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SKU | Size | Availability | Price | Qty |
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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
Synonyms | Tubastatin A BASE;1-(isoquinolin-6-yl)-3-(2-oxo-2-(pyrrolidin-1-yl)ethyl)urea; |
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Specifications & Purity | Moligand™, ≥97% |
Biochemical and Physiological Mechanisms | SGC707 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 Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ALLOSTERIC MODULATOR |
Mechanism of action | Allosteric 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 |
ALogP | 0.43 |
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HBD Count | 2 |
Rotatable Bond | 3 |
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IUPAC Name | 1-isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea |
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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 |
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Solubility | Solubility (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; |
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DMSO(mg / mL) Max Solubility | 59 |
DMSO(mM) Max Solubility | 197.7609439 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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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. |
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] |