A UAE inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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 (Request formulation change)
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $69

    Add

    5 mg

    $313

    Add

    10 mg

    $493

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    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).