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  4. KDM5B-IN-4

KDM5B-IN-4 (compound 11ad) 是一种新的赖氨酸去甲基化酶 5B (KDM5B) 抑制剂，对 KDM5B 的 IC50 为 0.025 μM。KDM5B-IN-4 通过抑制 PC-3 细胞内 KDM5B 增加底物 H3K4me1/2/3 浓度。KDM5B-IN-4 可将 PC-3 细胞阻滞在 G2/M 期。KDM5B-IN-4 能下调 PI3K/AKT 通路蛋白。KDM5B-IN-4 降低小鼠体内肿瘤体积且对脏器毒性较小。

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KDM5B-IN-4 Chemical Structure

KDM5B-IN-4 Chemical Structure

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Customer Review

KDM5B-IN-4 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs[1].

IC50 & Target

IC 50: 0.025 μM (Lysine demethylase 5B, KDM5B)[1].
体外研究
(In Vitro)

KDM5B-IN-4 (20 μM, 72 h) 对 PC-3 细胞中的 KDM5B 和诱导 H3K4me1/2/3 的产生有针对性的抑制作用[1]。
KDM5B-IN-4 (0-20 μM; 72 h) 不仅针对细胞中的 KDM5B，还能诱导 PC-3 细胞中 H3K4me1/2/3 的积累[1]。
KDM5B-IN-4 (0-10 μM, 0-24 h) 抑制前列腺癌细胞的增殖和迁移，在 G2/M 期阻断 PC-3 周期，并且能在一定程度上诱导 PC-3 细胞的凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KDM5B-IN-4 相关抗体:

Western Blot Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10, 20 μM
Incubation Time: 72 h
Result: Induced the concentrations of H3K4me1/2/3 significantly different from those of the control, and the results obtained were similar to those obtained using the CPI-455 positive control.
Had no significant effect on P110α, P85, and pAKT at low concentration levels (0-10μM), and P110α, P85, and pAKT were significantly decreased when 11ad was at high concentration (20 μM).

Cell Migration Assay [1]

Cell Line: PC-3
Concentration: 0, 5, 10 μM
Incubation Time: 0, 6, 12, 24 h
Result: Inhibited colony formation in a dosedependent manner, especially at high doses (10 μM).

Cell Cycle Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Blocked the cell cycle at G2/M phase in 10 μM.

Apoptosis Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced PC-3 cell apoptosis in a dose-dependent manner (7.58%, 26.14%, 28.20%, 45.66%).
体内研究
(In Vivo)

KDM5B-IN-4 (50 mg/kg, i.g., 50 mg/kg/d, 13 days) 的抑制肿瘤效果略好于 DOX 的疗效[1]。
KDM5B-IN-4 (50 mg/kg, i.g., 50 mg/kg/d, 25 days) 没有对小鼠造成明显的损害，证实在体内没有明显的毒性或副作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC-3 xenograft model in male Spraguee-Dawley rats[1].
Dosage: 25, 50 mg/kg
Administration: Intragastric administration to mice (i.g.) for 25 days, administered once daily.
Result: Compared with NaCl treatment, treatment with 25 mg/kg and 50 mg/kg significantly decreased tumor volume.
Animal Model: PC-3 xenograft model in male Spraguee-Dawley rats[1].
Dosage: 2 g/kg
Administration: Intragastric administration to mice (i.g.) for 14 days, administered once daily.
Result: No significant loss of major organs in the high-dose and low-dose groups.
分子量

490.60

Formula

C30H30N6O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KDM5B-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KDM5B-IN-4OthersPC-3LNCaPhuman prostate cancer cellPC-3 xenograft modelprostate cancer.Inhibitorinhibitorinhibit

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