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DNA Damage/DNA Repair Filter
DNA Damage/DNA RepairATM/ATR
ATM serine/threonine kinase, symbol ATM, is a serine/threonine protein kinase that is recruited and activated by DNA double-strand breaks. It phosphorylates several key proteins that initiate activation of the DNA damage checkpoint, leading to cell cycle arrest, DNA repair or apoptosis. Several of these targets, including p53, CHK2, BRCA1, NBS1 and H2AX are tumor suppressors. ATR is a serine/threonine kinase and belongs to the phosphoinositide 3- kinase related protein kinases (PIKKs), particularly to ATM (ataxia telangiectasia mutated) subfamily. It functions to maintain genome integrity by stabilizing replication forks and by regulating cell cycle progression and DNA repair.
Elimusertib
T73181876467-74-1
Elimusertib (BAY-1895344) is a potent, highly selective, and orally available ATR inhibitor with an IC50 of 7 nM, demonstrating significant anti-tumor efficacy as a monotherapy and strong combination potential with targeted alpha therapy Radium-223 dichloride.
- $31
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Ceralasertib
Cited
T33381352226-88-0
Ceralasertib (AZD6738) is an orally active, selective ATR kinase inhibitor with an IC50 of 1 nM.
- $43
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CitedBerzosertib
T26691232416-25-9
Berzosertib (VE-822) is an ATR inhibitor (Ki<0.2 nM) that also inhibits ATM (Ki=34 nM). Berzosertib has antitumor activity and has been used in trials investigating the treatment of ovarian tumors, plasmacytoid tumors of the ovary, solid tumors in adults, advanced solid tumors, and advanced solid tumors.
- $30
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Gartisertib
T104071613191-99-3In house
Gartisertib (VX-803) is an orally active and selective Rad3-related protein (ATR) inhibitor with antitumor activity, inhibiting the antiproliferative effect induced in ccRCC cells, and inhibiting ATR-driven phosphorylation of checkpoint kinase 1 (Chk1), useful for studying solid tumors.
- $136
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Wortmannin Cited
T628319545-26-7
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.
- $40
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CitedKU-60019
T63872925701-46-8
KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).
- $32
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Elimusertib hydrochloride(1876467-74-1 free base)
T10468
Elimusertib hydrochloride(1876467-74-1 free base) (BAY-1895344 hydrochloride) is a effective, orally available and selective ATR inhibitor with anti-tumor activity.
- $31
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Camonsertib
T620832417489-10-0
Camonsertib (RP-3500) is a novel, potent and selective ATR kinase inhibitor (ATRi) that exhibits potent antitumor effects with an IC50: 1.00 nM in biochemical assays.RP-3500 is 30-fold more selective for ATR than mTOR (IC50: 120 nM) and more than 2,000-fold more potent than ATM, DNA-PK and PI3Kα kinases. RP-3500 is 30 times more selective for ATR than mTOR (IC50: 120 nM), and 2,000 times more selective than ATM, DNA-PK and PI3Kα kinases.
- $172
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azd1390
T51752089288-03-7
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.
- $80
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Tuvusertib
T104061613200-51-3
Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.
- $68
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KU60019 Cited
T2474925701-49-1In house
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.
- $48
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CitedTorin 2 Cited
T61001223001-51-1
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.
- $35
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CitedKU-55933 Cited
T2685587871-26-9
KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.
- $43
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CitedAZD0156 Cited
T67701821428-35-6
AZD0156 , an effective and specific inhibitors of ATM kinase, is potential antineoplastic activities and chemo- radio-sensitizing.
- $31
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CitedSchisandrin B
T292561281-37-6
Schisandrin B (Schisandrin B (Sch B)) has an antioxidant effect on rodent liver and heart.
- $35
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Garcinone C
TN167376996-27-5
Garcinone C is a xanthone derivative extracted from Garcinia oblongifolia Champ with anti-inflammatory, astringency, and granulation-promoting activities. Garcinone C is an AChE inhibitor and has potential cytotoxic effects on certain cancers.
- $38
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Dactolisib Cited
T2235915019-65-7
Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR, with IC50 values of 4 nM for p110α, 5 nM for p110γ, 7 nM for p110δ, 75 nM for p110β, and 20.7 nM for mTOR.
- $39
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CitedNU 7026
T2433154447-35-5
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.
- $33
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VE-821 Cited
T30321232410-49-9
VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki IC50: 13 26 nM in cell-free assays).
- $30
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CitedLartesertib
T626842495096-26-7
Lartesertib (ATM Inhibitor-5) is an inhibitor of serine threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.
- $132
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Ro 90-7501
T16773293762-45-5In house
Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitizer for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest. Ro 90-7501 also exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.
- $30
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AD1058
T2001052907782-78-7
AD1058 is a potent and selective ATR inhibitor (IC50 = 1.6 nM) that crosses the blood-brain barrier with significant in vivo anticancer activity. It is commonly used in the study of brain metastasis and CNS metastasis by inhibiting cell proliferation, disrupting the cell cycle and inducing apoptosis.
- $188
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NU6027
T6612220036-08-8
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.
- $37
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KU 59403
T15673845932-30-1
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.
- $882
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AZ31
T196712088113-98-6In house
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.
- $38
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AZ20
T19581233339-22-4
AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
- $33
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CP-466722
T62611080622-86-1
CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.
- $30
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ART0380
T857312267316-76-5
ART0380 is a potent, selective, orally available, ATP-competitive ATR kinase inhibitor (IC50=51.7 nM) with antitumor activity for the study of ataxia telangiectasia mutated (ATM) cancer.
- $1,520
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GJ103 sodium salt
T42511459687-96-7
GJ103 sodium salt is an active analog of GJ072, a read-through compound. It has been shown to reduce the surface tension of aqueous solutions, which makes it easier for molecules to move through the solution. It has also been shown to reduce the viscosity of aqueous solutions, which makes it easier for molecules to move through the solution. Additionally, it has been shown to reduce the pH of aqueous solutions, which can have a variety of effects on the biochemical and physiological processes of living organisms.
- $42
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M3541
T708731360628-91-6
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.
- $518
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(Z)-Mirin
T31341198097-97-0
(Z)-Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity.
- $50
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CGK733
T1821905973-89-9
CGK733 (CGK 733) is a potent and selective inhibitor of ATM ATR.
- $30
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ETP-46464 Cited
T20841345675-02-6
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
- $34
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CitedMirin Cited
T60273299953-00-7
Mirin is a Mre11-Rad50-Nbs1 (MRN) complex inhibitor that inhibits MRN-dependent ATM activation without affecting ATM protein kinase activity. It also inhibits Mre11-associated exonuclease activity, thereby disrupting DNA double-strand break repair.Mirin induces cell cycle arrest in G1 phase.
- $30
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CitedAZ32 Cited
T44432288709-96-4
AZ32 is an orally bioavailable, blood-brain barrier-penetrating ATM inhibitor with an IC50 of <6.2 nM for the ATM enzyme and an IC50 of 0.31 μM for ATM in cells.
- $51
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CitedPIK-93
T2616593960-11-3
PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.
- $37
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ATR-IN-22
T790332905312-07-2
ATR-IN-22 (Compound 34), an orally active ATR inhibitor, exhibits potent anti-proliferative effects on MIAPaCa-2 cells with an IC50 value of less than 1 μM and demonstrates anti-tumor activity in colon cancer [1].
- Inquiry Price
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ATR-IN-21
T790312905312-17-4
ATR-IN-21, also known as compound 60, is a potent inhibitor of ATR, exhibiting an IC50 of less than 1000 nM [1].
- Inquiry Price
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ATR kinase-IN-2
T2016341613196-91-0
ATRkinase-IN-2 (Compound I-G-27) is an inhibitor of the ATR protein kinase, with a Ki value ranging from 0.01 to 1 μΜ. It is utilized in tumor research.
- Inquiry Price
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ATM Inhibitor-8
T79305
ATM Inhibitor-8 (Compound 10r) is a potent, selective, and orally active ATM inhibitor with anti-tumor activity, characterized by an IC50 value of 1.15 nM [1].
- Inquiry Price
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ATR kinase-IN-3
T2018051613196-92-1
ATRkinase-IN-3 (Compound I-G-28) is an inhibitor of the ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM, and is utilized in cancer research.
- Inquiry Price
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ATR-IN-24
T790582370889-43-1
ATR-IN-24 (Compound 1) is an ATR inhibitor exhibiting anticancer activity [1].
- $1,520
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A011
T78711
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].
- TBD
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CA-M11
T200892
CA-M11 (compound CA-M11) is capable of entering the liver's bile salt transport system to release Mirin.
- Inquiry Price
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ATR-IN-29
T791212761193-67-1
ATR-IN-29, a potent, orally active inhibitor of ATR kinase, exhibits an IC50 of 1 nM and demonstrates antiproliferative activity [1].
- Inquiry Price
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ATM Inhibitor-9
T79306
ATM Inhibitor-9 (Compd 7a) is a potent ATM kinase inhibitor with an IC50 of 5 nM, used in cancer research [1].
- Inquiry Price
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ATM Inhibitor-11
T2014572878473-51-7
ATMInhibitor-11 (Compound 1) is an inhibitor of ATM with an IC50 of 0.32 nM. It also inhibits KAP1 phosphorylation with an IC50 of 0.97 nM. This compound exhibits high exposure in the brain, heart, and plasma of ICR mice. Furthermore, ATMInhibitor-11 demonstrates antitumor activity in the NCI-H441 xenograft mouse model.
- Inquiry Price
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ATM Inhibitor-1
T103962135639-94-8
ATM Inhibitor-1 is a highly potent, selective, and orally active ATM inhibitor (IC50: 0.7 nM) with anti-tumor activity. It exhibits 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).
- $3,120
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