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DNA Damage/DNA Repair
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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.
- CamonsertibT620832417489-10-0Camonsertib (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.
- $172
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- BerzosertibT26691232416-25-9Berzosertib (VE-822) has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others.
- $30
SizeQTY - GartisertibT104071613191-99-3In houseATR inhibitor 2 is an orally active, ATP-competitive, and selective ATR inhibitor (Ki <150 pM) with antitumor activity. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation (IC50: 8 nM).
- $1,200
SizeQTY
- Ro 90-7501T16773293762-45-5In houseRo 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.
- $30
SizeQTY - AZ31T196712088113-98-6In houseAZ31 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.
- $45
SizeQTY - KU60019T2474925701-49-1In houseKu-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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Cited - AZ32T44432288709-96-4AZ32 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.
- $51
SizeQTY Cited - WortmanninT628319545-26-7Wortmannin (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.
- $32
SizeQTY Cited - VE-821T30321232410-49-9VE-821 (ATR Inhibitor IV) is a selective ATP competitive inhibitor of ATR( Ki IC50: 13 26 nM in cell-free assays).
- $30
SizeQTY Cited - DactolisibT2235915019-65-7Dactolisib (BEZ235) is an orally bioavailable inhibitor of PI3K and mTOR (IC50s: 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR).
- $39
SizeQTY Cited - Torin 2T61001223001-51-1Torin 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
SizeQTY Cited - AZD0156T67701821428-35-6AZD0156 , an effective and specific inhibitors of ATM kinase, is potential antineoplastic activities and chemo-/radio-sensitizing.
- $31
SizeQTY Cited - KU-55933T2685587871-26-9KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
- $43
SizeQTY Cited - CeralasertibT33381352226-88-0Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM.
- $43
SizeQTY Cited - ATR-IN-21T790312905312-17-4ATR-IN-21, also known as compound 60, is a potent inhibitor of ATR, exhibiting an IC50 of less than 1000 nM [1].
- Inquiry Price
SizeQTY - ATR-IN-22T790332905312-07-2ATR-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
SizeQTY - NU6027T6612220036-08-8NU6027 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.
- $38
SizeQTY - AZ20T19581233339-22-4AZ20 is an effective and specific inhibitor of ATR kinase (IC50: 5 nM, in a cell-free assay), 8-fold selectivity over mTOR.
- $33
SizeQTY - ATM Inhibitor-8T79305ATM 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.
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SizeQTY - CP-466722T62611080622-86-1CP-466722, an effective and reversible ATM inhibitor, does not inhibit ATR and PI3K or PIKK family members in cells.
- $30
SizeQTY - A011T78711A011, 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].
- $143
SizeQTY - ATR-IN-24T790582370889-43-1ATR-IN-24 (Compound 1) is an ATR inhibitor with demonstrated anticancer activity [1].
- $1,520
SizeQTY - KU 59403T15673845932-30-1KU 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
SizeQTY - CGK733T1821905973-89-9CGK733 (CGK 733) is a potent and selective inhibitor of ATM/ATR.
- $30
SizeQTY - LartesertibT626842495096-26-7Lartesertib (ATM Inhibitor-5) is an inhibitor of serine/threonine protein kinase ATM with potential anticancer activity for the study of lung cancer.
- $132
SizeQTY - GJ103 sodium saltT42511459687-96-7GJ103 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
SizeQTY - Garcinone CTN167376996-27-5Garcinone 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
SizeQTY - ATR-IN-29T791212761193-67-1ATR-IN-29, a potent, orally active inhibitor of ATR kinase, exhibits an IC50 of 1 nM and demonstrates antiproliferative activity [1].
- Inquiry Price
SizeQTY - ATM Inhibitor-9T79306ATM 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].
- Inquiry Price
SizeQTY - TuvusertibT104061613200-51-3Tuvusertib (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
SizeQTY - PIK-93T2616593960-11-3PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
- $37
SizeQTY - (Z)-MirinT31341198097-97-0(Z)-Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity.
- $50
SizeQTY - KU-60019T63872925701-46-8KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).
- $32
SizeQTY - M3541T708731360628-91-6M3541 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
SizeQTY - NU 7026T2433154447-35-5NU 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
SizeQTY - ElimusertibT73181876467-74-1Elimusertib (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.
- $31
SizeQTY - ATR-IN-23T789592923800-62-6ATR-IN-23 (Compound 34), a potent and selective ATR inhibitor, exhibits an IC50 of 1.5 nM, has demonstrated antiproliferative effects on LoVo cells, and induces synthetic lethality in HT-29 cells, suggesting its utility in researching DNA damage response (DDR)-deficient cancers [1].
- $1,520
SizeQTY - ATM Inhibitor-1T103962135639-94-8ATM 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).
- $2,420
SizeQTY - ETP-46464T20841345675-02-6ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
- $34
SizeQTY - azd1390T51752089288-03-7AZD1390 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
SizeQTY - Schisandrin BT292561281-37-6Schisandrin B (Schisandrin B (Sch B)) has an antioxidant effect on rodent liver and heart.
- $35
SizeQTY - Elimusertib hydrochloride(1876467-74-1 free base)T10468Elimusertib hydrochloride(1876467-74-1 free base) (BAY-1895344 hydrochloride) is a effective, orally available and selective ATR inhibitor with anti-tumor activity.
- $51
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