All AbMole products are for research use only, cannot be used for human consumption.
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 |
|---|
| AT-406
Xevinapant (Debio1143,AT-406, SM-406) is a potentially first-in-class, highly potent oral antagonist of inhibitor of apoptosis protein (IAP), which not only promotes cancer cell death by inhibiting IAP, but also It can enhance the anti-tumor immune response by inhibiting IAP. |
| Birinapant
Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. |
| BV6
BV6 is a small molecule Smac analog that antagonizes cIAP1 and XIAP. |
| LCL161
LCL161 is an orally bioavailable SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP). LCL161 enhanced the proapoptotic effects of nilotinib and PKC412, against leukemic disease in vitro and potentiated the activity of both kinase inhibitors against leukemic disease in vivo. |
| Embelin
Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties. Specifically antagonizes XIAP-mediated inhibition of caspase-9 activation by directly targeting the Smac and caspase-9 binding domain BIR3 (IC50 = 4.1 uM in a competitive binding assay with Smac peptide). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
