atm

ATM-3507 is a protomyosin inhibitor with anticancer activity that inhibits human melanoma and can be used to study ovarian cancer.

ATM-3507 trihydrochloride is a potent tropomyosin inhibitor (IC50s: 3.83-6.84 μM in human melanoma cell lines).

ATM Inhibitor-8 (Compound 10r) is a potent, selective, and orally active inhibitor of ATM, exhibiting anti-tumor activity [1], characterized by an IC50 value of 1.15 nM.

ATM-IN-1 is a potent inhibitor of ATM. ATM-IN-1 has shown research potential in cancer and neurological diseases.

ATM Inhibitor -2 is a potent and selective inhibitor of ATM (IC50<1 nM).

ATM Inhibitor-9 (Compd 7a) is a potent inhibitor of ATM kinase, exhibiting an IC50 value of 5 nM, and is utilized in cancer research [1].

ATM Inhibitor -4 is a selective and potent ATM inhibitor (IC50: 0.32 nM) that strongly inhibits the activity of the PI3K kinase family and exhibits good metabolic stability. ATM Inhibitor -4 completely inhibits mTOR at 1 μM.

ATM Inhibitor-3 is a potent and selective inhibitor of ATM (IC50: 0.71 nM). ATM Inhibitor-3 inhibits the PI3K kinase family and exhibits good metabolic stability.

ATM-3507 trihydrochloride, a potent inhibitor of tropomyosin, demonstrates inhibition concentration (IC50) values ranging from 3.83 to 6.84 μM across various human melanoma cell lines.

ATM-1001 is an inhibitor of the cancer-associated tropomyosin 3.1 (Tpm3.1), suppressing glucose-stimulated insulin secretion (GSIS) from the pancreatic islets.

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibito (IC50: 0.7 nM) anti-tumor activity. It 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).

KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.

ATMP is a phosphonic acid with chelating properties. It is an antiscalant.

Lartesertib (ATM Inhibitor-5) is an inhibitor of serine/threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.

Camonsertib (RP-3500) is a selective, orally active ATR kinase inhibitor (ATRi) with an IC50: 1.00 nM in biochemical assays and exhibits potent antitumour effects. Camonsertib is 30 times more selective for ATR than mTOR (IC50: 120 nM) and is a more active inhibitor of ATM, DNA-PK and PI3Kα kinases. PK and PI3Kα kinases.

Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitiser for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest.Ro 90-7501 exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.

AZ31 is an ATM inhibitor with potency, high selectivity, and oral activity.AZ31 inhibits ATM enzymes, intracellular ATM, with IC50 values of <1.2 nM and 46 nM, respectively.AZ31 exhibits excellent ATR selectivity, PIKK family selectivity, and pan-kinase selectivity.AZ31 is a potent in vitro radiosensitizer that can be used for cancer research.

Ku-60019 is a potent, reversible inhibitor of ATM kinase (IC50: 6.3 nM). It is much less effective or without effect against a panel of 229 other kinases.

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.

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.

VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki/IC50: 13/26 nM in cell-free assays).

AZD0156 , an effective and specific inhibitors of ATM kinase, is potential antineoplastic activities and chemo-/radio-sensitizing.

Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC 50 =12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Consistent with its ability to target the MRN complex, Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells [1].

Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM.

Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM/ATR/DNA-PK inhibition is 28 nM/35 nM/118 nM, respectively.

NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

Potent and selective ATM kinase inhibitor (IC50 = 0.6 nM in an enzyme inhibition assay). Exhibits > 600-fold selectivity for ATM over other kinases. Inhibits ATM kinase in an in vitro cellular assay (IC50 = 0.33 μM). Potentiates the antitumor effects of the topoisomerase 1 inhibitor irinotecan in tumor bearing, immunocompromised mice. Orally bioavailable. Degorce et al (2016) Discovery of novel 3-quinoline carboxamides as potent, selective and orally bioavailable inhibitors of ataxia telangiectasia mutated (ATM) kinase. J.Med.Chem. 59 6281 PMID:27259031

ATR-IN-20, a potent ATM/ATR inhibitor, showcases an IC50 value of 3 nM. It also exhibits inhibitory activity against mTOR with an IC50 of 18 nM, while maintaining selectivity over PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). Additionally, ATR-IN-20 has an excellent pharmacokinetic profile with an oral bioavailability (F) of 30%, and demonstrates anticancer effects.

AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.

GT-2227 is a histamine H3 receptor antagonist.

Tyrphostin AG1433 (AG1433) is an inhibitor of tyrosine kinases and also a dual inhibitor of PDGFRβ(IC50s = 5.0 μM) and VEGFR-2 (Flk-1/KDR)(IC50s = 9.3 μM).

AIM-100 is a Ack1 inhibitor (IC50: 24 nM).

CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide , with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response[1][2]. Phosphoramide mustard cyclohexanamine causes cytotoxicity through forming cross-linked DNA adducts which inhibit DNA strand separation during replication[1].Phosphoramide mustard cyclohexanamine destroys rapidly dividing cells by forming NOR-G-OH, NOR-G and G-NOR-G adducts with DNA, potentially leading to DNA damage[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 48 hours) reduces cell viability in rat spontaneously immortalized granulosa cells (SIGCs)[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces DNA adduct formation[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) induces ovarian DNA damage in rat ovaries[1].Phosphoramide mustard cyclohexanamine increases DNA damage responses (DDR) gene (Atm, Parp1, Prkdc, Xrcc6, Brca1, Rad51) mRNA expression level[1].Phosphoramide mustard cyclohexanamine (3-6 μM; 24-48 hours) increased DDR proteins[1]. Cell Viability Assay[1] Cell Line: SIGCs Phosphoramide mustard cyclohexanamine (2.1-20.7 mg/kg; i.p.; daily; for 5 days) inhibits subcutaneous tumor growth in rats[2].Phosphoramide mustard cyclohexanamine (86.0 mg/kg; i.v.) has a plasma disappearance half-life of 15.1 minutes[2]. Animal Model: Rat, subcutaneously implanted Walker 256 carcinosarcoma tumor[2] [1]. Shanthi Ganesan, et al. Phosphoramide mustard exposure induces DNA adduct formation and the DNA damage repair response in rat ovarian granulosa cells. Toxicol Appl Pharmacol. 2015 Feb 1; 282(3): 252-258. [2]. S Genka, et al. Brain and plasma pharmacokinetics and anticancer activities of cyclophosphamide and phosphoramide mustard in the rat. Cancer Chemother Pharmacol. 1990;27(1):1-7.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

Antitumor agent-28 is a compound that specifically targets and inhibits the activity of the ataxia telangiectasia mutated (ATM) kinase. By doing so, it effectively impedes the progression of ATM-mediated diseases and demonstrates significant anti-cancer activity.

Elimusertib (BAY-1895344) is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.Elimusertib shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.

NU 7026 (DNA-PK Inhibitor II) is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition against both ATM and ATR.

KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).

M3541 is a selectively potent and orally active ATM inhibitor with potential antitumor activity.M-3541 inhibits ATM kinase activity and ATM-mediated signaling by binding to ATM.M3541 prevents activation of DNA damage checkpoints, inhibits DNA damage repair, contributes to apoptosis, and induces death of ATM overexpressing tumor cells.

Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd

SU-11752 is a potent and selective DNA-PK inhibitor. Inhibition kinetics and a direct assay for ATP binding showed that SU11752 inhibited DNA-PK by competing with ATP. SU11752 inhibited DNA double-strand break repair in cells and gave rise to a five-fold sensitization to ionizing radiation. At concentrations of SU11752 that inhibited DNA repair, cell cycle progression was still normal and ATM kinase activity was not inhibited.

SKLB-197 is able to act on ATR (IC50: 0.013 μM), but has little or no activity on the other 402 protein kinases. In vitro and in vivo, SKLB-197 has shown significant antitumour effects against ATM-deficient tumours.

AZD1390 is an exceptionally potent inhibitor of ATM in cells (IC50: 0.78 nM) with >10,000-fold selectivity over closely related members of the PIKK family of enzymes.

BRD4770 is a histone methyltransferase G9a inhibitor and induces cell senescence.

ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).

A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle arrest when combined with CPT-11, displaying notable antitumor activity [1].

Americanin A natural thrombin inhibitor, suppressing melanin synthesis, regulating the ATM/ATR signaling pathway and the Skp2-p27 axis in human colon cancer cells.

KU 59403 is a selective and potent ATM inhibitor with antitumor and anticancer activity, inhibits ATM, DNA-PK and PI3K, and is often used in combination therapy with PARP or ATR inhibitors to slow the progression of cancer.

CGK733 (CGK 733) is a potent and selective inhibitor of ATM/ATR.