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

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.
(Pink: LSD1 ligand (HY-178826); Blue: Cereblon ligand (HY-14658); Black: linker).

For research use only. We do not sell to patients.

LD-110 trihydrochloride

LD-110 trihydrochloride Chemical Structure

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Other Forms of LD-110 trihydrochloride:

LD-110 trihydrochloride Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

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Description

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).

In Vitro

LD-110 (1-10 μM) trihydrochloride, with a linker containing four methylene groups, demonstrates good degradation activity, achieving degradation rates of 65, 70, and 84% against the LSD1 protein at concentrations of 1, 3, and 10 μM, respectively[1].
LD-110 (0.1-30 μM, 6-72 h) trihydrochloride effectively and dose-dependently degrades LSD1 protein, achieving near-complete depletion within 48-72 hours with DC50 values of 0.44, 1.18, and 1.24 μM in KYSE-150, KYSE-30, and EC9706 ESCC cells, respectively; this degradation is highly specific with minimal effect on CoREST/HDAC1/HDAC2 levels, and consequently leads to a potent 2 to 7-fold accumulation of H3K4me2[1].
LD-110 (72 h) trihydrochloride effectively suppresses the growth of ESCC cells with half-maximal inhibitory concentration (IC50) values of 3.94, 3.35, and 3.08 μM in KYSE-150, KYSE-30, and EC9706, respectively[1].
LD-110 (3-10 μM, 10-14 days) trihydrochloride can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM, 48 h) trihydrochloride dose-dependently induces both early-stage and late-stage apoptosis and causes cleavage of PARP and caspase-3 in KYSE-30 and EC9706 cells[1].

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

LD-110 trihydrochloride Related Antibodies

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.
In Vivo

LD-110 (30 mg/kg, 100 mg/kg, i.p., once daily for 24 days) trihydrochloride exhibits potent dose-dependent antitumor activity in the KYSE-150 xenograft mice model without causing significant toxicity[1].

MedChemExpress (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.
Molecular Weight

849.20

Formula

C42H44Cl3N7O6
Appearance

Solid

SMILES

O=C(NCCCCNC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)C4=CC=C(C5=NC=C(OCC6CCNCC6)C=C5C7=CC=C(C#N)C=C7)C=C4.Cl.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (117.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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LD-110 trihydrochloride Related Classifications

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 trihydrochloridePROTACsHistone DemethylaseApoptosisLSD1Lysine-Specific Demethylase 1PROTACProteolysis-Targeting ChimeraEsophageal Squamous Cell CarcinomaESCCH3K4me2Inhibitorinhibitorinhibit

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