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Sodium Oxamate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Sodium Oxamate图片
包装与价格:
包装价格(元)
100mg电议
500mg电议
1g电议
5g电议

产品介绍

Sodium oxamate as PDK1 and LDHA inhibitor with IC50 values (μg/mL) of 15.60.

Cell lines

BRCA ovarian cancer cells:A2780 and SKOV3

Preparation Method

Cell proliferation is evaluated using a Cell Counting Kit-8. SKOV3 cells and A2780 cells are seeded in a 96-well culture plates at a density of 2 105 cells/well and incubated with different concentrations of the drugs for different times(Sodium oxamate).

Reaction Conditions

50 mM Sodium oxamate for 24 h

Applications

Sodium oxamate enhances the suppressive effects of PARP inhibitors on ovarian cancer without BRCA mutations, remarkably promoting the inhibitory effects of PARP inhibitors on wild-type BRCA ovarian cancer cells.

Animal models

Four-week-old male BALB/c nude mice of CRC xenograft

Preparation Method

C. tropicalis was given by multipoint intratumoral injection, twice per week for three weeks.Oxaliplatin (10 mg/kg) and Sodium oxamate (500 mg/kg) were administered by intraperitoneal injection, twice per week for three weeks. The length and width of the tumors were measured every three days.

Dosage form

500 mg/kg Sodium oxamate Twice a week for three weeks

Applications

Sodium oxamate reduces the growth of colorectal cancer in CRC mice, by restoring the down-regulated MMR functional proteins and attenuating chemotherapy resistance to oxaliplatin caused by C. tropicalis.

产品描述

Sodium oxamate as PDK1 and LDHA inhibitor with IC50values (μg/mL) of 15.60[1]. Sodium oxamate can specifically inhibit LDH-A. Sodium oxamate by down-regulating CDK1/cyclin B1 Pathway induces G2/M cell cycle arrest and promotes apoptotic targets by increasing ROS production in mitochondria[4,5].

Sodium oxamate enhances the suppressive effects of PARP inhibitors on ovarian cancer without BRCA mutations, remarkably promoting the inhibitory effects of PARP inhibitors on wild-type BRCA ovarian cancer cells[3]. In the human PC cell line, Sodium oxamate caused cell inhibition, resulting in increased sensitivity of CRPC cells to DOC, and the combination of DOC and Sodium oxamate promoted apoptosis compared with DOC or Sodium oxamate alone[2].

Sodium oxamate reduces the growth of colorectal cancer in CRC mice, by restoring the down-regulated MMR functional proteins and attenuating chemotherapy resistance to oxaliplatin caused by C. tropicalis[6]. NETosis and lactate accumulation during LPS induced sepsis in mice was inhibited by sodium oxamate[7].

References:
[1]: Kamal S, Derbala HA, et,al. Synthesis, Biological, and Molecular Docking Studies on 4,5,6,7-Tetrahydrobenzo[b]thiophene Derivatives and Their Nanoparticles Targeting Colorectal Cancer. ACS Omega. 2021 Oct 25;6(43):28992-29008. doi: 10.1021/acsomega.1c04063. PMID: 34746589; PMCID: PMC8567357.
[2]: Muramatsu H, Sumitomo M, et,al. Targeting lactate dehydrogenase-A promotes docetaxel-induced cytotoxicity predominantly in castration-resistant prostate cancer cells. Oncol Rep. 2019 Jul;42(1):224-230. doi: 10.3892/or.2019.7171. Epub 2019 May 24. PMID: 31180564.
[3]: Xiang J, Zhou L, et,al. LDH-A inhibitors as remedies to enhance the anticancer effects of PARP inhibitors in ovarian cancer cells. Aging (Albany NY). 2021 Dec 16;13(24):25920-25930. doi: 10.18632/aging.203780. Epub 2021 Dec 16. PMID: 34919531; PMCID: PMC8751605.
[4]: Thornburg JM, Nelson KK, et,al. Targeting aspartate aminotransferase in breast cancer. Breast Cancer Res. 2008;10(5):R84. doi: 10.1186/bcr2154. Epub 2008 Oct 15. PMID: 18922152; PMCID: PMC2614520.
[5]: Zhai X, Yang Y, et,al. Inhibition of LDH-A by oxamate induces G2/M arrest, apoptosis and increases radiosensitivity in nasopharyngeal carcinoma cells. Oncol Rep. 2013 Dec;30(6):2983-91. doi: 10.3892/or.2013.2735. Epub 2013 Sep 19. PMID: 24064966.
[6]: Qu J, Sun Z, et,al. tropicalis promotes chemotherapy resistance in colon cancer through increasing lactate production to regulate the mismatch repair system. Int J Biol Sci. 2021 Jul 2;17(11):2756-2769. doi: 10.7150/ijbs.59262. PMID: 34345205; PMCID: PMC8326116.
[7]: Awasthi D, Nagarkoti S, et,al. Glycolysis dependent lactate formation in neutrophils: A metabolic link between NOX-dependent and independent NETosis. Biochim Biophys Acta Mol Basis Dis. 2019 Dec 1;1865(12):165542. doi: 10.1016/j.bbadis.2019.165542. Epub 2019 Aug 29. PMID: 31473341.