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JPH203

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.

Research Area

Cell Biology

Images & Validation

Key Properties

CAS Number1597402-27-1
MW545.2
Purity>98%
FormulaC23H19Cl2N3O4·2HCl
SMILESC1=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
TargetOthers
SolubilitySoluble in DMSO (up to at least 25 mg/ml)

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-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

KYT-0353; Nanvuralant

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Key Properties

No computed properties available.

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JPH203 (orb1309522)

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5 mg
¥ 3,120.00
25 mg
¥ 6,500.00
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