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Writer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

掲載日情報:2017/04/03 現在Webページ番号:65560

ヒストン関連研究において,”Eraser”,”Reader”または”Writer”各タンパク質に作用するCayman Chemical社の低分子化合物製品をご紹介致します。

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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)

Epigenetics Screening Library (#11076)



Eraser Reader Writer

Eraser, Reader, Writerについて

William P. Janzen, et al., Drug Discovery Today: Technologies, 7(1), (2010).
Alexander Tarakhovsky, Nature Immunology, 11, 565~568 (2010).




商品コード 品名 製品詳細
17079 BB-Cl-Amidine A Cl-amidine derivative with greater cellular potency against PAD4 activity (EC50=8.8μM, vs. >200μM for Cl-amidine) and a significantly longer in vivo half-life (1.75 h, vs. ~15 min for Cl-amidine); effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lpr mice
17490 GSK106 (hydrochloride) An inactive control for the selective PAD4 inhibitors, GSK484 and GSK199 (IC50s >100μM)
17491 GSK121 (trifluoroacetate salt) The initial compound identified in a screen for PAD4 inhibitors (IC50=3.2μM in functional assay) that was optimized to produce the more potent PAD4 inhibitors, GSK484 and GSK199
17489 GSK199 (hydrochloride) A selective inhibitor of PAD4 (IC50=200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils
17488 GSK484 (hydrochloride) A reversible inhibitor of PAD4 (IC50=50 nM) that binds to the low-calcium form of the enzyme; blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of NETs in both mouse and human neutrophils
14678 (R)-PFI-2 (hydrochloride) A potent, cell-permeable inhibitor of SET7/9 (IC50=2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases
18119 (S)-PFI-2 (hydrochloride) The inactive enantiomer of the SET7/9 inhibitor (R)-PFI-2 that may serve as a negative control
20526 (6R,S)-5,6,7,8-Tetrahydrofolic Acid (hydrochloride) A reduced form of folic acid that serves as a cofactor in methyltransferase reactions and is the major one-carbon carrier in one carbon metabolism; important for the synthesis of thymidine for incorporation into DNA or the synthesis of purines, as well as for the formation of methionine, which can be converted to the ubiquitous methyl donor, SAM
13373 2',3',5'-Triacetyl-5-Azacytidine A prodrug form of 5-azacytidine, an inhibitor of DNA methyltransferase, that may reverse epigenetic changes
13828 3-Deazaneplanocin A An inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in acute myeloid leukemia cells in a dose-dependent manner (0.2-1μM); increases expression of the cell-cycle regulators p21, p27, and FBXO32 leading to cell cycle arrest and apoptosis
11102 3-Deazaneplanocin A (hydrochloride) An analog of 3-deazaadenosine, an inhibitor of SAH hydrolase; depletes EZH2 levels and inhibits trimethylation of lysine 27 on histone H3 in primary human AML cells in a dose-dependent manner (0.2-1μM); acts synergistically with the pan-HDAC inhibitor panobinostat in inducing apoptosis of AML cells implanted in mice
18162 5-(Hydroxymethyl)-2’-Deoxycytidine A modified pyrimidine that is capable of producing interstrand cross-links in double-stranded DNA; used to quantify DNA hydroxymethylation levels in biological samples
11164 5-Azacytidine An inhibitor of DNA methyltransferases that reduces hypermethylation associated with certain diseases, including myelodysplastic syndromes (IC50=2.4 and 2.6μM for in vitro anti-myeloma activity) and cancer (IC50s ~ 0.4μM for inhibiting proliferation of various cancer cell lines)
16166 5-Methyl-2'-Deoxycytidine A pyrimidine nucleoside used in epigenetics research to investigate the dynamics of DNA methylation pattern in the control of gene expression
16111 5-Methylcytidine A modified nucleoside derived from 5-methylcytosine and is a minor constituent of RNA as well as DNA for certain organisms; used in epigenetics research, especially in studies involving DNA methylation processes
18317 A-196 A selective inhibitor of SUV420H1 and SUV420H2 (IC50=25 and 144 nM, respectively) that inhibits the di- and trimethylation of H4K20me in multiple cell lines
16081 A-366 A potent, peptide-competitive inhibitor of the lysine methyltransferase G9a (IC50=3.3 nM); significantly reduces the cellular levels of dimethylation on histone 3 at lysine 9 (H3K9Me2) in PC3 cells; also blocks the interaction of Spindlin1 with H3K4me3 by binding with a Spindlin1 Tudor domain (Kd=111 nM)
13965 AMI-1 (sodium salt) A cell permeable inhibitor of PRMTs; inhibits both yeast Hmt1p and human PRMT1 (IC50=3.0 and 8.8μM, respectively); also effectively blocks the activity of PRMTs 3, 4, and 6 but not that of lysine methyltransferases; inhibits HIV-1 reverse transcriptase (IC50=5.0μM)
16875 AZ 505 A potent inhibitor of SMYD2 (IC50=0.12μM) that is without effect on a panel of other protein lysine methyltransferases
13124 BIX01294 (hydrochloride hydrate) A selective inhibitor of G9a histone methyltransferase (IC50=1.7μM); less effectively inhibits G9a-like protein (GLP; IC50=38μM) and has no effect on other known histone methyltransferases
11787 BRD4770 An inhibitor of EHMT2, also known as G9a, decreasing di- and trimethylation on lysine 9 of histone 3 (EC50=5μM); induces senescence in the pancreatic cancer cell line PANC-1 without initiating apoptosis
14744 CAY10677 A cysmethynil analog that inhibits Icmt with an IC50 value of 0.86μM; demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells (IC50=2.63 vs. 27.4μM, respectively) and human prostate cancer PC3 cells (IC50=2.55 vs. 25.2μM, respectively)
13156 Chaetocin A fungal mycotoxin that inhibits the Lys9-specific histone methyltransferases SU(VAR)3-9 (IC50=0.8μM), G9a (IC50=2.5μM), and DIM5 (IC50=3μM)
18299 CPI-169 A selective EZH2 inhibitor (IC50=0.24, 0.51, and 6.1 nM for wild-type EZH2, Y641N mutant EZH2, and wild-type EZH1, respectively); decreases cellular levels of H3K27me3, triggering cell cycle arrest and apoptosis in NHL cell lines (EC50=70 nM) and NHL xenografts (200 mg/kg/twice a day)
19125 CPI-360 A selective EZH2 inhibitor (IC50=0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively); decreases cellular levels of H3K27me3 and H3K27me2 (EC50s=56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of NHL cell lines
14745 Cysmethynil An indole-based, time-dependent inhibitor of Icmt (IC50=i=0.14μM for the final complex); decreases mTOR signaling, accumulation of cells in the G1 phase, and autophagy-mediated cell death in PC3 prostate cancer cells
11166 Decitabine A 2' deoxy analog of 5-azacytidine which is incorporated into DNA and causes hypomethylation by inhibiting DNA methyltransferases in a concentration-dependent manner; useful in conditions characterized by DNA hypermethylation, as is found in myelodysplastic syndromes
19146 EI1 A selective EZH2 inhibitor that has activity against both wild-type and Y641F mutant EZH2 (IC50=15 and 13 nM, respectively); blocks cellular H3K27 methylation and activates PRC2-specific gene expression; decreases proliferation, cell cycle arrest, and apoptosis in diffused large B cell lymphoma cells carrying Y641 mutations
10569 Ellagic Acid A polyphenolic antioxidant that is abundant in many fruits, vegetables, plant bark, and peels; has anti-carcinogenic, anti-mutagenic, anti-inflammatory, and organ-preserving properties; blocks methylation of H3R17 by CARM1 without significantly altering histone acetylase or DNA methyltransferase activity
16173 EPZ004777 (formic acid salt) A potent DOT1L inhibitor (IC50=400 pM) that selectively kills (MLL) cells in vitro and prolongs survival in an MLL xenograft mouse model; accelerates the reprogramming of somatic cells into induced pluripotent stem cells
13966 EPZ005687 A potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki=24 nM), the enzymatic subunit of PRC2; blocks trimethylation of the PRC2 target H3K27 (IC50=80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2
19161 EPZ011989 A selective, orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutant of EZH2; demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma
17285 EPZ015666 A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki=5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice
19160 EPZ020411 An inhibitor of PRMT6 (IC50=10 nM) that less potently targets PRMT1 and PRMT8 (IC50=119 and 223 nM, respectively); dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing PRMT6 (IC50=0.637μM)
16175 EPZ5676 A highly potent and selective inhibitor of DOT1L histone methyltransferase activity (Ki=80 pM); inhibits the H3K79 methylation in various human leukemia cell lines (IC50=3-5 nM), decreasing MLL-fusion target gene expression and inhibiting proliferation; intravenous infusion of EPZ-5676 at a dose of 35 mg/kg can regress tumors in a rat xenograft model of MLL-rearranged leukemia
16174 EPZ6438 An orally bioavailable, selective inhibitor of EZH2 (Ki=2.5 nM); blocks H3K27 trimethylation in both wild-type and mutant lymphoma cells (IC50s range from 2-90 nM); induces apoptosis and differentiation specifically in SMARCB1-deleted malignant rhabdoid tumor cells and promotes their regression in xenograft-bearing mice
15415 GSK126 A selective, SAM-competitive small molecule inhibitor of EZH2 methyltransferase activity (Ki=0.57 nM; IC50=9.9 nM versus that of EZH1: Ki=89 nM; IC50=680 nM); inhibits global H3K27me3 levels, inhibiting the proliferation of EZH2 mutant DLBCL cell lines (IC50=28-61 nM) as well as the growth of EZH2 mutant DLBCL xenografts in mice receiving a daily dose of 50 mg/kg
14094 GSK343 A selective, cell-permeable EZH2 inhibitor (IC50=4 nM) that has been shown to inhibit the trimethylation of H3K27 in HCC1806 cells with an IC50 value of 174 nM
18531 GSK503 A selective inhibitor of EZH2 that prevents the methyltransferase activity of wild-type and mutant EZH2 with similar potency (Kiapp=3-27 nM); effective in vivo in mouse models of cancer
18354 GSK591 A chemical probe for PRMT5 that potently inhibits the PRMT5/MEP50 complex from methylating histone H4 (IC50=11 nM) in vitro; inhibits the symmetric arginine methylation of SmD3 (EC50=56 nM) in Z-138 cells
16441 LLY-507 A selective, cell-active, small molecule inhibitor of SMYD2 (IC50=15 nM); inhibits p53 lysine370 monomethylation in KYSE-150 esophageal squamous cell carcinoma cells stably expressing SMYD2 with an IC50 value of 0.6μM
11620 MI-2 (hydrochloride) Potently binds menin, blocks the menin-MLL fusion protein interaction (IC50=0.45μM), and induces apoptosis in cells expressing MLL fusion proteins
18361 MS023 (hydrochloride) A potent, selective inhibitor of type I PRMTs (IC50=20, 119, 83, 8, and 8 nM for PRMT1, 3, 4, 6, and 8, respectively)
18348 MS049 (hydrochloride) A selective inhibitor of PRMT4 (IC50=34 nM) and PRMT6 (IC50=43 nM); reduces H3R2me2a in HEK293 cells (IC50=0.97μM) and also, unexpectedly, to reduce H4R3me2a in HEK293 cells
18153 N6-Methyladenine A modified purine that is commonly found in genomes of prokaryotes, protists, and plants
13302 RG-108 A non-nucleoside DNA methyltransferase inhibitor (IC50=115 nM in vitro) that significantly reduces the methylation of genomic DNA in cells at 10μM without detectable toxicity
16376 S-(5'-Adenosyl)-L-methionine (sulfate tosylate) A stable salt of SAM that is included in nutritional supplements for oral use; reportedly ameliorates depression, pain associated with osteoarthritis and fibromyalgia, and liver toxicity
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
13967 SGC0946 A potent inhibitor of DOT1L (IC50=0.3 nM); over 100-fold selective over other PMTs; active in cells, reducing H3K79 dimethylation in A431 and MCF10A cells (IC50=2.6 and 8.8 nM, respectively)
17017 SGC707 A potent allosteric inhibitor of PRMT3 (IC50=50 nM) with >100-fold selectivity over other methyltransferases and other non-epigenetic targets; avidly binds PRMT3 (Kd=50 nM by isothermal titration calorimetry) and inhibits histone methylation in cells with an IC50 value below 1μM
11165 SGI-1027 An inhibitor of the DNA methyltransferases DNMT1, DNMT3A, and DNMT3B (IC50=12.5, 8, and 7.5μM, respectively, with Poly(dI-dC) as the substrate); reactivates silenced tumor suppressor genes by reducing CpG island hypermethylation
13829 Sinefungin A nucleoside structurally related to SAH and SAM that inhibits SET domain-containing methyltransferases (IC50 values range from 0.1-20μM)
13631 UNC0224 A potent and selective G9a HMTase inhibitor (IC50=15 nM, Kd=23 mM); more than 1,000-fold selective for G9a over SET7/9 and SET8
10582 UNC0321 (trifluoroacetate salt) A potent and selective G9a HMTase inhibitor (IC50=6 nM; Ki=63 pM); more than 40,000-fold selective for G9a over SET7/9, SET8, PRMT3, and JMJD2E
16400 UNC0379 A selective inhibitor of the lysine methyltransferase SET8 (IC50=7.3μM; Kd=18.3μM)
11084 UNC0631 A potent and selective inhibitor of G9a activity in vitro (IC50=4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50=25 nM)
10734 UNC0638 A potent, selective G9a and GLP HMTase inhibitor (IC50=MB231 cells (IC50=81 nM) and demonstrates favorable separation of functional and toxic effects
14604 UNC0642 A selective inhibitor of G9a and GLP methyltransferases that competitively inhibits binding of H3K9 substrates with a Ki=3.7 nM; reduces H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells (IC50=110 and 40 nM, respectively); displays improved pharmacokinetic properties relative to UNC0638
11085 UNC0646 A potent and selective inhibitor of G9a and GLP activities in vitro (IC50=6 and 15 nM, respectively) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50=26 nM)
14621 UNC1999 A selective, cell-permeable EZH2 inhibitor (IC50=2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC50 value of 124 nM
18122 UNC2327
17518 XY1 A close analog of SGC707 that is completely inactive against PRMT3 at concentrations as high as 100μM
10975 Zebularine A DNA methylation inhibitor that acts by forming a covalent complex with DNA methyltransferases (DNMTs); preferentially targets cancer cells demonstrating IC20 values of 20, 10, 20, and 5μM for reducing proliferation of TK6, Jurkat, KG-1, and HCT116 cells, respectively
10547 4-Pentynoyl-Coenzyme A (trifluoroacetate salt) An acyl-CoA donor that can be metabolically transferred onto lysine residues of proteins by lysine acetyltransferases; an azide-alkyne bioconjugation reaction, known as click chemistry, can then be used to tag the acetylated proteins with fluorescent or biotinylated labels for subsequent analysis
16160 Acetyl Coenzyme A (sodium salt) A pivotal molecule in the Krebs cycle, in the synthesis of fatty acids, and in isoprenoid-based protein modifications; serves as an intermediate in oxidation of fatty acids and amino acids; an essential cofactor or substrate for acetyltransferases and acyltransferases
13144 Anacardic Acid An alkyl salicylic acid isolated from cashew shells; inhibits the HAT activity of p300 and PCAF (IC50=8.5 and 5μM, respectively); suppresses NF-κB activation, inhibits IκBα phosphorylation, and prohibits p65 nuclear translocation
12095 Butyrolactone 3 Specifically inhibits the histone acetyltransferase Gcn5 (IC50=100μM) and can inhibit pre-RNA splicing with an IC50 value of 0.5 mM
10549 C646 An inhibitor of the HAT p300 (IC50=1.6μM); competitively binds p300 (Ki=400 nM) and does not inhibit several other acetyltransferases; blocks the growth of human melanoma, leukemia, lung, and prostate cancer cells in vitro
10974 CAY10669 An inhibitor of the HAT PCAF (p300/CREB-binding protein-associated factor; IC50=662μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid; dose dependently inhibits histone H4 acetylation in HepG2 cells in vitro at 30-60μM
16086 CAY10685 A cell-active analog of the lysine acetyltransferase inhibitor CPTH2 (Item No. 12086) that contains an alkyne moiety for use in click chemistry reactions; used to study changes in nuclear architecture associated with cancer and certain laminopathies
12086 CPTH2 (hydrochloride) Specifically inhibits Gcn5-dependent acetylation of histone H3K14 at a concentration of 0.8 mM both in vitro and in vivo
19570 CTPB An amide derivative that selectively activates the HAT p300, with maximal activation at 275μM
11012 Delphinidin (chloride) A natural plant pigment which induces the release of nitric oxide by vascular endothelium, causing vasorelaxation; inhibits signaling through EGFRs, suppressing the expression of ERα and inducing both apoptosis and autophagy at a dose of 1-40μM; inhibits the HAT activities of p300/CBP (IC50=~ 30μM)
10566 Garcinol An inhibitor of the HATs p300 and pCAF (IC50=7 and 5μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions
19835 HAT Inhibitor II A cell-permeable, selective inhibitor of the HAT p300 (IC50=5μM)
17778 L002 An inhibitor of p300 histone acetyltransferase (KAT3B; IC50=1.98μM in vitro); blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation
15346 NSC 697923 A selective inhibitor of the E2 ubiquitin-conjugating enzyme Ubc13 when heterodimerized with Uev1A, blocking polyubiquitin chain formation at concentrations of 0.5 to 2μM in vitro; blocks proliferation and induces apoptosis in DLBCL and NB cells
19093 PRT4165 An inhibitor of the ubiquitin ligase activity of PRC1; blocks BMI1/RING1A self-ubiquitination (IC50=3.9μM), as well as polyubiquitination of topoisomerase 2α in cells; inhibits ubiquitination of H2A by either RNF2 or RING1
16918 BG45 A selective inhibitor of HDAC3 (IC50=289 nM) that alone or in combination with bortezomib has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma
16919 BRD73954 A small molecule inhibitor that potently and selectively inhibits both HDAC6 and HDAC8 (IC50=36 and 120 nM, respectively)
16874 Nexturastat A A potent, selective inhibitor of HDAC6 (IC50=5.02 nM); dose-dependently induces hyperacetylation of α-tubulin in B16 murine melanoma cells without elevating histone H3 acetylation
16917 RGFP966 A selective inhibitor of HDAC3 (IC50=0.08μM) that does not affect other HDACs at concentrations up to 15μM; enhances long-term object memory acquisition/consolidation in mice; induces apoptosis of cutaneous T cell lymphoma cells by disrupting their DNA replication activity
16667 BMS 345541 (trifluoroacetate salt) A selective, cell permeable inhibitor of the IκB kinases IKKα and IKKβ (IC50=4 and 0.3μM); inhibits signaling through NF-κB both in cells and in vivo, showing excellent pharmacokinetics in mice
11796 Wedelolactone A natural coumestan that inhibits NF-κB signaling at the level of IKK action, resulting in suppression of NF-κB-mediated gene expression at concentrations of 1-100μM; also inhibits hepatitis C virus NS5B polymerase in vitro (IC50=36μM), STAT1 dephosphorylation (50μM), and EZH2-EED interactions (Kd=2.8μM)
18263 (6S)-Tetrahydrofolic Acid? A diastereomer of tetrahydrofolic acid that is 1,000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae
15774 6-Thioguanine A thio analog of the purine base guanine that incorporates into DNA during replication, inducing double-strand breaks that destabilize its structure and result in cytotoxicity; used as a chemotherapeutic for acute leukemia and other types of cancer, including BRCA2-mutated tumors
19551 Cyproheptadine A first-generation antihistamine that potently antagonizes the histamine H1 receptor (pKi=9.42); also antagonizes serotonin and muscarinic receptors at nanomolar concentrations
12092 Etoposide An inhibitor of topoisomerase II (IC50=60.3μM); can have much greater potencies when evaluated in cell-based cytotoxicity assays (e.g., IC50=5.14 nM for MCF-7 cells); can also inhibit nuclear receptor coactivator 3 (IC50 of 2.48μM)
14016 Iberin A natural isothiocyanate which induces the expression of phase II detoxification enzymes and activates Nrf2, promoting the expression of antioxidant and phase II genes; acts as a quorum sensing inhibitor, blocking acyl-homoserine lactone signaling in P. aeruginosa without affecting growth (IC50=31-62μM)
18098 ML167 A selective, ATP-competitive inhibitor of Clk4 (IC50=136 nM)
16972 RU-SKI 43 (hydrochloride) A cell-permeable inhibitor of Hhat (IC50=0.85μM); blocks palmitoylation of Shh without affecting palmitoylation of H-Ras or Fyn, myristoylation of c-Src, or acylation of Wnt3a; inhibits both autocrine and paracrine Shh-induced activation of Gli-mediated transcription
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.



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