2. Cell Cycle/DNA Damage Epigenetics
  3. PARP
  4. AZ0108

AZ0108 是一种聚 ADP-核糖聚合酶 (PARP) 抑制剂，可抑制 PARP1、PARP2、PARP3、PARP6、TNKS1、TNKS2，IC50 分别为 0.03、<0.03、2.8、0.083、3.2、>3 μM。AZ0108 可防止着丝粒聚集，EC50 为 0.053 μM，并在细胞 OCI-LY-19 中表现出细胞毒性，GI50 为 0.017 μM。AZ0108 在大鼠/小鼠模型中表现出良好的体内药代动力学特征。

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AZ0108 Chemical Structure

AZ0108 Chemical Structure

CAS No. : 1825345-52-5

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AZ0108 相关抗体

Top Publications Citing Use of Products

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models[1].

IC50 & Target

PARP1

0.03 μM (IC50)

PARP2

0.03 μM (IC50)

PARP6

0.083 μM (IC50)

PARP3

2.8 μM (IC50)

TNKS1

3.2 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCC1806 EC50
30 nM
Compound: 14f; AZ0108
Inhibition of PARP in human HCC1806 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human HCC1806 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
HeLa EC50
0.053 μM
Compound: 15; AZ0108
Inhibition of PARP in human HeLa cells assessed as induction of centrosomal clustering blockade by measuring increase in mitotic cells with multipolar spindles measured after 48 hrs by DAPI staining-based assay
Inhibition of PARP in human HeLa cells assessed as induction of centrosomal clustering blockade by measuring increase in mitotic cells with multipolar spindles measured after 48 hrs by DAPI staining-based assay
[PMID: 27578247]
HeLa EC50
0.053 μM
Compound: 14f; AZ0108
Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
MCF7 EC50
123 nM
Compound: 14f; AZ0108
Inhibition of PARP in human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
[PMID: 26546219]
OCI-LY19 GI50
0.017 μM
Compound: 14f; AZ0108
Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
[PMID: 26546219]
Sf9 IC50
< 0.03 μM
Compound: 14f; AZ0108
Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
< 0.03 μM
Compound: 14f; AZ0108
Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
> 3 μM
Compound: 14f; AZ0108
Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
0.083 μM
Compound: 14f; AZ0108
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
Sf9 IC50
3.2 μM
Compound: 14f; AZ0108
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
[PMID: 26546219]
分子量

500.45

Formula

C24H20F4N6O2
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

AZ0108 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 *
= × ×

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:

AZ01081825345-52-5AZ 0108AZ-0108PARPpoly ADP ribose polymerasedeclusteringCentrosomeInhibitorinhibitorinhibit

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产品名称：
AZ0108
目录号：
HY-100847
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