ULK
抑制剂选择性比较
特异性亚型抑制剂
ULK产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor)是一种有效的，特异性ATM抑制剂，在无细胞试验中IC50/Ki为12.9 nM/2.2 nM，与DNA-PK， PI3K/PI4K， ATR和mTOR相比，对ATM具有高度选择性。KU‑55933 (ATM Kinase Inhibitor)可抑制 autophagy‑initiating kinase ULK1 的激活从而导致自噬的显著减少。 |
Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated. |
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| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
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| S7885 |
SBI-0206965SBI-0206965 是一种高度选择性自吞噬激酶ULK1抑制剂，IC50为108 nM，选择性比作用于ULK2高7倍。SBI-0206965 可抑制人胶质母细胞瘤和肺癌细胞中的自噬而增强凋亡。 |
Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, ** p < 0.01, *** p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05. |
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| S6386New |
MRT67307MRT67307（IKKε/TBK1 Inhibitor II）抑制IKKϵ/TBK1，在体外ATP（终浓度 0.1 mM）实验中，其IC50分别为160和19 nM，但当其浓度为10 μM时，对 IKKα 和 IKKβ 没有抑制作用。MRT67307 也是 ULK1 和 ULK2的抑制剂 ，其IC50分别为45和38 nM。MRT67307可阻断细胞中的自噬（autophagy）。 |
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| S3393New |
SBP-7455SBP-7455 是一种双特异性 ULK1/2 自噬抑制剂，在 ADP-Glo 试验中对 ULK1 和 ULK2 的 IC50 分别为 13 nM 和 476 nM。 |
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| S7948 |
MRT67307 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。MRT67307 可有效地抑制 ULK1 和 ULK2 并限制自噬。 |
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| S7949 |
MRT68921 HClMRT68921是一个高效的双重的自噬激酶ULK1/2抑制剂，其IC50分别为2.9 nM和1.1 nM。 |
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| S8793 |
ULK-101ULK-101是一种有效的、选择性的ULK1抑制剂，对ULK1和ULK2的IC50值分别为8.3 nM和30 nM。 |
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| S0819 |
BL-918BL-918 是一种有效的口服活性的 UNC-51-like kinase 1 (ULK1) 的激活剂，EC50值为24.14 nM，Kd值为0.719 μM。BL-918 可诱导细胞保护性的自噬，用于治疗帕金森氏病。 |
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| S8597 |
LYN-1604LYN-1604是一种潜在的ULK1激动剂，在MDA-MB-231细胞中IC50为1.66 μM。它能与野生型ULK1结合，Kd=291.4 nM。与突变型ULK1蛋白ULK1(Y89A)的结合亲和力急剧减小，其Kd值比ULK1、ULK1 (K50A)和ULK1 (L53A)大。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor)是一种有效的，特异性ATM抑制剂，在无细胞试验中IC50/Ki为12.9 nM/2.2 nM，与DNA-PK， PI3K/PI4K， ATR和mTOR相比，对ATM具有高度选择性。KU‑55933 (ATM Kinase Inhibitor)可抑制 autophagy‑initiating kinase ULK1 的激活从而导致自噬的显著减少。 |
Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated. |
|
| S1113 |
GSK690693GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。 |
UPN cells were treated with GSK690693 or MK2206 (1 uM) for 1h followed by LPA (10 uM), EGF or IGF-1 (10 ng/ml) for another 1h and Western blot was performed. Band intensities of phospho-AKT (p-AKTS473), phospho-S6 (p-S6S240/S244), phospho-YB-1 (p-YB-1S102) and YB-1 were quantified and normalized to the intensity of ERK2. It directly determined the role of AKT using two potent, AKT inhibitors with distinct actions—a catalytic domain inhibitor, GSK690693, and an allosteric inhibitor, MK2206 -in UPN and SKOV3 cells, which showed appreciable AKT and YB-1 phosphorylation upon growth factor stimulation. GSK690693 increased basal and growth factor-induced AKT phosphorylation due to blocking a negative feedback loop downstream of AKT, whereas MK2206 abolished both basal and growth-factor-induced AKT phosphorylation.
|
|
| S7885 |
SBI-0206965SBI-0206965 是一种高度选择性自吞噬激酶ULK1抑制剂，IC50为108 nM，选择性比作用于ULK2高7倍。SBI-0206965 可抑制人胶质母细胞瘤和肺癌细胞中的自噬而增强凋亡。 |
Inhibition of autophagy advances LPS-induced accumulation of G-MDSCs in vivo and in vitro. (A-E) C57BL/6 mice were treated with SBI-0206965 (5 μg/g) or vehicle for 2 h followed by LPS challenge (10 μg/g). Percentages of CD11b+Gr-1+ MDSCs (A, C), CD11b+Ly6G+Ly6Clow G-MDSCs (B, D) and CD11b+Ly6G-Ly6Chigh M-MDSCs (B, E) in spleens of these mice were analyzed with FACS at 12, 24 and 36 hours. The data are shown as the means ± SEM (n=5 replicates/group) and are representative of three independent experiments. (F, G) Bone marrow cells were pretreated with SBI-0206965 (1 μg/ml) or vehicle for 2 h and then cultured with GM-CSF (40 ng/ml) and IL-6 (40 ng/ml). Four days later, the percentages of CD11b+Gr-1+ MDSCs (F), CD11b+Ly6G+Ly6Clow G-MDSCs (G) and CD11b+Ly6G- Ly6Chigh M-MDSCs (G) were analyzed with FACS. Data are representative from one out of three biological replicates, each with three technical replicates. Error bars represent S.E.M. * p < 0.05, ** p < 0.01, *** p < 0.001, as determined by ANOVA tests; ns denotes p > 0.05. |
|
| S6386New |
MRT67307MRT67307（IKKε/TBK1 Inhibitor II）抑制IKKϵ/TBK1，在体外ATP（终浓度 0.1 mM）实验中，其IC50分别为160和19 nM，但当其浓度为10 μM时，对 IKKα 和 IKKβ 没有抑制作用。MRT67307 也是 ULK1 和 ULK2的抑制剂 ，其IC50分别为45和38 nM。MRT67307可阻断细胞中的自噬（autophagy）。 |
||
| S3393New |
SBP-7455SBP-7455 是一种双特异性 ULK1/2 自噬抑制剂，在 ADP-Glo 试验中对 ULK1 和 ULK2 的 IC50 分别为 13 nM 和 476 nM。 |
||
| S7948 |
MRT67307 HClMRT67307是一种高效的双重的IKKϵ /TBK1抑制剂，其IC50分别为160和19 nM。MRT67307 可有效地抑制 ULK1 和 ULK2 并限制自噬。 |
|
|
| S7949 |
MRT68921 HClMRT68921是一个高效的双重的自噬激酶ULK1/2抑制剂，其IC50分别为2.9 nM和1.1 nM。 |
|
|
| S8793 |
ULK-101ULK-101是一种有效的、选择性的ULK1抑制剂，对ULK1和ULK2的IC50值分别为8.3 nM和30 nM。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S0819 |
BL-918BL-918 是一种有效的口服活性的 UNC-51-like kinase 1 (ULK1) 的激活剂，EC50值为24.14 nM，Kd值为0.719 μM。BL-918 可诱导细胞保护性的自噬，用于治疗帕金森氏病。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S8597 |
LYN-1604LYN-1604是一种潜在的ULK1激动剂，在MDA-MB-231细胞中IC50为1.66 μM。它能与野生型ULK1结合，Kd=291.4 nM。与突变型ULK1蛋白ULK1(Y89A)的结合亲和力急剧减小，其Kd值比ULK1、ULK1 (K50A)和ULK1 (L53A)大。 |
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