ATM/ATR

ATM Inhibitor-8 is a selective and potent inhibitor of Ataxia Telangiectasia Mutated (ATM) kinase, exhibiting an IC50 of 1.15 nM. This compound demonstrates significant anti-tumor activity, making it valuable for research in cancer biology and therapeutic development. Its oral bioavailability enhances its utility in in vivo studies exploring the role of ATM inhibition in various malignancies.

ATR kinase-IN-3 is a potent ATR protein kinase inhibitor with a Ki value ranging from 0.01 to 1 μM. This compound significantly modulates the ATR signaling pathway, making it valuable for studies in cancer biology, particularly in understanding DNA damage response mechanisms. Its ability to inhibit ATR activity can aid in assessing the therapeutic potential of targeting this pathway in various cancer models.

ATR-IN-16 is a potent inhibitor of the ATR kinase, a critical regulator of the DNA damage response pathway. This compound demonstrates significant anticancer activity, exhibiting an IC50 of 410 nM in LoVo cells. ATR-IN-16 is applicable in cancer research, particularly for studies focused on DNA repair mechanisms and therapeutic strategies targeting ATR signaling.

ATR-IN-33 is a selective ATR kinase inhibitor that targets the ataxia telangiectasia and Rad3-related protein, involved in the DNA damage response. By inhibiting ATR activity, ATR-IN-33 effectively impairs cellular repair mechanisms, which can lead to enhanced sensitivity to DNA-damaging agents. This compound is valuable for research applications in cancer biology, particularly in studies assessing tumor response to therapy and exploring mechanisms of resistance.

Ceralasertib formate is a highly potent and selective inhibitor of ATR (ataxia telangiectasia and Rad3-related protein) with an IC50 value of 1 nM. This compound effectively inhibits cell viability, induces DNA damage, and promotes cellular senescence. Ceralasertib formate demonstrates notable antitumor activity and is valuable for research applications focused on cancer therapeutics and DNA damage response pathways.

CGK733 is a selective inhibitor of ATR and ATM kinases. Induces cell death in prematurely senescent breast cancer cells.

AZ20 is a potent and selective inhibitor of ATR with an IC50 value of 5 nM.

NU6027 is a potent inhibitor of cellular ATR activity (IC(50)=6.7 μM) and enhanced hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

Mirin prevents ATM activation in response to double strand breaks (IC50 = 12 uM) and induces G2 cell cycle arrest.

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.

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).

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.

Gartisertib (VX-803, ATR inhibitor 2) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM.

KU 59403 is a potent ATM inhibitor, with an IC50 of 3 nM.

ATR inhibitor 1 is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, has a Ki value below 1 ?μ.

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC50 of 0.7 nM.

AD1058 is a selective, orally active inhibitor of Ataxia Telangiectasia and Rad3 related protein (ATR) with an IC50 of 1.6 nM. This compound demonstrates significant anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis in various cancer models. AD1058 is particularly relevant for research focused on advanced malignancies and brain metastases, providing a valuable tool for investigating therapeutic strategies in these challenging areas.

ART0380 is a potent and selective ATR kinase inhibitor that targets the ATR-ATRIP complex. With an IC50 of 51.7 nM, ART0380 effectively inhibits ATR-dependent Chk1 serine 345 phosphorylation, leading to cell cycle disruption and DNA damage. This compound exhibits significant antitumor activity in preclinical models featuring various ataxia-telangiectasia mutated (ATM) gene alterations. ART0380 is applicable for cancer research, particularly in studies related to colorectal and prostate cancer.

ATM Inhibitor-7 is a selective inhibitor of ataxia-telangiectasia mutated (ATM) with an IC50 of 1.0 nM. This compound effectively induces apoptosis and causes G2/M phase cell cycle arrest, particularly when combined with CPT-11. ATM Inhibitor-7 is utilized in research applications focused on elucidating mechanisms of tumor biology and enhancing the efficacy of chemotherapeutic agents.

Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit the growth of various hematopoietic cell lines. Furthermore, in combination with the ATR inhibitor Tuvusertib, Lartesertib enhances tumor cell apoptosis and activates immune signaling pathways, showcasing significant anti-tumor efficacy.

(Rac)-Lartesertib is a potent inhibitor of the serine/threonine protein kinase ATM. This compound has demonstrated the ability to inhibit cell proliferation in various hematopoietic cell lines. Moreover, when used in conjunction with the ATR inhibitor Tuvusertib, (Rac)-Lartesertib can enhance tumor cell death, activate immune signaling pathways, and exhibit notable anti-tumor efficacy, making it a valuable tool for cancer research.