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Decitabine DNA Methyltransferase inhibitor

Name: Decitabine
Brand: Selleck Chemicals
SKU: S1200
Availability: InStock
Rating: 5 (220 reviews)

Cat.No.S1200

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.

Chemical Structure

Molecular Weight: 228.21

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Quality Control

Batch: Purity: 99.90%

99.90

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK
Other DNA Methyltransferase Inhibitors	RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol CM272 GSK3685032 β-thujaplicin GSK-3484862 Bobcat339 DC-05

Cell Culture, Treatment & Working Concentration

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

Solubility

In vitro
Batch:

DMSO : 45 mg/mL (197.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 22.5 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	water Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (43.82mM)	Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight	228.21	Formula	C₈H₁₂N₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	2353-33-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716			Smiles	C1C(C(OC1N2C=NC(=NC2=O)N)CO)O

Mechanism of Action

Targets/IC₅₀/Ki	DNA methylation (HL-60, KG1a cells)
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. A recent study shows that this compound 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.
Kinase Assay	DNA synthesis assay
Kinase 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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12620295/ [2] https://pubmed.ncbi.nlm.nih.gov/22687603/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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Frequently Asked Questions

Question 1:
Is it a racemic mixture or a monomer?

Answer:
Its S1200 is R form.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):