SGC707; SGC 707; SGC-707
| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
SGC707 (SGC-707) is a novel, cell-permeable and allosteric PRMT3 inhibitor (protein arginine methyltransferase 3 inhibitor) with potential anticancer activity. It inhibits PRMT3 with an IC50 and a Kd of 31 nM and 53 nM, respectively. PRMT3 is involved in cancer development via interaction with the DAL-1 tumor suppressor protein. SGC707 is a chemical probe acting by inhibiting the activity of PRMT3 via targeting the dimerization interface of PRMT3.
| ln Vitro |
In HEK293 and A549 cells, SGC707 (0-10 μM; 6 hours) binds PRMT3 [1].
|
|---|---|
| ln Vivo |
In LDL receptor knockout mice given a Western diet, SGC707 (ip; 10 mg/kg; three times per week; three weeks) therapy decreases plasma triglyceride levels and produces pruritus [2].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: HEK293 and A549 cells Tested Concentrations: 0-10 μM Incubation Duration: 6 hrs (hours) Experimental Results: Stabilized PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. |
| Animal Protocol |
Animal/Disease Models: Western-type diet-fed LDL (lipoprotein) receptor knockout mice[2]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; 10 mg/kg; 3 times per week; 3 weeks Experimental Results: demonstrated 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels. |
| References |
[1]. Kaniskan HÜ, et al. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70.
[2]. de Jong LM, et al. PRMT3 inhibitor SGC707 reduces triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Sci Rep. 2022 Jan 10;12(1):483. |
| Molecular Formula |
C16H18N4O2
|
|
|---|---|---|
| Molecular Weight |
298.34
|
|
| CAS # |
1687736-54-4
|
|
| Related CAS # |
|
|
| SMILES |
O=C(C([H])([H])N([H])C(N([H])C1C([H])=C([H])C2C([H])=NC([H])=C([H])C=2C=1[H])=O)N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
|
|
| InChi Key |
DMIDPTCQPIJYFE-UHFFFAOYSA-N
|
|
| InChi Code |
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)
|
|
| Chemical Name |
N-6-isoquinolinyl-N-[2-oxo-2-(1-pyrrolidinyl)ethyl]-urea
|
|
| Synonyms |
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3519 mL | 16.7594 mL | 33.5188 mL | |
| 5 mM | 0.6704 mL | 3.3519 mL | 6.7038 mL | |
| 10 mM | 0.3352 mL | 1.6759 mL | 3.3519 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|---|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
