货号：A376712同义名：
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
3-Bromopyruvic acid是一种六磷酸葡萄糖激酶 II 抑制剂，具有有效的抗肿瘤活性。
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3-Bromopyruvate (3-BrPA) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-BrPA can induce growth inhibition in a dose-dependent pattern by cell apoptosis. 3-BrPA combined with rapamycin played a synergistic suppression role in NB cells, affected the cell apoptosis, cell cycle and the metabolic pathway[3]. Low concentration of 3-BrPA significantly affected both glutaminolysis and TCA cycle functions, through inhibition of isocitrate dehydrogenase, α-ketoglutarate dehydrogenase and succinate dehydrogenase. Additionally, 3-BrPA treatment significantly decreased the reduced status of thiol groups in HepG2 cells without proportional increase of oxidizing groups, suggesting that these chemical groups are the target of alkylation reactions induced by 3-BrPA[4]. 3-BrPA synergistically sensitized breast cancer cells to TRAIL‑induced apoptosis via the upregulation of death receptor 5 (DR5). And the protein levels of glucose‑related protein 78 (GRP78) and CCAAT‑enhancer‑binding protein homologous protein (CHOP) increased following treatment with 3-BrPA. 3-BrPA sensitized breast cancer cells to TRAIL via the AMPK (adenosine monophosphate-activated protein kinase)-mediated upregulation of DR5[5].
3-Bromopyruvic acid/3-溴丙酮酸 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary microglial cells
100 µM
24 hours
Inhibited LPS-induced NO production
J Neuroinflammation. 2021 Jun 9;18(1):129.
BV-2 microglial cells
100 µM
24 hours
Inhibited LPS-induced NO production
J Neuroinflammation. 2021 Jun 9;18(1):129.
Human erythrocytes
3.3 µM – 2 mM
1 minute
To study the kinetics of 3-BP transport in human erythrocytes. Results showed that 3-BP transport was linear during the initial 3-5 minutes and pH-dependent. The Km and Vm values were 0.89 mM and 0.94 mmol/(l cells x min), respectively. Transport was competitively inhibited by pyruvate and significantly inhibited by DIDS, SITS, CHC, and various polyphenols such as luteolin and quercetin.
Cell Mol Biol Lett. 2014 Jun;19(2):201-14.
MDA-MB-231
100 µM
1 or 24 hours
3BP was not toxic to MDA-MB-231 cells (>90% metabolic activity retained).
Cancer Metab. 2021 Oct 14;9(1):37.
BT20
100 µM
1 or 24 hours
3BP significantly reduced metabolic activity in BT20 cells (to 61% after 24-hour exposure).
Cancer Metab. 2021 Oct 14;9(1):37.
Pancreatic tumor organoids
100 µM
12 hours
To evaluate the effect of 3-BP on the metabolism of pancreatic tumor organoids, results showed significant inhibition of organoid growth and metabolic activity
Cell Death Discov. 2024 Mar 1;10(1):106.
THP-1 cells
25-100 µM
12 hours
Assessed the impact of 3-BP on THP-1 cell viability, found 25 μM 3-BP has no impact, 50 μM leads to 40% viability loss
Cells. 2020 May 8;9(5):1161.
Yeast cells
1-4 mM
1-4 hours
Assessed the impact of 3-BP on wild type cell viability, found 3 h incubation with 3 mM 3-BP is not toxic for the cells
To evaluate the effect of 3-bromopyruvic acid on OA FLS proliferation, migration, and cytokine secretion. Results showed that 3-bromopyruvic acid significantly inhibited OA FLS proliferation, migration, and secretion of IL-6.
To evaluate the effect of 3-bromopyruvic acid on RA FLS proliferation, migration, and cytokine secretion. Results showed that 3-bromopyruvic acid significantly inhibited RA FLS proliferation, migration, and secretion of IL-6 and MMP-3.
To evaluate the cytotoxicity of β-CD-3-BrPA and free 3-BrPA under normoxic and hypoxic conditions. Results showed that both drugs were more effective under hypoxic conditions in Suit-2 cells, though the difference was less pronounced compared to MiaPaCa-2 cells.
To evaluate the cytotoxicity of β-CD-3-BrPA and free 3-BrPA under normoxic and hypoxic conditions. Results showed that both drugs were more effective under hypoxic conditions in MiaPaCa-2 cells.
Clin Cancer Res. 2014 Dec 15;20(24):6406-17.
SiMCT1-BT20
200 µM
24 hours
SiMCT1-BT20 cells showed resistance to 3BP (72% viability vs 12% in wild type).
Evaluate the cytotoxicity of 3-BP on SKOV3 cells, results showed IC50 of 40.5 μM
Int J Mol Sci. 2021 Jan 12;22(2):709.
PEO1 ovarian cancer cells
18.7 µM (IC50)
24 hours
Evaluate the cytotoxicity of 3-BP on PEO1 cells, results showed IC50 of 18.7 μM
Int J Mol Sci. 2021 Jan 12;22(2):709.
KBM7 cells
50 µM
3 days
To determine the effect of MCT1 loss on 3-BrPA sensitivity, results showed MCT1-null cells were completely resistant to 3-BrPA.
Nat Genet. 2013 Jan;45(1):104-8.
SKOV-3 cells
10 µM–100 µM
3, 6, 24 hours
Evaluate the cytotoxicity and HK2 inhibition effect of 3-BPA on SKOV-3 cells. Results showed that liposomal formulations exhibited stronger inhibitory effects and cytotoxicity at 3, 6, and 24 hours post-administration.
Int J Nanomedicine. 2015 Jul 8;10:4405-23.
Breast cancer stem cells
5–40 μg/ml
4 hours
Evaluate the metabolic inhibition and photothermal therapy effect of 3BP on breast cancer stem cells, showing significant reduction in cell viability
Adv Healthc Mater. 2022 Apr;11(8):e2102272.
F98 rodent glioma cells
0.0001 mM–0.3 mM
48 and 72 hours
3-BrPA inhibited the growth and proliferation of F98 cells with IC50 values of 15.8–25.5 μM (48 hours) and 22.3–25.0 μM (72 hours).
Neuro Oncol. 2015 Jan;17(1):70-80.
9L rodent gliosarcoma cells
0.0001 mM–0.3 mM
48 and 72 hours
3-BrPA inhibited the growth and proliferation of 9L cells with IC50 values of 15.8–25.5 μM (48 hours) and 22.3–25.0 μM (72 hours).
Neuro Oncol. 2015 Jan;17(1):70-80.
U87 human glioblastoma cells
0.0001 mM–0.3 mM
48 and 72 hours
3-BrPA inhibited the growth and proliferation of U87 cells with IC50 values of 15.8–25.5 μM (48 hours) and 22.3–25.0 μM (72 hours).
Neuro Oncol. 2015 Jan;17(1):70-80.
RAW264.7 macrophages
200 μg/mL
48 hours
Evaluate the effect of MPB-3BP@CM NPs on macrophage polarization, results showed that MPB-3BP@CM NPs promoted macrophage polarization towards M1 phenotype
Signal Transduct Target Ther. 2024 Jun 12;9(1):158.
Panc-2 cells
20 µM and 40 µM
Significant decrease in HK2 expression level
Adv Healthc Mater. 2023 Dec;12(31):e2301815.
HT29 cells
200 μg/mL
6 hours
Evaluate the antitumor efficacy of MPB-3BP@CM NPs on HT29 cells, results showed that MPB-3BP@CM NPs significantly inhibited tumor cell proliferation and induced apoptosis
Signal Transduct Target Ther. 2024 Jun 12;9(1):158.
HCT116 cells
200 μg/mL
6 hours
Evaluate the antitumor efficacy of MPB-3BP@CM NPs on HCT116 cells, results showed that MPB-3BP@CM NPs significantly inhibited tumor cell proliferation and induced apoptosis
Signal Transduct Target Ther. 2024 Jun 12;9(1):158.
3-Bromopyruvic acid/3-溴丙酮酸 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
F344 rats
9L gliosarcoma allograft model
Intracranial implantation
1%, 5%, 10%, 25%, or 50%
Single implantation
To evaluate the efficacy of 5% 3-BrPA polymer wafer in the 9L gliosarcoma model. Results showed that 5% 3-BrPA wafer significantly increased survival (median survival 18 days, P=0.0027).
Single injection followed by photothermal therapy after 24 hours
Evaluate the metabolic inhibition and photothermal therapy effect of 3BP in vivo, showing significant tumor growth inhibition and reduced expression of CSC markers
Adv Healthc Mater. 2022 Apr;11(8):e2102272.
Balb/c nude mice
4T1 tumor model
Intravenous injection
10 mg/mL
Single injection, observed for 48 hours
Evaluate the in vivo distribution and therapeutic effects of 3BP@PLGA-IR780, showing effective accumulation in tumor sites and inhibition of tumor growth.
J Nanobiotechnology. 2021 Dec 20;19(1):440
BALB/c nude mice
HCT116 subcutaneous tumor model
Intravenous injection
30.0 mg/kg
Every other day for a total of three doses
Evaluate the antitumor efficacy of MPB-3BP@CM NPs in vivo, results showed that MPB-3BP@CM NPs significantly inhibited tumor growth and prolonged survival time
Signal Transduct Target Ther. 2024 Jun 12;9(1):158.
Mice
K/BxN serum transfer arthritis model
Intraperitoneal injection
5 mg/kg
Once daily for 6 days
To evaluate the effect of 3-bromopyruvic acid on arthritis severity. Results showed that 3-bromopyruvic acid significantly reduced clinical and histopathological scores of arthritis, decreased joint inflammation and cartilage damage.
Arthritis Rheumatol. 2016 Jul;68(7):1614-26.
Male athymic nude mice
Orthotopic xenograft model of human pancreatic ductal adenocarcinoma (PDAC)
Intraperitoneal injection
5 mg/kg
Daily for 4 weeks
To evaluate the antitumor efficacy and toxicity of β-CD-3-BrPA in vivo. Results showed that β-CD-3-BrPA significantly inhibited tumor growth without toxicity, while free 3-BrPA exhibited high toxicity.
Clin Cancer Res. 2014 Dec 15;20(24):6406-17.
Nude mice
Subcutaneous xenograft model
8 mg/kg
3 weeks
To evaluate the effect of MCT1 expression on tumor sensitivity to 3-BrPA, results showed MCT1 expression enhanced tumor sensitivity to 3-BrPA.
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