1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. PYZD-4409

PYZD-4409 

Cat. No.: HY-13297 Purity: >98.0%
Handling Instructions

PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay).

For research use only. We do not sell to patients.

PYZD-4409 Chemical Structure

PYZD-4409 Chemical Structure

CAS No. : 423148-78-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 178 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PYZD-4409 purchased from MCE. Usage Cited in: Mol Cell Biol. 2018 Jul 16;38(15). pii: e00024-18.

    Western blotting assays demonstrate that treatment of 20 μM PYR-41 or 20 μM PYZD-4409 inhibits ubiquitination and CD133 secretion. Hsp90 and β-actin are used as loading controls.
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    Description

    PYZD-4409 is a novel small molecule inhibitor of Ubiquitin-activating enzyme UBA1/E1 enzyme with an IC50 of 20 uM (cell-free enzymatic assay). IC50 Value: 20 uM (cell-free enzymatic assay) [1] Target: E1 enzyme (Ubiquitin-activating enzyme) in vitro: PYZD-4409 inhibited the ATP-dependent activation of ubiquitin and subsequent transfer of the activated ubiquitin from the E1 to the common human E2 enzyme UBE2E2 in a gel-based assay. The IC50 of inhibition was estimated to be 20μM in a cell-free enzymatic assay. Suggesting specificity of PYZD-4409 for the E1 enzyme, the compound had no effect on unrelated enzymes such as α-Mannosidase II glycosylation enzyme or Luciferase at concentrations up to 100μM (data not shown). It also did not inhibit the summo E1, Uba2, at concentrations up to 100μM. In 5 of 8 leukemia and myeloma cell lines, PYZD-4409 induced cell death with a LD50 less than 10μM. Myeloma cell lines were particularly sensitive to E1 inhibition because PYZD-4409 induced cell death with 3 of 4 myeloma cell lines (ie, LP1, KMS11, and U226) having an LD50 of 3μM or less. In contrast, solid tumor cell lines were less sensitive with an LD50 of approximately 15 to 20μM [1]. in vivo: SCID mice were injected subcutaneously with MDAY-D2 murine leukemia cells and then treated with PYZD-4409 (10 mg/kg) or buffer control intraperitoneally daily on alternate days over 8 days. Sixteen days after tumor implantation, the mice were killed, and the tumors excised and weighed. Compared with control-treated mice, treatment with PYZD-4409 delayed tumor growth and decreased tumor weight without untoward toxicity. Inhibition of the E1 can achieve an antitumor effect in vivo [1].

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 35 mg/mL (99.53 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8436 mL 14.2179 mL 28.4357 mL
    5 mM 0.5687 mL 2.8436 mL 5.6872 mL
    10 mM 0.2844 mL 1.4218 mL 2.8436 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Molecular Weight

    351.67

    Formula

    C₁₄H₇ClFN₃O₅

    CAS No.

    423148-78-1

    SMILES

    FC1=CC=C(N2C(/C(C(N2)=O)=C\C3=CC=C([N+]([O-])=O)O3)=O)C=C1Cl

    Shipping

    Room temperature in continental US; may vary elsewhere

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
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    Product Name:
    PYZD-4409
    Cat. No.:
    HY-13297
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    PYZD-4409

    Cat. No.: HY-13297