Art. -Nr.: HY-183105

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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CAS. Nr.: 2133291-32-2
Formel: C₂₂H₃₂FN₃O₂
Molecular Weight:389.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

DC551040 Chemical Structure

CAS. Nr.: 2133291-32-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

LSD1

2.14 nM (IC₅₀)

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen :

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.

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	AUC_0-t	MRT_0-t	CL	F	V_ss	C_max	T_1/2	T_max
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.

Chemical Information

CAS. Nr. 2133291-32-2
Molecular Weight 389.51
Formel C₂₂H₃₂FN₃O₂
SMILES

FC1(CCN(C(OCC2CCNCC2)=O)CC1)CN[C@H](C3)[C@@H]3C4=CC=CC=C4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wang J, et al. Potent and selective LSD1 inhibitor DC551040 reveals a promising combination therapy for AML with insight into epigenetic dysregulation. Signal Transduct Target Ther. 2026;11(1):108. Published 2026 Mar 23. [Content Brief]

Calculators

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)}

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DC551040

Alle Histone Demethylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

DC551040 Related Classifications

HY-183105 Related Classifications