GLPBio

WJ460

Catalog No.: GC38203Purity:>98.00%
WJ460 ist ein potenter Myoferlin (MYOF)-Inhibitor, der direkt mit MYOF interagiert und in Brustkrebszellen eine antimetastatische AktivitÄt im nanomolaren Bereich ausÜbt.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.


WJ460
Cas No.: 1415251-36-3
10mM (in 1mL DMSO)In Stock
$114.00
1
1mgIn Stock
$35.00
1
5mgIn Stock
$112.00
1
10mgIn Stock
$189.00
1
25mgIn Stock
$315.00
1
50mgIn Stock
$539.00
1
100mgIn Stock
$910.00
1

Zitate (Citations)

1 publicationsPublikationen von Forschern, die dieses Produkt verwenden

Beschreibung (Description)

WJ460 is a potent myoferlin (MYOF) inhibitor, which interacts directly with MYOF[2]. WJ460 blocks breast cancer cell invasion with IC50 values of 43.37±3.42nM in MDA-MB-231[2]. However , WJ460 was inadequate in terms of metabolic stability and water solubility as well as binding activity with MYOF[3].

WJ460 (1μM, 24h) reduced Human T-cell leukemia virus type 1 (HTLV-1 infection) , which was correlated with a reduction in the intracellular level of mature Env[4]. WJ460 (50nM, 15h, 2Gy x-rays) treated HCT116 (cancer cell lines) spheroids were significantly radiosensitized as observed by a reduction in growth at day 15 post-seeding , compared with vehicle cells[5].

WJ460 (10mg/kg; 28 days; intraperitoneal injection) inhibits breast tumor growth, angiogenesis, and spontaneous metastasis in a mouse model[2]. WJ460(10mg/kg; 4weeks; intraperitoneal injection) caused a reduction of the abundance of ferroptosis core regulators solute carrier family 7 member 11 (SLC7A11) and glutathione peroxidase 4 (GPX-4)[1].

THPTA ligand

WJ460 , a myoferlin inhibitor , exerts anti-metastatic activity in breast cancer[2].

References:

[1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324.

[2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726.

[3] GU H, ZHANG T, LI Y, et al. Discovery of 1,5-diaryl-1,2,4-triazole derivatives as myoferlin inhibitors and their antitumor effects in pancreatic cancer [J]. Future Med Chem, 2022, 14(20): 1425-40.

[4] POLAKOWSKI N, SARKER M A K, HOANG K, et al. HBZ upregulates myoferlin expression to facilitate HTLV-1 infection [J]. PLoS Pathog, 2023, 19(2): e1011202.

[5] FOWLER H, CLIFFORD R E, BOWDEN D, et al. Myoferlin: A Potential Marker of Response to Radiation Therapy and Survival in Locally Advanced Rectal Cancer [J]. Int J Radiat Oncol Biol Phys, 2024, 120(4): 1111-23.

Protokoll (Protocol)

Cell experiment[1]:

Cell lines

Pancreatic Cancer Cell Line 1 (PANC-1)

Preparation method

PANC-1 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS). Cells were cultured in a 37℃, 5% CO2 incubator. Cells were checked monthly for mycoplasma and used between passage 1 and 10. The cells culture were submitted to 50nM WJ460 during 24h.

Reaction Conditions

50nM ; 24h

Applications

WJ460 triggers a cell cycle arrest in G2/M phase and mitophagy

Animal experiment[2]:

Animal models

Female nude mice BALB/c athymic nude mice

Preparation method

For the spontaneous metastasis model , MDA-MB-231- Luciferase cells (1×106) were injected in the #4 mammary fat pad of the mice. Lung metastasis was monitored weekly by an in vivo image system and histological examination.  

Dosage form

10mg/kg ; 28 days ; intraperitoneal injection.

Applications

WJ460 caused significant inhibition of breast cancer pulmonary metastasis.

References:

[1] RADEMAKER G, BOUMAHD Y, PEIFFER R, et al. Myoferlin targeting triggers mitophagy and primes ferroptosis in pancreatic cancer cells [J]. Redox Biol, 2022, 53(102324.

[2] ZHANG T, LI J, HE Y, et al. A small molecule targeting myoferlin exerts promising anti-tumor effects on breast cancer [J]. Nat Commun, 2018, 9(1): 3726.

Produktdokumente (Product Documents)

Purity:>98.00%Appearance:A solid

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
1415251-36-3
SMILES
O=C(NCCCCC1=CC=CC=C1)C2=CC=CC(C(N3C4=CC=CC=C4OC)SCC3=O)=C2
Summenformel
C27H28N2O3S
Molekulargewicht
460.59
Löslichkeit
DMSO: 250 mg/mL (542.78 mM)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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