TAK-243 (MLN7243) is a potent ubiquitin activating enzyme (UAE) inhibitor with an IC50 of 1 ± 0.2 nM in the UBCH10 E2 thioate assay. In a selective test of kinase and receptor repertoires, it showed weak inhibition of off-target targets including type I and type II human carbonic anhydrases. TAK-243 (MLN7243) can induce ER stress, inhibit the activation of NFκB signaling pathway and promote apoptosis.

 

Brand: BCM

 

Target: Apoptosis; E1/E2/E3 Enzyme; NF-κB

 

Signaling Pathways: Apoptosis; NF-κB; Ubiquitination

 

In Vitro: TAK-243 (formerly known as MLN7243) as a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade.?TAK-243 treatment caused 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.

 

pKa: 9.35±0.70(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C1[C@@H]([C@H]([C@H]([C@@H]1NC2=CC=NC3=CC(=NN23)C4=CC(=CC=C4)SC(F)(F)F)O)O)COS(=O)(=O)N  

 

InChIKey: KJDAGXLMHXUAGV-DGWLBADLSA-N  

 

InChI: InChI=1S/C19H20F3N5O5S2/c20-19(21,22)33-12-3-1-2-10(6-12)13-8-16-24-5-4-15(27(16)26-13)25-14-7-11(17(28)18(14)29)9-32-34(23,30)31/h1-6,8,11,14,17-18,25,28-29H,7,9H2,(H2,23,30,31)/t11-,14-,17-,18+/m1/s1

 

Attribute
[Chem Name]	[(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-(trifluoromethylsulfanyl)phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl sulfamate
[Synonym]	TAK-243； MLN7243
[CAS No.]	1450833-55-2
[MDL No.]	MFCD28964160
[Formula]	C19H20F3N5O5S2
[Molecular]	519.52
[Form]	Solid Powder
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

Goods Tag