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SGC707 - 97%, high purity , CAS No.1687736-54-4, Allosteric modulator of protein arginine methyltransferase 3

  • Moligand™
  • ≥97%
Item Number
S413846
Grouped product items
SKUSizeAvailabilityPrice Qty
S413846-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$70.90
S413846-25mg
25mg
In stock
$159.90
S413846-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$244.90
S413846-100mg
100mg
In stock
$489.90

PRMT Inhibitors

Basic Description

SynonymsTubastatin A BASE;1-(isoquinolin-6-yl)-3-(2-oxo-2-(pyrrolidin-1-yl)ethyl)urea;
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsSGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase\u20053 (PRMT3) with IC50 and Kd of 31 nM and 53 nM, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeALLOSTERIC MODULATOR
Mechanism of actionAllosteric modulator of protein arginine methyltransferase 3
Product Description

Information

SGC707 SGC707 is a potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 ( PRMT3 ) with IC50 and K d of 31 nM and 53 nM, respectively.


Targets

PRMT3 ; PRMT3 31 nM; 53 nM(Kd)


In vitro

In cells, SGC707 binds to PRMT3 and reduces PRMT3-dependent H4R3me2a. SGC707 also stabilizes PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively.


In vivo

In CD-1 male mice, SGC707 (30 mg/kg, i.p.) gives good plasma exposure over 6 h with the peak plasma level of 38000 nM, which suggests that SGC707 is suitable for animal studies.


Cell Research(from reference)

Cell lines:293, LnCap, U2O s, HFF, MCF-7, and MDA-MB-231 cells 

Concentrations:100 μM 

Incubation Time:72 h 

Product Properties

ALogP0.43
HBD Count2
Rotatable Bond3

Associated Targets

DLK1 Tchem Protein delta homolog 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKX Tchem cAMP-dependent protein kinase catalytic subunit PRKX 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRKG2 Tchem cGMP-dependent protein kinase 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

BRSK1 Tchem Serine/threonine-protein kinase BRSK1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

AOX1 Tchem Aldehyde oxidase 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

HTR2B Tclin 5-hydroxytryptamine receptor 2B 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

PRMT3 Tchem Protein arginine N-methyltransferase 3 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RPS6KA4 Tchem Ribosomal protein S6 kinase alpha-4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

METTL21A Tbio Protein N-lysine methyltransferase METTL21A 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 1-isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea
INCHI InChI=1S/C16H18N4O2/c21-15(20-7-1-2-8-20)11-18-16(22)19-14-4-3-13-10-17-6-5-12(13)9-14/h3-6,9-10H,1-2,7-8,11H2,(H2,18,19,22)
InChi Key DMIDPTCQPIJYFE-UHFFFAOYSA-N
Canonical SMILES C1CCN(C1)C(=O)CNC(=O)NC2=CC3=C(C=C2)C=NC=C3
Isomeric SMILES C1CCN(C1)C(=O)CNC(=O)NC2=CC3=C(C=C2)C=NC=C3
PubChem CID 90642938
MeSH Entry Terms SGC707
Molecular Weight 298.34

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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2 results found

Lot NumberCertificate TypeDateItem
G2209330Certificate of AnalysisJun 08, 2022 S413846
G2209393Certificate of AnalysisJun 08, 2022 S413846

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 59 mg/mL (197.76 mM); Ethanol: 59 mg/mL warmed with 50ºC Water: bath (197.76 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility59
DMSO(mM) Max Solubility197.7609439
Water(mg / mL) Max Solubility<1

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H315:Causes skin irritation

H319:Causes serious eye irritation

H335:May cause respiratory irritation

H302:Harmful if swallowed

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

Related Documents

References

1. Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I et al..  (2015)  A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3)..  Angew Chem Int Ed Engl,  54  (17): (5166-70).  [PMID:25728001]

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