The ULK (UNC51-like) enzymes are a family of mammalian kinases that have critical roles in autophagy and development. ULK1 through ULK4 and STK36 are the 5 genes that make up the ULK family of kinases in mammals. It has been established that ULK1 and ULK2 play important roles in a variety of pathological, physiological, and developmental processes in mammals and are required for the proper induction of autophagy.
Serine/threonine protein kinases ULK1 and ULK2, which play redundant roles in the control of autophagy, are evolutionarily conserved orthologs of the yeast member of the Atg (autophagy related) family Atg1. Long-lived proteins or organelles are the targets of autophagy, which degrades them in lysosomes before recycling the byproducts for use in other cellular pathways. The four components of the RB1CC1/FIP200/ATG17, ULK1, ATG13, and ATG101 make up the canonical ULK/ATG1 complex.
By phosphorylating certain enzymes in the class III phosphatidylinositol 3-kinase complex (such as PI3K3C/Vps34, PIK3R4/Vps15, BECN1/Vps30/ATG6, ATG14), it helps to start the formation of autophagosomes, at least in part. Through ATG9, ULK/Atg1 also encourages membrane recycling. Mice lacking both ULK1 and ULK2 expression die soon after birth due to a defect in glycogen metabolism, similar to other autophagy-defective mice, which is consistent with the known role of ULK1/2 in autophagy. Disrupting ULK1 expression also causes a defect in the autophagy-mediated clearance of mitochondria during red blood cell maturation in mice.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V5203 | BL-918 | 2101517-69-3 | BL-918, a racemic mixture, is a novel and potent small molecule activator of UNC-51-like kinase 1 (ULK1), inducing cytoprotective autophagy for Parkinson’s disease treatment. |
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V88580 | DCC-3116 | 2543673-19-2 | DCC-3116 is an orally active ULK1/2 inhibitor. |
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V3195 | LYN-1604 | 2088939-99-3 | LYN-1604 (LYN1604) is a potent agonist or activator of the UNC-51-like kinase 1 (ULK1) with potential antitumor activity. |
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V3196 | LYN-1604 HCl | 2216753-86-3 | LYN-1604 HCl, the hydrochloride salt ofLYN-1604, is a novel and potent activator/agonist of the UNC-51-like kinase 1 (ULK1) (EC50= 18.94 nM) with anticancer activity. |
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V26016 | MRT-68921 HCl | 2080306-21-2 | MRT-68921 HCl, the hydrochloride salt ofMRT68921, is a dual inhibitor of ULK1 and ULK2 (theautophagy kinases) with potential anticancer activity. |
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V26017 | MRT68921 | 1190379-70-4 | MRT-68921 (MRT68921; MRT 68921) is a novel, potent and dual inhibitor of theautophagy kinase ULK1 and ULK2 with IC50s of 2.9 and 1.1 nM, respectively. |
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V75974 | MRT68921 hydrochloride | 2070014-87-6 | MRT68921 HCl is a potent inhibitor of ULK1 and ULK2 with IC50s of 2.9 nM and 1.1 nM respectively. |
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V88571 | NZ-66 | NZ-66 is a chimera targeting UNC-51-like kinase 1 (ULK1) for proximity-induced and ULK1-dependent mitochondrial degradation. | |
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V2248 | SBP-7455 | 1884222-74-5 | SBP-7455 is a potent, high-affinity, orally bioactive dual ULK1/ULK2 autophagy inhibitor (antagonist) with IC50 of 13 nM and 476 nM, respectively, in the ADP-Glo assay. |
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V75975 | ULK-101 | 2443816-45-1 | ULK-101 is a potent and specific ULK1 inhibitor (antagonist) with in vitro IC50s of 1.6 nM and 30 nM for ULK1 and ULK2, respectively. |
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