Home PI3K/Akt/mTOR ATM/ATR

ATM/ATR Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Cancer Cell, 2025, 43(8):1530-1548.e9
Cell Rep, 2025, 44(1):115114
Neoplasia, 2025, 60:101104
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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.
Cancer Cell, 2025, 43(8):1530-1548.e9
J Clin Invest, 2025, 135(8)e181659
Nucleic Acids Res, 2025, 53(12)gkaf544
S8096 Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. This compound inhibits MRN-dependent activation of ATM.
Nat Commun, 2025, 16(1):4491
Nucleic Acids Res, 2025, 53(11)gkaf468
Redox Biol, 2025, 80:103504
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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.
Cell Rep, 2025, 44(4):115431
iScience, 2025, 28(2):111842
Cancer Sci, 2025, 10.1111/cas.70043
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
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S3600 Schisandrin 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.
Phytomedicine, 2025, 141:156672
Front Pharmacol, 2025, 16:1547685
Sci Rep, 2025, 15(1):8452
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.
Cancer Cell, 2025, 43(8):1530-1548.e9
Mol Syst Biol, 2025, 21(3):231-253
Cell Death Dis, 2023, 14(6):348
S8050 ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.
EMBO J, 2025, 44(21):6112-6136
mBio, 2024, e0228723.
iScience, 2023, 25(7)
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. This compound potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. It exhibits potential antineoplastic activity.
Mol Syst Biol, 2025, 21(3):231-253
iScience, 2025, 28(3):111943
Nat Biomed Eng, 2024, 10.1038/s41551-024-01277-5
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)
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S0148 HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. This compound inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
Cell Commun Signal, 2024, 22(1):600
mBio, 2023, e0352822.
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
E1411 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. This compound increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. It inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, this chemical induces cell cycle arrest at the G2/M phase and apoptosis.
E1989 ART0380 (Alnodesertib) ART0380 (IACS-030380) is a potent and selective, orally bioavailable inhibitor of ATR kinase, with an IC50 of 51.7 nM effectively inhibiting the enzyme activity of the ATR-ATRIP complex. It functions as an ATP-competitive inhibitor, binding to the ATP pocket of ATR, where ATP would typically bind. It interacts with the hinge through its morpholine oxygen and occupies the ribose pocket with a sulfoximine group. It also exhibits antitumor activity.
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.
E1512 M3541 M3541 is a potent and selective inhibitor of ATM kinase activity with an IC50 value of 0.25 nM in cell-free assays. This compound 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. It inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell, induces autophagy, and suppresses HIV-1 replication. Phase 2.
Adv Mater, 2025, e12810.
Nat Commun, 2025, 16(1):8189
Nat Commun, 2025, 16(1):4502
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S2758 Wortmannin (SL-2052) 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, 2025, 16(1):1313
EMBO J, 2025, 10.1038/s44318-025-00507-z
EMBO Mol Med, 2025, 10.1038/s44321-025-00222-6
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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. This compound triggers DNA damage characterized by activation of the ATM/ATR pathway. It induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. This chemical 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