1. Autophagy
  2. ULK

ULK

The ULK (UNC51-like) enzymes are a family of mammalian kinases that have critical roles in autophagy and development. The ULK family of kinases comprises 5 genes in mammals: ULK1 through ULK4 and STK36. In mammals, ULK1 and ULK2 have been shown to be necessary for the proper autophagy induction and contribute to various developmental, physiological, and pathological processes.

The serine/threonine-protein kinases ULK1 and ULK2 are evolutionarily conserved serine/threonine kinase orthologs of the yeast autophagy related (Atg) family member Atg1, that have redundant roles in the regulation of autophagy. Autophagy targets long-lived proteins or organelles for degradation in lysosomes, and the products of this process are then recycled for other cellular pathways. The canonical ULK/Atg1 complex is composed of ULK1, ATG13, RB1CC1/FIP200/ATG17, and ATG101. It initiates autophagosome formation, at least in part by phosphorylating components of the autophagy-inducing class III phosphatidylinositol 3-kinase complex (e.g., PI3K3C/Vps34, PIK3R4/Vps15, BECN1/Vps30/ATG6, ATG14). ULK/Atg1 also promotes membrane recycling via ATG9. Consistent with the established role of ULK1/2 in autophagy, disrupting ULK1 expression in mice results in a defect in autophagy-mediated clearance of mitochondria during red blood cell maturation, and mice lacking both ULK1 and ULK2 expression die shortly after birth due to a defect in glycogen metabolism, which is similar to other autophagy-defective mice.

ULK Related Products (22):

Cat. No. Product Name Effect Purity
  • HY-114490
    ULK-101 Inhibitor 99.96%
    ULK-101 is a potent and selective ULK1 inhibitor, with IC50 values of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. ULK-101 suppresses autophagy and sensitizes cancer cells to nutrient stress[1].
  • HY-124729
    BL-918 Activator 99.98%
    BL-918 is an orally active UNC-51-like kinase 1 (ULK1) activator with an EC50 of 24.14 nM. BL-918 exerts its cytoprotective autophagic effect by targeting ULK complex. BL-918 has the potential for Parkinson’s disease (PD) treatment[1].
  • HY-13018
    MRT67307 Inhibitor 99.34%
    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells[2].
  • HY-16966
    SBI-0206965 Inhibitor 99.39%
    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2[1].
  • HY-100006A
    MRT68921 dihydrochloride Inhibitor 99.67%
    MRT68921 dihydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively[1].
  • HY-162100
    MR-2088 Inhibitor
    MR-2088 is a selective ULK1/ULK2 inhibitor with pEC50 values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition[1].
  • HY-N0867
    13-Oxyingenol-13-dodecanoate Inducer 99.37%
    13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM[1].13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis[2].
  • HY-160699
    DCC-3116 Inhibitor
    DCC-3116 is an orally active ULK1/2 inhibitor. DCC-3116 can promote autophagy in lung cancer cells by inhibiting KRASG12C signaling, thereby inhibiting the proliferation of lung cancer cells and exerting anti-cancer effects[1].
  • HY-101923B
    LYN-1604 dihydrochloride Activator
    LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].
  • HY-100006
    MRT68921 Inhibitor 99.71%
    MRT68921 is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  • HY-137506
    XST-14 Inhibitor 99.69%
    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[1].
  • HY-13018B
    MRT67307 dihydrochloride Inhibitor
    MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells[2].
  • HY-137742
    SBP-7455 Inhibitor 98.24%
    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research[1].
  • HY-101923A
    LYN-1604 hydrochloride Activator
    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)[1].
  • HY-100006B
    MRT68921 hydrochloride Inhibitor
    MRT68921 hydrochloride is a potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  • HY-101923
    LYN-1604 Activator
    LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC)[1].
  • HY-13018A
    MRT67307 hydrochloride Inhibitor
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells[2].
  • HY-148061
    DB1113 99.28%
    DB1113 (Example 24) is a bifunctional compound targeted protein degradation of kinases. DB1113 degrades ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, MAP3K20, MAP4K1, MAP4K2, MAP4K3, MAP4K5, MAPK14, MAPK7, MAPK8, MAPK9, MAPKAPK2, MAPKAPK3, NLK, PDIK1L, PTK2B, RIPK1, RPS6KA1, RPS6KA3, SIK2, SIK3, STK35, TNK2, and ULK1. DB1113 can be used for research of disease or disorder mediated by aberrant kinase activity[1].
  • HY-143466
    ULK1-IN-2 Inhibitor 99.09%
    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)[1].
  • HY-115570
    GW406108X Inhibitor
    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[1][2].