MS8511

Cat. No.: HY-150510: FAQs
Data Sheet SDS Handling Instructions

Molarity Calculator

MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC₅₀ values of 100 nM (G9a) and 140 nM (GLP), and K_d values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS).

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

MS8511 Chemical Structure

CAS No. : 2866408-21-9

Size	Price	Stock
1 mg	USD 340	Ask For Quote & Lead Time
5 mg	USD 840	Ask For Quote & Lead Time
10 mg	USD 1350	Ask For Quote & Lead Time
25 mg	USD 2700	Ask For Quote & Lead Time
50 mg	USD 4320	Ask For Quote & Lead Time

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

G9a

100 nM (IC₅₀)

G9a

44 nM (Kd)

GLP

140 nM (IC₅₀)

GLP

46 nM (Kd)

In Vitro

MS8511 (Compound 8, 0-100 μΜ, 10 min) selectively inhibits G9a and GLP against other PKMTs and PRMTs, with IC₅₀ values of 100 nM (G9a) and 140 nM (GLP)^[1].
MS8511 (50 min) prefers covalent modification for G9a over GLP, with K_d values of 44 nM (G9a) and 46 nM (GLP)^[1].
MS8511 (0-5 μM, 24-72 h) effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cellssup>[1].
MS8511 (0.8-25 μM, 3 days) inhibits the growth of MDA-MB-231 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231, K562 cells.
Concentration:	0.2, 1, 5 μM.
Incubation Time:	24, 48, 72 h.
Result:	Reduced the H3K9me2 mark in a concentration- and time-dependent manner.

Cell Viability Assay^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	0.8, 1.6, 3.1 6.3, 12.5, 25 μM.
Incubation Time:	3 days
Result:	Inhibited the growth of MDA-MB-231 cells.

Molecular Weight

495.66

Formula

C₂₈H₄₁N₅O₃

CAS No.

2866408-21-9

Appearance

Solid

Color

White to off-white

SMILES

COC1=CC(C(C=C1OCCCN2CCCC2)=NC(NC(C=C)=O)=C3)=C3NC4CCN(CC4)C(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (201.75 mM; Need ultrasonic; 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	2.0175 mL	10.0876 mL	20.1751 mL
5 mM	0.4035 mL	2.0175 mL	4.0350 mL
10 mM	0.2018 mL	1.0088 mL	2.0175 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (5.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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 (5.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
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 (5.04 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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

Data Sheet (273 KB) SDS (251 KB) Handling Instructions (2659 KB)

References

[1]. Kwang-Su Park, et al. Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J Med Chem. 2022 Jun 28. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.0175 mL	10.0876 mL	20.1751 mL	50.4378 mL
	5 mM	0.4035 mL	2.0175 mL	4.0350 mL	10.0876 mL
	10 mM	0.2018 mL	1.0088 mL	2.0175 mL	5.0438 mL
	15 mM	0.1345 mL	0.6725 mL	1.3450 mL	3.3625 mL
	20 mM	0.1009 mL	0.5044 mL	1.0088 mL	2.5219 mL
	25 mM	0.0807 mL	0.4035 mL	0.8070 mL	2.0175 mL
	30 mM	0.0673 mL	0.3363 mL	0.6725 mL	1.6813 mL
	40 mM	0.0504 mL	0.2522 mL	0.5044 mL	1.2609 mL
	50 mM	0.0404 mL	0.2018 mL	0.4035 mL	1.0088 mL
	60 mM	0.0336 mL	0.1681 mL	0.3363 mL	0.8406 mL
	80 mM	0.0252 mL	0.1261 mL	0.2522 mL	0.6305 mL
	100 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5044 mL

MS8511 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:

MS85112866408-21-9MS 8511MS-8511Histone MethyltransferaseCancersPKMTs inhibitorcovalent InhibitorsH3K9me2antiproliferationMDA-MB-231 cells.Inhibitorinhibitorinhibit

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