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MilliporeSigma™ Calbiochem™ NAE Inhibitor, MLN4924

Catalog No. 5054770001 Shop All MilliporeSigma Products
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50-547-70001 5 mg
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Catalog No. 50-547-70001 Supplier MilliporeSigma™ Supplier No. 5054770001
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Description

NAE Inhibitor, MLN4924, CAS 951950-33-7, is an AMP mimetic that forms a NAE-catalyzed NEDD8 adduct, which acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7nM).

A cell-permeable AMP mimetic that targets the NEDD8-activating E1 enzyme NAE nucleotide-binding site and undergoes a NAE-catalyzed covalent NEDD8 adduct formation, the adduct in turn acts as a tight-binding, ATP-competitive NAE inhibitor (IC50 = 4.7nM), exhibiting much reduced or little potency against UAE/UBA1, UBA6/UBE1L2, SAE, ATG7, adenosine receptors A1/A2A/A2B/A3, or a panel of 12 cellular kinases. Selectively reduces cellular Ubc12-NEDD8, but not Ubc9-SUMO or Ubc10-Ub, thioester formation (ICmax = 90nM in HCT-116 cultures in 24 h), resulting in cullin-RING ligases substrates elevation. Shown to inhibit the growth of various cancer cells both in cultures (IC50 from 50nM to 1.03μM) in vitro and in murine xenograft models (30 to 60mg/kg via s.c.) in vivo via apoptosis induction.
TRUSTED_SUSTAINABILITY

Specifications

Color Light Beige
Description 98% by HPLC
Target Proteins NEDD8-Activating Enzyme
Molecular Formula C21H25N5O4S
Solubility DMSO
Content And Storage Protect from light
Form Solid
Quantity 5 mg
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