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Submit ReviewBMS 303141 is an ATP citrate lyase (ACL) inhibitor (IC50 = 0.13 μM for human recombinant ACL); blocks lipid synthesis (IC50 = 8 μM in HepG2 cells). Displays no cytotoxicity up to a concentration of 50 μM. Lowers plasma glucose and triglycerides in a mouse model of hyperlipidemia; reduces cell proliferation in HepG2 and Huh-7 cell lines and in PD-1 deficient lymphomas. Orally bioavailable.
分子量 | 424.3 |
公式 | C19H15Cl2NO4S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 943962-47-8 |
PubChem ID | 90488956 |
InChI Key | LIZVMVYXZWADCK-UHFFFAOYSA-N |
Smiles | ClC1=CC(Cl)=C(O)C=C1S(NC2=C(C3=CC=CC=C3)C=CC(OC)=C2)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 4.24 | 10 | |
ethanol | 21.21 | 50 |
以下数据基于产品分子量 424.3。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.71 mL | 23.57 mL | 47.14 mL |
2.5 mM | 0.94 mL | 4.71 mL | 9.43 mL |
5 mM | 0.47 mL | 2.36 mL | 4.71 mL |
25 mM | 0.09 mL | 0.47 mL | 0.94 mL |
参考文献是支持产品生物活性的出版物。
Li et al (2007) 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg.Med.Chem.Lett. 17 3208 PMID: 17383874
Ma et al (2009) A novel direct homogeneous assay for ATP citrate lyase. J.Lipid Res. 50 2131 PMID: 19286649
Wartewig et al (2023) PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma. Nat.Cancer 4 1508 PMID: 37723306
If you know of a relevant reference for BMS 303141, please let us know.
关键词: BMS 303141, BMS 303141 supplier, BMS303141, ATP, citrate, lyases, inhibits, inhibitors, plasma, glucose, triglycerides, orally, bioavailable, synthases, transferases, ACLY, immunometabolism, Citrate, Lyase, 4609, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BMS 303141 的部分引用包括:
Márquez et al (2019) Tricarboxylic Acid Cycle Activity and Remodeling of Glycerophosphocholine Lipids Support Cytokine Induction in Response to Fungal Patterns. Cell Rep 27 525 PMID: 30970255
Shah et al (2016) Targeting ACLY sensitizes castration-resistant prostate cancer cells to AR antagonism by impinging on an ACLY-AMPK-AR feedback mechanism. Oncotarget 7 43713 PMID: 27248322
Bernhard et al (2022) Impact of ATP-citrate lyase catalytic activity and serine 455 phosphorylation on histone acetylation and inflammatory responses in human monocytic THP-1 cells. Front Immunol 13 906127 PMID: 36439127
Lars et al (2020) Cytoplasmic Citrate Flux Modulates the Immune Stimulatory NKG2D Ligand MICA in Cancer Cells. Front Immunol 11 1968 PMID: 32849657
Dong et al (2020) Autophagy deficiency promotes triple-negative breast cancer resistance to T cell-mediated cytotoxicity by blocking tenascin-C degradation. Nat Commun 11 3806 PMID: 32732922
Wartewig et al (2023) PD-1 instructs a tumor-suppressive metabolic program that restricts glycolysis and restrains AP-1 activity in T cell lymphoma. Nat.Cancer 4 1508 PMID: 37723306
Namgaladze et al (2018) Polarization of Human Macrophages by Interleukin-4 Does Not Require ATP-Citrate Lyase. Front Immunol 9 2858 PMID: 30568658
Catherine A et al (2021) Fructose reprogrammes glutamine-dependent oxidative metabolism to support LPS-induced inflammation. Nat Commun 12 1209 PMID: 33619282
Douglas R et al (2021) Polyamine metabolism is a central determinant of helper T cell lineage fidelity. Cell 184 4186-4202.e20 PMID: 34216540
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