CUR5g

CAS No. 1370032-20-4

CUR5g( —— )

Catalog No. M36540 CAS No. 1370032-20-4

CUR5g is an autophagy inhibitor that inhibits migration and colony formation in A549 cells and acts through a UVRAG-dependent mechanism by blocking the recruitment of STX17 to autophagosomes.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CUR5g
  • Note
    Research use only, not for human use.
  • Brief Description
    CUR5g is an autophagy inhibitor that inhibits migration and colony formation in A549 cells and acts through a UVRAG-dependent mechanism by blocking the recruitment of STX17 to autophagosomes.
  • Description
    CUR5g is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo.
  • In Vitro
    Cell Autophagy AssayCell Line:A549 cellsConcentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:3, 6, 12, and 24 h Result:Induced extensive cytoplasmic vacuolization, and GFP-LC3B signal shifted from diffuse cytosolic staining to a punctate pattern outlining autophagosomes.Western Blot Analysis Cell Line:A549 cells Concentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:0, 1, 3, 6, 12, and 24 h Result:Up-regulated LC3B-II and sequestosome 1 (SQSTM1) levels time- and dose-dependently. This increase was not the result of enhanced transcription, as mRNA expression of SQSTM1 and LC3B were not increased within CUR5g-exposed cells, suggesting that CUR5g might block autophagic flux rather than increase autophagosome formation.Cell Proliferation Assay Cell Line:A549 cells Concentration:0, 1, 5, 10, 20, and 40 μM Incubation Time:24 h Result:Exhibited great toxicity to A549 cells at 20 μM. Slightly decreased A549 cell number at 10 μM, while decreased the number of A549 cells significantly at 20 μM. Showed no discernable activity in healthy human umbilical vein endothelial cell (HUVEC) viability at 40?μM.
  • In Vivo
    Animal Model:BALB/c nude mice (4-week-old, A549 cells were subcutaneously injected into the right scapula of each nude mouse)Dosage:40?mg/kg, CUR5g (40 mg/kg) and Cisplatin (1 mg/kg) Administration:Injected via caudal vein, once every 2 days for up to 15 days Result:Retarded the growth of xenografted tumors, whereas the combination treatment with Cisplatin almost completely inhibited tumor growth. Promoted the cisplatin sensitivity of A549 cells by inhibiting autophagic flux.
  • Synonyms
    ——
  • Pathway
    Autophagy
  • Target
    Autophagy
  • Recptor
    Autophagy
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1370032-20-4
  • Formula Weight
    344.41
  • Molecular Formula
    C22H20N2O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 41.67 mg/mL (120.99 mM; Ultrasonic (<60°C)
  • SMILES
    C(\C=1C=2C(NC1)=CC=CC2)=C\3/C(=O)\C(=C\C4=CC=C(O)C=C4)\CN(C)C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Chen J, et al. CUR5g, a novel autophagy inhibitor, exhibits potent synergistic anticancer effects with cisplatin against non-small-cell lung cancer. Cell Death Discov. 2022 Oct 31;8(1):435.?
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