Azd5438

Manufactured by Selleck Chemicals

AZD5438 is a laboratory reagent used for research purposes. It is a chemical compound with a specific molecular structure and properties. The core function of AZD5438 is to serve as a research tool for scientific investigations, without further interpretation or extrapolation on its intended use.

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Lab products found in correlation

10 protocols using azd5438

Comprehensive Antibody Characterization Protocol

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Antibody for total RB was purchased from BD Biosciences (San Jose, CA, clone C245, catalog #554136). Antibodies purchased from Cell Signaling Technology (Beverly, MA) included: total RB (clone 4H1, Catalog #9309), phospho-RB (Ser608) (#2181), phospho-AKT (Ser473) (#4060), cyclin D1 (#9309), PARP-1 (#9542), caspase 3 (#9665), caspase 9 (#9502), and phospho-p70 S6K (Thr389, #9205). β-actin antibody was purchased from Sigma Aldrich (St. Louis, MO, catalog #A1978).
Laboratory-grade palbociclib was generously provided by Pfizer, Inc. (New York, NY) and purchased from Selleck Chemicals (Boston, MA). Everolimus and pemetrexed were purchased from LC chemical (Woburn, MA). Decitabine was purchased from Sigma (St. Louis, MO). Selumetinib, flavopiridol, sunitinib, AZD5438, ponatinib, AZD4547, erlotinib, pazopanib, imatinib, PF-04691502, dacomitinib and rapamycin were purchased from Selleck Chemicals (Boston, MA). Depsipeptide was obtained from the NCI Repository in the Developmental Therapeutics Program (NSC #309132, Bethesda, MD). Stock solutions for all the agents were prepared in 100% DMSO (Sigma, St. Louis, MO) at 10mM concentrations and stored at -20°C. Stock solutions were diluted in fresh RPMI 1640 media prior to each experiment.

Gopalan P.K., Villegas A.G., Cao C., Pinder-Schenck M., Chiappori A., Hou W., Zajac-Kaye M., Ivey A.M, & Kaye F.J. (2018). CDK4/6 inhibition stabilizes disease in patients with p16-null non-small cell lung cancer and is synergistic with mTOR inhibition. Oncotarget, 9(100), 37352-37366.

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Kinase Inhibitor Screening Protocol

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The serine kinase inhibitors used in this study were: AZD5438 (CDK1/2/9 inhibitor, Selleckchem), R547 (CDK1/2/4 inhibitor, Selleckchem), CVT313 (CDK1/2 inhibitor, EMD Millipore), PD0332991 (CDK4/6 inhibitor, Selleckchem), CX-4945 (CK2 inhibitor, Selleckchem or Pfizer), CHIR99021 (GSK3 inhibitor, Selleckchem), SB216763 (GSK3 inhibitor, Selleckchem), PLX-4720 (BRAFV600E inhibitor, Plexxikon) and LiCl (GSK3 inhibitor, Sigma). All the small molecule inhibitors were dissolved in DMSO and stock solutions were kept at −20°C, except LiCl which was dissolved in water and kept at room temperature.

Zhou J., Tien A.C., Alberta J.A., Ficarro S.B., Griveau A., Sun Y., Deshpande J.S., Card J.D., Morgan-Smith M., Michowski W., Hashizume R., James C.D., Ligon K.L., Snider W.D., Sicinski P., Marto J.A., Rowitch D.H, & Stiles C.D. (2017). A Sequentially Priming Phosphorylation Cascade Activates the Gliomagenic Transcription Factor Olig2. Cell reports, 18(13), 3167-3177.

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Kinase Inhibitor Evaluation Protocol

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Ribociclib, palbociclib, AZD5438, and dinaciclib were from Selleck (Houston, TX). All other chemicals used in this study were from Sigma (St. Louis, MO). The following antibodies were used: β-actin (#4970), Bcl-xL (#2764), phospho-Akt (#4051), total Akt (#9272), cyclin B1 (#4135), cyclin D1 (#2922), cyclin D3 (#2926), CDK4 (#2906), CDK6 (#3136), KU70 (#4104), PTEN (#9559), Phospho-RB (#9307), Bak (#3814), Bax (#2774), Mcl-1 (#4572), Cytochrome c (#4280), smac/DIABLO (#2954), total H2AX (#2595), phospho-H2AX (#2577), HSP70 (#4873), caspase-3 (#9664), caspase-7 (#9494), caspase-8 (#9746), caspase-9 (#9501), caspase-10 (#9752), and PARP (#9546) were from Cell Signaling Technology (Beverly, MA). AIF (sc-5586) was from Santa Cruz Biotechnology (Santa Cruz, CA). Monoclonal anti-Bax (#556467) and RAD51 (#ab63801) were from BD Pharmingen (San Diego, CA) and Abcam (Cambridge, MA), respectively.

Premkumar D.R., Jane E.P., Thambireddy S., Sutera P.A., Cavaleri J.M, & Pollack I.F. (2017). Mitochondrial dysfunction RAD51, and Ku80 proteolysis promote apoptotic effects of Dinaciclib in Bcl-xL silenced cells. Molecular carcinogenesis, 57(4), 469-482.

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Cell Cycle Inhibitor Effects on Blastula

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To assess the effect of specific cell cycle inhibitors on arresting blastula cell cycles, normal embryos were incubated with 100 μM of Cdk inhibitors, including RO-3306 (Sigma, Cat# SML0569), JNJ-7706621 (Selleck Chemicals, Cat# S1249), AZD5438 (Selleck Chemicals, Cat# S2621), BMS-265246 (Selleck Chemicals, Cat# S2014), and SKPin C1 (Selleck Chemicals, Cat# S8652), respectively, from 5 hpf to 7.5 hpf. Untreated and DMSO-treated embryos were used as negative controls, and CHX (0.2 mg/ml) treated embryos were used as positive controls. Live embryos at 7.5 hpf were imaged under a stereomicroscope using Leica Application Suite X (LAS X) (Leica Microsystems, Germany).

Chen H, & Good M.C. (2022). Nascent Transcriptome Reveals Orchestration of Zygotic Genome Activation in Early Embryogenesis. Current biology : CB, 32(19), 4314-4324.e7.

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Investigating RAS and Cell Cycle Inhibitors

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AZD5438, RO-3306, AT7519, Dinaciclib and PD023309 were purchased from Selleck chemicals. Antibodies targeting pan-RAS (Millipore), KRAS (Sigma), β-Actin, PARP-1 (F-2) (Santa Cruz), CDK1, Phospho-CDK1 (Thr161), Rb and Phospho-Rb (Ser 807/811) (Cell Signaling Technology), were employed in western blot.

Costa-Cabral S., Brough R., Konde A., Aarts M., Campbell J., Marinari E., Riffell J., Bardelli A., Torrance C., Lord C.J, & Ashworth A. (2016). CDK1 Is a Synthetic Lethal Target for KRAS Mutant Tumours. PLoS ONE, 11(2), e0149099.

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Monitoring DNA Double-Strand Break Repair

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For monitoring DSB repair, cells were seeded in chamber slides (Lab-Tek) and treated with TMZ (10 µM) for 48 hours, MNNG (1 µM) for 48 hours, CPT (50 nM) for 2 hours, or ETO (2 µM) for 1 hour, or irradiated at 1 Gy (cesium source; JL Shepherd and Associates). For assessing the effects of CDK inhibition on DSB repair, cells were first treated with TMZ (10 µM) for 48 hours after which TMZ-containing medium was replaced with medium containing either 5µM Roscovitine (Sigma-Aldrich) or 0.25µM AZD5438 (Selleck). Cells were fixed at the indicated times, and processed for immunofluorescence staining with anti-53BP1 antibody (Santa Cruz), as described before (31 (link)). The average numbers of 53BP1 foci per nucleus were determined after scoring at least 50 nuclei and subtracting background. Images were captured using a Leica DH5500B fluorescence microscope (40× objective lens) coupled to a Leica DFC340 FX camera using the Leica Application Suite v3 acquisition software.

Gil del Alcazar C.R., Todorova P.K., Habib A.A., Mukherjee B, & Burma S. (2016). Augmented HR Repair Mediates Acquired-temozolomide Resistance in Glioblastoma. Molecular cancer research : MCR, 14(10), 928-940.

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Maintenance and Manipulation of U2OS and HEK-293 Cells

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U2OS and HEK-293 cells (obtained from ATCC) were maintained in α-MEM and DMEM medium, respectively, supplemented with 10% fetal bovine serum and penicillin/streptomycin in a humidified atmosphere with 5% CO₂. A U2OS line with stable shRNA-mediated knockdown of BRCA1 was generated by transfection with a pGIPZ vector (TATGTGGTCACACTTTGTG; No: V2LHS_254648, Thermo Scientific) using Lipofectamine2000 (Invitrogen) followed by selection and continued maintenance in puromycin (1 μg/ml, Invitrogen). Control cells were generated by transfection with a pGIPZ vector expressing scrambled shRNA (No: RHS4346, Thermo Scientific). For CDK inhibition, cells were incubated with 2μM AZD5438 (Selleck) or 10μM Roscovitine (Sigma) for 5 hours before cells were harvested or irradiated.

Tomimatsu N., Mukherjee B., Hardebeck M.C., Ilcheva M., Camacho C.V., Harris J.L., Porteus M., Llorente B., Khanna K.K, & Burma S. (2014). Phosphorylation of EXO1 by CDKs 1 and 2 regulates DNA end resection and repair pathway choice. Nature communications, 5, 3561.

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DNA Damage and Replication Stress Compounds

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Unless stated otherwise the following compounds were used in this manuscript at the indicated final concentrations: ATRi Az-20 (1 μM, 5198, Tocris), ATRi VE-821 (10 μM, S8007, Selleckchem), Camptothecin (50 nM, S1288, Selleckchem), Roscovitine (20 μM, S1153, Selleckchem), Olaparib (10 μl, S1060, Selleckchem), DRB (100 μM, D1916, Sigma), Flavopiridol (1.25 μM, S1230, Selleckchem), AZD5438 (1 μM, S2621, Selleckchem), Hydroxyurea (HU, 2 mM, H8627, Sigma), Doxycycline (1-1000 ng/mL, D9891, Sigma), CDC7i (25 μM, S2742, Selleckchem), Aphidicolin (0.2 μM, A0781, Sigma), Diospyrin D (10 μM, gift of Dr. Pavel Janscak).

Teloni F., Michelena J., Lezaja A., Kilic S., Ambrosi C., Menon S., Dobrovolna J., Imhof R., Janscak P., Baubec T, & Altmeyer M. (2019). Efficient Pre-mRNA Cleavage Prevents Replication-Stress-Associated Genome Instability. Molecular Cell, 73(4), 670-683.e12.

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Compound Library Maintenance and Validation

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Compounds
in the DOS Informer, DOS-A, Repurposing,
and Bioactive libraries were maintained in the Broad Institute and
printed into 96- and 384-well plates using a Tecan D300e drug printer.
A subset of the repurposed compounds was purchased commercially for
validation studies: PIK-93, GSK2126458 (Omipalisib), Duvelisib (IPI-145,
INK1197), KD025 (SLx-2119), LY2784544, Palbociclib, Torin-2, AZD8186,
AT-9283, and AZD5438 (Selleckchem); ETP-45658 (R&D Systems); ETP-46464,
CP-640186, and BMS-536924 (Sigma-Aldrich); PF-03814735, TGX-221, and
Taselisib (GDC-0032) (Cayman Chemical); anandamide (VWR Scientific);
AM404 (Santa Cruz Biotech) and oleylethanolamide (Combi Blocks). Stock
solutions were prepared in DMSO and stored as per manufacturer’s
instructions.

Small J.C., Joblin-Mills A., Carbone K., Kost-Alimova M., Ayukawa K., Khodier C., Dancik V., Clemons P.A., Munkacsi A.B, & Wagner B.K. (2022). Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity. ACS Chemical Biology, 17(5), 1131-1142.

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Maintenance and Manipulation of U2OS and HEK-293 Cells

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