2. Epigenetics Immunology/Inflammation Apoptosis
  3. Histone Demethylase CD44 Apoptosis
  4. LSD1-IN-48

LSD1-IN-48 是一种反苯环丙胺-嘧啶衍生物，同时也是高选择性 LSD1 抑制剂，对人源靶点的 IC50 为 7.87 nM。LSD1-IN-48 可提高 H3K4me1/2 组蛋白甲基化水平。LSD1-IN-48 可诱导细胞凋亡 (apoptosis)，上调 CD86，下调 SOX2 和 CD44，并抑制癌细胞增殖。LSD1-IN-48 可用于急性髓系白血病的相关研究。

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LSD1-IN-48

LSD1-IN-48 Chemical Structure

CAS No. : 3104325-26-7

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LSD1-IN-48 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 KDM7

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

LSD1

7.87 nM (IC50)

体外研究
(In Vitro)

LSD1-IN-48 (7a) 可强效抑制重组 LSD1，其 IC50 为 7.87 nM，且对 LSD1 的选择性分别比对 MAO-A 和 MAO-B 高出 127 倍和 1270 倍[1]。
LSD1-IN-48 可抑制 MV-4-11、HL-60 和 THP-1 急性髓系白血病细胞的增殖，其 IC50 值分别为 0.36 μM、0.48 μM 和 1.12 μM[1]。
LSD1-IN-48 (10-100 μM) 可直接结合从 MV-4-11 细胞中提取的 LSD1，并以剂量依赖的方式保护该蛋白免受碱性蛋白酶水解[1]。
LSD1-IN-48 在人肝微粒体中表现出体外代谢稳定性，半衰期为 7.26 min，固有清除率为 172 mL/min/kg[1]。
LSD1-IN-48 (0.5-2 μM; 2 days) 可呈剂量依赖性地提升 MV-4-11 细胞中 H3K4me1 和 H3K4me2 的组蛋白甲基化水平[1]。
LSD1-IN-48 (0.5-2 μM; 2 days) 可呈剂量依赖性诱导 MV-4-11 细胞发生凋亡，在 2 μM 浓度下可将总凋亡率提升至 33.19%，并激活 caspase 介导的凋亡通路[1]。
LSD1-IN-48 (0.5-2 μM; 4 days) 可剂量依赖性地上调 MV-4-11 细胞中的分化标志物 CD86，在 2 μM 浓度下可使其表达量升高 19.18%[1]。
LSD1-IN-48 (0.5-2 μM; 96 h) 可剂量依赖性地降低 MV-4-11 细胞中干细胞相关蛋白 SOX2 和 CD44 的水平，从而削弱癌症干细胞特性[1]。

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

LSD1-IN-48 相关抗体:

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 2 days
Result: Dose-dependently increased the levels of H3K4me1 and H3K4me2; at 2 μM, H3K4me1 levels increased to ~4-fold and H3K4me2 levels increased to ~1.5-fold relative to the control.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 2 days
Result: Dose-dependently increased the total apoptosis rate; at 2 μM, the total apoptosis rate increased from 6.45% to 33.19%.
Dose-dependently increased the levels of cleaved caspase-3, cleaved caspase-7, and cleaved PARP.

Cell Differentiation Assay[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 4 days
Result: Dose-dependently increased CD86 expression; at 2 μM, CD86 expression increased by 19.18% relative to the control.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 96 h
Result: Dose-dependently reduced the protein levels of SOX2 and CD44; at 2 μM, SOX2 levels were reduced to ~0.15-fold and CD44 levels were reduced to ~0.55-fold relative to the control.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-∞ AUC0-t T1/2 Cmax CL
Rat[1] 1 mg/kg i.v. 26.0 μg/L·h 22.9 μg/L·h 0.863 h 57.2 μg/L 38794 mL/h/kg
分子量

436.44

Formula

C18H18F2N6O3S
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-48 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)

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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:

LSD1-IN-483104325-26-7Histone DemethylaseCD44ApoptosisIn (Lu)-related protein p80Pgp-1/Ly-24ECMRIIIHUTCH-1H3K4me2CD86apoptosisH3K4me1LSD1MAO-Aacute myeloid leukemiaMAO-BSOX2Inhibitorinhibitorinhibit

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