| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.62 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 237.5 mg/mL (457.15 mM), Sonication is recommended.
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| Keywords | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | UBA1 | TAK-243 | TAK243 | TAK 243 | Nuclear factor-κB | Nuclear factor-kappaB | NF-κB | NFκB | NF-kB | NFkB | MLN-7243 | MLN 7243 | Inhibitor | inhibit | E3Enzyme | E3 ligating enzyme | E3 Enzyme | E2Enzyme | E2 Enzyme | E2 conjugating enzyme | E1Enzyme | E1/E2/E3 Enzyme | E1 Enzyme | E1 activating enzyme | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Ethyl linoleate | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Bioactive Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Fibrosis Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
