ATM/ATR
特异性亚型抑制剂
ATM/ATR产品
产品目录 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1009 |
Dactolisib (BEZ235, NVP-BEZ235)Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。 |
![]() ![]() Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments. |
|
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。 |
![]() ![]()
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是一种改进的KU-55933类似物,在无细胞试验中作用于ATM,IC50为6.3 nM,作用于ATM比作用于DNA-PK和ATR的选择性分别高270和1600倍,并且是高度有效的放射增敏剂。 |
![]() ![]() |
|
S8007 |
VE-821VE-821是一种有效的,选择性的,ATP竞争性ATR抑制剂,在无细胞试验中Ki/IC50为13 nM/26 nM,抑制H2AX磷酸化,对PIKKs ATM, DNA-PK, mTOR和PI3Kγ具有很低的抑制活性。 |
![]() ![]() Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.
|
|
S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂,在无细胞试验中IC50为3 nM,对 PI3K 家族的选择性较低。也会抑制自噬体的形成,并有效抑制DNA-PK/ATM,在无细胞试验中IC50为16 nM和150 nM。 |
![]() ![]() 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 是一种有效的选择性mTOR抑制剂,在p53−/− MEFs细胞系中IC50为0.25 nM;作用于mTOR比作用于PI3K选择性高800倍,并且改善了药代动力学性能。抑制ATM/ATR/DNA-PK,在PC3细胞系中EC50分别为28 nM/35 nM/118 nM。 |
![]() ![]() U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/Pi before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
|
|
S2245 |
CP-466722CP-466722是一种有效的,可逆的ATM抑制剂,不影响ATR,且抑制PI3K或PIKK家族成员。 |
![]() ![]() |
|
S7102 |
Berzosertib (VE-822|VX970|M6620)VE-822是一种ATR抑制剂,在HT29细胞中IC50 为 19 nM。 |
![]() ![]() 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.
|
|
S8050 |
ETP-46464ETP-46464是一种有效的,选择性ATR抑制剂,IC50为25 nM。 |
||
S7136 |
CGK 733CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为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是一种新型有效的选择性ATR激酶抑制剂,无细胞试验中IC50为5 nM,比作用于mTOR的选择性高8倍。 |
![]() ![]() (B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
|
|
S8556 |
AZ31AZ31是一种选择性的ATM抑制剂,IC50小于0.0012 μM。它具有良好的选择性,对ATM的选择性比对DNA-PK和PI3Kα高500倍,比对mTOR、PI3Kβ和PI3Kγ的选择性高1000倍。 |
||
S7693 |
AZD6738AZD6738是一种口服具有活性的,选择性 ATR 激酶抑制剂,IC50 为 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.
|
|
S8729 |
AZ32AZ32是ATM kinase的特异性抑制剂,在小鼠中具有良好的血脑屏障通透性,对ATM酶的IC5值小于0.0062 μM。它具有充分的选择性和高细胞透性。 |
||
S8680 |
AZD1390AZD1390是一种具有口服活性的、能穿透中枢神经系统的ATM抑制剂,在细胞中IC50为0.78 nM。它对ATM的选择性是对PIKK家族其他相关酶的10,000以上,具有良好的选择性。 |
||
S3600 |
Schisandrin B (Sch B)Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。 |
||
S8096 |
MirinMirin是有效的Mre11–Rad50–Nbs1(MRN)复合体抑制剂,能够抑制Mre11相关的外切酶活性。 |
![]() ![]() 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是有效的、高选择性的、具有口服生物活性的ATR抑制剂,IC50为7 nM。 |
||
S8375 |
AZD0156AZD0156是有效的、选择性的ATM激酶抑制剂,具有潜在的化疗/辐射增敏和抗肿瘤活性。 |
||
S4157 |
Chloroquine diphosphateChloroquine diphosphate是一种4-氨基喹啉的抗疟疾和抗风湿药,也是一种ATM激活剂。 |
![]() ![]() 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. |
产品目录 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1009 |
Dactolisib (BEZ235, NVP-BEZ235)Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂,在无细胞试验中,抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR,IC50 为 21 nM,而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。 |
![]() ![]() Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments. |
|
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。 |
![]() ![]()
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是一种改进的KU-55933类似物,在无细胞试验中作用于ATM,IC50为6.3 nM,作用于ATM比作用于DNA-PK和ATR的选择性分别高270和1600倍,并且是高度有效的放射增敏剂。 |
![]() ![]() |
|
S8007 |
VE-821VE-821是一种有效的,选择性的,ATP竞争性ATR抑制剂,在无细胞试验中Ki/IC50为13 nM/26 nM,抑制H2AX磷酸化,对PIKKs ATM, DNA-PK, mTOR和PI3Kγ具有很低的抑制活性。 |
![]() ![]() Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.
|
|
S2758 |
WortmanninWortmannin是一种首次命名的PI3K抑制剂,在无细胞试验中IC50为3 nM,对 PI3K 家族的选择性较低。也会抑制自噬体的形成,并有效抑制DNA-PK/ATM,在无细胞试验中IC50为16 nM和150 nM。 |
![]() ![]() 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 是一种有效的选择性mTOR抑制剂,在p53−/− MEFs细胞系中IC50为0.25 nM;作用于mTOR比作用于PI3K选择性高800倍,并且改善了药代动力学性能。抑制ATM/ATR/DNA-PK,在PC3细胞系中EC50分别为28 nM/35 nM/118 nM。 |
![]() ![]() U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/Pi before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
|
|
S2245 |
CP-466722CP-466722是一种有效的,可逆的ATM抑制剂,不影响ATR,且抑制PI3K或PIKK家族成员。 |
![]() ![]() |
|
S7102 |
Berzosertib (VE-822|VX970|M6620)VE-822是一种ATR抑制剂,在HT29细胞中IC50 为 19 nM。 |
![]() ![]() 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.
|
|
S8050 |
ETP-46464ETP-46464是一种有效的,选择性ATR抑制剂,IC50为25 nM。 |
||
S7136 |
CGK 733CGK 733是一种有效的ATM/ATR选择性抑制剂,IC50约为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是一种新型有效的选择性ATR激酶抑制剂,无细胞试验中IC50为5 nM,比作用于mTOR的选择性高8倍。 |
![]() ![]() (B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
|
|
S8556 |
AZ31AZ31是一种选择性的ATM抑制剂,IC50小于0.0012 μM。它具有良好的选择性,对ATM的选择性比对DNA-PK和PI3Kα高500倍,比对mTOR、PI3Kβ和PI3Kγ的选择性高1000倍。 |
||
S7693 |
AZD6738AZD6738是一种口服具有活性的,选择性 ATR 激酶抑制剂,IC50 为 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.
|
|
S8729 |
AZ32AZ32是ATM kinase的特异性抑制剂,在小鼠中具有良好的血脑屏障通透性,对ATM酶的IC5值小于0.0062 μM。它具有充分的选择性和高细胞透性。 |
||
S8680 |
AZD1390AZD1390是一种具有口服活性的、能穿透中枢神经系统的ATM抑制剂,在细胞中IC50为0.78 nM。它对ATM的选择性是对PIKK家族其他相关酶的10,000以上,具有良好的选择性。 |
||
S3600 |
Schisandrin B (Sch B)Schisandrin B (Sch B)是中草药五味子(Turcz.)中含量最丰富的二苯并环辛二烯木酚素。它是一种安全的ATR和P-gp抑制剂。 |
||
S8096 |
MirinMirin是有效的Mre11–Rad50–Nbs1(MRN)复合体抑制剂,能够抑制Mre11相关的外切酶活性。 |
![]() ![]() 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是有效的、高选择性的、具有口服生物活性的ATR抑制剂,IC50为7 nM。 |
||
S8375 |
AZD0156AZD0156是有效的、选择性的ATM激酶抑制剂,具有潜在的化疗/辐射增敏和抗肿瘤活性。 |
产品目录 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S4157 |
Chloroquine diphosphateChloroquine diphosphate是一种4-氨基喹啉的抗疟疾和抗风湿药,也是一种ATM激活剂。 |
![]() ![]() 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. |