JPH203 ( KYT-0353 )
JPH203(also known as KYT-0353) is a potent and selective LAT1 selective ( L-type amino acid transporter 1) inhibitor. JPH203 can very potently inhibit l-leucine uptake. JPH203 inhibits YD-38 cell growth. JPH203 up-regulated the population of apoptotic YD-38 cells through the activation of apoptotic factors, including caspases and PARP.
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Chemical Information
| Name | JPH203 ( KYT-0353 ) |
|---|---|
| Iupac Chemical Name | (S)-2-amino-3-(4-((5-amino-2-phenylbenzo[d]oxazol-7-yl)methoxy)-3,5-dichlorophenyl)propanoic acid |
| Synonyms | JPH203 ; JPH-203 ; JPH 203 ; KYT-0353 ; KYT 0353 ; KYT0353 |
| Molecular Formula | C23H19Cl2N3O4 |
| Molecular Weight | 471.1 |
| Smile | O=C(O)[C@@H](N)CC1=CC(Cl)=C(OCC2=C(OC(C3=CC=CC=C3)=N4)C4=CC(N)=C2)C(Cl)=C1 |
| InChiKey | XNRZJPQTMQZBCE-SFHVURJKSA-N |
| InChi | InChI=1S/C23H19Cl2N3O4/c24-16-6-12(8-18(27)23(29)30)7-17(25)21(16)31-11-14-9-15(26)10-19-20(14)32-22(28-19)13-4-2-1-3-5-13/h1-7,9-10,18H,8,11,26-27H2,(H,29,30)/t18-/m0/s1 |
| CAS Number | 1037592-40-7 |
| Related CAS | 1597402-27-1 (2HCl) 1037592-40-7 (free base) |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | light-yellow to off-white solid |
|---|---|
| Purity | ≧98.0% |
| Storage | 3 years -20ºCpowder 6 months-80ºCin solvent |
| Solubility | Soluble in DMSO, not in water |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1. Choi DW, Kim DK, Kanai Y, Wempe MF, Endou H,, Kim JK. JPH203, a selective L-type amino acid transporter 1 inhibitor, induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. Korean J Physiol Pharmacol. 2017 Nov;21(6):599-607. doi: 10.4196/kjpp.2017.21.6.599. Epub 2017 Oct 30.
2. Muto Y, Furihata T, Kaneko M, Higuchi K, Okunushi K, Morio H, Reien Y, Uesato M, Matsubara H, Anzai N., Different Response Profiles of Gastrointestinal Cancer Cells to an L-Type Amino Acid Transporter Inhibitor, JPH203. Anticancer Res. 2019 Jan;39(1):159-165. doi: 10.21873/anticanres.13092.
3. Häfliger P, Graff J, Rubin M, Stooss A, Dettmer MS, Altmann KH, Gertsch J, Charles RP.,The LAT1 inhibitor JPH203 reduces growth of thyroid carcinoma in a fully immunocompetent mouse model. J Exp Clin Cancer Res. 2018 Sep 21;37(1):234. doi: 10.1186/s13046-018-0907-z.
4. Yun DW, Lee SA, Park MG, Kim JS, Yu SK, Park MR, Kim SG, Oh JS, Kim CS, Kim HJ, Kim JS, Chun HS, Kanai Y, Endou H, Wempe MF, Kim DK., JPH203, an L-type amino acid transporter 1-selective compound, induces apoptosis of YD-38 human oral cancer cells. J Pharmacol Sci. 2014;124(2):208-17. Epub 2014 Feb
Chemical Structure
