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
E1136	SKLB-197	<1 mg/mL	85 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
S9864	Elimusertib (BAY-1895344)	<1 mg/mL	17 mg/mL	''3 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
S4157	Chloroquine diphosphate	100 mg/mL	<1 mg/mL	<1 mg/mL
S3224	Cinobufagin	-1 mg/mL	100 mg/mL	-1 mg/mL
S6885	Ailanthone	-1 mg/mL	100 mg/mL	-1 mg/mL

亜型選択性的な製品

ATM/ATR製品

All (27) ATM/ATR阻害剤(24) ATM/ATR活性剤(3)

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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cancer Res, 2022, canres.2609.2021 Theranostics, 2022, 12(9):4348-4373	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.	Nat Commun, 2022, 13(1):360 Nucleic Acids Res, 2022, gkac375 Cancer Res, 2022, canres.2229.2021	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.	EMBO Rep, 2022, 23(2):e53658 Cell Rep, 2022, 38(2):110216 Cell Biosci, 2022, 12(1):43
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.	EMBO J, 2022, 10.15252/embj.2021108599 FASEB J, 2022, 36(3):e22221 Sci Signal, 2022, 15(715):eabh2290	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.	Nat Commun, 2022, 13(1):2111 Cancer Res, 2022, canres.2292.2021 Cell Rep, 2022, 38(7):110373	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.
E1136^新	SKLB-197 SKLB-197 exerts selectively inhibition against ataxia telangiectasia mutated and Rad3-related (ATR) kinase with IC50 of 0.013 μM, also displays potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
E1057^新	M4076 M4076 is an ATP-competitive inhibitor of the Ataxia telangiectasia mutated (ATM) kinase with IC50 of 0.2 nM, which targets tumor cell survival and growth by inhibiting double-strand break (DSB) repair as well as checkpoint control.
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.	Adv Sci (Weinh), 2022, 10.1002/advs.202104055 Cancer Res, 2022, canres.1397.2021 Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021	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.	Am J Cancer Res, 2022, 12(4):1577-1592 Cancer Cell, 2021, S1535-6108(21)00383-4 Mol Cell, 2021, S1097-2765(21)00420-2	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.	Exp Cell Res, 2022, S0014-4827(22)00218-X Aging (Albany NY), 2021, 13(8):11705-11726 mBio, 2020, 11(1)	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.	J Med Chem, 2022, 65(5):4182-4200 Sci Rep, 2022, 12(1):5827 Nat Commun, 2021, 12(1):4856	(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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Dev Cell, 2022, 57(5):638-653.e5 Cancer Res, 2022, canres.1707.2021	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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Sci Transl Med, 2022, 14(638):eabc7480 Nucleic Acids Res, 2022, 50(5):2700-2718
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.	Ann Transl Med, 2021, 9(19):1500 Drug Dev Res, 2021, 10.1002/ddr.21905 Pharmacol Res, 2021, 166:105459
S9864	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.	J Med Chem, 2022, 65(5):4182-4200 Sci Rep, 2022, 12(1):5827 Nat Commun, 2021, 12(1):6813
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.	NAR Cancer, 2022, 4(2):zcac012 Mol Cell, 2021, S1097-2765(21)00390-7 Mol Cancer Ther, 2021, 20(9):1561-1571	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 Res, 2021, 81(18):4676-4684 Cancer Discov, 2021, 11(2):362-383
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.	Sci Transl Med, 2022, 14(638):eabc7480 Cell Rep, 2022, 38(2):110216 Int J Mol Sci, 2022, 23(7)3834
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.
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).	Bioact Mater, 2022, 18:459-470 Phytomedicine, 2022, 98:153958 Bone, 2022, 154:116262	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.
S3224	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.
S6885	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.

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.	Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7 Cancer Res, 2022, canres.2609.2021 Theranostics, 2022, 12(9):4348-4373	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.	Nat Commun, 2022, 13(1):360 Nucleic Acids Res, 2022, gkac375 Cancer Res, 2022, canres.2229.2021	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.	EMBO Rep, 2022, 23(2):e53658 Cell Rep, 2022, 38(2):110216 Cell Biosci, 2022, 12(1):43
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.	EMBO J, 2022, 10.15252/embj.2021108599 FASEB J, 2022, 36(3):e22221 Sci Signal, 2022, 15(715):eabh2290	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.	Nat Commun, 2022, 13(1):2111 Cancer Res, 2022, canres.2292.2021 Cell Rep, 2022, 38(7):110373	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.
E1136^新	SKLB-197 SKLB-197 exerts selectively inhibition against ataxia telangiectasia mutated and Rad3-related (ATR) kinase with IC50 of 0.013 μM, also displays potent antitumor activity against ATM-deficent tumors both in vitro and in vivo.
E1057^新	M4076 M4076 is an ATP-competitive inhibitor of the Ataxia telangiectasia mutated (ATM) kinase with IC50 of 0.2 nM, which targets tumor cell survival and growth by inhibiting double-strand break (DSB) repair as well as checkpoint control.
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.	Adv Sci (Weinh), 2022, 10.1002/advs.202104055 Cancer Res, 2022, canres.1397.2021 Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021	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.	Am J Cancer Res, 2022, 12(4):1577-1592 Cancer Cell, 2021, S1535-6108(21)00383-4 Mol Cell, 2021, S1097-2765(21)00420-2	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.	Exp Cell Res, 2022, S0014-4827(22)00218-X Aging (Albany NY), 2021, 13(8):11705-11726 mBio, 2020, 11(1)	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.	J Med Chem, 2022, 65(5):4182-4200 Sci Rep, 2022, 12(1):5827 Nat Commun, 2021, 12(1):4856	(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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Dev Cell, 2022, 57(5):638-653.e5 Cancer Res, 2022, canres.1707.2021	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.	Cancer Cell, 2022, S1535-6108(21)00662-0 Sci Transl Med, 2022, 14(638):eabc7480 Nucleic Acids Res, 2022, 50(5):2700-2718
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.	Ann Transl Med, 2021, 9(19):1500 Drug Dev Res, 2021, 10.1002/ddr.21905 Pharmacol Res, 2021, 166:105459
S9864	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.	J Med Chem, 2022, 65(5):4182-4200 Sci Rep, 2022, 12(1):5827 Nat Commun, 2021, 12(1):6813
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.	NAR Cancer, 2022, 4(2):zcac012 Mol Cell, 2021, S1097-2765(21)00390-7 Mol Cancer Ther, 2021, 20(9):1561-1571	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 Res, 2021, 81(18):4676-4684 Cancer Discov, 2021, 11(2):362-383
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.	Sci Transl Med, 2022, 14(638):eabc7480 Cell Rep, 2022, 38(2):110216 Int J Mol Sci, 2022, 23(7)3834
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
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).	Bioact Mater, 2022, 18:459-470 Phytomedicine, 2022, 98:153958 Bone, 2022, 154:116262	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.
S3224	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.
S6885	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.

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

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).

Bioact Mater, 2022, 18:459-470

Phytomedicine, 2022, 98:153958

Bone, 2022, 154:116262

S3224

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.

S6885

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.