Rgfp966

Manufactured by Selleck Chemicals

Sourced in United States

RGFP966 is a selective and potent inhibitor of HDAC9. It functions by inhibiting the enzymatic activity of HDAC9, a histone deacetylase enzyme. RGFP966 exhibits a high level of specificity for HDAC9 compared to other HDAC isoforms.

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Lab products found in correlation

41 protocols using rgfp966

Cytoskeletal Modulation in M1 Activation

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Actin depolymerization studies were performed with 100 nM Lat-A (L5163 Sigma). BMDMs were treated with Lat-A for 60 min before the addition of LPS, and Lat-A was kept in the medium along with LPS during M1 activation. Myosin II motor activity was inhibited with 50 μM blebbistatin (B0560 Sigma). BMDMs were treated with blebbistatin for 60 min before the addition of LPS, and the blebbistatin was kept in the medium along with LPS during M1 activation. For HDAC3 inhibition studies, BMDMs were treated with 20 μM RGFP966 (S7229 Selleckchem) for 24 h before LPS addition, and RGFP966 was kept in the medium along with LPS during M1 activation.

Jain N, & Vogel V. (2018). Spatial confinement downsizes the inflammatory response of macrophages. Nature materials, 17(12), 1134-1144.

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Adenine-Induced Chronic Kidney Disease Model

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Use of animals and the experimental protocol were in accordance with the university's guidelines and approved by the Institutional Animal Care Committee of Nanjing University Medical School. C57BL/6 male mice (Model Animal Research Center of Nanjing University) were housed in the animal facility on site under standard temperature (22 AE 2 C), humidity (50%-60%), and light conditions (12-hour light-dark cycles). Adenine model was established with 8-week-old male mice by adenine-containing diet (Sigma-Aldrich, St. Louis, MO) feeding (0.2% adenine in diet) for 4 to 6 weeks according to a previously established protocol, by which mice started to develop typical renal pathogenesis of CKD by 4 weeks and the much severer renal damage with bone complications by 6 weeks of adenine feeding. 33 Mice were randomly assigned to 1 of 4 groups consisting of 6 mice in each group: (i) Control: mice were on regular diet; (ii) TSA/RGFP966: mice received TSA (0.5 mg/kg body weight in 100 ml of phosphate-buffered saline i.p. injection daily; MedChem Express, USA) or RGFP966 (Selleck Chemical, Houston, TX; 3 mg/kg body weight subcutaneous injection every other day) treatment; 55 (iii) adenine: mice were on adenine diet feeding; and (iv) TSA or RGFP966-treated adenine mice.

Lin W., Zhang Q., Liu L., Yin S., Liu Z, & Cao W. (2017). Klotho restoration via acetylation of Peroxisome Proliferation-Activated Receptor γ reduces the progression of chronic kidney disease. Kidney international, 92(3).

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Cytotoxicity Evaluation of HDAC Inhibitors

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The cytotoxicity of cells treated with TSA (Sigma-Aldrich), NIC, Ms275, HPOB (Sigma-Aldrich), TMP269, RGFP966, PCI-34051 (Selleckchem) or VPA (Cayman Chemical) was measured by MTT assay as described previously ^{13 (link)}.

Bandyopadhaya A., Tsurumi A., Maura D., Jeffrey K.L, & Rahme L.G. (2016). A Quorum Sensing Signal Promotes Host Tolerance Training Through HDAC1-Mediated Epigenetic Reprogramming. Nature microbiology, 1, 16174.

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Compound Cytotoxicity Screening in Cells

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Cells were plated at 4000 cells/well in NS media into laminin-poly-l-ornithine coated 96-well plates (Corning). The compounds MI-3, RGFP-966, and AZD6102 (Selleckchem) were tested at different concentrations (range: 2 μM to 8 nM in serial dilutions) with six technical replicates per dose, and a DMSO control. Cell viability was assessed on day 7. Alamar blue (Thermo Fisher Scientific, Cat# DAL1025) was added and cells were incubated at 37 °C in the dark for 4 h. Fluorescence was measured on the Spectramax spectrophotometer and was normalized to the DMSO control.

Nikolic A., Maule F., Bobyn A., Ellestad K., Paik S., Marhon S.A., Mehdipour P., Lun X., Chen H.M., Mallard C., Hay A.J., Johnston M.J., Gafuik C.J., Zemp F.J., Shen Y., Ninkovic N., Osz K., Labit E., Berger N.D., Brownsey D.K., Kelly J.J., Biernaskie J., Dirks P.B., Derksen D.J., Jones S.J., Senger D.L., Chan J.A., Mahoney D.J., De Carvalho D.D, & Gallo M. (2023). macroH2A2 antagonizes epigenetic programs of stemness in glioblastoma. Nature Communications, 14, 3062.

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Selective HDAC Inhibitors for Lung Allograft Transplant

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Valproic acid for selective HDAC1 inhibition, RGFP966 for selective HDAC3 inhibition, LMK-235 for selective HDAC4 inhibition, Tubastatin A for selective HDAC6 inhibition, PCI-34051 for selective HDAC8 inhibition, and TSA for pan-HDAC inhibition were purchased from Selleckchem (Houston, TX, USA) and were used in various treatment groups. The chemicals were dissolved in dimethyl sulfoxide (DMSO; Sigma-Aldrich, St. Louis, MO, USA). Vehicle (DMSO) was used in control groups. 2 d before lung allograft transplant, the lung allograft recipient mice were treated with the vehicle, Valproic acid (300 mg/kg) 70 (link),71 (link), RGFP966 (10 mg/kg) 72 (link),73 (link), LMK-235 (20 mg/kg) 74 (link), Tubastatin A (30 mg/kg) 75 (link), PCI-34051 (40 mg/kg) 76 (link), or TSA (1 mg/kg) 77 (link) by intraperitoneal injection every day until lung allograft loss which was determined by Micro-Computer Tomography (micro-CT) Scans, unless specified.

Zhou W., Yang J., Saren G., Zhao H., Cao K., Fu S., Pan X., Zhang H., Wang A, & Chen X. (2020). HDAC6-specific inhibitor suppresses Th17 cell function via the HIF-1α pathway in acute lung allograft rejection in mice. Theranostics, 10(15), 6790-6805.

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Investigating the Effects of HDAC and DNA Methylation Inhibitors on Pituitary Tumor Cells

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The pituitary tumor-derived folliculostellate cell (PDFS) line (30 (link)) was maintained in DMEM (Life Technologies) supplemented with 10% FBS, 1% NEAA and PSG at 37°C with 10% CO₂. DNA methyltransferase inhibitor 5’-aza-2’-deoxycytidine (5’-AZA) was purchased from Sigma-Aldrich (Allentown, PA, USA). The HDAC3-specific inhibitor RGFP966 was purchased from Selleckchem (Houston, TX, USA) (31 (link)). To examine the effect of HDAC inhibition on the growth of PDFS, 1x10⁶ PDFS cells were plated on 100 mm cell culture dishes. After 24 hours, cells were treated with 10μM RGFP966 and/or 1μM 5’-AZA; with DMSO as a control. Culture medium was changed daily with fresh drug added. RNA was extracted from cells at Day 5. Cell proliferation was monitored at 24, 48, 72, and 96 hours by CCK8 Assay (see below).

Zhao W., Jiang X., Weisenthal K., Ma J., Botticelli E.M., Zhou Y., Hedley-Whyte E.T., Wang B., Swearingen B., Soberman R.J., Klibanski A, & Zhang X. (2022). High Histone Deacetylase 2/3 Expression in Non-Functioning Pituitary Tumors. Frontiers in Oncology, 12, 875122.

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Small Molecule Inhibitor Procurement

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SAHA, FK228, CI994, CAY10481, PCI24781, PCI34051, and RGFP966 were purchased from Selleck Chemicals (Houston, TX, USA). GGTase-I specific inhibitor GGTI-298 was purchased from Sigma-Aldrich (St. Louis, MO, USA). Anti-human GGTase-Iβ subunit and RhoA antibodies were purchased from Santa Cruz Biotechnology (Santa Cruz, CA, USA).

Li R, & Gan Y.H. (2017). Inhibiting HDAC1 Enhances the Anti-Cancer Effects of Statins through Downregulation of GGTase-Iβ Expression. International Journal of Molecular Sciences, 18(5), 1010.

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Protein Extraction and Analysis of HDAC Inhibitors

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Cells were seeded so that they would reach at ~90% confluency on the following day. After one wash with PBS, cells were treated with the medium supplemented with the vehicle solvent, sodium propionate (Sigma-Aldrich, P5436), sodium valproate (Sigma-Aldrich, P4543), SAHA (Sigma-Aldrich, SML0061), β-hydroxybutyrate (Sigma-Aldrich, H6501), TSA (Sigma-Aldrich, T8552), sodium butyrate (Sigma-Aldrich, B5887), or HDAC3 inhibitor RGFP966 (Selleckchem, S7229) for 24 hours. Cells were washed with PBS and lysed in the RIPA buffer (Thermo Fisher Scientific, 89900) to prepare soluble protein extracts or in the Triton extraction buffer (PBS containing 0.5% Triton X-100, 2 mM phenylmethylsulfonyl fluoride, 0.02% NaN₃, and protease inhibitors) to prepare protein extracts. Extracts were prepared in buffer K and further analyzed by immunoblotting with various antibodies as described above.

Yan K., Rousseau J., Machol K., Cross L.A., Agre K.E., Gibson C.F., Goverde A., Engleman K.L., Verdin H., De Baere E., Potocki L., Zhou D., Cadieux-Dion M., Bellus G.A., Wagner M.D., Hale R.J., Esber N., Riley A.F., Solomon B.D., Cho M.T., McWalter K., Eyal R., Hainlen M.K., Mendelsohn B.A., Porter H.M., Lanpher B.C., Lewis A.M., Savatt J., Thiffault I., Callewaert B., Campeau P.M, & Yang X.J. (2020). Deficient histone H3 propionylation by BRPF1-KAT6 complexes in neurodevelopmental disorders and cancer. Science Advances, 6(4), eaax0021.

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Angiotensin II Signaling Pathway

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Ang II was obtained from EMD Millipore (Billerica, MA, USA). MS-275 (S1053) and RGFP966 (S7229) were purchased from Selleckchem (Houston, TX, USA).

Ryu Y., Kee H.J., Sun S., Seok Y.M., Choi S.Y., Kim G.R., Kee S.J., Pflieger M., Kurz T., Kim H.S, & Jeong M.H. (2019). Class I histone deacetylase inhibitor MS-275 attenuates vasoconstriction and inflammation in angiotensin II-induced hypertension. PLoS ONE, 14(3), e0213186.

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Cytotoxicity Evaluation of HDAC Inhibitors

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