1. Epigenetics
  2. Histone Methyltransferase
  3. SGC2085

SGC2085 

Cat. No.: HY-100565 Purity: 99.87%
Handling Instructions

SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.

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

SGC2085 Chemical Structure

SGC2085 Chemical Structure

CAS No. : 1821908-48-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 227 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 330 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM.

IC50 & Target

IC50: 50 nM (CARM1)[1]

In Vitro

SGC2085 which features a methyl at position R1 and a 3,5-dimethylphenoxy at R2 has an IC50 of 50 nM for CARM1 and is over 100-fold selective for CARM1 over PRMT6. These results indicate that the presence of a substituent at R1 is essential for potent and selective inhibition of CARM1. With the exception of PRMT6 (IC50=5.2 μM), SGC2085 does not inhibit other PRMTs. Considering its small size (MW=312.4 Da), SGC2085 has an excellent selectivity profile, which can probably be further improved by exploiting differences in the binding sites of the two enzymes outside the arginine binding pocket. Compound SGC2085 also shows complete selectivity against a panel of 21 human protein methyltrans- ferases tested at three different concentrations (1,10, and 50 μM). To characterize the mechanism of action of SGC2085 in solution, IC50 values are determined at various concentrations of SAM and peptide substrate. Increasing concentration of substrate peptide or cofactor does not affect IC50 values, indicative of a noncompetitive mechanism of inhibition, which has been previously shown for other protein methyltransferase inhibitors binding at the substrate pocket[1]. No cellular activity is observed for SGC2085 when tested up to 10 μM (48 h exposure in HEK293 cells), while methylation of BAF155 is abrogated by 10 μM of the dual CARM1/PRMT6 inhibitor MS049. We assume that the absence of cellular activity for SGC2085 is due to poor permeability[1].

Molecular Weight

312.41

Formula

C₁₉H₂₄N₂O₂

CAS No.

1821908-48-8

SMILES

CC1=CC(OC2=CC=C(CNC([[email protected]@H](N)C)=O)C=C2C)=CC(C)=C1

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 : ≥ 32 mg/mL (102.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2009 mL 16.0046 mL 32.0092 mL
5 mM 0.6402 mL 3.2009 mL 6.4018 mL
10 mM 0.3201 mL 1.6005 mL 3.2009 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

SGC2085 is dissolved in DMSO and diluted with appropriate medium before use. HEK293 cells are grown in 12-well plates in DMEM supplemented with 10% FBS, penicillin (100 U/mL), and streptomycin (100 μg/mL). Thirty percent confluent cells are treated with inhibitors or DMSO. After 48 h, media are removed and cells are lysed in 100 μL of total lysis buffer (20 mM Tris-HCl pH 8.0, 150 mM NaCl, 1 mM EDTA, 10 mM MgCl2, 0.5% Triton X-100, 12.5 U/mL benzonase), complete EDTA-free protease inhibitor cocktail. After 3 min incubation at room temperature, SDS is added to 1% final concentration. Lysates are run on SDS-PAGE, and immunoblotting is done as outlined below to determine the levels of unmethylated and methylated BAF155[1].

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

References
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Keywords:

SGC2085SGC 2085SGC-2085Histone MethyltransferaseInhibitorinhibitorinhibit

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