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About This Item
Empirical Formula (Hill Notation):
C68H94N4O8
CAS Number:
Molecular Weight:
1095.50
UNSPSC Code:
12352200
Assay:
≥96% (HPLC)
Form:
powder
Pricing and availability is not currently available.
Quality Segment
assay
≥96% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Biochem/physiol Actions
EL133 is a highly cell-permeable Polymerization-Inducing Chimera (PINCH) rationally designed to exploit protein symmetry (homodimerism) as a selective vulnerability for functional protein knockout. Comprising two bardoxolone (BDX) moieties conjugated via a precise short polyethylene glycol (PEG2) linker, EL-133 acts as a covalent molecular bridge targeting Cysteine 151 (C151) within the Keap1 BTB domain to induce supramolecular assembly. This mechanism drives the rapid (>90%) and high-specificity precipitation of Keap1 from the soluble cytosolic fraction (insolubility EC50 = 102 nM in OCI-AML2; effective >500 nM), with global proteomics confirming COL1A1 as the sole significant off-target. By locking Keap1 in an inactive polymeric state, EL133 triggers robust, proteasome-independent activation of the Nrf2 pathway and Antioxidant Response Element (ARE) genes, resulting in distinct, sustained upregulation of NAD(P)H quinone dehydrogenase 1 (NQO1). Distinct from PROTACs or simple inhibitors, EL-133 functions as an autonomous sequestrator independent of cellular degradation machinery (lysosome/proteasome) or E3 ligase co-expression, effectively circumventing resistance mechanisms associated with effector dependency.
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This Item | |||
|---|---|---|---|
| description ≥96% (HPLC) | description - | description IgG fraction of antiserum | description Prestige Antibodies® Powered by Atlas Antibodies, affinity isolated antibody, buffered aqueous glycerol solution |
| assay ≥96% (HPLC) | assay - | assay - | assay - |
| form powder | form liquid | form buffered aqueous solution | form buffered aqueous glycerol solution |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level 100 |
| storage temp. -10 to -25°C | storage temp. −20°C | storage temp. −20°C | storage temp. −20°C |
| solubility DMSO: 2 mg/mL, clear | solubility - | solubility - | solubility - |
| color white to beige | color - | color - | color - |
Signal Word
Warning
Hazard Codes
Precautionary Statements
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - Skin Sens. 1B
Storage Class
11 - Combustible Solids
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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