2. Epigenetics
  3. Epigenetic Reader Domain
  4. Eleven-Nineteen-Leukemia Protein IN-3

Eleven-Nineteen-Leukemia Protein IN-3 

目录号: HY-152471
产品使用指南

摩尔计算器

Eleven-Nineteen-Leukemia Protein IN-3 是一种口服有效的 ENL YEATS 结构域抑制剂，IC50 值为 15.4 nM。Eleven-Nineteen-Leukemia Protein IN-3 通过细胞中的 ENL 下调 MYC 的表达，能增强 ENL 蛋白体外热稳定性。

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Eleven-Nineteen-Leukemia Protein IN-3 Chemical Structure

Eleven-Nineteen-Leukemia Protein IN-3 Chemical Structure

CAS No. : 2894121-83-4

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Eleven-Nineteen-Leukemia Protein IN-3 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

Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro[1].

IC50 & Target[1]

Eleven-Nineteen-Leukemia YEATS domain

15.4 nM (IC50)

体外研究
(In Vitro)

Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) 对 MV4-11 和 MOLM-13 细胞系有显著的抑制作用，IC50 值分别为 4.8 µM 和 8.3 µM[1]。
Eleven-Nineteen-Leukemia Protein IN-3 (5 µM；6 h) 显著提高内源性 ENL 蛋白的热稳定性，对 GAS41 蛋白的热稳定性无明显影响。Eleven-Nineteen-Leukemia Protein IN-3 能有效地抑制 MOLM-13 细胞生长[1]。
Eleven-Nineteen-Leukemia Protein IN-3 (5 µM；72 h) 抑制了关键癌基因 MYC 的表达 (约 50 %)。Eleven-Nineteen-Leukemia Protein IN-3 与 JQ-1 (HY-13030) 协同作用时，能进一步下调 ENL 靶基因中 MYC 的表达[1]。

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

Eleven-Nineteen-Leukemia Protein IN-3 相关抗体:

RT-PCR[1]

Cell Line: MOLM-13 cells.
Concentration: 5 µM.
Incubation Time: 72 h.
Result: Showed inhibitory for MYC.
体内研究
(In Vivo)

Eleven-Nineteen-Leukemia Protein IN-3 (Compound 28) (30 mg/kg；口服；单剂量) 具有口服暴露特性[1]。
Eleven-Nineteen-Leukemia Protein IN-3 (5 mg/kg；静脉注射；单剂量) 在体内有较高的暴露量[1]。
雄性 BALB/c 小鼠的药代动力学 (PK) 研究[1]

Administration t1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h•ng/mL) AUC0-∞ (h•ng/mL) MRT0-∞ (h)
p.o. 5.2 0.5 71.8 257 272 5.5
Administration t1/2 (h) AUC0-t (h•ng/mL) AUC0-∞ (h•ng/mL) Vss (L/kg) CL (mL/min/kg) MRT0-∞ (h) F (%)
i.v. 4.0 8290 8690 0.8 9.6 1.3 0.5

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

Animal Model: Male BALB/c mice[1].
Dosage: 30 mg/kg.
Administration: Oral gavage; single dose.
Result: Showed an oral activity.
Animal Model: Male BALB/c mice[1].
Dosage: 5 mg/kg.
Administration: Intravenous injection; single dose.
Result: Exhibited efficacy.
分子量

465.55

Formula

C28H27N5O2
CAS 号
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

Eleven-Nineteen-Leukemia Protein IN-3 相关分类

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  • 稀释计算器

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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:

Eleven-Nineteen-Leukemia Protein IN-32894121-83-4Epigenetic Reader DomainMV4-11MOLM-13Male BALB/c miceInhibitorinhibitorinhibit

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