SGI-1027

Name: SGI-1027
Brand: MedChemExpress
SKU: HY-13962
Rating: 5.0 (11 reviews)

Cat. No.: HY-13962 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

For research use only. We do not sell to patients.

SGI-1027 Chemical Structure

CAS No. : 1020149-73-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 86	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 86	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 85	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 136	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 408	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 11 publication(s) in Google Scholar

11 Publications Citing Use of MCE SGI-1027

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DNA Methyltransferase DNMT1 DNMT3 MGMT

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

SGI-1027 is a DNA methyltransferase (DNMT) inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate.

IC₅₀ & Target^[1]

DNMT3B

7.5 μM (IC₅₀)

DNMT3A

8 μM (IC₅₀)

DNMT1

12.5 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	EC₅₀	> 10 μM Compound: SGI1027	Antiproliferative activity against human HCT116 cells after 2 to 4 days by ATPlite 1step luminescence assay Antiproliferative activity against human HCT116 cells after 2 to 4 days by ATPlite 1step luminescence assay	[PMID: 26220519]
HCT-116	IC₅₀	3.2 μM Compound: SGI-1027	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue assay	[PMID: 34333394]
K562	IC₅₀	1.16 μM Compound: SGI-1027	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 28419930]
KARPAS-299	EC₅₀	1.8 μM Compound: SGI1027	Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay Antiproliferative activity against human KARPAS299 cells after 2 to 4 days by ATPlite 1step luminescence assay	[PMID: 26220519]
KG-1	EC₅₀	4.4 μM Compound: SGI1027	Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay Antiproliferative activity against human KG1 cells after 2 to 4 days by ATPlite 1step luminescence assay	[PMID: 26220519]
MDA-MB-231	IC₅₀	4.8 μM Compound: 1, SGI-1027	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by trypan blue exclusion assay	[PMID: 24387159]
PBMC	IC₅₀	23.8 μM Compound: 1, SGI-1027	Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay Cytotoxicity against human PBMC after 48 hrs by trypan blue exclusion assay	[PMID: 24387159]
PC-3	IC₅₀	6.5 μM Compound: 1, SGI-1027	Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay Cytotoxicity against human PC3 cells after 48 hrs by trypan blue exclusion assay	[PMID: 24387159]
Raji	IC₅₀	9.1 μM Compound: 1, SGI-1027	Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay Cytotoxicity against human Raji cells after 48 hrs by trypan blue exclusion assay	[PMID: 24387159]
Sf9	IC₅₀	6 μM Compound: 7, SGI1027	Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil Inhibition of His6-tagged human recombinant DNMT1 expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintil	[PMID: 25406944]
Sf9	IC₅₀	7.5 μM Compound: 7, SGI1027	Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti	[PMID: 25406944]
Sf9	IC₅₀	8 μM Compound: 7, SGI1027	Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti Inhibition of His6-tagged human recombinant DNMT3a expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scinti	[PMID: 25406944]
U-937	IC₅₀	1.56 μM Compound: SGI-1027	Antiproliferative activity against human U937 cells after 72 hrs by MTT assay Antiproliferative activity against human U937 cells after 72 hrs by MTT assay	[PMID: 28419930]
U-937	IC₅₀	1.7 μM Compound: 1, SGI-1027	Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay Cytotoxicity against human U937 cells after 48 hrs by trypan blue exclusion assay	[PMID: 24387159]

In Vitro

SGI-1027 is a DNMT inhibitor, with IC₅₀s of 7.5 μM, 8 μM, and 12.5 μM for DNMT3B, DNMT3A, and DNMT1 with poly(dI-dC) as substrate. SGI-1027 shows an IC₅₀ of 6 μM for DNMT1 (hemimethylated DNA). SGI-1027 (1, 2.5, or 5 μM) causes selective degradation of DNMT1 in several human cancer cell lines, but shows little or no cytotoxic effect on rat hepatoma cells, and does not induce apoptosis in rat hepatoma cells^[1]. SGI-1027 shows an EC₅₀ of 0.9 μM for hDNMT3A, and causes cytotoxicity on KG-1 cells, with an EC₅₀ of 4.4 μM^[2].

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

Molecular Weight

461.52

Formula

C₂₇H₂₃N₇O

CAS No.

1020149-73-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=C(NC2=NC(N)=NC(C)=C2)C=C1)C3=CC=C(NC4=CC=NC5=CC=CC=C45)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 27 mg/mL (58.50 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1668 mL	10.8338 mL	21.6675 mL
5 mM	0.4334 mL	2.1668 mL	4.3335 mL
10 mM	0.2167 mL	1.0834 mL	2.1668 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.42 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (248 KB) RP-HPLC (244 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Datta J, et al. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009 May 15;69(10):4277-85. [Content Brief]

[2]. Rilova E, et al. Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation. ChemMedChem. 2014 Mar;9(3):590-601. [Content Brief]

Kinase Assay ^[1]	To determine the nature of inhibition of DNMTase activity by SGI-1027, DNMT1 enzyme activity is measured in presence of a fixed concentration of SGI-1027 (0, 2.5, 5, and 10 μM) while one of the two (Ado-Met or DNA) is varied in a particular reaction mixture. At a fixed concentration of DNA (500 ng) varying concentrations of Ado-Met used are from 25-500 nM, respectively. Similarly, final DNA concentrations are varied from (25-500 ng) at 75 nM Ado-Met^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Rat hepatoma H4IIE cells are grown in DMEM supplemented with fetal bovine serum (10%) and calf serum (10%). Cells are seeded into 96-well plates and after 48 h exposed to SGI-1027 at concentrations ranging from 0 to 300 µM. The solubility is determined by Nephalometry techniques immediately after dosing and before harvesting the cells at 24 h. Following the exposure period, the cells or their supernatant (culture medium) are analyzed for changes in cell proliferation (propidium iodide), membrane leakage (α-GST), mitochondrial function [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and cellular ATP], oxidative stress (intracellular GSH and 8-isoprostane), and apoptosis (caspase-3). The half-maximal toxic concentration (TC₅₀) is determined from the dose-response curves^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Datta J, et al. A new class of quinoline-based DNA hypomethylating agents reactivates tumor suppressor genes by blocking DNA methyltransferase 1 activity and inducing its degradation. Cancer Res. 2009 May 15;69(10):4277-85. [Content Brief] [2]. Rilova E, et al. Design, synthesis and biological evaluation of 4-amino-N- (4-aminophenyl)benzamide analogues of quinoline-based SGI-1027 as inhibitors of DNA methylation. ChemMedChem. 2014 Mar;9(3):590-601. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1668 mL	10.8338 mL	21.6675 mL	54.1688 mL
	5 mM	0.4334 mL	2.1668 mL	4.3335 mL	10.8338 mL
	10 mM	0.2167 mL	1.0834 mL	2.1668 mL	5.4169 mL
	15 mM	0.1445 mL	0.7223 mL	1.4445 mL	3.6113 mL
	20 mM	0.1083 mL	0.5417 mL	1.0834 mL	2.7084 mL
	25 mM	0.0867 mL	0.4334 mL	0.8667 mL	2.1668 mL
	30 mM	0.0722 mL	0.3611 mL	0.7223 mL	1.8056 mL
	40 mM	0.0542 mL	0.2708 mL	0.5417 mL	1.3542 mL
	50 mM	0.0433 mL	0.2167 mL	0.4334 mL	1.0834 mL

SGI-1027 Related Classifications

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:

SGI-10271020149-73-8SGI1027SGI 1027DNA MethyltransferaseApoptosisDNMTsDNA MTasesInhibitorinhibitorinhibit

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SGI-1027

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SGI-1027 Related Antibodies

11 Publications Citing Use of MCE SGI-1027

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References

Customer Review

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Complete Stock Solution Preparation Table

SGI-1027 Related Classifications

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