2. Cell Cycle/DNA Damage Stem Cell/Wnt Epigenetics
  3. Casein Kinase HDAC
  4. IOR-160

IOR-160 是 casein kinase 2 (CK2) 和 HDAC 双重抑制剂。IOR-160 对 CK2 表现出高选择性 (IC50 =1.7 nM)，并且对 HDAC (HDAC 1、2、3 和 6，IC50 分别为 3.3 nM、24.0 nM、3.9 nM、13.0 nM，HDAC8 活性低) 具有广泛的抑制活性。IOR-160 通过抑制 AKT 磷酸化和乙酰化 α-微管蛋白的增加调节关键的细胞信号通路。IOR-160 通过双重 CK2/HDAC 抑制肿瘤生长并降低了肿瘤负荷。IOR-160 可用于三阴性乳腺癌研究。

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IOR-160

IOR-160 Chemical Structure

CAS No. : 2421119-78-8

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IOR-160 相关抗体

Top Publications Citing Use of Products

查看 Casein Kinase 亚型特异性产品:

查看所有亚型
CK1 CK2

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research[1].

IC50 & Target[1]

CK2

1.7 nM (IC50)

HDAC1

3.3 nM (IC50)

HDAC2

24 nM (IC50)

HDAC3

3.9 nM (IC50)

HDAC6

13 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
104.73 μM
Compound: 15c
Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human A549 cells incubated for 96 hrs by resazurin assay
[PMID: 32435375]
LNCaP IC50
16.31 μM
Compound: 15c
Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human LNCAP cells incubated for 96 hrs by resazurin assay
[PMID: 32435375]
MCF7 IC50
52.48 μM
Compound: 15c
Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human MCF7 cells incubated for 96 hrs by resazurin assay
[PMID: 32435375]
PC-3 IC50
40.42 μM
Compound: 15c
Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay
Antiproliferative activity against human PC3 cells incubated for 96 hrs by resazurin assay
[PMID: 32435375]
体外研究
(In Vitro)

IOR-160 (0.5 μM) 对 CK2 和 HIPK2 表现出较高的抑制作用，残留活性分别为 -6% 和 7%，而对 DYRK1A、CLK2、Pim-1、Mnk2、DRAK1 和 TrkA 表现出中等至低度抑制作用 (从 18% 到 65%)[1]。
IOR-160对 HDAC8 的抑制作用较弱，IC50 为 2200 nM[1]。

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

IOR-160 相关抗体:
体内研究
(In Vivo)

IOR-160 (1.0 mg 溶于 100 μL PBS，肿瘤内注射，每周三次，共 26 天) 通过双重 CK2/HDAC 抑制来减少携带 MDA-MB-231 细胞的非肥胖糖尿病 (NOD) scid γ 小鼠的肿瘤生长[1]。

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

Animal Model: MDA-MB-231 cells (3 × 106) xenograft NOD scid gamma mice (8-week-old) Model[1]
Dosage: 1.0 mg in 100 μL of PBS
Administration: injected intratumorally, three times a week, 26 days
Result: Reduced tumor growth.
Reduced pAKT levels and increased acetylated α-tubulin.
分子量

510.46

Formula

C23H25F3N4O6
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

IOR-160 相关分类

  • 摩尔计算器

  • 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:

IOR-1602421119-78-8IOR160IOR 160Casein KinaseHDACHistone deacetylasesInhibitorNOD scid gamma miceMDA-MB-231 cellsinhibitorinhibit

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