LKT Labs

Biochemicals for Life Science Research

MLN-4924

Product ID M4454
Cas No. 905579-51-3
Purity ≥99%
Product Unit SizeCostQuantityStock
1 mg $120.30 In stock
5 mg $370.40 In stock
25 mg $1,296.30 Please Inquire
Bulk Quote

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Description

MLN4924 acts as a Nedd8-activating enzyme inhibitor, blocking proteasomal cullin protein neddylation by Cullin-RING E3 ubiquitin ligases. As a result, these proteins accumulate, inducing cell cycle arrest, senescence, autophagy, and/or apoptosis in cellular and animal models. This compound’s inhibition of neddylation decreases NF-κB-mediated release of pro-inflammatory cytokines TNF-α and IL-6. Pro-angiogenic HIF-1 also accumulates, potentially responsible for downstream inhibition of mTOR and the induction of autophagy.

Product Info

Cas No.

905579-51-3
Purity

≥99%
Formula

C21H25N5O4S
Formula Wt.

443.16
IUPAC Name

[(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamate
Synonym

MLN4924, Pevonedistat
Solubility

Ethanol (12.5 mg/ml) DMSO (20 mg/ml) DMF (20 mg/ml)
Appearance

White to off white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

M4454 MSDS PDF
Info Sheet

M4454 Info Sheet PDF

References

Yan ZH, Burkhardt A, Loke HK, et al. Quantifiable analysis of cellular pathway inhibition of a Nedd8-activating enzyme inhibitor, MLN4924, using AlphaScreen. Anal Biochem. 2013 Aug 15;439(2):109-15. PMID: 23624319.

Li L, Liu B, Dong T, et al. Neddylation pathway regulates the proliferation and survival of macrophages. Biochem Biophys Res Commun. 2013 Mar 15;432(3):494-8. PMID: 23416079.

Zhao Y, Xiong X, Jia L, et al. Targeting Cullin-RING ligases by MLN4924 induces autophagy via modulating the HIF1-REDD1-TSC1-mTORC1-DEPTOR axis. Cell Death Dis. 2012 Sep 6;3:e386. PMID: 22951983.

Luo Z, Pan Y, Jeong LS, et al. Inactivation of the Cullin (CUL)-RING E3 ligase by the NEDD8-activating enzyme inhibitor MLN4924 triggers protective autophagy in cancer cells. Autophagy. 2012 Nov;8(11):1677-9. PMID: 22874562.

Nawrocki ST, Griffin P, Kelly KR, et al. MLN4924: a novel first-in-class inhibitor of NEDD8-activating enzyme for cancer therapy. Expert Opin Investig Drugs. 2012 Oct;21(10):1563-73. PMID: 22799561.

Yang D, Tan M, Wang G, et al. The p21-dependent radiosensitization of human breast cancer cells by MLN4924, an investigational inhibitor of NEDD8 activating enzyme. PLoS One. 2012;7(3):e34079. PMID: 22457814.

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