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MS049 2HCl (1502816-23-0(free base))

Catalog No. T4393 CAS T4393

MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = <130, <220, and 1.6 μM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional methyltransferases or nonepigenetic targets tested.

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MS049 2HCl (1502816-23-0(free base)) Chemical Structure

MS049 2HCl (1502816-23-0(free base)), CAS T4393

Pack Size	Availability	Price/USD
2 mg	In stock	$ 32.00
5 mg	In stock	$ 47.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 308.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.9%

Biological Description

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Storage & Solubility Information

Description	MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 μM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional methyltransferases or nonepigenetic targets tested.
Targets&IC50	PRMT4:34 nM, PRMT6:43 nM
In vitro	MS049 has been shown to reduce the H3R2me2a mark in HEK293 cells with an IC50 value of 0.97 μM and also, unexpectedly, to reduce H4R3me2a in HEK293 cells.
Cell Research	HEK293 cells were grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 units/mL) and streptomycin (100 μg/mL). 30% confluent cells were treated with different concentrations of compounds in triplicates or DMSO control for 72 h. Cells were lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% TritonX-100, 12.5 U/mL benzonase, complete EDTA-free protease inhibitor cocktail ). After 3 min incubation at RT, SDS was added to final 1% concentration. Lysates were run on SDS-PAGE and immunoblotting was done as outlined below to determine Med12-Rme2a levels in Western blot. They are for reference only.

Molecular Weight	321.28
Formula	C15H26Cl2N2O
CAS No.	T4393

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

PBS(pH7.2): 10 mg/ml

DMSO: 30 mg/mL

Ethanol: 30 mg/mL

References and Literature

1. Shen Y, etal. Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6[J]. Journal of Medicinal Chemistry, 2016, 59(19):9124-9139.

Related compound libraries

This product is contained In the following compound libraries：

Reprogramming Compound Library Chromatin Modification Compound Library Methylation Compound Library

Related Products

Related compounds with same targets

CPI-1205 WDR5-0103 CPUY074020 BRD9539 WM-3835 EPZ032597 LLY-283 PRMT5-IN-29

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Keywords

MS049 2HCl (1502816-23-0(free base)) T4393 Chromatin/Epigenetic Histone Methyltransferase MS049 2HCl (1502816230(free base)) MS049 2HCl (1502816 23 0(free base)) MS-049 2HCl (1502816-23-0(free base)) inhibitor inhibit

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