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ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP, it potently inhibited the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively. ASTX660 induced degradation of cIAP1, with an EC50 of 0.22 nmol/L after 2 hours of treatment. ASTX660 treatment of WSU-DLCL2 cells leads to significant cIAP1 and cIAP2 degradation after 1 and 4 hours. ASTX660 is orally bioavailable in mice and demonstrates prolonged antagonism of XIAP and cIAP1 in vivo.
| Molecular Weight | 539.68 |
| Formula | C30H42FN5O3 |
| CAS Number | 1799328-86-1 |
| Solubility (25°C) | DMSO ≥ 80 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 |
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| 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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