MS023 (type I PRMTs inhibitor抑制劑) | CAS# 1831110-54-3APExBIO貨號 B6183
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PRMTs 抑制劑系列商品->>MS023
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MS023 (type I PRMTs inhibitor抑制劑) | CAS# 1831110-54-3APExBIO貨號 B6183
表觀遺傳學(Epigenetics)是基因表達的可遺傳修飾(heritable modifications)，與 DNA 序列(DNA sequence)的變化無關。表觀遺傳修飾(Epigenetic modifications)主要發生在 DNA 或組蛋白八聚體(histone octamer)上。有幾種類型的表觀遺傳學修飾(epigenetics modifications)，DNA-甲基轉移酶 (DNMT) 的 DNA 甲基化和組蛋白的共價修飾，例如乙醯化(acetylation)、甲基化(methylation)、磷酸化(phosphorylation)和泛素化(ubiquitination)。組蛋白乙醯轉移酶 (HAT) 的組蛋白乙醯化參與轉錄激活，而組蛋白去乙醯化酶 (HDAC) 的組蛋白去乙醯化與轉錄抑制(transcriptional repression)有關。組蛋白去甲基化(Histone demethylation)與賴氨酸特異性去甲基化酶 (lysine-specific demethylase , LSD) 和含有組蛋白去甲基化酶 (JHDM) 的 JmjC 結構域(JmjC domain)有關。
核小體(nucleosome)由四種組蛋白（H2A、H2B、H3 和 H4）組成，它們是染色質(chromatin)的主要組成部分。特定化學基團的添加和去除稱為表觀遺傳標記(epigenetic marks)，它調節染色質結構並影響基因表達。此外，RNA 與抑制性染色質狀態(repressive chromatin state)的形成密切相關。
表觀遺傳(Epigenetic)機制在細胞水平上響應環境變化，從而影響細胞可塑性(plasticity)。染色質(Chromatin)和表觀遺傳調控(epigenetic regulation)在發育和應激反應期間的基因組編程中發揮重要作用，表觀遺傳學缺陷(defects in epigenetics)可導致癌症(cancer)、炎症(inflammation)和代謝紊亂(metabolic disorders)等。MG 149 是一種組蛋白乙醯轉移酶 (HAT) 抑制劑，對 Tip60 和 MOF 的 IC50 值分別為 74μM 和 47μM [1]。
MS023 is a type I PRMTs inhibitor.Protein arginine methyltransferases (PRMTs) play a critical role in various biological processes. PRMT overexpression has been observed in a variety of human diseases including cancer. PRMTs has been divided into three categories: type I PRMTs for catalyzing mono- and asymmetric dimethylation of arginine residues, type II PRMTs for catalyzing mono- and symmetric dimethylation of arginine residues, and type III PRMT for catalyzing only monomethylation of arginine residues.
MS023 是一種 I 型 PRMTs 抑制劑。蛋白質精氨酸甲基轉移酶 (inhibitor.Protein arginine methyltransferases ,PRMT) 在各種生物過程中發揮著關鍵作用。已在包括癌症(cancer)在內的多種人類疾病中觀察到 PRMT 過度表達(overexpression)。 PRMTs分為三類：I型PRMTs用於催化精氨酸殘基(arginine residues)的單甲基化和不對稱二甲基化，II型PRMTs用於催化精氨酸殘基(arginine residues)的單甲基化和對稱二甲基化(symmetric demethylation)，III型PRMTs僅催化精氨酸殘基的單甲基化(monomethylation)。體外(In vitro)：先前的研究表明，MS023 對 I 型 PRMT 具有出色的效力，但對 II 型和 III 型 PRMT、蛋白質賴氨酸甲基轉移酶(protein lysine methyltransferases)以及 DNA 甲基轉移酶(DNA methyltransferases)均完全無活性。此外，PRMT6 與 MS023 的晶體結構表明 MS023 與底物結合位點結合。此外，MS023 可以有效降低組蛋白精氨酸不對稱二甲基化的細胞水平。此外，MS023 可以降低精氨酸不對稱二甲基化的水平，同時還可以增加精氨酸單甲基化和對稱二甲基化的細胞水平 [1]。體內：到目前為止，還沒有動物體內數據報導。臨床試驗：截至目前，MS023仍處於臨床前開發階段。
- 1. Pyun JH, Kim HJ, et al. “Cardiac specific PRMT1 ablation causes heart failure through CaMKII dysregulation.” Nat Commun. 2018 Nov 30;9(1):5107. PMID:30504773
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 287.4 |
| Cas No. | 1831110-54-3 |
| Formula | C17H25N3O |
| Solubility | ≥28.7 mg/mL in DMSO; ≥13.7 mg/mL in EtOH; ≥23.3 mg/mL in H2O |
| Chemical Name | N1-((4-(4-isopropoxyphenyl)-1H-pyrrol-3-yl)methyl)-N1-methylethane-1,2-diamine |
| SDF | Download SDF |
| Canonical SMILES | NCCN(C)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2 |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
| 品項 | CAS# | #貨號 | 應用 |
| MG 149 (Tip60 HAT inhibitor) 選擇性抑制劑 | CAS# 1243583-85-8 | 貨號 B3276 | HAT inhibitor |
| 4′-bromo-Resveratrol | CAS# 1224713-90-9 | 貨號 C3552 | Sirt1 和 Sirt3 抑制劑 |
| MS023 | CAS# 1831110-54-3 | 貨號 B6183 | type I PRMTs inhibitor抑制劑 |
| CHZ868 | N/O | 貨號B5980 | Type II JAK2 inhibitor |
| Chidamide | CAS#743420-02-2 | 貨號B5916 | Novel HDAC inhibitor |
| RGFP966 | CAS#1357389-11-7/1396841-57-8 | 貨號A8803 | Specific HDAC3 inhibitor |
| EPZ-6438 | CAS#1403254-99-8 | 貨號A8221 | EZH2 inhibitor, potent and selective |
| Bromodomain Inhibitor, (+)-JQ1 | CAS# 1268524-70-4 | 貨號A1910 | BET bromodomain inhibitor |
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| A8743 | SYBR Safe DNA Gel Stain |
| A6001 | 3X (DYKDDDDK) Peptide |
| K1018 | Cell Counting Kit-8 (CCK-8) |
| A1902 | Z-VAD-FMK |
| A3008 | Y-27632 dihydrochloride |
| A6002 | DYKDDDDK tag Peptide |
| B8362 | 2’3′-cGAMP (sodium salt) |
| F4002 | Phos binding reagent (Phosbind) acrylamide |
| A8011 | Biotin-tyramide |
| A2585 | MG-132 |
| F4005 | Prestained Protein Marker (Triple color, EDTA free, 10-250 kDa) |
| B1274 | AP20187 |
| K1007 | Protease Inhibitor Cocktail(EDTA-Free,100X in DMSO) |
| B8226 | InstaBlue Protein Stain Solution |
| A3011 | CHIR-99021 (CT99021) |
| A3007 | ABT-263 (Navitoclax) |
| B1524 | Erastin |
| B6055 | TCEP hydrochloride |
| K1031 | Phusion high-fidelity DNA polymerase |
| B1387 | (-)-Blebbistatin |
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| A1901 | Q-VD-OPh hydrate |
| A8950 | UM 171 |
| K1046 | RNase Inhibitor, Murine |
| A3317 | Clozapine N-oxide (CNO) |
| A2614 | Bortezomib (PS-341) |
| A8003 | Sulfo-NHS-LC-Biotin |
| A4154 | Olaparib (AZD2281, Ku-0059436) |
| A8012 | Biotin-XX Tyramide Reagent |
| K1101 | PreScission Protease (PSP) |
| A8627 | Bafilomycin A1 |
| A8001 | Sulfo-NHS-Biotin |
| A3017 | Dasatinib (BMS-354825) |
| A2576 | E-64 |
| K1051 | Cy3 TSA Fluorescence System Kit |
| K1034 | 2X Taq PCR Master Mix (with dye) |
| B7972 | Pseudo-UTP |
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| A4219 | Birinapant (TL32711) |
| A4371 | Ferrostatin-1 (Fer-1) |
| A8200 | DAPT (GSI-IX) |
| A8249 | SB 431542 |
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| A4393 | Paclitaxel (Taxol) |
| A8315 | NU7441 (KU-57788) |
| A4213 | Necrostatin-1 |
| A8885 | Ro 3306 |
| L1021 | DiscoveryProbe™ FDA-approved Drug Library |
| B1464 | KPT-330 |
| A8815 | SM-164 |
| B4879 | Blasticidin S HCl |
| A8793 | N3-kethoxal |
| K1047 | HyperScribe™ T7 High Yield RNA Synthesis Kit |
| A6004 | Influenza Hemagglutinin (HA) Peptide |
| B1036 | MLN4924 |
| A8178 | Panobinostat (LBH589) |
| A3963 | A-769662 |
| A3847 | SU5416 |
| B3252 | Dorsomorphin (Compound C) |
| B4758 | BAPTA-AM |
| A2513 | Geneticin, G-418 Sulfate |
| B6004 | PX-478 2HCl |
| A8955 | Z-YVAD-FMK |
| A8193 | ABT-737 |
| B2083 | Caspofungin Acetate |
| A8002 | NHS-Biotin |
| A8337 | CX-5461 |
| A8312 | Torin 1 |
| A2570 | Leupeptin, Microbial |
| K2170 | Alanine Aminotransferase (ALT or SGPT) Activity Colorimetric/Fluorometric Assay Kit |
| A4381 | FK866 (APO866) |
| B2143 | Tacrolimus (FK506) |
| A2571 | Pepstatin A |
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