7ACC2
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
7ACC2, a carboxycoumarin derivative, is a potent inhibitor of monocarboxylate transporter 1 (MCT1), with an IC50 value of ~ 10 nM for lactate uptake in the human cervix carcinoma cell line SiHa. The family of MCT is composed of 14 members, among which only four isoforms (i.e. MCT1-4) have been documented to act as proton-linked transporters carrying short chain monocarboxylates such as lactate and pyruvate across cell membranes. In cancer cells, MCT1 and MCT4 are the most widely expressed, and MCT1 shows a better affinity for L-lactate than MCT4, enabling lactate entry into oxidative tumor cells. Thus, MCT1 blockade could serve as a potential therapeutic strategy to limit cancer progression. In addition, 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport, which interferes with pyruvate import into mitochondria and ultimately prevents extracellular lactate uptake as efficiently as a MCT1 inhibitor.
References:
1. Draoui N, Schicke O, Fernandes A, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorganic & Medicinal Chemistry, 2013, 21(22): 7107-7117.
2. Corbet C, Bastien E, Draoui N, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nature Communications, 2018, 9(1): 1208.
Storage | Store at -20°C |
M.Wt | 309.32 |
Cas No. | 1472624-85-3 |
Formula | C18H15NO4 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥47.5 mg/mL in DMSO |
Chemical Name | 7-(benzyl(methyl)amino)-2-oxo-2H-chromene-3-carboxylic acid |
SDF | Download SDF |
Canonical SMILES | OC(C(C(O1)=O)=CC2=C1C=C(N(C)CC3=CC=CC=C3)C=C2)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Cell experiment:[1] | |
Cell lines |
SiHa cells |
Reaction Conditions |
72 h incubation |
Applications |
7ACC2 inhibited SiHa cells proliferation by reducing lactate uptake (an MCT1-dependent process), with an EC50 value of 0.22 μM. |
Animal experiment:[1,2] | |
Animal models |
A SiHa mouse xenograft model |
Dosage form |
3 mg/kg Intraperitoneal administration |
Applications |
A single dose of 7ACC2 (3 mg/kg) to mice led to a Cmax of 1246 ng/ml (4 μM) in a very short time (Tmax = 10 min) associated with a plasma half-life of 4.5 h. 7ACC2 (3 mg/kg, q.d., for 5 and 10 days), when combined with radiotherapy, significantly delayed tumor growth in a SiHa mouse xenograft model. |
Note |
The technical data provided above is for reference only. |
References: 1. Draoui N, Schicke O, Fernandes A, et al. Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorganic & Medicinal Chemistry, 2013, 21(22): 7107-7117. 2. Corbet C, Bastien E, Draoui N, et al. Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects. Nature Communications, 2018, 9(1): 1208. |
质量控制和MSDS
- 批次: