A UAE inhibitor
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MLN7243

Item No. 30108

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
sulfamic acid, [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-[(trifluoromethyl)thio]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl ester
CAS Number
1450833-55-2
Synonyms
  • TAK-243
Molecular Formula
C19H20F3N5O5S2
Formula Weight
519.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/mlMethanol: 10 mg/ml
λmax
217, 262, 309 nm
SMILES
FC(F)(F)SC1=CC(C2=NN3C(N=CC=C3N[C@H]4[C@H](O)[C@H](O)[C@@H](COS(N)(=O)=O)C4)=C2)=CC=C1
InChi Code
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
InChi Key
KJDAGXLMHXUAGV-DGWLBADLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $493

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    Cayman Chemical
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    Product Description

    MLN7243 is an inhibitor of ubiquitin-activating enzyme (UAE; IC50 = 1 nM).1 It is selective for UAE over NEDD8-activating enzyme (NAE), SUMO-activating enzyme (SAE), and the autophagy-activating enzyme ATG7 (IC50s = 28, 850, and >10,000 nM, respectively). MLN7243 inhibits proliferation in a panel of 30 cancer cell lines (EC50s = 0.006-1.1 µM). It activates the unfolded protein response (UPR) and expansion of the endoplasmic reticulum surface area, a marker of ER stress, in HCT116 cells. In vivo, MLN7243 (12.5-25 mg/kg) reduces tumor growth in WSU-DLCL2, HCT116, Calu-6, THP-1, CWR22, HCC70, and MM.1S mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models of colon, lung, breast, ovarian, and neck cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hyer, M.L., Milhollen, M.A., Ciavarri, J., et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat. Med. 24(2), 186-193 (2018).