SGC2085 structure
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Common Name | SGC2085 | ||
|---|---|---|---|---|
| CAS Number | 1821908-49-9 | Molecular Weight | 348.8717 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C19H24N2O2*ClH | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SGC2085SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins[1]. |
| Name | SGC2085 |
|---|
| Description | SGC2085 hydrochloride is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 hydrochloride also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins[1]. |
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| Related Catalog | |
| Target |
PRMT6:5.2 μM (IC50) |
| In Vitro | SGC2085 hydrochloride (1 μM, 10 μM, 50 μM;48 h) 对 21 种人类蛋白质甲基转移酶的具有完全选择性[1]。 SGC2085 hydrochloride (10 μM;48 h) 表现出低细胞渗透性,在 HEK293 细胞中无细胞活性[1]。 |
| Cell Assay | 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]. |
| Molecular Formula | C19H24N2O2*ClH |
|---|---|
| Molecular Weight | 348.8717 |
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Name: Selectivity index, ratio of IC50 for RMT6 (unknown origin) to IC50 for full-length Ha...
Source: ChEMBL
Target: N/A
External Id: CHEMBL4426996
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Name: Non-competitive inhibition of full-length Halo-tagged human CARM1 (1 to 608 residues)...
Source: ChEMBL
Target: Histone-arginine methyltransferase CARM1
External Id: CHEMBL4427001
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Name: Inhibition of full-length Halo-tagged human CARM1 (1 to 608 residues) expressed in 29...
Source: ChEMBL
Target: Histone-arginine methyltransferase CARM1
External Id: CHEMBL4426986
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Name: Non-competitive inhibition of full-length Halo-tagged human CARM1 (1 to 608 residues)...
Source: ChEMBL
Target: Histone-arginine methyltransferase CARM1
External Id: CHEMBL4427002
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Name: Inhibition of CARM1 in HEK293 cells assessed as reduction in BAF155 methylation at 10...
Source: ChEMBL
Target: Histone-arginine methyltransferase CARM1
External Id: CHEMBL4427003
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Name: Inhibition of PRMT6 (unknown origin)
Source: ChEMBL
Target: Protein arginine N-methyltransferase 6
External Id: CHEMBL4426987
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Name: Inhibition of CARM1 in HEK293 cells assessed as reduction in BAF155 methylation at 1 ...
Source: ChEMBL
Target: Histone-arginine methyltransferase CARM1
External Id: CHEMBL4427004
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Name: Inhibition of PRMT8 (unknown origin)
Source: ChEMBL
Target: Protein arginine N-methyltransferase 8
External Id: CHEMBL4426988
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