GLPBio

JQEZ5

Catalog No.: GC19211Purity:>98.00%
JQEZ5 は、強力かつ選択的な EZH2 リジン メチルトランスフェラーゼ阻害剤です。 JQEZ5 ポリコーム抑制複合体 2 (PRC2) の SAM 競合阻害で、IC50 は 80 nM です。 JQEZ5には抗腫瘍効果があります。

製品は研究用途にのみ使用できます。人体には使用できません。患者への販売は行っておりません。


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

引用文献 (Citations)

現在、この製品の引用文献はありません。以下はGlpBio製品を引用した代表的な文献です。
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
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    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

製品説明 (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.

実験プロトコル (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.

製品資料 (Product Documents)

Purity:>98.00%Appearance:A solid

化学的性質 (Chemical Properties)

CAS番号
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
分子式
C30H38N8O2
分子量
542.68
溶解性
DMSO : 25 mg/mL (46.07 mM);Water : < 0.1 mg/mL (insoluble)
保存条件
Store at -20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。

計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度

g/mol

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