2. Cell Cycle/DNA Damage Epigenetics GPCR/G Protein
  3. HDAC Adenosine Receptor
  4. A2AAR/HDAC-IN-2

A2AAR/HDAC-IN-2 是一种有效的 A2AAR/HDAC 双重抑制剂，其对 A2AAR 具有良好的亲和力 (Ki=10.3 nM), 对 HDAC1 具有良好的抑制活性 (IC50=18.5 nM). A2AAR/HDAC-IN-2 可用于抗肿瘤的研究。

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A2AAR/HDAC-IN-2 Chemical Structure

A2AAR/HDAC-IN-2 Chemical Structure

CAS No. : 2767560-94-9

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A2AAR/HDAC-IN-2 相关抗体

Top Publications Citing Use of Products

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

查看 Adenosine Receptor 亚型特异性产品:

查看所有亚型
Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor[1].

IC50 & Target

HDAC1

18.5 nM (IC50)

HDAC2

16.0 nM (IC50)

HDAC3

13.6 nM (IC50)

HDAC6

2.1 nM (IC50)

HDAC8

1408.9 nM (IC50)

A1AR

105.6 nM (Ki)

A2AAR

10.3 nM (Ki)

A2BAR

513.0 nM (Ki)

A3AR

＞10 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CT26 GI50
12.61 μM
Compound: 30c
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK-8 assay
[PMID: 35390714]
MC-38 GI50
12.16 μM
Compound: 30c
Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against mouse MC38 cells after 72 hrs by CCK-8 assay
[PMID: 35390714]
体外研究
(In Vitro)

A2AAR/HDAC-IN-2 (compound 30c) (5 nM-100 µM; 72 h) shows anti-proliferative activity, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively[1].
A2AAR/HDAC-IN-2 (0.1, 1, 5, 10 µM; 24 h) increases histone H3 and H4 acetylation in a concentration-dependent manner in MC38 cells[1].

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

A2AAR/HDAC-IN-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MC38 and CT26 cells
Concentration: 5 nM-100 µM
Incubation Time: 72 h
Result: Showed good anti-proliferative activity in cancer cell lines, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively.

Western Blot Analysis[1]

Cell Line: MC38 cells
Concentration: 0.1, 1, 5, 10 µM
Incubation Time: 24 h
Result: Significantly increases histone H3 and H4 acetylation at 10 µM and in a concentration-dependent manner.
分子量

450.49

Formula

C23H26N6O4
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

A2AAR/HDAC-IN-2 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:

A2AAR/HDAC-IN-22767560-94-9HDACAdenosine ReceptorHistone deacetylasesP1 receptorimmunotherapyTMEadenosineantitumorMC38CT26Inhibitorinhibitorinhibit

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