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Submit Review666-15 is a potent and selective CREB inhibitor (IC50 = 81 nM). Inhibits cancer cell growth, without harming normal cells (up to 1 μM). Completely suppresses tumor growth in a breast cancer xenograft model.
666-15 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 620.52 |
公式 | C33H30ClN3O5.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 1433286-70-4 |
PubChem ID | 71566396 |
InChI Key | LELLCPHHYHLWBH-UHFFFAOYSA-N |
Smiles | NCCCOC1=CC2=CC=CC=C2C=C1C(NCCOC3=C(C(NC4=CC=C(Cl)C=C4O)=O)C=C(C=CC=C5)C5=C3)=O.Cl |
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 | 62.05 | 100 |
以下数据基于产品分子量 620.52。 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 |
---|---|---|---|
1 mM | 1.61 mL | 8.06 mL | 16.12 mL |
5 mM | 0.32 mL | 1.61 mL | 3.22 mL |
10 mM | 0.16 mL | 0.81 mL | 1.61 mL |
50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
参考文献是支持产品生物活性的出版物。
Xie et al (2015) Identification of a potent inhibitor of CREB-mediated gene transcription with efficacious in vivo anticancer activity J.Med.Chem. 58 5075 PMID: 26023867
Li et al (2016) Systemic inhibition of CREB is well-tolerated in vivo. Sci.Rep. 6 34513 PMID: 27694829
If you know of a relevant reference for 666-15, please let us know.
关键词: 666-15, 666-15 supplier, cyclic, adenosine, monophosphate, cAMP, response, element, binding, protein, CREB, inhibitors, inhibits, breast, cancer, potent, selective, Other, Transcription, Factors, 5661, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 666-15 的部分引用包括:
Phua (2017) Angiopoietin-like 4 mediates colonic inflammation by regulating chemokine transcript stability via tristetraprolin. Sci Rep 7 44351 PMID: 28287161
Israel et al (2021) Disruption of innate defense responses by endoglycosidase HPSE promotes cell survival. JCI Insight 6 PMID: 33621216
Asya et al (2021) Optogenetic activation of local colonic sympathetic innervations attenuates colitis by limiting immune cell extravasation. Immunity 54 1022-1036.e8 PMID: 33932356
Zhou et al (2019) Microglia Are Indispensable for Synaptic Plasticity in the Spinal Dorsal Horn and Chronic Pain. Cell Rep 27 3844 PMID: 31242418
Jiehan et al (2022) G protein-coupled receptor 151 regulates glucose metabolism and hepatic gluconeogenesis. Nat Commun 13 7408 PMID: 36456565
Ping et al (2022) Molecular and cellular mechanisms for differential effects of chronic social isolation stress in males and females. Mol Psychiatry 27 3056-3068 PMID: 35449296
Qinkun et al (2022) Cardiac natriuretic peptide deficiency sensitizes the heart to stress-induced ventricular arrhythmias via impaired CREB signalling. Cardiovasc Res 118 2124-2138 PMID: 34329394
Qing et al (2022) MTAP loss correlates with an immunosuppressive profile in GBM and its substrate MTA stimulates alternative macrophage polarization. Sci Rep 12 4183 PMID: 35264604
Konrad et al (2022) SS18-SSX drives CREB activation in synovial sarcoma. Cell Oncol (Dordr) 45 399-413 PMID: 35556229
Juan L et al (2019) PML hyposumoylation is responsible for the resistance of pancreatic cancer. FASEB J 33 12447-12463 PMID: 31557059
Reza et al (2019) Signal Transduction of Improving Effects of Ibudilast on Methamphetamine Induced Cell Death. Asian Pac J Cancer Prev 20 2763-2774 PMID: 31554375
Andreas et al (2020) Osmotic and hypoxic induction of osteopontin in retinal pigment epithelial cells: Involvement of purinergic receptor signaling. Mol Vis 26 188-203 PMID: 32214785
Hwa-Jung et al (2020) Mycobacterium avium subsp. paratuberculosis MAP1889c Protein Induces Maturation of Dendritic Cells and Drives Th2-biased Immune Responses. Cells 9 PMID: 32290379
Lara et al (2020) A dopamine-induced gene expression signature regulates neuronal function and cocaine response. Sci Adv 6 eaba4221 PMID: 32637607
Chris et al (2020) Neuronal hyperexcitability is a DLK-dependent trigger of herpes simplex virus reactivation that can be induced by IL-1. Elife 9 PMID: 33350386
Martin et al (2020) A high-throughput CRISPR interference screen for dissecting functional regulators of GPCR/cAMP signaling. PLoS Genet 16 e1009103 PMID: 33052901
Asma et al (2020) Resolvin E1 is a pro-repair molecule that promotes intestinal epithelial wound healing. Proc Natl Acad Sci U S A 117 9477-9482 PMID: 32300016
Cirle A et al (2023) Adenosine receptors differentially mediate enteric glial cell death induced by Clostridioides difficile Toxins A and B. Front Immunol 13 956326 PMID: 36726986
Hamnett et al (2019) Vasoactive intestinal peptide controls the suprachiasmatic circadian clock network via ERK1/2 and DUSP4 signalling. Nat Commun 10 542 PMID: 30710088
Kleiner et al (2018) Activator protein-1 contributes to the NaCl-induced expression of VEGF and PlGF in RPE cells. Mol Vis 24 647 PMID: 30310263
O'Reilly et al (2019) Nutritionally Derived Metabolic Cues Typical of the Obese Microenvironment Increase Cholesterol Efflux Capacity of Adipose Tissue Macrophages. Mol Nutr Food Res 63 e1800713 PMID: 30411491
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