2. Metabolic Enzyme/Protease
  3. Endogenous Metabolite
  4. Largazole

Largazole ((+)-Largazole)是一种强效且选择性的组蛋白去乙酰化酶（HDAC）抑制剂，具有抗增殖活性。Largazole能够调节基因表达，影响细胞生长和分化。Largazole还显示出在抗肿瘤抑制中具有潜在的应用价值。

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Largazole

Largazole Chemical Structure

CAS No. : 1009815-87-5

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Largazole 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

Largazole ((+)-Largazole) is a potent and selective histone deacetylase (HDAC) inhibitor with antiproliferative activity. Largazole is able to modulate gene expression and affect cell growth and differentiation. Largazole has also shown potential application value in anti-tumor suppression[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
16HBE14o- IC50
> 10 μM
Compound: 1
Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay
Cytotoxicity against human 16HBE cells after 48 hrs by CCK-8 assay
[PMID: 24900585]
A549 GI50
1.46 μM
Compound: 158a
Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
[PMID: 31926469]
A549 IC50
0.077 μM
Compound: 1
Cytotoxicity against human A549 cells after 48 hrs by CCK-8 assay
Cytotoxicity against human A549 cells after 48 hrs by CCK-8 assay
[PMID: 24900585]
A549 IC50
0.46 μM
Compound: Largazole
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31505452]
DU-145 GI50
11 nM
Compound: 7
Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay
[PMID: 26331334]
HCT-116 GI50
0.065 μM
Compound: 5
Growth inhibition of human HCT-116 cells incubated for 96 hrs by MTS assay
Growth inhibition of human HCT-116 cells incubated for 96 hrs by MTS assay
[PMID: 27809521]
HCT-116 GI50
10 nM
Compound: 1
Growth inhibition of human HCT116 cells after 96 hrs by MTS assay
Growth inhibition of human HCT116 cells after 96 hrs by MTS assay
[PMID: 21936551]
HCT-116 IC50
0.044 μM
Compound: Largazole
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31505452]
HCT-116 IC50
0.39 μM
Compound: 158a
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability
[PMID: 31926469]
HCT-116 IC50
18 nM
Compound: 3
Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against human HIF1alpha and HIF2alpha deficit HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
[PMID: 27380142]
HCT-116 IC50
20 nM
Compound: 5
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 28416100]
HCT-116 IC50
3.7 nM
Compound: 3
Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against oncogenic KRAS knockout human HCT116 cells expressing wild type KRAS assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
[PMID: 27380142]
HCT-116 IC50
6.41 nM
Compound: 3
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability measured after 48 hrs by ATPlite 1step luminescence assay
[PMID: 27380142]
HEK293 GI50
> 100 μM
Compound: 158a
Antiproliferative activity against human HEK293 cells
Antiproliferative activity against human HEK293 cells
[PMID: 31926469]
MDA-MB-231 IC50
1.6 nM
Compound: 5
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 28416100]
MDA-MB-231 IC50
4.75 μM
Compound: Largazole
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31505452]
MOLT-4 GI50
16.2 nM
Compound: 7
Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay
[PMID: 26331334]
NCI-H1975 IC50
0.083 μM
Compound: 1
Cytotoxicity against human NCI-H1975 cells after 48 hrs by CCK-8 assay
Cytotoxicity against human NCI-H1975 cells after 48 hrs by CCK-8 assay
[PMID: 24900585]
NCI-H460 IC50
0.12 μM
Compound: 1
Cytotoxicity against human NCI-H460 cells after 48 hrs by CCK-8 assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by CCK-8 assay
[PMID: 24900585]
SK-OV-3 IC50
0.25 μM
Compound: Largazole
Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 31505452]
Sf9 IC50
120 nM
Compound: Largazole
Inhibition of full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 240 mins by fluorescence based assay
Inhibition of full length C-terminal His-tagged human HDAC8 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 240 mins by fluorescence based assay
[PMID: 31505452]
Sf9 IC50
1520 nM
Compound: Largazole
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
[PMID: 31505452]
Sf9 IC50
2002 nM
Compound: Largazole
Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
Inhibition of human recombinant full length C-terminal His-tagged HDAC3 (1 to 428 residues)/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
[PMID: 31505452]
Sf9 IC50
228 nM
Compound: Largazole
Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
Inhibition of recombinant full length C-terminal FLAG/His-tagged human HDAC1 expressed in baculovirus infected Sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins by fluorescence based assay
[PMID: 31505452]
U-937 GI50
16.8 nM
Compound: 7
Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay
[PMID: 26331334]
WI-38 GI50
82.5 nM
Compound: 7
Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay
[PMID: 26331334]
分子量

622.86

Formula

C29H42N4O5S3
CAS 号
结构分类
初始来源

Floridian Marine Cyanobacterium Symploca sp.
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

Largazole 相关分类

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  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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× = ×
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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:

Largazole1009815-87-5(+)-LargazoleEndogenous MetaboliteInhibitorinhibitorinhibit

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