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

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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

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Hazard and Precautionary Statements (GHS)

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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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E3 ligase Ligand 12 Suppliers

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2095244-42-9, E3 ligase Ligand 12Related Search:

Acetic acid, 2-[2-[2-[2-[3-[[2-[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-[[(1,1-dimethylethoxy)carbonyl]methylamino]-1-oxopropyl]amino]acetyl]-2-pyrrolidinyl]-4-thiazolyl]carbonyl]phenoxy]ethoxy]ethoxy]ethoxy]- E3 ligase Ligand-Linker Conjugates 37 E3 ligase Ligand-Linker Conjugates 41 E3 ligase Ligand-Linker Conjugates 33 E3 ligase Ligand 11 E3 ligase Ligand-Linker Conjugates 36 E3 ligase Ligand-Linker Conjugates 39 E3 ligase Ligand-Linker Conjugates 34 E3 ligase Ligand-Linker Conjugates 38

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

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

(S)-2-[Boc(methyl)amino]-N-[(S)-1-cyclohexyl-2-[(S)-2-[4-(3-hydroxybenzoyl)-2-thiazolyl]-1-pyrrolidinyl]-2-oxoethyl]propanamide

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

2095244-42-9