ATM/ATR

亜型選択性的な製品

シグナル伝達経路

ATM/ATRシグナル伝達経路

ATM/ATR製品

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  • ATM/ATR阻害剤 (27)
  • ATM/ATR活性剤(3)
  • 新製品
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S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
S1092 KU-55933 KU-55933 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. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S8007 VE-821 VE-821(ATR inhibitor IV) 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 Rep Med, 2024, 5(2):101393
Genes Dev, 2024, 38(1-2):70-94
Cell Rep, 2024, 43(2):113779
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S1570 KU-60019 KU-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.
Adv Sci (Weinh), 2023, 10(28):e2206931
Blood Cancer J, 2023, 13(1):42
Cancer Res, 2023, 83(1):141-157
S7102 Berzosertib (VE-822) Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
Genes Dev, 2024, 38(1-2):70-94
Neurooncol Adv, 2024, 6(1):vdad165
Cell, 2023, 186(3):528-542.e14
S7693 Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Neurooncol Adv, 2024, 6(1):vdad165
Nat Commun, 2023, 14(1):5003
J Exp Clin Cancer Res, 2023, 42(1):8
S2817 Torin 2 Torin 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. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
S7050 AZ20 AZ20 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.
Nucleic Acids Res, 2023, 51(19):10467-10483
Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
Nucleic Acids Res, 2023, gkad732
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Mol Cancer, 2023, 22(1):100
Nat Commun, 2023, 14(1):5003
Int J Biol Sci, 2023, 19(3):981-993
S8096 Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.
Nat Struct Mol Biol, 2023, 30(1):115-124
Nat Struct Mol Biol, 2023, 30(1):115-124
Nat Commun, 2023, 14(1):6265
S8680 AZD1390 AZD1390 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.
Int J Biol Sci, 2023, 19(3):981-993
Int J Biol Sci, 2023, 19(3):981-993
Cancer Chemother Pharmacol, 2023, 92(1):57-69
S2245 CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.
G3 (Bethesda), 2020, 4;10(5):1585-1597
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S8666 Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Cell Death Dis, 2023, 14(6):348
Cell Rep, 2023, 42(4):112296
Commun Biol, 2023, 6(1):660
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
mBio, 2024, e0228723.
iScience, 2023, 25(7)
Cell Rep, 2022, 41(11):111836
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.
Viruses, 2022, 14(2)353
Pharmacol Res, 2021, 166:105459
Ann Transl Med, 2021, 9(19):1500
S7136 CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Exp Cell Res, 2022, S0014-4827(22)00218-X
Aging (Albany NY), 2021, 13(8):11705-11726
mBio, 2020, 11(1)
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
Neurooncol Adv, 2024, 6(1):vdad165
Cancer Chemother Pharmacol, 2023, 92(1):57-69
Am J Transl Res, 2023, 15(7):4902-4911
S9639 VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
bioRxiv, 2024,
Viruses, 2023, 15(5)1112
NAR Cancer, 2023, 5(1):zcac045
S8556 AZ31 AZ31 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).
Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S8729 AZ32 AZ32 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.
Cancers (Basel), 2022, 14(20)4984
S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
mBio, 2023, e0352822.
E1411New Tuvusertib Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines.
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
E1108 Camonsertib (RP-3500) Camonsertib (RP-3500) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM.
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
Theranostics, 2024, 14(4):1371-1389
E1057 Lartesertib (M4076) Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines.
E1136 SKLB-197 SKLB-197 exerts selectively inhibition against ataxia telangiectasia mutated and Rad3-related (ATR) kinase with IC50 of 0.013 μM, also displays potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
E1512New M3541 M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. M3541 suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Mol Oncol, 2024, 10.1002/1878-0261.13577
Mil Med Res, 2023, 10(1):35
Mil Med Res, 2023, 10(1):35
S1092 KU-55933 KU-55933 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. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.
Nucleic Acids Res, 2024, gkad1224
Cell Rep Med, 2024, 5(2):101393
Clin Cancer Res, 2024, 30(1):187-197
S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
S8007 VE-821 VE-821(ATR inhibitor IV) 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 Rep Med, 2024, 5(2):101393
Genes Dev, 2024, 38(1-2):70-94
Cell Rep, 2024, 43(2):113779
S1570 KU-60019 KU-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.
Adv Sci (Weinh), 2023, 10(28):e2206931
Blood Cancer J, 2023, 13(1):42
Cancer Res, 2023, 83(1):141-157
S7102 Berzosertib (VE-822) Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.
Genes Dev, 2024, 38(1-2):70-94
Neurooncol Adv, 2024, 6(1):vdad165
Cell, 2023, 186(3):528-542.e14
S7693 Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.
Neurooncol Adv, 2024, 6(1):vdad165
Nat Commun, 2023, 14(1):5003
J Exp Clin Cancer Res, 2023, 42(1):8
S2817 Torin 2 Torin 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. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
S7050 AZ20 AZ20 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.
Nucleic Acids Res, 2023, 51(19):10467-10483
Cell Death Differ, 2023, 10.1038/s41418-023-01167-4
Nucleic Acids Res, 2023, gkad732
S8375 AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.
Mol Cancer, 2023, 22(1):100
Nat Commun, 2023, 14(1):5003
Int J Biol Sci, 2023, 19(3):981-993
S8096 Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.
Nat Struct Mol Biol, 2023, 30(1):115-124
Nat Struct Mol Biol, 2023, 30(1):115-124
Nat Commun, 2023, 14(1):6265
S8680 AZD1390 AZD1390 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.
Int J Biol Sci, 2023, 19(3):981-993
Int J Biol Sci, 2023, 19(3):981-993
Cancer Chemother Pharmacol, 2023, 92(1):57-69
S2245 CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.
G3 (Bethesda), 2020, 4;10(5):1585-1597
Cell, 2019, 36(2):179-193
Cancer Cell, 2019, 36(2):179-193
S8666 Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.
Cell Death Dis, 2023, 14(6):348
Cell Rep, 2023, 42(4):112296
Commun Biol, 2023, 6(1):660
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
mBio, 2024, e0228723.
iScience, 2023, 25(7)
Cell Rep, 2022, 41(11):111836
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.
Viruses, 2022, 14(2)353
Pharmacol Res, 2021, 166:105459
Ann Transl Med, 2021, 9(19):1500
S7136 CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.
Exp Cell Res, 2022, S0014-4827(22)00218-X
Aging (Albany NY), 2021, 13(8):11705-11726
mBio, 2020, 11(1)
S9864 Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
Neurooncol Adv, 2024, 6(1):vdad165
Cancer Chemother Pharmacol, 2023, 92(1):57-69
Am J Transl Res, 2023, 15(7):4902-4911
S9639 VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
bioRxiv, 2024,
Viruses, 2023, 15(5)1112
NAR Cancer, 2023, 5(1):zcac045
S8556 AZ31 AZ31 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).
Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S8729 AZ32 AZ32 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.
Cancers (Basel), 2022, 14(20)4984
S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
mBio, 2023, e0352822.
E1411New Tuvusertib Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines.
E1108 Camonsertib (RP-3500) Camonsertib (RP-3500) is a highly potent and selective inhibitor of ATR kinase with an IC50 of 1 nM.
E1057 Lartesertib (M4076) Lartesertib (M4076) inhibits Ataxia telangiectasia-mutated (ATM) kinase activity with a sub-nanomolar potency and shows remarkable selectivity against other protein kinases, suppresses DSB repair, clonogenic cancer cell growth, and potentiates antitumor activity of ionizing radiation in cancer cell lines.
E1136 SKLB-197 SKLB-197 exerts selectively inhibition against ataxia telangiectasia mutated and Rad3-related (ATR) kinase with IC50 of 0.013 μM, also displays potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
E1512New M3541 M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. M3541 suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines.
S4157 Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).
Nat Commun, 2024, 15(1):1642
Sci Rep, 2024, 14(1):4000
Cell Discov, 2023, 9(1):92
S3224 Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S6885 Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.
Theranostics, 2024, 14(4):1371-1389
E1411New Tuvusertib Tuvusertib (M1774, ATR inhibitor 1) is a potent ATR inhibitor, which exhibits anti-proliferative and anti-tumor effects in cancer cell lines.
E1512New M3541 M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. M3541 suppresses double-strand breaks (DSB) repair, clonogenic cancer cell growth and potentiates antitumor activity of ionizing radiation in cancer cell lines.

ATM/ATR阻害剤の選択性比較

Tags: ATM inhibition | ATR inhibition | ATM kinase activation | ATM kinase assay | ATM protein kinase | ATM signaling pathway | ATM inhibitor drugs | ATM tumor | ATM phosphorylation | ATM targets | ATM cancer | ATM activity | ATM inhibitor clinical trial | ATM inhibitor review