- ULK1
- ULK2
ULK1 选择性抑制剂 | 激活剂 | 激动剂
| 目录号 | 产品名 | 产品描述 | Selective / Pan | IC50 / Ki |
|---|---|---|---|---|
| S3393 | SBP-7455 | SBP-7455 is a dual-Specific ULK1/2 autophagy inhibitor with IC50s of 13 nM and 476 nM for ULK1 and ULK2 in ADP-Glo assay, respectively. | Selective | ULK1, IC50: 13 nM |
| S8597 | LYN-1604 | LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants. | Selective | ULK1, EC50: 18.94 nM |
| S0819 | BL-918 | BL-918 is a potent, orally active activator of UNC-51-like kinase 1 (ULK1) with EC50 of 24.14 nM and Kd of 0.719 μM. BL-918 induces cytoprotective autophagy for Parkinson's disease treatment. | Selective | ULK1, EC50: 24.14 nM; ULK1, Kd: 0.719 μM |
| S6386 | MRT67307 | MRT67307 (IKKε/TBK1 Inhibitor II) inhibits IKKε and TBK1 with IC50 values of 160 nM and 19 nM at 0.1 mM ATP in vitro, but does not inhibit IKKα or IKKβ even at 10 μM. MRT67307 also is a highly potent ULK1 and ULK2 inhibitor with IC50s of 45 and 38 nM, respectively. MRT67307 can blocks autophagy in cells. |
Selective | ULK1, IC50: 45 nM |
| S1113 | GSK690693 | GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1. | Selective | |
| S7949 | MRT68921 HCl | MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively. | Pan | ULK1, IC50: 2.9 nM |
| S8793 | ULK-101 | ULK-101 is a potent and selective ULK1 inhibitor with IC50 values of 8.3 nM and 30 nM for ULK1 and ULK2, respectively. | Pan | ULK1, IC50: 8.3 nM |
| S7885 | SBI-0206965 | SBI-0206965 is a highly selective autophagy kinase ULK1 inhibitor with IC50 of 108 nM, about 7-fold selectivity over ULK2. SBI-0206965 inhibits autophagy and enhances apoptosis in human glioblastoma and lung cancer cells. | Pan | ULK1, IC50: 108 nM |
