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MLN-4924 hydrochloride

Chemical Structure : MLN-4924 hydrochloride

CAS No.: 1160295-21-5

MLN-4924 hydrochloride (Pevonedistat hydrochloride;TAK-924 hydrochloride)

Catalog No.: PC-42613Not For Human Use, Lab Use Only.

MLN-4924 (Pevonedistat) hydrochloride is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.

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Biological Activity

MLN-4924 (Pevonedistat) hydrochloride is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.
MLN-4924 also inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 of 1.5 and 8.2 uM, respectively.
MLN-4924 disrupts CRL-mediated protein turnover leading to apoptosis in HCT116 cells.
MLN-4924 suppresses the growth of human tumor xenografts in mice (30-60 mg/kg).

Physicochemical Properties

M.Wt 479.9803
Formula C21H26ClN5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 160 mg/mL

Chemical Name/SMILES

Sulfamic acid, [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl ester, hydrochloride (1:1)

References

1. Soucy TA, et al. Nature. 2009 Apr 9;458(7239):732-6.

2. Milhollen MA, et al. Blood. 2010 Sep 2;116(9):1515-23.

3. Brownell JE, et al. Mol Cell. 2010 Jan 15;37(1):102-11.

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