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ULK

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ULK1, a serine/threonine protein kinase, is an enzyme that in humans is encoded by the ULK1 gene. ULK1 is essential for the initial stages of autophagy. ULK1 is an important protein in autophagy. It is part of the ULK1-complex, which is needed in early steps of autophagosome biogenesis. ULK1 inhibition results in accumulation of stalled early autophagosomal structures, indicating a role for ULK1 in the maturation of autophagosomes as well as initiation.

ULK2 is essential for astrocyte transformation and tumor growth. ULK2 also inhibits the growth of glioma cells, which requires autophagy induction as kinase mutant of ULK2 fails to induce autophagy and inhibit growth. ULK2 and its homologue ULK1 are only down-regulated in all grades of glioma. Thus these results altogether suggest that inhibition of autophagy by ULK1/2 down-regulation is essential for glioma development.

Products Related to ULK(13)

  • GC14086 structure
    GC14086MRT68921
    CAS: 1190379-70-4
    Purity: >98%

    MRT68921 is a potent dual inhibitor of ULK1 and ULK2 with IC 50 values of 2.9nM and 1.1nM, respectively.

  • GC15654 structure
    GC15654SBI-0206965
    CAS: 1884220-36-3
    Purity: >99.00%

    SBI-0206965 , the pyrimidine derivative , is a highly selective kinase ULK1 inhibitor with an IC 50 value of 108nM.

  • GC17136 structure
    GC17136MRT67307
    CAS: 1190378-57-4
    Purity: >98.50%

    A kinase inhibitor

  • GC19236 structure
    GC19236LYN-1604
    CAS: 2088939-99-3
    Purity: >98%

    LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) agonist with an EC50 of 18.94 nM.

  • GC34315 structure
    GC34315ULK-101
    CAS: 2443816-45-1
    Purity: >99.50%

    ULK-101 is a selective ULK1 inhibitor (IC₅₀=1.6nM) that inhibits ULK2 activity (IC₅₀=30nM).

  • GC36517 structure
    GC36517LYN-1604 hydrochloride
    CAS: 2216753-86-3
    Purity: >98%

    LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).

  • GC36654 structure
    GC36654MRT68921 dihydrochloride
    CAS: 2080306-21-2
    Purity: >99.50%

    MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.

  • GC60891 structure
    GC60891GW406108X
    CAS: 1644443-92-4
    Purity: >98.00%

    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.

  • GC62146 structure
    GC62146XST-14
    CAS: 2607143-50-8
    Purity: >99.50%

    XST-14 is a potent, competitive and highly selective ULK1 inhibitor with an IC50 of 26.6 nM. XST-14 induces autophagy inhibition by reducing the phosphorylation of the ULK1 downstream substrate. XST-14 induces apoptosis in hepatocellular carcinoma (HCC) cells and has antitumor effects.

  • GC73892 structure
    GC73892DCC-3116
    CAS: 2543673-19-2
    Purity: >99.00%

    DCC-3116 is an orally active ULK1/2 inhibitor.

  • GC78994 structure
    GC78994SBP-1750
    CAS: 1884219-70-8
    Purity: >98.00%

    SBP-1750 is an orally active ULK inhibitor and an ATG13 degrader.

  • GC81304 structure
    GC81304GW296115
    CAS: 118458-58-5
    Purity: >98.50%

    GW296115 is a multi-target inhibitor with the following IC 50 values against its targets: 8.4 nM for BRSK2, 21 nM for BRSK1, 1.8 μM for PDGFRβ, 5.5 nM for STK17B/DRAK2, 28 nM for DRAK1, 20 nM for PHKG1, and 89 nM for DCAMKL3.

  • GC81673 structure
    GC81673UE01
    CAS: 486440-74-8
    Purity: >98%

    UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2.