LD-110 triTFA

Cat. No.: HY-178825A Purity: 99.56%: Data Sheet
COA

SDS
Handling Instructions
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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).

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

LD-110 triTFA Chemical Structure

Size		Stock
5 mg		Check price and availability
10 mg		Check price and availability
25 mg		Check price and availability

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of LD-110 triTFA:

LD-110 Get quote
LD-110 trihydrochloride Get quote

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•Related Screening Libraries:

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View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Demethylase Isoform Specific Products:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

Biological Activity
Purity & Documentation
References
Customer Review

Description

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).

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.

Molecular Weight

1081.89

Formula

C₄₈H₄₄F₉N₇O₁₂

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.56%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (245 KB) HNMR (109 KB) RP-HPLC (135 KB) LCMS (90 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

LD-110 triTFA 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 triTFAPROTACsApoptosisHistone DemethylaseInhibitorinhibitorinhibit

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