ATM/ATR

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1009	Dactolisib (BEZ235)	<1 mg/mL	0.01 mg/mL	'<1 mg/mL
S1092	KU-55933 (ATM Kinase Inhibitor)	<1 mg/mL	33 mg/mL	<1 mg/mL
S1570	KU-60019	<1 mg/mL	18 mg/mL	<1 mg/mL
S8007	VE-821	<1 mg/mL	74 mg/mL	<1 mg/mL
S2758	Wortmannin (KY 12420)	<1 mg/mL	85 mg/mL	'''<1 mg/mL
S9864	Elimusertib (BAY-1895344)	<1 mg/mL	17 mg/mL	''3 mg/mL
S6885	Ailanthone	-1 mg/mL	100 mg/mL	-1 mg/mL
S2817	Torin 2	<1 mg/mL	20 mg/mL	<1 mg/mL
S2245	CP-466722	<1 mg/mL	0.28 mg/mL	<1 mg/mL
S7102	Berzosertib (VE-822)	<1 mg/mL	36 mg/mL	''''''<1 mg/mL
S8050	ETP-46464	<1 mg/mL	6 mg/mL	<1 mg/mL
S7136	CGK 733	<1 mg/mL	100 mg/mL	<1 mg/mL
S7050	AZ20	<1 mg/mL	83 mg/mL	3 mg/mL
S8556	AZ31	<1 mg/mL	53 mg/mL	<1 mg/mL
S7693	Ceralasertib (AZD6738)	<1 mg/mL	82 mg/mL	'41 mg/mL
S8729	AZ32	<1 mg/mL	66 mg/mL	7 mg/mL
S8680	AZD1390	<1 mg/mL	14 mg/mL	95 mg/mL
S3600	Schisandrin B (Sch B)	<1 mg/mL	80 mg/mL	10 mg/mL
S8096	Mirin	<1 mg/mL	44 mg/mL	<1 mg/mL
S8666	Elimusertib (BAY-1895344) hydrochloride	82 mg/mL	82 mg/mL	''''82 mg/mL
S0148	HAMNO	<1 mg/mL	53 mg/mL	<1 mg/mL
S8375	AZD0156	<1 mg/mL	0.3 mg/mL	2 mg/mL
S9639	VX-803 (M4344)	<1 mg/mL	15 mg/mL	'<1 mg/mL
S3224	Cinobufagin	-1 mg/mL	100 mg/mL	-1 mg/mL
S4157	Chloroquine diphosphate	100 mg/mL	<1 mg/mL	<1 mg/mL

亜型選択性的な製品

ATM/ATR製品

All (25) ATM/ATR阻害剤(23) ATM/ATR活性剤(2)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1009	Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Cell Rep, 2021, 34(11):108870 Cell Rep, 2021, 35(1):108940 Cell Rep, 2021, 35(8):109181	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1092	KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/K_i of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.	Cancer Cell, 2021, S1535-6108(20)30658-9 Mol Cell, 2021, S1097-2765(21)00315-4 Mol Cell, 2021, S1097-2765(20)30951-5	Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated.
S1570	KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.	Nat Commun, 2021, 12(1):2529 Nat Commun, 2021, 12(1):476 Theranostics, 2021, 11(4):1795-1813
S8007	VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with K_i/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.	Mol Cell, 2021, S1097-2765(21)00458-5 Mol Cell, 2021, S1097-2765(20)30951-5 Nat Commun, 2021, 12(1):3827	Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.
S2758	Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.	J Extracell Vesicles, 2021, 10(8):e12091 Proc Natl Acad Sci U S A, 2021, 118(19)e2017645118 Biomaterials, 2021, 271:120720	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S9864^新	Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
S6885^新	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S2817	Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.	Nat Commun, 2021, 12(1):245 Cell Rep, 2021, 35(1):108940 Cancer Commun (Lond), 2021, 10.1002/cac2.12189	U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/P_i before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
S2245	CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.	G3 (Bethesda), 2020, 4;10(5):1585-1597 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193
S7102	Berzosertib (VE-822) Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.	Mol Cell, 2021, S1097-2765(21)00420-2 Sci Adv, 2021, 7(25)eabd9208 Nat Commun, 2021, 12(1):3520	Western blot analysis of scr or siPNUTS transfected cells without IR or 6 h after 10 Gy. VE-822 was added for 2, 5, 15, 30 or 60 min to indicated samples 6 h after 10 Gy.
S8050	ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.	Nat Commun, 2019, 10(1):5718 Nat Commun, 2019, 10(1):3585 Oncogenesis, 2019, 8(7):38
S7136	CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.	Aging (Albany NY), 2021, 13(8):11705-11726 mBio, 2020, 11(1) Mol Cells, 2016, 39(12):869-876	K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
S7050	AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.	NAR Cancer, 2021, 3(1):zcab010 Nature, 2020, 586(7828):292-298 Nature, 2020, 10.1038/s41586-020-2959-4	(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
S8556	AZ31 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).	Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S7693	Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.	Mol Cell, 2021, S1097-2765(21)00315-4 Proc Natl Acad Sci U S A, 2021, 118(17)e2024258118 Theranostics, 2021, 11(4):1795-1813	Number of γH2AX foci per cell of irradiated (2 Gy) SAS cells treated with inhibitors against ATM (ATMi, KU55933), DNA-PK (DNA-PKi, KU57788), or ATR (ATRi, AZD6738) with or without LY364947.
S8729	AZ32 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.
S8680	AZD1390 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.	Mol Cell, 2021, 81(7):1515-1533.e5 Cells, 2021, 10(3)532 Senologie, 2021, 18(02): e28-e29
S3600	Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.	Pharmacol Res, 2021, 166:105459 Neurol Res, 2020, 42(8):693-702 J Med Virol, 2019, 91(8):1440-1447
S8096	Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.	Mol Cell, 2021, S1097-2765(21)00390-7 FEBS Open Bio, 2021, 10.1002/2211-5463.13198 Cell Death Differ, 2021, 10.1038/s41418-020-00733-4	Wildtype bone marrow-derived macrophages (BMDMs) were incubated with and without the MRN complex inhibitor mirin (administered dose of 100 μM) for 2 hours, then were treated with PM (100 μg/mL) for an additional 24 hours. (A) The relative levels of Cxcl1, Cxcl2 and Ifn-γ mRNA transcripts were determined using quantitative PCR. (B) The protein levels of Cxcl1, Cxcl2 and Ifn-γ in the culture supernatants were measured using ELISA. Data are presented as means ± SEMs across at least 3 independent experiments. p < 0.05; *p < 0.01.
S8666	Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.	Clin Cancer Res, 2021, clincanres.1010.2021 Cancer Discov, 2021, 11(2):362-383 Nucleic Acids Res, 2019, 10.1093/nar/gkz518
S0148	HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
S8375	AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.	Cells, 2021, 10(3)532 Genes (Basel), 2021, 12(6)925 Cell Rep, 2020, 32(8):108068
S9639	VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S4157	Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Gut, 2021, 70(5):890-899 Dev Cell, 2021, S1534-5807(21)00518-9 Theranostics, 2021, 11(2):700-714	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1009	Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.	Cell Rep, 2021, 34(11):108870 Cell Rep, 2021, 35(1):108940 Cell Rep, 2021, 35(8):109181	Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S1092	KU-55933 (ATM Kinase Inhibitor) KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor with IC50/K_i of 12.9 nM/2.2 nM in cell-free assays, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR. KU‑55933 (ATM Kinase Inhibitor) inhibits the activation of autophagy‑initiating kinase ULK1 and results in a significant decrease of autophagy.	Cancer Cell, 2021, S1535-6108(20)30658-9 Mol Cell, 2021, S1097-2765(21)00315-4 Mol Cell, 2021, S1097-2765(20)30951-5	Effects of NVP-BKM120 and KU-55933 and their combination on the DNA damage response. A, HCC1937 cells were treated for 18 hours with NVP-BKM120 at 2.5 μmol/L, KU-55933 at 10 μmol/L, or their combination, subjected to ionizing radiation(IR) with 10 Gy or mock, lysed 6 hours later, and subjected to immunoblotting with antibodies as indicated.
S1570	KU-60019 KU-60019 is an improved analogue of KU-55933, with IC50 of 6.3 nM for ATM in cell-free assays, 270- and 1600-fold more selective for ATM than DNA-PK and ATR,and is a highly effective radiosensitizer.	Nat Commun, 2021, 12(1):2529 Nat Commun, 2021, 12(1):476 Theranostics, 2021, 11(4):1795-1813
S8007	VE-821 VE-821 is a potent and selective ATP competitive inhibitor of ATR with K_i/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.	Mol Cell, 2021, S1097-2765(21)00458-5 Mol Cell, 2021, S1097-2765(20)30951-5 Nat Commun, 2021, 12(1):3827	Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.
S2758	Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.	J Extracell Vesicles, 2021, 10(8):e12091 Proc Natl Acad Sci U S A, 2021, 118(19)e2017645118 Biomaterials, 2021, 271:120720	L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
S9864^新	Elimusertib (BAY-1895344) Elimusertib (BAY-1895344) is a very potent and highly selective ATR (ataxia telangiectasia and Rad3-related) inhibitor with IC50 of 7 nM. Elimusertib potently inhibits proliferation of a broad spectrum of human tumor cell lines with median IC50 of 78 nM.
S6885^新	Ailanthone Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR_1-651) with IC50 of 69 nM and 309 nM, respectively.
S2817	Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.	Nat Commun, 2021, 12(1):245 Cell Rep, 2021, 35(1):108940 Cancer Commun (Lond), 2021, 10.1002/cac2.12189	U2OS cells were plated in six-well plates using complete medium. The next day the cells were washed four times with NaCl/P_i before maintaining them for 6 h in serum- and glucose-free DMEM supplemented as indicated in the absence or presence of 0.1 uM Torin 2 for the last 1 h. The cells were control- treated, treated with 1 ug/mL insulin or treated with 1 mM H2O2 for 15 min. Thereafter, cell lysates were prepared and western blotting was performed using the indicated antibodies.
S2245	CP-466722 CP-466722 is a potent and reversible ATM inhibitor, does not affect ATR and inhibits PI3K or PIKK family members in cells.	G3 (Bethesda), 2020, 4;10(5):1585-1597 Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193
S7102	Berzosertib (VE-822) Berzosertib (VE-822, VX970, M6620) is an ATR inhibitor with IC50 of 19 nM in HT29 cells.	Mol Cell, 2021, S1097-2765(21)00420-2 Sci Adv, 2021, 7(25)eabd9208 Nat Commun, 2021, 12(1):3520	Western blot analysis of scr or siPNUTS transfected cells without IR or 6 h after 10 Gy. VE-822 was added for 2, 5, 15, 30 or 60 min to indicated samples 6 h after 10 Gy.
S8050	ETP-46464 ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.	Nat Commun, 2019, 10(1):5718 Nat Commun, 2019, 10(1):3585 Oncogenesis, 2019, 8(7):38
S7136	CGK 733 CGK 733 is a potent and selective inhibitor of ATM/ATR with IC50 of ~200 nM.	Aging (Albany NY), 2021, 13(8):11705-11726 mBio, 2020, 11(1) Mol Cells, 2016, 39(12):869-876	K562 and K562R cells were pre-treated for 1 h with CGK733 (5 μM), then treated with CTD (10 μM) for 24 h, and protein levels of cleaved PARP, Mcl-1, and phosphorylated H3 were determined by Western blotting. GAPDH served as a normal control.
S7050	AZ20 AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR.	NAR Cancer, 2021, 3(1):zcab010 Nature, 2020, 586(7828):292-298 Nature, 2020, 10.1038/s41586-020-2959-4	(B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.
S8556	AZ31 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).	Proc Natl Acad Sci U S A, 2020, 117(50):31891-31901
S7693	Ceralasertib (AZD6738) Ceralasertib (AZD6738) is an orally active, and selective ATR kinase inhibitor with IC50 of 1 nM. Phase 1/2.	Mol Cell, 2021, S1097-2765(21)00315-4 Proc Natl Acad Sci U S A, 2021, 118(17)e2024258118 Theranostics, 2021, 11(4):1795-1813	Number of γH2AX foci per cell of irradiated (2 Gy) SAS cells treated with inhibitors against ATM (ATMi, KU55933), DNA-PK (DNA-PKi, KU57788), or ATR (ATRi, AZD6738) with or without LY364947.
S8729	AZ32 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.
S8680	AZD1390 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.	Mol Cell, 2021, 81(7):1515-1533.e5 Cells, 2021, 10(3)532 Senologie, 2021, 18(02): e28-e29
S3600	Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.	Pharmacol Res, 2021, 166:105459 Neurol Res, 2020, 42(8):693-702 J Med Virol, 2019, 91(8):1440-1447
S8096	Mirin Mirin is a potent Mre11–Rad50–Nbs1 (MRN) complex inhibitor, and inhibits Mre11-associated exonuclease activity. Mirin inhibits MRN-dependent activation of ATM.	Mol Cell, 2021, S1097-2765(21)00390-7 FEBS Open Bio, 2021, 10.1002/2211-5463.13198 Cell Death Differ, 2021, 10.1038/s41418-020-00733-4	Wildtype bone marrow-derived macrophages (BMDMs) were incubated with and without the MRN complex inhibitor mirin (administered dose of 100 μM) for 2 hours, then were treated with PM (100 μg/mL) for an additional 24 hours. (A) The relative levels of Cxcl1, Cxcl2 and Ifn-γ mRNA transcripts were determined using quantitative PCR. (B) The protein levels of Cxcl1, Cxcl2 and Ifn-γ in the culture supernatants were measured using ELISA. Data are presented as means ± SEMs across at least 3 independent experiments. p < 0.05; *p < 0.01.
S8666	Elimusertib (BAY-1895344) hydrochloride Elimusertib (BAY-1895344) hydrochloride is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.	Clin Cancer Res, 2021, clincanres.1010.2021 Cancer Discov, 2021, 11(2):362-383 Nucleic Acids Res, 2019, 10.1093/nar/gkz518
S0148	HAMNO HAMNO (NSC-111847) is a potent and selective replication protein A (RPA) inhibitor with anti-tumor activity. HAMNO inhibits both ATR autophosphorylation and phosphorylation of RPA32 Ser33 by ATR.
S8375	AZD0156 AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities. AZD0156 prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells.	Cells, 2021, 10(3)532 Genes (Basel), 2021, 12(6)925 Cell Rep, 2020, 32(8):108068
S9639	VX-803 (M4344) VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S3224^新	Cinobufagin Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S4157	Chloroquine diphosphate Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).	Gut, 2021, 70(5):890-899 Dev Cell, 2021, S1534-5807(21)00518-9 Theranostics, 2021, 11(2):700-714	NCI-H929 EV and miR-137 OE cells were treated with ATM activator Chloroquine Phosphate (CQ), specific ATM inhibitor KU-55933, and ATR inhibitor AZ20 for 12 hr. Immunoblotting showed the expression of p-ATM, p-Chk2, p-BRCA1, p-ATR and p-Chk1.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S3224^新

Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

S4157

Chloroquine diphosphate

Chloroquine diphosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator. Chloroquine is also an inhibitor of toll-like receptors (TLRs).

Gut, 2021, 70(5):890-899

Dev Cell, 2021, S1534-5807(21)00518-9

Theranostics, 2021, 11(2):700-714