Art. -Nr.: HY-178825A

LD-110 triTFA

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

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.56%
Formel: C₄₈H₄₄F₉N₇O₁₂
Molecular Weight:1081.89

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LD-110 triTFA Chemical Structure

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

In Vitro

LD-110 (1-10 μM) triTFA, 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) triTFA 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) triTFA 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) triTFA can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells^[1].
LD-110 (3-10 μM, 48 h) triTFA 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.

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, 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) triTFA 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.

Chemical Information

Appearance Solid
Molecular Weight 1081.89
Formel C₄₈H₄₄F₉N₇O₁₂
Color Light yellow to yellow
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.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O.OC(C(F)(F)F)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (92.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9243 mL

4.6215 mL

9.2431 mL

5 mM

0.1849 mL

0.9243 mL

1.8486 mL

10 mM

0.0924 mL

0.4622 mL

0.9243 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhuo J, et al. Discovery of LD-110 as an Effective LSD1 PROTAC Degrader for the Treatment of Esophagus Squamous Cancer. J Med Chem. 2025 Oct 23;68(20):21860-21877. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	0.9243 mL	4.6215 mL	9.2431 mL	23.1077 mL
	5 mM	0.1849 mL	0.9243 mL	1.8486 mL	4.6215 mL
	10 mM	0.0924 mL	0.4622 mL	0.9243 mL	2.3108 mL
	15 mM	0.0616 mL	0.3081 mL	0.6162 mL	1.5405 mL
	20 mM	0.0462 mL	0.2311 mL	0.4622 mL	1.1554 mL
	25 mM	0.0370 mL	0.1849 mL	0.3697 mL	0.9243 mL
	30 mM	0.0308 mL	0.1541 mL	0.3081 mL	0.7703 mL
	40 mM	0.0231 mL	0.1155 mL	0.2311 mL	0.5777 mL
	50 mM	0.0185 mL	0.0924 mL	0.1849 mL	0.4622 mL
	60 mM	0.0154 mL	0.0770 mL	0.1541 mL	0.3851 mL
	80 mM	0.0116 mL	0.0578 mL	0.1155 mL	0.2888 mL

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LD-110 triTFA

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

PROTAC Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LD-110 triTFA

Apoptosis Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Cancer Metabolism Compound Library

PROTAC Library

Cell Death Library

Bioactive Compound Library Max

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LD-110 triTFA Related Classifications

HY-178825A Related Classifications