ULK1-IN-2

CAS No. 2497409-01-3

ULK1-IN-2( —— )

Catalog No. M35716 CAS No. 2497409-01-3

ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 78 Get Quote
5MG 116 Get Quote
10MG 188 Get Quote
25MG 419 Get Quote
50MG 635 Get Quote
100MG 1008 Get Quote
500MG 2007 Get Quote
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Biological Information

  • Product Name
    ULK1-IN-2
  • Note
    Research use only, not for human use.
  • Brief Description
    ULK1-IN-2 is a potent ULK1 inhibitor with potential anticancer activity, inducing apoptosis while blocking autophagy.
  • Description
    ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer).
  • In Vitro
    ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7.ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells.ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner.ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.Cell Proliferation Assay Cell Line:Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7 Concentration: 10 μM Incubation Time:24 h Result:Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.Cell Autophagy Assay Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Blocked autophagy of A549 cells via inhibiting ULK.Western Blot Analysis Cell Line:A549 cells Concentration:0, 2, 4, 8 μM Incubation Time:24 h Result:Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Autophagy
  • Target
    Autophagy
  • Recptor
    Autophagy | Apoptosis
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2497409-01-3
  • Formula Weight
    495.26
  • Molecular Formula
    C19H16BrFN4O6
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 33.33 mg/mL (67.30 mM; Ultrasonic )
  • SMILES
    O(C)C1=C(OC)C=C(NC=2N=C(OC3=C(F)C=C(N(=O)=O)C=C3)C(Br)=CN2)C=C1OC
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Sun D, Yang Z, Zhen Y, et al. Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer. Eur J Med Chem. 2020;208:112782.?
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