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Structure

TAK-243, inhibitor

TAK-243

Purity
98.00%
Synonyms
TAK-243; MLN7243; inhibitor
Ordering
 
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For Research Use Only!
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 50mg/mL (96.24mM) Need ultrasonic
H2O: 1mg/mL (1.92mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C19H20F3N5O5S2
SMILES
O=S(OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](NC2=CC=NC3=CC(C4=CC=CC(SC(F)(F)F)=C4)=NN23)C1)(N)=O
CAS Number
1450833-55-2
Target & IC50
UBA1: ic50 1nM
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Structure

Related Product Information for TAK-243, inhibitor
TAK-243 is a small molecule inhibitor of ubiquitin-activating enzyme (UAE,IC50=1nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-kappaB pathway activation and promotes apoptosis,with potential antineoplastic activity.
References
Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment, Nat Med. 2018 Feb;24(2):186-193.
Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment, Nat Med. 2018 Feb;24(2):186-193.
Best SR, et al. TAK-243, a small molecule inhibitor of ubiquitin-activating enzyme (UAE), induces ER stress and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. Blood 2017 130:1533.
Best SR, et al. TAK-243, a small molecule inhibitor of ubiquitin-activating enzyme (UAE), induces ER stress and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. Blood 2017 130:1533.
Samir H. Barghout, et al. TAK-243 Is a Selective UBA1 Inhibitor That Displays Preclinical Activity in Acute Myeloid Leukemia (AML). Blood 2017, 130:814.
Samir H. Barghout, et al. TAK-243 Is a Selective UBA1 Inhibitor That Displays Preclinical Activity in Acute Myeloid Leukemia (AML). Blood 2017, 130:814.
Ubiquitin-activating enzyme inhibition induces an unfolded protein response and overcomes drug resistance in myeloma.[J]. Blood, 2019.

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Product Notes

The TAK-243 (Catalog #AAA5755577) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "TAK-243, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.

Precautions

All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.

Disclaimer

Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.

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