ATM/ATR Inhibitor

ETP-46464 is an effective mTOR and ATR inhibitor with IC₅₀s of 0.6 and 14 nM, respectively.

Ro 90-7501 is an amyloid β₄₂ (Aβ₄₂) fibril assembly inhibitor that reduces Aβ₄₂-induced cytotoxicity (EC₅₀ of 2 μM). Ro 90-7501 inhibits ATM phosphorylation and DNA repair. RO 90-7501 selectively enhances toll-like receptor 3 (TLR3) and RIG-I-like receptor (RLR) ligand-induced IFN-β gene expression and antiviral response. Ro 90-7501 also inhibits protein phosphatase 5 (PP5) in a TPR-dependent manner. Ro 90-7501 has significant radiosensitizing effects on cervical cancer cells.

XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC₅₀s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.

AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC₅₀: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases.

CP-466722 is a rapidly reversible inhibitor of ATM, with an IC₅₀ of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.

(S)-Ceralasertib ((S)-AZD6738) is the S-enantiomer of Ceralasertib (HY-19323). (S)-Ceralasertib is the inhibitor for ataxia telangiectasia mutated and rad3 related (ATR).

AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC₅₀ of <1.2 nM for ATM enzyme, and an IC₅₀ of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.

NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with K_is of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

WSD0628 is a brain penetrant and potent ATM inhibitor with profound radiosensitizing effect.

M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC₅₀ of 0.25 nM. M3541 shows remarkable selectivity against other protein kinases. M3541 suppresses double-strand breaks (DSB) repair and has antitumor activities.

Hexapeptide-11 is an anti-aging peptide that can protect fibroblasts from premature cell senescence mediated by oxidative stress. Hexapeptide-11 is also a potential stimulator of hyaluronic acid in keratinocytes, and can enhance skin barrier function by upregulating the expression of HAS2 and EGR3, and downregulating the expression of HYAL2. Hexapeptide-11 can also improve skin elasticity.

AZ32 is an orally bioavailable and blood-brain barrier-penetrating ATM inhibitor with an IC₅₀ of <6.2 nM for ATM enzyme, and an IC₅₀ of 0.31 μM for ATM in cell.

KU 59403 is a potent ATM inhibitor, with IC₅₀ values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively.

ATM Inhibitor-10 (compound 74), a 3-quinoline carboxamide, is a highly selective and orally active ATM inhibitor (IC₅₀: 0.6 nM). ATM Inhibitor-10 has anti-tumor activity in SW620 xenograft models. ATM Inhibitor-10 is synergistic with Top I inhibitors.

Elimusertib-d3 (BAY 1895344-d3) is the deuterium labeled Elimusertib (BAY 1895344). Elimusertib is a potent, orally active and selective ATR inhibitor and has anti-tumor activity.

ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC₅₀s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13).

(S)-WSD0628 (Compound 28) is the S-isomer of WSD0628 (HY-162002). (S)-WSD0628 is the inhibitor for ATM that inhibits the phosphorylation of ATM in MCF-7 cell with IC₅₀ <100 nM. (S)-WSD0628 exhibits radiosensitizing activity. (S)-WSD0628 can cross blood-brain barrier.

YY2201 is a highly potent and selective ATR inhibitor with an IC₅₀ of 8 nM. YY2201 shows >200-fold more selective for ATR than mTOR. YY2201 inhibits tumor progression in broad-spectrum cancer types (such as lung cancer).

ATR-IN-9 is a potent inhibitor of Ataxia-telangiectasia and RAD-3-related protein kinase (ATR) extracted from patent WO2020087170A1, compound 59, has an IC₅₀ of 10 nM.

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibitor, with an IC₅₀ of 0.7 nM, shows weak activity against mTOR (IC₅₀, 21 μM), DNAPK (IC₅₀, 2.8 μM), PI3Kα (IC₅₀, 3.8 μM), PI3Kβ (IC₅₀, 10.3 μM), PI3Kγ (IC₅₀, 3 μM) and PI3Kδ (IC₅₀, 0.73 μM). ATM Inhibitor-1 exhibits anti-tumor activity.