TAK-243 (MLN7243)

Catalog No.S8341

TAK-243 (MLN7243) Chemical Structure

Molecular Weight(MW): 519.52

TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II.

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Biological Activity

Description TAK-243 (MLN7243) is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE) with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioester assay. It has minimal inhibitory activity in a panel of kinase and receptor assays, as well as on human carbonic anhydrase type I and type II.
Targets
UAE [1]
(Cell-free assay)
1 nM
In vitro

TAK-243 treatment causes depletion of cellular ubiquitin conjugates, resulting in disruption of signaling events, induction of proteotoxic stress, and impairment of cell cycle progression and DNA damage repair pathways. TAK-243 has weaker inhibitory activity against other closely related E1 ubiquitin-like activating enzymes such as Fat10-activating enzyme (UBA6; 7 ± 3 nM), NEDD8-activating enzyme (NAE; 28 ± 11 nM), SUMO-activating enzyme (SAE; 850 ± 180 nM), ISG15-activating enzyme (UBA7; 5,300 ± 2,100 nM) and autophagy-activating enzyme (ATG7; >10,000 nM) than it does against UAE. TAK-243 inhibits UAE from transferring ubiquitin to an E2 enzyme. TAK-243 shows equally potent inhibition of the two E1 enzymes capable of activating ubiquitin (UBA6 and UAE), as indicated by comparable decreases in levels of charged USE1 and UBCH10. Downstream UAE pathway inhibition by TAK-243 is evident, as shown by a dose- and time-dependent loss of both polyubiquitin chains and mono-ubiquitylated histone H2B; however, TAK-243 treatment does not affect UAE (UBE1) protein levels. TAK-243 treatment also causes accumulation of short-lived proteins such as c-Jun, c-Myc, MCL1 and p53[1].

In vivo

TAK-243 treatment causes death of cancer cells and, in primary human xenograft studies. TAK-243 demonstrates broad antitumor activity in models of solid and hematological tumors[1].

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: HCT-116 and WSU-DLCL2 cells
  • Concentrations: 0.01, 0.10 or 1.00 μM
  • Incubation Time: 1, 2, 4, 8, 16 and 24 h
  • Method:

    HCT-116 and WSU-DLCL2 cells are maintained in log-phase growth in McCoy's 5A modified or RPMI-1460 medium, respectively supplemented with 10% fetal bovine serum at 37℃ in a 5% CO2 incubator. Cells are grown in 6-well cell culture dishes and treated with DMSO (0.1%) or with 0.01, 0.10 or 1.00 μM TAK-243 for the times indicated. Whole-cell extracts are prepared using RIPA buffer.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: SCID mice bearing WSU-DLCL2 NHL xenograft tumors
  • Formulation: 20% hydroxypropyl β-cyclodextrin
  • Dosages: 12.5, 18.75 and 25 mg/kg
  • Administration: IV
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (192.48 mM)
Ethanol 25 mg/mL (48.12 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 519.52
Formula

C19H20F3N5O5S2

CAS No. 1450833-55-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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E1 Activating Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID