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BioChemicals
MLN4924 (hydrochloride)
tcsc0068
Pevonedistat hydrochloride
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$
171.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
Pevonedistat hydrochloride (MLN4924 hydrochloride) is a potent and selective NEDD8-activating enzyme (
NAE
) inhibitor, with an
IC
50
of 4.7 nM.
IC50 & Target: IC50: 4.7 nM (NAE)
In Vitro:
Pevonedistat (MLN4924) is a potent inhibitor of NAE (half-maximal inhibitory concentration (IC
50
=0.004 μM), and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC
50
=1.5, 8.2, 1.8 and >10 μM, respectively). Pevonedistat (MLN4924) treatment inhibits overall protein turnover in cultured HCT-116 cells. Treatment of HCT-116 cells with Pevonedistat (MLN4924) for 24 h results in a dose-dependent decrease of Ubc12-NEDD8 thioester and NEDD8-cullin conjugates, with an IC
50
< 0.1 μM, resulting in a reciprocal increase in the abundance of the known CRL substrates CDT1, p27 and NRF2 (also known as NFE2L2), but not non-CRL substrates
[1]
. Pevonedistat induces CLL cell apoptosis and circumvented stroma-mediated resistance. Pevonedistat promotes induction of Bim and Noxa in the CLL cells leading to rebalancing of Bcl-2 family members toward the proapoptotic BH3-only proteins
[2]
. Pevonedistat (MLN4924) rapidly inhibits cullin 1 neddylation and remarkably suppressed growth and survival as well as migration in a dose-and time-dependent manner in gastric cancer cells, and significantly suppresses migration by transcriptionally activating E-cadherin and repressing MMP-9
[3]
.
In Vivo:
Pevonedistat (MLN492410, 30 or 60 mg/kg, s.c.) leads to a dose- and time-dependent increase in the steady state levels of NRF2 and CDT1 in HCT-116 tumour-bearing mice, and decreases NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells. Pevonedistat (MLN4924) administered on a BID schedule at 30 and 60 mg/kg inhibits tumour growth with T/C values of 0.36 and 0.15, respectively
[1]
.
Information
CAS No
1160295-21-5
Formula
C
21
H
26
ClN
5
O
4
S
Clinical Information
clinicalinformation
Pathway
Metabolic Enzyme/Protease
Target
NEDD8-activating Enzyme
Specifications
Purity / Grade
>98%
Solubility
DMSO : ≥ 160 mg/mL (333.35 mM)
Smiles
smiles
Misc Information
Alternative Names
MLN4924 (hydrochloride)
Observed Molecular Weight
479.98
related data
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