ULK Inhibitor

VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma.

DRAK2-IN-2 is a selective DRAK2 inhibitor with an IC₅₀ value of 198.5 nM. DRAK2-IN-2 inhibits DRAK2-mediated phosphorylation of ULK1 at the Ser56 site. DRAK2-IN-2 enhances insulin secretion, increases mitochondrial membrane potential, alleviates Palmitic acid (HY-N0830)-induced mitochondrial membrane potential damage and Apoptosis, and improves glucose tolerance in vivo. DRAK2-IN-2 can be used for the research of type 2 diabetes.

ULK1/2-IN-1 is a tissue-targeted ULK1/2 inhibitor conjugated to the RGR (CRGRRST) tumor neovasculature-homing peptide. ULK1/2-IN-1 mediates autophagy inhibition and induces cytotoxicity in endothelial cells. ULK1/2-IN-1 can be used for the research of tumor-targeted autophagy inhibitors.

MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC₅₀s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC₅₀s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.

MRT68921 hydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 hydrochloride inhibits ULK1 and ULK2 with IC₅₀ values of 2.9 nM and 1.1 nM, respectively. MRT68921 hydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 hydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 hydrochloride can be used for the research of cancer, such as breast cancer.

ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.

ULK1-IN-4 (compound 12i) is a ULK1 inhibitor with an IC₅₀ of 4.7 μM against human ULK1, and it exhibits selectivity for Aurora A/Aurora B kinases. ULK1-IN-4 forms a covalent bond with the thiol group of the Cys182 residue of ULK1, thereby inhibiting the kinase activity of ULK1. ULK1-IN-4 inhibits the growth of colorectal cancer cells and exerts tumor-suppressive activity in a mouse model of colorectal cancer.

Ulk2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ulk2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

ULK-100 is a potent ULK1/ULK2 inhibitor, with IC₅₀ values of 1.6 nM and 2.6 nM against human ULK1 and ULK2, respectively. ULK-100 reduces ULK1-mediated phosphorylation of Beclin 1 at Ser15, inhibits autophagy by targeting the ULK1 pathway, and also suppresses autophagy in tumor cells. ULK-100 enhances the sensitivity of tumor cells to nutrient deprivation. ULK-100 can be used in research on autophagy initiation and cancer.

ULK1-IN-5 (Compound D1) is a selective ULK1 inhibitor with an IC₅₀ of 14.91 nM. ULK1-IN-5 functionally inhibits the kinase activity of ULK1. ULK1-IN-5 reduces the phosphorylation level of ATG13. ULK1-IN-5 exerts antiproliferative effects on cervical cancer cells. ULK1-IN-5 is applicable to relevant research on cervical cancer.

SBP-5147 is an orally active ULK1/ULK2 inhibitor, with an IC₅₀ of 2 nM against ULK1 and an IC₅₀ of 53 nM against ULK2. SBP-5147 inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagy flux, downregulates the expression of ATG13 and ATG101, upregulates the expression of MHC-I, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. SBP-5147 is applicable to research related to non-small cell lung cancer^[1].

SBI-0206965 (Standard) is the analytical standard of SBI-0206965 (HY-16966). This product is intended for research and analytical applications. SBI-0206965 is a potent, selective and cell permeable autophagy K_inase ULK1 inhibitor with IC₅₀s of 108 nM for ULK1 K_inase and 711 nM for the highly related K_inase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.

MRT68921 (dihydrochloride) (Standard) is the analytical standard of MRT68921 (dihydrochloride) (HY-100006A). This product is intended for research and analytical applications. MRT68921 dihydrochloride is a potent NUAK1/ULK1 dual inhibitor. MRT68921 dihydrochloride inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 dihydrochloride can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 dihydrochloride can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 dihydrochloride can be used for the research of cancer, such as breast cancer.

SR-17398 is an inhibitor for Unc-51-Like Kinase 1 (ULK1) with an IC₅₀ of 22.4 μM.