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How to Cite 1. For In-Text Citation (Materials & Methods): 2. For Key Resources Table: |
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Technical Data
| Formula | C28H31N5O2 |
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| Molecular Weight | 469.58 | CAS No. | 2755823-12-0 | |
| Solubility (25°C)* | In vitro | DMSO | 94 mg/mL (200.17 mM) | |
| Ethanol | 4 mg/mL (8.51 mM) | |||
| Water | Insoluble | |||
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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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Biological Activity
| Description | SETDB1‑TTD‑IN‑1 is a SETDB1 methyltransferase activator and a competitive inhibitor of the SETDB1 tandem tudor domain (SETDB1‑TTD), binding SETDB1‑TTD with a Kd of 88 nM and showing strong selectivity over other tudor and bromodomain proteins. It enhances SETDB1 catalytic activity, promoting Akt1 Lys64 methylation and subsequent Akt1 Thr308 phosphorylation and activation. By blocking SETDB1‑TTD binding to histone H3 peptides, it drives global gene‑expression changes and functions as a tool compound to study SETDB1‑TTD, including in breast cancer models. |
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Protocol (from reference)
References
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