(10-12-21)28-22(15-33)29-37-25-7-2-3-8-26(25)39(29)30(23(28)16-34)38-31(41)20-6-4-5-18(13-20)14-24(35)32(42)43/h2-13,24H,14,17,35H2,1H3,(H,36,40)(H,38,41)(H,42,43)/t24-/m0/s1
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| Chemical Name |
(S)-2-amino-3-(3-((2,4-dicyano-3-(4-(2-(methylamino)-2-oxoethoxy)phenyl)benzo[4,5]imidazo[1,2-a]pyridin-1-yl)carbamoyl)phenyl)propanoic acid
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| Synonyms |
KMH-233 KMH 233 KMH233.
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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) |
DMSO : ~100 mg/mL (~170.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (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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