ATM/ATR
シグナル伝達経路
研究分野
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S1092 | KU-55933 (ATM Kinase Inhibitor) | <1 mg/mL | 33 mg/mL | <1 mg/mL |
| S1570 | KU-60019 | <1 mg/mL | 18 mg/mL | <1 mg/mL |
| S8007 | VE-821 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2758 | Wortmannin | <1 mg/mL | 85 mg/mL | <1 mg/mL |
| S2817 | Torin 2 | <1 mg/mL | 20 mg/mL | <1 mg/mL |
| S8556 | AZ31 | <1 mg/mL | 53 mg/mL | <1 mg/mL |
| S8729 | AZ32 | <1 mg/mL | 66 mg/mL | 7 mg/mL |
| S8680 | AZD1390 | <1 mg/mL | 14 mg/mL | 95 mg/mL |
| S2245 | CP-466722 | <1 mg/mL | 0.28 mg/mL | <1 mg/mL |
| S7102 | VE-822 | <1 mg/mL | 36 mg/mL | <1 mg/mL |
| S7136 | CGK 733 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7050 | AZ20 | <1 mg/mL | 83 mg/mL | 3 mg/mL |
| S7693 | AZD6738 | <1 mg/mL | 82 mg/mL | 41 mg/mL |
| S3600 | Schisandrin B (Sch B) | <1 mg/mL | 80 mg/mL | 10 mg/mL |
| S8096 | Mirin | <1 mg/mL | 44 mg/mL | <1 mg/mL |
| S8666 | BAY 1895344 (BAY-1895344) | 82 mg/mL | 82 mg/mL | 82 mg/mL |
| S8375 | AZD0156 | <1 mg/mL | 0.3 mg/mL | 2 mg/mL |
| S4157 | Chloroquine Phosphate | 100 mg/mL | <1 mg/mL | <1 mg/mL |
亜型選択性的な製品
ATM/ATR製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. |
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. |
|
| S1570 |
KU-60019KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. |
The ATM-dependent Ser15-p53 phosphorylation was monitored by Western blotting. Protein loading levels were monitored by probing for actin.
|
|
| S8007 |
VE-821VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ. |
Cell viability response to ATR inhibitor.
|
|
| S2758 |
WortmanninWortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
|
| S2817 |
Torin 2Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. |
Immunofluorescent imaging of HAECs using VE-CAD (red) and p120 (green) antibodies was performed 12 h after DMSO (control), Torin-2 (100 nM), or EVL (500 nM) treatments. White arrows denote interendothelial gaps. White bar indicates 50 μm. EVL treatment increased VE-CAD mobilization from the membrane into the cytosol (relative to DMSO) with evidence of intracellular deposits and interendothelial gaps, whereas in DMSO-treated cells, there was colocalization of p120 and VE-CAD (yellow border) with no evidence of gap formation. In Torin-2-treated cells, there was evidence of colocalization of p120 and VE-CAD at cell borders with minimal interendothelial gap formation.
|
|
| S8556新 |
AZ31AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). |
||
| S8729新 |
AZ32AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. |
||
| S8680新 |
AZD1390AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. |
||
| S2245 |
CP-466722CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells. |
HCT116 cells expressing the DDR-Act reporter were treated with Etoposide 20 μM (E20) for 24 hours, in the absence or in the presence of KU-55933 or CP-466722 at the indicated concentration. (A) Western blot analysis of p53 and actin as control.
|
|
| S7102 |
VE-822VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells. |
Western blot analysis of scr or siPNUTS transfected cells without IR or 6 h after 10 Gy. VE-822 was added for 2, 5, 15, 30 or 60 min to indicated samples 6 h after 10 Gy.
|
|
| S7136 |
CGK 733CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
|
|
| S7050 |
AZ20AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. |
(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
|
|
| S7693 |
AZD6738AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. |
Number of γH2AX foci per cell of irradiated (2 Gy) SAS cells treated with inhibitors against ATM (ATMi, KU55933), DNA-PK (DNA-PKi, KU57788), or ATR (ATRi, AZD6738) with or without LY364947.
|
|
| S3600 |
Schisandrin B (Sch B)Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety. |
||
| S8096 |
MirinMirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. |
Wildtype bone marrow-derived macrophages (BMDMs) were incubated with and without the MRN complex inhibitor mirin (administered dose of 100 μM) for 2 hours, then were treated with PM (100 μg/mL) for an additional 24 hours. (A) The relative levels of Cxcl1, Cxcl2 and Ifn-γ mRNA transcripts were determined using quantitative PCR. (B) The protein levels of Cxcl1, Cxcl2 and Ifn-γ in the culture supernatants were measured using ELISA. Data are presented as means ± SEMs across at least 3 independent experiments. *p < 0.05; **p < 0.01.
|
|
| S8666 |
BAY 1895344 (BAY-1895344)BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. |
||
| S8375 |
AZD0156AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. |
||
| S4157 |
Chloroquine PhosphateChloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. |
NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S1092 |
KU-55933 (ATM Kinase Inhibitor)KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/Ki of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. |
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. |
|
| S1570 |
KU-60019KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer. |
The ATM-dependent Ser15-p53 phosphorylation was monitored by Western blotting. Protein loading levels were monitored by probing for actin.
|
|
| S8007 |
VE-821VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ. |
Cell viability response to ATR inhibitor.
|
|
| S2758 |
WortmanninWortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. |
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment. |
|
| S2817 |
Torin 2Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. |
Immunofluorescent imaging of HAECs using VE-CAD (red) and p120 (green) antibodies was performed 12 h after DMSO (control), Torin-2 (100 nM), or EVL (500 nM) treatments. White arrows denote interendothelial gaps. White bar indicates 50 μm. EVL treatment increased VE-CAD mobilization from the membrane into the cytosol (relative to DMSO) with evidence of intracellular deposits and interendothelial gaps, whereas in DMSO-treated cells, there was colocalization of p120 and VE-CAD (yellow border) with no evidence of gap formation. In Torin-2-treated cells, there was evidence of colocalization of p120 and VE-CAD at cell borders with minimal interendothelial gap formation.
|
|
| S8556新 |
AZ31AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ). |
||
| S8729新 |
AZ32AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability. |
||
| S8680新 |
AZD1390AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. |
||
| S2245 |
CP-466722CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells. |
HCT116 cells expressing the DDR-Act reporter were treated with Etoposide 20 μM (E20) for 24 hours, in the absence or in the presence of KU-55933 or CP-466722 at the indicated concentration. (A) Western blot analysis of p53 and actin as control.
|
|
| S7102 |
VE-822VE-822 is an ATR inhibitor with IC50 of 19 nM in HT29 cells. |
Western blot analysis of scr or siPNUTS transfected cells without IR or 6 h after 10 Gy. VE-822 was added for 2, 5, 15, 30 or 60 min to indicated samples 6 h after 10 Gy.
|
|
| S7136 |
CGK 733CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM. |
K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
|
|
| S7050 |
AZ20AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. |
(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
|
|
| S7693 |
AZD6738AZD6738 is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2. |
Number of γH2AX foci per cell of irradiated (2 Gy) SAS cells treated with inhibitors against ATM (ATMi, KU55933), DNA-PK (DNA-PKi, KU57788), or ATR (ATRi, AZD6738) with or without LY364947.
|
|
| S3600 |
Schisandrin B (Sch B)Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety. |
||
| S8096 |
MirinMirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. |
Wildtype bone marrow-derived macrophages (BMDMs) were incubated with and without the MRN complex inhibitor mirin (administered dose of 100 μM) for 2 hours, then were treated with PM (100 μg/mL) for an additional 24 hours. (A) The relative levels of Cxcl1, Cxcl2 and Ifn-γ mRNA transcripts were determined using quantitative PCR. (B) The protein levels of Cxcl1, Cxcl2 and Ifn-γ in the culture supernatants were measured using ELISA. Data are presented as means ± SEMs across at least 3 independent experiments. *p < 0.05; **p < 0.01.
|
|
| S8666 |
BAY 1895344 (BAY-1895344)BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM. |
||
| S8375 |
AZD0156AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S4157 |
Chloroquine PhosphateChloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. |
2017, 10.1038/leu.2016.325 2016, 28(8):1086-98 2017, 10.3892/ijmm.2017.3008 |
NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1. |
