GLPBio

JQEZ5

Catalog No.: GC19211Purity:>98.00%
JQEZ5 es un inhibidor potente y selectivo de la lisina metiltransferasa EZH2. JQEZ5 InhibiciÓn competitiva de SAM del complejo represivo polycomb 2 (PRC2) con una IC50 de 80 nM. JQEZ5 tiene efectos antitumorales.

Los productos son exclusivamente para uso en investigación. No aptos para uso humano. No vendemos a pacientes.


JQEZ5
Cas No.: 1913252-04-6
10mM (in 1mL DMSO)In Stock
$64.00
1
5mgIn Stock
$53.00
1
10mgIn Stock
$78.00
1
25mgIn Stock
$150.00
1
50mgIn Stock
$222.00
1
100mgIn Stock
$323.00
1

Citas (Citations)

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  • Nature cover
    Nature
    641, 529–536 (2025)
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    Nature
    628, 630–638 (2024)
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    Nature
    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    Science
    388(6745) (2025)
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    387(6739) (2025)
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    Science
    387(6734) (2025)
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    Cell Research
    35, 97–116 (2025)
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    Cell Research
    34, 683–706 (2024)
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    Cell Research
    33, 273–287 (2023)
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    33, 546–561 (2023)
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    33, 904–922 (2023)
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    Cell Research
    31, 1291–1307 (2021)

Descripción (Description)

JQEZ5 is a novel and potent EZH2 inhibitor.

Animals treated with JQEZ5 exhibit rapid and pronounced tumor regression over the three week treatment course. H3K27me3 levels are largely reduced with treatment further confirming the on-target effect of JQEZ5 in mice. The level of H3K27me3 is largely reduced with the treatment without effect on EZH2 levels in both the tumor and in the lung tissue of JQEZ5 treated animals[1].

References:
[1]. Zhang H, et al. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21.

Protocolo (Protocol)

Animal experiment:

Tumor-bearing genetically-engineered mouse models (GEMMs) are monitored for onset of symptoms (breath distress) and then treated with JQEZ5 for three weeks (75 mg/kg IP daily). Tumors are visualized by MRI and tumor volume of the lungs is calculated using 3D Slicer. For xenograft experiments, H661 cells are dissociated into single cells, counted and resuspended at 2×106 cells per 250 µL of 1:1 media/matrigel. Eight- to 12-week-old female Foxn1nu/Foxn1nu mice are injected subcutaneously with 2×106 cells in two to three spots on the flanks. Tumors are allowed to grow to an approximate size of 200 mm3 (~10 weeks) and the mice are randomized for vehicle (n=3) or JQEZ5 administration (n=6, 75 mg/kg/d, i.p.) for 18 days. Tumor growth is measured by caliper measurements and tumor volume is calculated by standard methods[1].

References:

[1]. Zhang H, et al. Oncogenic Deregulation of EZH2 as an Opportunity for Targeted Therapy in Lung Cancer. Cancer Discov. 2016 Sep;6(9):1006-21.

Documentos del producto (Product Documents)

Purity:>98.00%Appearance:A solid

Propiedades químicas (Chemical Properties)

N.º CAS
1913252-04-6
SMILES
CC(N1N=CC2=C(C(NCC3=C(C=C(NC3=O)C)CCC)=O)C=C(C4=CC=C(N=C4)N5CCN(C)CC5)N=C12)C
Fórmula molecular
C30H38N8O2
Peso molecular
542.68
Solubilidad
DMSO : 25 mg/mL (46.07 mM);Water : < 0.1 mg/mL (insoluble)
Almacenamiento
Store at -20°C
Consejos generales
Seleccione un disolvente adecuado según los datos de solubilidad del producto. Una vez preparada, divida la solución madre en alícuotas para evitar ciclos repetidos de congelación y descongelación.
Utilice las soluciones madre en un plazo de 6 meses si se conservan a -80°C, o de 1 mes si se conservan a -20°C.
Para mejorar la solubilidad, caliente el tubo a 37°C y soníquelo durante un periodo adecuado.
Condiciones de envío
Las muestras de evaluación se envían con acumuladores de frío. Los demás tamaños se envían a temperatura ambiente o, previa solicitud, con acumuladores de frío.

Calculadoras (Calculators)Molaridad / Dilución / Peso molecular / Conversión de unidades / Formulación in vivo / Solubilidad

g/mol

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