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

LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 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

LD-110 Chemical Structure

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LD-110 Related Antibodies

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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  • References

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Description

LD-110 is a highly efficient and effective LSD1 PROTAC degrader (DC50 = 0.44 μM). LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis. LD-110 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), 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) 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) 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) can effectively inhibit the proliferation of ESCC KYSE-30 and EC9706 cells[1].
LD-110 (3-10 μM, 48 h) 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 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 μM, 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) 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

739.82

Formula

C42H41N7O6
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LD-110 Related Classifications

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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-110LD110LD 110PROTACsHistone DemethylaseApoptosisLSD1Lysine-Specific Demethylase 1PROTACProteolysis-Targeting ChimeraEsophageal Squamous Cell CarcinomaESCCH3K4me2Inhibitorinhibitorinhibit

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