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ヒストン認識タンパク質（Reader）関連化合物
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Cayman Chemical社 エピジェネティクス関連低分子化合物
ヒストン認識タンパク質（Reader）関連化合物
Reader関連低分子化合物
Cayman Chemical社 エピジェネティクス関連低分子化合物
ヒストン認識タンパク質（Reader）関連化合物
掲載日情報：2017/04/03 現在Webページ番号：65559
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Epigenetics Screening Library
エピジェネティクスにおいて、”writer”、”eraser”、”reader”として知られる約140種の低分子化合物のライブラリー「Epigenetics Screening Library」の詳細については、こちらをご覧下さい。
Epigenetics Screening Library (#11076)
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低分子化合物製品
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| Eraser | Reader | Writer |
|---|
細胞ごとにクロマチンの状態は、さまざまな修飾によって制御されています。修飾を担う酵素“Writer”、修飾されたヒストンを認識するタンパク質“Reader”、脱修飾する酵素“Eraser”が関与し、細胞の分化・発達を調節しています。
参考文献
William P. Janzen, et al., Drug Discovery Today: Technologies, 7(1), (2010).
Alexander Tarakhovsky, Nature Immunology, 11, 565～568 (2010).
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Reader関連化合物
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| 商品コード | 品名 | 製品詳細 |
|---|---|---|
| 11232 | (-)-JQ1 | The inactive stereoisomer of a selective BET bromodomain inhibitor |
| 11187 | (+)-JQ1 | Displaces BET proteins from chromatin by competitively binding to the acetyl-lysine recognition pocket of BET bromodomains; binds BRD4 bromodomains 1 and 2 with Kd values of ~50 and 90 nM, respectively |
| 17448 | BAZ2-ICR | A selective inhibitor of BAZ2A (Kd=109 nM; IC50=130 nM) and BAZ2B (Kd=170 nM; IC50=180 nM) bromodomains |
| 17385 | BI-2536 | A selective inhibitor of Plk1 (IC50=0.83 nM); induces mitotic arrest and apoptosis in diverse human cancer cell lines and drives regression of human tumor xenografts in nude mice; also an inhibitor of BRD4 (IC50=25 nM) |
| 20311 | BI-7273 | A potent and selective BRD9 bromodomain inhibitor (Kd=15.4 nM; IC50=19 nM) that less effectively inhibits the BRD7 bromodomain (IC50=117 nM); inhibits the growth of EOL-1 acute myeloid leukemia cells in vitro (EC50=1.4μM) |
| 17897 | BI-9564 | A selective inhibitor of BRD9 and BRD7 bromodomains (Kds=14.1 and 239 nM; IC50=75 nM and 3.4μM; ~90% inhibition in FRAP assay at 0.1μM and 1μM, respectively); inhibits the growth of EOL-1 AML cells both in vitro (EC50=800 nM) and in a disseminated mouse model of AML (180 mg/kg/day) |
| 14119 | Bromosporine | A non-selective bromodomain inhibitor that at 1μM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells |
| 19956 | CeMMEC1 | A selective inhibitor of TAF1 bromodomain 2 (Kd=1.8μM; IC50=0.9μM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells |
| 20224 | CeMMEC13 | A selective inhibitor of TAF1 bromodomain 2 (IC50=2.1μM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells |
| 15479 | CPI-203 | A primary amide analog of (+)-JQ1 which has shown superior bioavailability with oral or i.p. administration; inhibits BRD4 binding and action in vitro or in cells; arrests the growth of leukemia T cells in vitro (EC50=91 nM) and rapidly suppresses leukemia burden in mice |
| 18044 | dBET1 | A hybrid molecule that combines (+)-JQ1 and lenalidomide; induces cereblon-dependent BET protein degradation in vitro (EC50=430 nM) and in vivo and delays leukemia progression in mice |
| 14120 | GSK2801 | A selective, cell-permeable inhibitor of the BAZ2 family of bromodomain containing proteins (IC50=9-350 nM in a BAZ2B AlphaScreen; KDs=0.26 and 0.14μM, for BAZ2A and BAZ2B respectively) |
| 18123 | GSK5959 | A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC50=80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3 |
| 11181 | I-BET151 | An isoxazole class pan-BET family inhibitor, blocking BRD2, BRD3, and BRD4 with IC50 values of 0.5, 0.25, and 0.79μM, respectively); induces apoptosis or triggers G0/G1 cell cycle arrest in MLL-fusion cell lines; effective in vivo, suppressing MLL leukemia progression in two different mouse models |
| 10676 | I-BET762 | A synthetic compound which interacts with BET proteins with high-affinity (Kd=32.5-42.5 nM); disrupts binding of BET proteins with acetylated histones, suppressing the expression of specific inflammatory genes involved in sepsis and endotoxic shock |
| 17749 | I-BRD9 | A selective BRD9 bromodomain inhibitor (pIC50=7.3; pKd=8.7); used to identify genes regulated by BRD9 in Kasumi-1 cells involved in cancer and immune response signaling |
| 14468 | I-CBP112 (hydrochloride) | A selective inhibitor of CBP and EP300 which directly binds their bromodomains (Kds=0.142 and 0.625 μM); shows only weak cross reactivity with the bromodomains of BET proteins and shows no interaction with other bromodomains |
| 17662 | NI-57 | A selective, potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry |
| 18316 | NVS-CECR2-1 | A potent and selective inhibitor of CECR2 (IC50=0.047μM by Alpha screen, Kd=0.80μM by ITC); shows robust activity in cells, by FRAP assay, due to its slow off-rate |
| 17124 | OF-1 | A chemical probe for the bromodomains of the BRPF family of proteins; binds BRPF1B, BRPF2, and BRPF3 with Kd values of 0.1, 0.,5 and 2.4μM, respectively, as determined by ITC, |
| 15947 | OTX015 | An orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50=10-19 nM) that displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias |
| 18811 | PF-CBP1 | An inhibitor of the CBP and p300 bromodomains (IC50=125 and 363 nM, respectively) |
| 11155 | PFI-1 | A BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 bromodomain 2 and BRD4 bromodomain 1 with IC50 values of 98 nM and 0.22 μM, respectively |
| 15267 | PFI-3 | Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases |
| 17663 | PFI-4 | A chemical probe that specifically binds to the bromodomain of BRPF1 (Kd=13 nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21); potent in cells, with an IC50 value of 250 nM |
| 16424 | RVX-208 | A selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50=0.04-0.28μM) over BD1 (IC50=1.8-3.1μM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces atherosclerosis in hyperlipidemic ApoE-deficient mice |
| 14469 | SGC-CBP30 | A potent inhibitor of CREBBP and EP300 bromodomains (IC50=21-69 and 38 nM, respectively) |
| 17123 | UMB-32 | An inhibitor of BRD4 (Kd=550 nM; IC50=637 nM),TAF1 (Kd=560 nM), and TAF1L (Kd=1.3μM) |
| 20566 | UNC1079 | An inactive analog of UNC1215 intended for use as a negative control |
| 13968 | UNC1215 | A potent, selective chemical probe for the methyl lysine reading function of L3MBTL3 (Kd=120 nM; IC50=40 nM) that competitively displaces mono- or dimethyl-lysine containing peptides |
| 17699 | MM-102 | A WDR5/MLL interaction inhibitor (IC50=2.4 nM) that blocks MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis; inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins |
| 13956 | S-(5'-Adenosyl)-L-Methionine Chloride (hydrochloride) | A ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by DNA and protein methyltransferases |
| 13945 | WDR5-0103 | A small molecule that binds a peptide-binding pocket on WDR5 (Kd=450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50=39μM) |
| 14422 | Doxycycline (hyclate) | A tetracycline-like antibiotic which effectively controls or prevents a diverse array of infections; used as the regulator for inducible gene expression systems; inhibits certain MMPs, such as MMP-8 (Ki=36μM) |
| 11076 | Epigenetics Screening Library (96-Well) | The Epigenetics Screening Library contains more than 140 small molecules that are known to modulate the activity of a variety of epigenetic 'writers and erasers' and “reader” proteins in a 96-well Matrix tube rack format as 10 mM stocks in DMSO. It may include compounds that modulate the activity of methyltransferases, demethylases, histone acetyltransferases, histone deacetylases, and acetylated histone binding proteins. |
| 14190 | Gilvocarcin V | An antitumor antibiotic that inhibits DNA synthesis by promoting the selective cross-linking of both histone H3 and the heat shock protein, GRP78 to DNA when photoactivated by near-UV or visible light |
| 17533 | MS37452 | A competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki=43μM); derepresses transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells at 250μM |
| 14102 | OAC1 | An Oct4-activating compound that activates expression through the Oct4 gene promoter; at 1 μM, enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells from embryonic fibroblasts expressing Oct4 with Sox2, Klf4, and c-Myc |
| 14103 | OAC2 | An Oct4-activating compound which activates expression through the Oct4 gene promoter; at 1 μM, enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells from embryonic fibroblasts expressing Oct4 with Sox2, Klf4, and c-Myc |
| 14104 | OAC3 | An Oct4-activating compound which activates expression through the Oct4 gene promoter; at 1 μM, enhances reprogramming efficiency by increasing the rate of production of induced pluripotent stem cells from embryonic fibroblasts expressing Oct4 with Sox2, Klf4, and c-Myc |
| 16365 | Octyl-α-Hydroxyglutarate | A cell-permeable derivative of 2-HG |
| 18167 | Riboflavin 5'-Monophosphate (sodium salt hydrate) | A coenzyme that is tightly bound to enzymes catalyzing oxidation and reduction reactions in a variety of biosynthetic pathways; binds the FMN riboswitch (RFN element) on RNA to alter gene regulation; a substrate of FMN phosphohydrolases |
| 14749 | Fostriecin | An inhibitor of PP2A and PP4 (IC50=3.2 and 3 nM, respectively); less effectively inhibits topoisomerase II and PP1 (IC50=40 and 131 μM, respectively) and does not inhibit PP2B |
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