2. Epigenetics PROTAC Apoptosis
  3. PROTACs Apoptosis Histone Demethylase
  4. 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).

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

LD-110 triTFA

LD-110 triTFA Chemical Structure

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Other Forms of LD-110 triTFA:

LD-110 triTFA 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

  • Purity & Documentation

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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.

LD-110 triTFA 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: 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
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.

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