1. Epigenetics
  2. Histone Demethylase
  3. KDM5-C49

KDM5-C49  (Synonyms: KDOAM-20)

目录号: HY-119397
产品使用指南

KDM5-C49 (KDOAM-20) 是一种有效和选择性的 KDM5 去甲基化酶抑制剂,抑制 KDM5AKDM5BKDM5CIC50 值分别为 40 nM,160 nM 和 100 nM。KDM5-C49 可用于癌症的研究。

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KDM5-C49 Chemical Structure

KDM5-C49 Chemical Structure

CAS No. : 1596348-16-1

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规格 是否有货
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100 mg   询价  
250 mg   询价  

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KDM5-C49 的其他形式现货产品:

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查看 Histone Demethylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KDM5-C49 (KDOAM-20) is a potent and selective inhibitor of KDM5 demethylases, with IC50s of 40 nM, 160 nM, and 100 nM for KDM5A, KDM5B, and KDM5C enzymes, respectively. KDM5-C49 can be used for the research of cancer[1].

IC50 & Target

KDM5

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
1 μM
Compound: 128
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 120 hrs by ATPlite assay
[PMID: 26710088]
Sf9 IC50
< 0.1 μM
Compound: 128
Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of human N-terminal GST-tagged KDM4B (1 to 500 residues) expressed in baculovirus infected sf9 cells using biotinylated histone H3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
[PMID: 26710088]
Sf9 IC50
< 0.1 μM
Compound: 128
Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
Inhibition of recombinant human N-terminal FLAG-tagged KDM5C (2 to 1560 residues) expressed in baculovirus infected sf9 cells using biotin-H3K4me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
[PMID: 26710088]
Sf9 IC50
> 1 μM
Compound: 128
Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of recombinant KDM3B (842 to 1761 residues) (unknown origin) expressed in baculovirus infected sf9 cells using biotin-H3K9me as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
[PMID: 26710088]
Sf9 IC50
> 1 μM
Compound: 128
Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
Inhibition of human C-terminal FLAG-tagged KDM6B (1043 residues) expressed in baculovirus infected sf9 cells using H3K27me3 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa assay
[PMID: 26710088]
Sf9 IC50
0.1 μM
Compound: 128
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
Inhibition of recombinant human C-terminal FLAG-tagged KDM2B (1 to 650 residues) expressed in baculovirus infected sf9 cells using biotin-H3K36me2 as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by AlphaLisa ass
[PMID: 26710088]
U2OS IC50
1 μM
Compound: 128
Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
Inhibition of KDM5B in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
[PMID: 26710088]
U2OS IC50
1 μM
Compound: 128
Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
Inhibition of KDM5C in human U2OS cells assessed as reduction in demethylation of H3K4me3 after 20 hrs by Hoechst 33342 staining based immunofluorescence assay
[PMID: 26710088]
体外研究
(In Vitro)

KDM5-C49 渗透性差。将 KDM5-C49 的羧基转化为乙酯,得到具有细胞渗透性的前药(KDM5-C70)。

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

分子量

308.38

Formula

C15H24N4O3

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
  • 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 *
= × ×

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.

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产品名称:
KDM5-C49
目录号:
HY-119397
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