JPH203 dihydrochloride

SKU: orb1309522

Description

JPH203 dihydrochloride, also known as KYT-0353, is a tyrosine-based selective inhibitor of the L-type amino acid transporter 1 (LAT1). It is utilized in cancer research to investigate LAT1 function and inhibit tumor cell proliferation in both in vitro and in vivo experimental models.

Key Properties

• CAS Number: 1597402-27-1
• MW: 545.24
• Purity: 97.28% (May vary between batches)
• Formula: C₂₃H₂₁Cl₄N₃O₄
• SMILES: C1=CC=C(C=C1)C2=NC3=CC(=CC(=C3O2)COC4=C(C=C(C=C4Cl)C[C@@H](C(=O)O)N)Cl)N.Cl.Cl
• Target: Others
• Solubility: H2O:10 mg/mL (18.34 mM);DMSO:50 mg/mL (91.7 mM)

Bioactivity

• In Vivo:
  JPH203 exhibits dose-dependent inhibition on HT-29 tumor growth in nude mice.
• In Vitro:
  JPH203 (30 mM) induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. JPH203 (0.001-100 μM) inhibits 14C-leucine (1.0 μM) uptake slightly in FOB cells with an IC50 value of 92.12 ± 10.71 μM, but potently exihibts such effects in Saos2 cells with an IC50 value of 1.31 ± 0.27 μM. JPH203 (0.01 to 30 mM, 1-4 d) potently inhibits cell proliferation in Saos2 cells in a dose- and time-dependent manner, with an IC50 of 4.09-0.09 mM, but slightly inhibits that of FOB cells, with an IC50 of 24.1-2.8 mM.JPH203 Dihydrochloride is a selective inhibitor of LAT1. JPH203 inhibits 14C-leucine uptake in S2-hLAT1 and HT-29 cells, with IC50s of 0.14 μM and 0.06 μM. JPH203 (3-1000 μM) exhibits concentration-dependent inhibitory effects on S2-hLAT1 cell growth with an IC50 of 16.4 μM. JPH203 also displays inhibitory activities against HT-29 cell growth, with an IC50 value of 4.1 μM. JPH203 (0.001-100 μM) inhibits the 14C-leucine (1.0 μM) uptake in a concentration dependent way by the YD-38 cells with an IC50 value of 0.79 ± 0.06 μM. JPH203 slightly shows such effects in normal human oral keratinocytes (NHOKs). JPH203 (0.01-30 mM, 1-4 d) completely inhibits the proliferation of YD-38 cells in a dose- and time-dependent manner. However, JPH203 slightly inhibits the proliferation of NHOKs. JPH203 (30 mM) induces apoptosis of YD-38 cells. JPH203 (3 mM) also increases the level of cleaved PARP in activation of the caspases cascade.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KYT 0353, KYT 0353 Dihydrochloride, KYT0353, KYT-0353, KYT0353 Dihydrochloride, KYT-0353 Dihydrochloride, KYT-0353 dihydrochloride, JPH 203, JPH 203 Dihydrochloride, JPH203, JPH-203, JPH203 dihydrochloride, JPH203 Dihydrochloride, JPH-203 Dihydrochloride, JPH-203 dihydrochloride, LAT1

Compound Identifiers

PubChem CID

122553374