| 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 |
United States
