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Pf 3644022

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PF-3644022 is a selective small molecule inhibitor of Bromodomain-containing protein 4 (BRD4), a member of the bromodomain and extraterminal (BET) family of proteins. It functions by binding to the bromodomains of BRD4, thereby disrupting its interactions with acetylated chromatin and inhibiting its transcriptional regulatory activities.

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Lab products found in correlation

Cycloheximide (chx), by Merck Group (4 mentions) α thrombin, by Enzyme Research (3 mentions) Tpca 1, by Bio-Techne (2 mentions) 7 oxozeanol, by Bio-Techne (2 mentions) Bx795, by InvivoGen (2 mentions) Nec 1, by Abcam (2 mentions) Mrt67307, by Merck Group (2 mentions) Z vad fmk, by Abcam (2 mentions) Sp600125, by Selleck Chemicals (2 mentions) Poly 1 c, by InvivoGen (2 mentions) Tak1 inhibitor 5z 7 oxozeaenol, by Bio-Techne (2 mentions) Lps eb ultrapure, by InvivoGen (2 mentions) Ikk16, by Bio-Techne (2 mentions) Vx 745, by Selleck Chemicals (1 mentions) Doxorubicin, by Cayman Chemical (1 mentions) Staurosporine, by Cayman Chemical (1 mentions) Gemcitabine, by Selleck Chemicals (1 mentions) Gsk872, by MedChemExpress (1 mentions) Nec 1, by Enzo Life Sciences (1 mentions) Lps escherichia coli o55 b5, by Merck Group (1 mentions)

10 protocols using pf 3644022

1

Kinase Inhibitor Assay Protocol

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The ERK1/2 inhibitor PD184352 was from Axon and was used at a final concentration of 2 μm. The p38 inhibitor VX-745 was from Selleck and was used at a final concentration of 1 μm. The PI3K inhibitor GDC-0941 was from Axon and was used at a final concentration of 1 μm. The MK2/3 inhibitor PF3644022 was from Tocris and was used at a final concentration of 5 μm. These concentrations were used because they have previously been established to inhibit the target kinases in cultured cells (50 (link), 66 (link), 67 (link)). The N-terminal MSK1/2 inhibitor SB747651A, which also inhibits RSK, was from Axon and was used at a final concentration of 10 μm. The C-terminal RSK/MSK1/2 inhibitor compound 20 (51 (link)) was generated in-house and was used at a final concentration of 10 μm. The RSK inhibitor LJI308 (47 (link), 48 (link)) was also generated in-house and was used at a final concentration of 10 μm unless otherwise stated. The selectivity of PD184352, VX745, and SB747641 has been published previously (33 (link), 50 (link), 66 (link)). The selectivity of LJI308 is given in Fig. S2. The CREB–CBP interaction inhibitor Naphthol AS-E (CAS 92-78-4) was from Calbiochem and used at 20 μm.
Sutavani R.V., Phair I.R., Barker R., McFarlane A., Shpiro N., Lang S., Woodland A, & Arthur J.S. (2017). Differential control of Toll-like receptor 4–induced interleukin-10 induction in macrophages and B cells reveals a role for p90 ribosomal S6 kinases. The Journal of Biological Chemistry, 293(7), 2302-2317.
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2

Kinase Inhibitor Library for Cell Treatments

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The kinase inhibitor library, composed of 149 selective or broad-spectrum kinase inhibitors dissolved in DMSO (10 mM stock concentration), was purchased from Cayman Chemicals (#10505). The following reagents were used for cell treatments at given concentrations: LPS (Escherichiacoli O55:B5, #L2880, Sigma-Aldrich, 100 ng ml−1), recombinant human TNFα (rHuTNF, #50435.50, Biomol, 10 ng/ml), Birinapant/SM (#HY-16591, MedChem Express, 1 µM), pan-caspase inhibitor zVAD-fmk (#4026865.0005, Bachem, 25 μM), MK2 inhibitor PF3644022 (#4279, Tocris, 5 μM), RIPK1 inhibitor Nec-1 (#BML-AP309-0020, Enzo Life Sciences, 50 µM), RIPK1 inhibitor Nec-1s (# 10-4544-5 mg, Tebu-Bio, 50 µM), RIPK3 inhibitor GSK872 (#HY-101872, MedChem Express, 5 µM), IKKβ inhibitor BMS345541 (#Axon 1731, Axon Medchem, 5 µM), TBK1/IKKε inhibitor BX795 (#T1830, Tebu-Bio), 5-Iodotubercidin (#HY-15424, MedChem Express, 2.5–10 µM), ABT-702 dihydrochloride (#HY-103161, MedChem Express, 5 µM), Staurosporine (#81590, Cayman, 5 µM), Etoposide (#E1383, Sigma, 5 µM), Doxorubicin (#15007, Cayman, 5 µM), Gemcitabine (#S1714, Selleckchem, 100 nM).
Chauhan C., Kraemer A., Knapp S., Windheim M., Kotlyarov A., Menon M.B, & Gaestel M. (2023). 5-Iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFκB signaling. Cell Death Discovery, 9, 262.
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3

Inhibitors for Cell Signaling Pathways

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The following inhibitors were used at the indicated final concentration in vitro, unless otherwise specified in the figure or figure legends: MRT-67307 (Sigma-Aldrich, 2 µM), BX-795 (Invivogen, 1 µM), TPCA-1 (Tocris Bioscience, 5 µM), PF-3644022 (Tocris Bioscience, 1 µM), 7-oxozeanol (Tocris Bioscience, 1 µM), Nec-1s (Biovision, 10 µM) zVAD-fmk (Abcam, 20 µM), cycloheximide (Sigma-Aldrich).
All antibodies used in this study are listed in supplementary table 7 including information regarding dilutions and validation.
Lafont E., Draber P., Rieser E., Reichert M., Kupka S., de Miguel D., Draberova H., von Mässenhausen A., Bhamra A., Henderson S., Wojdyla K., Chalk A., Surinova S., Linkermann A, & Walczak H. (2018). TBK1 and IKKε prevent TNF-induced cell death by RIPK1 phosphorylation. Nature cell biology, 20(12), 1389-1399.
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4

Molecular Mechanisms of Thrombosis and Angiogenesis

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α-Thrombin was purchased from Enzyme Research Laboratories. The murine PAR1 agonist peptide TFLLRN and the human PAR1 agonist peptide TFLLRNPNDK were synthesized and purified by reverse-phase, high-pressure liquid chromatography at Tufts University Core Facility. Histamine dihydrochloride was obtained from Tocris. VEGF was purchased from PeproTech. Rabbit IgG antibody and purified GST-HSP27 were obtained from Rockland Immunochemicals. The J2 HSP27 inhibitor was synthesized and purchased from ProbeChem. PF3644022 was purchased from Tocris. SB203580 was from LC laboratories. Vorapaxar was from Axon MedChem and Fasudil was from LC Laboratories. Polyclonal rabbit anti-p38, polyclonal rabbit anti-MK2, polyclonal rabbit anti-MK3, polyclonal rabbit phospho-MK2 (Thr334), polyclonal rabbit anti-MLC, polyclonal rabbit anti-MYPT1, polyclonal rabbit anti-phospho-MYPT1, monoclonal mouse anti-phospho-MLC, monoclonal mouse anti-HSP27, and polyclonal rabbit phospho-HSP27 (Ser15, Ser78, and Ser82) antibodies were purchased from Cell Signaling Technology. Monoclonal mouse anti-GAPDH antibody was from GeneTex. Monoclonal mouse anti-RhoA antibody was from Santa Cruz Biotechnology. HRP-conjugated goat–anti rabbit and goat–anti mouse antibodies were from Bio-Rad Laboratories.
Rada C.C., Mejia-Pena H., Grimsey N.J., Cordova I.C., Olson J., Wozniak J., Gonzalez D.J., Nizet V, & Trejo J. (2021). Heat shock protein 27 activity is linked to endothelial barrier recovery after proinflammatory GPCR-induced disruption. Science signaling, 14(698), eabc1044.
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5

Inhibitors for Cell Signaling Pathways

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The following inhibitors were used at the indicated final concentration in vitro, unless otherwise specified in the figure or figure legends: MRT-67307 (Sigma-Aldrich, 2 µM), BX-795 (Invivogen, 1 µM), TPCA-1 (Tocris Bioscience, 5 µM), PF-3644022 (Tocris Bioscience, 1 µM), 7-oxozeanol (Tocris Bioscience, 1 µM), Nec-1s (Biovision, 10 µM) zVAD-fmk (Abcam, 20 µM), cycloheximide (Sigma-Aldrich).
All antibodies used in this study are listed in supplementary table 7 including information regarding dilutions and validation.
Lafont E., Draber P., Rieser E., Reichert M., Kupka S., de Miguel D., Draberova H., von Mässenhausen A., Bhamra A., Henderson S., Wojdyla K., Chalk A., Surinova S., Linkermann A, & Walczak H. (2018). TBK1 and IKKε prevent TNF-induced cell death by RIPK1 phosphorylation. Nature cell biology, 20(12), 1389-1399.
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6

DR3-Fc Synthesis Protocol

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α-CD40 (FGK4.5) was from Bioxcel. DSS was purchased from MP biomedicals. Z-VAD-FMK was from Apexbio Technology. Compound inhibitors used for in vitro study were SB 203580 (Selleck Chemicals), PF-3644022 (Tocris), SP600125 (Selleck Chemicals), Bay11-7085 (Selleck Chemicals), and SCH772984 (Apexbio Technology). Recombinant human TL1A was from Peprotech. DR3-Fc was synthesized by Biointron Biological Inc. Briefly, DR3-Fc was constructed by conjugating extracellular domain of mouse DR3 with mouse IgG1. The plasmid was purified from transiently transfected supernatant of the HEK293F cells by Protein A affinity column.
Li J., Shi W., Sun H., Ji Y., Chen Y., Guo X., Sheng H., Shu J., Zhou L., Cai T, & Qiu J. (2019). Activation of DR3 signaling causes loss of ILC3s and exacerbates intestinal inflammation. Nature Communications, 10, 3371.
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7

Modulation of Cell Death Pathways

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The Smac-mimetic Compound A, the caspase inhibitor IDN-6556 (Idun Pharmaceuticals) and the RIPK1 inhibitor Necrostatin were synthesized by TetraLogic Pharmaceuticals. The RIPK3 inhibitor GSK’872 was from Calbiochem. The TAK1 inhibitor (5Z)-7-Oxozeaenol, the IKK inhibitor IKK-16 and the MK2 inhibitor PF-3644022 were from Tocris Bioscience. Cycloheximide was from Sigma. Recombinant Fc-TNF was produced in house. Ultrapure LPS-EB and poly(I:C) were purchased from Invivogen.
Lalaoui N., Boyden S.E., Oda H., Wood G.M., Stone D.L., Chau D., Liu L., Stoffels M., Kratina T., Lawlor K.E., Zaal K.J., Hoffmann P.M., Etemadi N., Shield-Artin K., Biben C., Tsai W.L., Blake M.D., Kuehn H.S., Yang D., Anderton H., Silke N., Wachsmuth L., Zheng L., Moura N.S., Beck D.B., Gutierrez-Cruz G., Ombrello A.K., Pinto-Patarroyo G.P., Kueh A.J., Herold M.J., Hall C., Wang H., Chae J.J., Dmitrieva N.I., McKenzie M., Light A., Barham B.K., Jones A., Romeo T.M., Zhou Q., Aksentijevich I., Mullikin J.C., Gross A.J., Shum A.K., Hawkins E.D., Masters S.L., Lenardo M.J., Boehm M., Rosenzweig S.D., Pasparakis M., Voss A.K., Gadina M., Kastner D.L, & Silke J. (2019). Mutations that prevent caspase cleavage of RIPK1 cause autoinflammatory disease. Nature, 577(7788), 103-108.
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8

Modulation of Cell Death Pathways

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The Smac-mimetic Compound A, the caspase inhibitor IDN-6556 (Idun Pharmaceuticals) and the RIPK1 inhibitor Necrostatin were synthesized by TetraLogic Pharmaceuticals. The RIPK3 inhibitor GSK’872 was from Calbiochem. The TAK1 inhibitor (5Z)-7-Oxozeaenol, the IKK inhibitor IKK-16 and the MK2 inhibitor PF-3644022 were from Tocris Bioscience. Cycloheximide was from Sigma. Recombinant Fc-TNF was produced in house. Ultrapure LPS-EB and poly(I:C) were purchased from Invivogen.
Lalaoui N., Boyden S.E., Oda H., Wood G.M., Stone D.L., Chau D., Liu L., Stoffels M., Kratina T., Lawlor K.E., Zaal K.J., Hoffmann P.M., Etemadi N., Shield-Artin K., Biben C., Tsai W.L., Blake M.D., Kuehn H.S., Yang D., Anderton H., Silke N., Wachsmuth L., Zheng L., Moura N.S., Beck D.B., Gutierrez-Cruz G., Ombrello A.K., Pinto-Patarroyo G.P., Kueh A.J., Herold M.J., Hall C., Wang H., Chae J.J., Dmitrieva N.I., McKenzie M., Light A., Barham B.K., Jones A., Romeo T.M., Zhou Q., Aksentijevich I., Mullikin J.C., Gross A.J., Shum A.K., Hawkins E.D., Masters S.L., Lenardo M.J., Boehm M., Rosenzweig S.D., Pasparakis M., Voss A.K., Gadina M., Kastner D.L, & Silke J. (2019). Mutations that prevent caspase cleavage of RIPK1 cause autoinflammatory disease. Nature, 577(7788), 103-108.
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9

Chemical Reagents for Mast Cell Study

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Reagents used in this study were acquired from the indicated suppliers: trans-resveratrol, cyclodextrin, 5Z-7-Oxozeaenol and Evans blue (Sigma-Aldrich, St. Louis, MO, USA); LY294002, wortmannin, and ICI 182,780 (Abcam, Cambridge, UK); PF-3644022 (TOCRIS Bioscience, Bristol, U.K.); recombinant mouse IL-3, recombinant mouse stem cell factor (SCF), and recombinant human IL-33 (PeproTech, Rocky Hill, NJ, USA); recombinant human IL-3 (Thermo Fisher Scientific, Wilmington, DE, USA); recombinant mouse IL-33 (R & D systems, Minneapolis, MN, USA); anti-TNP IgE, anti–DNP mouse IgE mAb, anti–mouse CD16/32, PE–conjugated anti–mouse c-kit Ab, and APC–conjugated anti–mouse ST2 Ab (BD Bioscience, San Jose, CA, USA); DNP–BSA (Cosmo Bio, Tokyo, Japan); APC–conjugated anti–mouse CD63 Ab (Miltenyi Biotec, Bergisch Gladbach, Germany); anti–phospho–transforming growth factor β-activated kinase 1 (TAK1) Ab (Thr184/187; #4508), anti–phospho–IκB kinase (IKK) α/β Ab (Ser176/177; #2078), anti–phospho–p65 Ab (Ser536; #3033), anti–phospho–p38 Ab (Thr180/Thy182; #4511), anti–phospho–MK2 Ab (Thr334; #3007), anti–phospho–Akt Ab (Ser473; #4060), anti–phospho–Gab2 Ab (Tyr452; #3882), anti–phospho–Syk Ab (Tyr525/526; #2710), anti–phospho–p70S6K Ab (Tyr389; #9234), anti–phospho–AMPK Ab (Thr172; #2535), anti–β-actin Ab (#4970), and AICAR (#9944) (Cell Signaling Technology, Danvers, MA, USA).
Nakajima S., Ishimaru K., Kobayashi A., Yu G., Nakamura Y., Oh-oka K., Suzuki-Inoue K., Kono K, & Nakao A. (2019). Resveratrol inhibits IL-33–mediated mast cell activation by targeting the MK2/3–PI3K/Akt axis. Scientific Reports, 9, 18423.
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10

In Vitro and In Vivo Anticancer Drug Screening

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All reagents and drugs were obtained from the following (Table S2): Gemcitabine and irinotecan (Washington University Siteman Cancer Center Pharmacy), 5-FU (Sigma-Aldrich #F6627), oxaliplatin (Sigma #O9512), SN-38 (Sellekchem #S4908), PF3644022 (Tocris #4279), (5Z)-7-Oxozeaenol (Tocris #3604), hydroxychloroquine (Sigma-Aldrich #H0915), recombinant TNFα (BioLegend #570104), trametinib (Selleckchem #S2673), AS2444697 (Tocris #5430), KU55933 (Selleckchem #S1092), VE821 (Selleckchem #S8007), SP600125 (Selleckchem #S1460), IMD0354 (Tocris #2611), GSK963 (Selleckchem cat# S8642). ATI-450 was provided by Aclaris Therapeutics Inc. under material transfer agreement. For in vivo experiments, ATI-450 was formulated in chow at 1000 parts per million, which achieved >60% inhibition of LPS-induced TNFα expression in mice (51 (link))
Grierson P.M., Dodhiawala P.B., Cheng Y., Chen T.H., Khawar I.A., Wei Q., Zhang D., Li L., Herndon J., Monahan J.B., Ruzinova M.B, & Lim K.H. (2021). The MK2/Hsp27 axis is a major survival mechanism for pancreatic ductal adenocarcinoma under genotoxic stress. Science translational medicine, 13(622), eabb5445.
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