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BT165712

TAK 243 - Bio-X

A potent inhibitor of ubiquitin activating enzyme E1. Lowers ubiquitin conjugates in cells, thereby disrupting cell signalling, cell cycle progression and repair of DNA damage. Anti-tumor effects have been demonstrated in vitro and in vivo. TAK 243 has been used to study the biology of ubiquitins and its potential as anti-cancer therapy. 

Technical Data

CAS No: 1450833-55-2
Product Code: BT165712
Chemical Formula: C19H20F3N5O5S2
Molecular Weight: 519.52

References


  • Barghout SH et al (2018). Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia. (published online ahead of print 8 Jun 2018). Available at: doi: 10.1038/s41375-018-0167-0.
  • Hyer ML et al (2018). A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med 24(2):186-193.
  • McHugh A et al (2018). Preclinical comparison of proteasome and ubiquitin E1 enzyme inhibitors in cutaneous squamous cell carcinoma: the identification of mechanisms of differential sensitivity. Oncotarget 9(29):20265-20281.

Solubility

Stability

Further Information


Datasheets


TAK 243 - Bio-X

CAS No:
1450833-55-2
Chemical Formula:
Molecular Weight:
519.52
Product Structure
References:
1. Barghout SH et al (2018). Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia. (published online ahead of print 8 Jun 2018). Available at: doi: 10.1038/s41375-018-0167-0.
2. Hyer ML et al (2018). A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med 24(2):186-193.
3. McHugh A et al (2018). Preclinical comparison of proteasome and ubiquitin E1 enzyme inhibitors in cutaneous squamous cell carcinoma: the identification of mechanisms of differential sensitivity. Oncotarget 9(29):20265-20281.

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