2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. LSD1-IN-25

LSD1-IN-25 (Compound 9j) 是一种有效的、选择性的、口服活性的 LSD1 抑制剂，其 IC50 为 46 nM (Ki = 30.3 nM)。LSD1-IN-25 诱导癌细胞凋亡 (apoptosis)。

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LSD1-IN-25 Chemical Structure

LSD1-IN-25 Chemical Structure

CAS No. : 2911585-60-7

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LSD1-IN-25 相关抗体

Top Publications Citing Use of Products

查看 Histone Demethylase 亚型特异性产品:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1-IN-25 (Compound 9j) is a potent, selective and orally active LSD1 inhibitor with an IC50 of 46 nM (Ki = 30.3 nM). LSD1-IN-25 induces cancer cell apoptosis[1].

IC50 & Target[1]

LSD1

46 nM (IC50)

LSD1

30.3 nM (Ki)

体外研究
(In Vitro)

LSD1-IN-25 (Compound 9j; 0-20 μM; 72 h) 抑制实体瘤细胞增殖[1]。
LSD1-IN-25 (1-4 μM; 24 h) 诱导细胞 H3K4me2 升高，抑制 H1650 细胞的 EMT 过程[1]。
LSD1-IN-25 (1-4 μM; 24 h) 诱导 H1650 细胞凋亡和 S 阻滞[1]。

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

LSD1-IN-25 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MGC-803, MGC-803LSD1-KO, SGC-7901, GES-1, MCF-7, H1650, A549, H460, PC-3 and EC-109
Concentration: 0-20 μM
Incubation Time: 72 h
Result: Antiproliferative activity of LSD1-IN-25 (Compound 9j) on solid tumor cell lines[1]
Cell line Origin IC50 (μM)
MGC-803 Gastric cancer 5.1 ± 0.7
MGC-803LSD1-KO Gastric cancer >20
SGC-7901 Gastric cancer 9.5 ± 2.1
GES-1 Normal gastric epithelial cell >20
MCF-7 Breast cancer 13.4 ± 2.4
H1650 Lung cancer 4.3 ± 0.9
A549 Lung cancer 7.9 ± 1.5
H460 Lung cancer 13.6 ± 4.2
PC-3 Prostate cancer 7.5 ± 1.1
EC-109 Esophageal cancer 15.2 ± 2.9

Western Blot Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: Induced the elevation of cellular H3K4me2. Elevated the expression of the epithelial marker E-cadherin, decreased the expression of the mesenchymal markers such as N-cadherin, slug and vimentin.

Apoptosis Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: Induced an evident increase in cell apoptosis, with the percentage of apoptotic cells of 43.9% (1 μM), 44.5% (2 μM) and 45.7% (4 μM), respectively, in comparison with 12.7% of the control.

Cell Cycle Analysis[1]

Cell Line: H1650 cell
Concentration: 1, 2 and 4 μM
Incubation Time: 24 h
Result: The percentage of cells in S phase were 29.97% 33.32%, 39.81%, 43.26% at concentrations of 0, 1 μM, 2 μM, 4 μM, respectively.
体内研究
(In Vivo)

LSD1-IN-25 (Compound 9j; 10 and 20 mg/kg; oral; once daily for 21 days) 在 H1650 细胞的小鼠异种移植模型中显示出抗肿瘤活性[1]。

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

Animal Model: Nude mice, xenograft model of H1650 cells[1]
Dosage: 10 mg/kg and 20 mg/kg
Administration: Oral, once daily for 21 days
Result: Presented a remarkable reduction of average tumor weight by 41.5% and 64.0% at dosages of 10 and 20 mg/kg, respectively. Evidently prolonged the mice's survival.
分子量

617.16

Formula

C32H33ClN6O3S
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

LSD1-IN-25 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:

LSD1-IN-252911585-60-7Histone DemethylaseApoptosisH3K4me2EMTH1650MGC-803SGC-7901GES-1MCF-7A549H460PC-3EC-109Inhibitorinhibitorinhibit

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目录号：
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