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TAK-243

TAK-243

Item no.	HY-100487-100mg
Manufacturer	MedChem Express
CASRN	1450833-55-2
Amount	100 mg
Quantity options	100 mg 10mM/1mL 10 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	98.38
Formula	C19H20F3N5O5S2
Citations	[1]Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med. 2018 Feb;24(2):186-193.<br/>[2]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.<br/>[3]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.
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	MLN7243
Available
Product Description	TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis[1][2].
StorageTemperature	-20°C, 3 years; 4°C, 2 years (Powder)
Shipping	Room Temperature
Manufacturers Applications	Cancer-programmed cell death
MolecularWeight	519.52
Clinical Information	Phase 1
Manufacturers Research Area	Cancer
Solubility	DMSO : 50 mg/mL (ultrasonic)\|H2O : < 0.1 mg/mL (ultrasonic)
Target	Apoptosis; E1/E2/E3 Enzyme; NF-κB
Manufacturers Target	Apoptosis; E1/E2/E3 Enzyme; NF-κB
Manufacturers Pathway	Apoptosis; Metabolic Enzyme/Protease; NF-κB
Manufacturers Product type	Reference compound

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HY-100487-100mg-safety-datasheet.pdf