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

LD-110 trihydrochloride 是一种高效的 LSD1 PROTAC 降解剂 (DC50 = 0.44 μM)。LD-110 trihydrochloride 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 trihydrochloride 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 trihydrochloride 可用于食管鳞状细胞癌的研究。
(粉色: LSD1 配体 (HY-178826)；蓝色: Cereblon 配体 (HY-14658)；黑色: 连接子)。

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LD-110 (trihydrochloride)

LD-110 (trihydrochloride) Chemical Structure

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LD-110 (trihydrochloride) 的其他形式现货产品:

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Other Forms of LD-110 (trihydrochloride):

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

体外研究
(In Vitro)

LD-110 (1-10 μM) trihydrochloride 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 (0.1-30 μM，6-72 小时) trihydrochloride 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 (72 小时) trihydrochloride 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) trihydrochloride 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) trihydrochloride 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 (trihydrochloride) 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: 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) trihydrochloride 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: 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

849.20

Formula

C42H44Cl3N7O6
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (117.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1776 mL 5.8879 mL 11.7758 mL
5 mM 0.2355 mL 1.1776 mL 2.3552 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

LD-110 (trihydrochloride) 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1776 mL 5.8879 mL 11.7758 mL 29.4395 mL
5 mM 0.2355 mL 1.1776 mL 2.3552 mL 5.8879 mL
10 mM 0.1178 mL 0.5888 mL 1.1776 mL 2.9439 mL
15 mM 0.0785 mL 0.3925 mL 0.7851 mL 1.9626 mL
20 mM 0.0589 mL 0.2944 mL 0.5888 mL 1.4720 mL
25 mM 0.0471 mL 0.2355 mL 0.4710 mL 1.1776 mL
30 mM 0.0393 mL 0.1963 mL 0.3925 mL 0.9813 mL
40 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7360 mL
50 mM 0.0236 mL 0.1178 mL 0.2355 mL 0.5888 mL
60 mM 0.0196 mL 0.0981 mL 0.1963 mL 0.4907 mL
80 mM 0.0147 mL 0.0736 mL 0.1472 mL 0.3680 mL
100 mM 0.0118 mL 0.0589 mL 0.1178 mL 0.2944 mL
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-110 (trihydrochloride)PROTACsHistone DemethylaseApoptosisLSD1Lysine-Specific Demethylase 1PROTACProteolysis-Targeting ChimeraEsophageal Squamous Cell CarcinomaESCCH3K4me2Inhibitorinhibitorinhibit

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