(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) (Synonyms: (2R)Octyl2-HG) |
| Catalog No.GC32754 |
(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG)는2-Hydroxyglutarate의 D-이성질체의 세포 투과성 변형물이다.
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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)는2-Hydroxyglutarate의 D-이성질체의 세포 투과성 변형물이다.(2R)-Octyl-α-hydroxyglutarate는 IDH1 돌연변이 종양 세포에서 생성되는 암 대사물질 (R)-2-hydroxyglutarate (R-2HG)의 막 투과성 전구체이다 [2].(2R)-Octyl-α-hydroxyglutarate는 α- ketoglutarate (α-KG) 의존하는 탈산소효소의 경쟁적 억제제로 작용할 수 있다 [3].(2R)-Octyl-α-hydroxyglutarate는 IDH1/2 돌연변이 세포에서 동원 지향 수리(HDR) 활성을 억제할 수 있다 [4].
체외 실험에서 (2R)-Octyl-α-hydroxyglutarate(0-1000μM)로 야생형 HCT116 세포를 10일간 처리하면 세포의 폴리 (아데노신 5'-이인산 리보스) 폴리머라제(PARP) 저해제에 대한 민감성이 증가한다 [5]. (2R)-Octyl-α-hydroxyglutarate(300μM)로 THP1 세포를 7일간 처리하면 세포 내 (R)-2-hydroxyglutarate의 수준이 증가하지 않는다 [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.
| 세포 실험 [1]: | |
세포 라인 | 야생형 HCT116 쥐 |
제조 방법 | 300nM BMN-673 또는 DMSO 대조 그룹 존재 하에 4일 동안 배양한 후 야생형 HCT116 세포는 (2R)-Octyl-α-hydroxyglutarate((2R)-Octyl-2-HG) (0-1000μM)의 증가하는 농도로 단기 성장 지연 검사를 받았습니다. (2R)-octyl-2HG를 포함하는 성장 지연 검사의 경우 세포는 접시에 놓기 전에 표시된 농도로 10일 동안 배양했습니다. |
반응 조건 | 0-1000μM; 10 일 동안 |
응용 분야 | (2R)-Octyl-α-hydroxyglutarate로 야생형 HCT116 세포를 처리하면 폴리 (아데노신 5'-이인산 리보스)폴리머라제(PARP) 저해제에 대한 민감성이 증가합니다. |
| 동물 실험 [2]: | |
동물 모형 | THP1 세포 |
제조 방법 | 부모 THP1 세포를 5×10⁴ cells/ml의 밀도로 접종하고 1% 혈청이 보충된 RPMI 배양액에서 7일 동안 배양했습니다. 배양 조건은 300μM (2R)-Octyl-α-hydroxyglutarate, 5μM IACS-010759, 둘의 조합또는 DMSO 대조 그룹이었습니다. BD FACSCanto™II 유동 세포계를 사용하고 제3일, 제5일, 제7일에 생존 DAPI 양성 세포와 CountBright™ 절대 카운팅 비드의 비율을 확인했습니다. |
제형 | 300μM; 7 일 동안 |
응용 분야 | (2R)-Octyl-α-hydroxyglutarate는 THP1 세포에서 (R)-2-hydroxyglutarate 수준을 상승시키지 않습니다. |
References: | |
| Cas No. | 1391194-67-4 | SDF | |
| Synonyms | (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 | |||
|
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 |
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Quality Control & SDS
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- Purity: >97.00%
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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