Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signaling as well as overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis.
説明 | TAK-243 (MLN7243) is a selective inhibitor of the ubiquitin-activating enzyme UAE (IC50=1 nM). TAK-243 blocks ubiquitin binding and disrupts mono-ubiquitin signaling as well as overall protein ubiquitination. TAK-243 exhibits antitumor activity and promotes apoptosis. |
ターゲット&IC50 | UBA1:1 nM |
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] |
別名 | MLN7243 |
分子量 | 519.52 |
分子式 | C19H20F3N5O5S2 |
CAS No. | 1450833-55-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL
5% DMSO+95% Saline: 2.5 mg/mL (4.81 mM, suspension)
DMSO: 50 mg/mL (96.24 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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TAK-243 1450833-55-2 Apoptosis NF-Κb Ubiquitination NF-κB E1/E2/E3 Enzyme Ubiquitin conjugating enzyme MLN 7243 E1 activating enzyme Inhibitor Ubiquitin activating enzyme inhibit TAK 243 MLN-7243 E2 conjugating enzyme Nuclear factor-κB E3 ligating enzyme MLN7243 Nuclear factor-kappaB Ubiquitin ligase TAK243 inhibitor