GSK3326595
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- 应用范围
- Inhibition (Inh)
- 原理
- Selective PRMT5 inhibitor
- 产品特性
- GSK3326595 is a potent (IC50 = 6.2nM), selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5. PRMT5 inhibition activated the p53 pathway via induction of alternative splicing of MDM4 leading to a potent anti-proliferative response both in vitro and in vivo. Combination therapy with palbociclib (CDK4/6 inhibitor) and GSK3326595 lead to increased efficacy of palbociclib in treating native and resistant models of melanoma via regulation of the PRMT5-MDM4 axis. Currently in clinical Trials.
- 纯度
- >98 %
- Chemical Name
- 6-[(1-Acetylpiperidine-4-yl)amino]-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyrimidine-4-carboxamide
- Formula
- C24H32N6O3
- Solubility
- Soluble in DMSO (up to 20 mg/ml)
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Geldanamycin
Inh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
RadicicolInh 12772-57-5
Geldanamycin- FITCInh 30562-34-6 (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1] docosa-1(21),4,6,10,18-pentaen-9-yl carbamate
ResveratrolAct 501-36-0 3,4',5-Trihydroxy-trans-stilbene
PanobinostatInh 404950-80-7 (E)-N-Hydroxy-3-(4-((2-(2-methyl-1H-indol-3-yl)ethylamino)methyl)phenyl)acrylamide
HPA (Hexyl-4-pentynoic acid)Inh Cell-permeable 96017-59-3 2-(2-Propynyl)octanoic acid (racemic)
EX-527Inh Cell-permeable 49843-98-3 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-xarboxamide (racemic)
DaminozideInh 1596-84-5 1-(2,2-Dimethylhydrazide)butanedioic acid
Mithramycin AInh 18378-89-7
PiceatannolInh 10083-24-6 3,3',4,5'-Tetrahydroxy-trans-stilbene
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- 限制
- 仅限研究用
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- 状态
- Powder
- 储存条件
- -20 °C
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- 背景
- EPZ015938,Proliferation,Epigenetics,Posttranslational modification,Protein methyltransferase,RNA,Cancer,Chromatin,p53
- 分子量
- 452.56
- CAS-编号
- 1616392-22-3
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