Product Details
| Product Name:
TAK-243 |
CAS No.:
1450833-55-2 |
| Purity:
98.93% |
Supply Ability:
10g |
| Release date:
2024/11/20 |
Product Introduction
Bioactivity
| Name | TAK-243 |
| Description | TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM), blocking ubiquitin binding and disrupting both mono-ubiquitin signaling and overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis. |
| In vitro | METHODS: Seven myeloma cells were treated with TAK-243 (6.25-500 nM) for 24 h. Cell viability was measured by WST-1 Assay.
RESULTS: Most myeloma cells are very sensitive to TAK-243 with IC50 of 25-100 nM, e.g. MM1.S cells with IC50 of 25 nM. [1]
METHODS: Human colorectal cancer cells HCT-116 were treated with TAK-243 (0.008-1 μM) for 24 h, and the expression levels of target proteins were detected by Western Blot.
RESULTS: TAK-243 showed strong selectivity for Sumo and autophagic UBL pathways, and TAK-243 inhibited two E1 enzymes (UBA6 and UAE), which are capable of activating ubiquitin, with equal potency. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, TAK-243 (12.5 mg/kg twice weekly; or 25 mg/kg once weekly) was administered intravenously for two weeks to SCID mice bearing myeloma MM1.S or MOLP-8.
S and MOLP-8 models, twice-weekly administration of 12.5 mg/kg produced 60% and 73% tumor growth inhibition at 14 days. 25 mg/kg produced a greater effect. [1]
METHODS: To test the antitumor activity in vivo, TAK-243 (20 mg/kg) was injected intravenously twice weekly into SCID mice bearing the human AML tumor OCI-AML2.
RESULTS: TAK-243 significantly delayed tumor growth (T/C=0.02) in mice without toxicity. [3] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL
DMSO : 50 mg/mL (96.24 mM), Sonication is recommended.
|
| Keywords | Ubiquitin conjugating enzyme | TAK-243 | MLN 7243 | E1 activating enzyme | Inhibitor | Ubiquitin activating enzyme | inhibit | TAK 243 | MLN-7243 | E2 conjugating enzyme | Nuclear factor-κB | NF-κB | Apoptosis | E3 ligating enzyme | E1/E2/E3 Enzyme | Nuclear factor-kappaB | Ubiquitin ligase | TAK243 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Glucosamine | Diallyl disulfide |
| Related Compound Libraries | NF-κB Signaling Compound Library | Bioactive Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | 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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