SGC707
- CAS NO.:1687736-54-4
- Empirical Formula: C16H18N4O2
- Molecular Weight: 298.34
- MDL number: MFCD28411624
- Update Date: 2023-06-30 15:45:59
What is SGC707?
Description
SGC707 (1687736-54-4) is a potent (IC50?= 31 nM) and selective allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).1? Selective against 31 other methyltransferases. An extremely useful probe for investigating the role of PRMT3 in normal and pathophysiology. Cell permeable and active in vivo.
The Uses of SGC707
SGC 707 is a potent, selective and cell-active allosteric inhibitor of PRMT3.
in vitro
the ic50 and kd value of sgc707 against prmt3was 31 ± 2 nm and 53 ± 2 nm respectively. sgc707 showed an outstanding selectivity for prmt3 against 31 other methyltransferases and a broad range of 250 non-epigenetic targets, g protein-coupled receptors (gpcrs), ion channels, and transporters. the residence time of sgc707 was 9.7 min. in both hek293 and a549 cells, sgc707 stabilized prmt3 with ec50 values of 1.3 μm and 1.6 μm, respectively. sgc707 treatment at high concentrations 50 and 100 mm for 72 h lead to some toxicity [1].
in vivo
in cd-1 male mice, intraperitoneal injection of sgc707 at 30 mg/kg for over 6 h showed good plasma exposure with the peak plasma level of 38 μm. after injection 6 h, the plasma level of sgc707 decreased to 208 nm. the half-life of sgc707 was about 1 h. the 30 mg/kg dose was well tolerated in the tested mouse model [1].
storage
Store at +4°C
References
1) Kaniskan?et al. (2015), A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3); Angew. Chem. Int. Ed. Engl., 54?5166
Properties of SGC707
storage temp. | -20°C |
solubility | Soluble in DMSO (up to 35 mg/ml) |
form | solid |
color | Beige |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Safety information for SGC707
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for SGC707
New Products
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