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How to Cite 1. For In-Text Citation (Materials & Methods): 2. For Key Resources Table: |
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| Formula | C33H31Cl2N3O5 |
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| Molecular Weight | 620.52 | CAS No. | 1433286-70-4 | ||||||||||||
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (161.15 mM) | ||||||||||||
| Ethanol | 3 mg/mL (4.83 mM) | ||||||||||||||
| Water | Insoluble | ||||||||||||||
| In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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| Description | Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells. | ||
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| In vitro | Compound 3i (666-15) could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for this compound is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and 0.31 μM. It inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction. |
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| In vivo | In an in vivo MDA-MB-468 xenograft model, compound 3i (666-15) completely suppresses tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of it is well tolerated in mice. |
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| MLK4 promotes glucose metabolism in lung adenocarcinoma through CREB-mediated activation of phosphoenolpyruvate carboxykinase and is regulated by KLF5 [ Oncogenesis, July 5, 2023, 35] | PubMed: 37407566 |
| JAK-STAT Signaling in Inflammatory Breast Cancer Enables Chemotherapy-Resistant Cell States [ Cancer Research, January 18, 2023, 264-284] | PubMed: 36409824 |
| Aspartate signaling drives lung metastasis via alternative translation [ Nature, January 1, 2025, 244-250] | PubMed: 39743589 |
| The delta subunit of the GABAA receptor is necessary for the GPT2-promoted breast cancer metastasis [ Theranostics, February 21, 2023, 1355-1369] | PubMed: 36923530 |
| Transcriptional Repression of CCL2 by KCa3.1 K+ Channel Activation and LRRC8A Anion Channel Inhibition in THP-1-Differentiated M2 Macrophages [ International Journal of Molecular Sciences, August 6, 2025, 7624] | |
| Renalase activates mitochondrial leak metabolism in response to cellular stress and to repair damage after injury [ bioRxiv, August 20, 2025, 2025.08.19.671117] | PubMed: 40894758 |
| Transcriptional Repression of CCL2 by KCa3.1 K+ Channel Activation and LRRC8A Anion Channel Inhibition in THP-1-Differentiated M2 Macrophages [ Int J Mol Sci, 2025, 26(15)7624] | PubMed: 40806751 |
| Renalase activates mitochondrial leak metabolism in response to cellular stress and to repair damage after injury [ bioRxiv, 2025, 2025.08.19.671117] | PubMed: 40894758 |
| Characterization of dipyridamole as a novel ferroptosis inhibitor and its therapeutic potential in acute respiratory distress syndrome management [ Theranostics, 2024, 14(18):6947-6968] | PubMed: 39629132 |
| Enforced activation of the CREB/KDM2B axis prevents alcohol-induced embryonic developmental delay [ Cell Rep, 2024, 43(12):115075] | PubMed: 39661511 |
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