E3 ligase Ligand 12
- Product Name
- E3 ligase Ligand 12
- CAS No.
- 2095244-42-9
- Chemical Name
- E3 ligase Ligand 12
- Synonyms
- cIAP1 ligand 1;E3 ligase Ligand 12;(S)-2-[Boc(methyl)amino]-N-[(S)-1-cyclohexyl-2-[(S)-2-[4-(3-hydroxybenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]propanamide;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;tert-butyl N-[(1S)-1-{[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(3-hydroxybenzoyl)-1,3-thiazol-2-yl]pyrrolidin-1-yl]-2-oxoethyl]carbamoyl}ethyl]-N-methylcarbamate;Carbamic acid, N-[(1S)-2-[[(1S)-1-cyclohexyl-2-[(2S)-2-[4-(3-hydroxybenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]amino]-1-methyl-2-oxoethyl]-N-methyl-, 1,1-dimethylethyl ester
- CBNumber
- CB88054706
- Molecular Formula
- C31H42N4O6S
- Formula Weight
- 598.75
- MOL File
- 2095244-42-9.mol
E3 ligase Ligand 12 Property
- 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
E3 ligase Ligand 12 Chemical Properties,Usage,Production
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_ _x000D_ 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_ _x000D_ 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
E3 ligase Ligand 12 Preparation Products And Raw materials
Raw materials
Preparation Products
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