A UAE inhibitor
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PYZD-4409

Item No. 44131

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(3-chloro-4-fluorophenyl)-4-[(5-nitro-2-furanyl)methylene]-3,5-pyrazolidinedione
CAS Number
423148-78-1
Molecular Formula
C14H7ClFN3O5
Formula Weight
351.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
ClC1=CC(N(NC2=O)C(C2=CC3=CC=C([N+]([O-])=O)O3)=O)=CC=C1F
InChi Code
InChI=1S/C14H7ClFN3O5/c15-10-5-7(1-3-11(10)16)18-14(21)9(13(20)17-18)6-8-2-4-12(24-8)19(22)23/h1-6H,(H,17,20)
InChi Key
MSYMKEYWUWVZQY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $160

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    25 mg

    $304

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    50 mg

    $468

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    Cayman Chemical
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    Product Description

    PYZD-4409 is an inhibitor of ubiquitin-activating enzyme (UAE; IC50 = 20 µM in a cell-free assay).1 It decreases levels of ubiquitinated cell division cycle 34 (Cdc34) in K562 chronic myeloid leukemia (CML) cells when used at a concentration of 50 µM. PYZD-4409 increases levels of cyclin D3 and p53 in HCT116 colorectal cancer cells. It selectively reduces colony formation in primary patient-derived acute myeloid leukemia (AML) cells over primary human hematopoietic cells when used at a concentration of 10 µM. PYZD-4409 (10 mg/kg) decreases tumor weight in an MDAY-D2 murine lymphoma model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Xu, G.W., Ali, M., Wood, T.E., et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. Blood 115(11), 2251-2259 (2021).