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Cayman Chemical Company
ケイマン ケミカル / Cayman Chemical Company
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[掲載日情報:2017/04/03 現在]

Eraser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
ヒストン脱修飾酵素(Eraser)関連化合物

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。

本製品は研究用です。臨床用途には使用できません。

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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)


低分子化合物製品

項目をクリックすると一覧表がご覧いただけます。

Eraser Reader Writer

Eraser, Reader, Writerについて

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).

Eraser関連化合物

商品コードをクリックすると価格表がご覧いただけます。

商品コード 品名 製品詳細
15205 2-Hexyl-4-Pentynoic Acid Inhibits HDAC activity much more potently (IC50=13μM) than valproic acid (IC50=398μM); induces histone hyperacetylation in cerebellar granule cells significantly at 5μM; induces the expression of Hsp70-1a and Hsp70-1b and protects cerebellar granule cells from glutamate-induced excitotoxicity
10495 4-iodo-SAHA A hydrophobic derivative of the class I and class II HDAC inhibitor SAHA that demonstrates >60% inhibition of HDAC1 and HDAC6 activity in a deacetylase activity assay; inhibits proliferation of SK-BR-3 breast-derived, HT29 colon-derived, and U937 leukemia cell lines with EC50 values of 1.1, 0.95, and 0.12μM, respectively
13856 5-Nitroso-8-quinolinol An HDAC inhibitor, antitumor agent that at 10μM can induce oxidative stress contributing to apoptosis and differentiation in MCF-7 breast cancer cells; inhibits T. gondii tachyzoite propagation in human fibroblasts (EC50=80 nM) and inhibits P. falciparum growth in human red blood cells (EC50=1.3μM)
10575 Apicidin A fungal toxin that demonstrates selective inhibition of HDAC3/NcoR over HDAC6 (IC50=15.8 and 665.1 nM, respectively); has broad spectrum activity against Apicomplexan parasites and exhibits antiproliferative activity against various cancer cell lines (IC50=0.13-2.36μM)
19834 BRD4884 An HDAC inhibitor (IC50=29 nM, 62 nM, and 1.09μM for HDAC1, 2, and 3, respectively); possesses preferential binding kinetics with seven-fold longer half-life on HDAC2 compared to HDAC1 (143 min vs. 20 min)
19836 BRD6688 An HDAC inhibitor (IC50=21 nM, 100 nM, and 11.48μM for HDAC1, 2, and 3, respectively); possesses six6-fold extended half-life for binding on HDAC2 compared to HDAC1 (381 min vs. 65 min); rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model of neurodegeneration
89740 CAY10398 An inhibitor of HDAC (IC50=10μM)
10005019 CAY10433 An HDAC inhibitor with an IC50 value of 30μM when tested in HeLa cell nuclear extracts using 200μM acetylated fluorometric substrate
13146 CAY10603 A potent and selective inhibitor of HDAC6 (IC50=0.002 nM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively); prevents the growth of several pancreatic cancer cell lines (IC50=0.1-1μM)
15403 CAY10683 A potent HDAC inhibitor that inhibits HDAC2 and HDAC6 with IC50 values of 0.119 and 434 nM; ineffective against HDAC4 (IC50=>1,000 nM); inhibits the growth of HCT116 cells and HuT-78 cells (GI50=29.4 and 1.4μM, respectively) more effectively than human dermal fibroblasts (GI50=>100μM)
13172 CBHA HDAC1 and HDAC3 inhibitor (ID50=0.01 and 0.07μM, respectively, in vitro); induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0μM) and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg
13686 Chidamide An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4μM; dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle arrest in colon cancer cells
12084 CI-994 An inhibitor of class I HDACs with IC50 values of 0.9, 0.9, 1.2, and >20μM for recombinant human HDAC 1, 2, 3, and 8, respectively; displays a wide spectrum of antitumor activity, particularly in tumors normally refractory to conventional anticancer agents
10671 Coumarin-SAHA A fluorescent probe that competitively binds HDAC; demonstrates fluorescence excitation and emission maxima of 325 and 400 nm, respectively, which is quenched by 50% when bound to HDAC
16426 CUDC-101 A multi-target inhibitor that potently blocks EGFR and HER2 (IC50=2.4 and 16.4 nM, respectively) and inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC50=4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively)
10576 HC Toxin A cell-permeable, reversible inhibitor of HDACs (IC50=30 nM)
15200 HDAC6 Inhibitor A potent and selective inhibitor of HDAC6 (IC50=36 nM) that poorly blocks other HDAC enzymes; cell permeable, inhibiting the acetylation of tubulin in cells with an IC50 value of 210 nM
13295 HNHA A cell-permeable inhibitor of HDAC activity (IC50=100 nM)
15066 HPOB A potent, selective inhibitor of HDAC6 (IC50=56 nM); induces acetylation of α-tubulin but not histones; enhances the cytotoxicity of the broad spectrum HDAC inhibitor SAHA against cancer cells in nude mice carrying an androgen-dependent CWR22 human prostate cancer xenograft
11045 ITF 2357 Inhibits maize HDACs: HD2, HD-1B, and HD-1A (IC50 =7.5-16 nM) and reduces TNFα, IL-1α, and IL-1β production (IC50=10-22 nM); inhibits activity of cells expressing JAK2V617F (IC50=1-10 nM), which are implicated in the pathophysiology of many myeloproliferative diseases
18681 ITSA1 A cell-permeable suppressor of TSA action, reducing TSA-induced acetylation of histone and tubulin in A549 cells when given at 50μM; prevents TSA-mediated cell cycle arrest and apoptosis; blocks the action of the HDAC inhibitor SAHA, preventing SAHA-induced hyperacetylation of tubulin in A549 cells
14088 JNJ-26481585 A hydroxamate-based HDAC inhibitor that shows activity toward all HDAC enzymes with highest potency in vitro toward HDAC1 (IC50=0.11 nM)
16427 LAQ824 A hydroxamate-based inhibitor of HDACs with an IC50 value of 30 nM; inhibits the growth of colon, breast, prostate, and non-small cell lung cancer cell lines at concentrations of less than 1μM; augments the actions of fludarabine and imatinib mesylate in human leukemia cells
14969 LMK 235 An HDAC inhibitor that selectively targets HDACs 4 and 5 (IC50=12 and 4 nM, respectively) over other HDACs (IC50=56, 320, 850, 880, and 1,280 for HDACs 6, 1, 11, 2, and 8, respectively); displays enhanced cytotoxic effects against human cancer cell lines, compared to SAHA or TSA
13174 M 344 An inhibitor of HDACs, inhibiting maize HDAC (IC50=100 nM) as well as human HDAC1 (IC50=46 nM); shows a 3-fold selectivity for HDAC6 over HDAC1
18288 MI-192 An HDAC inhibitor that preferentially inhibits HDAC2 (IC50=30 nM) and HDAC3 (IC50=16 nM) over HDAC1, 4, 6, 7, and 8 (IC50=4.8, 5, >10, 4.1, and >10μM, respectively).{29271} At 0.1-0.4μM, it induces differentiation and promotes apoptosis of acute myeloid leukemic cell lines U937, HL60, and Kasumi-1
18287 Mocetinostat An orally available HDAC inhibitor that selectively targets HDAC1 and 2 (IC50=0.15 and 0.29μM, respectively), less potently inhibits HDAC3 and 11 (IC50=1.66 and 0.59μM, respectively); induces hyperacetylation of histones, causes cell cycle blockade, and induces apoptosis in cancer cells in vitro
13284 MS-275 An inhibitor of HDACs that preferentially inhibits HDAC1 (IC50=300 nM) over HDAC3 (IC50=8μM); does not inhibit HDAC8; induces p21/CIP1/WAF1, slowing cell growth, differentiation, and tumor development in vivo
13176 Oxamflatin A potent inhibitor of HDACs (IC50=15.7 nM); has been shown to alter the expression of several genes whose products are involved in cell morphology, motility, apoptosis, and cell cycle control, reducing the proliferation of cancer cells
13280 Panobinostat A potent inhibitor of all HDACs, with Ki values ranging from 0.6 to 31 nM for HDAC1-11; leads to acetylation of a range of cellular proteins, resulting in cell cycle arrest and apoptosis in cancer cells; has potential applications in spinal muscular atrophy and HIV therapy
20059 PCI 24781
10444 PCI 34051 A potent HDAC8 inhibitor (IC50=0.01μM) with >200-fold selectivity over HDAC isoforms 1, 2, 3, 6, and 10 (IC50=4, >50, >50, 2.9, and 13μM, respectively); induces caspase-dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias (GI50s=2.4 - 4μM)
13212 Pimelic Diphenylamide 106 A slow, tight-binding inhibitor of class I HDACs, progressively binding HDACs and remaining bound after wash-out; inhibits class I HDACs (IC50=150, 760, 370, and 5,000 nM for HDAC1, 2, 3, and 8, respectively) but not class II HDACs (IC50 > 180μM for HDAC4, 5, and 7)
13870 Pyroxamide An inhibitor of HDAC, including HDAC1 (IC50=0.1-0.2μM); induces growth suppression and cell death of certain types of cancer cells in culture
17553 Resminostat (hydrochloride) An orally bioavailable inhibitor of HDAC1, HDAC3, and HDAC6 (IC50=43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells; abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC50=2.5-3μM); dose-dependently inhibits HDAC activity in vivo
17130 Romidepsin A natural bicyclic depsipeptide that, following reduction, selectively inhibits class I HDACs (IC50=53, 39, 53, and 26 nM, for HDACs 1, 2, 3, and 8, respectively); has anti-cancer activities, particularly against certain T cell lymphomas
10009929 SAHA An HDAC inhibitor of class I and class II HDACs at around 50 nM; arrests cell growth in a wide variety of transformed cells in culture at 2.5-5.0μM
10675 SAHA-BPyne A SAHA derivative with a benzophenone crosslinker and an alkyne tag to be used for profiling HDAC activities in proteomes and live cells; labels HDAC complex proteins both in proteomes at 100 nM and in live cells at 500 nM; IC50=~3μM for inhibition of HDAC activity in HeLa cell nuclear lysates in an HDAC activity assay
10443 SB939 A pan-HDAC inhibitor (IC50=77 nM in an in vitro HDAC1 activity assay) that prevents proliferation of ovarian (A2780), colon (COLO 205 and HCT116), and prostate cancer (PC-3) cell lines at IC50 values of 0.48, 0.56, 0.48, and 0.34μM, respectively; binds all HDAC isozymes with similar affinity (Kis=16-28 nM) with the exception of HDAC6 and 7 (Kis=247 and 104 nM, respectively)
10572 Scriptaid An HDAC inhibitor that has an optimal effective concentration of 6-8μM in a cell-based assay, is less toxic than trichostatin A, and works in a wide variety of biological systems; induces cell cycle arrest in cancer cells in vitro and in vivo; facilitates the cloning of inbred mouse strains produced by somatic cell nuclear transfer
11323 Sodium 4-Phenylbutyrate A chemical chaperone that rescues the trafficking of misfolded proteins and weakly blocks HDAC activity (IC50=0.4 mM), leading to cell cycle arrest, differentiation, and/or apoptosis of various tumors
13121 Sodium Butyrate A short chain fatty acid that inhibits HDACs, induces growth arrest, differentiation and apoptosis in cancer cells, and suppresses inflammation by reducing the expression of pro-inflammatory cytokines
13168 Splitomicin A small molecule inhibitor of Sir2p HDAC activity, displaying higher activity in vivo (minimal inhibitory concentration=0.49μM) than in vitro (IC50=60μM); has diverse effects on mammalian cells
10574 Suberohydroxamic Acid A competitive HDAC inhibitor that inhibits HDAC1 (IC50=0.25μM) and HDAC3 (IC50=0.30μM); causes cell differentiation, cell cycle arrest, or apoptosis
10496 Sulforaphane An isothiocyanate that potently induces chemopreventative enzymes via Keap1-Nrf2 signaling and ARE-driven gene expression; at 15μM, inhibits class I and II HDAC activity and suppresses tumor growth selectively in cancerous prostate epithelial cells without affecting normal cells
17692 Tasquinimod An orally-active quinoline-3-carboxamide that inhibits tumor angiogenesis and supplements radiation or chemotherapy in animal models of prostate cancer
17738 TMP269 A cell-permeable inhibitor of class IIa HDACs (IC50=126, 80, 36, and 19 nM for HDAC4, 5, 7, and 9, respectively)
89730 Trichostatin A A potent, reversible inhibitor of HDAC (IC50=70 mM)
20220 Trichostatin C A glycosylated derivative of trichostatin A that has been shown to induce the differentiation of a mouse erythroleukemia cell line and to increase histone H4 acetylation in B cells, though at higher concentrations than trichostatin A
13691 Tubacin A selective HDAC6 inhibitor (IC50=4 nM) used as a biochemical tool to control microtubule-dependent intracellular trafficking, to manipulate the aggresome formation of misfolded proteins in certain diseases, and to study the dynamics of cellular adhesion
15785 Tubastatin A Potent HDAC6 inhibitor (IC50=15 nM) with 1,000-fold selectivity against all other HDAC isoforms (IC50 > 16μM), excluding HDAC8 (IC50=0.9μM); displays dose-dependent neuronal protection of primary cortical neuron cultures at 5-10μM
10559 Tubastatin A (trifluoroacetate salt) Potent HDAC6 inhibitor (IC50=15 nM) with 1,000-fold selectivity against all other HDAC isoforms (IC50 >16μM), excluding HDAC8 (IC50=0.9μM); induces α-tubulin hyperacetylation at 2.5μM in primary cortical neuron cultures; displays dose-dependent neuronal protection of primary cortical neuron cultures at 5-10μM
13033 Valproic Acid (sodium salt) An analog of valeric acid, long used as an anticonvulsant; inhibits Class I HDACs with an IC50 of ~2 mM; also inhibits GSK3 and depletes cellular IP3
14314 Plumbagin A natural 1,4-naphthoquinone that has diverse effects in cells and animals; causes the generation of ROS and induces apoptosis in cancer cells; activates signaling through Nrf2 and ARE, inducing the expression of Nrf2 target genes, including NQO1 and HO-1 in cultured neuronal cells
11138 2,4-Pyridinedicarboxylic Acid Structurally mimics 2-OG and chelates zinc; blocks the activity of 2-OG oxygenases (certain lysine demethylases and hydroxylases); inhibits several Jumonji domain-containing lysine demethylases at low micromolar concentrations and prolyl hydroxlase 1 (IC50=1.5μM)
12033 Daminozide A selective inhibitor of the human 2-oxoglutarate (JmjC) histone demethylases KDM2A, PHF8, and KDM7A (IC50=1.5, 0.55, and 2.1μM, respectively)
12054 GSK-J1 (sodium salt) A potent, cell impermeable inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50=18 and 56μM, respectively as measured by mass spectrometry; IC50=60 nM in JMJD3 antibody-based assays)
12056 GSK-J2 (sodium salt) A pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100μM), making it an appropriate negative control for in vitro studies involving GSK-J1
12073 GSK-J4 (hydrochloride) An ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production, including that of TNFα (IC50=9μM) in human primary macrophages
12074 GSK-J5 (hydrochloride) A pyridine regio-isomer of the JMJD3 inhibitor GSK-J4; cell-permeable and hydrolyzed to a free base, which is a weak inhibitor of JMJD3 (IC50 > 100μM), making it an ideal negative control molecule
11572 IOX1 A broad-spectrum inhibitor of 2OG oxygenases that inhibits JMJD2 demethylase activity (IC50=87μM); inhibits JMJD2A, JMJD2E and the 2OG oxygenases PHF8, PHD2, and FIH (IC50=1.7, 2.4, 13.3, 14.3, and 20.5μM, respectively)
15338 JIB-04 A pyridine hydrazone that broadly inhibits Jumonji histone demethylases (IC50 values are 230, 340, 435, 445, 855, and 1100 nM for JARID1A, JMJD2E, JMJD2B, JMJD2A, JMJD3 and JMJD2C, respectively); inhibits Jumonji demethylase activity, alters gene expression, and blocks viability of cancer cells both in vitro and in vivo
17472 ML-324 A cell-permeable inhibitor of JMJD2E (KDM4DL; IC50=920 nM); reduces the expression of immediate early genes of HSV (IC50=~10μM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice
13944 N-Oxalylglycine A cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E (IC50=250, 500, and 24μM, respectively); inhibits the prolyl hydroxylase domain-containing proteins PHD1 and PHD2 with IC50 values of 2.1 and 5.6μM, respectively
16272 PBIT A reversible, cell-permeable inhibitor of JARID1 family demethylases (IC50=6, 3, 4.9, and 28μM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively); increases trimethylation of H3K4 in HeLa cells and blocks the proliferation of tumor cells expressing high levels of JARID1B
10010494 2-PCPA (hydrochloride) An irreversible, mechanism-based inhibitor of lysine-specific demethylase 1 (LSD1) with an IC50 value of 20.7μM and a Ki value of 242.7μM that effectively inhibits histone demethylation in vivo; irreversibly inhibits monoamine oxidases (MAO) A and MAO B with IC50 values of 2.3 and 0.95μM and Ki values of 101.9 and 16μM, respectively
19403 GSK2879552 A selective, orally bioavailable, mechanism-based inactivator of LSD1/CoREST activity; enhances H3K4 methylation, increasing the expression of tumor-suppressor genes and preventing growth of AML cell lines (EC50s=2-240 nM)
16439 GSK-LSD1 (hydrochloride) An irreversible, mechanism-based inhibitor of LSD1 (IC50=16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC50s <5 nM)
17471 OG-L002 A potent inhibitor of LSD1 (IC50=0.02μM) that less effectively inhibits MAO-A and MAO-B (IC50=1.38 and 0.72μM); blocks the expression of IE genes of HSV and hCMV in mammalian cells; represses HSV primary infection in mice and blocks HSV reactivation from latency in a mouse ganglion explant model
19136 ORY-1001 An orally available, selective inhibitor of LSD1 (IC50 < 20 nM); targets AML stem cells
18124 RN-1 (hydrochloride) A potent, irreversible inhibitor of LSD1 (IC50=70 nM); penetrates the blood-brain barrier and blocks long-term but not short-term memory in mice
15487 SP2509 A reversible inhibitor of LSD1 (IC50=13 nM); allows increased methylation of H3K4, driving increased expression of p21, p27 and CCAAT/enhancer binding protein α in cultured AML cells; improves survival alone and synergizes with panobinostat in improving survival of mice engrafted with AML cells
13145 AGK2 A cell-permeable, selective inhibitor of SIRT2 (IC50=3.5μM) that minimally affects either SIRT1 or SIRT3; rescues dopamine neurons from α-synuclein toxicity in both in vitro and in vivo Parkinson’s disease models
14004 AK-7 A cell- and brain-permeable inhibitor of SIRT2 (IC50=15.5μM); dimishes neuronal cell death induced by mutant huntingtin fragment in culture; down-regulates cholesterol biosynthetic gene expression and reduces total cholesterol levels in neurons in vivo
10009797 CAY10591 An activator of SIRT1 that decreases TNF-α levels from 325 pg/ml (control) to 104 and 53 pg/ml at 20 and 60μM, respectively; exhibits a significant dose-dependent effect on fat mobilization in differentiated adipocytes
10009796 CAY10602 Derived from HTS for compounds that increase the SIRT1-mediated deacetylation of a SIRT1-specific substrate; dose-dependently suppresses the NF-κB-dependent induction of TNF-α by LPS in THP-1 cells, with approximately 75% inhibition achieved at 60μM, without cytotoxicity
10009798 EX-527 A cell-permeable, selective inhibitor of SIRT1 (IC50=98 nM); inhibits other SIRTs only at much higher concentrations and has no effect on other HDACs
19771 Inauhzin A cell-permeable, selective SIRT1 inhibitor (IC50=0.7-2μM) that reactivates p53 by inhibiting SIRT1 deacetylation activity; inhibits cell proliferation by inducing p53-dependent apoptosis in various human cancer cells (IC50=5.4, 51.9, 3.2, 33.9, and 85.4μM for H460, H1299, A549, HT-29, and WI38 cells, respectively), as well as in xenograft tumors
14648 JFD00244 An inhibitor of SIRT2 (IC50=56.7μM); induces granulocytic differentiation in the acute promyelocytic leukemia cell line NB4
10641 JGB1741 A SIRT1-specific inhibitor (IC50=15μM); inhibits metastatic breast cancer MDA-MB 231 cell proliferation (IC50=512 nM), dose-dependently increasing p53 acetylation and p53-mediated apoptosis in these cells
13178 Salermide An inhibitor of SIRT1 and SIRT2, causing tumor-specific apopoptic cell death; causes 90% apoptosis within 72 hours (IC50 ~ 20μM) by reactivating proapototic genes that are repressed by SIRT1 in MOLT4 leukemia cells
18116 SirReal2 An aminothiazole that acts as a SIRT-rearranging ligand to selectively inhibit SIRT2 (IC50=140 nM) without effect on SIRT1 or SIRT3-6; increases α-tubulin acetylation in HeLa cells
14407 SIRT1/2 Inhibitor IV A cell-permeable inhibitor of SIRT1 (IC50=56μM) and SIRT2 (IC50=59μM); less effectively inhibits SIRT5 (IC50 >300μM) and has no effect on class I and II HDACs; sensitizes H460 lung cancer cells to etoposide and paclitaxel; blocks a SIRT1-dependent hypoxic response in vivo
10523 Sirtinol A cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38μM, respectively; does not alter HDAC1 activity
13085 Tenovin-1 A small molecule activator of p53 that decreases the growth of BL2 Burkitt’s lymphoma and ARN8 melanoma cells; inhibits the deacetylase activity of purified human SIRT1 and SIRT2
13086 Tenovin-6 A analog of tenovin-1; elevates p53 activity in MCF-7 cells at 10μM and reduces growth of ARN8 melanoma xenograft tumors in SCID mice at a dose of 50 mg/kg
20534 (+)-Biotin 4-Amidobenzoic Acid (sodium salt) A substrate of biotinidase, releasing PABA, which can be quantified by either fluorescent or colorimetric methods
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.
11931 GSK4112 A synthetic agonist for REV-ERBα (EC50=0.4μM) that mimics the action of heme; at 10μM inhibits the expression of the circadian target gene bmal1 and reduces glucose output by 30% in mouse primary hepatocytes by repressing the expression of several gluconeogenic genes
11573 IOX2 Potent, cell permeable inhibitor of PHD2 (IC50=21 nM) with over 100-fold selectivity compared to inhibition of JMJD2A, JMJD2C, JMJD2E, JMJD3, or the 2OG oxygenase FIH (IC50 > 100μM); inhibits HIF-1α hydroxylation in RCC4 cells at 50μM
18181 IOX4 A selective, potent inhibitor of PHD2 (IC50=1.6 nM); active in vivo, inhibiting prolyl hydroxylation and increasing HIF1α levels in cells (IC50 values range from 5.6 to 11.7μM) and inducing HIF1α and HIF2α expression in mice; penetrates the blood-brain barrier to induce HIF expression in the brain
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
16288 Tenovin-3
16374 α-Hydroxyglutaric Acid (sodium salt) An α-hydroxy acid, overproduced in 2-hydroxyglutaric aciduria; mutations in IDH1 and IDH2 cause these enzymes to convert isocitrate to 2-hydroxyglutarate; competitively inhibits α-ketoglutarate-dependent dioxygenases, including lysine demethylases and DNA hydroxylases

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