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Submit ReviewBMS 195614 is a neutral retinoic acid receptor (RAR) α-selective antagonist (Ki = 2.5 nM). Displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. Antagonizes agonist-induced coactivator (CoA) recruitment.
分子量 | 448.51 |
公式 | C29H24N2O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 182135-66-6 |
PubChem ID | 445091 |
InChI Key | WGLMBRZXZDAQHP-UHFFFAOYSA-N |
Smiles | O=C(NC4=CC=C(C(O)=O)C=C4)C3=CC1=C(C=C3)C(C)(C)CC=C1C2=CN=C(C=CC=C5)C5=C2 |
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 | 11.21 | 25 |
以下数据基于产品分子量 448.51。 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 |
---|---|---|---|
0.25 mM | 8.92 mL | 44.59 mL | 89.18 mL |
1.25 mM | 1.78 mL | 8.92 mL | 17.84 mL |
2.5 mM | 0.89 mL | 4.46 mL | 8.92 mL |
12.5 mM | 0.18 mL | 0.89 mL | 1.78 mL |
参考文献是支持产品生物活性的出版物。
Gehin et al (1999) Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem.Biol. 6 519 PMID: 10421757
Germain et al (2009) Differential action on coregulator interaction defines retinoid agonists and neutral antagonists. Chem.Biol. 16 479 PMID: 19477412
Schoenermark et al (1999) Retinoid-mediated suppression of tumor invasion and matrix metalloproteinase synthesis. Ann.N.Y.Acad.Sci. 30 878
If you know of a relevant reference for BMS 195614, please let us know.
关键词: BMS 195614, BMS 195614 supplier, BMS195614, retinoic, acid, receptor, RAR, alpha, α, RARa, antagonists, neutral, selective, BMS614, 253310-42-8, Retinoic, Acid, Receptors, 3660, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 BMS 195614 的部分引用包括:
Johansson et al (2013) Retinoic acid receptor alpha is associated with tamox. resistance in breast cancer. Nat Commun 4 2175 PMID: 23868472
Flamini et al (2014) Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor beta. J Cell Mol Med 18 1113 PMID: 24720764
Gerald et al (2016) All Trans Retinoic Acid, Transforming Growth Factor β and Prostaglandin E2 in Mouse Plasma Synergize with Basophil-Secreted Interleukin-4 to M2 Polarize Murine Macrophages. PLoS One 11 e0168072 PMID: 27977740
Chen et al (2013) A critical role for the retinoic acid signaling pathway in the pathophysiology of gastrointestinal graft-versus-host disease. Blood 121 3970 PMID: 23529927
Liang et al (2013) Retinoic acid inhibits CD25+ dendritic cell expansion and γδ T-cell activation in experimental autoimmune uveitis. Invest Ophthalmol Vis Sci 54 3493 PMID: 23611991
Mickaël M et al (2020) A Comprehensive Map of the Monocyte-Derived Dendritic Cell Transcriptional Network Engaged upon Innate Sensing of HIV. Cell Rep 30 914-931.e9 PMID: 31968263
Tobias M et al (2019) Retinoic acid worsens ATG10-dependent autophagy impairment in TBK1-mutant hiPSC-derived motoneurons through SQSTM1/p62 accumulation. Autophagy 15 1719-1737 PMID: 30939964
Metzler et al (2018) RDH10-mediated retinol metabolism and RARα-mediated retinoic acid signaling are required for submandibular salivary gland initiation. Development 145 PMID: 29986869
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