Home Epigenetics DNA Methyltransferase inhibitor - Apoptosis related activator - Nucleoside Analog/Antimetabolite inhibitor Decitabine For research use only.

Decitabine

Synonyms: Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716

Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.

Decitabine Chemical Structure

Decitabine Chemical Structure

CAS No. 2353-33-5

Purity & Quality Control

Decitabine Related Products

Signaling Pathway

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Eca109 Function Assay 0.5 μM 24 h water modulates the gene expression of MAGE-A members 25123082
Eca109 Growth Inhibition Assay 0.5/2.5/5 μM 24/48/72 h water inhibits cell growth in both dose- and time- dependent manner 25123082
Eca109 Function Assay 0.5 μM 6/12/24 h water inhibits cell migration  25123082
Eca109 Function Assay 0.5 μM 24 h water inhibits cell invasion 25123082
Eca109 Growth Inhibition Assay 0.5 μM 24 h water induces G2/M arrest in the cell cycle 25123082
Eca109 Function Assay 0.5/1 μM 24 h water decreases expression of NF-κB2 and MMP2 25123082
SW1116  Growth Inhibition Assay 0.5/1/2/5 μM 48 h DMSO enhances the Gefitinib induced cell inhibition 24874286
LOVO Growth Inhibition Assay 0.5/1/2/5 μM 48 h DMSO enhances the Gefitinib induced cell inhibition 24874286
SW1116  Function Assay 10 μM 48 h DMSO increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib 24874286
LOVO Function Assay 10 μM 48 h DMSO increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib 24874286
SW1116  Apoptosis Assay 10 μM 48 h DMSO enhances Gefitinib-induced apoptosis 24874286
LOVO Apoptosis Assay 10 μM 48 h DMSO enhances Gefitinib-induced apoptosis 24874286
RPMI-8226 Apoptosis Assay 1/2 μM 48/72/96 h DMSO induces cell apoptosis 24833108
OPM-2  Apoptosis Assay 1/2 μM 72/96/120 h DMSO induces cell apoptosis 24833108
JJN3  Apoptosis Assay 0.5/1 μM 24/48 h DMSO induces cell apoptosis 24833108
NCI-H929  Apoptosis Assay 1/2 μM 72/96/120 h DMSO induces cell apoptosis 24833108
RPMI-8226 Growth Inhibition Assay 1/2 μM 24/48/72 h DMSO affects cell cycle progression negatively 24833108
OPM-2  Growth Inhibition Assay 1/2 μM 24/48/72 h DMSO affects cell cycle progression negatively 24833108
JJN3  Growth Inhibition Assay 0.5/1 μM 24/48/72 h DMSO affects cell cycle progression negatively 24833108
NCI-H929  Growth Inhibition Assay 1/2 μM 24/48/72 h DMSO affects cell cycle progression negatively 24833108
HeLa Kinase Assay Ki=1000–5000 μM for hENT1 24780098
HeLa Kinase Assay Ki=5.6 ± 0.5 μM for hENT2 24780098
HeLa Kinase Assay Ki=21.6 ± 3.0 μM for hCNT1 24780098
HeLa Kinase Assay Ki=14.4 ± 4.6 μM for hCNT3 24780098
NB4 Function Assay 2.5/5/7.5/10 μM 24 h DMSO increasea the expression of precursor miR-125a 24484870
CD4+ CD25− T  Function Assay 1/5 μM reduceS global DNA methylation 24476360
BV-173 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h  PBS induces cell apoptosis in both dose- and time- dependent manner 24423613
ML-1 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h  PBS induces cell apoptosis in both dose- and time- dependent manner 24423613
HL-60 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h  PBS induces cell apoptosis in both dose- and time- dependent manner 24423613
KG-1a Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h  PBS induces cell apoptosis in both dose- and time- dependent manner 24423613
BV-173 Function Assay 250/500nM 48 h  PBS induces delayed and sustained ROS increase 24423613
CEM Function Assay 250/500nM 48 h  PBS induces delayed and sustained ROS increase 24423613
HL-60 Function Assay 250/500nM 48 h  PBS induces delayed and sustained ROS increase 24423613
ML-1 Function Assay 250/500nM 48 h  PBS induces delayed and sustained ROS increase 24423613
DLD-1 Function Assay 250/500nM 48 h  PBS do not induces delayed and sustained ROS increase 24423613
HCT-116 Function Assay 250/500nM 48 h  PBS do not induces delayed and sustained ROS increase 24423613
U937-A/E-9/14/18  Apoptosis Assay 0.01/0.1/1/10 μM 48 h induces cell apoptosis in a dose-dependent manner 24300456
HT29 Growth Inhibition Assay 72 h IC50=1400±179 μM 24172061
SW48 Growth Inhibition Assay 72 h IC50=15.2±6.2 μM 24172061
HCT116 Growth Inhibition Assay 72 h IC50=1.7±0.4 μM 24172061
HepG2 Function Assay 0.5/1 μM 24 h DMSO up-regulated the relative OCTN2 mRNA and protein expression 24146874
LS174T Function Assay 0.5/1 μM 24 h DMSO lead to an increase of OCTN2 levels 24146874
HepG2 Apoptosis Assay 1/10/100 μM 7 d DMSO induces cell apoptosis in a dose-dependent manner 24146874
LS174T Apoptosis Assay 1/10/100 μM 7 d DMSO induces cell apoptosis in a dose-dependent manner 24146874
QBC-939 Apoptosis Assay 1/10/100 μM 7 d DMSO induces cell apoptosis in a dose-dependent manner 24146874
U251 Apoptosis Assay 1/10/100 μM 7 d DMSO induces cell apoptosis in a dose-dependent manner 24146874
HL-60 Growth Inhibition Assay 1 μM 48 h increases G2-phase cell fraction 24000324
MDA‑MB‑453 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
HCC1569 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
BT‑474 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
AGS Apoptosis Assay 5/10/20/50 μM 48 h  DMSO inhibits the cell viability  23582784
A549 Apoptosis Assay 5/10/20/50 μM 48 h  DMSO inhibits the cell viability  23582784
AGS  Growth Inhibition Assay 5/10/20/50 μM 48 h  DMSO induces G2/M phase arrest  23582784
Kasumi-1 Apoptosis Assay 0.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
OCI-AML3 Apoptosis Assay 2.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
MV4-11 Apoptosis Assay 2.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
NK  Cytotoxity Assay 0.02-20 μM 5 d decreases the cytolytic activity of NK cells at intermediate concentrations resulting in a U-shaped dose–response curve 23328088
NK  Apoptosis Assay 0.02-20 μM 5 d decrease NK cell proliferation and viability as the concentration increased 23328088
NK  Function Assay 0.01-20 μM 5 d causes hypomethylation of NK cells in a dose–response 23328088
MOLT4/DNR Function Assay 5 μM 4 d reduces ABCB1 mRNA expression 23060570
Jurkat/DOX Function Assay 5 μM 4 d reduces ABCB1 mRNA expression 23060570
MOLT4/DNR Growth Inhibition Assay 5 μM 4 d reduces the IC50 value for daunorubicin sensitivity 23060570
Jurkat/DOX Growth Inhibition Assay 5 μM 4 d reduces the IC50 value for daunorubicin sensitivity 23060570
ccRCC  Apoptosis Assay 0.01-10μM 72 h DMSO has minimal effect on cell proliferation 22826467
TNBC  Apoptosis Assay 0.01-10μM 72 h DMSO has minimal effect on cell proliferation 22826467
A498 Apoptosis Assay 0.01-10μM 72 h DMSO induces synergistic responses with romidepsin 22826467
KIJ265T Apoptosis Assay 0.01-10μM 72 h DMSO induces synergistic responses with romidepsin 22826467
MDA-231 Apoptosis Assay 0.01-10μM 72 h DMSO induces synergistic responses with romidepsin 22826467
BT-20 Apoptosis Assay 0.01-10μM 72 h DMSO induces synergistic responses with romidepsin 22826467
U937 Growth Inhibition Assay 5-20 μM 24/48/72 h induces a decrease in cell viability in a concentration- and time-dependent manner 22767021
HL60 Growth Inhibition Assay 5-20 μM 24/48/72 h induces a decrease in cell viability in a concentration- and time-dependent manner 22767021
U937 Apoptosis Assay 15 μM 24/48/72 h induces cell apoptosis 22767021
HL60 Apoptosis Assay 15 μM 24/48/72 h induces cell apoptosis 22767021
LS411N  Apoptosis Assay 0.5 μM 72 h increases Fas mRNA level 22461695
MDA-MB-231 Apoptosis Assay 10 μM 48 h reduces cell viability in a dose-dependent manner 21887697
MCF-7  Apoptosis Assay 10 μM 48 h reduces cell viability in a dose-dependent manner 21887697
A375 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL1 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL3 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL28 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
MeWo Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
B16 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
Ly 1 Growth Inhibition Assay 24 h IC50=7.3 μM 21772049
Ly 7 Growth Inhibition Assay 24 h IC50=10.7 μM 21772049
Su-DHL6 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Ly 10 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
RIVA Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Ly 1 Growth Inhibition Assay 48 h IC50=0.34 μM 21772049
Ly 7 Growth Inhibition Assay 48 h IC50=0.025 μM 21772049
Su-DHL6 Growth Inhibition Assay 48 h IC50＞20 μM 21772049
Ly 10 Growth Inhibition Assay 48 h IC50=1.8 μM 21772049
RIVA Growth Inhibition Assay 48 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 48 h IC50=17.4 μM 21772049
Ly 1 Growth Inhibition Assay 72 h IC50=0.01 μM 21772049
Ly 7 Growth Inhibition Assay 72 h IC50=0.018 μM 21772049
Su-DHL6 Growth Inhibition Assay 72 h IC50=1.6 μM 21772049
Ly 10 Growth Inhibition Assay 72 h IC50=1.2 μM 21772049
RIVA Growth Inhibition Assay 72 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 72 h IC50=11.2 μM 21772049
U373-MAGI Antiviral assay 0.25 to 8 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method 27117260
U373-MAGI Antiviral assay 0.25 to 8 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method 27117260
Click to View More Cell Line Experimental Data

Biological Activity

Description Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
Targets
DNA methylation [1]
(HL-60, KG1a cells)
In vitro
In vitro

Decitabine inhibits cell growth in a dose and time-dependent manner with IC50 of approximately 438 nM and 43.8 nM for 72 hours and 96 hours exposure in HL-60 and KG1a leukemic cells, respectively. [1] A recent study shows that Decitabine exhibits high anti-proliferative and pro-apoptotic activity against anaplastic large cell lymphoma (ALCL), and inhibits [3H]–thymidine uptake in KARPAS-299 cells with EC50 of 0.49 μM. [2]
Kinase Assay DNA synthesis assay
The rate of DNA synthesis is measured by the incorporation of radioactive thymidine into DNA. HL-60 and KG1a cells are suspended in 2 mL RPMI medium containing 10% fetal serum in 6-well (35 mm diameter) dishes and incubated with different concentrations of corresponding drugs for 48 hours (drugs are added simultaneously). At 48 hours, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) is added to each well and incubated for an additional 24 hours. The cells are placed on GF/C glass fiber filters (2.4 cm diameter), washed with cold 0.9% NaCl, 5% cold trichloroacetic acid and ethanol. The filters containing the DNA are then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using Beckman LS 6000IC scintillation counter. The IC50 is defined as the concentration of drug that inhibits 50% of the DNA synthesis of the leukemic cell lines from the dose–response curve.
Cell Research Cell lines HL-60 and KG1a
Concentrations 0-500 nM
Incubation Time 96 hours
Method

For the growth inhibition assay, cells in log phase are placed in 5 mL of medium. Different concentrations of Decitabine are added to the medium simultaneously. Cell counts are performed at the indicated times using a model ZM Coulter Counter. The concentration that produces 50% inhibition of growth (IC50) is determined from the growth curves of the drug treated leukemic cell lines.
Experimental Result Images Methods Biomarkers Images PMID
Western blot E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 phospho-p38 / p38 / phospho-NFκB / NFκB p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN Survivin / Bcl-2 / p53 / c-Myc / DNMT1 28152502
Immunofluorescence E-cadherin / MMP-9 DNMT1 28152502
Growth inhibition assay Cell viability 26384351
In Vivo
In vivo

In a ALK+ KARPAS-299 murine xenograft model, Decitabine at a dose of 2.5 mg/kg causes increased apoptosis and reduced proliferation of tumor cells, and also results in demethylation of tumor suppressor p16INK4A. [2]
Animal Research Animal Models KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice.
Dosages ≤2.5 mg/kg
Administration Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06291285 Not yet recruiting
Healthy Volunteers
Novo Nordisk A/S
 February 27 2024 Phase 1
NCT05960773 Recruiting
Mesothelioma|Malignant Mesothelioma (MM)|Early-stage Mesothelioma|Subclinical Mesothelioma|BRCA1-Associated Protein-1 (BAP1) Mutations|Early-stage BAP1-associated Malignancies
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 January 31 2024 Phase 2
NCT05835011 Terminated
Myelodysplastic Syndromes
Astex Pharmaceuticals Inc.
 July 14 2023 Phase 2
NCT05816356 Recruiting
Healthy
EpiDestiny Inc.|Worldwide Clinical Trials
 March 24 2023 Phase 1

Chemical Information & Solubility

Molecular Weight 228.21 Formula

C8H12N4O4
CAS No. 2353-33-5 SDF Download Decitabine SDF
Smiles C1C(C(OC1N2C=NC(=NC2=O)N)CO)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (197.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 22.5 mg/mL

Ethanol : Insoluble


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In vivo
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Question 1:
Is S1200 a racemic mixture or a monomer?

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S1200 is R form

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