Basic Description

Synonyms	HY-100868 \| JPH203 free base \| (2S)-2-amino-3-[4-[(5-amino-2-phenyl-1,3-benzoxazol-7-yl)methoxy]-3,5-dichlorophenyl]propanoic acid \| JPH203 \| JPH-203 \| L-Tyrosine, O-((5-amino-2-phenyl-7-benzoxazolyl)methyl)-3,5-dichloro- \| D71159 \| (S)-2-amino-3-(4-((5-a
Specifications & Purity	Moligand™, ≥97%
Biochemical and Physiological Mechanisms	JPH203 (KYT-0353, JPH-203SBECD), a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leu
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of L-type amino acid transporter 1
Product Description	Information JPH203 JPH203 (KYT-0353, JPH-203SBECD), a selective L-type amino acid transporter 1 inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells. Targets LAT1 (Cell-free assay) In vitro JPH203 completely and slightly inhibited the L-Leucine uptake in YD-38 cells (IC50 value: 0.79 μM) and NHOKs (IC50 value: >100 μM), respectively. JPH203 inhibited HT-29 cell growth, generating an apparent IC50 of 4.1 μM, but the JPH203 IC50 concentration (0.06 μM) needed to inhibit the L-Leucine uptake did not inhibit HT-29 cell growth, which represents a 68-fold difference in susceptibility. JPH203 activated the mitochondria-dependent apoptotic signaling pathway by upregulating pro-apoptotic factors, such as Bad, Bax, and Bak, and the active form of caspase-9, and downregulating anti-apoptotic factors, such as Bcl-2 and Bcl-xL in Saos2 human osteosarcoma cells. JPH203 can distinguish relative abundance between LAT1 and LAT2. It has high selectivity for LAT1. JPH203 was metabolically stable in mouse, rat, dog, monkey and human liver microsomal incubations. JPH203 induces both G2/M and G0/G1 cell cycle arrest, as well as reduced the S phase accompanied by altered expression of the proteins in cell cycle progression: cyclin D1, CDK4, and CDK6. In vivo Daily intravenous administration of JPH203 (12.5 and 25 mg/kg) significantly inhibited tumor growth in KKU-213 cholangiocarcinoma cell xenografts in the nude mice model in a dose-dependent manner with no statistically significant change in the animal’s body weight and with no differences in the histology and appearance of the internal organs compared with the control group. Thus, JPH203 shows anti-tumor efficacy in nude mice bearing human cholangiocarcinom (CCA) cell xenografts without general toxicity. Cell Research(from reference) Cell lines：Saos2 human osteosarcoma cells Concentrations：100 µM Incubation Time：72 h

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organic acids and derivatives
  - Class Carboxylic acids and derivatives
    - Subclass Amino acids, peptides, and analogues
      - Level5 Amino acids and derivatives
        Level6 Alpha amino acids and derivatives
        Level7 Phenylalanine and derivatives

Kingdom	Organic compounds
Superclass	Organic acids and derivatives
Class	Carboxylic acids and derivatives
Subclass	Amino acids, peptides, and analogues
Intermediate Tree Nodes	Amino acids and derivatives - Alpha amino acids and derivatives
Direct Parent	Phenylalanine and derivatives
Alternative Parents	Phenylpropanoic acids Phenyl-1,3-oxazoles L-alpha-amino acids Amphetamines and derivatives Benzoxazoles Phenoxy compounds Dichlorobenzenes Phenol ethers Aralkylamines Alkyl aryl ethers Aryl chlorides Heteroaromatic compounds Amino acids Oxacyclic compounds Azacyclic compounds Carboxylic acids Monocarboxylic acids and derivatives Carbonyl compounds Hydrocarbon derivatives Monoalkylamines Organic oxides Organochlorides
Molecular Framework	Aromatic heteropolycyclic compounds
Substituents	Phenylalanine or derivatives - Phenyl-1,3-oxazole - 3-phenylpropanoic-acid - Alpha-amino acid - Amphetamine or derivatives - L-alpha-amino acid - Benzoxazole - Phenol ether - Phenoxy compound - 1,3-dichlorobenzene - Alkyl aryl ether - Aralkylamine - Chlorobenzene - Halobenzene - Benzenoid - Aryl halide - Aryl chloride - Monocyclic benzene moiety - Heteroaromatic compound - Azole - Oxazole - Amino acid - Carboxylic acid - Monocarboxylic acid or derivatives - Azacycle - Oxacycle - Ether - Organoheterocyclic compound - Organic nitrogen compound - Primary aliphatic amine - Organohalogen compound - Carbonyl group - Organochloride - Organonitrogen compound - Organooxygen compound - Primary amine - Hydrocarbon derivative - Organic oxide - Amine - Organic oxygen compound - Aromatic heteropolycyclic compound
Description	This compound belongs to the class of organic compounds known as phenylalanine and derivatives. These are compounds containing phenylalanine or a derivative thereof resulting from reaction of phenylalanine at the amino group or the carboxy group, or from the replacement of any hydrogen of glycine by a heteroatom.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Associated Targets(Human)

SLC7A5 Tchem Large neutral amino acids transporter small subunit 1 (2 Activities)

Discover Target: SLC7A5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HT-29 (80576 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

IUPAC Name	(2S)-2-amino-3-[4-[(5-amino-2-phenyl-1,3-benzoxazol-7-yl)methoxy]-3,5-dichlorophenyl]propanoic acid
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
InChIKey	XNRZJPQTMQZBCE-SFHVURJKSA-N
Smiles	C1=CC=C(C=C1)C2=NC3=CC(=CC(=C3O2)COC4=C(C=C(C=C4Cl)CC(C(=O)O)N)Cl)N
Isomeric 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
Molecular Weight	472.32
Reaxy-Rn	34121265
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=34121265&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

8 results found

Lot Number	Certificate Type	Date	Item
I2404550	Certificate of Analysis	Aug 26, 2024	J414105
I2404546	Certificate of Analysis	Aug 26, 2024	J414105
I2404547	Certificate of Analysis	Aug 26, 2024	J414105
I2404548	Certificate of Analysis	Aug 26, 2024	J414105
I2404549	Certificate of Analysis	Aug 26, 2024	J414105
I2404551	Certificate of Analysis	Aug 26, 2024	J414105
I2404552	Certificate of Analysis	Aug 26, 2024	J414105
I2404553	Certificate of Analysis	Aug 26, 2024	J414105

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro 5%TFA 2.31 mg/mL warmed with 50ºC Water: bath (4.89 mM); DMSO: 0.01 mg/mL (0.02 mM); Water: Insoluble;
Molecular Weight	472.300 g/mol
XLogP3	2.100
Hydrogen Bond Donor Count	3
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	7
Exact Mass	471.075 Da
Monoisotopic Mass	471.075 Da
Topological Polar Surface Area	125.000 Å²
Heavy Atom Count	32
Formal Charge	0
Complexity	626.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	1
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Mass

=

Concentration

x

Volume

x

M. Wt*

g/mol

*When preparing stock solutions, always use the batch-specific molecular weight of the product found on the vial label and the Certificate of Analysis (available online).

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

Concentration 1 (C1)

x

Volume 1 (V1)

=

Concentration 2 (C2)

x

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator enables you to quickly determine the volume of a reagent needed to reconstitute your vial. Just enter the mass of the reagent and the target concentration, and the calculator will do the rest.

Volume (to add to vial)

=

Mass (in vial)

÷

Desired Reconstitution Concentration

SKU	Size	Availability	Price
J414105-5mg	5mg	2	$77.90
J414105-10mg	10mg	2	$108.90
J414105-25mg	25mg	1	$189.90
J414105-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$289.90
J414105-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$449.90

JPH203 - 97%, high purity , CAS No.1037592-40-7, Inhibitor of L-type amino acid transporter 1