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BX-795
| Product Name | BX-795 |
| Price: | Inquiry |
| Catalog No.: | CN00371 |
| CAS No.: | 702675-74-9 |
| Molecular Formula: | C23H26IN7O2S |
| Molecular Weight: | 591.47 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | O=C(N1CCCC1)Nc1cccc(c1)Nc1ncc(c(n1)NCCCNC(=O)c1cccs1)I |
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| Description | BX795 is a potent and selective PDK1 inhibitor with an IC50 of 6 nM, showing 50-fold selectivity over PKA, PKC, c-Kit, GSK3β etc. |
| Target | IC50: 2 nM (TBK1), 6 nM (PDK1) |
| In Vitro | BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively[1]. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation[3]. |
| Cell Assay | Cells seeded at a low density (1,500-3,000 cells/well, 0.1 mL/well, 96-well plates) are incubated overnight. Compound treatments are made by adding 10 μL/well of the compound in 1% dimethyl sulfoxide and growth medium (final concentration of dimethyl sulfoxide, 0.1%), followed by brief shaking. Treated cells are incubated for 72 hours, and viability is measured by the addition of 10 μL of the metabolic dye WST-1. The WST-1 signal is read in a plate reader at 450 nm, and a no cell, or zero time cell, background is subtracted to calculate the net signal. Results are reported as the average±S.E. of two or more replicates. |
| Density | 1.6±0.1 g/cm3 |
| Exact Mass | 591.091309 |
| PSA | 139.52000 |
| LogP | 2.73 |
| Storage condition | 2-8°C |