N-Oxalylglycine (Synonyms: NOG) |
| カタログ番号GC12458 |
細胞浸透性のα-ケトグルタレート依存性酵素阻害剤であり、JMJD2A、JMJD2C、およびJMJD2Eを含みます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 5262-39-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
The jumonji domain-containing protein 2 (JMJD2) subfamily of histone demethylases have been shown to catalyze demethylation of the methylated forms of histone 3 lysine 9 (H3K9) and H3K36 in vitro and in cells.[1] Because histone demethylases are implicated in certain diseases, including cancer, selective inhibitors are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs.2 N-Oxalylglycine, the amide analog of α-ketoglutarate, is a cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E (IC50s = 250, 500, and 24 μM, respectively).[3],[4],[5],[6] It can also inhibit the prolyl hydroxylase domain-containing proteins PHD1 and PHD2 with IC50 values of 2.1 and 5.6 μM, respectively.[4],[5],[6]
Reference:
[1]. Krishnan, S., Horowitz, S., and Trievel, R.C. Structure and function of histone H3 lysine 9 methyltransferases and demethylases. ChemBioChem 12(2), 254-263 (2011).
[2]. Tian, X., and Fang, J. Current perspectives on histone demethylases. Acta Biochimica et Biophysica Sinica 39(2), 81-88 (2007).
[3]. Hamada, S., Kim, T.D., Suzuki, T., et al. Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors. Bioorganic & Medicinal Chemistry Letters 19, 2852-2855 (2009).
[4]. Hamada, S., Suzuki, T., Mino, K., et al. Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of Jumonji domain-containing protein 2 histone demethylase inhibitors. Journal of Medicinal Chemistry 53, 5629-5638 (2010).
[5]. Rose, N.R., Ng, S.S., Mecinovic, J., et al. Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. Journal of Medicinal Chemistry 51, 7053-7056 (2008).
[6]. Rose, N.R., Woon, E.C.Y., Kingham, G.L., et al. Selective inhibitors of the JMJD2 histone demethylases: Combined nondenaturing mass spectrometric screening and crystallographic approaches. Journal of Medicinal Chemistry 53, 1810-1818 (2010).
| Cas No. | 5262-39-5 | SDF | |
| 同義語 | NOG | ||
| Chemical Name | N-(carboxycarbonyl)-glycine | ||
| Canonical SMILES | OC(C(NCC(O)=O)=O)=O | ||
| Formula | C4H5NO5 | M.Wt | 147.1 |
| 溶解度 | 10mg/ml in ethanol;10mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 6.7981 mL | 33.9905 mL | 67.981 mL |
| 5 mM | 1.3596 mL | 6.7981 mL | 13.5962 mL |
| 10 mM | 0.6798 mL | 3.399 mL | 6.7981 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *