ULK|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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ULK1 (unc-51 like autophagy activating kinase 1), a mammalian serine/threonine kinase, is the core component of autophagic initiation complex and induces cellular autophagy. Canonical autophagy pathway is a process that, through the autophagy-lysosome pathway, which is mediated by a series of autophagy-related proteins, autophagosome can encompass deserted protein and organelles and deliver them to the lysosome. The deserted protein and organelles are finally degraded in the lysosome. Thus the ULK1-induced canonical autophagy is no doubt an important part of cellular “quality control”.

Other than the classic function of ULK1 in autophagy, ULK1 can also exert distinct impacts on many life processes, such as apoptosis, pentose phosphate pathway and innate immune response. Moreover, ULK1 is indispensible in glucose and lipid metabolism, red cell formation, endoplasmic reticulumstress response, tumor and nervous system diseases. Considering the importance of ULK1, a general overview is given on ULK1 functions via autophagy and non-autophagy pathways in a variety of human physiological, pathological and disease processes.

Cat. No.	Product Name	CAS No.	Information
H9181	SBP-7455	1884222-74-5	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.
H1822	ULK1 inhibitor 1	1644063-60-4	ULK1-IN-1 highly potent ULK1 inhibitor with IC50 of 8 nM, with no enough selectivity but sufficient potency, a cellular probe of autophagy.
H1821	ULK-101	2443816-45-1	ULK-101 (ULK101) is a potent and selective ULK1 inhibitor with in vitro IC50 of 8.3 nM, inhibits ULK2 with IC50 of 30 nM; reduces Ser15 phosphorylation in a concentration-dependent manner in cell-based assay (EC50=390 nM), which is more potent than SBI-0206965 showing a cellular EC50 of 2.4 uM; displays desirable kinome selectivity profile; suppresses autophagy induction and autophagic flux in response to different stimuli, ULK1 inhibition sensitizes KRAS mutant lung cancer cells to nutrient stress.
H1820	ULK-100		ULK-100 (ULK100) is a potent and selective ULK1 inhibitor with in vitro IC50 of 1.6 nM, inhibits ULK2 with IC50 of 2.6 nM; reduces Ser15 phosphorylation in a concentration-dependent manner in cell-based assay (EC50=83 nM), which is more potent than SBI-0206965 showing a cellular EC50 of 2.4 uM; displays desirable kinome selectivity profile.
H1819	SR-20295	2166091-48-9	SR-20295 (SR20295) is a novel potent ULK1 inhibitor with IC50 of 45 nM.
H1818	SR-19871		A novel potent ULK1 inhibitor with IC50 of 11 nM.
H1817	SBI-0206965	1884220-36-3	SBI-0206965 (SBI 0206965) is a potent and specific small molecule ULK1 kinase inhibitor with IC50 of 108 nM; displays 7-fold less potency for ULK2 (IC50=711 nM); inhibits Beclin1 Ser15 and Vps34 Ser249 phosphorylation to comparable extents in HEK-293T cells; suppresses autophagy induced by mTOR inhibition and prevents ULK1-dependent cell survival; greatly synergized with mTOR inhibitors to kill tumor cells.
H1816	MRT67307	1190378-57-4	MRT67307 is a potent, dual inhibitor of IKKε and TBK-1 with IC50 of 160 and 19 nM at 0.1 mM ATP in vitro, also potently inhibit ULK1 and ULK2 in vitro (IC50=45 and 38 nM) and block autophagy in cells; the autophagy-inhibiting capacity of MRT67307 is specifically through ULK1, results in accumulation of stalled early autophagosomal structures in treated cells; increases IL-10 production and suppresses proinflammatory cytokine production in macrophages, increases CREB-dependent gene transcription by promoting the dephosphorylation of CRTC3; also inhibits MARK, NUAK and SIK isoforms in vitro with comparable potency to the IKK-related kinases.
H1815	MRT-68921 hydrochloride	2080306-21-2	MRT-68921 hydrochloride (MRT68921) is a potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively; inhibits a number of kinases by over 80% in a broad panel of 80 protein kinases, including TBK1 and AMPK; reduces phospho-ATG13 and blocks autophagy in cells.
H1814	MRT-68921	1190379-70-4	A potent, relatively specific inhibitor of both ULK1 and ULK2 with IC50 of 2.9 and 1.1 nM, respectively; inhibits a number of kinases by over 80% in a broad panel of 80 protein kinases, including TBK1 and AMPK; reduces phospho-ATG13 and blocks autophagy in cells.

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