An inhibitor of LAT1 (IC50 = 0.14 μM for 14C-leucine uptake in S2 cells expressing the human transporter); selective for LAT1 over LAT2 (IC50 = >10 μM); inhibits 14C-leucine uptake by

JPH203 – 10 mg

Brand:
Cayman
CAS:
1037592-40-7
Storage:
-20
UN-No:
Non-Hazardous - /

JPH203 is an inhibitor of L-type amino acid transporter 1 (LAT1; IC50 = 0.14 μM for 14C-leucine uptake in S2 cells expressing the human transporter).{52371} It is selective for LAT1 over LAT2 (IC50 = >10 μM). JPH203 inhibits 14C-leucine uptake by, and growth of, HT-29 cells (IC50s = 0.06 and 4.1 μM, respectively). It induces apoptosis and increases levels of cleaved caspase-3, caspase-7, caspase-9, and poly(ADP-ribose) polymerase (PARP) in YD-38 oral cancer cells when used at a concentration of 3 mM.{52372} JPH203 (6.3, 12.5, and 25 mg/kg) reduces tumor growth in an HT-29 mouse xenograft model.{52371}  

 

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SKU: 29715 - 10 mg Category:

Description

An inhibitor of LAT1 (IC50 = 0.14 μM for 14C-leucine uptake in S2 cells expressing the human transporter); selective for LAT1 over LAT2 (IC50 = >10 μM); inhibits 14C-leucine uptake by, and growth of, HT-29 cells (IC50s = 0.06 and 4.1 μM, respectively); induces apoptosis and increases levels of cleaved caspase-3, caspase-7, caspase-9, and PARP in YD-38 oral cancer cells at 3 mM; reduces tumor growth in an HT-29 mouse xenograft model at 6.3, 12.5, and 25 mg/kg

Formal name: O-[(5-amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine

Synonyms:  KYT-0353

Molecular weight: 472.3

CAS: 1037592-40-7

Purity: ≥98%

Formulation: A crystalline solid

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