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GDC-0152 is a small-molecule IAP antagonist that triggers tumor cell apoptosis by selectively antagonizing IAPs. GDC-0152 binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with K(i) values of 28, 14, 17, and 43 nM, respectively. GDC-0152 inhibits tumor growth when dosed orally in the MDA-MB-231 breast cancer xenograft model. GDC-0152 induces activation of caspase-3/7, and lead to decreased viability of breast cancer cells without affecting normal mammary epithelial cells. GDC-0152 induces NF-κB transcriptional activity leading to expression of several chemokines and cytokines, of which tumor necrosis factor alpha (TNF-α) is the most important for single-agent tumor activity.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231, mormal HMECs cell lines |
| Preparation method | Cell Viability and Caspase Activation Assays Human breast carcinoma MDA-MB-231 were obtained from ATCC. Normal human mammary epithelial cells (HMECs) were obtained from Cambrex Corp. Cells were dissociated from tissue culture flasks by incubation with Accutase for 5–10 minutes. Detached cells were washed with phosphate-buffered saline (PBS) and were resuspended in assay media (MDA-MB-231 cells: RPMI1640 supplemented with 10% fetal bovine serum and 2 mM L-glutamine [AbMole, M5740]) or culture media. Cells were placed in tissue culture-treated, white-wall or black-wall, clear-bottom, 96-well plates at 1 × 10^4 cells/well in a volume of 50 μL. The plates were incubated at 37°C and 5% CO2 overnight, the media was removed, and 1 or it's enantiomer were added in assay media. Cells cultured in white-wall, clear-bottom plates were incubated at 37°C and 5% CO2 for 3 days before cell viability was measured using the CellTiter-Glo luminescent cell viability assay kit according to the manufacturer's instructions. Cells seeded in black-wall, clear-bottom plates were incubated at 37°C and 5% CO2 for 3–24 hours before caspase-3 and -7 homogeneous activities were assessed using the Apo-ONE caspase-3/7 assay kit according to the manufacturer's instructions. |
| Concentrations | |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | Human breast cancer MDA-MB-231 cells tumor xenograft mice |
| Formulation | PBS |
| Dosages | 4.0 ml/kg |
| Administration | oral gavage |
| Molecular Weight | 498.64 |
| Formula | C25H34N6O3S |
| CAS Number | 873652-48-3 |
| Solubility (25°C) | DMSO 79 mg/mL Ethanol 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related IAP Products |
|---|
| AZD5582 dihydrochloride
AZD5582 dihydrochloride is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. |
| Sanggenon G
Sanggenon G is a cell-permeable and potent inhibitor of X-linked inhibitor of apoptosis protein (XIAP). |
| TD-1092
TD-1092 is a pan-inhibitor of apoptosis (IAP) degrader with two different types of E3 ligase conjugates, IAP and CRBN, that induces proteasomal degradation of cIAP2 and XIAP in a CRBN-dependent manner. TD1092 also activates apoptotic proteases (apoptosis 3/7) and leads to apoptosis by promoting IAP degradation. In addition, TD1092 also blocks the TNFα-mediated NF-κB signaling pathway and inhibits the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can be used as a PROTAC for cancer research. |
| LBW242
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells. |
| UC-112
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor. UC-112 potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM). |
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