(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) (Synonyms: (2R)Octyl2-HG) |
| Catalog No.GC32754 |
(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) est une modification cellule - perméable de D - isomère de 2-Hydroxyglutarate.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1391194-67-4
Sample solution is provided at 25 µL, 10mM.
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(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) est une modification cellule - perméable de D - isomère de 2-Hydroxyglutarate[1]. (2R)-Octyl-α-hydroxyglutarate est un précurseur membrane - perméable d' oncométabolite (R)-2-hydroxyglutarate (R-2HG) qui est produit dans les cellules tumorales mutantes[2]. (2R)-Octyl-α-hydroxyglutarate peut agir en tant qu'un inhibiteur compétitif de la désoxygénase α-ketoglutarate (α-KG)-dépendente[3]. (2R)-Octyl-α-hydroxyglutarate peut inhiber l'activité de réparation homologie - dirigée (HDR) dans les cellules mutantes IDH1/2[4].
Le traitement in vitro par (2R)-Octyl-α-hydroxyglutarate (0-1000μM) aux cellules HCT116 sauvage - type pendant 10 jours a augmenté la sensibilité des cellules aux inhibiteurs de la polymérase poly (adénosine 5'-diphosphate ribose) (PARP)[5]. Le traitement par (2R)-Octyl-α-hydroxyglutarate (300μM) aux cellules THP1 pendant 7 jours n'a pas augmenté le niveau de (R)-2-hydroxyglutarate dans les cellules[6].
References:
[1] Reitman Z J, Duncan C G, Poteet E, et al. Cancer-associated isocitrate dehydrogenase 1 (IDH1) R132H mutation and d-2-hydroxyglutarate stimulate glutamine metabolism under hypoxia[J]. Journal of Biological Chemistry, 2014, 289(34): 23318-23328.
[2] Kim G H, Choi S Y, Oh T I, et al. IDH1R132H causes resistance to HDAC inhibitors by increasing NANOG in glioblastoma cells[J]. International Journal of Molecular Sciences, 2019, 20(11): 2679.
[3] Wang X, Liu R, Qu X, et al. α-Ketoglutarate-activated NF-κB signaling promotes compensatory glucose uptake and brain tumor development[J]. Molecular cell, 2019, 76(1): 148-162. e7.
[4] Dow J, Krysztofiak A, Liu Y, et al. Vulnerability of IDH1-mutant cancers to histone deacetylase inhibition via orthogonal suppression of DNA repair[J]. Molecular Cancer Research, 2021, 19(12): 2057-2067.
[5] Sulkowski P L, Corso C D, Robinson N D, et al. 2-Hydroxyglutarate produced by neomorphic IDH mutations suppresses homologous recombination and induces PARP inhibitor sensitivity[J]. Science translational medicine, 2017, 9(375): eaal2463.
[6] Bassal M A, Samaraweera S E, Lim K, et al. Germline mutations in mitochondrial complex I reveal genetic and targetable vulnerability in IDH1-mutant acute myeloid leukaemia[J]. Nature communications, 2022, 13(1): 2614.
| Expériences cellulaires [1]: | |
Lignées cellulaires | Cellules HCT119 sauvage - type |
Méthode de préparation | Après 4 jours de culture en présence de 300nM BMN-673 ou de DMSO en tant que témoin, les cellules HCT116 sauvage - type ont été traitées par (2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) (0-1000μM) des concentrations croissantes pour un essai de retard de croissance court - terme. Pour les essais de retard de croissance qui contiennent (2R)-octyl-2HG, les cellules ont été cultivées à la concentration indiquée pendant 10 jours avant le placage. |
Conditions de réaction | 0-1000μM; 10 jours |
Domaines d'application | Le traitement par (2R)-Octyl-α-hydroxyglutarate aux cellules HCT116 sauvage - type a augmenté la sensibilité des cellules aux inhibiteurs de la polymérase poly (adénosine 5'-diphosphate - ribose) (PARP). |
| Expériences cellulaires [2]: | |
Lignées cellulaires | Cellules THP1 |
Méthode de préparation | Les cellules THP1 parentales qui sont ensemencées à 5×104 cellules/ml ont été cultivées pendant 7 jours dans RPMI supplémenté avec 1% sérum en présence soit de 300µM (2R)-Octyl-α-hydroxyglutarate, de 5μM IACS-010759, de la combinaison des deux ou de DMSO en tant que témoin. Le taux de cellules vivantes DAPI - positives par rapport à CountBright™ Absolute Counting Beads a été déterminé les jours 3, 5 et 7 par utiliser le système de cytométrie en flux BD FACSCanto™II. |
Conditions de réaction | 300μM; 7 jours |
Domaines d'application | (2R)-Octyl-α-hydroxyglutarate n'induit pas l'élevation du niveau de (R)-2-hydroxyglutarate dans les cellules THP1. |
References: | |
| Cas No. | 1391194-67-4 | SDF | |
| Synonymes | (2R)Octyl2-HG | ||
| Canonical SMILES | O=C(OCCCCCCCC)[C@H](O)CCC(O)=O | ||
| Formula | C13H24O5 | M.Wt | 260.33 |
| Solubility | DMSO : 100 mg/mL (384.13 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8413 mL | 19.2064 mL | 38.4128 mL |
| 5 mM | 0.7683 mL | 3.8413 mL | 7.6826 mL |
| 10 mM | 0.3841 mL | 1.9206 mL | 3.8413 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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