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5.05477

MLN4924

≥98% (HPLC), solid, NAE inhibitor, Calbiochem®

Synonym(s):

NAE Inhibitor, MLN4924, ((1S,2S,4R)-4-(4-((1S)-2,3-Dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulphamate, NEDD8-Activating Enzyme Inhibitor, NEDD8-Activating Enzyme Inhibitor, ((1S,2S,4R)-4-(4-((1S)-2,3-Dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl}-2-hydroxycyclopentyl)methyl sulphamate

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Size/SKUAvailabilityPrice
5 mg
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$264.00

About This Item

Empirical Formula (Hill Notation):
C21H25N5O4S
CAS Number:
905579-51-3
Molecular Weight:
443.52
MDL number:
MFCD00003858
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$264.00

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Product Name

NAE Inhibitor, MLN4924,

assay

≥98% (HPLC)

Quality Segment

100

form

solid

potency

4.7 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

light beige

solubility

DMSO: 100 mg/mL

storage temp.

2-8°C

General description

MLN4924 is a specific small molecule NEDD8-activating enzyme (NAE) inhibitor. Neddylation involves adding Nedd8, an ubiquitin-like molecule, to target proteins. This post-translational protein modification is associated with cancer development. MLN4924 is known to induce dose-dependent anti-proliferation, anti-migration, anti-invasion in ccRCC cells. MLN4924 is a cell-permeable AMP mimetic. The mechanism of action is found to target 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 = 4.7 nM), 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 = 90 nM 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 50 nM to 1.03 µM) in vitro and in murine xenograft models (30 to 60 mg/kg via s.c.) in vivo via apoptosis induction.

Application

MLN4924 has been used as a neddylation inhibitor:

  • to treat cell lines stably expressing a GaLV/MLV chimera construct in order to study its effects on viral transduction and infectivity
  • to study its effects on the accumulation of LCMT1, suggesting a potential role in regulating LCMT1 stability and degradation in LNCaP cells
  • to study UBX-390-mediated degradation of androgen receptor (AR) via proteasomal action in a prostate cancer cell line

Biochem/physiol Actions

Cell permeable: yes
Primary Target
NEDD8-Activating Enzyme
Reversible: no

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
Use only fresh DMSO for reconstitution.

Other Notes

Milhollen, M.A., et al. 2010. Blood116, 1515.

Brownell, J.E., et al. 2010. Mol. Cell37, 102.

Soucy, T.A., et al. 2009. Nature458, 73.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

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Sigma-Aldrich

505477

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Sigma-Aldrich

324890

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Sigma-Aldrich

531372

Caspase-1/4 Inhibitor, VX-765

description

-

description

The Akt Inhibitor XVIII, SC66 controls the biological activity of Akt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

description

The E-64 Protease Inhibitor, also referenced under CAS 66701-25-5, controls the biological activity of E-64 Protease. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

description

-

form

solid

form

solid

form

solid

form

solid

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

200

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

solubility

DMSO: 100 mg/mL

solubility

DMSO: 25 mg/mL

solubility

water: 20 mg/mL, DMSO: 25 mg/mL

solubility

DMSO: 100 mg/mL

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

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