GSK2801
GSK2801
CAS: 1619994-68-1
Molecular Formula: C20 H21 N O4 S
GSK2801 - Names and Identifiers
GSK2801 - Physico-chemical Properties
| Molecular Formula | C20 H21 N O4 S |
| Molar Mass | 371.45 |
| Density | 1.23±0.1 g/cm3(Predicted) |
| Solubility | 10 mM in DMSO |
| Storage Condition | -20°C |
| In vitro study | GSK2801 binds TAF1L(2) with an affinity K B of 0.31μM (K D : 3.2 μM) and a binding enthalpy change ΔH of −8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K B of 0.826 μM (K D : 1.1 μM) and ΔH of −9.8 kcal/mol. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC. |
| In vivo study | In order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. |
GSK2801 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
GSK2801 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.692 ml | 13.461 ml | 26.922 ml |
| 5 mM | 0.538 ml | 2.692 ml | 5.384 ml |
| 10 mM | 0.269 ml | 1.346 ml | 2.692 ml |
| 5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
Last Update：2024-01-02 23:10:35
GSK2801 - Reference Information
| biological activity | GSK2801 is an effective, selective, orally active and cell active acetyllysine competitive BAZ2A and BAZ2B bromide domain inhibitors with Kd values of 136 nM and 257 nM respectively. The selectivity of GSK2801 to BAZ2A/B is more than 50 times that of BRD4. |
| target | Kd: 136 nM (BAZ2A) and 257 nM (BAZ2B) |
| in vitro study | GSK2801 binds TAF1L(2) with an affinity K B of 0.31μM (K D : 3.2 μ M) and a binding enthalpy changeΔ H of − 8.6 kcal/mol. ITC experiments using the bromodomain of BRD9 results in the determination of an affinity K B of 0.826 μ M (K D : 1.1 μ m) and Δ h of − 9.8 kcal/mol. GSK2801 or RNAi knockdown of BAZ2A/B with JQ1 selectively displaced BRD2 at promoters/enhancers of ETS-regulated genes. In 2D cultures, enhances displacement of BRD2 from chromatin by combination drug treatment induced senescence. In spheroid cultures, combination treatment induces cleaved caspase-3 and cleaved PARP characteristic of apoptosis in tumor cells. Thus, GSK2801 blocks BRD2-driven transcription in combination with BET inhibitor and induces apoptosis of TNBC. |
| in vivo research | in order to determine the suitability of GSK2801 for in vivo experiments, pharmacokinetic parameters after intraperitoneal and oral dosing to male CD1 mice is measured. GSK2801 has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability. |
Last Update：2024-04-09 21:54:55
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