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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
GY04405

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.

GY10123

ULK-101

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.

GY10124

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.

GY02214

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.

GY01974

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.

GY05245

ULK1-IN-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.

GY03778

LYN-1604

2088939-99-3

LYN-1604 is a potential ULK1 agonist (enzymatic activity=195.7% at 100 nM and IC50=1.66 uM against MDA-MB-231 cells), displays a good effect on ULK1 activation with an EC50 of 18.94 nM; induces cell death, associated with autophagy by the ULK complex (ULK1-mATG13-FIP200-ATG101) in MDA-MB-231 cells; induces cell death involved in ATF3, RAD21, and caspase3, accompanied by autophagy and apoptosis; inhibits the growth of xenograft TNBC.

GY05195

BL-918

2101517-69-3

BL-918 is a small molecule activator of ULK1 with EC50 of 24 nM (243% kinase activity at 100 nM), induces autophagy via the ULK complex in SH-SY5Y cells; displays a cytoprotective effect on MPP+-treated SH-SY5Y cells, as well as protected against MPTP-induced motor dysfunction and loss of dopaminergic neurons by targeting ULK1-modulated autophagy in mouse models of PD.

GY05188

SR-20295

2166091-48-9

SR-20295 (SR20295) is a novel potent ULK1 inhibitor with IC50 of 45 nM.

GY01574

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.

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