Pevonedistat NEW
| Price | $48 | $64 | $97 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Pevonedistat | CAS No.: 905579-51-3 |
| Purity: 99.92% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Pevonedistat |
| Description | Pevonedistat (MLN4924) is a potent and selective NEDD8 activating enzyme (NAE) inhibitor (IC50=4.7 nM) with therapeutic potential for myelodysplastic syndromes (MDS) and antitumor activity. |
| Cell Research | MLN4924 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. HCT-116 cells grown in 6-well cell-culture dishes are treated with 0.1% DMSO (control) or 0.3 μM MLN4924 for 24 h. Whole cell extracts are prepared and analysed by immunoblotting. For analysis of the E2-UBL thioester levels, lysates are fractionated by non-reducing SDS-PAGE and immunoblotted with polyclonal antibodies to Ubc12, Ubc9 and Ubc10. For analysis of other proteins, lysates are fractionated by reducing SDS-PAGE and probed with primary antibodies as follows: mouse monoclonal antibodies to CDT1, p27, geminin, ubiquitin, securin/PTTG and p53 or rabbit polyclonal antibodies to NRF2, Cyclin B1 and GADD34[1]. |
| Kinase Assay | Bcl-2 Binding affinity calculation: A predicted binding affinity for Obatoclax binding to BCL-2 is calculated using the SIE scoring function. [4] As a control in determining the reliability of the calculation, predicted binding affinities Ki) are calculated for a set of 12 small molecules with experimentally measured binding affinities to BCL-2. |
| In vitro | METHODS: Nine neuroblastoma cell lines were treated with Pevonedistat (12-1000 nM) for 72 h. Cell viability was measured by MTT. RESULTS: All neuroblastoma cell lines tested were sensitive to Pevonedistat with IC50 values ranging from 136-400 nM. [1] METHODS: Human colorectal cancer cells HCT-116 were treated with Pevonedistat (0.001-3 μM) for 24 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Pevonedistat treatment resulted in a dose-dependent decrease in Ubc12-NEDD8 thioester and NEDD8-cullin couplings, leading to an increase in the abundance of known CRL substrates CDT1, p27 and NRF2. [2] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, Pevonedistat (30-60 mg/kg in 10% cyclodextrin) was injected subcutaneously into BALB/c mice harboring the human colorectal cancer tumor HCT-116 either once or twice daily for twenty days. RESULTS: Pevonedistat inhibited the growth of HCT-116 xenograft tumors. [2] METHODS: To assay in vivo antitumor activity, Pevonedistat (60 mg/kg, intraperitoneal injection, once daily), venetoclax (50 mg/kg, oral administration, once daily), and azacitidine (8 mg/kg, intravenously three times every seven days) were administered to NSGS mice harboring the AML tumor OCI-AML2-Red- Fluc for fourteen days. RESULTS: Pevonedistat/venetoclax/azacitidine triple therapy induced durable responses in a systemic xenograft model of acute myeloid leukemia. [3] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 125 mg/mL (281.83 mM）, Sonication is recommended. |
| Keywords | NEDD8-activating Enzyme | MLN-4924 | Inhibitor | Pevonedistat | MLN 4924 | inhibit | NAE |
| Inhibitors Related | NSC697923 | PYZD-4409 | Nutlin-3 | NAcM-OPT | RG7112 | PYR-41 | BC-1382 | NSC232003 | NAE-IN-M22 | Indole-3-carbinol | Idasanutlin | Navtemadlin |
| Related Compound Libraries | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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