2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. DC551040

DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia.

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DC551040

DC551040 Chemical Structure

CAS No. : 2133291-32-2

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Description

DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

LSD1

2.14 nM (IC50)

In Vitro

DC551040 (1 h) potently inhibits recombinant human LSD1 enzymatic activity with an IC50 of 2.14 nM[1].
DC551040 exhibits excellent selectivity for recombinant human LSD1 over recombinant human LSD2, MAO-A, and MAO-B[1].
DC551040 (300 nM; 1 h pre-incubation) irreversibly inhibits recombinant human LSD1, as enzyme activity does not recover post-dilution[1].
DC551040 (50-250 nM; 24 h) disrupts the LSD1-GFI1B-CoREST complex in MV-4-11 AML cells[1].
DC551040 (7 days) potently inhibits proliferation of MV-4-11, Kasumi-1, and HL-60 AML cell lines with IC50 values of 79.51 nM, 25.77 nM, and 40.35 nM respectively, while showing weak activity against non-AML blood cancer cell lines[1].
DC551040 (7 days) inhibits proliferation of AML patient-derived cells with IC50 values ranging from 0.68 nM to 4157 nM across four samples[1].
DC551040 (0.5-4 μM; 72 h) induces dose-dependent apoptosis in MV-4-11 AML cells, with apoptosis rates of 7.16%, 7.78%, and 10.76%, respectively[1].
DC551040 (24 h) induces differentiation in MV-4-11 AML cells, as shown by increased CD86 expression and characteristic morphological changes[1].
DC551040 (0.1-2 μM; 1-7 days) dose-dependently increases H3K4me2 levels in MV-4-11 AML cells after 1, 3, 5, or 7 days of treatment[1].
DC551040 has low toxicity to normal peripheral blood mononuclear cells, with an IC50 greater than 10 μM[1].
DC551040 (1-5 μM; 12 h) upregulates STAT3 phosphorylation in MV-4-11 AML cells after 12 h treatment at 1 μM or 5 μM[1].
DC551040 (0.3-3 μM; 48 h) dose-dependently upregulates IL6, MYC, CCL5, and VEGFA mRNA expression in MOLM-13, MV-4-11, and HL-60 AML cells after 48 h treatment[1].
DC551040 (0.23-5000 nM; 10 days) and HHT (HY-14944) act synergistically to inhibit proliferation of MOLM-13, MV-4-11, HL-60, Kasumi-1 AML cell lines, and AML PDC (32#) cells, with strong synergy scores (ZIP >10, Bliss score 21.25) after 10 days of combined treatment[1].
DC551040 (0.5 μM; 24 h) plus HHT significantly increases Caspase 3/7 activity in MV-4-11 AML cells after 24 h treatment[1].

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

DC551040 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 50 nM; 250 nM
Incubation Time: 24 h
Result: Disrupted the association between LSD1 and GFI1B, as shown by reduced co-immunoprecipitation of LSD1 with GFI1B.

Apoptosis Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 0.5 μM; 2 μM; 4 μM
Incubation Time: 72 h
Result: Induced apoptosis in a dose-dependent manner: 7.16% apoptosis at 0.5 μM, 7.78% at 2 μM, and 10.76% at 4 μM, compared to 4.07% in the DMSO control.

Western Blot Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 0.1 μM; 0.5 μM; 2 μM
Incubation Time: 1 day, 3 days, 5 days, 7 days
Result: Increased H3K4me2 levels in a dose-dependent manner across all time points: at 1 day, relative ratios were 1.01 at 0.1 μM, 1.25 at 0.5 μM, 1.25 at 2 μM; at 3 days, 1.20 at 0.1 μM, 1.67 at 0.5 μM, 1.51 at 2 μM; at 5 days, 1.22 at 0.1 μM, 1.52 at 0.5 μM, 1.53 at 2 μM; at 7 days, 1.11 at 0.1 μM, 1.25 at 0.5 μM, 1.35 at 2 μM.

Western Blot Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 1 μM; 5 μM
Incubation Time: 12 h
Result: Upregulated phosphorylation of STAT3.

Real Time qPCR[1]

Cell Line: MOLM-13, MV-4-11, HL-60 AML cells
Concentration: 0.3 μM; 1 μM; 3 μM
Incubation Time: 48 h
Result: Dose-dependently upregulated IL6 mRNA expression in MOLM-13, MV-4-11, and HL-60 cells.
Dose-dependently upregulated MYC, CCL5, and VEGFA mRNA expression in MOLM-13 cells.

Apoptosis Analysis[1]

Cell Line: MV-4-11 AML cells
Concentration: 0.5 μM; 0.5 μM plus 5 nM HHT
Incubation Time: 24 h
Result: Significantly increased Caspase 3/7 activity (to ~3-fold) compared to either monotherapy (both ~1.5-fold) or DMSO control (~1-fold).
Parmacokinetics
Species Dose Route AUC0-t MRT0-t CL F Vss Cmax T1/2 Tmax
Mice[1] 20 mg/kg p.o. 2566 ng·h/mL / / 74.4 % 18.6 L/kg 1257 ng/mL 7.96 h 0.5 h
Mice[1] 10 mg/kg i.v. 1712 ng·h/mL 3.18 h 97.4 mL/min/kg / / / / /
Rat[1] 20 mg/kg p.o. 5777 ng·h/mL / / 92.0 % 14.0 L/kg 851 ng/mL 3.34 h 3 h
Rat[1] 10 mg/kg i.v. 3133 ng·h/mL 4.37 h 53.2 mL/min/kg / / / / /
Dog[1] 5 mg/kg p.o. 10940 ng·h/mL / / 78.6 % 6.76 L/kg 850 ng/mL 10.5 h 1.2 h
Dog[1] 2 mg/kg i.v. 10940 ng·h/mL 6258 h 19.5 mL/min/kg / / / / /
In Vivo

DC551040 (0.5-2 mg/kg; p.o.; daily; 17 days) exhibits dose-dependent antitumor activity in Kasumi-1 xenograft mice, achieving a maximum TGI of 86.99% at 2 mg/kg daily oral dosing[1].
DC551040 (5-10 mg/kg; p.o.; daily; 22 days) exerts dose-dependent antitumor activity in MV-4-11 xenograft mice, achieving a TGI of 61.23% at 10 mg/kg daily oral dosing, and induces dose-dependent upregulation of the CD86 differentiation biomarker[1].
DC551040 (0.5-4 mg/kg; p.o.; daily; 21 days) dose-dependently extends survival in mice with disseminated MV-4-11 AML[1].
DC551040 (1 mg/kg; p.o.; daily; 28 days) synergizes with HHT to significantly extend survival in mice with disseminated MV-4-11 AML[1].
DC551040 (2 mg/kg; p.o.; daily; 21 days) reduces residual leukemia burden in AML patient-derived xenograft mice, and synergizes with HHT to enhance this effect[1].
DC551040 (2 mg/kg; p.o.; daily; up to 21 days) induces dynamic activation of immune and inflammatory pathways, alongside time-dependent metabolic reprogramming, in MV-4-11 xenograft tumors[1].

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

Animal Model: Nu/Nu nude mice (subcutaneously inoculated in the right flank with 5 × 106 Kasumi-1 cells for a subcutaneous xenograft model)[1]
Dosage: 0.5 mg/kg; 1 mg/kg; 2 mg/kg
Administration: p.o.; daily; 17 days
Result: Demonstrated dose-dependent tumor suppressive activity, with corresponding tumor growth inhibition (TGI) rates of 48.82%, 60.81%, and 86.99%, respectively.
Exhibited superior antitumor effect at 2 mg/kg compared to GSK2879552 (HY-18632) at 2 mg/kg.
Animal Model: Nu/Nu nude mice (subcutaneously inoculated in the right flank with 5 × 106 MV-4-11 cells for a subcutaneous xenograft model)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: p.o.; daily; 22 days
Result: Demonstrated dose-dependent tumor suppressive activity, with TGI rates of 41.08% and 61.23%, respectively.
Showed significantly better tumor inhibitory effect at 10 mg/kg compared to GSK2879552 at 10 mg/kg .
Caused dose-dependent upregulation of CD86 positivity in tumor tissues, with higher CD86 expression observed at 10 mg/kg compared to 5 mg/kg.
Animal Model: B-NDG mice (received tail
vein injection of 1 × 107 MV-4-11 cells for intravenous engraft-
ment)[1]
Dosage: 0.5 mg/kg; 2 mg/kg; 4 mg/kg
Administration: p.o.; daily; 21 days
Result: Demonstrated dose-dependent improvement in mouse survival, with longer survival observed at higher doses compared to vehicle control.
Animal Model: B-NDG mice (received tail
vein injection of 1 × 107 MV-4-11 cells for intravenous engraft-
ment)[1]
Dosage: 1 mg/kg
Administration: p.o.; daily; 28 days
Result: Combination treatment with homoharringtonine (HHT, 0.5 mg/kg) significantly extended median mouse survival to 57.5 days, compared to 47.5 days for monotherapy and 48.5 days for HHT monotherapy.
Animal Model: B-NDG mice (received tail
vein injection of 1 × 107 primary AML cells for intravenous engraft-
ment)[1]
Dosage: 2 mg/kg
Administration: p.o.; daily; 21 days
Result: Significantly reduced the proportion of human CD33+ cells in mouse bone marrow compared to vehicle control.
Combination treatment with HHT (0.5 mg/kg) produced a further significant reduction in CD33+ cells, demonstrating a synergistic effect.
Animal Model: Nu/Nu nude mice (subcutaneously inoculated in the right flank with 5 × 106 MV-4-11 cells for a subcutaneous xenograft model)[1]
Dosage: 2 mg/kg
Administration: p.o.; daily; up to 21 days
Result: Induced dynamic changes in protein and gene expression: 233, 276, and 256 proteins were significantly changed at 3, 7, and 21 days, respectively (|log2(fold change)| > 0.585 and p < 0.05).
Activated immune and inflammation-related pathways (including IL6-JAK-STAT3, IL2-STAT5, interferon-γ response) across all time points.
Caused time-dependent alterations in metabolic pathways: oxidative phosphorylation was weakened at 21 days, carbon metabolism and glycolysis/gluconeogenesis were enhanced at 21 days, fatty acid metabolism decreased at 3 days then increased at 7 and 21 days.
Molecular Weight

389.51

Formula

C22H32FN3O2
CAS No.
SMILES

FC1(CCN(C(OCC2CCNCC2)=O)CC1)CN[C@H](C3)[C@@H]3C4=CC=CC=C4
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Purity & Documentation
References
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DC551040 Related Classifications

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    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:

DC5510402133291-32-2DC 551040DC-551040Histone DemethylaseApoptosisKasumi-1LSD2AMLacute myeloid leukemiaHL-60MV-4-11MAO-Alysine demethylase 1MAO-BLSD1Inhibitorinhibitorinhibit

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