2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Demethylase Apoptosis
  4. LD-110

LD-110 是一种高效的 PROTAC 降解剂，靶向 LSD1 (DC50 = 0.44 μM)。LD-110 以泛素-蛋白酶体依赖的方式促进 LSD1 降解并提高 H3K4 二甲基化水平。LD-110 通过诱导细胞凋亡 (apoptosis) 抑制多种食管鳞状细胞癌 (ESCC) 细胞系的生长和存活。LD-110 可用于食管鳞状细胞癌的研究。红色：LSD1 配体 (HY-178826)；蓝色：E3 连接酶 CRBN 配体 (HY-14658) ；黑色：连接子 (HY-N2578)。

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LD-110

LD-110 Chemical Structure

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Customer Review

LD-110 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Demethylase 亚型特异性产品:

查看所有亚型
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

LD-110 is a highly efficient and effective PROTAC degrader targeting LSD1 (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 can be used for the study of esophagus squamous cancer. Red: LSD1 ligand (HY-178826); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-N2578)[1].

体外研究
(In Vitro)

LD-110 (1-10 μM) 具有含四个亚甲基的连接基团，表现出良好的降解活性，在浓度分别为 1、3 和 10 μM 时，对 LSD1 蛋白的降解率分别为 65%、70% 和 84%[1]。
LD-110 (0.39-12.5 μM) 对 LSD1 具有很强的结合亲和力 (Kd = 6.2 μM)[1]。
LD-110 (0.1-30 μM，6-72 小时) 能有效且剂量依赖性地降解 LSD1 蛋白，在 48-72 小时内几乎完全降解，在 KYSE-150、KYSE-30 和 EC9706 食管鳞状细胞癌 (ESCC) 细胞中的 DC50 值分别为 0.44、1.18 和 1.24 μM。这种降解具有高度特异性，对CoREST/HDAC1/HDAC2水平的影响极小，因此可导致H3K4me2显著积累2至7倍[1]。
LD-110 (3 μM，42 小时) 在KYSE-150食管鳞状细胞癌细胞中，诱导的LSD1降解可被LSD1抑制剂 (LI-1)、cereblon E3配体 (Thalidomide) 、NAE抑制剂 (MLN4924) 和蛋白酶体抑制剂 (MG132) 有效阻断[1]。
LD-110 (72 小时) 可有效抑制食管鳞状细胞癌 (ESCC) 细胞的生长，在KYSE-150、KYSE-30和EC9706细胞中的半数抑制浓度 (IC50) 值分别为3.94、3.35和3.08 μM[1]。
LD-110 (3-10 μM，10-14 天) 可有效抑制食管鳞癌细胞系 KYSE-30 和 EC9706 的增殖[1]。
LD-110 (3-10 μM，48 小时) 呈剂量依赖性地诱导 KYSE-30 和 EC9706 细胞的早期和晚期凋亡，并导致 PARP 和 caspase-3 的裂解[1]。

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

LD-110 相关抗体:

Western Blot Analysis[1]

Cell Line: KYSE-150, KYSE-30, and EC9706 ESCC cells
Concentration: 10 μM
Incubation Time: 6 h, 12 h, 24 h, 48 h, 72 h
Result: Effectively reduced the LSD1 protein levels after 24-48 h treatment, achieving near-complete depletion of LSD1 at 48−72 h, consequently causing the accumulation of H3K4me2.

Western Blot Analysis[1]

Cell Line: KYSE-150, KYSE-30, and EC9706 ESCC cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 48 h
Result: Caused the dose-dependent degradation of LSD1 with DC50 values of 0.44, 1.18, and 1.24 μM in the KYSE-150, KYSE-30, and EC9706, respectively.
Caused accumulation of H3K4me2, which also occurred in a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: KYSE-30, EC9706 ESCC cells
Concentration: 3 μM, 10 μM
Incubation Time: 10-14 days
Result: Significantly reduced the number of clones formed in ESCC KYSE-30 and EC9706 cells in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: KYSE-30 cells, EC9706 ESCC cells
Concentration: 3 μM, 10 μM
Incubation Time: 48 h
Result: Induced both early-stage and late-stage apoptosis in a dose-dependent manner.
体内研究
(In Vivo)

LD-110 (30 mg/kg，100 mg/kg，腹腔注射，每日一次，持续 24 天) 在 KYSE-150 异种移植小鼠模型中表现出强效的剂量依赖性抗肿瘤活性，且未引起明显的毒性[1]。

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

Animal Model: 5 × 106 KYSE-150 cells were injected into both flanks of the male BALB/c nude mice[1].
Dosage: 30 mg/kg, 100 mg/kg
Administration: I.p., once daily for 24 days
Result: Dose-dependently inhibited the tumor growth at both 30 and 100 mg/ kg via intraperitoneal administration without any effect on body weight.
At a dose of 100 mg/kg also effectively reduced the levels of LSD1 protein in the tumor tissues harvested and collected at the end of the study without causing any morphological changes of major organs, including heart, liver, spleen, lung, and kidney.
分子量

739.82

Formula

C42H41N7O6
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

LD-110 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

LD-110LD110LD 110PROTACsHistone DemethylaseApoptosisLSD1Lysine-Specific Demethylase 1PROTACProteolysis-Targeting ChimeraEsophageal Squamous Cell CarcinomaESCCH3K4me2Inhibitorinhibitorinhibit

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