General
Preferred name
SGC2085
Synonyms
SGC2085 HCl ()
SGC2085 (hydrochloride) ()
P&D ID
PD048245
CAS
1821908-48-8
1821908-49-9
Tags
available
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
SGC2085 is a selective inhibitor of the protein arginine N-methyltransferase, coactivator associated arginine methyltransferase 1, CARM1 (a.k.a. PRMT4) . PRMT4 is reported to be involved in neoplastic transformation in colorectal cancer, and in estrogen-stimulated breast cancer growth. The selectivity of SGC2085 provides a useful tool compound to validate this PRMT as a therapeutic target.
(GtoPdb)
DESCRIPTION
SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 ¦ÌM, but not other PRMT proteins[1].
PRICE
268
PRICE
263
DESCRIPTION
SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/??-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.
DESCRIPTION
SGC2085 is an effective and selective coactivator-associated arginine methyltransferase 1 (CARM1) inhibitor (IC50: 50 nM).
(TargetMol Bioactive Compound Library)
DESCRIPTION
SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
9
Axon Medchem Screening Library
Cayman Chemical Bioactives
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
34
Molecular Weight
312.18
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
2
Aromatic Ring Count
2
cLogP
3.37
TPSA
64.35
Fraction CSP3
0.32
Chiral centers
1.0
Largest ring
6.0
QED
0.89
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
CARM1
Histone methyltransferase
CARM1 inhibitor
Histone Methyltransferase,PRMT
MOA
Histone Methyltransferase inhibitor
Pathway
Epigenetics
Chromatin/Epigenetic
Recommended Cell Concentration
1 uM
Source data
