| Identification | Back Directory | [Name]
E3 ligase Ligand 12 | [CAS]
2095244-42-9 | [Synonyms]
cIAP1 ligand 1
E3 ligase Ligand 12
tert-Butyl ((S)-1-(((S)-1-cyclohexyl-2-((S)-2-(4-(3-hydroxybenzoyl)thiazol-2-yl)pyrrolidin-1-yl)-2-oxoethyl)amino)-1-oxopropan-2-yl)(methyl)carbamate | [Molecular Formula]
C31H42N4O6S | [MDL Number]
MFCD32215338 | [MOL File]
2095244-42-9.mol | [Molecular Weight]
598.75 |
| Chemical Properties | Back Directory | [Boiling point ]
805.4±65.0 °C(Predicted) | [density ]
1.245±0.06 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);167.01(Max Conc. mM) | [form ]
Solid | [pka]
8.78±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
LCL-161-phenol is a functionalized IAP ligand for PROTACs. | [in vitro]
Through derivatization of the SNIPER(AR) molecule at the AR ligand and IAP ligand and linker, this study developed 42a (SNIPER(AR)-51), which shows effective protein knockdown activity against AR. Consistent with the degradation of the AR protein, 42a inhibits AR-mediated gene expression and proliferation of androgen-dependent prostate cancer cells. In addition, 42a efficiently induces caspase activation and apoptosis in prostate cancer cells, which was not observed in the cells treated with AR antagonists._x000D_
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Reference: J Med Chem. 2018 Jan 25;61(2):543-575. https://pubmed.ncbi.nlm.nih.gov/28594553/ | [in vivo]
This study recently developed a protein knockdown system based on hybrid small molecule SNIPERs (Specific and Nongenetic IAP-dependent Protein Erasers) that recruit inhibitor of the apoptosis protein (IAP) ubiquitin ligases to specifically degrade targeted proteins. By incorporating a high affinity IAP ligand, this study developed a novel SNIPER against estrogen receptor α (ERα), SNIPER(ER)-87, that has a potent protein knockdown activity. The SNIPER(ER) reduced ERα levels in tumor xenografts and suppressed the growth of ERα-positive breast tumors in mice._x000D_
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Reference: J Biol Chem. 2017 Mar 17;292(11):4556-4570. https://pubmed.ncbi.nlm.nih.gov/28154167/ | [target]
cIAP1 ligand 1 is the LCL161 derivative based IAP ligand. cIAP1 ligand 1 can be connected to the ABL ligand for protein by a linker to form SNIPER. | [storage]
Store at -20°C |
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